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‫ﻟﻠﻤﺰﻳﺪ ﻋﻦ ﻛﻞ ﻣﺎ ﻳﺨﺺ اﻟﺼﻴﺪﻟﺔ و اﻟﺘﺪرﻳﺐ اﺿﻐﻂ ﻫﻨﺎ‬

‫‪https://t.me/Pharmacists_worlds‬‬
https://t.me/Pharmacists_worlds

Summer Training Guide


For
Third Stage
Pharmacy Students

‫ﻋﺎﻟﻢ ﺍﻟﺼﻴﺎﺩﻟﺔ‬
https://t.me/Pharmacists_worlds
‫ص َذلَ ٍح‬
‫ز ‪َ ِِْٓ :‬‬ ‫اخ ا ْت ُٓ آ َد ََ ا ْٔمَطَ َع َع ٍَُُّٗ إِال ِِْٓ شَال ٍ‬ ‫(إِ َرا َِ َ‬
‫ح ٌَ ْذ ُع‪)ٌَُٗ ٛ‬‬ ‫َجا ِسٌَ ٍح ‪ ،‬أَ ْ‪ِ ٚ‬ع ٍْ ٍُ ٌُ ْٕرَفَ ُع تِ ِٗ ‪ ،‬أَ ْ‪ٍ ٌََٚ ٚ‬ذ َ‬
‫صاٌ ِ ٍ‬

‫حذٌس ٔث‪ٛ‬ي ششٌف‬

‫"ال يؤلف أحد كتابا إال في أحد أقسام سبعة‪ ،‬و ال‬
‫يمكن التأليف في غيرها‪ ،‬وهي‪ :‬إ ّما أن يؤلف من‬
‫شيء لم يسبق إليه فيخترعه‪ .‬أو شيء ناقص يتممه‪.‬‬
‫أو شيء مستغلق يشرحه‪ .‬أو طويل يختصره‪ ،‬دون‬
‫أن يخل بشيء من معانيه‪ .‬أو شيء مختلط يرتبه‪ .‬أو‬
‫شيء أخطأ فيه مصنف يبينه‪ .‬أو شيء مفرق‬
‫يجمعه"‪.‬‬
‫شّظ اٌذٌٓ اٌثاتًٍ سحّٗ هللا‬
‫إ٘ذاء‪.....‬‬
‫إٌى ‪....‬‬
‫ص‪ٚ‬جرً ‪ٚ‬أ‪ٚ‬الدي (ٌاعش ‪ٚ‬حّضج)‪....‬‬
‫عٍى ِا أخزخ ِٓ ‪ٚ‬لد ٘‪ ِٓ ٛ‬حم‪.... ُٙ‬‬
‫أ٘ذي عّـــــــــــــــــــًٍ ٘ـــــــــــــــــــزا ‪....‬‬

‫ضٍاء‬
‫‪0200‬‬
‫ذّ‪ٍٙ‬ـذ‬
‫ٍُ‬
‫ّٓ اٌ َّش ِح ِ‬ ‫غ ُِ هللاِ اٌ َّش ْح ِ‬ ‫ت ْ‬
‫ع ٰى َ٘ ًْ أَذَّثِ ُعهَ َعٍَ ٰى أَْْ ذُ َعٍِّ َّ ِٓ ِِ َّّا ُعٍِّ ّْدَ ُس ْ‬
‫ش ًذا)‬ ‫(لَا َي ٌَُٗ ُِ‪َ ٛ‬‬
‫ع‪ٛ‬سج اٌى‪ٙ‬ف اٌَح ﴿‪﴾٦٦‬‬
‫ٌّصً اٌرذسٌة اٌصٍفً ٌطالب اٌّشحٍح اٌصاٌصح فً وٍٍاخ اٌصٍذٌح اٌمغُ األ‪ٚ‬ي ِٓ‬
‫ِرطٍثاخ اٌرذسٌة اٌصٍفً ‪ٚ‬ذأذً اٍّ٘رٗ ِٓ و‪ ٗٔٛ‬اٌّحطح اال‪ٌٚ‬ى اٌرً ٌى‪ ْٛ‬فٍ‪ٙ‬ا‬
‫اٌطاٌة ترّاط ِثاشش ِع اٌّشضى ِٓ جأة ‪ٚ‬ترّاط ِثاشش اٌضا ِع عاٌُ االد‪ٌٚ‬ح‬
‫‪ٚ‬فما ألشىاٌ‪ٙ‬ا اٌصٍذالٍٔح اٌّخرٍفح ‪ٚ‬اعرعّاالذ‪ٙ‬ا اٌّرعذدج‪٘ٚ ..‬زا ٌرٍح ٌ‪ ُٙ‬اٌرعشف‬
‫عٍى عٍش اٌعًّ فً اٌصٍذٌٍح ‪ٚ‬اٌرعشف عٍى ع‪ٛ‬ق اٌعًّ ‪ِٚ‬عاٌشح ظش‪ٚ‬ف اٌعًّ‬
‫اٌحمٍمٍح اٌرً عٍ‪ٛ‬اج‪ٙٔٛٙ‬ا فً اٌّغرمثً فضال عٓ ذعٍّ‪ ُٙ‬أعاٌٍة اٌرعاًِ ِع‬
‫اٌّشضى‪..‬‬
‫طٍثرٕا األعضاء (صِالء اٌغذ) ٌرضّٓ ٘زا اٌذًٌٍ اعرعشاضا ٌٍمغُ األعظُ ِٓ األد‪ٌٚ‬ح‬
‫اٌرً ٔر‪ٛ‬لع ِٓ اٌطاٌة أْ ٌشا٘ذ٘ا ‪ٌٚ‬رعاًِ ِع‪ٙ‬ا أشٕاء ذذستٗ فً اٌصٍذٌٍح ‪ٚ‬لذ‬
‫اذثعٕا فً وراترٗ إٌّ‪ٙ‬ج ٌراًٌ‪:‬‬
‫‪ -1‬ذُ ذمغٍُ اٌذًٌٍ إٌى فص‪ٛ‬ي ‪ٚ‬وً فصً ٌخرص تّجّ‪ٛ‬عح ِٓ األد‪ٌٚ‬ح ذشرشن فً‬
‫االعرعّاي اٌعاَ ف‪ٕٙ‬ان األد‪ٌٚ‬ح اٌخاصح تاٌج‪ٙ‬اص اٌ‪ٙ‬ضًّ ‪ٕ٘ٚ‬ان األد‪ٌٚ‬ح اٌخاصح‬
‫تاٌج‪ٙ‬اص اٌمٍثً اٌ‪ٛ‬عائً ‪٘ٚ‬ىزا ‪ٚ‬ضّٓ وً ِجّ‪ٛ‬عح ٕ٘اٌه ِجّ‪ٛ‬عح اصغش ِٓ‬
‫األد‪ٌٚ‬ح حغة االعرعّاي األوصش ذخصصا ٌ‪ٙ‬ا‪.‬‬
‫‪ -0‬ذُ اٌرّ‪ٍٙ‬ذ ٌىً ِجّ‪ٛ‬عح ذخصصٍح ِٓ األد‪ٌٚ‬ح تاعرعشاض ِ‪ٛ‬جض عٍى شىً‬
‫ٔماط ألتشص ‪ٚ‬اُ٘ اٌج‪ٛ‬أة اٌعٍٍّح اٌّرعٍمح ت‪ٙ‬ا ‪ٚ‬رٌه عٍى عثًٍ االخرصاس‪.‬‬
‫‪ -3‬ذُ إٌحاق جذ‪ٚ‬ي ِع وً ِجّ‪ٛ‬عح أد‪ٌٚ‬ح ذخصصٍح ‪ٌ..‬رضّٓ ٘زا اٌجذ‪ٚ‬ي شالشح‬
‫حم‪ٛ‬ي أعاعٍح ً٘ االعُ اٌعًٍّ ‪ٚ‬االعُ اٌرجاسي ‪ٚ‬اٌشىً اٌصٍذالًٔ ٌألد‪ٌٚ‬ح ‪ٚ‬لذ‬
‫ذشن ٌٍطاٌة ِ‪ّٙ‬ح إوّاي ٘زٖ اٌجذا‪ٚ‬ي خالي ذذستٗ فً اٌصٍذٌح ‪ٚ‬وً حغة األد‪ٌٚ‬ح‬
‫اٌّر‪ٛ‬فشج فً اٌصٍذٌٍح اٌرً ٌرذسب ت‪ٙ‬ا‪.‬‬
‫‪ -4‬وّا ‪ٚ‬ذُ إٌحاق جذ‪ٚ‬ي فاسغ صغٍش ِع وً ِجّ‪ٛ‬عح ذخصصٍح ِٓ األد‪ٌٚ‬ح ‪ٚ‬لذ‬
‫ذشن ٘زا اٌجذ‪ٚ‬ي فاسغا ٌٍرغٕى ٌٍطاٌة وراتح أٌح ِالحظح إضافٍح ٌشا٘ا ِ‪ّٙ‬ح ‪ٌٚ‬ىٓ‬
‫ٌُ ذرُ اإلشاسج إٌٍ‪ٙ‬ا فً ٘زا اٌذًٌٍ‪.‬‬
‫‪ٚ‬أخٍشا التذ ِٓ اإلشاسج إٌى إْ ٘زا اٌذًٌٍ لذ اعذ ٌٍى‪ِ ْٛ‬غاعذا ٌطٍثرٕا األعضاء‬
‫خالي فرشج اٌرذسٌة اٌصٍفً ‪ٌٍ ٛ٘ٚ‬ظ تذٌال عٓ اٌرذسٌة فً إي حاي ِٓ األح‪ٛ‬اي‬
‫أغجاِا ِع اٌحىّح اٌرعٍٍٍّح اٌمائٍح‪:‬‬
‫(لً ًٌ‪ٚ..‬ع‪ٛ‬ف أٔغى‪..‬أسًٔ ‪ٚ ..‬ع‪ٛ‬ف أذزوش ‪ ..‬أششوًٕ ‪ٚ ..‬ع‪ٛ‬ف أذعٍُ)‬
‫‪ ِٓٚ‬اٌٍــــــــــــــــــٗ اٌر‪ٛ‬فٍـــــــــــــــك‬
‫ضٍــــــــــــــــــــــــــــــــاء‬
‫‪0200‬‬
Contents
Chapter Title Page
1 Dosage form-specific counseling points 1

0 Cardiovascular System 11

3 Gastro-intestinal System 07

4 Respiratory System 43

5 Central nervous system 55

6 Infections 72

7 Endocrine system 88

8 Genito-urinary system 126

9 Nutrition and blood 100

12 Musculoskeletal and joint diseases 134

11 Eye 145

10 Ear, nose, and oropharynx 154

13 Skin 163
Chapter One: Dosage form-specific counseling points

1.1-Administration of ear drops and sprays (1, 2)

1. Wash hands with soapy water.

2. Clean and dry the ear gently with a facecloth.

3. If necessary, shake the bottle of drops or spray. Some drops and sprays are
suspensions
and will need shaking; if applicable,
this direction will be on the label.

4. Warm the ear drops or spray by


holding the bottle in the hand for a
few minutes.

5. Remove the lid.

6. Lie down on side with the


affected ear uppermost (or tilt the
head to one side).

7. Gently pull the ear lobe backward


and upward to open the ear canal
(see drawing A). If the patient is a
child younger than 3 years old, pull
the ear backward and downward
(see drawing B).

8. Drop the drops or spray into the


ear canal.

9. Gently massage just in front of


the ear.

10. Stay lying down or with the


head tilted for five minutes to allow
the medication to run down the ear
canal.

11. Return to the upright position and wipe away any excess medication.

12. Repeat if necessary in the other ear.

13. Replace the lid.


1
1.2-Administration of nasal preparations (1).

How to use nasal drop How to use nasal sprays


1. Gently blow the nose to clear the nostrils. 1. Gently blow nose to clear nostrils.
2. Wash hands. 2. Wash hands with soapy water before using the
3. Shake the bottle of drops. Some are spray.
suspensions and will need shaking; if 3. Gently shake the spray. Some are suspensions
applicable, this direction will be on the and will need shaking; if applicable, this
label. direction will be on the label.
4. Remove the lid from the bottle. If the lid 4. Remove the cap from the spray.
includes an integral dropper draw some 5. Tilt head slightly forward (look down at feet).
liquid into the dropper. 6. Close one nostril; gently press against the side
5. Position the head as shown in figure of the nose with one finger.
below. The easiest way to do this is to lie on 7. Insert tip of nasal spray into open nostril and
a bed with your head hanging over the edge. slowly breathe in through the open nostril, and
Bending forward or kneeling is an while breathing in squeeze the spray to deliver
alternative but maintaining the position for 2 one dose. It is important to keep the spray
minutes after using the drops is more upright (do not sniff hard as the spray will travel
difficult. Tilting the head back is not a straight to the back of the throat, failing to
suitable position as the drops will not cover deposit any medication in the nostril).
the upper surface of the nostril. 8. Remove spray from the nose and breathe out
6. Drop the required number of drops into through the mouth. Tilt head backwards for
each nostril. The intention is to spread the about a minute to prevent the liquid spray
drop(s) evenly over the surface of the running out of the nose.
nostril. Do not allow the dropper to touch 9. Repeat in other nostril as directed.
the nose. 10. Replace cap on spray.
7. Stay in this position for 2 minutes to 11. Try not to blow nose for several minutes
prevent the drops running out of the nose after using the spray.
and down the back of the throat.
8. Replace the lid.

2
1.3-Administration of drugs to the eye (1):
How to use eye drops How to use eye ointment
1. Wash hands with soapy water. 1. Wash hands with soapy water.
2. If necessary, clean the eyes with boiled and 2. Clean your eye if necessary (as with eye
cooled water and a tissue (one tissue for each drops)
eye) to remove any discharge or remaining 3. Sit in front of a mirror.
wateriness (do not use cotton wool as it may 4. Remove the cap from the eye ointment
leave fibers behind that may irritate the eye). tube. Applying the ointment (see figure):
3. Shake the bottle of drops if necessary. Some 5. Gently pull down the lower eyelid,
eye drops are suspensions and will need forming a pocket between the lid and the eye.
shaking; if applicable, this direction will be on 6. Hold the tube above the eye without
the label. touching it.
4. Remove the cap from the bottle. 7. Gently squeeze the tube and place about 1
5. Either sit down or lie down and tilt the head cm of ointment into the pocket, starting from
backwards so that you are looking at the ceiling. nearest the nose to the outer edge.
6. Gently pull down the lower eyelid with a 8. Twist the wrist to break the strip of
finger to make a pocket between the eye and the ointment from the tube.
lower lid. 9. Close the eye and blink to help spread the
7. Look upwards. eye ointment over the eyeball. Body
8. Rest the dropper bottle on the forehead above temperature will help to melt the ointment so
the eye (see figure). that it will spread over the surface of the eye.
9. Squeeze one drop inside the lower eyelid (do 10. Vision will be blurred for a few
not allow the dropper tip to touch the eye). moments. Keep blinking and the vision will
10. Close the eye and gently blot away any clear.
excess drops on a clean tissue. 11. Wipe away excess ointment using a clean
11. Apply slight pressure to the inner corner of tissue.
the eye for about 30 seconds. This will prevent 12. Replace the cap of the tube.
the drops running down the tear duct and into 13. Remember to discard any remaining
the back of the throat, avoiding any unpleasant ointment four weeks after opening.
after taste and also minimizing any absorption
into the body, reducing the risk of possible side-
effects.
12. Replace the cap on the bottle.
13. Remember to discard any remaining drops
four weeks after opening.

3
1.4-Respiratory system drug delivery devices (1).

An example of a metered A metered dose inhaler A metered dose inhaler attached


dose inhaler. attached to a spacer to a spacer device with a mask
device.

An example of a Breath actuated inhaler An example of an Accuhaler.


Turbohaler

Figure 3-1: Examples of respiratory system drug delivery devices (1).

4
Device-specific patient counseling (1).

How to use a metered dose inhaler How to use a metered dose inhaler
with the aid of a spacer device
1. First assemble the spacer device if necessary as
directed by the manufacturer (with or without a
1. Remove the cap covering the mouthpiece and face mask).
check that there is no fluff or dirt in the 2. Remove the cap from the inhaler and insert the
mouthpiece. mouthpiece of the inhaler into the opening at the
2. Shake the inhaler. end of the spacer.
3. If the inhaler is new or has not been used for 3. Hold the spacer and inhaler together and shake.
some time it will need to be tested. To test: Hold 4. Breathe out.
the inhaler away from body. Press the top of the 5. Put the spacer mouthpiece in the mouth and seal
aerosol canister once. A fine mist should be with the lips.
puffed into the air. The inhaler is now ready to 6. Press the inhaler once and then breathe in and
use. out four or five times.
4. Tilt head back slightly. 7. Further doses may be taken waiting a few
5. Breathe out gently. seconds between puffs.
6. Place the mouthpiece in the mouth between the 8. Separate the spacer and inhaler. Replace the
teeth (do not bite). Close lips around the inhaler cap and store until next dose.
mouthpiece.
7. Start to breathe in slowly through the How to use an Accuhaler
mouth, at the same time press down on
1. With the Accuhaler mouthpiece facing you, slide
the inhaler to release the medicine in to the lungs.
the lever away until it clicks. This will have loaded
8. Hold breath for between 5 and 10 seconds, then
a dose ready for inhalation and the Accuhaler will
breathe out slowly.
move the dose counter on.
9. If a second dose is required, wait approximately
2. Hold the Accuhaler flat and breathe out
30 seconds and repeat the process.
away from the inhaler.
10. Replace the cap and if the inhaler is a
3. Seal lips around the Accuhaler mouthpiece and
corticosteroid inhaler, rinse the mouth out with
inhale deeply.
water.
4. Remove inhaler from the mouth and hold
breath as long as is comfortable.
5. Slide the thumb grip back towards you to
close the inhaler.
6. For further doses repeat above steps.

How to use a Turbohaler How to use a Breath actuated inhaler


1. Unscrew the cover and remove it. 1. Shake the inhaler.
2. Hold the Turbohaler upright with one hand and 2. Hold the inhaler upright and open the cap.
with the other twist the grip in one direction as far 3. Breathe out, away from the inhaler.
as it will go. 4. Put the mouthpiece in the mouth, seal lips
3. Now twist back as far as it will go – a click around the mouthpiece.
should be heard, showing the inhaler is primed 5. Breathe in steadily through the mouthpiece.
and ready for use. 6. Hold breath for about ten seconds.
4. Breathe out gently. 7. Keeping the inhaler upright, close the cap.
5. Place the mouthpiece between the lips and 8. For further doses repeat the above steps.
breathe in through the mouth as deeply and as
hard as possible.
6. Remove the inhaler from the mouth and breathe
out slowly.
7. Replace the cover.
8. Repeat the above steps if more than one puff is
required.

5
How to use a HandiHaler (3)
1-Immediately before use, open one sealed blister foil and HandiHaler device,
insert capsule, press HandiHaler button once to pierce capsule.
2-Exhale completely before placing mouthpiece into mouth with head upright.
3-Then breathe in slowly and deeply at a rate fast enough to hear capsule vibrate,
until lungs are full.
4-Holding breath as long as comfortable take HandiHaler device out of mouth.
5-Then place device back in mouth and inhale again to get full dose.

1.5-Applying vaginal products (pessaries or vaginal cream) (1):

1.Wash hands with soapy water before


using the pessaries/cream.
2.Remove any external foil or plastic
packaging from the pessary and
applicator.
3.If an applicator is provided, load the
applicator as directed by the
manufacturer.
4.Stand with one leg on a chair or lie
down with knees bent and legs apart.
5.Press the applicator plunger to insert
the pessary or cream into the vagina
(see the figure ). If no applicator is provided, insert the pessary as high into the
vagina as is comfortable by pushing gently but firmly in an upwards and
backwards direction using the middle finger. (If pregnant, do NOT use an
applicator to insert pessaries; insert using finger method.)
6.If an applicator is used, wash it ready for next use.
7.Wash hands once more.

6
1.6-Administration of rectal suppositories and enemas (2) :

Suppositories
1-Gently squeeze the suppository to determine if it is firm enough to insert. Chill a soft
suppository by placing it in the refrigerator for a few minutes or by running it under cool
running water.
2-Remove the suppository from its wrapping.
3-Dip the suppository for a few seconds in lukewarm water to soften the exterior.
4-Lie on your left side with knees bent or in the knee-to-chest position (see drawings A and
B). Position A is best for self-administration of a suppository. Small children can be held in
a crawling position.
5-Relax the buttock just before inserting the suppository to ease insertion. Gently insert the
tapered end of the suppository high into the rectum. If the suppository slips out, it was not
inserted past the anal sphincter (the muscle that keeps the rectum closed).
6-Continue to lie down for a few minutes, and hold the buttocks together to allow the
suppository to dissolve in the rectum. The parent/caregiver may have to gently hold a
child's buttocks closed.
7-Remember that the medication is most effective when the bowel is empty. Try to avoid a
bowel movement after insertion of the suppository for up to 1 hour so that the intended
action can occur.

Enemas
1-If someone else is administering the enema, lie on your left side with knees bent or in the
knee-to-chest position (see drawings A and B). Position A is preferred for children older
than 2 years. If self-administering the enema, lie on your back with your knees bent and
buttocks raised (see drawing C). A pillow may be placed under the buttocks.
2-If using a concentrated enema solution, dilute solution according to the product
instructions. Prepare 1 pint (500 mL) for adults and 1/2 pint (250 mL) for children.
3-Lubricate the enema tip with petroleum jelly or other non-medicated ointment/cream.
Apply the lubricant to the anal area as well.
4-Gently insert the enema tip 2 (recommended depth for children) to 3 inches into the
rectum.
5-Allow the solution to flow into the rectum slowly. If you experience discomfort, the flow
is probably too fast.
6-Retain the enema solution until definite lower abdominal cramping is felt. The
parent/caregiver may have to gently hold a child's buttocks closed to prevent the solution
from being expelled too soon.

7
1.7-Administration of drugs to the skin:
How to use patches (1):
1. Freshly wash and dry the area of skin where the patch is to be applied. Do not
use talc, oil, moisturizers or creams as this may prevent the patch sticking.
2. Tear open the patch package where indicated (use the fingers rather than
scissors to prevent accidental damage to the patch).
3. Remove the protective backing from the patch. Try not to touch the adhesive
with fingers.
4. Press the adhesive side of the patch to the prepared skin site firmly. Ensure that
there is good skin contact, particularly at the edges of the patch.
5. Wash hands thoroughly with soap and water to remove any possible
contamination with medicament.

Special considerations when using patches (1):


• Hormone replacement patches should be applied below the waist on the buttocks
or thighs; NOT on the breasts.
• Contraceptive patches should be applied to the buttocks, abdomen, upper outer
arm or upper torso; NOT on the breasts.
• Andropatch skin patches containing testosterone should be applied on the back,
abdomen, upper arms or thighs. Avoid bony areas such as shoulders and hips that
may be subjected to prolonged pressure during sleeping or sitting, as this may
cause burn-like reactions of the skin. Do not apply the patches to the scrotum.
• Glyceryl trinitrate patches for angina should be applied to the chest or upper
arm.
• Nicotine replacement patches should be applied to the chest, upper arm or hip.
• The site of application for fentanyl patches (an analgesic) depends on the brand
of product used. Read the individual patient information leaflet for more details.

Tips when using patches (1):


• Choose an area of skin that is not hairy, scarred, calloused or broken.
• Try to choose an area where the patch is unlikely to be rubbed off by tight
clothing (for example, avoid the waist).
• Remove the old patch each time you apply a new one.
• Try not to reuse the same area to apply patches as this will make irritation more
likely.
• Skin patches should be covered and protected from sunlight. The application of
heat may increase the amount of medication absorbed.
• Make sure the edges of the patch are well sealed with no air pockets. This will
ensure that you can bathe, shower or swim without removing the patch. (Not all
patches allow this; the patient information leaflet will give guidance as to whether
or not the patch will remain in place after bathing, etc.)
• Problems with the patch ‗sticking‘ may be due to the fact that the skin is too hot
when the patch is applied. After washing the skin, dry carefully and allow the skin
to cool before applying. This may improve the adhesive properties.
• If the skin feels sticky once the old patch has been removed this can be cleaned
away using baby oil.
8
1.8-Administration of drugs by mouth:
How to take tablets and capsules (1): How to take sublingual tablets (1):
1. Ideally the tablets or capsules should 1. Sit down.
be taken while standing or at least 2. Take a sip of water to moisten the
sitting upright. mouth if it is dry.
2. Place the tablet or capsule in the 3. Swallow or spit out the water.
mouth. 4. Place the tablet under the tongue.
3. Swallow with the aid of a glass of 5. Close the mouth and do not swallow
water. (Plenty of water ensures that the until the tablet has dissolved completely.
tablet or capsule reaches the stomach Do not hasten the process by moving the
and does not feel that it is ‗stuck‘ in the tablet around the mouth with the tongue.
throat.) Do not chew or swallow the tablet and
4. Do not lie down flat for at least 2 do not eat drink or smoke while the
minutes. tablet is dissolving.
6. Do not rinse out the mouth for several
How to take soluble tablets (1): minutes after the tablet has dissolved.
1. Place the tablet or tablets into a
small glassful of water.
2. Stir to dissolve the tablets.
3. Drink the resultant solution.

How to take buccal tablets (1):


1. Sit down.
2. Take a sip of water to moisten the
mouth if it is dry.
3. Swallow or spit out the water.
4. Place the tablet between the cheek
and the upper or lower gum (or
alternatively between the upper gum
and the lip)
5. Close the mouth and do not swallow
until the tablet has dissolved
completely. Do not hasten the process
by moving the tablet around the mouth
with the tongue. Do not chew or
swallow the tablet and do not eat drink
or smoke while the tablet is dissolving.
6. Do not rinse out the mouth for several minutes after the tablet has dissolved.
9
References
1-Christopher A Langley, Dawn Belcher. Applied Pharmaceutical Practice.
Pharmaceutical Press. 2009.
2-American pharmacists association. Handbook of Non-prescription drugs: An
Interactive Approach to Self-Care. 18th edition. 2016.
3-Nursing Spectrum Drug Handbook. 2016.

11
Chapter Two: Cardiovascular System
2.1-Angiotensin-converting enzyme inhibitors (ACE inhibitors)
1-They inhibit ACE, thereby inhibiting the conversion of angiotensin I to
angiotensin II, a potent vasoconstrictor (1).
2- Members of the drug class include: (captopril, enalapril, fosinopril, imidapril,
lisinopril, perindopril, quinapril, ramipril, and trandolapril) (2).
3-The main uses of ACE inhibitors are in the management of heart failure,
hypertension, and myocardial infarction (3). In addition, they are used for the
prevention and treatment of diabetic nephropathy (1) (early evidence of
nephropathy is the presence of albumin in the urine) (4).
4-Pronounced hypotension may occur at the start of therapy with ACE inhibitors
(first dose hypotension) (3). Therefore:
A-Therapy should be started with low doses followed by gradual titration as
tolerated to target doses (5).
B-For hypertension the first dose should preferably be given at bedtime (2).
5-Other adverse effects include persistent dry cough (3)[see Angiotensin II
receptor blocker (ARBs) below]. (Occurs in up to 20% of patients and is thought
to be due to inhibition of bradykinin breakdown) (5).
6-An ACEi, as well as an ARB or direct renin inhibitor, are contraindicated in
pregnancy (5).
7-Counseling points for the drug class
● Notify a healthcare professional if a cough develops (1).
● For hypertension the first dose should preferably be given at bedtime (2).
ACE inhibitors
Scientific name Trade names Dosage form
1

Any extra notes:

11
2.2-Angiotensin II receptor blockers(ARBs).
1-They block the binding of angiotensin II to the AT1 receptor, thereby inhibiting
the effects of angiotensin II, a potent vasoconstrictor (1).
2-Members of the drug class include: (azilsartan, candesartan, eprosartan,
irbesartan, losartan, olmesartan, telmisartan, and valsartan) (sartans) (2).
3-They are used for hypertension, heart failure, diabetic nephropathy, and
myocardial infarction (1).
4-As with ACE inhibitors, initiate therapy with low doses and then titrate to target
doses (5).
5-Imortant: unlike ACE inhibitors, they are less likely to cause the persistent
dry cough (2) (less than 1%) (6) which can complicate ACE inhibitor therapy. They
are therefore a useful alternative for patients who have to discontinue an ACE
inhibitor because of persistent cough (2).
Angiotensin II receptor blockers
Scientific name Trade names Dosage form
1

Any extra notes:

2.3-Angiotensin receptor–neprilysin inhibitor (ARNI)


1-Sacubitril (a neprilysin inhibitor) inhibits the breakdown of natriuretic peptides
resulting in varied effects including increased diuresis, natriuresis, and vasodilation
(2)
.
2-The combination of (ARNI) is indicated for chronic heart failure with reduced
ejection fraction (Systolic HF) (2).
Scientific name Trade name Dosage form
1 Valsartan/sacubitril

Any extra notes:

12
2.4-Beta-adrenoceptor blocking drugs (beta-blockers)
1-Beta blockers block response to beta-adrenergic stimulation at the receptor level,
which results in decreases in heart rate, myocardial contractility, blood pressure,
and myocardial oxygen demand (1).
2-Members of the drug class include (atenolol, bisoprolol, carvedilol, metoprolol,
nadolol, oxprenolol, pindolol, and propranolol) (2).
3-Usage for the drug class:
●Cardiovascular uses: Angina, arrhythmias, heart failure (bisoprolol,
carvedilol, metoprolol(1) and nebivolol(2)), hypertension, and myocardial
infarction (1).
●Noncardiovascular uses: Essential tremors, prophylaxis of migraine and of
variceal bleeding associated with portal hypertension, management of alcohol
withdrawal, anxiety disorders, and treatment of thyrotoxicosis symptoms. Some
beta blockers are used as eye drops in the management of glaucoma and ocular
hypertension (1, 3).
4-Important:
A-β-blockers are effective for reducing blood pressure but other
antihypertensives are usually more effective for reducing the incidence of
stroke, myocardial infarction, and cardiovascular mortality, especially in the
elderly (2). Therefore, for patients with hypertension but without compelling
indications, a β-blocker should not be used as the initial first-line agent (5).
B-A β-blocker is only an appropriate first-line agent in hypertension when
used to treat specific compelling indications (e.g., ischemic heart disease,
heart failure) (5).
5-Atenolol, and nadolol are the most water soluble; they are less likely to enter
the brain, and may therefore cause less sleep disturbance and nightmares. They are
excreted by the kidneys and dosage reduction is often necessary in renal
impairment (2).
6-Beta-blockers can precipitate bronchospasm and should therefore usually be
avoided in patients with a history of asthma (2).
7-Atenolol, bisoprolol, metoprolol, and nebivolol, have less effect on the β2
(bronchial) receptors and are, therefore, relatively cardioselective. They have a
lesser effect on airways resistance but are not free of this side-effect (2).
8-Beta-blockers are also associated with fatigue, coldness of the extremities (may
be less common with those with ISA), and sleep disturbances with nightmares
(may be less common with the water-soluble beta-blockers) (2).

9-Abrupt cessation of β-blocker therapy may produce unstable angina, MI, or


even death in patients with coronary disease. In patients without heart disease,
abrupt discontinuation of β-blockers may be associated with tachycardia, sweating,

13
and generalized malaise in addition to increased BP. For these reasons, the dose
should always be tapered gradually over 1 to 2 weeks before discontinuation (5).
10-Counseling points for the drug class: Do not abruptly stop taking
medication. Beta blockers should be gradually tapered when stopping (1).
Beta-blockers
Scientific name Trade name Dosage form
1

Any extra notes:

2.5-Calcium-channel blockers (CCBs)


1-These agents block calcium channels in the peripheral blood vessels and/or the
heart (7).
A-Dihydropyridine CCBs (examples: amlodipine, felodipine, nifedipine,
isradipine, nicardipine, nimodipine, nisoldipine) (1) : They have a greater
selectivity for vascular smooth muscle than for heart and therefore their main
effect is vasodilatation (3).
B-Non-Dihydropyridine CCBs (examples diltiazem and verapamil): They
have a greater selectivity for heart than for vascular smooth muscle (3).
Verapamil decreases heart rate. Diltiazem decreases heart rate to a lesser extent
than verapamil (5).
2-The main use of CCBs is in the management of angina pectoris and
hypertension (both types of CCBs) ; some are also used in cardiac arrhythmias
(non-dihydropyridine CCBs) (3). All are valuable in forms of angina associated
with coronary vasospasm (2).
3-Verapamil is used also as prophylaxis of cluster headache (2) and migraine
prophylaxis (1). Nifedipine is also indicated for Raynaud’s syndrome,
postponement of premature labour, hiccup in palliative care, and chronic
anal fissure (by rectum using ointment). Diltiazem is also indicated for chronic
anal fissure (by rectum using ointment) (2).

14
4-Amlodipine and felodipine have a longer duration of action and can be given
once daily (2).
5-Side-effects associated with vasodilatation such as flushing and headache (which
become less obtrusive after a few days), and ankle swelling (which may respond
only partially to diuretics) are common (2). Constipation is the most common side-
effect of verapamil (2).
6- Calcium channel blockers, with the exception of amlodipine, should be avoided
in heart failure as they can further depress cardiac function and exacerbate
symptoms (2).

CCBs
Scientific name Trade names Dosage form
1

Any extra notes:

2.6-Diuretics
1-The principal groups of diuretics are as follows (Table 2-12).
Table 2-1: Types of diuretics
Diuretic type examples
Thiazide and related diuretics Hydrochlorothiazide, Chlortalidone
Loop Diuretics Furosemide, Bumetanide and Torasemide
Potassium (K+)-sparing diuretics Amiloride and triamterene
Aldosterone antagonist Spironolactone
Carbonic anhydrase inhibitors Acetazolamide (mainly for glaucoma)
Osmotic diuretics Mannitol (used in cerebral edema)
2-Diuretics promote the excretion of water and electrolytes by the kidneys. They
are used in the treatment of heart failure, hypertension and other diseases when
salt and water retention has resulted in edema (3).

15
(5)
3-Thiazides are the preferred type of diuretic for hypertension . Loop
diuretics are the most widely used diuretics in heart failure (4).
4-The loop diuretics are more potent than thiazides, and retain their effectiveness
in renal insufficiency. Thus, in most patients with HF, loop diuretics are
preferred (8).
5-Potassium-sparing diuretics are weak antihypertensives when used alone.
Their primary use is in combination with another diuretic to counteract potassium-
wasting properties (5).
6-Mannitol is an osmotic diuretic that can be used to treat cerebral edema and
raised intra-ocular pressure (2).
7-Hypokalemia can occur with both thiazide and loop diuretics. Potassium-
sparing diuretics may cause hyperkalemia (5).
8-Spironolactone is given after food (2). It has an anti-androgenic properties,
therefore:
A-It may cause side effects like gynecomastia (breast enlargement), and
impotence in men (3).
B- It has been used for its anti-androgenic properties in some cases of acne and
for women with hirsutism (hair on the face) (3).

Diuretics
Scientific name Trade names Dosage form
1

Any extra notes:

https://t.me/Pharmacists_worlds

16
Note : Fixed-dose combination products
1-Several fixed-dose combination products are available , their use can reduce
the number of tablets or capsules taken by patients. This has been demonstrated
to improve adherence compared with using two separate single-drug
products. Improved adherence may increase the likelihood of achieving goal BP
values (8).
2-Most fixed-dose combinations include a thiazide diuretic. Other fixed-dose
combination products combine a CCB with either an ACEI or ARB (8).

Fixed-dose combination products


Scientific name Trade name Dosage form
1

2.7-Lipid-regulating drugs
1-Lipid regulating drugs are used to modify blood lipid concentrations in the
management of dyslipidemias and for the reduction of cardiovascular risk (3).
2-The principal groups of lipid regulating drugs are (Table 2-2) (2, 5):

Table 2-2: Types of lipid regulating drugs (2, 5)


Class Examples
1 Statins Atorvastatin, Fluvastatin, Pravastatin, Rosuvastatin,
and Simvastatin
2 Fibrates Bezafibrate, Ciprofibrate, Fenofibrate, and
Gemfibrozil
3 Nicotinic acid Acipimox, and Nicotinic acid.
derivatives
4 Bile acid sequestrants Colesevelam, Colestipol, and Colestyramine.,
5 Absorption inhibitors Ezetimibe
6 Others Omega-3 fatty acid compounds
2.7.1-Statins
1-Statins inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase,
interrupting conversion of HMG-CoA to mevalonate, the rate-limiting step in
cholesterol biosynthesis (5).

17
2-Statins are more effective than other lipid-regulating drugs at lowering
LDL-cholesterol concentration but they are less effective than the fibrates in
reducing triglyceride concentration (2).
3-Statins are used adjunct to diet and exercise for various dyslipidemias (1).
4-Rosuvastatin and atorvastatin have the longest half-lives. The long half-life
also allows for administration at any time of day rather than at bedtime for
maximum effect, which is recommended for simvastatin, lovastatin, pravastatin,
and fluvastatin (8) (Cholesterol synthesis in the liver peaks during the early morning
(midnight to 3 a.m.) (3).
5-Muscle toxicity can occur with all statins, however the likelihood increases with
higher doses. Therefore, advise patients to report promptly unexplained muscle
pain, tenderness, or weakness (2).
6-Liver enzymes should be measured before treatment, and repeated within 3
months and at 12 months of starting treatment, unless indicated at other times by
signs or symptoms suggestive of hepatotoxicity (2).
7-Avoid drinking grapefruit juice with statins metabolized by the CYP3A4
system (1)[ lovastatin, simvastatin, atorvastatin (avoid excess quantities :> 1.2
L/day)] (6).
2.7.2-Fibrates
1-Fibrates are mainly used for the treatment of hypertriglyceridemia (1).
2-Bezafibrate and fenofibrate are given with or just after food while gemfibrozil is
given 30 to 60 minutes before food (2).
2.7.3-Cholesterol absorption inhibitor (Ezetimibe)
1-Ezetimibe inhibits the intestinal absorption of cholesterol. If used alone, it
has a modest effect on lowering LDL-cholesterol, with little effect on other
lipoproteins (2).
2-It is specifically used in combination with a statin to lower LDL. Ezetimibe is
taken without regard to meals (1).
2.7.4-Others
Fish oil supplementation (omega-3 polyunsaturated fatty acids) lowers TG by
26%–45% (9). Used as adjunctive therapy to treat hypertriglyceridemia and as
adjunct in secondary prevention in those who have had a myocardial infarction in
the preceding 3 months (2).
Lipid-regulating drugs
Scientific name Trade names Dosage form
1

18
3

Any extra notes:

2.8-Nitrates
1-Nitrates are peripheral and coronary vasodilators used in the management of
angina pectoris, heart failure, myocardial infarction (3), for anal fissure (by rectum
using ointment), and prophylaxis of phlebitis and extravasation (‗5‘ patch only) (2).
2-Sublingual Glyceryl trinitrate (GTN)(Nitroglycerin: NTG) is effective for
providing rapid symptomatic relief of angina. The aerosol spray provides an
alternative method of rapid relief of symptoms for those who find difficulty in
dissolving sublingual preparations (2).
3-If using the GTN spray, patient should apply the spray on or under the tongue
and not swallow or inhale it (8).
4-Patient education about sublingual glyceryl trinitrate (Table 2-3)
Table 2-3: Patient education about sublingual glyceryl trinitrate
1-In the event of an acute attack, patients should be instructed to sit or lie down,
place the dose (spray or tablet) under the tongue, and not swallow the tablet.
Relief of pain should occur within 5 minutes (9). If the pain persists or is
unimproved 5 minutes after the first dose of GTN, the patient should call an
ambulance transport as they may be experiencing an MI. If patient needs more
than one tablet, he can take a maximum of three tablets in 15 minutes (8).
2-SL NTG can also be used to prevent acute episodes of angina. When patients
want to participate in activities which they know lead to angina, they can take a
dose of SL NTG 2 to 5 minutes in advance. This prophylactic dose provides up to
30 minutes of protection and allows patients to participate in activities that they
might otherwise be unable (5).
3-The tablets should be dispensed in the original, unopened manufacturer‘s
container and stored in the original brown bottle (8).
4-The bottle should be stored in a cool, dry place, but not refrigerated. The bottle
should be closed tightly after each opening (8).
5-GTN tablets should be supplied in glass containers of not more than 100 tablets
closed with a foil-lined cap, and containing no cotton wool wadding; they should
be discarded after 8 weeks in use (2).
6-Expiration dating should be monitored closely, and tablets should be replaced
immediately if they are exposed to excessive light, heat, moisture, or air (8).
19
5-Transdermal GTN patches, isosorbide dinitrate (ISDN) and isosorbide
mononitrate (ISMN) are most commonly prescribed for long-term prevention
(prophylaxis) of angina episodes (5).
6-ISMN is the primary metabolite of ISDN. To minimize the potential
development of nitrate tolerance, ISMN should be used in a twice-daily (the first
dose is taken on awakening and the second dose about 7 hours later) (8).
7-Modified release formulations of ISMN should only be given once daily (dose
to be taken in the morning), and used in this way do not produce tolerance (2).
8-Despite the availability of ISMN, oral ISDN is still commonly used. ISDN needs
to be dosed three times a day (7 AM, noon, and 5 PM ) (8). In the case of
modified release tablets of ISDN, the second of the two daily doses should be
given after about 8 hours rather than after 12 hours (2).
9-Common side effects of nitrate therapy include hypotension, dizziness, and
headache (5). Headache usually resolves after about two weeks of continued
therapy (4) and may be treated with acetaminophen (8).
10-Rectal ointment should be discarded 8 weeks after first opening (2).
11-Transdermal patch: Apply once daily to skin site that is free of hair and not
subject to excessive movement. Avoid areas with cuts or irritations. Do not apply
to distal parts of the extremities. Use caution when discarding to keep out of the
reach of children or pets. Remove at night for a 12-hour ―nitrate-free interval.‖
May contain metal; remove prior to MRI (1).
Nitrates
Scientific name Trade names Dosage form
1

Any extra notes:

2.9-Antiplatelet drugs
1-Antiplatelet drugs reduce platelet aggregation and are used to prevent further
thromboembolic events in patients who have suffered myocardial infarction,
ischemic stroke or transient ischemic attacks, or unstable angina, and for
primary prevention of a thromboembolic event in patients at risk (3).

21
2-Antiplatelet drugs include aspirin, P2Y12 inhibitor antiplatelet [cangrelor (I.V),
clopidogrel, prasugrel, ticagrelor), dipyridamole, and Glycoprotein IIb/IIIa
inhibitors (abciximab, eptifibatide and tirofiban) (2).
3-Aspirin is given following coronary bypass surgery. It is also used in atrial
fibrillation, for intermittent claudication, for stable angina and acute coronary
syndromes, for use following placement of coronary stents and for use in stroke (2).
4-Clopidogrel monotherapy may be an alternative when aspirin is contra-
indicated, for example in those with aspirin hypersensitivity, or when aspirin is not
tolerated despite the addition of a proton pump inhibitor (2).
5-Aspirin is also used as an analgesic and antipyretic (2).
6-Owing to an association with Reye’s syndrome, aspirin-containing
preparations should not be given to children under 16 years, unless specifically
indicated, e.g. for Kawasaki disease (2).
7-Contra-indications of aspirin include: Active peptic ulceration, bleeding
disorders, children under 16 years (risk of Reye‘s syndrome), haemophilia.
previous peptic ulceration (analgesic dose) and cardiac failure (analgesic dose) (2).
8-Aspirin is contraindicated in history of hypersensitivity to aspirin or any other
NSAID—which includes those in whom attacks of asthma, angioedema, urticaria,
or rhinitis have been precipitated by aspirin or any other NSAID (2).
9-Aspirin tablet commonly formulated as enteric coated tablet to decrease GIT
irritation.
Antiplatelet drugs
Scientific name Trade names Dosage form
1

Any extra notes:

2.10-Anticoagulants
1-Anticoagulants are used in the treatment and prophylaxis of thromboembolic
disorders (3).
21
2-Different types of anticoagulants are available (Table 2-4) (2).
Table 2-4: Types of anticoagulants (2).
Parenteral anticoagulants Oral anticoagulants
1 Unfractionated Heparin (UFH) 1 Warfarin
Low molecular weight heparins Direct Oral Anticoagulants
(LMWHs) (dalteparin, enoxaparin and (DOACs) Dabigatran,
2 tinzaparin) 2 Rivaroxaban, apixaban ,
betrixaban, and edoxaban

2.10.1-Unfractionated heparin (UFH)


1-UFH can be administered via the intravenous (IV) or subcutaneous (SC) route (4).
2-The activated partial thromboplastin time (aPTT) is the most widely used test in
clinical practice to monitor UFH. Traditionally, therapeutic aPTT range is defined
as 1.5 to 2.5 times the control aPTT value (4).
3-Side effects associated with UFH include bleeding, thrombocytopenia, and with
prolonged use, alopecia, hyperkalemia, and osteoporosis (4).
A-Bleeding is the most common adverse effect associated with antithrombotic
drugs including UFH therapy. Patients receiving UFH therapy should be closely
monitored for signs and symptoms of bleeding, including epistaxis, hemoptysis,
hematuria, hematemesis, and melena (4).
B-If major bleeding occurs, discontinue UFH immediately and give IV
protamine sulfate (5).
2.10.2-Low-molecular-weight heparins
1-Advantages of LMWHs over UFH include: (A) predictable anticoagulation
dose response, (B) improved SC bioavailability, (C) dose-independent
clearance, (D) longer biologic half-life, E) lower incidence of
thrombocytopenia, and (F) reduced need for routine laboratory monitoring (5).
2-As with other anticoagulants, bleeding is the most common adverse effect of
LMWH therapy, but major bleeding may be less common than with UFH. If major
bleeding occurs, administer protamine sulfate IV, although it cannot neutralize the
anticoagulant effect completely (5).
3-Thrombocytopenia can occur with LMWHs, but the incidence of HIT is three
times lower than with UFH (5).
2.10.3-Warfarin
1-Warfarin inhibits the production of vitamin K–dependent clotting factors.
Warfarin has no effect on circulating coagulation factors that have been previously
formed, and its therapeutic antithrombotic activity is delayed for 5 to 7 days (4).

22
2-Monitor warfarin therapy by the international normalized ratio (INR); the
recommended target INR for treatment and prevention of VTE is 2.5, with an
acceptable range of 2 to 3(4).
3-Similar to other anticoagulants, warfarin’s primary side effect is bleeding.
Bleeding in the gastrointestinal tract is most common. Intracranial hemorrhage
(ICH) is one of the most serious complications because it often causes severe
disability and death (4).
4-Warfarin is prone to numerous clinically significant drug–drug and drug–food
interactions. Patients on warfarin should be questioned at every encounter to
assess for any potential interactions with foods, drugs, herbal products, and
nutritional supplements (4).
5-Vitamin K is the antidote of warfarin (1). In cases of life-threatening bleeding,
fresh-frozen plasma or clotting factor concentrates should also be administered, in
addition to IV vitamin K (4).
2.10.4-Direct oral anticoagulants:
1-These currently include two categories, direct thrombin (factor IIa) inhibitor
(DTI) (dabigatran) and direct Xa inhibitors (rivaroxaban, apixaban, and
edoxaban) (10).
2-As compared to warfarin, these oral anticoagulants have a more rapid onset,
shorter half-life, wider therapeutic window, and more predictable
pharmacokinetics (10).
Anticoagulants
Scientific name Trade names Dosage form
1

Any extra notes:

23
2.11-Anti-arrhythmic drugs
1-Anti-arrhythmic drugs can be classified clinically into those that act on
supraventricular arrhythmias (e.g. verapamil), those that act on both
supraventricular and ventricular arrhythmias (e.g. amiodarone), and those that act
on ventricular arrhythmias (e.g. lidocaine) (2) (Table 2-5) (11).
Table 2-5: classification of Anti-arrhythmic drugs according to principal site
of action

2-Amiodarone is the most commonly used antiarrhythmic agent. It is used for rate
and rhythm control of atrial fibrillation and to treat and prevent ventricular
arrhythmias (1).
3-Although amiodarone is the most commonly used antiarrhythmic, it should be
reserved for patients with life-threatening arrhythmias due to its substantial
toxicity (1).
4-Digoxin is a cardiac glycoside that increases the force of myocardial contraction
(so used for HF) and reduces conductivity within the atrioventricular (AV) node
(so used for atrial fibrillation or flutter) (2).
Anti-arrhythmic drugs
Scientific name Trade names Dosage form
1

Any extra notes:

24
2.12-Miscellaneous cardiovascular drugs
2.12.1-Fibrinolytic drugs (alteplase, reteplase, tenecteplase)
1-Thrombolytic drugs are indicated for any patient with acute ST-segment
elevation myocardial infarction (STEMI) for whom the benefit is likely to
outweigh the risk of treatment (2).
2-Alteplase can be used for other thromboembolic disorders such as deep-vein
thrombosis and pulmonary embolism (2). Alteplase is also used for acute
ischaemic stroke (2).
3-Serious bleeding calls for discontinuation of the thrombolytic and may require
administration of coagulation factors and antifibrinolytic drugs (2).
2.12.2-Antifibrinolytic drugs
Fibrin dissolution can be impaired by the administration of tranexamic acid,
which inhibits fibrinolysis. It can be used to prevent bleeding or to treat
bleeding associated with excessive fibrinolysis (e.g. in surgery, dental extraction,
and obstetric disorders) and in the management of menorrhagia (2).
Scientific name Trade names Dosage form
1

2.12.3-Centrally acting antihypertensive drugs


Methyldopa is a centrally acting antihypertensive; it may be used for the
management of hypertension in pregnancy (2).
Scientific name Trade names Dosage form
1

2.12.4-Peripheral vasodilators (e.g. cilostazol, pentoxifylline)


1-Peripheral vascular disease can be either occlusive (e.g. intermittent
claudication) in which occlusion of the peripheral arteries is caused by
atherosclerosis, or vasospastic (e.g. Raynaud’s syndrome) (2).
2-Cilostazol is licensed for use in intermittent claudication to improve walking (2).
3-Pentoxifylline is another agent approved by the FDA for the treatment
intermittent claudication (limited role) (8).
Scientific name Trade names Dosage form
1

25
References
1-Michael AM, Jason. Frequently prescribed medications. Third edition 2019.
2-BNF-81 (2021)
3-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
4- Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
5-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.
6-ACCP Updates in Therapeutics® 2021: The Pharmacotherapy Preparatory
Review and Recertification Course.
7-Roger Walker. Clinical Pharmacy and Therapeutics. Sixth edition 2019
8-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
9-David J Quan, Richard A Helms. Textbook of Therapeutics: Drug and Disease
Management. 8th edition. 2006.
10-Pavan Bhat, et al. Washington Manual of Medical Therapeutics, The, 35th
Edition. Copyright 2016.
11-Helen Williams.V Arrhythmia : part 1. The pharmaceutical journal (VOL 271)
(2003):368-370.

26
Chapter Three: Gastro-intestinal System
3.1-Drugs for inflammatory bowel disease.
Notes:
1-Chronic inflammatory bowel diseases (IBD) include crohn’s disease (CD) and
ulcerative colitis (UC) (1). UC is confined to the rectum and colon, while CD can
involve any part of the gastrointestinal (GI) tract (2).
2-The major drug therapies used in IBD are aminosalicylates; corticosteroids;
immunomodulators (azathioprine, mercaptopurine, and methotrexate);
immunosuppressive agents (ciclosporine and tacrolimus); antimicrobials
(metronidazole and ciprofloxacin) monoclonal antibodies (infliximab,
adalimumab, golimumab, certolizumab, natalizumab, ustekinumab, and
vedolizumab) or Janus kinase function (tofacitinib) (2).
3.1.1-Aminosalicylates
1-Aminosalicylates include Sulfasalazine [a combination of 5-aminosalicylic
acid, (‗5-ASA‘) and sulfapyridine (acts as a carrier and believed to be responsible
for many of the adverse reactions to sulfasalazine)], and the safer sulfa-free
compounds [mesalazine (mesalamine)(5-ASA), balsalazide (a pro-drug of 5-ASA)
and olsalazine (a dimer of 5-ASA)] (1-3).
2-The aminosalicylates are among the most commonly used drugs for inducing
and maintaining remission in patients with mild to moderate IBD (4).
3-Enemas are appropriate for patients with
left-sided disease because the medication will
reach the splenic flexure. Suppositories
deliver mesalamine up to approximately 20 cm
and are most appropriate for treating
proctitis (4).
4-Oral and topical mesalamine preparations
may be used together for maximal effect.
Oral mesalamine may also be used for patients
who are unwilling or unable to use topical
preparations (4).
5-The extent of disease should be considered when choosing the route of
administration. If the inflammation is distal, a rectal preparation is adequate but if
the inflammation is extended, systemic medication is required (1).
6-Enemas or suppositories (when given once daily) are preferably administered at
bedtime, preferably after a bowel movement (1).
7-Oral aminosalicylates for the treatment of ulcerative colitis are available in
different preparations and release forms. The preparation and dosing schedule
should be chosen taking into account the delivery characteristics and suitability
for the patient (1).

27
8-Unlike sulfasalazine, sulfa-free compounds are safe to use for patients with
sulfonamide allergies (3).
9-Blood count should be performed and the drug stopped immediately if there is
suspicion of a blood dyscrasia (1).
10-Patients receiving aminosalicylates, and their carers, should be advised to report
any unexplained bleeding, bruising, purpura, sore throat, fever or malaise that
occurs during treatment (Blood disorders) (1).
11-Olsalazine is associated with a higher incidence of secretory diarrhea than
other aminosalicylates (4).
12-Aminosalicylates are contra-indicated in salicylate hypersensitivity (1).
13-Balsalazide and olsalazine are taken after food (1).
14-Note: sulfasalazine is also used for rheumatoid arthritis [it is one of the
Disease-Modifying Antirheumatic Drugs (DMARDs)] (1).

Aminosalicylates
Scientific name Trade names Dosage form(s)
1

Any extra notes:

3.2-Proton pump inhibitors (PPIs)


1-Drug action: Proton pump inhibitors inhibit gastric acid secretion by blocking
the H+/K+-ATPase (the ‗proton pump‘) of the gastric parietal cell (1).
2-PPIs are the most potent inhibitors of gastric acid secretion. PPIs include
omeprazole, lansoprazole, rabeprazole, pantoprazole, and esomeprazole (2).
3-PPIs are used for the treatments of gastric and duodenal ulcers; they are also
used in combination with antibacterials for the eradication of Helicobacter
pylori (a bacteria that is common cause of ulcer). PPIs can be used for the
treatment of dyspepsia and gastro-oesophageal reflux disease. They are also
used for the prevention and treatment of NSAID-associated ulcers (1).

28
4-PPIs are most effective when taken 30 to 60 minutes before meals (3).The once
daily dose usually given in the morning before meals. Large doses should be
given in 2 divided doses (1) (for divided dosing, give evening dose before evening
meal instead of at bedtime) (5).
5-PPIs are formulated as delayed-release enteric-coated dosage forms that have
pH-sensitive granules contained in gelatin capsules (omeprazole, esomeprazole,
and lansoprazole), rapidly disintegrating tablets (lansoprazole), and delayed-release
enteric-coated tablets (rabeprazole, pantoprazole, and nonprescription omeprazole).
Omeprazole is also available in a delayed-release tablet and in a combination
product with sodium bicarbonate in an immediate-release capsule and oral
suspension (Zegerid®) (2). The sodium bicarbonate raises intragastric pH,
permitting rapid absorption of omeprazole from the duodenum (6).
6-PPIs are generally considered interchangeable; selection of agent is usually
based on cost and formulary considerations (7).
PPIs
Scientific names Trade name Dosage form

Any extra notes:

3.3-Histamine-2 receptor antagonists (H2RAs)


1-Drug action: H2RAs reduce gastric acid output as a result of histamine H2-
receptor blockade (1).
2-H2RAs include cimetidine, ranitidine, famotidine, and nizatidine (2).
3-H2RAs are used for the treatments of gastric and duodenal ulcers. They can be
used for the treatment of dyspepsia and gastro-oesophageal reflux disease (1).
4-Cimetidine inhibits several CYP450 isoenzymes, resulting in numerous drug
interactions (e.g., theophylline, warfarin, and clopidogrel) (2). Avoidance of the
combination, or a reduction in the dosage of these drugs may be required (8).

29
5-Ranitidine has less potential for hepatic CYP450 drug interactions, while
famotidine and nizatidine do not interact with drugs metabolized by the hepatic
CYP450 pathway (3).
6-Cimetidine has demonstrated weak antiandrogenic effects, and its use in high
doses has been associated with gynecomastia and impotence in men. This effect
is reversible with discontinuation of the medication or by switching to another
H2RA (3).
H2RAs
Scientific names Trade name Dosage form

Any extra notes:

3.4-Treatment of H. pylori–associated ulcers


1-H. pylori is a common cause of both gastric and duodenal ulcer. General
recommendations, are to include an antisecretory agent (preferably a PPI) plus at
least two antibiotics in the eradication regimen (5).
(5)
2-Therapy duration is usually 10–14 days .
3-Several first-line therapies are recommended, but bismuth quadruple therapy
(bismuth subsalicylate, metronidazole, tetracycline, and a PPI ) for 10-14 days
should be used preferentially (2). (Table 3-1)
4-Another recommended first line therapy is concomitant therapy (PPI,
clarithromycin, with amoxicillin and metronidazole) for 10 to 14 days (2).
5-Clarithromycin triple therapy is no longer recommended in areas where H.
pylori resistance exceeds 15% (2).
6-Sequential therapy: Sequential therapy involves administration of a PPI and
amoxicillin given for the first 5 days, followed by a PPI, clarithromycin, and
tinidazole for an additional 5 days (5).
7-Quadruple-based therapy:
A-Bismuth subsalicylate, metronidazole, tetracycline, and a PPI (5).
B-Nonbismuth quadruple therapy (also called ―concomitant‖ therapy)
contains a PPI, amoxicillin, clarithromycin, and metronidazole taken together
at standard doses for 10 -14 days (2).
31
8-Hybrid therapy (combines the strategies of concomitant and sequential therapy)
involves 7 days of dual therapy (PPI and amoxicillin) followed by 7 days of
quadruple therapy (PPI, amoxicillin, clarithromycin, and metronidazole) (2).
9-Levofloxacin-Based Therapy
Levofloxacin has been studied as first-line therapy and (after initial treatment
failure) for H. pylori eradication. Three regimens using levofloxacin have been
suggested (levofloxacin triple therapy, levofloxacin sequential therapy and
Quadruple therapy) (Table 3-1). Concerns about using fluoroquinolones to
treat H. pylori include development of resistance and adverse effects (e.g.,
tendonitis and hepatotoxicity) (2).

Table 3-1. Recommended Treatment Regimens for Helicobacter pylori


Infection (5).

31
BID: twice daily; PPI : proton pump inhibitor; QID : four times daily; TID : three times daily.

3.5-Antacids:
1-Antacids are basic compounds that neutralize hydrochloric acid in the gastric
secretions. They are used in the symptomatic management of gastrointestinal
disorders associated with gastric hyperacidity such as dyspepsia, GERD, and
peptic ulcer disease (8).
2-Antacid agents include a variety of aluminum, magnesium, and calcium
products available as single and combination therapy preparations in multiple
dosage forms (7).
3-Antacids are best given when symptoms occur (i.e. when required) or are
expected, usually between meals and at bedtime (1). When taken 1 h after a meal,
antacids may act for up to 3 h compared with only 30 min–1 h if taken before
meals (9).
4-Liquids and powders generally provide faster relief and have greater
neutralizing capacity than tablets. Advantages of tablets over liquids include ease
of portability and administration (10). It might be appropriate for the patient to have
both; the liquid could be taken before and after working hours, while the tablets
could be taken during the day for convenience (9).
5-Tablets should not be swallowed whole; they should be chewed to initiate
disintegration or sucked to provide a relatively slow but sustained delivery of
antacid to the stomach (10).
32
6-Interactions:
A-Antacids can affect the absorption of a number of drugs (via chelation and
adsorption) (11). This interactions can usually be avoided when potentially
interacting drugs are separated by at least 2 hours (7).
B-Antacids also interact with enteric-coated tablets, capsules and granules
(Enteric coatings may be disrupted prematurely in the presence of antacids,
causing unwanted release of the drug in the stomach) (10).
7-Side effects of antacids:
A-AL-containing antacids tend to be constipating. Mg-containing antacids tend
to cause osmotic diarrhea and are useful in patients who are slightly
constipated. Thus combination products of AL and Mg salts cause minimum
bowel disturbances (9).
B-Antacids containing sod. Bicarbonate: The high sodium content may cause
fluid overload in patients with congestive heart failure, renal failure, cirrhosis,
or pregnancy, and in those on sodium restricted diets (6).
C-Calcium carbonate: It acts quickly, has a prolonged action and is a potent
neutralizer of acid. It can cause acid rebound and, if taken over long periods at
high doses, can cause hypercalcaemia and so should not be recommended for
long-term use (9).
8-Other drugs that may be combined with antacid formulations include
simeticone, which acts as a defoaming agent to reduce excess gas in the stomach,
and alginates, which form a gel or foam on the surface of the stomach contents
thereby impeding reflux and protecting the oesophageal mucosa from acid
attack (8).
Antacids (including those combined with simethicone, and alginate)
Scientific names Trade names Dosage form
1

Any extra notes:

33
3.6-Laxatives:
1-Laxatives (purgatives or cathartics) promote defecation and are used in the
treatment of constipation and for bowel evacuation before investigational
procedures such as endoscopy or radiological examination, or before surgery (8)
to ensure the bowel is free of solid contents (1).
(10)
2-Laxatives can be classified into groups depending on their mode of action
(Table 3-2).
Table 3-2: types of laxatives
Type of laxative Example(s) Approximate onset
of action
Senna, Bisacodyl, Sodium Oral:6-12hours (9)
1-Stimulant laxative picosulfate, and Glycerin (supp.) Rectal: within 1
hour (9)
Methylcellulose, Bran , Sterculia 12 -24 hours, but
2-Bulk-forming and Ispaghula (Metamucil®) onset may be
laxative delayed as long as
72 hours (6)
4-Osmotic laxative Lactulose 1-2 days (9)
3.6.1-Stimulant laxatives:
1-Stimulant laxatives are thought to act mainly by stimulating the intestinal
mucosa to secrete water and electrolytes (12).
2-The main adverse effects of stimulant laxatives are griping and intestinal
cramps. Prolonged use may result in loss of colonic smooth muscle tone (10) .
However, many experts now believe that the risk of long-term use of stimulant
laxatives use have been overestimated and they are safe for daily use) (13).
3-Bisacodyl tablet is enteric-coated; therefore, it should be swallowed whole and
should not be taken within one hour of antacid or milk as this will lead to
dissolution of the coating and release of the drug into the stomach and cause
gastric irritation (10).
4-Senna is excreted via the kidney and may color the urine a yellowish-brown to
red color depending on its PH (12).
5-Senna is secreted in breast milk, and large dosages may cause increased gastric
motility and diarrhea in breastfed infants. Breastfeeding mothers should, therefore,
avoid this laxative (12). (However BNF-81 states that specialist sources indicate
suitable for use in breast-feeding in infants over 1 month (1)).
6-Usual doses:
Bisacodyl 5 mg tab. Adult dose: usually 1-2 tablets (dose to be taken at night).
While the dose of supp. Is one supp. (usually in the morning) (1).
Senna tab. Adult dose: usually 2 tablets (preferably at bedtime) (11).
Glycerin suppositories: Glycerol suppositories are normally used when a bowel
movement is needed quickly. The patient should experience a bowel movement in
34
15 to 30 minutes. Varying sizes are made to accommodate use for different ages.
The 1-g suppositories are designed for infants, the 2-g for children and the 4-g for
adults. (11).
3.6.2-Bulk-forming laxative:
1-Bulk laxatives are those that most closely resemble the normal physiological
mechanisms involved in bowel evacuation. Bulk laxatives work by swelling in the
gut and increasing faecal mass so that peristalsis is stimulated . The laxative effect
can take several days to develop (9).
2-Bulk laxatives should not be taken immediately before going to bed, because
there may be a risk of oesophageal blockage if the patient lies down directly after
taking them (10).
3-When recommending the use of a bulk laxative, the pharmacist should advise
that an increase in fluid intake would be necessary (9).
4-Adverse effects and disadvantages are relatively minor. They include:
 Risk of oesophageal and intestinal obstruction if preparations are not taken
with sufficient water.
 Abdominal distension and flatulence.
 They may not be suitable for patients who must restrict their fluid intake
severely (12).
5-Bulk-forming drugs are useful in controlling diarrhea associated with
diverticular disease (1).
3.6.3-Lactulose:
1-It can be taken by all age group, have no drug interactions and can be safely used
in pregnancy (11). However, there are some factors that may deter patients from
using lactulose: It may take 72 hours of regular dosing to produce an effect. It is
intensely sweet in taste which makes it more palatable for children, to whom it
can be given safely (10). Adult laxative dose (1): 15 ml twice daily.
2-Serious adverse effects with lactulose are rare. Relatively minor side-effects
occur in about 20% of patients taking full doses and include flatulence, cramp and
abdominal discomfort, particularly at the start of treatment (12).
3-Lactulose syrup should be used with caution in diabetic patients because it
contains lactose and galactose (14).
3.6.4-Product selection guidelines (Table 3-3).
Table 3-3:Product selection guidelines
Patient Preferred laxative
Pregnant women Bulk-forming laxative. Lactulose may be used (13)
Breast-feeding mother Bulk-forming laxative, lactulose (13)
Children Glycerin(supp.), lactulose (13)
Advanced age(elderly) Bulk-forming laxative, also lactulose and glycerin
(supp.) are safe (6, 11).
35
Laxatives (try to include the different types of laxatives )
Scientific name Trade names Type Dosage form(s)
1

Any extra notes:

3.7-Antidiarrheals
The priority in acute diarrhea is the prevention or reversal of fluid and electrolyte
depletion. This is particularly important in infants and elderly patients. Oral
rehydration preparations are used in the prevention or reversal of fluid and
electrolyte depletion. Severe depletion of fluid and electrolytes requires immediate
admission to hospital and urgent replacement treatment with an intravenous
rehydration fluid is recommended (1).
3.7.1-Antimotility drugs
[Loperamide , Co-phenotrope (Diphenoxylate+Atropine)]
Note: Atropine is included at a subtherapeutic dose to discourage abuse
(unpleasant antimuscarinic effects will be experienced if higher than recommended
doses are taken)] (12).
1-Antimotility drugs are not recommended for acute diarrhea in young children (1).
In the UK, diphenoxylate hydrochloride is not licensed for children under 4 years
of age. In the UK, loperamide is not licensed for children under 4 years of age.
In the USA, loperamide is not recommended for children under the age of 2 years
(8)
.
2-Adult doses :
Loperamide: Initially 4 mg (2 tablets or capsules) , followed by 2 mg (1 tablet or
capsule) to be taken after each loose stool; usual dose 6–8 mg daily; maximum 16
mg per day (1).
Co-phenotrope: Initially 4 tablets, followed by 2 tablets every 6 hours until
diarrhea controlled (1).
36
3.7.2-Adsorbents (pectin +kaolin)
1-There is insufficient evidence to recommend adsorbent preparations (such as
kaolin) in acute diarrhea (1).
2-Kaolin can form insoluble complexes with some drugs in the gastrointestinal
tract and reduce their absorption; oral doses should not be taken at the same
time (8).
3.7.3-Oral rehydration solution (ORS)
1-A premixed solutions (6) or sachets of powder for reconstitution are available;
these contain sodium as chloride and bicarbonate, glucose and potassium (9).
2-Only water should be used to make the solution and that boiled and cooled
water should be used for children < 1 year (9).
3-To avoid risk of possible exposure to further infection, the solution should be
discarded not later than 1 hour after reconstitution, or it may be kept for up to 24
hours if stored in a refrigerator (10).
Table 3-4:Amount of rehydration
4-Table 3-4 provides the volumes
solution to be offered to patients (9).
required per watery stool (9).
Age Quantity of solution (per
3.7.4-Probiotics (dietary watery stool)
supplement): Under 1 year 50 mL (quarter of a glass)
Probiotics are dietary supplements 1–5 years 100 mL (half a glass)
containing bacteria (including 6–12 years 200 mL (one glass)
several Lactobacillus species) that Adult 400 mL (two glasses
may promote health by enhancing
the normal microflora of the GI tract while resisting colonization by potential
pathogens (4). Probiotics have been shown to decrease the duration of infectious
and antibiotic-induced diarrhea (AAD) in adults and children (2).
3.7.5-Use of zinc in children with diarrhea:
Several large studies performed in developing countries have shown that daily
zinc supplementation in young children with acute diarrhea reduces both the
duration and severity of diarrhea. The WHO/UNICEF recommends that children
with acute diarrhea also receive zinc (10 mg of elemental zinc/day for infants
younger than 6 months; 20 mg of elemental zinc/day for older infants and children)
for 10 to 14 days (6).
Antidiarrheals
Scientific name Trade names Dosage form
1

37
Any extra notes:

3.8-Antispasmodics
1- Antispasmodics are drugs used for their relaxant action on smooth muscle. They
play a role in the management of gastrointestinal spasm and irritable bowel
syndrome (IBS) as well as other disorders associated with smooth muscle spasm
(8)
.
2-Antispasmodics include antimuscarinics (e.g. hyoscine butylbromide). Other
antispasmodics (mebeverine, alverine citrate, and peppermint oil) are used to
relieve pain in irritable bowel syndrome (1).
3-Conerning IBS (1):
A-Laxative (excluding lactulose as it may cause bloating) can be used to treat
constipation in IBS.
B-Loperamide is the first-line choice of anti-motility drug for relief of
diarrhea in IBS.
C-A low-dose tricyclic antidepressant, such as amitriptyline, can be used for
abdominal pain or discomfort as a second line option in patients who have not
responded to antispasmodics. A selective serotonin reuptake inhibitor may
be considered in those who do not respond to a tricyclic antidepressant.
Antispasmodics
Scientific name Trade names Dosage form
1

Note: antichloinergics may be combined with benzodiazepine (librax®) or


phenothiazine (stelabid®). Also they may be combined with an analgesics. They
areused for GIT disorders associated with smooth muscle spasm (8).
Compound anticholinergics
Trade names Scientific name Dosage form
Librax®

Stelabid®

Antispasmine-
co®
Riabal-co®

38
Any extra notes:

3.9-Nausea and vomiting


1-Prochlorperazine, metoclopramide and domperidone are used to treat or
prevent nausea and vomiting (1).
2-Cinnarizine is used to prevent motion sickness where the dose is taken 2 hours
before travel then every 8 hours if required (1).
3-Domperidone has the advantage over metoclopramide and the
prochlorperazine of being less likely to cause central effects such as dystonic
reactions (a tetanus-like reaction) because it does not readily cross the blood-
brain barrier (1).
4-Granisetron, ondansetron and palonosetron (5HT3-receptor antagonists) are of
value in the management of nausea and vomiting in patients receiving cytotoxics
and in postoperative nausea and vomiting (1).
5-Dexamethasone has antiemetic effects and it is used in vomiting associated
with cancer chemotherapy. It can be used alone or with metoclopramide,
prochlorperazine, lorazepam, or a 5HT3-receptor antagonist (1).
6-Doxylamine (antihistamine ) with pyridoxine (B6) combination is used for
nausea and vomiting in pregnancy (1).
7-Side effects:
A-Cinnarizine may cause drowsiness which may affect performance of skilled
tasks (e.g. cycling, driving) (1).
B-Domperidone is associated with a small increased risk of serious cardiac
side-effects (arrhythmia). Patients and their carers should be told how to
recognize signs of arrhythmia and advised to seek medical attention if
symptoms such as palpitation or syncope develop (1).
C-Metoclopramide can induce acute dystonic reactions involving facial and
skeletal muscle spasms and oculogyric crises. These dystonic effects are more
common in the young (especially girls and young women) and the very old;
they usually occur shortly after starting treatment with metoclopramide and
subside within 24 hours of stopping it (1).
Antiemetics
Scientific name Trade names Dosage form(s)
1

39
4

Any extra notes:

3.10-Anti-obesity drugs
1-An anti-obesity drug should be considered only for those with a BMI of ≥ 30
kg/m2, in whom diet, exercise and behavior changes fail to achieve a realistic
reduction in weight. In the presence of associated risk factors, it may be
appropriate to prescribe an anti-obesity drug to individuals with a BMI of ≥28
kg/m2 (1).
2-Orlistat is a gastric and pancreatic lipase inhibitor that reduces the absorption of
dietary fat. Other drugs used for obesity is liraglutide (1).
3-Orlistat is given in a usual dose of 120 mg orally three times daily, immediately
before, during, or up to 1 hour after meals. If a meal is missed or contains no
fat, the dose should be omitted (1).
4-Treatment with orlistat may also be used to maintain weight loss rather than to
continue to lose weight (1).
5-Discontinuation of treatment with orlistat should be considered after 12 weeks if
weight loss has not exceeded 5% since the start of treatment (1).
6-Orlistat may reduce the absorption of fat-soluble vitamins (A, D, E, and K)
and patients should take a multivitamin supplement that contains these vitamins.
The supplement should be taken once a day at least 2 hours before or after the
administration of orlistat, such as at bedtime (3).
7-Because orlistat‘s main effect is to prevent dietary fat from being absorbed, the
fat is excreted unchanged in the feces and so the stool may become oily or loose
(steatorrhoea) (9).
8-Increased flatulence is also common. Bowel movements may become
frequent or urgent, and cases of fecal incontinence have been seen (9).
9-To minimize these effects, foods with high fat content should be avoided.
Taking drugs for diarrhea (such as loperamide) will not control these symptoms (9).
10-It is important to have adopted the low fat diet a few days before introducing
orlistat. Oily stools and flatulence can be controlled by reducing the dietary fat
content to somewhere in the region of 15 g per meal, and it has been suggested

41
that the decrease in side effects over time may be associated with long-term
acceptance and adoption of a low fat diet (9).
11-Liraglutide (Saxenda®) [a glucagon-like peptide-1 (GLP-1) receptor agonist].
A-Liraglutide, is an injectable medication, FDA-approved for long-term
obesity management as an adjunct to lifestyle modification. When used for
obesity, the dose is titrated to 3 mg daily (3).

Scientific name Trade names Dosage form


Orlistat

Liraglutide

Any extra notes:

3.11-Local preparations for anal and rectal disorders


1-These products are used mainly for hemorrhoids, pruritus ani and anal fissure
(1)
.
2-They are usually formulated as ointments and creams or suppositories.
Ointments and creams can be used for internal and external hemorrhoids while
suppositories are used for internal hemorrhoids. However both are used twice
daily (morning and evening) and after each bowel movement (9).
3-Many people prefer suppositories, but these products are often not effective
because they tend to slip into the rectum and melt, thus bypass the anal canal
where the medication is needed. In general ointments and creams are preferred
over suppositories (13).
4-When used intrarectally, the ointment may be inserted using an applicator or
finger but the applicator is preferred because it can reach an area where the
finger cannot reach. The applicator should be lubricated by the ointment before
insertion (6).
5-Topical preparations that contain a combination of local anaesthetics,
corticosteroids, astringents, lubricants, and antiseptics are available. They can
offer symptomatic relief of local pain and itching (1).
6-Long-term use of corticosteroid creams can cause ulceration or permanent
damage due to thinning of the perianal skin and should be avoided (1).

Local preparations for anal and rectal disorders


Scientific name Trade names Dosage form
1

41
2

Any extra notes:

References
1-BNF-81 (2021)
2-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.
3-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
4-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
5-ACCP Updates in Therapeutics® 2021: The Pharmacotherapy Preparatory
Review and Recertification Course.
6-American pharmacists association. Handbook of Non-prescription drugs: An
Interactive Approach to Self-Care. 18th edition. 2016.
7-Michael AM, Jason. Frequently prescribed medications. Third edition 2019.
8-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
9-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the
pharmacy . A guide to the managements of common illness. 8th edition. 2018.
10-Nathan A. Non-prescription medicines. 4th edition. London: Pharmaceutical
Press. 2010.
11-Paul Rutter. Community Pharmacy. Symptoms, Diagnosis and Treatment. 5 th
edition. 2021.
12-Nathan A. fasttrack. Managing Symptoms in the Pharmacy. Pharmaceutical
Press. 2008.
13-Canadian pharmacists association (CPhA). CTMA: Compendium of
Therapeutics for Minor Ailments. 2018.
14-Virginia P A. Pharmacotherapeutics for Advanced Practice A Practical
Approach. 3rd edition. 2013.

42
Chapter Four: Respiratory System
4.1-Respiratory system, drug delivery
4.1.1-Inhalation
1-This route delivers the drug directly to the airways; the dose required is smaller
than when given by mouth and side effects are reduced (1).
2-Inhaler devices include pressurized metered-dose inhalers (MDI), breath
actuated inhalers, and dry powder inhalers (DPI). Many patients can be taught
to use a pressurized MDI effectively but some patients, particularly the elderly and
children, find them difficult to use. Spacer devices can help such patients because
they remove the need to co-ordinate actuation with inhalation (1).
3-DPI may be useful in adults and children over 5 years who are unwilling or
unable to use a pressurized MDI. Alternatively, breath-actuated inhalers are
suitable for adults and older children (1).
4-Spacer devices remove the need for coordination between actuation of a
pressurized MDI and inhalation. Spacer devices are particularly useful for patients
with poor inhalation technique, for children, for patients requiring high doses of
inhaled corticosteroids, for nocturnal asthma, and for patients prone to candidiasis
with inhaled corticosteroids (1).
5-Nebulizers:
A-A nebulizer converts a solution of a drug into an aerosol for inhalation.
Solutions for nebulization are available for use in severe acute asthma or
COPD (1).
B-They are administered over 5–10 minutes from a nebulizer usually driven by
oxygen in hospital (1).
C-Nebulization may be carried out using an undiluted nebulizer solution or it
may require dilution beforehand. The usual diluent is sterile sodium chloride
0.9% (physiological saline) (1).
4.1.2-Oral
The oral route is used when administration by inhalation is not possible. Systemic
side-effects occur more frequently when a drug is given orally rather than by
inhalation (1).
4.1.3-Parenteral
Drugs such as β2 agonists, corticosteroids, and aminophylline can be given by
injection in acute severe asthma when administration by nebulization is
inadequate or inappropriate (1).

4.2-Drugs used for asthma and/or Chronic Obstructive Pulmonary


Disease (COPD)
1-Drugs used for asthma and COPD are summarized in (Table 4-1).

43
Table 4-1: Drugs used for asthma and/or COPD (1-3)
Class Example(s) Route
Salbutamol (called albuterol Systemic
1 Bronchodilators β2-agonists in USA) terbutaline, and inhaled
formoterol and salmeterol
Antimuscarinic Ipratropium, and tiotropium Inhaled
Methylxanthines Theophylline and as Systemic
aminophylline
2 Corticosteroids Inhaled CS Beclometasone, Inhaled
(CS) mometasone, budesonide,
fluticasone.
Systemic CS Prednisolone, Systemic
hydrocortisone
3 Leukotriene Receptor Zileuton, montelukast and Oral
Antagonists (Leukotriene zafirlukast
Modifiers)
4 Mast Cell Stabilizers Cromolyn sodium (Sodium Inhaled
cromoglicate)
5 Immunosuppressants Omalizumab, and S.C
(monoclonal mepolizumab injection
antibodies) Reslizumab I.V infusion
6 Phosphodiesterase type-4 Roflumilast Oral
inhibitor
2-Treatment guidelines for asthma are shown in table (Table 4-2) (2).

Table 4-2: Treatment guidelines for asthma (2).

44
4.2.1-Beta2-adrenoceptor agonist
1-The inhaled beta-2 agonists are primarily used for the treatment and
prevention of bronchospasms in patients with obstructive airway disease (asthma
and COPD) (3).
2-Note: The beta2 agonists salbutamol and terbutaline sulfate are no longer
recommended for inhibiting uncomplicated premature labour (1).
3-Adverse effects of β2-agonists include tachycardia, tremor, and hypokalemia,
which are usually not troublesome with inhaled dosage forms (4).
4-Inhaled Short-Acting β2-Agonists (SABAs) [e.g., salbutamol and
terbutaline)
A-Inhaled SABAs are commonly used on an as-needed basis (3) .SABAs are the
most effective agents for reversing acute airway obstruction caused by
bronchoconstriction and are the drugs of choice for acute symptom relief
(asthma or COPD) (4).
B-SABAs inhaled immediately before exertion reduces exercise-induced
asthma (3).
5-Inhaled Long-Acting β2-Agonists (LABAs): Salmeterol and formoterol
A-LABAs provide 12-24 hours of bronchodilation after a single dose (4).
B-Three ultra-LABAs (indacaterol, olodaterol, and vilanterol) have a 24-hour
bronchodilator duration of effect (5).
C-LABAs are indicated for chronic treatment of asthma and COPD (4).
Inhaled LABAs are a first-line addition to ICSs and can be administered as an
individual ingredient or in a combination inhaler with an ICS (6).
D- Salmeterol has a slow onset of action (7). Salmeterol should not be used for
the relief of an acute symptom relief; it has a slower onset of action than
salbutamol or terbutaline (1, 4).
45
Note: Combination ICS with formoterol are also used on-demand for acute
relief of symptoms (5). (Formoterol has a rapid onset and, although it is effective
for rescue therapy, it should be used only for rescue treatment when combined with
an ICS) (7).
Beta2-adrenoceptor agonist
Scientific name Trade names Dosage form
1

Any extra notes:

4.2.2-Corticosteroids
1-Corticosteroids are potent anti-inflammatory agents and are available in inhaled,
oral, and injectable dosage forms (4).
2-Inhaled corticosteroids:
A-ICS are the preferred therapy for all forms of persistent asthma in all age
groups (4).
B-The clinical benefits of ICS therapy (including decreased COPD
exacerbation frequency) have been observed with combination therapy,
primarily as an addition to LABA monotherapy. ICS monotherapy is not
recommended for patients with COPD (6).
C-Although some beneficial effect is seen within 12 hours of administration of
an ICS, 2 weeks of therapy is necessary to see significant clinical effects (4).
D-Local adverse effects of ICS include oral candidiasis, cough, and
dysphonia. The incidence of local adverse effects can be reduced by using a
spacer device and by having the patient rinse the mouth with water and
expectorate after using the ICS (4).
E-Budesonide has the most safety data in humans and is the preferred ICS
during pregnancy (4).
3-Systemic corticosteroids
A-Prednisone, prednisolone, and methylprednisolone are systemic
corticosteroids. These medications are the cornerstone of treatment for acute
asthma and COPD exacerbations not responding to an inhaled SABA (4).
B-Because of serious potential adverse effects, systemic corticosteroids are
avoided as long-term controller medication for asthma, if possible. If

46
systemic therapy is necessary, once-daily or every-other-day therapy is used
(4)
.
C-Chronic systemic corticosteroids should be avoided in COPD
management because of questionable benefits and high risk of toxicity (6).
4-Combination of inhaled corticosteroids and long-acting bronchodilators:
Combination products of ICS and LABAs (ICS/LABA) have been developed.
Fluticasone / salmeterol and mometasone/ formoterol are given on a regular BID
schedule. Budesonide/ formoterol can be used for as needed reliever therapy in
mild asthma; in moderate to severe asthma, it can be used for both
maintenance/controller therapy (regular BID schedule) and as-needed (reliever)
therapy (7).
Inhaled Corticosteroids (including combination products)
Scientific name Trade names Dosage form
1

Any extra notes:

4.2.3- Antimuscarinic:
1-The drug class appears to produce bronchodilation by blocking acetylcholine
at muscarinic receptors, therefore, blocking the direct constrictor effects of
acetylcholine on bronchial smooth muscle (3).
2-Two antimuscarinic medications are available: ipratropium bromide [a short -
acting muscarinic receptor antagonist (SAMA)] and tiotropium bromide [a long-
acting muscarinic receptor antagonist (LAMA)] (1, 4).
3-Ipratropium is a short-acting agent used during acute asthma and COPD
exacerbations but in combination with short-acting beta-adrenergic agonists.
Ipratropium may also be used as a short-acting rescue inhaler in patients with
COPD (3).
4-Tiotropium bromide is a long-acting inhaled antimuscarinic available in a DPI
and Respimat. It is use as a long-term maintenance treatment for patients with
asthma and COPD (1, 3).
47
Inhaled Antimuscarinics (including combination products)
Scientific name Trade names Dosage form
1

Any extra notes:

4.2.4-Leukotriene receptor antagonists (LTRAs) (Leukotriene Modifiers):


1-The available drugs are (zileuton, montelukast and zafirlukast) (4). They are
indicated for asthma prophylaxis. In addition, montelukast is used for symptomatic
relief of seasonal allergic rhinitis in patients with asthma (1).
2-Although these agents offer the convenience of oral administration, they are
significantly less effective than low ICS doses (4).
3-They are not used to treat acute asthma exacerbations and must be taken on a
regular basis, even during symptom-free periods (5).
4-Montelukast is given once daily in the evening (1).
A-The chewable tablet is taken on an empty stomach. This means an hour
before food or 2 hours after food (1).
B-Granules may be swallowed or mixed with cold, soft food (not liquid) and
taken immediately (1).
5-Zileuton and zafirlukast are less commonly used because of the risk of
hepatotoxicity (4).
Leukotriene Receptor Antagonists
Scientific name Trade names Dosage form
1

Any extra notes:

48
4.2.5-Methylxanthines:
1-Theophylline causes bronchodilation. Its use is limited because of lower
efficacy, a narrow therapeutic index (high risk of severe life-threatening toxicity),
and multiple clinically important drug interactions (4, 5).
2-Methylxanthines must be taken systemically (orally or IV). Modified release
preparations are more commonly used as they reduce adverse effects and the need
for frequent dosing (8). Theophylline is given by slow I.V infusion as
aminophylline (due to increased solubility) for severe acute asthma or severe acute
exacerbation of COPD (1).
3-Phyllocontin Continus ® Forte tablets are for smokers and other patients where
theophylline half-life is shorter (1).
4-For intravenous injection, give very slowly over at least 20 minutes (1).
5-Modified-release theophylline tablet should be taken with or just after food (1).
Methylxanthines
Scientific name Trade names Dosage form
1

Any extra notes:

4.2.6-Mast cell stabilizers:


1-Sodium cromoglicate (mast cell stabilizer) (by inhalation) is indicated for
prophylaxis of asthma (1).
2-Other uses: sodium cromoglicate and nedocromil sodium may also have a role
in allergic conjunctivitis; sodium cromoglicate is used also in allergic rhinitis (1).
Mast cell stabilizers
Scientific name Trade names Dosage form
1

Any extra notes:

49
4.3-Antihistamines
1-All antihistamines are of potential value in the treatment of nasal allergies,
particularly seasonal allergic rhinitis (hayfever). They reduce rhinorrhoea and
sneezing but are usually less effective for nasal congestion (1).
2-Antihistamines are also used topically in the eye, in the nose, and on the skin (1).
3-Oral antihistamines are also of some value in preventing urticaria and are used
to treat urticarial rashes, pruritus, and insect bites and stings; they are also used
in drug allergies (1).
4-Injections of antihistamines are used as an adjunct to adrenaline/epinephrine in
the emergency treatment of anaphylaxis and angioedema (1).
5-Some antihistamines (including cinnarizine, cyclizine) may also have a role in
nausea and vomiting. Buclizine is included as an anti-emetic in a preparation for
migraine (1).
6-Antihistamines may also have a role in occasional insomnia (1).
7-The antihistamines may be classified into :
A-Sedating antihistamines: older antihistamines that are associated with
troublesome sedative and antimuscarinic effects. Example are (chlorphenamine
(chlorpheniarmine), clemastine, cyproheptadine, hydroxyzine, ketotifen,
diphenhydramine, and dimethindene maleate ). Drowsiness is a major problem
with the sedating antihistamines and those affected should not drive or operate
machinery (8). Drowsiness may diminish after a few days of treatment (1).
B-Non-sedating antihistamines: are newer antihistamines, they generally
cause little or no drowsiness (8). Example are (acrivastine, bilastine, cetirizine,
desloratadine, fexofenadine, levocetirizine , loratadine , mizolastine, and
rupatadine). [Although drowsiness is rare, nevertheless patients should be
advised that it can occur and may affect performance of skilled tasks (e.g.
cycling or driving); alcohol should be avoided. If drowsiness occurs, it may
diminish after a few days of treatment] (1).
8-Because of their antimuscarinic actions; the sedating antihistamines should be
used with care in conditions such as angle-closure glaucoma, urinary retention,
prostatic hyperplasia. Antimuscarinic adverse effects are not a significant
problem with the nonsedating antihistamines (8).
9-Antihistamines are more effective when taken 1 to 2 hours before anticipated
exposure to the offending allergen (5).
10-Important : Cyproheptadine has been widely used as an appetite stimulant,
but in the long-term appears to have little value in producing weight gain and such
use is no longer generally recommended (8).
11-Diphenhydramine has pronounced sedative properties and may be used as a
hypnotic in the short-term management of insomnia (taken before bedtime) (8).
51
Antihistamines
Scientific name Trade names Dosage form
1

10

Any extra notes:

4.4-Cough and cold preparations


Notes :
1-Children under 6 years should not be given OTC cough and cold medicines
containing the listed ingredients in (Table 4-2) (1).
Table 4-2: Over the counter cough and cold medicines for children (1)
1-Children under 6 years should not be given OTC cough and cold medicines
containing the following ingredients:
-Brompheniramine, chlorphenamine, diphenhydramine, doxylamine,
promethazine, or triprolidine (antihistamines);
-Dextromethorphan or pholcodine (cough suppressants);
-Guaifenesin (expectorants);
-Phenylephrine, pseudoephedrine, ephedrine, oxymetazoline, or xylometazoline
(decongestants).
2-Sympathomimetics (e.g. pseudoephedrine) can be effective in reducing the
symptoms of nasal congestion. Nasal decongestants work by constricting the
dilated blood vessels in the nasal mucosa. Sympathomimetics can cause
stimulation of the heart and an increase in blood pressure and may affect diabetic
51
control because they can increase blood glucose levels. They should be used with
caution in people with diabetes, those with heart disease or hypertension and
those with hyperthyroidism (9).
4.4.1-Cough suppressants (Antitussive):
1-Codeine, pholcodeine and dextromethorphan are used for dry cough.
Although all three may be effective, dextromethorphan and pholcodeine have a
lower risk of constipation and dependence developing. In addition, both
pholcodeine and codeine can cause drowsiness whereas dextromethorphan is non-
sedating in most people (10).
2-The FDA recommended that the use of codeine-containing cough medicines
should be contraindicated in children younger than 18 years (11).
3-Side effects: even at OTC doses codeine can cause constipation and at high
doses, respiratory depression (9). Patients with impaired respiratory reserve (e.g.,
asthma or COPD) or preexisting respiratory depression, drug addicts, and
individuals who take other respiratory depressants or sedatives, including alcohol,
should use codeine with caution (12).
4-Codeine is well known as a drug, which is misused, and many pharmacists
choose not to recommend it (9).
5-Generally dextromethorphan is considered non-sedating and has fewer side
effects and thought to have a low potential for abuse (13).
6-Sedating antihistamines are used as the cough suppressant component of many
compound cough preparations on sale to the public; all tend to cause drowsiness
which may reflect their main mode of action (1).
4.4.2-Expectorants and mucolytics
1-Expectorants are claimed to promote expulsion of bronchial secretions, but
there is no evidence that any drug can specifically facilitate expectoration (9).
2-Expectorants and mucolytics are used for wet cough. Expectorants are claimed
to promote expulsion of bronchial secretions, but there is no evidence that any drug
can specifically facilitate expectoration (9). Examples of expectorant is glyceryl
guaiacolate (also called Guaifenesin) and examples of is Mucolytics is
bromohexine.
4.4.3-Lozenges (Demulcents)
1-Nonmedicated lozenges may reduce cough by decreasing throat irritation (12).
They may contain ingredients such as honey and lemon, or glycerol. They are
thought to coat the pharyngeal mucosa, soothing inflammation and reducing
irritation, and can be used to treat both productive and non-productive coughs
(10)
.
2-Demulcents provide a safe alternative for at-risk patient groups, such as older
adults, pregnant women, young children and those taking multiple medications (14).

52
3-They are considered to be safe in children and pregnant women (9) but should
not be given to children under three years of age because of the risk of choking
(10)
. If recommended they should be given 3-4 times daily (14).
Cough preparations
Scientific name Trade names Dosage form
1

Any extra notes:

4.5-Orally administered nasal decongestants


1-Sympathomimetics (e.g. pseudoephedrine) can be effective in reducing the
symptoms of nasal congestion (9).
2-Oral decongestants may be used short term to reduce nasal congestion alone or in
combination with an antihistamine (9).
Orally administered nasal decongestants
Scientific name Trade names Dosage form
1

53
Any extra notes:

References
1-BNF 81(2021).
2-ACCP Updates in Therapeutics® 2021: The Pharmacotherapy Preparatory
Review and Recertification Course.
3-Michael AM, Jason. Frequently prescribed medications. Third edition 2019.
4-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
5-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.
6-Roger Walker. Clinical Pharmacy and Therapeutics. Sixth edition 2019.
7-Canadian pharmacists association. Therapeutic choices. 2019.
8-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
9-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the
pharmacy . A guide to the managements of common illness. 8th edition. 2018.
10- Sarah Marshall . Over-the-counter advice for coughs. The Pharmaceutical
Journal (Vol 278) 20 January 2007 . page:85-88
11-The U.S. Food and Drug Administration (FDA). FDA Drug Safety
Communication: FDA requires labeling changes for prescription opioid cough and
cold medicines to limit their use to adults 18 years and older. 2018.
12-American pharmacists association. Handbook of Non-prescription drugs: An
Interactive Approach to Self-Care. 18th edition. 2016.
13-Nathan A. fasttrack. Managing Symptoms in the Pharmacy. Pharmaceutical
Press. 2008.
14-Paul Rutter. Community Pharmacy. Symptoms, Diagnosis and Treatment. 5th
edition. 2021.

54
Chapter Five : Central Nervous System (CNS)
Note: many of the CNS drugs (like antipsychotics, antidepressant,
antiepileptics, anxiolytics, hypnotics, opioid analgesics) can cause drowsiness,
thereby affecting the ability to drive and operate hazardous machinery and patients
should be warned about this.
5.1-Drugs for dementia
1-In dementia, there is a is a deterioration memory, judgement, language and
communication. Alzheimer’s disease is the most common cause of dementia
and accounts for over half of all patients; about one-third of dementia cases
are due to vascular disease (1).
2-Donepezil, galantamine, and rivastigmine are the main cholinesterase
inhibitors. All have produced modest improvement in patients with mild to
moderately severe disease (1). Acetylcholinesterase inhibitors can cause unwanted
cholinergic side-effects (2).
3-Memantine is a glutamate receptor antagonist; it is licensed for treating
moderate to severe Alzheimer‘s disease (2).
4-Rivastigmine and galantamine are given with or just after meal (2).
Drugs for dementia
Scientific name Trade names Dosage form
1

Any extra notes:

5.2-Epilepsy and other seizure disorders


1- How to administer first aid for seizures: Table 5-1(3).
Table 5-1:How to administer first aid for seizures (3).
• Move the person away from danger (fire, water, machinery, furniture)
• After convulsions cease, turn the person into the ‗recovery‘ position (semi-prone)
• Ensure the airway is clear but do NOT insert anything in the mouth (tongue-
biting occurs at seizure onset and cannot be prevented by observers)
• If convulsions continue for more than 5 minutes or recur without the person
regaining consciousness, summon urgent medical attention
• Do not leave the person alone until fully recovered (drowsiness and delirium
can persist for up to 1 hour)

55
2-Antiepileptic drug (AEDs) include : Brivaracetam, Carbamazepine,
Clonazepam, Eslicarbazepine, Ethosuximide, Ezogabine, Felbamate, Gabapentin,
Lacosamide, Lamotrigine, Levetiracetam, Oxcarbazepine, Perampanel,
Phenobarbital or Primidone, Phenytoin, Pregabalin, Rufinamide, Stiripentol,
Tiagabine, Topiramate, Valproate, Vigabatrin and Zonisamide (2, 4).
3-Adverse effects of AEDs (5).
A-Two types of adverse effects occur with AEDs: concentration -related and
idiosyncratic.
B-For many AEDs, common concentration-related adverse effects include
sedation, ataxia, and diplopia (If a patient has a job that requires mental
alertness, it is best to choose an AED that is less likely to cause sedation (e.g.,
lamotrigine, levetiracetam).
C-Idiosyncratic adverse effects will almost always result in the AED being
discontinued. Severe skin, hepatic, or hematological reactions occur rarely,
but are potentially life-threatening. The AED should be discontinued
immediately when these reactions occur.
D-Chronic Adverse Reactions : One chronic adverse effect that is of concern
is osteoporosis. Carbamazepine, phenytoin, phenobarbital , oxcarbazepine, and
valproate have all been shown to decrease bone mineral density, even after only
6 months of treatment. Patients taking these drugs for longer than 6 months
should take supplemental calcium and vitamin D.
4-Drug–drug interactions (4, 5).
AEDs are associated with many different drug interactions:
A-Phenobarbital, phenytoin, primidone, and carbamazepine are potent
inducers of various cytochrome P-450 (CYP450) isoenzymes, increasing the
clearance of other drugs metabolized through these pathways.
B-Valproic acid inhibits many hepatic enzyme systems and displaces some
drugs from plasma albumin.
5-Withdrawal of AEDs is done slowly (5).
6-Other uses: another indications for some AEDs are: neuropathic pain, migraine
prophylaxis, trigminal neuralgia, bipolar disorder, and anxiety disorder (2).
Antiepileptic drugs
Scientific name Trade names Dosage form
1

56
5

Any extra notes:

5.3-Hypnotics and anxiolytics


1-Hypnotics are used for patients with insomnia, while anxiolytics are used for
patients with anxiety (2).
2-Prescribing of these drugs is widespread but dependence and tolerance occur.
This may lead to difficulty in withdrawing the drug (2).
3-Benzodiazepines (e.g. alprazolam, diazepam, chlordiazepoxide, lorazepam) are
the most commonly used anxiolytics and hypnotics (2).
4-Short-acting hypnotics (e.g. loprazolam, lormetazepam, and temazepam) are
preferable in patients with sleep onset insomnia, when sedation the following day
is undesirable, or when prescribing for elderly patients (2).
5-Long-acting hypnotics (e.g. diazepam) are indicated in patients with poor sleep
maintenance (e.g. early morning waking) that causes daytime effects, when an
anxiolytic effect is needed during the day, or when sedation the following day is
acceptable (2).
6-Zaleplon, zolpidem, and zopiclone are non-benzodiazepine hypnotics (2).
7-Melatonin is a pineal hormone; it is licensed for the short-term treatment of
insomnia in adults over 55 years; and for the short-term treatment of jet-lag in
adults (2).
8-Benzodiazepine anxiolytics can be effective in alleviating anxiety states (2).
9-Beta-blockers do not affect psychological symptoms of anxiety, such as worry,
tension, and fear, but they do reduce autonomic symptoms, such as palpitation and
tremor (2).
10-Nonbenzodiazepine antianxiety agents for generalized anxiety disorder include
(4)
: antidepressants, anticonvulsant (pregabalin), and atypical antipsychotic
(quetiapine). Antidepressants are the drugs of choice for chronic generalized
anxiety disorder because of a tolerable side-effect profile; no risk for dependency
(5)
.
Hypnotics and anxiolytics
Scientific name Trade names Dosage form
1

57
2

Any extra notes:

5.4-Antipsychotic drugs (for treatment of schizophrenia)


1-Both first-generation antipsychotics (FGAs, also known as traditional) and
second-generation antipsychotics (SGAs, also known as atypical) are used to
treat schizophrenia (Table 5-2) (4).

Table 5-2: Antipsychotics (4)


First-generation Chlorpromazine , Fluphenazine , Haloperidol , Loxapine ,
Perphenazine, Thioridazine, Thiothixene, Trifluoperazine
Second- Aripiprazole , Asenapine , Brexpiprazole , Cariprazine ,
generation Clozapine, Iloperidone , Lurasidone , Olanzapine ,
Paliperidone , Quetiapine , Quetiapine XR , Risperidone ,
Ziprasidone
2-A large number of adverse effects are associated with antipsychotic medicines.
In general the frequent or troublesome side effects of the older first generation
antipsychotics include extrapyramidal side effects (EPSE), tardive dyskinesia
(TD), anticholinergic effects, cardiac effects and hypotension,
(6)
hyperprolactinaemia and sexual dysfunction .
3-In contrast, in general the frequent or troublesome side effects of the newer
second generation antipsychotics, including metabolic changes such as
diabetes, weight gain and sexual dysfunction, can affect adherence in many
patients (6).
4-Long-acting depot injections antipsychotic are used for maintenance therapy
especially when adherence with oral treatment is unreliable. Depot
antipsychotics are administered by deep intramuscular injection (2).

Antipsychotics (Both typical and atypical antipsychotics)


Scientific name Trade names Dosage form
1

58
4

Any extra notes:

5.5-Antidepressant drugs
1-Currently available classes of antidepressant medications are shown in (Table 5-
3) (3).
Table 5-3: Antidepressant drugs (2, 4, 5).
Class of Antidepressant Example(s)
1 Selective serotonin reuptake Citalopram, Escitalopram, Fluoxetine,
inhibitors (SSRIs) Fluvoxamine, Paroxetine, Sertraline
2 Tricyclic antidepressants Amitriptyline, Desipramine, Dosulepin ,
(TCAs) and tetracyclic Doxepin, Lofepramine, Imipramine,
antidepressants Nortriptyline, Mianserin (tetracyclic),
Trimipramine
3 Norepinephrine and dopamine Bupropion
reuptake inhibitor (NDRI)
4 Mixed serotonergic effects Nefazodone, Trazodone, Vilazodone,
(Mixed 5-HT) Vortioxetine
5 Serotonin and α2-adrenergic Mirtazapine
antagonist
6 Monoamine oxidase inhibitors Phenelzine, Selegiline, Tranylcypromine
(MAOIs)
7 Melatonin receptor agonist Agomelatine
8 Noradrenaline reuptake Reboxetine
inhibitors
9 Serotonin and noradrenaline Duloxetine, Venlafaxine, Desvenlafaxine
re-uptake inhibitors.
10 Others Tryptophan, Vortioxetine

2-There is little to choose between the different classes of antidepressant drugs in


terms of efficacy (2).
3-The use of antidepressants has been linked with suicidal thoughts and
behavior. Patients should be monitored for suicidal behavior, self-harm, or
hostility, particularly at the beginning of treatment or if the dose is changed (2).

59
5.5.1-Selective serotonin reuptake inhibitors
1-The SSRIs inhibit the reuptake of 5-HT into the presynaptic neuron. They are
generally chosen as first-line antidepressants because of their relative safety in
overdose and improved tolerability compared with earlier agents (4).
2-The primary adverse effects for SSRIs are nausea, vomiting, diarrhea,
headache, insomnia, fatigue, and sexual dysfunction and have a reduced
incidence of sedative, anticholinergic, and cardiovascular adverse effects or weight
gain (4).
3-Paroxetine is the most sedating of the SSRIs and usually requires dosing at
bedtime to improve tolerability (7).
4-In the treatment of depression the usual initial dose of fluoxetine is 20 mg once
daily; US product information recommends giving this dose in the morning (1).
5-Some SSRIs are also used as part of the management of generalised anxiety
disorder, obsessive-compulsive disorder, panic disorders, social phobia, and post-
traumatic stress disorder, and bulimia nervosa. Fluoxetine is also used in the
treatment of premenstrual syndrome (1).
5.5.2-Tricyclic antidepressants
1-Tricyclic antidepressant (TCA) use has diminished because of the availability
of equally effective therapies that are safer on overdose and better tolerated (2).
2-TCAs cause anticholinergic side effects (eg, dry mouth, blurred vision,
constipation, urinary retention, tachycardia, memory impairment, and delirium)
and sedation (2).
3-Additional adverse effects include weight gain, orthostatic hypotension, cardiac
conduction delay, and sexual dysfunction (2).
4-Some TCAs are used for treatment of neuropathic pain, migraine
prophylaxis, treatment of anxiety disorders and in nocturnal enuresis in
children (2, 8).
Antidepressant drugs
Scientific name Trade names Dosage form
1

61
7

10

11

12

Any extra notes:

5.6-Drugs used in parkinsonism


1-The primary objective of drug therapy is to enhance dopaminergic activity
within the damaged areas of the basal ganglia, and this is achieved in various
ways (Table 5-4) (9).
Table 5-4: Drugs used in parkinsonism (9).

61
2-Regarding Levodopa and Carbidopa/Levodopa:
A-L-dopa, is the most effective drug available. Ultimately, all Parkinson
disease (PD) patients will require L-dopa (4).
B-The immediate response to levodopa is often dramatic, but the long-term
use is limited by the development of motor fluctuations. The most common
of these is the wearing-off effect (11).
C-Wearing off occurs when patients experience recurrence of symptoms
before the next dose of medication (11). Possible options to solve such problem
include (5): Carbidopa/L-dopa needs to be given more frequently or the
addition of the COMT inhibitor entacapone or the MAO-B inhibitor
rasagiline or a dopamine agonist (e.g., pramipexole, ropinirole), add or
switch to extended-release carbidopa/levodopa (4).
D-Another complication of L-dopa therapy is dyskinesia [an involuntary
choreiform movements (too much movement )involving the neck, trunk, and
extremities (lower/upper)]. Possible options to solve such problem include:
The use of lower individual doses of L-dopa (with an increase in dosage
frequency) or addition of amantadine (4).
3-Regarding dopamine agonists:
The ergot derivative (bromocriptine, pergolide, cabergoline) and the nonergots
(safer) pramipexole , rotigotine , and ropinirole are beneficial adjuncts in
patients with limited clinical response to L-dopa 4).

4-Regarding Catechol-O-Methyltransferase (COMT) Inhibitors:


A-Tolcapone, entacapone and opicapone are used only in conjunction with
carbidopa/L-dopa. Thus, ―on‖ time is increased (2, 4).
B-Tolcapone can cause hepatotoxicity. Hpatotoxicity is not reported with
entacapone (4).
C-Entacapone may discolor the urine (2).
5-Regarding Monoamine Oxidase Type-B (MAO-B) Inhibitors
A-Selegiline is a first-generation MAO-B inhibitor. Selegiline is metabolized
to the amphetamine derivatives, which have been implicated in producing
side effects such as insomnia and vivid dreaming (12). So it is not given in the
evening because excess stimulation from metabolites can cause insomnia.
The orally disintegrating tablet formulation dissolves in the mouth on contact
with saliva and undergoes pregastric absorption (this minimizes the effect of
first-pass and reduces the production of amphetamine-based metabolites)
(13)
.
B-Rasagiline is a second-generation selective inhibitor of MAO-B. It is more
potent inhibitor of MAO-B than selegiline, and it is not metabolized into
amphetamine-based metabolites (13).

62
6-Regarding anticholinergic medications:
A-Anticholinergics [e.g. procyclidine, and trihexyphenidyl (benzhexol)] are
more helpful in alleviating tremor and rigidity than bradykinesia. However,
these medications are often poorly tolerated, especially in older adults (14).
B-Their use is mostly restricted to patients with tremor that is intractable to
levodopa treatment (10).
7-Regarding amantadine:
A-Amantadine has been found to have antidyskinesia effects, the finding has
shifted its use from use as monotherapy in early disease to that of an adjunctive
agent in managing levodopa-induced dyskinesias (12, 13).
B-It is also used for post-herpetic neuralgia (2).
Antiparkinsonian drugs
Scientific name Trade names Dosage form
1

Any extra notes:

5.7-Analgesics
5.7.1-Non-steroidal anti-inflammatory drugs (NSAIDs).
See chapter ten.
5.7.2-Paracetamol
1-Paracetamol has analgesic and antipyretic effects but no anti-inflammatory
effect (2).
2-Over-dosage with paracetamol is particularly dangerous as it may cause
hepatic damage (2).
3-Patient should be advised not to take more than 1g (usually 2 tablet of 500 mg)
at any one time. And not take more than 8 tablets (4 gm) in 24 hours (2).
4-Compound analgesic preparations containing paracetamol with a low dose of
an opioid analgesic (e.g. 8 mg of codeine phosphate per compound tablet) are
commonly used, but the advantages have not been substantiated. The low dose of
the opioid may be enough to cause opioid side-effects (in particular, constipation)
63
and can complicate the treatment of overdosage yet may not provide significant
additional relief of pain (2).

5-Rectal administration results in erratic absorption (15).


Paracetamol (Including compound analgesic preparations)
Scientific name Trade names Dosage form
1

Any extra notes:

5.7.3-Opioid analgesics
1-Opioid analgesics are usually used to relieve moderate to severe pain. Repeated
administration may cause dependence and tolerance (2).
2-Opioids such as codeine or dextropropoxyphene are used in the treatment of less
severe pain, and are often combined with non-opioid analgesics such as aspirin,
other NSAIDs, or paracetamol (1).
3-More potent opioids such as morphine are used in severe acute and chronic
pain, including cancer pain (1).
4-Tramadol has fewer of the typical opioid side-effects (notably, less respiratory
depression, less constipation and less addiction potential (2).
(Note: However, tramadol is abused by some Iraqi addicts).
5-The most common side-effects include nausea and vomiting (particularly in
initial stages), and constipation (2).
6-Opioids should be used with caution in patients with impaired respiratory
function (avoid in chronic obstructive pulmonary disease) and asthma (avoid
during an acute attack) (2).

Opioid analgesics
Scientific name Trade names Dosage form
1

64
2

Any extra notes:

5.7.4-Non-opioid, centrally acting nalgesics


Nefopam may have a place in the relief of persistent pain unresponsive to other
non-opioid analgesics. It causes little or no respiratory depression, but
sympathomimetic and antimuscarinic side-effects may be troublesome (2).
5.7.5-Neuropathic pain
1-Neuropathic pain, occurs as a result of damage to neural tissue (2).
2-Neuropathic pain is generally managed with a tricyclic antidepressant (e.g.
amitriptyline ) or with certain antiepileptic drugs (carbamazepine, gabapentin,
and pregabalin) (2).
3-Neuropathic pain may respond to opioid analgesics (2).
4-Capsaicin (topical) is licensed for neuropathic pain (but the intense burning
sensation during initial treatment may limit use) (2).
5.7.6-Antimigraine drugs
5.7.6.1-Treatment of acute migraine
1-Analgesics, such as aspirin, nonsteroidal anti-inflammatory drugs (NSAIDs),
acetaminophen, and combination products containing caffeine, with or without an
opioid, are the initial pharmacologic option for the acute management of
migraine headache especially when severity is mild to moderate (5).
2-If these analgesics prove to be ineffective, and when headaches are severe, then
migraine-specific medications, such as triptans (5) (like almotriptan, eletriptan,
frovatriptan, naratriptan, rizatriptan, sumatriptan, and zolmitriptan) (2), are
administered (5).
3-Larger doses of oral medications may be necessary for pain relief, due to the
enteric stasis and poor drug absorption accompanying migraine attacks (5).
4-Intranasal, parenteral, and rectal administration can circumvent this
complication (5).
5-The timing of doses is important in migraine where the analgesic should be
taken at the first sign of an attack, preferably in soluble form, since
gastrointestinal (GI) motility is slowed during an attack and absorption of
analgesics delayed (16).
6-Metoclopramide or prochlorperazine can be given orally or by injection to
relieve nausea or vomiting. Domperidone [unlicensed in those weighing less
65
than 35 kg] may be used as an alternative antiemetic (2). An antiemetic given 15 to
30 minutes prior to an oral migraine medication limits nausea and vomiting and
improves absorption of migraine medication (7).
7-Ergot derivatives, including ergotamine tartrate and dihydroergotamine, are
migraine-specific medications used for moderate to severe migraine headaches (7).
(2)
8-Triptans and ergotamine are contra-indicated in ischemic heart disease .
Do not use ergotamine derivatives and triptans within 24 hours of each other (4).
Note: Very important: The maximum recommended doses of ergotamine
preparations should not be exceeded (should not exceed the maximum dose per
attack, the maximum dose per day as well as the maximum dose per week).
Triptans and ergotamine
Scientific name Trade names Dosage form
1

Any extra notes:

5.7.6.2-Prophylaxis of migraine
1-Migraine headaches that are severe, frequent, or lead to significant disability
require long-term medication therapy (5).
2-Drugs that are used for prophylaxis of migraine include:
A-The beta-blockers (e.g. propranolol is recommended as first line preventative
treatment) (2).
B-Tricyclic antidepressants (amitriptyline), and antiepileptics (topiramate,
sodium valproate) are also effective for preventing migraine (2).
C-Flunarizine, candesartan cilexetil and pizotifen (2).
D-Botulinum toxin type A (2).
E-Erenumab, fremanezumab, and galcanezumab are monoclonal antibodies
preventing migraine attacks (2).

66
Prophylaxis of migraine
Scientific name Trade names Dosage form
1

Any extra notes:

5.8-Drugs for vertigo and tinnitus


Betahistine is an analogue of histamine licensed for vertigo, tinnitus, and hearing
loss associated with Ménière's disease. Antihistamines (such as cinnarizine), and
phenothiazines (such as prochlorperazine) are also used (2).
Scientific name Trade names Dosage form

Any extra notes:

5.9-Drugs for mania and hypomania


1-Antipsychotic drugs (normally olanzapine, quetiapine , or risperidone) are
useful in acute episodes of mania and hypomania; if the response to antipsychotic
drugs is inadequate, lithium or valproate may be added (2).
2-Lithium salts are used in the prophylaxis and treatment of mania, hypomania
and depression in bipolar disorder (manic-depressive disorder), and in the
prophylaxis and treatment of recurrent unipolar depression (2).
3-Valproate is used for the treatment of manic episodes associated with bipolar
disorder. Carbamazepine may be used for the prophylaxis of bipolar disorder
(manic-depressive disorder) in patients unresponsive to a combination of other
prophylactic drugs (2).
Drugs mania and hypomania
Scientific name Trade names Dosage form
1

67
Any extra notes:

5.10-Dugs used for nicotine dependence


1-Drugs used for nicotine dependence are summarized in (Table 5-5) (2).
Table 5-5: Drugs used for nicotine (2).
Bupropion (oral tablet) , and varenicline (oral tablet) Nicotine replacement
therapy (gum, lozenges, patches, nasal spray, inhalator, sublingual tablets,
mouth (oral) spray, and orodispersible tablets).

2-For full description of NRT usage guideline, see (Community Pharmacy A


Guide to the Management of Minor Ailments. By Dr. Dheyaa Jabbar Kadhim)
Drugs used for nicotine
Scientific name Trade names Dosage form
1

Any extra notes:

References
1-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
2-BNF -81 (2021)
3-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.
4-Stuart HR, Ian DP, Mark WJ, et al, eds. Davidson‘s Principles and Practice of
Medicine. 23th edition; 2018.
5-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
6-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
7-Roger Walker. Clinical Pharmacy and Therapeutics. Sixth edition 2019.
8-NAPLEX® Review Guide, Fourth Edition. Copyright © 2021 by McGraw-Hill.
9-ACCP Updates in Therapeutics® 2021: The Pharmacotherapy Preparatory
Review and Recertification Course.
10-Russell J Greene, Norman D Harris . Pathology and Therapeutics for
Pharmacists : A basis for clinical pharmacy practice third edition . 2008 by
pharmaceutical press.
11-Edward T. Bope, et al, eds. Conn‘s Current Therapy. Copyright 2018.
68
12-Michele A. Faulkner. Early Versus Delayed Diagnosis and Treatment of
Parkinson‘s Disease: What You Need To Know . Us pharmacist. December, 2008.
13-David J Quan, Richard A Helms. Textbook of Therapeutics: Drug and Disease
Management. 8th edition.
14-Maxine A. Papadakis, et al, eds. Current Medical Diagnosis & Treatment, 58th
Edition 2019.
15-Canadian Pharmacist Association. Compendium of Therapeutics For Minor
Ailments (CTMA ).2018.
16-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the
pharmacy . A guide to the managements of common illness. 8th edition. 2018

69
Chapter Six : Infections
6.1-Antibacterials
6.1.1-Aminoglycosides
1-These include amikacin, gentamicin, neomycin, streptomycin, and tobramycin
(1)
.
2-All are bactericidal and active against some Gram-positive and many Gram-
negative organisms. Tobramycin has similar activity to gentamicin. It is slightly
more active against Ps. aeruginosa (1).
3-Amikacin is more stable than gentamicin to enzyme inactivation. Amikacin is
used in the treatment of serious infections caused by gentamicin-resistant Gram-
negative bacilli (1).
4-The aminoglycosides are not absorbed from the gut and must therefore be
given by injection for systemic infections (1). Neomycin sulfate may be given
orally to reduce the bacterial population of the colon prior to bowel surgery or in
hepatic failure (1).
5-The important side-effects are ototoxicity, and nephrotoxicity (1).
6-Streptomycin is used mainly for tuberculosis (2nd line drug) and for brucellosis
and endocarditis (1).
7-Monitoring requirements (1).
 Serum concentration monitoring.
 Renal function should be assessed before starting an aminoglycoside and
during treatment.
 Auditory and vestibular function should also be monitored during treatment.
Aminoglycosides
Scientific name Trade names Dosage form
1

Any extra notes:

6.1.2-Carbapenems
1-These include imipenem (with cilastatin), ertapenem and meropenem (1).

71
2-The carbapenems are beta-lactam antibacterials with a broad-spectrum of
activity which includes many Gram-positive and Gram-negative bacteria, and
anaerobes. Unlike the other carbapenems, ertapenem is not active against
Pseudomonas (1).
3-Imipenem is partially inactivated by enzymatic activity and is therefore
administered in combination with cilastatin, a specific enzyme inhibitor (1).
4-Meropenem has less seizure-inducing potential and can be used to treat central
nervous system infection (1).
5-Some products contain combination of carbapenems with vaborbactam or
relebactam (beta-lactamase inhibitors) (1).
Carbapenems
Scientific name Trade names Dosage form
1

Any extra notes:

6.1.3-Cephalosporins
Cephalosporins are antibacterials that cause bacterial cell lysis and death (1).
1-Classification (Table 6-1) (1, 2)

Table 6-1: Cephalosporins (1, 2)


Groups Examples
1 First-generation Cefalexin and cefadroxil
2 Second -generation Cefuroxime
3 Third-generation Cefotaxime, ceftazidime ceftriaxone,
cefixime, cefpodoxime
4 Fourth-generation Cefepime
5 Fifth generation [Anti- methicillin Ceftaroline
resistant Staphylococcus aureus
(MRSA) cephalosporin)
2-They have more broad-spectrum antimicrobial activity than penicillins,
activity that broadens in spectrum when moving from first- to fourth-generation
agents (2). In general the activity against gram negative bacteria is increase and the
activity against gram positive bacteria is decrease when we move from first to third
generations cephalosporins (3).
3-Some important properties for specific agents (Table 6-2):
71
Table 6-2: Properties for specific cephalosporins
Drug Properties
Ceftriaxone Has a longer half-life (may be given once daily) (1).
Ceftazidime Has good activity against pseudomonas (1).
Cefixime Oral third-generation cephalosporin (1).
Cefpodoxime Oral third-generation cephalosporin (administer tablets with
food; suspension may be administered without regard to food)
(4)
.
4-The principal side-effect of the cephalosporins is hypersensitivity and about
0.5–6.5% of penicillin-sensitive patients will also be allergic to the cephalosporins.
Patients with a history of immediate hypersensitivity to penicillin should not
receive a cephalosporin (contraindicated) (1).
5-Note: Arrhythmias following rapid injection are reported (1).
6-Important:
A-Ceftriaxone is incompatible with Ca-containing solutions, e.g. Hartmann‘s,
Ringer‘s. Fatalities have occurred in neonates and infants due to precipitates
forming in lungs and kidneys (5).
B-Ceftriaxone should not to be given simultaneously with infusion fluids
containing Ca, even by different infusion lines. May be infused sequentially (1)
(EXCEPT in neonate (4)) with infusion fluids containing Ca if flush with NaCl
0.9% between infusions or give infusions by different infusion lines at different
sites (1).
7-Some products contain combination of cephalosporins with tazobactam or
avibactam (beta-lactamase inhibitors) (1).

Cephalosporins
Scientific name Trade names Dosage form
1

Any extra notes:

72
6.1.4-Glycopeptide antibiotic
1-The glycopeptides teicoplanin, telavancin and vancomycin have bactericidal
activity against aerobic and anaerobic Gram-positive bacteria including multi-
resistant staphylococci (1).
2-Teicoplanin is similar to vancomycin, but has a significantly longer duration of
action, allowing once daily administration and is associated with a lower
incidence of nephrotoxicity than vancomycin (1).
3-Injection of (teicoplanin and vancomycin) can be used to prepare solution for
oral administration (for Clostridium difficile infection) (1).
4-Vancomycin is typically administered by slow IV infusion. More rapid infusion
rates can cause the red man syndrome (rash, flushing, tachycardia, hypotension)
If red man syndrome occurs, it may be ameliorated by slowing the rate of infusion
(2)
.
Glycopeptide
Scientific name Trade names Dosage form
1

Any extra notes:

6.1.5-Lincosamides (lincomycin and clindamycin)


1-Active against Gram-positive cocci, and also against many anaerobes (1). The
main indication for the use of lincosamides is now in the treatment of severe
anaerobic infections (3).
2-Clindamycin is much better absorbed from the GIT than lincomycin. They
both penetrate well into bone and have been used successfully in osteomyelitis (3).
3-The capsules of clindamycin should be taken with a glass of water (3).
4-They have also been used topically in the treatment of acne vulgaris (3).
5-Important: Patients and their carers should be advised to discontinue and
contact a doctor immediately if severe, prolonged or bloody diarrhea develops. (1)
(Lincosamides are reported to produce diarrhea. In some patients severe
antibiotic-associated or pseudomembranous colitis may develop during therapy or
up to several weeks afterwards) (3).

Lincosamides
Scientific name Trade names Dosage form
1

73
2

Any extra notes:

6.1.6-Macrolides
1-These include erythromycin, azithromycin and clarithromycin (1).
2-This class of antibiotics has activity against gram-positive cocci, including
streptococci and staphylococci, and some upper respiratory gram-negative
bacteria, but minimal activity against enteric gram-negative rods (6).
3-Azithromycin has a long half-life and once daily dosage is recommended (1).
4-Important : Azithromycin capsules must be given on an empty stomach (an
hour before food or 2 hours after food) while azithromycin tablet and
suspension are given without regard to meal (1).
5-Clarithromycin is usually given twice daily. And it is one of the component of
triple therapy for eradication of H. pylori (a bacteria that cause ulcer) (1).
6-Spiramycin is also a macrolide which is used for the treatment of toxoplasmosis
(1)
.
Macrolides
Scientific name Trade names Dosage form
1

Any extra notes:

6.1.7-Monobactam
Aztreonam is monobactam antibiotic with an antibacterial spectrum limited to
Gram-negative aerobic bacteria including Pseudomonas aeruginosa, Neisseria
meningitidis, and Haemophilus influenzae (1).
Scientific name Trade names Dosage form

Any extra notes:

74
6.1.8-Metronidazole and tinidazole
1-They are active against anaerobic bacteria and protozoa (Entamoeba
histolytica, giardia lamblia). Tinidazole is similar to metronidazole but has a
longer duration of action (1, 3).
2-Metronidazole and tinidazole tablets are taken with or after food (1).
3-Tinidazole may be given at a dose of 2 g (4 tablets) for some vaginal and GIT
infections (3).
4-They can produce nausea and an unpleasant metallic taste (3).
5-When given with alcohol, metronidazole and tinidazole may provoke a
disulfiram-like reaction in some patients (3).
Scientific name Trade names Dosage form
1

Any extra notes:

6.1.9-Penicillins
The penicillins are bactericidal and act by interfering with bacterial cell wall
synthesis (1).
1-Classification of penicillins (Table 6-3) (1).
Table 6-3: Classification of penicillins
Penicillin groups Examples
1 Natural penicillins Benzylpenicillin and phenoxymethylpenicillin
2 Penicillinase-resistant Flucloxacillin, Temocillin
penicillins
3 Broad-spectrum Amoxixillin, ampicillin
penicillins
4 Antipseudomonal Piperacillin (combined with the beta-lactamase
penicillins inhibitor tazobactam), Ticarcillin (combined with
the beta-lactamase inhibitor clavulanic acid)
2-Ampicillin and amoxicillin are active against certain gram-positive and gram-
negative organisms but are inactivated by penicillinases (1).
3-Both piperacillin and ticarcillin have a broad spectrum of activity against a
range of Gram-positive and Gram-negative bacteria, and anaerobes. High doses
may lead to hypernatremia (owing to sodium content of preparations) (1).

75
4-Co-amoxiclav consists of amoxicillin with the beta-lactamase inhibitor
clavulanic acid. Clavulanic acid inactivates beta-lactamases, making the
combination active against beta-lactamase-producing bacteria that are resistant to
amoxicillin (1).
5-Various combinations between amoxicillin and clavulanic acid are presents
(Table 6-4):
Table 6-4: Amoxicillin-Clavulanic acid combinations
Combinations Dosage form Notes
156 ( 125 +31) suspension
312 ( 250 + 62) suspension
457( 400 + 57) suspension Given twice daily(every 12 hours)
375 ( 250 + 125) Tablet
625( 500 + 125) Tablet
1000 ( 875 +125) Tablet Given twice daily(every 12 hours)
600 (500 + 100) Injection For intravenous injection only
1200 (1000 + 200) Injection For intravenous injection only
6-The most important side-effect of the penicillins is hypersensitivity which
causes rashes and anaphylaxis and can be fatal (1).
7-Ampicillin, and flucloxacillin must be given on an empty stomach (this
means an hour before food or 2 hours after food) while amoxicillin may be
taken without regard to meal (1).
8-For the eradication of H. pylori (a bacteria that cause ulcer), amoxicillin is given
in combination with other drugs; usual doses of amoxicillin for the eradication
of H. pylori is 1 g twice daily (1).
9-Benzathine penicillin G is indicated for prophylaxis of rheumatic fever. It is
given by deep intramuscular injection every 3–4 weeks. (1).
Penicillins
Scientific name Trade names Dosage form
1

Any extra notes:

76
6.1.10-Quinolones
1-These include Nalidixic acid, Delafloxacin, Ciprofloxacin, Gatifloxacin,
Ofloxacin, Levofloxacin, Moxifloxacin (1, 3).
2-Nalidixic acid: Because bactericidal concentrations can only be achieved in
urine its use has generally been limited to the treatment of urinary-tract
infections. (3).
3-Ciprofloxacin is active against both Gram-positive and Gram-negative bacteria.
It is particularly active against Gram-negative bacteria. Ciprofloxacin can be
used for infections like respiratory tract infections (but not for pneumococcal
pneumonia), urinary-tract infections, and infections of the gastro-intestinal system
(including typhoid fever) (1).
4-Respiratory fluoroquinolones: Levofloxacin, moxifloxacin, and gemifloxacin
have improved coverage of streptococci but generally less gram-negative activity
than ciprofloxacin (except levofloxacin, which does cover P. aeruginosa) (6).
5-Quinolones cause arthropathy in the weight-bearing joints of immature
animals and are therefore generally not recommended in children and growing
adolescents. However, the significance of this effect in humans is uncertain and in
some specific circumstances short-term use of ciprofloxacin may be justified
in children (7).
6-Nalidixic acid should be avoided in infants less than 3 months old (3).
7-Administration: Ciprofloxacin should not be taken with dairy products
(interfere with the absorption) (1).
8-Driving and skilled tasks: Quinolones may impair performance of skilled tasks
(e.g. driving) (1).
9-Quinolones cause acute haemolytic anaemia when taken by individuals with
Glucose 6-phosphate dehydrogenase (G6PD) deficiency (1).
10-Concomitant administration with aluminum- or magnesium-containing
antacids, oral iron, oral calcium, and oral zinc preparations can markedly
impair absorption of all orally administered fluoroquinolones (6).

Quinolones
Scientific name Trade names Dosage form
1

77
5

Any extra notes:

6.1.11-Sulfonamides and trimethoprim


1-Sulfamethoxazole and trimethoprim are used in combination (as co-
trimoxazole) because of their synergistic activity (1). Trimethoprim is also used
alone particularly in the treatment of infections of the urinary and respiratory tracts
(3)
.
2-It is commonly used for treating sinusitis, otitis media, bronchitis, prostatitis, and
UTIs (6).
3-Co-trimoxazole should not generally be given to infants below 6 weeks of age
because of the risk of kernicterus. Co-trimoxazole should be avoided by people
with G6PD deficiency (3).
4-All patients should be asked whether they are allergic to "sulfa drugs" (6).
Scientific name Trade names Dosage form
1

Any extra notes:

6.1.12-Tetracyclines (like Tetracycline, and Doxycycline)


1-Tetracyclines all have a broad spectrum of activity which includes Gram-positive
and Gram-negative bacteria, chlamydias, rickettsias, mycoplasmas, spirochaetes,
and some mycobacteria, and some protozoa (3).
2-Doxycycline has longer duration than tetracycline and may be given once or
twice daily (1).
3-Important : Oral administration:
A-Tetracycline must be given on an empty stomach (this means an hour
before food or 2 hours after food) (1).
B-Capsules (of tetracycline, and doxycycline) should be swallowed whole with
plenty of fluid while sitting or standing (1) (because it may cause oesophageal
irritation).
4-Gastrointestinal disturbances are common and other important toxic effects
include deposition in bones and teeth, precluding their use in pregnancy (2), breast-
78
feeding (1) and young children; and photosensitivity, especially with
demeclocycline (3).
5-They may cause photosensitivity: Patients should be advised to avoid exposure
to sunlight or sun lamps (1).
6-Di- and trivalent cations: Greatly decrease absorption of tetracyclines (2).
Tetracyclines
Scientific name Trade names Dosage form
1

Any extra notes:

6.1.13-Antituberculosis drugs
1-First-line agents form the core of initial regimens for the treatment of TB.
Currently, isoniazid, rifampicin (rifampin), pyrazinamide, and ethambutol are
considered first-line agents. In specific situations, rifabutin and rifapentine may be
considered first-line agents (8).
2-Treatment of active TB : The standard treatment of active tuberculosis is
completed in two phases—an initial phase using four drugs (isoniazid, rifampin,
pyrazinamide, and ethambutol for 2 months) and a continuation phase using two
drugs (isoniazid and rifampin for 4 months) (1, 9).
3-Multidrug resistant tuberculosis (MDR-TB), caused by strains resistant to both
isoniazid and rifampicin, requires a combination of first- and second -line drugs for
at least 1 8 to 24 months (3).
4-The second -line drugs are generally less effective and more toxic than
standard therapy and need be taken daily. They include injectable drugs such
as aminoglycosides (amikacin and kanamycin), polypeptide capreomycin, as well
as further oral drugs such as the fluoroquinolones (levofloxacin, moxifloxacin,
and ofloxacin) (3).
5-Isoniazid is the preferred drug for treating latent TB infection. Generally,
isoniazid alone is given for 9 months. Rifampin for 4 months can be used when
isoniazid resistance is suspected or when the patient cannot tolerate isoniazid (9).
6-INH antagonizes vitamin B6 metabolism and potentially can cause a
peripheral neuropathy. This can be avoided or minimized by coadministration of
pyridoxine, 25-50 mg PO daily, especially in the elderly, in pregnant women, and
in patients with diabetes, renal failure, alcoholism, and seizure disorders (6).

79
7-Rifampicin in combination with doxycycline is also used for brucellosis. It also
used for prevention of secondary case of meningococcal meningitis (used for 2
days) (1).
8-Isoniazid must be taken 30 to 60 minutes before food. Rifampicin is Taken on
an empty stomach (an hour before food or 2 hours after food) (1).
9-Important : Rifampicin causes a harmless orange-red discoloration of the
urine, faeces, sweat, saliva, sputum, tears, and other body fluids (3).
10-Ethambutol ocular toxicity (color blindness, loss of visual acuity, optic
neuritis) : The patients should be advised to discontinue therapy immediately if
they develop deterioration in vision and promptly seek further advice (1).
Antituberculosis drugs
Scientific name Trade names Dosage form
1

Any extra notes:

6.1.14-Other antibacterials (Table 6-5):


Table 6-5: Other antibacterials
Antibacterials comments
1-It is active against a range of Gram-positive and
Gram-negative (1).

1 Fosfomycin 2-A single 3 gm dose is used for acute uncomplicated


lower urinary-tract infections. It is also used for other
indications (Osteomyelitis, hospital-acquired lower
respiratory-tract infections, and Bacterial meningitis) (1).
Narrow spectrum antibiotics used for staphylococcal
2 Fusidic acid infections (1).

81
1-Nitrofurantoin is used in the treatment and
prophylaxis of urinary-tract infections (UTI) (3).
2-It is given orally, with food or milk (3).
8 Nitrofurantoin 3-Important: Prophylactic dose of antibiotic for UTI
usually given at bedtime (10).
4-Nitrofurantoin may cause a brownish discoloration
of the urine (3).
6.2-Antifungal drugs (systemic use)
1-Examples of systemic antifungal drugs are listed in (Table 6-6) (1).
Table 6-6: Systemic antifungal drugs (1).
Class Examples
1 Echinocandin Anidulafungin, Caspofungin, Micafungin,
antifungals
2 Polyene antifungals Amphotericin B, Nystatin.
3 Triazole antifungals Fluconazole, Isavuconazole, Itraconazole,
Posaconazole, Voriconazole
4 Others Flucytosine, Griseofulvin
2-Fluconazole 150 mg as a single oral dose may be used for vaginal candidiasis
and Candidal balanitis. While for recurrent vulvovaginal candidiasis: Initially
150 mg every 72 hours for 3 doses, then 150 mg once weekly for 6 months (1).
3-Itraconazole can be administered as intermittent ‗pulse’ therapy (1).
4-Concerning griseofulvin (important) :
A-Effective contraception required during and for at least 1 month after
administration to women. Also men should avoid fathering a child during
and for at least 6 months after administration (1).
B-Absorption of griseofulvin from the GIT is enhanced by reducing the particle
size or when given with a fatty meal (should be given with or after meals) (2).
C-Duration of therapy is dependent on the site of the infection and may
extend to a number of months (1) (2 to 8 weeks for infections of the hair and
skin, up to 6 months for infections of the fingernails, and 12 months or more for
infections of the toenails) (3).
D-It may impair performance of skilled tasks (e.g. driving) (1).
E-Griseofulvin use has been superseded by newer antifungals, particularly for
nail infections (1).
5-Nystatin is used for oral, oropharyngeal, and perioral infections by local
application in the mouth (1). And it may be given orally for the treatment of
intestinal candidiasis (3).
6-Itraconazole capsule must be given after food. While Oral solution is taken
on an empty stomach (an hour before food or 2 hours after food) (1).
81
Systemic antifungal drugs
Scientific name Trade names Dosage form
1

Any extra notes:

6.3-Anthelmintics
1-The most common anthelmintics drugs available in Iraq are mebendazole and
albendazole.
2-Other anthelmintics are ivermectin, levamisole, and praziquantel (1).
3-For the treatment of pinworms (Enterobius vermicularis):
A-Mebendazole is the drug of choice for treating threadworm infection in
patients of all ages over 6 months. It is given as a single dose of 100 mg; as
reinfection is very common, a second dose may be given after 2 weeks (1).
B-Albendazole may also be given as a single dose of 400 mg; as reinfection
is very common, a second dose may be given after 2 weeks (3, 10).
4-Mebendazole is effective against Ascaris lumbricoides and is generally
considered to be the drug of choice; the usual dose is 100 mg twice daily for 3
days (1).
Anthelmintics
Scientific name Trade names Dosage form
1

Any extra notes:

82
6.4-Antiprotozoal drugs
6.4.1-Amoebicides
1-Amoebicides [Metronidazole, Tinidazole (discussed previously)] and
Diloxanide furoate.
2-Metronidazole is the drug of choice for acute invasive amoebic dysentery.
Tinidazole is also effective. Treatment with metronidazole (or tinidazole) is
followed by a 10-day course of diloxanide furoate (1).
3-Diloxanide furoate is the drug of choice for asymptomatic patients with E.
histolytica cysts in the faeces; metronidazole and tinidazole are relatively
ineffective. The usual course is of 10 days (1).
4-For amoebic abscesses of the liver metronidazole is effective; tinidazole is an
alternative (1).
5-Flatulence is the most common adverse effect during treatment with diloxanide
furoate (3).
Scientific name Trade names Dosage form
1

Any extra notes:

6.4.2-Drugs for toxoplasmosis (Spiramycin)


1-Seropositive females infected 6 months before conception have no risk of fetal
transmission. (11). If toxoplasmosis is acquired in pregnancy, transplacental
infection may lead to severe disease in the fetus (1).
2-Spiramycin may reduce the risk of transmission of maternal infection to the
fetus (1). Spiramycin (3 g daily in divided doses) should be given until term (11).
Note: 1 g = 3,000,000 units.
Scientific name Trade names Dosage form

Any extra notes:

6.5-Antiviral drugs
6.5.1- Hepatitis
1-The most common types of viral hepatitis include hepatitis: A (HAV), B (HBV),
C (HCV), D (HDV), and E (HEV) (12).

83
2-Most persons with acute hepatitis (especially hepatitis A, B, and E) recover
spontaneously and do not require specific antiviral therapy (13).
3-Chronic Hepatitis B Treatment
A-The immune-mediating agents approved for HBV treatment are interferon
(IFN)-alfa and pegylated (peg) IFN-alfa. The nucleos(t)ide antiviral agents
lamivudine, telbivudine, adefovir, entecavir, and tenofovir diprovoxil and
tenofovir alafenamide are approved treatment options for chronic HBV (9).
B-Although pegIFN has lack of resistance, its disadvantages include the need
for subcutaneous injections and a pronounced adverse-effect profile that may
require dosage reductions or treatment discontinuation (12).
C-Entecavir and tenofovir are potent antivirals with a high barrier to genetic
resistance, and so are the most appropriate first-line agent (11).
D-Adefovir, lamivudine, and telbivudine are not recommended due to high
rates of resistance (12).
4-Chronic Hepatitis C Treatment
A-Treatment is recommended for all HCV-infected persons (9).
B-Before starting treatment, the genotype of the infecting hepatitis C virus
should be determined as this may affect the choice and duration of treatment
(9)
.
C-IFN and pegIFN are no longer recommended for chronic HCV (12).
Direct-acting antiviral agents: [simeprevir, paritaprevir (boosted with
ritonavir), ledipasvir, ombitasvir, sofosbuvir, dasabuvir, daclatasvir, velpatasvir,
grazoprevir, elbasvir, voxilaprevir] (1) have higher cure rates (well above
90%), fewer adverse effects, and shorter treatment durations (12)
5-The recommended treatment for HDV is pegIFN for 48 weeks (12).
Drugs for viral hepatitis
Scientific name Trade names Dosage form
1

Any extra notes:

84
6.5.2- Herpes virus infections
1-Antivral agents for herpes virus infections are aciclovir, famciclovir,
valaciclovir, foscarnet (1).
2-Foscarnet is use for simplex virus infection unresponsive to aciclovir in
immunocompromised patients; men should avoid fathering a child during and
for 6 months after treatment (1).
6.5.2.1-Herpes simplex infections
1-Herpes infection of the mouth and lips and in the eye is generally associated with
herpes simplex virus serotype 1 (HSV-1). Genital infection is most often
associated with HSV-2 and also HSV-1 (1).
2-Topical antiviral treatment is not routinely recommended in
immunocompetent individuals with uncomplicated infection of the lips (herpes
labialis or cold sores) or herpetic gingivostomatitis. However, some patients may
find application of a topical antiviral drug helpful when used from the onset
of the prodromal phase (1).
3-Oral antiviral treatment may be considered in patients with severe, frequent or
persistent oral infection usually for 5 days (longer if new lesions appear during
treatment or if healing incomplete) (1).
6.5.2.2-Varicella-zoster infections
1-Chickenpox is an acute disease caused by the varicella-zoster virus.
Chickenpox in otherwise healthy children is usually self-limiting and
complications are rare; antiviral treatment is not routinely recommended (1).
2-Chickenpox is more severe in adolescents (aged 14 years and over) and adults
than in children; antiviral treatment started within 24 hours of the onset of
rash may be considered, particularly for those with severe infection or at risk of
complications (1).
3-Shingles (herpes zoster) is a viral infection of an individual nerve and the skin
surface affected by the nerve. The infection is caused by the reactivation of the
varicella-zoster virus, the same virus that causes chickenpox (1).
4-Oral antiviral treatment should be offered to patients with shingles who are
immunocompromised, have non-truncal involvement (e.g. neck, limbs, perineum),
or to those with moderate to severe pain or rash. Consider oral antiviral treatment
for patients aged over 50 years to reduce the risk of post-herpetic neuralgia.
Treatment with the antiviral should be started within 72 hours of the onset of rash
(1)
.
5-Chronic pain which persists after the rash has healed (post-herpetic neuralgia)
requires specific management (1).

85
Drugs for herpes simplex infections
Scientific name Trade names Dosage form
1

Any extra notes:

6.5.3-Influenza
1-The antivirals oseltamivir and zanamivir are used for both treatment (ideally
within 48 hours of symptom onset) and post-exposure prophylaxis of influenza (1).
2-Antiviral medications can be used to prevent influenza (1) (Table 6-11).
Table 6-11: Indications and duration of use of oseltamivir and zanamivir (1).
Oseltamivir (Tamiflu) Zanamivir (Relenza)
Treatment Daily for 5 days Daily for 5 days
Post-exposure Daily for 10 days Daily for 10 days
prophylaxis of influenza
Prevention of influenza Daily for up to 6 weeks Daily for up to 28 days
during an epidemic

Any extra notes:

References
1-BNF-81 (2021).
2-Michael AM, Jason. Frequently prescribed medications. Third edition 2019.
3-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
4-UPTODATE: 2021.Available at: https://www.uptodate.com/contents/search.
5-Alistair G., Jane W., Vincent G., Lynn B. Injectable Drugs Guide. 1st edition.
Royal Pharmaceutical Society of Great Britain 2011.
6-Pavan Bhat, et al. Washington Manual of Medical Therapeutics, The, 35th
Edition. Copyright 2016.
7-BNF-For children. 2019-2020.
8-David J Quan, Richard A Helms. Textbook of Therapeutics: Drug and Disease
Management. 8th edition. 2006.
9-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.

86
10-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The
clinical use of drugs, 11th ed., 2018.
11-Stuart HR, Ian DP, Mark WJ, et al, eds. Davidson‘s Principles and Practice of
Medicine. 23th edition; 2018.
12-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
13-J. Larry Jameson, Anthony S. Fauci, Dennis L. Kasper, Stephen L. Hauser, Dan
L. Longo, Joseph Loscalzo. Harrison's Principles of Internal Medicine, 20th
Edition. 2018 by the McGraw-Hill Companies, Inc.

87
Chapter Seven : Endocrine System
7.1-Drugs used in diabetes
7.1.1-Oral Antidiabetics
Note: they are given for type II diabetes.
1-Classification and administration with respect to food (Table 7-1) :
Table 7-1: Classification and administration of oral antidiabetics
Groups Example(s) Administration
Glibenclamide, With food (1)
Gliclazide,
Glimepiride,
Tolbutamide
Extended release: Administer with
1 Sulphonylureas breakfast or the first meal of the
day.
Glipizide Immediate release: Administer 30
minutes before a meal (preferably
before breakfast if once-daily
dosing) (2).
2 Biguanides Metformin Take with or just after food (1)
Alogliptin, Without regard to meal (3)
Linagliptin,
Dipeptidylpeptidas
3 e-4 inhibitors
Sitagliptin,
Saxagliptin,
Vildagliptin
4 Thiozolidinediones Pioglitazone Without regard to meal (2).
Nateglinide, Within 30 minutes before meals (1).
5 Meglitinides
Repaglinide
Tablets should be chewed with first
Alpha-glucosidase mouthful of food or swallowed
6 inhibitor Acarbose whole with a little liquid
immediately before food (1).
May be administered with or
Canagliflozin without food. It is recommended to
Sodium-glucose
take before the first meal of the day
cotransporter (2)
7 2 (SLGT2)
.
Dapagliflozin, Administer in the morning with or
inhibitors
Empagliflozin, without food (2).
Ertugliflozin
7.1.1.1-Biguanides:
1-Metformin is the only biguanide approved by the Food and Drug
Administration (FDA). This agent is thought to lower blood glucose by decreasing
hepatic glucose production and increasing insulin sensitivity (4).

88
2-Metformin is recommended as first-line pharmacotherapy in patients with
type 2 DM due to extensive experience, high efficacy, minimal hypoglycemia risk,
positive or neutral effects on weight, potential positive impact on CV risk,
manageable side-effect profile, and low cost (5).
3-Metformin frequently causes GI side effects (diarrhea, abdominal discomfort,
stomach upset); these effects are usually dose-dependent, transient, mild, and can
be minimized with slow dose titration, taking metformin with or immediately
after meals (5), and through use of extended-release products (4). Rarely it may
cause lactic acidosis (4).
4-Metformin may cause a metallic taste and may lower vitamin B12
concentrations (5).
5-Important: Metformin is prescribed as an insulin sensitizing drug in women
with polycystic ovary syndrome who are not planning pregnancy [unlicensed
indication]. Metformin may improve short-term insulin sensitivity and reduce
androgen concentrations, but there is insufficient supporting evidence that
metformin improves weight gain, hirsutism, acne or regulation of the menstrual
cycle (1).
Biguanides
Scientific name Trade names Dosage form

Any extra notes:

7.1.1.2-Sulfonylureas
1-Sulfonylureas enhance insulin secretion from the of pancreatic β-cells.
Common adverse effects include hypoglycemia and weight gain. There may be
some cross-sensitivity in patients with sulfa allergy (4).
2-Glimepiride and glipizide have lower risk of hypoglycemia (5).
3-Sulfonylureas with long durations of action (such as glibenclamide) and those
with active metabolites should be used with extreme caution in older patients
and those with renal insufficiency due to the high risk of hypoglycemia (5).
4-Glibenclamide can be used during the second and third trimesters of
pregnancy in women with gestational diabetes (1).

89
Sulfonylureas
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.1.3-Meglitinides
1-Nateglinide and repaglinide stimulate insulin secretion from pancreatic β-cells
by. They are similar to sulfonylureas except that they have a faster onset and
shorter duration of action (5). Because they have a rapid onset and short duration
of action, they should be taken 15 to 30 minutes before a meal (4).
2-Similar to sulfonylureas, the main side effects are hypoglycemia and weight
gain (5).
Meglitinides
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.1.4-Thiazolidinediones (TZDs)
The TZDs (pioglitazone and rosiglitazone) act by enhancing insulin sensitivity in
muscle, liver, and fat tissues. Maximum effects may not be seen until 3–4
months of therapy. TZDs are considered second- or third-line agents (5).

91
Thiazolidinediones
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.1.5-Dipeptidyl peptidase-4 (DPP-4) inhibitors


1-DPP-4 inhibitors prolong the half-life of endogenously produced GLP-1, thereby
increasing glucose-dependent insulin secretion from the pancreas without an
increase in hypoglycemia when used as monotherapy (5).
2-There are no clear differences in efficacy among agents in the class.
Advantages include once-daily dosing, oral administration, weight neutrality, low
risk of hypoglycemia, and good tolerability (5).
3-Adverse effects are uncommon and include stuffy, runny nose; headache; and
upper respiratory tract infections (5).
Dipeptidyl peptidase-4 (dpp-4) inhibitors
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.1.6-Sodium-glucose cotransporter-2 inhibitors


1-Sodium-glucose cotransporter-2 inhibitors reduce plasma glucose by preventing
the kidneys from reabsorbing glucose back into the bloodstream, leading to
increased glucose excretion in the urine (5).
2-The most common adverse effect is genital mycotic infections, which are
more common in women and uncircumcised men. There is also a slightly
increased risk of urinary tract infections (5).

91
Sodium-glucose cotransporter-2 inhibitors
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.1.7-α-Glucosidase inhibitors
1-Acarbose and miglitol delay the breakdown of sucrose and complex
carbohydrates in the small intestine (5) so delay absorption of carbohydrates and
reduce postprandial glucose concentrations (4).
2-The most common side effects are flatulence, abdominal pain, and diarrhea,
which can be reduced by slow dosage titration (5).
Other oral Antidiabetics
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.2-Parenteral anti-diabetes agents


Parenteral anti-diabetes agents include: insulins, GLP-1 receptor agonists
(incretin mimetic) and amylin mimetic (5).
7.1.2.1-Insulins
1-Treatment of T1DM requires providing exogenous insulin to replace the
endogenous loss of insulin from the nonfunctional pancreas. It is also used for
T2DM (4).
2-Commercially available insulin products differ in their the pharmacokinetics (6).
There are currently four pharmacokinetic profiles available: (1) rapid (aspart,
glulisine, and lispro) (2) short (regular insulin) (3) Intermediate (NPH: Neutral

92
Protamine Hagedorn insulin) (4) long-acting insulin (Glargine, degludec and
detemir) (7) (Table 7-2) (8).
Table 7-2: Summary of characteristics of insulins (8)

3-Regular insulin commonly referred to as natural insulin. It is a clear solution.


Patients should be counseled to inject regular insulin subcutaneously 30
minutes before consuming a meal (4).
4-The fast (rapid)-acting recombinant insulin analogues (insulin lispro, insulin
aspart and insulin glulisine) offer greater convenience and flexibility, due to a
more rapid absorption and shorter duration of action. They can be given
immediately before a meal rather than the 30 minutes before recommended
for human soluble insulin (9).
5-Rapid-acting insulin has an advantage over short-acting soluble insulin in terms
of reduction in the incidence of severe hypoglycemia, including nocturnal
hypoglycaemia (1).
6-Intermediate-duration (NPH) insulin has a delayed onset but extended
duration of action, and is designed to cover insulin requirements in between
meals and/or overnight (4). It usually requires twice daily dosing (5).
7-NPH insulin can be mixed with regular insulin and used immediately or stored
for future use. NPH insulin can be mixed with either aspart or lispro insulins, but it
must be injected immediately after mixing. Whenever mixing insulin products with
NPH insulin, the shorter acting insulin should be drawn into the syringe first (4).
8-Long-duration: Glargine, detemir, and degludec are designed as once-daily-
dosing basal insulins which provide a relatively constant insulin concentration over
24 hours (4). Glargine, and degludec are peakless (5).
9-Combination products: A number of combination insulin products are available
commercially. These combination products allow some patients to manage their
insulin therapy with only two injections per day, and avoids the difficulty and
possible errors that can occur when manually mixing insulins [e.g., NPH is
available in a combination of 70/30 (70% NPH and 30% regular insulin)] (4).

93
10-The most common route of insulin administration is subcutaneous injection
using a syringe or pen device. Patients should be educated to rotate injection sites
to minimize lipohypertrophy, a buildup of fat that decreases or prevents proper
insulin absorption (4).
11-Regular insulin, insulin lispro, insulin
aspart, and insulin glulisine can be
administered intravenously (IV) (4).
12-Additionally, patients should
understand that the absorption rate may
vary among injection sites (abdomen,
thigh, arm, and buttocks) because of
differences in blood flow, with absorption
occurring fastest in the abdomen and
slowest in the buttocks (4).
13-All oral antidiabetic drugs, except
metformin, should be discontinued
before pregnancy (or as soon as an
unplanned pregnancy is identified) and substituted with insulin therapy (1).
14-Insulin is typically refrigerated, though most vials are good for 28 days at
room temperature (4).
15-Disadvantages include the risk of
hypoglycemia, need for injections, and weight
gain. Inhaled human insulin can cause cough
and upper respiratory infections, and it is
contraindicated in chronic obstructive pulmonary
disease and asthma due to bronchospasm risk (5).
16-Most insulin products are administered
subcutaneously (SC) for chronic diabetes
management, except for inhaled human insulin, which is a dry powder of regular
insulin that is inhaled and
absorbed through pulmonary
tissue (5).
17-The primary sites used for
injecting insulin are the lateral
thigh, abdomen and upper arm.
Many practitioners recommend
using the abdominal area because
absorption from this site is least
affected by exercise and is the
most predictable (3).

94
18-Insulin pen devices are also available for injecting insulin. Pen devices are
often preferred as they make insulin administration much easier, especially for
patients who need to take their insulin doses away from home. They also can
increase dosing accuracy (3).
19-Insulin pump consists of a pump that can programmed to deliver
predetermined amounts of insulin [i.e., regular, or rapid (mostly)] from a
reservoir to a subcutaneously inserted catheter or needle (3).
20-The dose of insulin is expressed as units.

Insulin preparations
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.2.2-Glucagon-like peptide-1 receptor agonists (GLP1-RAs )


1-Dulaglutide, exenatide, exenatide XR, lixisenatide, liraglutide, and
semaglutide stimulate insulin secretion and suppress inappropriately high
postprandial glucagon secretion, decreasing hepatic glucose output. They also slow
gastric emptying, increase satiety, and cause weight loss (average 1–3 kg) (5).
2-Glucagon-like peptide-1 receptor agonists should be reserved for combination
therapy when other treatment options for type 2 DM have failed (1).
3-Liraglutide (Saxenda®) was also approved for long-term obesity management
as an adjunct to lifestyle modification (3) (See Chapter 3).
4-The GLP1-RAs are administered SC. The most common adverse effects of
GLP1-RAs are nausea, vomiting, and diarrhea (5).
Glucagon-like peptide-1 receptor agonists
Scientific name Trade names Dosage form
1

95
2

Any extra notes:

7.1.3-Diabetic complications (Table 7-3)

Table 7-3: Recommended drug(s) for some diabetic complications


Complications Recommended drug(s)
1 Cardiovascular disease ACE inhibitor, low dose aspirin and a
lipid-regulating drug (1).
2 Diabetic nephropathy ACE inhibitor or ARBs (1).
Gabapentin, pregabalin, carbamazepine,
Painful opioid analgesics, duloxetine,
neuropathy amitriptyline, nortriptyline, and capsaicin
cream (1).
Diabetic Diabetic diarrhea Doxycycline or metronidazole.
3 neuropathy Octreotide may be useful in
(5)
unresponsive cases .
Gastroparesis Metoclopramide or erythromycin may
be helpful (5).
Orthostatic Fludrocortisone, midodrine (5).
hypotension
Erectile Sildenafil, vardenafil, tadalafil (5).
dysfunction
4 Diabetic retinopathy Bevacizumab (used off-label) and
(proliferative retinopathy) ranibizumab are anti-vascular endothelial
growth factor (VEGF) monoclonal
antibodies, and aflibercept is a VEGF decoy
receptor (5).
5 Peripheral arterial disease Statin therapy, antiplatelet therapy are
important strategies. Cilostazol may be useful
in select patients to reduce symptoms (5).
7.1.4-Hypoglycaemia
1-Treatment of hypoglycemia dictates ingestion of carbohydrates. Glucose is
preferred. Patients should be counseled to carry a source of fast-acting glucose
with them at all times (5).
2-The “rule of 15” is commonly used to teach patients the proper treatment.
First, the patient should glucose level to confirm a glucose < 70 mg/dL and then
ingest 15 grams of fast-acting carbohydrates (1/2 cup [125 mL] of milk, juice, or
soda, 1 tablespoon of honey) (5).
96
3-Glucose level should be repeated in 15 minutes; if the glucose is <70 mg/dL,
the process should be repeated. Once the blood glucose is normalized, the patient
should eat a snack or meal that includes complex carbohydrates and protein to
prevent further hypoglycemic episodes (5).
4-If the patient is unconscious, IV glucose or glucagon (either via the
intramuscular or intranasal route) should be given. Glucagon may be given in any
situation in which IV glucose cannot be rapidly administered (5).

7.2-Thyroid and antithyroid drugs


7.2.1-Thyroid hormone
1-Thyroid hormone [thyroxine (levothyroxine)] is used in hypothyroidism (1).
(Hypothyroidism is readily treated by lifelong replacement therapy with
thyroxine) (10).
2-Thyroxine dose preferably taken 30–60 minutes before breakfast, caffeine
containing liquids (e.g. coffee, tea), or other medication (1). (Taking levothyroxine
at bedtime results in somewhat higher serum T 4 and lower TSH levels.
Therefore, the administration timing for levothyroxine should be kept
constant) (8).
3-Levothyroxine is the drug of choice for pregnant women (5).
Scientific name Trade names Dosage form
1

Any extra notes:

7.2.2-Antithyroid drugs
1-Thionamides:
A-Thionamides (carbimazole, methimazole and propylthiouracil) are
effective in treating hyperthyroidism (3).
B-Antithyroid drug therapy should continue for 12 to 24 months to induce a
long-term remission (5).
C-Propylthiouracil is drug of choice during the first trimester of pregnancy,
during the second and third trimesters, methimazole (hence carbimazole) is
the drug of choice (5).
2-Radioactive iodine (RAI) or surgery may be considered in the management of
Graves’ disease or toxic nodular goiter (1).
3-Iodide acutely blocks thyroid hormone release, inhibits thyroid hormone
biosynthesis, and decreases size and vascularity of the gland. Iodides are often

97
used as adjunctive therapy to prepare a patient with Graves’disease for
surgery (5).
4-β-adrenergic blockers:
A-Because many manifestations of hyperthyroidism appear to be mediated by
the β-adrenergic system, β-adrenergic blockers are used to rapidly relieve
palpitations, tremor, anxiety, and heat intolerance (4).
B-Because β-blockers do not reduce the synthesis of thyroid hormones, they are
used only until more specific antithyroid therapy is effective. Because
nonselective agents can impair the conversion of T4 to T3, propranolol and
nadolol are preferred (4).
C-Propranolol has been used for several weeks preoperatively (4) (The thyroid
gland is rendered less vascular thus making surgery easier) (1) and 7–10
days after surgery to maintain pulse rate <90 beats/min (4).
Antithyroid drugs
Scientific name Trade names Dosage form
1

Any extra notes:

7.3-Corticosteroids
1-The corticosteroids are used in physiological doses for replacement therapy in
adrenal insufficiency. Pharmacological doses are used when anti-inflammatory
or immunosuppressant effects are required (10) (for so many different diseases).
2-Cortisone and hydrocortisone have very appreciable mineralocorticoid (or
sodium-retaining) properties relative to their glucocorticoid (or
antiinflammatory) properties, prednisolone have considerably less, and others,
such as betamethasone and dexamethasone, have none or virtually none (10).
3-As a rough guide, the approximate equivalent doses of the main corticosteroids
in terms of their glucocorticoid (or anti-inflammatory) properties alone, are:
Betamethasone 0.75 Mg = Cortisone Acetate 25 Mg = Dexamethasone 0.75 Mg
= Hydrocortisone 20 Mg = Methylprednisolone 4 Mg = Prednisolone 5 Mg =
Prednisone 5 Mg = Triamcinolone 4 Mg (10).
4-Important:
A-The use of pharmacological doses of corticosteroids suppresses the
endogenous secretion of steroids by the anterior pituitary (10).
98
B-The adrenal suppression is less when the corticosteroid is given as a single
dose in the morning, and even less if this morning dose is given on alternate
days or less frequently (10).
C-Sudden withdrawal or reduction in dosage, may precipitate acute
adrenocortical insufficiency (10).
D-Gradual withdrawal of systemic corticosteroids is required for example :
-Patient who received more than 40 mg prednisolone (or equivalent)
daily for more than 1 week (1).
-Patient who received more than 3 weeks‘ treatment (1).
5-Corticosteroids have numerous side effects including nearly all body systems.
A-Most Common: Gastrointestinal irritation, increased appetite, nervousness/
restlessness, weight gain, acne, glucose intolerance (transient), lipid
abnormalities (transient) (11).
B-Rare/Severe/Important: infections, adrenal suppression, rounding out of the
face, hirsutism, glaucoma, osteoporosis, peptic ulceration (11).
6-Important: Corticosteroids (especially dexamethasone) are frequently abused
in Iraq. (prolonged use of glucocorticoids have a dramatic effect on body fat
distribution, resulting in the characteristic appearance of moon face) (11).
Corticosteroids
Scientific name Trade names Dosage form
1

Any extra notes:

7.4-Disorders of bone metabolism


1-Osteoporosis occurs most commonly in postmenopausal women and in those
taking long-term oral corticosteroids (glucocorticosteroids) (1).
99
2-Two main classes of medications are available for osteoporosis: antiresorptives,
which decrease bone resorption, and anabolics, which promote bone
formation (6).
3-Those at risk of osteoporosis should maintain an adequate intake of calcium and
vitamin D and if necessary, receive other preventative therapy. (1). Calcium
carbonate is the salt of choice. It should be ingested with meals to enhance
absorption. Calcium citrate need not be taken with meals (5).
4-Bisphosphonates (alendronic acid, ibandronic acid, pamidronate disodium,
risedronate sodium, sodium clodronate, and zoledronic acid) (1).
A-Bisphosphonates are first-line therapy for osteoporosis in both men and
women (1).
B-Oral bisphosphonates must be administered correctly to optimize clinical
benefit and minimize adverse GI effects. Each oral tablet should be taken in
the morning with at least (180 mL) of plain water (not coffee, juice, mineral
water, or milk) at least 30 minutes (60 minutes for oral ibandronate) before
consuming any food, supplements, or medications. An exception is delayed-
release risedronate, which is administered immediately after breakfast with at
least (120 mL) of plain water (5).
C-The patient should remain upright (sitting or standing) for at least 30
minutes after alendronate and risedronate and 1 hour after ibandronate
administration to prevent esophageal irritation and ulceration (5).
D-If a patient misses a weekly dose, it can be taken the next day. If more
than 1 day has elapsed, that dose is skipped until the next scheduled
ingestion. If a patient misses a monthly dose, it can be taken up to 7 days
before the next scheduled dose (5).
E-Weekly, monthly and quarterly dosing may increase adherence with
taking bisphosphonate (5, 6).
F-I.V. zoledronic is approved for once-yearly treatment of postmenopausal
osteoporosis, and administered once every other year to prevent osteoporosis
(6)
.
G-Bisphosphonates are also used in the treatment of Paget’s disease,
hypercalcaemia of malignancy, and in bone metastases in breast cancer (1).

Drugs for osteoporosis


Scientific name Trade names Dosage form
1

111
3

Any extra notes:

7.5-Sex hormones
7.5.1-Female sex hormones
7.5.1.1-Hormone replacement therapy
1-Hormone replacement therapy (HRT) with small doses of an estrogen (e.g.
estradiol, estrone, estriol , ethinylestradiol) (together with a progestogen in women
with a uterus to reduces the risk of endometrial cancer) is appropriate for
alleviating menopausal symptoms such as vaginal atrophy or vasomotor
instability (1) [vasomotor symptoms (hot flushes and night sweats)] (5).
2-Menopausal atrophic vaginitis may respond to topical vaginal estrogen
(Chapter 8) preparation used for a few weeks and repeated if necessary (1).
3-An estrogen may be given by mouth or by transdermal administration, which
avoids first-pass metabolism (1).

Hormone replacement therapy (HRT)


Scientific name Trade names Dosage form
1

Any extra notes:

7.5.1.2-Progestogens
1-Progestogens are used as hormonal contraceptives, either alone or combined with
an estrogen (10).
2-Progestogens and drugs with progestogenic actions (e.g. dydrogesterone and
medroxyprogesterone and norethisterone) may be used in menstrual disorders
such as dysmenorrhoea and menorrhagia associated with dysfunctional uterine
bleeding (1, 10).
3-Progestogens may also be used in the management of endometriosis (10).
4-Progestogens sometimes are used with estrogens for HRT (see above) (10).

111
5-Important: Progestogens have been used for the prevention of spontaneous
abortion in women with a history of recurrent miscarriage but there is no
evidence of benefit and they are not recommended for this purpose (1).
6-Ulipristal is a progesterone receptor modulator with a partial progesterone
antagonist effect. Ulipristal is used as an hormonal emergency contraceptive (1).
Progestogens
Scientific name Trade names Dosage form
1

Any extra notes:

7.5.2- Male sex hormones


1-The primary indication for androgens (e.g. mesterolone, testosterone or its
esters) is as replacement therapy in male hypogonadal disorders caused by either
pituitary or testicular disorders (10).
2-Androgens are useless as a treatment of impotence and impaired
spermatogenesis unless there is associated hypogonadism (1).
3-The testosterone esters are usually formulated as oily solutions for
intramuscular use to give a prolonged duration of action (10).
Male sex hormones
Scientific name Trade names Dosage form
1

Any extra notes:

7.6-Hypothalamic and anterior pituitary hormones and


antiestrogens
7.6.1-Anti-estrogens
1-Clomifene (clomiphene) :
A-Clomifene is indicated for female infertility due to ovulatory dysfunction (1).

112
B-Patients should be warned that there is a risk of multiple pregnancy (rarely
more than twins) (1).
C-Manufacturer advises clomifene should not normally be used for longer than
6 cycles (possible increased risk of ovarian cancer) (1).
2-Tamoxifen (10) :
A-Tamoxifen is an estrogen antagonist with actions similar to those of
clomifene citrate.

B-It is used in the treatment of breast cancer.


C-Tamoxifen is also used to stimulate ovulation in women with anovulatory
infertility.
Anti-estrogens
Scientific name Trade names Dosage form
1

Any extra notes:

7.6.2-Gonadotrophins
Follicle-stimulating hormone (FSH) and luteinizing hormone (LH) together,
follicle-stimulating hormone alone, or chorionic gonadotrophin, are used in the
treatment of infertility in women with proven hypopituitarism or who have not
responded to clomifene (1).
Gonadotrophins
Scientific name Trade names Dosage form
1

Any extra notes:

7.6.3-Growth hormone
Growth hormone (Recombinant Human Growth Hormone somatropin) is used to
treat deficiency of the hormone in children and in adults (1).

113
7.7-Antidiuretic hormone disorders
1-Vasopressin (antidiuretic hormone, ADH) is used in the treatment of pituitary
(‗cranial‘) diabetes insipidus as is its analogue desmopressin (1).
2-Desmopressin is more potent and has a longer duration of action than
vasopressin; unlike vasopressin it has no vasoconstrictor effect (it is given by
mouth or intranasally for maintenance therapy) (1).
3-Other uses:
A-Desmopressin may also have a role in nocturnal enuresis. Patients being
treated for primary nocturnal enuresis should be warned to limit fluid intake to
minimum from 1 hour before dose until 8 hours afterwards; and to stop
taking desmopressin during an episode of vomiting or diarrhea (until fluid
balance normal) (1).
B-Desmopressin is also used to boost factor VIII concentration in mild to
moderate haemophilia and in von Willebrand‘s disease (1).
7.8-Bromocriptine and other dopaminergic drugs
1-Bromocriptine is a stimulant of dopamine receptors in the brain; it also inhibits
release of prolactin by the pituitary. Cabergoline has actions and uses similar to
those of bromocriptine, but its duration of action is longer (7)(it may be given
once weekly for some indications) (1).
2-Uses:
A-Bromocriptine, inhibits the secretion of prolactin from the anterior pituitary
and is used in the treatment of prolactinoma (prolactin-secreting pituitary
adenomas) and endocrinological disorders associated with hyperprolactinaemia,
including amenorrhoea, galactorrhoea, and infertility in both men and
women (7).
B-Growth hormone secretion may be suppressed by bromocriptine in some
patients with acromegaly (7).
C-Because of its dopaminergic activity bromocriptine is also used in the
management of Parkinson’s disease (7).
D-Bromocriptine is also approved for type 2 diabetes mellitus (9).
3-Adverse Effects:
A-Nausea is the most common adverse effect at the beginning of treatment
with bromocriptine, but vomiting, dizziness, and orthostatic hypotension may
also occur. Syncope has followed initial doses (7).
B-Adverse effects are generally dose-related and may therefore be more
frequent with the higher doses (7).
C-Nausea may be reduced by gradual increase of the dose, taking
bromocriptine with food; domperidone may also be given at least 1 hour
before bromocriptine, for the first few days of therapy (7).

114
Bromocriptine and other dopaminergic drugs
Scientific name Trade names Dosage form
1

Any extra notes:

References
1-BNF-81 (2021).
2-Uptodate 2021. Available at: https://www.uptodate.com/contents/search.
3-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
4-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
5-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.
6-Edward T. Bope, et al, eds. Conn‘s Current Therapy . Copyright 2018.
7-NAPLEX® Review Guide, Fourth Edition. Copyright © 2021 by McGraw-Hill.
8-Maxine A. Papadakis, et al, eds. Current Medical Diagnosis & Treatment, 58th
Edition 2019.
9-Roger Walker. Clinical Pharmacy and Therapeutics. Sixth edition 2019.
10-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
11-Michael AM, Jason. Frequently prescribed medications. Third edition 2019.

115
Chapter Eight : Genito-urinary System
7.1-Drugs for genito-urinary disorders
7.1.1-Drugs for benign prostatic hyperplasia (BPH):
1-Drug therapy for BPH can be categorized into three types: agents that relax
prostatic smooth muscle (α1-adrenergic antagonists and phosphodiesterase
inhibitors), agents that interfere with testosterone's stimulatory effect on
prostate gland enlargement (5-α-reductase inhibitors), and agents that relax
bladder detrusor muscle (improving the urine storage capacity of the bladder)
(antimuscarinic agents and mirabegron) (1).
2-Initiate therapy with an α1-adrenergic antagonist for faster onset of symptom
relief (2).
3-Combination medication regimens are reserved for patients who have voiding
symptoms that do not respond to an adequate trial of single drug treatment or
patients who are at high risk of developing complications of BPH (those with an
enlarged prostate) (3).
7.1.1.1-α1-Adrenergic antagonists
1-They do not reduce the prostate size or prevent progression of BPH. Efficacy
of α1-adrenergic antagonists is comparable (1).
2-Immediate-release (IR) terazosin and doxazosin require dose titration to
prevent cardiovascular side effects (orthostatic hypotension, syncope), thus
delaying the time to reach an effective dose (1).
3-To minimize first-dose syncope from terazosin and doxazosin immediate-
release, a slow up-titration from a subtherapeutic to a therapeutic dose is essential.
The first dose should be given at bedtime (3).
4-Patient should be warned to lie down if symptoms such as dizziness, fatigue or
sweating develop, and to remain lying down until they abate completely (4).
5-Tamsulosin and silodosin are uroselective based on their affinity for α1A-
receptors and alfuzosin is functionally uroselective based on its ER formulation
preventing peaks in serum concentrations. These agents target α1A-receptors in the
prostate and are less likely to cause hypotension or syncope. These agents improve
urinary symptoms within 1 week because they do not require dose titration (1).
6-Silodosin has significantly greater α1A-adrenergic selectivity than tamsulosin
and is preferred when a patient has minimal tolerance for any blood pressure–
lowering adverse effects (3).
7-Uroselective are preferred in patients who usually have low blood pressure
or those taking multiple antihypertensives (3).
8-Modified- or extended-release formulations of doxazosin, alfuzosin, tamsulosin,
and silodosin produce lower peak levels, but more sustained therapeutic
plasma levels, than immediate-release formulations and have less potential for

116
producing hypotensive episodes. This allows for initiation of treatment with a
therapeutic dose, a faster onset of peak clinical effects, and once daily dosing (3).
9-Reversible delayed, absent or retrograde ejaculation occur with all α1-
adrenergic antagonists (3).
10-Nasal congestion and malaise occur with α1-adrenergic antagonists.
Tolerance often develops to these adverse effects and they rarely require
discontinuation of treatment. Avoid use of topical or oral decongestants, as these
may exacerbate obstructive voiding symptoms (3).
11-Note: Tamsulosin, may be used also for expulsion of lower ureteral stones
(for both male and female)(5).
7.1.1.2-: 5-α-Reductase inhibitors (5ARIs)
1-The conversion of testosterone to dihydrotestosterone (DHT) mediated by the
enzyme 5-α-reductase stimulates prostate growth. Inhibiting 5-α-reductase
decreases symptoms of BPH by reducing prostate size and decreases prostate-
specific antigen by 25% (1).
2-Two 5ARIs include finasteride and dutasteride. The difference between
agents is that finasteride inhibits type II 5-α-reductase while dutasteride inhibits
type I and II. This mechanism results in a faster, complete decrease in
intraprostatic DHT; however, there is no known clinical advantage compared to
finasteride (1).
3-Monotherapy with a 5ARI should be considered in patients with BPH due to an
enlarged prostate. Combination therapy with a 5ARI and an α1-adrenergic
antagonist improves urinary flow rates and prevents progression of BPH in patients
with moderate to severe BPH with evidence of an enlarged prostate (>40 g) (1).
4-5α-Reductase inhibitors may be preferred in patients with uncontrolled
arrhythmias, poorly controlled angina, requirement for multiple antihypertensives,
or intolerance to the hypotensive effects of α1-adrenergic antagonists (2).
5-Unlike α1- adrenergic antagonists, long-term use of 5 α-reductase inhibitors is
used to prevent BPH-related complications and disease progression (3).
6-Side effects include reduced libido and rarely gynecomastia (1). These agents
reduce the incidence of prostate cancer by 25%, but are suspected to increase the
risk of developing moderate to high grade cancer, if prostate cancer does develop
(3)
.
7-Exposure to 5α-reductase inhibitors is contraindicated in pregnant females, as
the drugs may cause feminization of a male fetus. Women who are pregnant or
seeking to become pregnant should not handle these drugs unless they are wearing
gloves. Also should not contact with semen from men taking 5α-reductase
inhibitors (2, 3).
8-Note: In the treatment androgenetic alopecia in men, finasteride is given
orally in a low dose (1 mg daily) while the dose used for BPH is 5 mg daily (4).
117
7.1.1.3-Phosphodiesterase inhibitors
Tadalafil is approved for symptoms secondary to BPH. The recommended dose is
5 mg once daily (1). Although other phosphodiesterase type 5 inhibitors share the
same mechanism of action as tadalafil, tadalafil is preferred because of its
longer plasma half-life, which is theoretically beneficial in the management of
BPH, a chronic disease (3).
7.1.1.4-Anticholinergics
1-Irritative voiding symptoms (urinary frequency, nocturia, urinary urgency, and
urge incontinence) (1) are due to involuntary detrusor muscle contraction in
response to small volumes of urine in the bladder (3).
2-Anticholinergic agents are indicated when a patient has bothersome irritative
voiding symptoms despite treatment with an α1-adrenergic antagonist.
Typically, an anticholinergic agent is added sequentially to an established α1-
adrenergic antagonist regimen (3).
3-A variety of anticholinergic agents, including oxybutynin or tolterodine, have
been added to an α-adrenergic antagonist regimen to relieve these symptoms (1).
4-Uroselective anticholinergic agents, which preferentially inhibit M3 receptors
(eg, darifenacin or solifenacin), or transdermal (oxybutynin), or ER
formulations of anticholinergic agents (eg, tolterodine) are recommended for
patients who poorly tolerate systemic adverse effects of other anticholinergic
agents (1).
5-Because older patients are sensitive to the central nervous system adverse
effects and dry mouth, such patients should be started on the lowest effective dose
and then slowly titrated up (1).
7.1.1.5-Mirabegron
1-In the urinary bladder, 95% of all β-adrenergic receptors are of the β3 type.
Receptor stimulation relaxes the detrusor muscle, but does not interfere with the
bladder‘s contractility (3).
2-Mirabegron is a β3-adrenergic agonist. It causes release of norepinephrine
which stimulates β3-adrenergic receptors (3). Mirabegron reduces irritative voiding
symptoms, increases urinary bladder capacity, and increases the interval between
voidings (1).
3-The clinical effect of mirabegron for symptoms is similar to that of
anticholinergic agents, but mirabegron is better tolerated. Mirabegron does not
produce anticholinergic adverse effects, nor does it cause acute urinary retention
(1)
.
4-Mirabegron is an alternative to an anticholinergic agent in patients who
poorly tolerate or are at high risk of anticholinergic adverse effects, or when
irritative voiding symptoms do not respond to an anticholinergic agent.
Mirabegron is typically added to an α1-adrenergic antagonist (3).

118
7.1.1.6-Herbal
1-Saw palmetto is a herbal agent with mixed clinical results. Saw palmetto has a
modest effect at reducing BPH symptoms; however, a large trial found no
difference compared to placebo. Based on a lack of clinical studies
demonstrating improvement in symptoms, the AUA does not recommend this
product (1).
2-Patients taking saw palmetto along with antiplatelet agents or anticoagulants
should be counseled on possible bleeding side effects (1).

Drugs for benign prostatic hyperplasia


Scientific name Trade names Dosage form
1

Any extra notes:

7.1.2-Urinary incontinence (UI)


1-UI occurs as a result of
overfunctioning or underfunctioning
of the urethra, bladder, or both.
Urethral underactivity is known as
stress UI. Bladder overactivity is
known as Urge UI (UUI) (bladder
muscle is overactive and contracts
inappropriately) (2).

119
7.1.2.1-Bladder overactivity: urge urinary incontinence
The pharmacotherapy of first choice for UUI includes antimuscarinic agents and
β3-adrenergic agonists drugs, which antagonize muscarinic cholinergic receptors
(2)
.
7.1.2.1.1-Antimuscarinic agents (oxybutynin, tolterodine, trospium,
solifenacin, darifenacin, and fesoterodine)
1-Oxybutynin immediate-release (IR) is the oldest and least expensive treatment
for UUI. Many patients discontinue oxybutynin IR because of adverse effects due
to antimuscarinic effects (eg, dry mouth, constipation, vision impairment,
confusion, cognitive dysfunction, and tachycardia), α-adrenergic inhibition (e.g.,
orthostatic hypotension), and histamine H1 inhibition (e.g., sedation and weight
gain) (2).
2-Oxybutynin extended-release (XL) is better tolerated than oxybutynin IR (2).
3-Oxybutynin transdermal system (TDS) has similar efficacy but is better
tolerated than oxybutynin IR presumably because this route avoids first-pass
metabolism in the liver, which generates the metabolite thought to cause adverse
events, especially dry mouth (2).
4-Oxybutynin gel causes significantly less dry mouth than oxybutynin IR (2).
5-Solifenacin succinate and darifenacin are second-generation antimuscarinic
agents. Both have been shown to improve urinary symptoms and quality-of-life (2).
7.1.2.1.2- β3-adrenergic agonists drugs
1-Mirabegron is a β3-adrenergic agonist alternative to
anticholinergic/antimuscarinic drugs for managing UUI (2).
2-Hypertension, nasopharyngitis, urinary tract infection, and headache are the
most common adverse effects (2).
7.1.2.2-Urethral underactivity: stress urinary incontinence (SUI)
Treatment of SUI is aimed at improving urethral closure by:
1-Stimulating α-adrenergic receptors in smooth muscle of the bladder neck and
proximal urethra (α-Adrenergic receptor agonists) (2).
2-Enhancing supportive structures underlying the urethral epithelium (topical
estrogen) (2).
3-Enhancing serotonin and norepinephrine effects in the micturition reflex
pathways (duloxetine) (2).
Drugs for urinary incontinence
Scientific name Trade names Dosage form
1

111
3

Any extra notes:

7.1.3-Nocturnal enuresis
1-Children are generally expected to be dry by a developmental age of 5 years,
and historically it has been common practice to consider children for treatment
only when they reach 7 years; however, symptoms may still persist in a small
proportion by the age of 10 years (4).
2-Initially, advice should be given on fluid intake, diet, toileting behavior. For
children who do not respond to this advice (more than 1–2 wet beds per week), an
enuresis alarm should be the recommended (4).
3-Treatment with oral or sublingual desmopressin is recommended for children
over 5 years of age when alarm use is inappropriate or undesirable, or when rapid
or short-term results are the priority (for example, to cover periods away from
home) (4).
4-Treatment should be assessed after 4 weeks and continued for 3 months if there
are signs of response. Repeated courses of desmopressin can be used in responsive
children who experience repeated recurrences of bedwetting, but should be
withdrawn gradually at regular intervals (for 1 week every 3 months) for full
reassessment (4).
5-Desmopressin dose is taken at bedtime (4). To reduce the risk of water
intoxication, children should drink no more than 240 mL of fluid from 1 hour
before to 8 hours after administration of desmopressin (3).
6-Important : Desmopressin should not be given intranasally for nocturnal
enuresis due to an increased incidence of side-effects (4).
7-Tricyclic antidepressants such as imipramine, are used but relapse is common
after withdrawal. Initial treatment should continue for 3 months; further courses
can be considered following a medical review every 3 months (4).
Drugs for urinary incontinence
Scientific name Trade names Dosage form
1

Any extra notes:

111
7.1.4-Drugs for erectile dysfunction
1-Phosphodiesterase type-5 inhibitors: avanafil, sildenafil, tadalafil and
vardenafil are licensed for the treatment of erectile dysfunction (ED)(4).
2-They have no effect on the penis in the absence of sexual stimulation (5).
(adequate sexual stimulation is needed to trigger the events leading to erection) (6).
3-Adverse effects most commonly reported are related to vasodilatation and
include headache and flushing. Also common are visual disturbances such as
blurred vision (5).
4-Phosphodiesterase type-5 inhibitors may potentiate the hypotensive effects of
nitrates, and are therefore contra-indicated in patients receiving such drugs (5).
5-Adminstraion
A-Onset of effect of sildenafil (but not tadalafil or vardenafil ) may be delayed
if taken with food (4).
B-Dose to be taken (avanafil: 15–30 minutes, sildenafil: 1 hour, tadalafil: at
least 30, and vardenafil 25–60 minutes) before sexual activity (4).
C-Tadalafil is a longer-acting drug. It can be used as required, but can also be
used as a regular lower daily dose to allow for spontaneous (rather than
scheduled) sexual activity or in those who have frequent sexual activity (4).
6-Important :
A-Sildenafil, and tadalafil are licensed for the treatment of pulmonary arterial
hypertension (4) .
B-Tadalafil (5 mg daily) is approved to treat the signs and symptoms of benign
prostatic hyperplasia (4).
Drugs for erectile dysfunction
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.5-Premature ejaculation
Dapoxetine is a short-acting selective serotonin re-uptake inhibitor indicated for
premature ejaculation to be taken approximately 1–3 hours before sexual activity
(4)
.
112
Scientific name Trade names Dosage form
1

Any extra notes:

7.1.6-Other preparations for urinary disorders


7.1.6.1-Alkalinisation of urine
1-The alkalinizing action may relieve the discomfort of cystitis caused by lower
urinary tract infections (4).
2-Prevention of uric acid stones is also an indication for alkalinization of urine
(5)
.
3-Potassium citrate, sodium citrate and sodium bicarbonate are used for this
purpose (4).

Drugs for Alkalinisation of urine


Scientific name Trade names Dosage form
1

Any extra notes:

7.1.6.2-Phenazopyridine and rowatinex®


1-Phenazopyridine exerts an analgesic effect on the mucosa of the urinary tract and
is used to provide symptomatic relief of pain and irritability in conditions such as
cystitis and prostatitis, and urethritis. It is given after food (5). It cause
discoloration of urine (4).
2-Important: If phenazopyridine is given with an antibacterial for the treatment of
urinary-tract infections, treatment should usually not exceed 2 days (2)
(Urinary analgesics may mask signs and symptoms of UTIs not responding to
antimicrobial therapy) (2).
3-A terpene mixture (Rowatinex®) is used for urolithiasis (stone) for the
expulsion of calculi. It is given before food (4).

113
Scientific name Trade names Dosage form

Any extra notes:

7.2-Preparations for vaginal and vulval conditions


7.2.1-Topical hormone replacement therapy for vaginal atrophy
A cream containing an estrogen may be applied on a short-term basis to improve
the vaginal epithelium in menopausal atrophic vaginitis (4).

Scientific name Trade names(if available) Dosage form

Any extra notes:

7.2.2- Vaginal and vulval infections


7.2.2.1-Vaginal fungal infections
1-Vaginal candidiasis is treated primarily with antifungal pessaries or cream
inserted high into the vagina (including during menstruation) (4).
2-Single-dose preparations offer an advantage when adherence is a problem (4).
3-Imidazole drugs (clotrimazole, econazole, fenticonazole and miconazole) are
effective against candida in short courses of 1 to 14 days according to the
preparation used; treatment can be repeated if initial course fails to control
symptoms or if symptoms recur (4).
4-Most internal preparations should be administered at night (this give the drug
time to be absorbed, and eliminate the possibility of accidental loss which is more
likely to occur if the person is mobile) (7).
5-Use the product every day without skipping any days, even during menstrual
flow (8).
6-Oral treatment of vaginal infection (e.g. with fluconazole or itraconazole) is
also effective (4).

114
Antifungals for Vaginal Fungal infections
Scientific name Trade Dosage Treatment course
names form
1

Any extra notes:

7.2.2.2-Other infections
1-Trichomonal infections commonly involve the lower urinary tract as well as the
genital system and need systemic treatment with metronidazole or tinidazole (4).
2-Bacterial infections with Gram-negative organisms are particularly common in
association with gynecological operations and trauma. Metronidazole is effective
against certain Gram-negative organisms, especially Bacteroides spp. and can be
used prophylactically in gynecological surgery (4).
3-Clindamycin cream and metronidazole gel are indicated for bacterial
vaginosis (4).
4-Vaginal preparations intended to restore normal acidity may prevent recurrence
of vaginal infections and permit the re-establishment of the normal vaginal flora (4).
5-The antiviral drugs aciclovir, famciclovir, and valaciclovir can be used in the
treatment of genital infection due to herpes simplex virus (4).

Scientific name Trade names Dosage form

Any extra notes:

115
7.3-Drugs used in obstetrics
7.3.1-Tocolytics (myometrial relaxants)
1-Tocolytics inhibit uterine contractions and are used in premature labour to
delay early delivery (5).
2-The oxytocin receptor antagonist, atosiban (5), is licensed for the inhibition of
uncomplicated premature labour between 24 and 33 weeks of gestation (4).
3-The dihydropyridine CCB nifedipine is also used (5).
4-The beta2 agonists salbutamol and terbutaline sulfate are no longer
recommended for inhibiting uncomplicated premature labour (4).

Scientific name Trade names Dosage form

Any extra notes:

7.3.2-Induction and augmentation of labour


1-Oxytocin is administered by slow intravenous infusion, using an infusion pump,
to induce or augment labour (4).
2-Dinoprostone is available as vaginal tablets, pessaries and vaginal gels for the
induction of labour (4).
3-Mifepristone and misoprostol (vaginally) can be given for the induction of
labour (4).

Drugs for Induction and augmentation of labour


Scientific name Trade names Dosage form
1

Any extra notes:

7.3.3-Termination of pregnancy
1-Gemeprost, a prostaglandin administered vaginally as pessaries, is licensed for
the medical induction of abortion in the second trimester of pregnancy (4).

116
2-The prostaglandin misoprostol is given by mouth, buccally, sublingually, or
vaginally, to induce medical abortion (4).
3-Pre-treatment with mifepristone can facilitate the process of medical abortion.
It sensitizes the uterus to subsequent administration of a prostaglandin and,
therefore, abortion occurs in a shorter time and with a lower dose of prostaglandin
(4)
.
Drugs for Termination of pregnancy
Scientific name Trade names Dosage form
1

Any extra notes:

7.3.4-Prevention and treatment of uterine hemorrhage


1-If the uterus fails to contract adequately after delivery (uterine atony), or if
retained placental remnants prevent retraction of the placental bed, postpartum
hemorrhage may occur. These two causes account for about 80% of cases of
postpartum hemorrhage (5).
2-Postpartum hemorrhage may be fatal to the mother unless promptly dealt with,
and management generally involves:
• removal of the placenta if it has not been expelled.
• the use of oxytocics to contract the uterus.
• transfusion if blood loss is severe (5).
3-Prophylactic oxytocin is given by intramuscular injection. Alternatively,
ergometrine with oxytocin can be given by intramuscular injection in the absence
of hypertension (4).
4-Oxytocic drugs are used to treat postpartum haemorrhage caused by uterine
atony; treatment options include oxytocin, ergometrine maleate, or a combination
of ergometrine with oxytocin. Carboprost and misoprostol are alternative options
(4)
.
Scientific name Trade names Dosage form

Any extra notes:

117
7.4-Hormonal contraceptives
7.4.1-Combined oral contraceptives (COCs)
1-COCs are a combination of estrogen (prevent the development of the dominant
follicle) and progestin (prevent ovulation) (6).
2-The COCs are available in a variety of cycle lengths.
The most common is the 28-day pack that contains 21
days of active pills (pills that contain estrogen and
progestin) followed by 7 days of placebo pills (to
minimize confusion) the patient takes one pill daily. After
taking the last pill of a 28-day pack, the patient should
begin a new pack the next day (6).
3-Combined oral contraceptives containing a fixed amount
of an estrogen and a progestogen in each active tablet are termed ‗monophasic’;
those with varying amounts of the two hormones are termed ‗multiphasic’ (4).
4-A transdermal patch and a vaginal ring, both containing an estrogen with a
progestogen, are also available (4).
5-The majority of combined oral contraceptives contain ethinylestradiol as the
estrogen component; mestranol and estradiol are also used (4).
6-Dosing for the drug class:
A-In the first-day start method, women take the first pill on the first day of
the next menstrual cycle (2).
B-If reasonably certain woman is not pregnant, first course can be started on
any day of cycle—if starting on day 6 of cycle or later, additional precautions
(barrier methods) necessary during first 7 days (4).
C-Each tablet should be taken at approximately same time each day; if
delayed, contraceptive protection may be lost (4).
D-21-day combined preparations, 1 tablet daily for 21 days; subsequent
courses repeated after a 7-day interval (during which withdrawal bleeding
occurs) (4).
E-Every day (ED) combined preparations, 1 active tablet daily for 21 days,
followed by 1 inactive or iron tablet daily for 7 days; subsequent courses
repeated without interval (withdrawal bleeding occurs when inactive tablets
being taken) (4).
(Some product needed to be taken as 1 active tablet once daily for 24 days,
followed by 1 inactive tablet once daily for 4 days) (4).
7-Interactions:
Women using combined hormonal contraceptive patches, vaginal rings or oral
tablets who require enzyme inducing drugs or griseofulvin should be advised
to change to a reliable contraceptive method that is unaffected by enzyme-
inducers, such as some parenteral progestogen-only contraceptives or intra-
118
uterine devices. This should be continued for the duration of treatment and for
four weeks after stopping (4).
8-COCs have benefits aside from pregnancy prevention that include treatment of
acne, hirsutism, premenstrual syndrome (PMS), menstrual cycle regulation (6).
9-Diarrhea and vomiting:
A-Vomiting and persistent, severe diarrhea can interfere with the absorption of
combined oral contraceptives. It is recommended to follow the instructions
for missed pills if vomiting occurs within 3 hours of taking a combined oral
contraceptive or severe diarrhea occurs for more than 24 hours (4).
B-Use of non-oral contraception should be considered if diarrhea or
vomiting persist (4).

7.4.2-Progestogen-only contraceptives
7.4.2.1-Oral progestogen-only contraceptives
1-Advantages
A-Progestin-only contraceptives are alternative agents for women with
contraindications to COCs (6).
B-Confusion with pill taking is minimized because there is no placebo week
and all 28 pills in each pack are the same (6).
2-Disadvantage
They must be taken even more regularly than COCs (6) starting on day 1 of
the cycle then continuously, dose is to be taken at the same time each day, if
administration delayed for 3 hours or more it should be regarded as a "missed
pill (4).
3-Interactions:
The efficacy of oral progestogen-only preparations is reduced by enzyme-
inducing drugs or griseofulvin and an alternative contraceptive method,
unaffected by the interacting drug, is recommended during treatment with an
interacting drug and for at least 4 weeks afterwards (4).
7.4.2.2-Parenteral progestogen-only contraceptives
Injectable medroxyprogesterone acetate is given as a 150-mg intramuscular
injection repeated every 12 weeks. First dose to be administered within the first 5
days of cycle or within first 5 days after parturition (delay until 6 weeks after
parturition if breast-feeding) (4).
7.4.3-Emergency hormonal contraception
1-Hormonal emergency contraceptives include levonorgestrel and ulipristal ;
either drug should be taken as soon as possible after unprotected intercourse to
increase efficacy (4).
2-Levonorgestrel is effective if taken within 72 hours (3 days) of unprotected
intercourse. Ulipristale, is effective if taken within 120 hours (5 days) of
unprotected intercourse (4).
119
7.4.4-Use of oral contraceptives during breast-feeding
1-The American College Of Gynecology (ACOG) recommends waiting at least 6
weeks before starting any estrogen-containing contraceptive regardless of
breast-feeding status (by this time, the increased risk of thrombosis that occurs
during pregnancy should be reduced to baseline). However, COCs have been
reported to decrease milk quantity and quality. Therefore, many providers suggest
avoiding COCs in women who are exclusively breastfeeding (6).
2-For non–breast-feeding women, a progestin-only contraceptive may be used
immediately postpartum and 6 weeks postpartum if solely breast-feeding and in
some cases 3 weeks postpartum if partially breast-feeding (6).

Hormonal contraceptives
Scientific name Trade names Dosage form
1

Any extra notes:

7.5-Spermicidal contraceptives (nonoxinol ‘9’)


1-Nonoxynol-9, a surfactant that destroys the cell membranes of sperm, is the most
commonly used spermicide (3).
2-Nonoxynol-9 is available in a variety of forms, including a cream, foam, film,
gel, and suppository (3).
3-To be used most effectively, spermicides must be placed in the vagina not more
than 1 hour prior to sexual intercourse, and they must come in contact with the
cervix (3).

121
4-Spermicides may be used alone, with a barrier method, or adjunctively with
other forms of contraceptives to provide additional protection against unwanted
pregnancy (3). However, they are generally considered relatively ineffective when
used as the sole method of contraception, and such use is not recommended (5).
Scientific name Trade names Dosage form
1

Any extra notes:

References
1-NAPLEX® Review Guide, Fourth Edition. Copyright © 2021 by McGraw-Hill.
2-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021
3-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
4-BNF-81 (2021).
5-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
6-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
7-Paul Rutter. Community Pharmacy. Symptoms, Diagnosis and Treatment. 5th
edition. 2021
8-American pharmacists association. Handbook of Non-prescription drugs: An
Interactive Approach to Self-Care. 18th edition. 2016.

121
Chapter Nine: Nutrition and Blood
9.1-Iron deficiency anemia
Treatment with an iron preparation is justified only in the presence of a
demonstrable iron-deficiency state. Prophylaxis with an iron preparation may be
appropriate in some conditions (1).
9.1.1-Oral iron
1-The oral dose of elemental iron for iron-deficiency anemia should be 100 to 200
mg daily (1). Table 9-1: Iron content of different iron
2-When the hemoglobin is in the salts (1).
normal range, treatment should be
continued for a further 3 months
to replenish the iron stores (1).
3-The iron content of various
iron salts is tabulated in the table
9-1 (1).
4-Administer iron on an empty
stomach (1 hour before or 2 hours
after a meal) is preferred for maximal absorption. If patients develop intolerable
GI side effects (ie, heartburn, nausea, bloating) after taking iron on an empty
stomach, they should be advised to take it with meals (2).
5-The patient should be told that oral iron therapy produces dark stools (3).
6-Oral iron preparations sometimes produces gastrointestinal irritation and
abdominal pain with nausea and vomiting. Adverse effects can be reduced by
giving it with or after food (rather than on an empty stomach) or by beginning
therapy with a small dose and increasing gradually (4).
7-Important: Oral Liquid preparations containing iron salts should be well
diluted with water and swallowed through a straw to prevent discoloration of
the teeth (4).
8-Modified-release preparations of iron have no therapeutic advantage and
should not be used (1).
9-Iron should be stored in a safe place, inaccessible to young children.
Accidental ingestion of even small amounts (three to four tablets) of oral iron can
cause serious consequences in small children (3).
10-Some oral preparations contain ascorbic acid to aid absorption of the iron but
the therapeutic advantage of such preparations is minimal (1).
11-Preparations containing iron and folic acid are used during pregnancy in
women who are at high risk of developing iron and folic acid deficiency (1).

122
12-Potentially clinically significant drug–drug interactions involving iron
products include fluoroquinolones, tetracyclines, and mycophenolate mofetil.
Iron decreases the absorption of these drugs (2).
Oral iron (including combination products)
Scientific name Trade names Dosage form
1

Any extra notes:

9.1.2-Parenteral iron
1-Parenteral iron (Table 9-2) (5) (e.g. iron dextran, iron sucrose) is generally
reserved for use when oral therapy is unsuccessful because the patient cannot
tolerate oral iron, or does not take it reliably, or if there is continuing blood loss, or
in malabsorption (1).
2-Parenteral iron may also have a role in the management of chemotherapy-
induced anemia. Many patients with chronic renal failure who are receiving
hemodialysis also require parenteral iron (1).
3-Depending on the preparation used, parenteral iron is given as a total dose or in
divided doses (1).
4-With the exception of patients with severe renal failure receiving haemodialysis,
parenteral iron does not produce a faster hemoglobin response than oral iron
provided that the oral iron preparation is taken reliably and is absorbed adequately
(1)
.
5-Anaphylactoid reactions occur in less than 1% of patients treated with
parenteral iron therapy and are more commonly associated with iron dextran
than with iron sucrose (3).
6-Test dose for iron dextran: the recommendation is differs between UK and
USA:
A-USA: Because of the potential for anaphylaxis with iron dextran, an IM or
IV test dose should be given. The test dose for adults is 25 mg of iron dextran.
A period of 1 hour or longer should elapse before the remaining portion of the

123
initial dose be given. Subsequent use of test doses should be considered during
iron dextran therapy but is not required (3).
B-UK: Test doses are no longer recommended and caution is needed with
every dose of intravenous iron (1).
Table 9-2. Parental iron products (5).

Parenteral iron
Scientific name Trade names Dosage form
1

Any extra notes:

9.2-Epoetins
1-Epoetins (recombinant human erythropoietins) are used to treat the anemia
associated with erythropoietin deficiency in chronic renal failure, and to shorten
the period of symptomatic anemia in patients receiving cytotoxic chemotherapy
(1)
.
2-Darbepoetin alfa is a derivative of epoetin; it has a longer half-life and can be
administered less frequently than epoetin (1).
3-Methoxy polyethylene glycol-epoetin beta is a continuous erythropoietin
receptor activator that is licensed for the treatment of symptomatic anemia
associated with chronic kidney disease. It has a longer duration of action than
epoetin (1).

124
4-The most common adverse effect seen with erythropoiesis-stimulating agents
(ESAs) is increased blood pressure, which may require antihypertensive agents
to control blood pressure (2).
Epoetins
Scientific name Trade names Dosage form
1

Any extra notes:

9.3-Megaloblastic anemia
Most megaloblastic anemias result from a lack of either vitamin B12 or folate and
treated accordingly (1).
9.4-Sickle-cell anemia
Hydroxycarbamide (Hydroxyurea) can reduce the frequency of crises and the
need for blood transfusions in sickle-cell disease. The beneficial effects of
Hydroxyurea may not become evident for several months (1).
9-Glucose 6-phosphate dehydrogenase (G6PD) deficiency
1-Individuals with G6PD deficiency are susceptible to developing acute
hemolytic anemia when they take a number of common drugs (Table 9-3) (1).
Table 9-3: Drugs with definite and possible risk of hemolysis in some G6PD-
deficient individuals (1).
Drugs with definite risk of hemolysis in most Drugs with possible risk of
G6PD-deficient individuals hemolysis in some G6PD-
deficient individuals
. Dapsone and other sulfones (higher doses for
dermatitis herpetiformis more likely to cause problems) . Aspirin (acceptable up to a dose
. Methylthioninium chloride of at least 1 g daily in most G6PD-
. Niridazole deficient individuals)
. Nitrofurantoin . Chloroquine (acceptable in acute
. Pamaquin malaria and malaria
. Primaquine (30 mg weekly for 8 weeks has been found chemoprophylaxis)
to be without undue harmful effects in African and . Menadione, water-soluble
Asian people) derivatives (e.g. menadiol sodium
. Quinolones (including ciprofloxacin, moxifloxacin, phosphate)
nalidixic acid, norfloxacin, and ofloxacin). . Quinidine (acceptable in acute
. Rasburicase malaria)
. Sulfonamides (including co-trimoxazole; some . Quinine (acceptable in acute
sulfonamides, e.g. sulfadiazine, have been tested and malaria)
found not to be hemolytic in many G6PD-deficient . Sulfonylureas
individuals)

125
9.6-Folic acid
1-Prevention of neural tube defects (NTD):
A-Folic acid supplements taken before and during pregnancy can reduce the
occurrence of neural tube defects (4).
B-For women of child-bearing potential at high risk
of having a pregnancy affected by NTD ( e.g. if they
have had a previous pregnancy affected by a neural
tube defect), the dose of folic acid is 4 or 5 mg daily
starting before pregnancy (in the USA the
recommendation is 4 weeks before) and continued
through the first trimester (until week 12 of pregnancy)
(4)
.
C-For women at a low risk of having a child with a
NTD the dose is 400 micrograms daily and continued through the first
trimester (until week 12 of pregnancy) (4).
2-Other indications for folic acid include (1):
A-Folate-deficient megaloblastic anemia.
B-Prevention of methotrexate-induced side-effects (dose to be taken on a
different day to methotrexate dose).
C-Prophylaxis of folate deficiency in dialysis.
Scientific name Trade names Dosage form
Folic acid

Any extra notes:

9.7-Minerals and Electrolyte


9.7.1-Calcium supplements
1-Calcium salts are used in the management of hypocalcaemia and calcium
deficiency states resulting from dietary deficiency or ageing (4).
2-Intravenous calcium (e.g. calcium gluconate) salts are also used to reverse the
toxic cardiac effects of potassium in the emergency treatment of severe
hyperkalemia (calcium act to protect the heart from hyperkalemia) (4).
3-Intravenous calcium gluconate is given by slow intravenous injection or
infusion (risk of arrhythmias if given too rapidly). Calcium chloride injection is
also available, but is more irritant; care should be taken to prevent extravasation
(1)
.
4-Calcium carbonate or acetate are effective phosphate binders and are given
orally (with food) to reduce phosphate absorption from the gut in patients with
126
hyperphosphataemia; this is particularly relevant to patients with chronic renal
failure (4). In general, calcium-containing phosphate binders (CCPBs) should not
be used if corrected serum calcium levels are near or above the upper end of
the normal range or if arterial calcifications are present (2).
5-Oral calcium supplements can also be used as an adjunct in the management of
osteoporosis (4).
9.7.2-Phosphate-binding agents
1-When serum phosphorus levels cannot be controlled by restriction of dietary
intake, phosphate-binding agents are used to bind dietary phosphate in the GI
tract to form an insoluble complex that is excreted in the feces (these agents
should be administered with each meal) (2).
2-Calcium-containing preparations are used as phosphate-binding agents in
the management of hyperphosphataemia complicating renal failure (1).
3-Sevelamer and lanthanum is licensed for the treatment of hyperphosphataemia
in patients with chronic kidney disease (1). Sevelamer and lanthanum phosphate
binders do not contain calcium, iron, or aluminum. These agents are particularly
useful in patients with hyperphosphatemia who have elevated serum calcium
levels. The most common side effects of sevelamer are GI complaints including
nausea, constipation, and diarrhea (2).
4-Sucroferric oxyhydroxide and ferric citrate are iron-based phosphate binders
that lower phosphate levels. Ferric citrate can also increase serum ferritin (2).
9.7.3-Potassium
1-Potassium salts are used for the prevention and treatment of hypokalaemia (4).
2-An intravenous potassium salt (KCL) may be required in severe acute
hypokalaemia (4).
3-When i.v potassium is added to i.v fluid, it is important to mix thoroughly; if
the solutions are not thoroughly mixed a concentrated layer of potassium chloride
may form (layering effect) owing to differences in density. If such a mixture is
administered it may have a serious effect (1).
4-Calcium or sodium polystyrene sulfonate are cation exchange resins given (by
mouth or by rectum) to treat hyperkalemia associated with anuria or severe
oliguria, and in dialysis patients (1).
9.7.4-Zinc
1-Zinc supplement is used for zinc deficiency (1).
2-Zinc supplements have been shown to reduce the incidence, intensity, or duration
of acute diarrhea in children in developing countries (6).
3- Zinc prevents the absorption of copper in Wilson’s disease (1).
9.7.5-Magnesium
Magnesium is indicated for (1):
127
1-Hypomagnesaemia.
2-Emergency treatment of serious arrhythmias (torsade de pointes).
3-Severe acute asthma.
4-Prevention and treatment of seizures in pre-eclampsia.
5-Rapid bowel evacuation (by mouth).
9.7.6-Selenium
Selenium deficiency can occur as a result of inadequate diet or prolonged
parenteral nutrition. A selenium supplement should not be given unless there is
good evidence of deficiency (1).
Minerals and Electrolyte
Scientific name Trade names Dosage form
1

Any extra notes:

9.8-Vitamins
9.8.1-Vitamin A:
1-Vitamin A, a fat-soluble vitamin, is essential for growth, for the development
and maintenance of epithelial tissue, and for vision (4).
2-Vitamin A is used in the treatment and prevention of vitamin A deficiency.
Vitamin A has also been used to treat various skin disorders including acne
and psoriasis (4).
3-In view of evidence suggesting that high levels of vitamin A may cause birth
defects (teratogenic), women who are (or may become) pregnant are advised not
to take vitamin A supplements ( except on the advice of a doctor ); nor should
they eat liver (1).
4-The Royal College of Obstetricians and Gynaecologists has advised that high -
dose vitamin A supplementation (more than 2300 units daily) is not
recommended during pregnancy. The Australian Adverse Drug Reactions
Advisory Committee has advised women in this category to avoid vitamin A
supplements and to not exceed the recommended daily allowance of 2500 units
from all sources (4).

9.8..2-Vitamin B Substances (Table 9-4)

128
Table 9-4: Vitamin B substance and their uses
Vit. B Scientific name Uses
B1 Thiamine Thiamine is used in the treatment and prevention
of thiamine deficiency (4).
B2 Riboflavin Riboflavin is used in the treatment and prevention
of riboflavin deficiency (4).
Pyridoxine is used in:
-Treatment and prevention of pyridoxine
B6 Pyridoxine deficiency states (4).
-Prevention of isoniazid-induced neuropathy (4).
-Treatment of premenstrual syndrome (4).
-Indicated in both idiopathic acquired and
hereditary sideroblastic anemias (1).
-Vitamin B12 is used in the treatment and
B12 Cobalamins prevention of vitamin B12 deficiency (4).
-Treatment of B12- deficient megaloblastic
anemias (4).
9.8.3-Vitamin C (Ascorbic acid)
Vitamin C (ascorbic acid) therapy is essential in scurvy. Claims that vitamin C
ameliorates colds or promotes wound healing have not been proved (1).
9.8.4-Vitamin D
1-The term Vitamin D is used for a range of compounds which possess the
property of preventing or curing rickets. They include ergocalciferol (calciferol,
vitamin D2), colecalciferol (vitamin D3), alfacalcidol (1-α
(1)
hydroxycholecalciferol), and calcitriol (1,25-dihydroxycholecalciferol) .
2-Vitamin D requires hydroxylation by the kidney to its active form, therefore the
hydroxylated derivatives alfacalcidol or calcitriol should be prescribed if
patients with severe renal impairment require vitamin D therapy (1).
3-Preparations containing calcium with Vitamin D are available for the
management of combined calcium and vitamin D deficiency (1).
9.8.5-Vitamin E
1-Vitamin E is used in the treatment and prevention of vitamin E deficiency (4).
2-Vitamin E has been tried for various other conditions but there is little
scientific evidence of its value (1).
9.8.6-Vitamin K
1-Vitamin K is necessary for the production of blood clotting factors (1).
2-Vitamin K compounds are used in the treatment and prevention of hemorrhage
associated with vitamin K deficiency (4).
3-Because vitamin K is fat soluble, patients with fat malabsorption, especially in
biliary obstruction or hepatic disease, may become deficient. Menadiol sodium

129
phosphate is a water-soluble synthetic vitamin K derivative that can be given
orally to prevent vitamin K deficiency in malabsorption syndromes (1).
9.8.7-Multivitamin preparations
1-It is generally considered that healthy persons eating a normal balanced diet
should have no need for vitamin supplementation (4).
2-Supplementation should concentrate on groups of people at risk of deficiency
such as pregnant and lactating women, who need calcium, folic acid, and iron; and
certain groups who need vitamin D. A multivitamin supplement might be
considered for some groups such as the elderly and those with reduced calorie
intake (4).
Vitamins
Scientific name Trade names Dosage form
1

10

Any extra notes:

9.9-Fluid management
1-Solutions of electrolytes are given intravenously, to meet normal fluid and
electrolyte requirements or to replace substantial deficits or continuing losses (1).
2-Crystalloids are intravenous fluids that can contain water, sodium (Na+),
chloride (Cl), and other electrolytes (5).

131
3-Colloids include packed red blood cells, pooled human plasma (5% albumin,
25% albumin, and 5% plasma protein fraction), semisynthetic glucose polymers
(dextran), and semisynthetic hydroxyethyl starch (hetastarch) (5).
4-Crystalloids (0.9% sodium chloride or lactated Ringer solution) are
recommended for fluid resuscitation in hypovolemia. The lactate in lactated Ringer
solution is metabolized to bicarbonate, and it can theoretically be useful for
metabolic acidosis (5).
6-Colloids can be considered after fluid resuscitation with crystalloid (usually 4–6
L) has failed to achieve hemodynamic goals or after clinically significant edema
limits the further administration of crystalloid (5).
Fluids
Trade names Composition
1

Any extra notes:

10.10-Dietary supplement
Dietary supplements (DS) as products intended to supplement the diet that contain
one or more of the following dietary ingredients: vitamins, minerals, herbs or
other botanicals, and amino acids (6). Some of the dietary supplements and their
uses are summarized in (Table 9-5) (7).
Table 9-5: Some of the dietary supplements and their uses (7).
DS Uses
1 Caffeine Increased alertness, wakefulness.
2 Chamomile GI antispasmodic, calmative, anti-inflammatory.
Pain relief from osteoarthritis, maintenance of joint
3 Chondroitin
cartilage.
4 Cinnamon Antimicrobial, antidiabetic agent, antioxidant.
5 Coconut oil Alzheimer‘s disease.
Antioxidant activity for several disorders, particularly
cardiovascular disease (e.g., cardiomyopathy, heart
6 CoQ-10
failure, hypertension), HIV, and Parkinson‘s disease;
prevention of statin-induced myopathy.
131
7 Cranberry Prevention of urinary tract infections.
Improves muscle strength, athletic performance, and
8 Creatine
recovery during exercise.
Dehydroepiand ―Anti-aging,‖ muscle building, libido booster,
rosterone, perimenopausal symptoms.
9
better known
as DHEA
Immune system booster, treatment of the common cold,
10 Echinacea prevention and treatment of minor upper respiratory
infections.
Pain and inflammation; headache, including migraine
11 Feverfew
treatment and prophylaxis.
Cardioprotectant, Anti-inflammatory, diabetes,
12 Flaxseed oil
menopause, hyperlipidemia.
Treatment of hyperlipidemia; treatment of high blood
13 Garlic
pressure; antiseptic agent.
Treatment and management of nausea, motion sickness,
14 Ginger chemotherapy-related nausea, postoperative nausea,
pregnancy-related nausea.
Memory enhancer, cerebrovascular insufficiency
15 Ginkgo biloba (dementia, memory impairment), vertigo, tinnitus,
peripheral vascular disease (intermittent claudication).
16 Ginseng Improved well-being, energy boost, stress relief.
Pain relief from osteoarthritis, maintenance of joint
17 € Glucosamine
Function.
Promotion of sleep, prevention of symptoms of jet lag,
18 Melatonin
treatment of insomnia.

Hepatoprotectant for hepatitis, cirrhosis, and other liver


19 Milk thistle diseases; treatment of toxicity due to Amanita mushroom
poisoning.

Treatment of uncomplicated diarrhea, particularly that


caused by modification of intestinal flora by antibiotic
20 Probiotics therapy; diarrhea due to infections; ulcerative colitis;
patients with colostomies with diarrhea or constipation;
spastic diarrhea; bacterial vaginosis.
21 Saw palmetto Symptoms of benign prostatic hypertrophy (BPH)
22 St. John’s wort Mild-to-moderate depression.
23 € Valerian Sleep aid, insomnia caused by anxiety, restlessness.

132
References
1-BNF-81 (2021).
2-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
3-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
4-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
5-ACCP Updates in Therapeutics® 2021: The Pharmacotherapy Preparatory
Review and Recertification Course.
6-American pharmacists association. Handbook of Non-prescription drugs: An
Interactive Approach to Self-Care. 18th edition. 2016.
7-Michael AM, Jason. Frequently prescribed medications. Third edition 2019.

133
Chapter Ten: Musculoskeletal and Joint Diseases
10.1-Drugs for rheumatoid arthritis (RA), osteoarthritis (OA), and
other related disorders
1-The following medication classes are prescribed commonly for the treatment of
RA:
A-Non-steroidal anti-inflammatory drugs (NSAIDs).
B-Glucocorticoids.
C-Conventional synthetic Disease-Modifying Antirheumatic Drugs
(csDMARDs). Commonly used agents include methotrexate (MTX),
sulfasalazine, hydroxychloroquine, and leflunomide (1, 2).
D-Biologic DMARDs.
E- JAK inhibitors include (baricitinib, tofacitinib, and upadacitinib) (1).
2-DMARDs are the mainstay of RA treatment (3). Current RA treatment
guidelines recommend initiating conventional DMARDs irrespective of disease
activity once a diagnosis is established (1).
3-Because DMARDs may take 2 to 6 months to reach full effect, NSAIDs and
sometimes glucocorticoids can be used in the interim to reduce pain and swelling
(2)
.
4-Biologic DMARDs are indicated in patients who have received an adequate trial
of nonbiologic DMARD monotherapy or combination therapy but have failed to
achieve treatment goals (3).
5-The following medications are used for the treatment of OA (1):
A-Acetaminophen
B-NSAIDs
C-Topical Therapies (Capsaicin, NSAIDs)
E-Duloxetine and tramadol
F-Glucosamine and Chondroitin
G-Intraarticular (IA)Therapy (corticosteroids, hyaluronic acid derivatives).
10.1.1-Conventional synthetic DMARDs
1-Regular monitoring of DMARD therapy is essential because of the risk of liver
and haematological toxicity. (e.g. liver function test to detect hepatotoxicity and
complete blood count (CBC) to detect bone marrow suppression) (3).
2-The patient is warned to report immediately the onset of any feature of blood
disorders (e.g. sore throat, bruising, and mouth ulcers), liver toxicity (e.g. nausea,
vomiting, abdominal discomfort, and dark urine) (4).
3-Concerning Methotrexate:
A-Methotrexate (MTX) is the most commonly used DMARD because of its
oral, once-weekly administration, well defined safety profile (when monitored
appropriately), demonstrated efficacy, and low cost (2, 3).
134
B-Other uses for MTX include: IBD, neoplastic diseases, and severe psoriasis
(5)
.
C-It is usually given once weekly (4).
D- In patients who experience mucosal or gastro-intestinal side-effects with
methotrexate, folic acid given every week [unlicensed indication], on a different
day from the methotrexate, may help to reduce the frequency of such side-effects
(4)
.
E-Withdraw treatment if stomatitis or diarrhea develops—may be first sign of
gastro-intestinal toxicity (4).
F-Folinic acid following methotrexate administration helps to prevent
methotrexate-induced mucositis and myelosuppression. Treatment with folinic
acid (as calcium folinate) may be required in acute toxicity (4).
G-Pulmonary toxicity may be a special problem in rheumatoid arthritis (warn
patient to seek medical attention if dyspnoea, cough or fever develop); monitor
for symptoms at each visit—discontinue if pneumonitis suspected (4).
4-Concerning hydroxychloroquine:
A-Periodic ophthalmologic examinations are necessary for patients taking
hydroxychloroquine for early detection of reversible retinal toxicity (1)
C-To avoid excessive dosage in obese patients, the dose of
hydroxychloroquine should be calculated on the basis of ideal body-weight (4).
D-Hydroxychloroquine should be taken with or just after meal (4).
5-Concerning leflunomide:
A-Patients should be advised not to drink alcohol for as long as they are
receiving leflunomide (4).
B-Washout procedure: The active metabolite persists for a long period; to aid
drug elimination in case of serious adverse effect, or before starting another
DMARD, or before conception, stop treatment and give either colestyramine or
charcoal, activated. Procedure may be repeated as necessary (4).
6-Concerning penicillamine:
A-In addition to RA, it is used also for cystinuria (therapeutic and prophylaxis),
aids the elimination of copper ions in Wilson’s disease, and for autoimmune
hepatitis (used rarely; after disease controlled with corticosteroids) (4).
B-Patients who are hypersensitive to penicillin may react rarely to penicillamine
(4)
.
C-Proteinuria: Proteinuria occurs in up to 30% of patients—can be a sign of
immune mediated nephropathy. Discontinue immediately if nephrotoxicity
occurs (4).

135
D-Counselling on the symptoms of blood disorders is advised. Warn patient and
carers to tell doctor immediately if sore throat, fever, infection, non-specific
illness, unexplained bleeding and bruising, purpura, mouth ulcers, or rashes
develop (4).
DMARDs
Scientific name Trade names Dosage form
1

Any extra notes:

10.1.2-Non-steroidal anti-inflammatory drugs (NSAIDs)


1-NSAIDs have analgesic, anti-inflammatory, and antipyretic properties.
NSAIDs are used for the relief of mild to moderate pain, minor febrile conditions,
and for acute and chronic inflammatory disorders such as osteoarthritis, and
rheumatoid arthritis (5).
2-Some NSAIDs are applied topically for the relief of muscular and rheumatic
pain, and some (like diclofenac) are used in ophthalmic preparations for ocular
disorders (4).
3-In single doses NSAIDs have analgesic activity. In regular full dosage NSAIDs
have both a lasting analgesic and an anti-inflammatory effect (4).
4-Differences in anti-inflammatory activity between NSAIDs are small, but there is
considerable variation in individual response and tolerance to these drugs. About
60%of patients will respond to any NSAID; of the others, those who do not
respond to one may well respond to another (4).
5-Pain relief starts soon after taking the first dose and a full analgesic effect
should normally be obtained within a week, whereas an anti-inflammatory effect
may not be achieved (or may not be clinically assessable) for up to 3 weeks. If
appropriate responses are not obtained within these times, another NSAID should
be tried (4).

136
6-The commonest adverse effects of NSAIDs are generally GI disturbances,
such as GI discomfort. These are usually mild and reversible but in some patients
peptic ulceration and severe GI bleeding may occur (5).
7-They vary in their selectivity for inhibiting different types of cyclo-oxygenase
(COX); selective inhibitors of COX-2 (celecoxib, etoricoxib and parecoxib) are
associated with less GI intolerance. This advantage may be lost in patients who
require concomitant low-dose aspirin (4).
Aceclofenac, diclofenac, etodolac, ibuprofen, indometacin, ketoprofen, mefenamic
acid, meloxicam, naproxen, piroxicam, sulindac and tenoxicam are examples of
non-selective COX-2inhibitors (4).
8-The combination of a NSAID and low-dose aspirin can increase the risk of
GI side-effects; this combination should be used only if absolutely necessary (4).
9-Systemic as well as local effects of NSAIDs contribute to GI damage; taking
oral formulations with milk or food, or using enteric-coated formulations, or
changing the route of administration may only partially reduce symptoms such
as dyspepsia (4).
10-Patients at risk of GI ulceration (including the elderly), who need NSAID
treatment should receive gastroprotective treatment (4) (e.g. PPIs) (3).
11-All NSAID use (including COX-2 selective inhibitors) can, to varying degrees,
be associated with a small increased risk of thrombotic events (e.g. myocardial
infarction and stroke); however, the greatest risk may be in those receiving high
doses long term. COX-2 selective inhibitors, diclofenac (150mg daily) are
associated with an increased risk of thrombotic events. The increased risk for
diclofenac (and hence aceclofenac) is similar to that of licensed doses of etoricoxib
(4)
.
12- Naproxen (1 g daily) is associated with a lower thrombotic risk, and low doses
of ibuprofen (1.2 g daily or less) have not been associated with an increased risk of
myocardial infarction (4).
13-It is preferable to avoid NSAIDs in patients with active or previous gastro-
intestinal ulceration or bleeding and patients with a history of hypersensitivity to
aspirin or any other NSAID. Celecoxib is contra-indicated in patients with
sulfonamide sensitivity (4).
14-NSAIDs should be used with caution in patients with asthma, and
hypertension (it cause sodium and water retention) (5).

15-Important: Use of more than one NSAID together should be avoided


because of the increased risk of adverse effects (5).
16-Indometacin use associated with a high incidence of side-effects including
headache, dizziness [may affect performance of skilled tasks (e.g. driving)], and
GI disturbances. Mefenamic acid has occasionally been associated with diarrhea
which require discontinuation of treatment. Piroxicam has more GI side effects
137
than most other NSAIDs, and is associated with more frequent serious skin
reactions. (4).
17-Accordig to its leaflet, Olfen® 50/100mg rectocaps is given before meals.
NSAIDs
Scientific name Trade names Dosage form
1

10

11

12

Any extra notes:

10.1.3-Glucosamine and chondroitin


1-The glucosamine sulfate and chondroitin sulfate are dietary supplements (1).
Both compounds are found naturally in the body and are essential to the formation
of cartilage (6).
2-The combination is believed to have a synergistic effect by stimulating
cartilage production(glucosamine) and inhibiting its destruction (chondroitin) (7)
but convincing evidence for this effect is lacking (2).

138
3-Indicated for symptomatic relief of mild to moderate osteoarthritis of the knee
(4)
.
4-Glucosamine and/or chondroitin lack uniform efficacy and are not preferred
treatment options (1) (any true clinical value remains to be shown)(2)
(Glucosamine is not recommended for the treatment of osteoarthritis) (4).
Glucosamine and chondroitin
Scientific name Trade names Dosage form

Any extra notes:

10.1.4-Intraarticular (IA) hyaluronic acid derivatives


1-Hyaluronic acid derivatives are intended to improve elasticity and viscosity of
synovial Fluid (7).

2-However, IA hyaluronic acid is not routinely recommended for knee OA pain


(Limited efficacy and risks of serious events limit the routine use of these agents)
(1)
(are not recommended) (4). Injections do not provide clinically meaningful
improvement and may be associated with serious adverse events (e.g., increased
pain, joint swelling, and stiffness) (1).

3-A new hyaluronan preparation (Monovisc®) has been developed, containing 4


or 5 times the amount of hyaluronan used in the usual knee injection. It is
designed to treat the symptoms of osteoarthritis with only one injection. The
approach, if effective, would simplify the procedure especially for ―needle shy‖
patients (2).

Hyaluronic acid derivatives


Scientific name Trade names Dosage form
1

Any extra notes:

139
10.1.5-Biologic DMARDs
1-Five of the available biologic agents are inhibitors of TNF-α: infliximab,
etanercept , adalimumab, golimumab, and certolizumab (8). Non-TNF agents are:
abatacept, anakinra, tocilizumab, Sarilumab, and rituximab (1).

2-These drugs are administered parenterally (Sc or I.V) (1).

3-Treatment costs are much higher than with DMARDs and many countries have set
guidelines restricting their use to patients who have active disease despite having
had an adequate trial of standard therapies (9).
4-Because of immunosuppressive effects:
A-Patients taking biologics should notify their providers if they are being treated
for an infection or plan to undergo major surgery. Treatment may need to be
held until appropriate postsurgical healing and/or resolution of infection can be
confirmed (1).
B-Live vaccines should not be given to patients taking biologic agents (1).

C-A tuberculin skin test should be obtained before starting a biologic to detect
and treat latent or active tuberculosis. Patients should also be screened for
hepatitis B before starting biologic therapy because of the risk for reactivation (1).

5-TNF inhibitors should not be used in patients with moderate-to-severe heart


failure (New York Heart Association [NYHA] class III/IV) because new-onset and
worsening heart failure have been reported (1).

6-Secukinumab is indicated for ankylosing spondylitis, plaque psoriasis, and


psoriatic arthritis (4).
7-Ustekinumab is indicated for IBD (UC and CD), plaque psoriasis, and psoriatic
arthritis (4).

8-Other indications for the biological agents are summarized in (Table 10-1) (4).

9-Biosimilars are biologic products that have been verified to have no clinically
meaningful differences compared to an FDA-approved reference biologic
product. These agents can increase access to RA treatment because their costs are
lower than the originator products (1).

Table 10-1: Other indications for biological agents (4).


Drug Other indications
plaque psoriasis, IBD (UC and CD), uveitis, ankylosing
1 Adalimumab
spondylitis, axial spondyloarthritis, and psoriatic arthritis
Certolizumab Ankylosing spondylitis, axial spondyloarthritis, psoriatic
2
pegol Arthritis, and plaque psoriasis
Ankylosing spondylitis, plaque psoriasis, axial
3 Etanercept
spondyloarthritis, psoriatic arthritis
141
Ulcerative colitis, ankylosing spondylitis, psoriatic arthritis,
4 Golimumab
and axial spondyloarthritis.
IBD (UC and CD), ankylosing spondylitis, plaque psoriasis
5 Infliximab
and psoriatic arthritis.
Lymphoma (non-Hodgkin‘s), chronic lymphocytic
6 Rituximab leukaemia, granulomatosis with polyangiitis and microscopic
polyangiitis, pemphigus vulgaris.
Biological agents
Scientific name Trade names Dosage form
1

Any extra notes:

10.2-Drugs for hyperuricemia and gout


10.2.1-Acute attacks of gout
1-Nonsteroidal anti-inflammatory drugs (NSAIDs), colchicine, and
corticosteroids are considered first-line monotherapy for acute attacks (3).
2-Treatment should begin as soon as possible after the onset of an attack (1).
3-Acute attacks of gout are usually treated with either colchicine or high doses
of an NSAID (excluding aspirin) (4).
10.2.1.1-Colchicine
1-Colchicine is highly effective in relieving acute gout attacks but it is used
infrequently today because of its low therapeutic index (1, 3).
2-Oral colchicine causes dose-dependent GI adverse effects (nausea, vomiting,
and diarrhea). Non-GI adverse effects include neutropenia and neuromyopathy,
which may be worsened in patients taking other myopathic drugs (e.g., statins) or
with impaired kidney function. (1).
3-Use colchicine with caution in patients taking P-glycoprotein or strong CYP450
3A4 inhibitors (eg, clarithromycin) due to increased plasma colchicine levels and
potential toxicity; colchicine dose reductions may be required (1).

141
4-Colchicine is also used for short-term prophylaxis during initial therapy with
allopurinol and uricosuric drugs (4).
10.2.2-Long-term control of gout
1-After the first attack of acute gout, prophylactic pharmacotherapy is
recommended if patients have two or more attacks per year. Other indications
include presence of tophi, chronic kidney disease, or history of urolithiasis (1).
2-Urate-lowering therapy can be started during an acute attack if anti-
inflammatory prophylaxis has been initiated. The guidelines recommend low-dose
oral colchicine or low-dose NSAIDs as first-line prophylactic therapies (1).
Continue prophylaxis until at least 1 month after hyperuricaemia corrected
(usually for first 3 months) to avoid precipitating an acute attack (4).
10.2.2.1-Xanthine oxidase inhibitors (allopurinol, febuxostat)
1-Xanthine oxidase inhibitors reduce uric acid by impairing conversion of
hypoxanthine to xanthine and xanthine to uric acid. They are the most widely
prescribed agents for long-term prevention of recurrent gout attacks (1).
2-Allopurinol:
A-Mild adverse effects of allopurinol include skin rash, GI problems, headache,
and urticarial. A more severe adverse reaction known as allopurinol
hypersensitivity syndrome (1).
B-Allopurinol should not be taken with ampicillin owing to increased risk of
rash (2).
C-It also used for the prophylaxis of (hyperuricaemia associated with cancer
chemotherapy, uric acid and calcium oxalate renal stones) (4).
D-Take allopurinol with food to minimize GI upset (10).
3-Febuxostat :
A-Febuxostat is a nonpurine xanthine oxidase inhibitor. Due to differences in
chemical structure, febuxostat would not be expected to cross-react in
patients with a history of allopurinol hypersensitivity syndrome (3).

B-It is also used for prophylaxis and treatment of acute hyperuricaemia with
initial chemotherapy for hematologic malignancies (4).
10.2.2.2-Uricosuric Drugs
1-Uricosurics (such as probenecid or sulfinpyrazone) are considered second-line
treatment (2).
2-Patients with a history of urolithiasis should not receive uricosurics. Starting
with low, maintaining adequate urine flow and alkalinization of the urine
during the first several days of therapy may decrease likelihood of uric acid stone
formation (1).

142
10.2.2.3-Pegloticase
1-Pegloticase is a recombinant form of uricase bound to polyethylene glycol
that is approved for the treatment of chronic gout refractory to other therapy (3).
2-Pegloticase should be limited to patients with severe gout with tophi or
nephropathy that has not responded to other agents because of significant adverse
effects, including anaphylaxis (in up to 5% of patients) that mandates
pretreatment with antihistamines and corticosteroids, and its high cost (3).
Drugs for hyperuricemia and gout
Scientific name Trade names Dosage form
1

Any extra notes:

10.3-Intra-articular corticosteroid injections


1-Corticosteroids (e.g. methylprednisolone, triamcinolone) are injected locally for
an anti-inflammatory effect. They are given by intra-articular injection (4) (e.g.in
case of RA, OA or gout) (1) to relieve pain, increase mobility, and reduce deformity
in one or a few joints; they can also provide symptomatic relief while waiting for
DMARDs to take effect (4).
2-Specific instructions are given to the patient to refrain from weight-bearing
activity for 3 days, except getting up for meals and going to the bathroom (2).
Local corticosteroid injections
Scientific name Trade names Dosage form
1

Any extra notes:

10.4-Skeletal muscle relaxants:


A-The skeletal muscle relaxants are used for the relief of chronic muscle
spasm or spasticity associated with multiple sclerosis or other neurological
damage; they are not indicated for spasm associated with minor injuries (4).
143
B-Baclofen, diazepam, pridinol and tizanidine act principally on the central
nervous system. While dantrolene has a peripheral site of action; cannabis
extract has both a central and a peripheral action (4).
Drugs for neuromuscular disorders
Scientific name Trade names Dosage form
1

Any extra notes:

References
1-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.
2-Edward T. Bope, et al, eds. Conn‘s Current Therapy. Copyright 2018.
4-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
4-BNF-81 (2021).
5-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
6-David J Quan, Richard A Helms. Textbook of Therapeutics: Drug and Disease
Management. 8th edition. 2006.
7-Leon Shargel , Alan H. Mutnick . Comprehensive pharmacy review. 8 th edition
2013.
8-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
9-Stuart HR, Ian DP, Mark WJ, Richard PH. Davidson's Principles and Practice of
Medicines . 23th Edition 2018.
10-Michael AM, Jason. Frequently prescribed medications. Third edition 2019.

144
Chapter Eleven: Eye
11.1.Administration of drugs to the eye
1-When two different eye preparations are used at the same time of day, the
patient should leave an interval of at least 5 minutes between the two, to allow
the first to be fully absorbed; eye ointment should be applied after drops (1).
2-Eye drops and ointments may cause temporary blurring of vision. If affected,
patients should be warned not to drive or perform other skilled tasks until vision
is clear (1).
3-Eye preparations in multiple-application containers for use by the patient at
home are normally discarded 4 weeks after first opening (unless otherwise
stated by the manufacturer) (1).
4-Systemic effects may arise from absorption of drugs into the
general circulation either directly from the conjunctival sac or
after the excess preparation has drained down through the tear ducts
into the nasal cavity. Nasal drainage of drugs is associated with eye
drops much more often than with eye ointments. Applying
pressure on the lacrimal punctum for at least a minute after
administering eye drops reduces nasolacrimal drainage and therefore decreases
systemic absorption from the nasal mucosa (1).
5-Very important: If using a suspension, shake well before instilling. If using
the suspension with another dosage form, place the suspension drop last, because
it has prolonged retention time in the tear film (2).
Note: most steroid eye drops present as a suspension.
6-Important: If both drop and ointment therapy are indicated, instill the drops
at least 10 minutes before the ointment so that the ointment does not become a
barrier to the drops' penetrating the tear film or cornea (2).
7-The intravitreal route is used to administer drug into the posterior segment of
the eye for conditions such as macular oedema and age-related macular
degeneration. The intracameral route can be used to deliver certain drugs to the
anterior chamber, for example antibacterials after cataract surgery. These
injections should only be used under specialist supervision (1).
11.2. Contact lenses and drug treatment
1-Unless medically indicated, soft lenses should be removed before instillation
of the eye preparation. Alternatively, unpreserved drops can be used, as
preservatives accumulate in soft lenses and can cause irritation (1). Patients
who wear soft contact lenses should be advised to stop wearing them while
treatment continues and for 48 hours afterwards. This is because preservatives in
the eye drops can damage lenses (3).
2-Eye drops, however, may be instilled while patients are wearing hard contact
lenses but removal prior to instillation is still generally advised (1).

145
3-Ointment preparations should never be used in conjunction with contact
lens wear; oily eye drops can cause lens deposits and should also be avoided.
Many drugs given systemically can also have adverse effects on contact lens wear
(1)
.
11.3-Antibacterials eye preparations
1-Most acute superficial eye infections can be treated topically with eye drops or
ointment. Systemic administration is sometimes appropriate in blepharitis (1).
2-Common antibacterials available as an eye preparations include (1):
A-Aminoglycosides: gentamicin, neomycin , and tobramycin.
B-Cephalosporins (second-generation): cefuroxime (intra-ocular injection
injection).
C-Macrolides: azithromycin.
D-Quinolones: ciprofloxacin, levofloxacin, moxifloxacin, and ofloxacin.
E-Others: chloramphenicol, fusidic acid and polymyxin B.
Antibacterials alone
Scientific name Trade names Dosage form
1

6-

Any extra notes:

11.4.Antivirals and antifungals


1-Commonly used antivirals are aciclovir (acyclovir) or ganciclovir for hrpes
simplex infections. (2).
2-Fungal infections of the cornea are rare. Antifungal preparations for the eye are
not generally available. Treatment will normally be carried out at specialist centers
(2)
.

146
Antivirals
Scientific name Trade names Dosage form

Any extra notes:

11.5. Corticosteroids and other anti-inflammatory preparations


1-Commonly used corticosteroids are: betamethasone, dexamethasone,
fluorometholone, hydrocortisone, and prednisolone (1).
2-They are used to treat inflammatory eye conditions. Topical corticosteroids are
applied frequently for the first 24–48 hours; once inflammation is controlled, the
frequency of application is reduced (1).
3-Combination products containing a corticosteroid with an anti-infective
drug are sometimes used after ocular surgery to reduce inflammation and prevent
infection; use of combination products is otherwise rarely justified (1).
4-An intravitreal implant containing dexamethasone or fluocinolone are also
available for certain eye conditions (1).
5-Steroid glaucoma’ can follow the use of corticosteroid eye preparations in
susceptible individuals; a ‗steroid cataract’ can follow prolonged use (1).
6-Other anti-inflammatory preparations used for the topical treatment of
inflammation and allergic conjunctivitis include sodium cromoglicate (sodium
cromoglycate), and nedocromil sodium. Lodoxamide eye drops are used for
allergic conjunctival conditions including seasonal allergic conjunctivitis (1).
7-NSAIDs:
A-NSAIDs eye drops such as bromfenac, diclofenac, flurbiprofen , and
ketorolac are used for the prophylaxis and treatment of inflammation, pain,
and other symptoms associated with ocular surgery or laser treatment of the
eye (1).
B-Diclofenac sodium and flurbiprofen are also used to prevent miosis during
ocular surgery (1).
C-Diclofenac eye drops may be used for seasonal allergic conjunctivitis (1).
D-Contra-indicated in patients with a history of hypersensitivity to aspirin or
any other NSAID (1).
8-Eye drops containing antihistamines, such as antazoline, azelastine, epinastine,
ketotifen, olopatadine, can be used for allergic conjunctivitis (1).

147
Corticosteroids
Scientific name Trade names Dosage form
1

2 Eye drop

Antibacterials with corticosteroids


Scientific name Trade names Dosage form
1

Other anti-inflammatory preparations


Scientific name Trade names Dosage form
1 Sodium cromoglicate

NSAIDs
Scientific name Trade names Dosage form
1

Antihistamines alone
Scientific name Trade names Dosage form
1

Any extra notes:

148
11.6.Decongestants and decongestants-antihistamine combination
1-Such preparation may be intended for the treatment of allergic conjunctivitis (3).
2-These agents can be used to reduce redness of the eye. Products contain a
combination of sympathomimetic and antihistamine or sympathomimetic alone.
They are useful in reducing redness in the eye but will not treat the underlying
pathology that is causing the eye to be red. They should be limited to short-term
use to avoid rebound effects (3).
3-Common decongestants-antihistamine combination is (naphazoline-
antazoline).

Decongestants and decongestants-antihistamine combination


Scientific name Trade names Dosage form
1

Any extra notes:

11.7.Drugs for dry eye (tear deficiency) (artificial tears).


1-Hypromellose is the most frequently used treatment for tear deficiency in
patients with mild dry eye. Initially, it may need to be instilled frequently (e.g.
hourly) for adequate symptom relief, then at a reduced frequency. Carbomers and
polyvinyl alcohol are suitable alternatives (1).
2-The ability of carbomers and polyvinyl alcohol to cling to the eye surface and
their higher viscosity may help reduce frequency of application to 4 times daily
(1)
.
3-Preservative-free tear replacement is preferred in cases of frequent and
chronic application (1). The preservative that most often causes eye irritation is
benzalkonium chloride. If a product causes irritation or if soft contact lenses are
worn, consider switching to one that is preservative-free. If more than six
applications are used daily, consider using a preservative free product as the risk
of irritation from the preservative increases with the frequency of dosing (4).
4-Sodium chloride (saline) is short acting and suitable as ‗comfort drops‘ or for
use with contact lenses (4).
5-Eye ointments containing a paraffin can be used to lubricate the eye surface,
especially in cases of recurrent corneal epithelial erosion. They may cause

149
temporary visual disturbance and are best suited for application before sleep.
Ointments should not be used during contact lens wear. (1).
6-Sodium hyaluronate eye drops are also used in the management of tear
deficiency (1).
7-Ciclosporin eye drop [to be applied to the affected eye(s) at bedtime]is licensed
for severe keratitis in patients with dry eye disease, which has not improved
despite treatment with tear substitutes (1).
Drugs for dry eye
Scientific name Trade names Dosage form
1

Any extra notes:

11.8. Antiglaucoma Drugs


1-Glaucoma characterized by a loss of visual field associated with optic nerve
damage. While glaucoma is generally associated with raised intra-ocular pressure
(IOP), it can occur when IOP is within the normal range (1).
2-The most common form of glaucoma is primary open-angle glaucoma, where
drainage of the aqueous humour is restricted. Patients with ocular hypertension are
at high risk of developing primary open-angle glaucoma (1).
3-Acute angle-closure glaucoma is less common and occurs when the outflow of
aqueous humour from the eye is totally obstructed. It is a medical emergency that
requires urgent reduction of IOP to prevent loss of vision (1).
4-Glaucoma medications with different IOP-lowering approaches are summarized
in Table 11-1 (5).
5-If more than one agent is needed, fixed combination products reduce the
number of daily doses, which might improve adherence and prevent washout
effect seen when a second medication is administered too soon after the initial
medication. They also reduce exposure to ophthalmic preservatives (6).
11.7.1.Ocular Hypotensive Lipids
1-The ocular hypotensive lipids are considered first-line agents because of their
superior efficacy and safety profiles (7).

151
2-Prostaglandin analogs Table11-1: Drugs used in the treatment of primary
offer once-daily dosing, open-angle glaucoma (5).
better IOP reduction,
good tolerance, and
availability of lower-
cost generics (8).
3-The ocular
hypotensive lipids are
administered once daily
at bedtime and should
not be increased to twice
daily, as this may
decrease effectiveness
(7)
.
4-Patients should also be
advised to avoid
repeated contact of the
eye drop solution with
skin as this can lead to
hair growth or skin
pigmentation (1).
5-Patients receiving
latanoprost or
tafluprost should be instructed to refrigerate unopened medication. Once open
latanoprost can stored at room temperature for 6 weeks. Tafluprost single-use
containers can be stored at room temperature for up to 28 days (7).
11.7.2.β-Adrenergic Antagonists
1-Topical β-blockers are typically administered twice daily. A gel-forming
solution of timolol (Timoptic-XE) can be administered once daily (7).
2-Tachyphylaxis may occur in 20% to 50% of patients on monotherapy with a β -
blocker, resulting in the need for a different agent or combination therapy (7).
3-β-Blockers can cause significant systemic adverse effects through nasolacrimal
drainage and subsequent systemic absorption. Bronchospasm is the most
common pulmonary effect of topical β -blockers. Patients prescribed topical β-
blockers should be counseled on the nasolacrimal occlusion technique to decrease
systemic absorption (7).
4-Topical β-blockers are generally contraindicated in patients with asthma,
chronic obstructive pulmonary disease (COPD), sinus bradycardia, second- or
third-degree heart block, cardiac failure, and hypersensitivity to the product (7).
5-Stinging of the eyes upon instillation is the most common adverse effect (7).

151
11.7.3.α2-Adrenergic agonists (brimonidine and apraclonidine)
1-Apraclonidine is often used for the prevention and treatment of postsurgical IOP
elevations and is no longer commonly used for long-term treatment of POAG
because of tachyphylaxis and high rate of blepharoconjunctivitis (7).
2-Brimonidine-purite 0.1% and 0.15% solution (Alphagan-P) (7) (preserved with
purite rather than benzalkonium chloride) (9) has similar efficacy compared
with the brimonidine 0.2% solution, because the purite solution‘s higher pH allows
for more drug to penetrate the cornea (7).
3-Brimonidine cause both local and systemic effects. Local effects include
blepharoconjunctivitis, conjunctivitis, and ocular allergy. Systemic effects include
headache, dry mouth, and fatigue (7).
11.7.4.Carbonic anhydrase inhibitors
11.7.4.1-Topical carbonic anhydrase inhibitors
1-Dorzolamide and brinzolamide are administered every 8 hours and are used as
adjunctive therapy or as monotherapy for patients who cannot tolerate first-line
therapies. Nasolacrimal occlusion may allow for an every-12-hour dosing
interval (7).
2-Local side effects include burning, stinging, itching, foreign body sensation, dry
eyes, and conjunctivitis. Brinzolamide may have fewer incidences of these side
effects since the drug is in a neutral pH solution (7).
3-Both topical carbonic anhydrase inhibitors are sulfonamides and are
contraindicated in patients with history of sulfonamide hypersensitivity (7).
11.7.4.2-Systemic carbonic anhydrase inhibitors
1-The systemic carbonic anhydrase inhibitors (e.g. acetazolamide given by mouth
or by injection (1)) are reserved as third-line to fourth-line agents because of their
significant adverse effects (7).
2-The systemic carbonic anhydrase inhibitors are associated with significant
adverse effects that include paresthesias of the hands and feet (7).
3-Sulfonamide allergy is a contraindication of systemic carbonic anhydrase
inhibitor therapy (7).
4-Note: Acetazolamide is also used for epilepsy (1).
12.7.7.Hyperosmotics
1-Glycerin, isosorbide, and mannitol are hyperosmotic agents that increase the
osmolality of blood. These agents create an osmotic gradient that draws water from
the vitreous humor, thus decreasing IOP (7).
2-The resulting dehydration of the vitreous humor may cause posterior movement
of the lens, which then causes the anterior chamber to deepen, thus opening the
anterior angle (7).
3-If the patient is not vomiting, glycerin solution and isosorbide can be given
orally. If the patient has nausea or vomiting, mannitol (20%) can be given IV (7).
152
Antiglaucoma drugs (single drug and combined preparations)
Scientific name Trade names Dosage form
1

Any extra notes:

11.8. Sodium chloride


Sodium chloride may be used for tear deficiency, irrigation, including first-aid
removal of harmful substances, intra-ocular or topical irrigation during surgical
procedures (1).
References
1-BNF-81 (2021)
2-American pharmacists association. Handbook of Non-prescription drugs: An
Interactive Approach to Self-Care. 18th edition. 2016.
3-Paul Rutter. Community Pharmacy. Symptoms, Diagnosis and Treatment. 5th
edition. 2021
4-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the
pharmacy . A guide to the managements of common illness. 8th edition. 2018.
5-Roger Walker. Clinical Pharmacy and Therapeutics. Sixth edition 2019.
6-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.
7-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
8-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
9-Canadian pharmacists association. Therapeutic choices. 2019.
11-NAPLEX® Review Guide, Fourth Edition. Copyright © 2021 by McGraw-Hill.

153
Chapter Twelve: Ear, Nose, and Oropharynx
12.1-Drugs acting on the ear
12.1.1-Treatment of otitis externa
1-Otitis externa is a general term used to describe inflammation of the skin of
the external auditory canal that may be due to infection with bacteria, viruses, or
fungi or secondary to skin disorders such as eczema (1).
2-Otitis externa may be acute or chronic. The treatment of both acute and chronic
otitis externa includes thorough cleansing and the use of appropriate
antibacterial ear drops, with or without a corticosteroid, even though some
have doubted the value of topical antibacterials (1).
3-Solution of acetic acid 2% acts as an antifungal and antibacterial in the external
ear canal. It may be used to treat mild otitis externa. If infection is present, a
topical anti-infective with or without a corticosteroid may be considered (2).
4-If a mild to moderate, uncomplicated fungal infection is suspected in the context
of chronic otitis externa, a topical antifungal such as clotrimazole 1% solution
can be offered (2).
5-Ear drops containing aminoglycosides, such as gentamicin, neomycin, or
framycetin, or polymyxins should not be used when the ear drum is perforated
because of the risk of ototoxicity (1).
Ear products for otitis externa
(Corticosteroids, Anti-infective, and combination products)
Trade names Scientific name Dosage form
1

6-

Any extra notes:

12.1.2-Treatment of acute otitis media


1-Acute otitis media is a self-limiting condition that mainly affects children. It is
characterized by inflammation in the middle ear associated with effusion and
accompanied by the rapid onset of signs and symptoms of an ear infection. The
154
infection can be caused by viruses or bacteria; often both are present
simultaneously (2).
2-Children with acute otitis media usually present with symptoms such as ear
pain, rubbing of the ear, fever, irritability, crying, poor feeding, restlessness at
night, cough, or rhinorrhoea. Symptoms usually resolve within 3 to 7 days
without antibacterial drugs (2).
3-An immediate antibacterial drug should be given if the child is systemically
very unwell, has signs or symptoms of a more serious illness, or is at high risk of
complications (2).
4-Pain of otitis media should be treated with oral analgesics. Acetaminophen or a
NSAID, such as ibuprofen, should be offered early to relieve pain of acute otitis
media (3).
5-High-dose amoxicillin (80–90 mg/kg/day) is recommended for most children.
Children who have received amoxicillin in the last 30 days, have concurrent
purulent conjunctivitis, or have a history of recurrent infection unresponsive to
amoxicillin should receive high-dose amoxicillin–clavulanate (90 mg/kg/day of
amoxicillin, with 6.4 mg/kg/day of clavulanate, in two divided doses) instead of
amoxicillin (3).
12.1.3.Removal of ear wax (cerumen)
A-Nonpharmacologic therapy
1-The only recommended nonpharmacologic method of removing cerumen is to
use a wet, wrung-out washcloth draped over a finger (4). (The common use of
cotton-tipped swabs to remove earwax is ineffective and potentially dangerous) (5).
B-Pharmacologic therapy (cerumunolytics)
1-Constituents of cerumenolytic products include fixed and volatile oils (olive,
arachis, almond and camphor oils), glycerol, docusate, and urea hydrogen peroxide
(6)
.
2-The manufacturers docusate (dioctyl sodium sulpho-succinate) recommend that
adults and children use enough ear drops to fill the affected ear then place a
small plug of cotton wool in the ear and repeat for two consecutive nights (7).
3-Sodium bicarbonate ear drop should be instilled two to three times a day for up
to 3 days (7).

Cerumunolytics
Scientific name Trade names Dosage form
1

155
Any extra notes:

12.2-Drugs acting on the nose


12.2.1.General notes:
1-Nasal sprays are preferable for adults and children over 6 years old because
the small droplets in the spray mist reach a large surface area. Drops are more
easily swallowed, which increases the possibility of systemic effects (8).
2-For children under 6 years old, drops are preferred because in young
children the nostrils are not sufficiently wide to allow the effective use of sprays (8).
12.2.2-Drugs used in nasal allergy
12.2.2.1-Corticosteroids (intranasal)
1-Nasal preparations containing corticosteroids (beclometasone, betamethasone,
budesonide, fluticasone, mometasone, and triamcinolone) are used for allergic
rhinitis (2).
2-In seasonal allergic rhinitis (e.g. hay fever), treatment should begin 2 to 3
weeks before the season commences and may have to be continued for several
months (2).
3-Some patients improve within a few days, but peak response may require 2 to
3 weeks (3).
4-The dosage may be reduced once a response is achieved (3).
5-When nasal congestion is severe, intranasal administration may not be effective
due to limited exposure to the nasal mucosa. Short-term use of intranasal
decongestants may facilitate better exposure (9).
Intranasal corticosteroids
Trade names Scientific name Dosage form
1

Any extra notes:

12.2.2.2-Topical nasal decongestants


1-Symptoms of nasal congestion associated with allergic rhinitis, the common
cold, and sinusitis may be relieved by the short-term use (usually not longer than 7
days) of decongestant (2) (sympathomimetics such as ephedrine, phenylephrine,
naphazoline, oxymetazoline, and xylometazoline (1)) nasal drops and sprays (2).
156
2-Topical nasal decongestants (sympathomimetics) can be recommended for those
patients in whom systemic (oral) decongestants are less suitable (8).
3-Irritated nasal tissue may be soothed with commercial nasal saline solutions as
they can improve symptoms and decrease medication use (10).
4-If nasal sprays/drops are to be recommended, the pharmacist should advise the
patient not to use the product for longer than 7 days. Rebound congestion
(rhinitis medicamentosa) can occur with topically applied, but not oral
sympathomimetics (8).
5-Many treatment options have been proposed for rhinitis medicamentosa
including slow reduction in the use of decongestant, a switch to inhaled
corticosteroids or an abrupt discontinuation. Abrupt cessation is effective but it
is difficult because the patients will be congested for several days or weeks (10).
Note: some of these product may present in two concentrations (one for children
and one for adults).
Topical nasal decongestants
Scientific name Trade names Dosage form
1

Any extra notes:

12.2.2.3. The topical antihistamine, mast-cell stabilizers, and antimuscarinics


1-Mild allergic rhinitis is controlled by antihistamines or topical nasal
corticosteroids. Topical antihistamines (e.g. azelastine) are faster acting than oral
antihistamines and therefore useful for controlling breakthrough symptoms in
allergic rhinitis; they are less effective than topical nasal corticosteroids (2).
2-Caution patients using intranasal azelastine about potential for drowsiness
because systemic availability is approximately 40% (3).
3-Sodium cromoglicate (mast-cell stabilizers (3)) is a weakly effective alternative
in patients with mild symptoms, sporadic seasonal problems, or limited allergen
exposure (2). For seasonal rhinitis, treatment should be initiated just before the
start of the offending allergen’s season and continue throughout the season. In

157
persistent rhinitis, improvement may not be seen for 2–4 weeks; antihistamines
or decongestants may be needed during this initial phase of therapy (3).
4-Nasal ipratropium bromide may be added to allergic rhinitis treatment when
watery rhinorrhoea persists despite treatment with topical nasal corticosteroids
and antihistamines; it has no effect on other nasal symptoms (3).
Scientific name Trade names Dosage form

Any extra notes:

12.3-Drugs acting on the oropharynx


12.3.1-Oropharyngeal fungal infections
1-Topical antifungals for oropharyngeal fungal infections (thrush) include nystatin
as an oral suspension drop and miconazole (as an oral gel) (2).
2-Concerning miconazole oral gel: treatment should be continued for at least 7
days after lesions have healed or symptoms have cleared, to be administered after
meals, retain near oral lesions before swallowing (2).
3-Concerning nystatin oral drop: continued for 48 hours after lesions have
resolved (2).

Topical antifungals for oropharyngeal fungal infections


Scientific name Trade names Dosage form
1

Any extra notes:

158
12.3.2-Mouthwashes and gargles
1-Mouthwashes (e.g. those containing chlorhexidine, hydrogen peroxide,
hexetidine, sodium bicarbonate with sodium chloride) are used for general oral
hygiene (2).
2-Chlorhexidine (antiseptic) (2):
A-Can be used as a mouthwash, spray or gel for (oral hygiene and plaque
inhibition , oral candidiasis, gingivitis , and management of aphthous ulcers) (2).
B-Rinse or gargle 10 mL twice daily (rinse or gargle for about 1 minute). It
may cause tongue and tooth discoloration (2).
C-Chlorhexidine may be incompatible with some ingredients in toothpaste,
rinse the mouth thoroughly with water between using toothpaste and
chlorhexidine-containing products (wait 30 minutes between using these two
preparations). (2).
Mouthwashes and gargles
Scientific name Trade names Dosage form
1

Any extra notes:

12.3.3-Oral ulceration and inflammation


1-Ulceration of the oral mucosa may be caused by trauma (physical or chemical),
recurrent aphthae, infections, carcinoma, dermatological disorders, nutritional
deficiencies, gastro-intestinal disease, hematopoietic disorders, and drug therapy
(Chemotherapy induced mucositis) (2).
2-Secondary bacterial infections may occur with mucosal ulceration; it can
increase discomfort and delay healing (2).
3-Topical corticosteroids are usually considered to be first-line treatment. A
short course of systemic corticosteroids may be prescribed for patients with severe
recurrent aphthous ulcers (2).
4-Other therapies that may be used alone or in combination with topical
corticosteroids include topical anaesthetics (e.g. lidocaine), topical
analgesics/anti-inflammatory agents (e.g. benzydamine, diclofenac and

159
flurbiprofen), and topical antimicrobial agents (e.g. chlorhexidine mouthwash)
(2)
.
5-Doxycycline [unlicensed indication], rinsed in the mouth and expelled, may be
considered for recurrent aphthous ulceration when other treatments are
unsuccessful or unsuitable (2).
(by mouth using dispersible tablet: 100 mg 4 times a day usually for 3 days,
dispersible tablet can be stirred into a small amount of water then rinsed around
the mouth for 2–3 minutes, it should preferably not be swallowed) (2).
6-Expert sources advise that local anaesthetics have a short duration of action;
there is limited evidence for their use in the management of oral ulceration (2).
7-When local anaesthetics are used in the mouth, care must be taken to avoid
causing anesthesia of the pharynx before meals, as this might lead to choking
(2)
.
8-Mucositis occurs as a nonspecific effect of chemotherapy and radiation
therapy on the basal epithelium of the mouth. Equal portions of lidocaine,
diphenhydramine, and magnesium-containing or aluminum-containing antacids
can be used for their anesthetic and astringent properties. Many institutions
compound mouthwash products containing these ingredients as well as antibiotics,
nystatin, or corticosteroids (11).
Oral ulceration and inflammation (corticosteroids, NSAID, local
anaesthetics)
Scientific name Trade names Dosage form
1

Any extra notes:

12.3.4-Fluoride
1-Fluoride is a naturally occurring mineral found in water supplies in varying
amounts and in some foods; it has beneficial topical effects on teeth (2).
2-Public Health England recommends the daily use of a fluoride mouthwash in
adults and children aged 7 years and over who are causing concern to their
dentist (e.g. those with active caries, dry mouth, or special needs). They should be
161
used at a different time to brushing to avoid removal of the beneficial effects of
fluoride in toothpaste (2).
3-Directions for administration
A-With oral use: Tablets should be sucked or dissolved in the mouth at a
different time of day to tooth brushing. (4).
B-With oral (topical) use: for mouthwash, rinse mouth for 1 minute and then
spit out (4).
C-Toothpaste: avoid drinking or rinsing mouth for 30 minutes after use (4).
Fluoride
Scientific name Trade names Dosage form
1

Any extra notes:

12.3.5-Treatment of dry mouth (xerostomia)


1-Dry mouth may be caused by drugs with antimuscarinic (anticholinergic) side-
effects, by diuretics, by irradiation of the head and neck region, dehydration,
anxiety, or Sjögren’s syndrome (2).
2-Patients with dry mouth may be at greater risk of developing dental caries,
periodontal disease, and oral infections (particularly candidiasis) (2).
3-Dry mouth may be relieved in many patients by simple measures that
stimulate salivation such as frequent sips of cold unsweetened drinks, or sucking
pieces of ice or sugar-free fruit pastilles, or chewing sugar free gum (2).
4-An artificial saliva substitute can be considered if simple stimulatory measures
are inadequate. Artificial saliva products below are available in oral lozenges, oral
gel, oral spray, and pastille forms (2).
Products for dry mouth
Scientific name Trade names Dosage form
1

Any extra notes:

161
References
1-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
2-BNF-81 (2021)
3-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021
4-American pharmacists association. Handbook of Non-prescription drugs: An
Interactive Approach to Self-Care. 18th edition. 2016.
5-W. Steven Pray, Gabriel E. Pray .Treating Minor Ear Problems. US Pharm.
2012;37(5):16-23.
6-Nathan A. Non-prescription medicines. 4th edition. London: Pharmaceutical
Press. 2010.
7-Paul Rutter. Community Pharmacy. Symptoms, Diagnosis and Treatment. 5th
edition. 2021.
8-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the
pharmacy . A guide to the managements of common illness. 8th edition. 2018.
9-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
10-Canadian pharmacists association (CPhA). CTMA: Compendium of
Therapeutics for Minor Ailments. 2018.
11-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The
clinical use of drugs, 11th ed., 2018.

162
Chapter Thirteen: Skin
13.1-Common skin diseases by body location
Common skin diseases by body location are shown in (Table 13-1) (1)
Table 13-1: Common skin diseases by body location (1).

13.2-Dermatologic drug delivery systems


1-Dermatologic formulations are available in a variety of forms: solutions,
suspensions or shake lotions, powders, lotions, emulsions, gels, creams, ointments,
and aerosols. Each dermatologic delivery vehicle has specific characteristics and
uses based on the type, relative acuteness, and location of the lesion (1) (Table 13-
2).
2-Powders are used mainly in intertriginous areas (e.g., groin, under the breasts,
or in skin folds) to decrease friction, which can cause mechanical irritation. They
also are useful in the treatment of tinea pedis (athlete‘s foot), tinea cruris (jock
itch), and diaper dermatitis (diaper rash) (1).
3-Lotions are suspensions or solutions of powder in a water vehicle. They are
especially advantageous in the treatment of conditions characterized by significant
inflammation and tenderness. In these situations, creams or ointments may cause
pain on application. Also, lotions are useful for hairy areas of the body and
scalp (1).
4-Gels are most useful when applied to hairy areas or other areas such as the
face or scalp, where it is considered cosmetically unacceptable to have the residue
of a vehicle remain on the skin (1).
5-Creams are the most commonly used vehicle in dermatology. The most
common mistake made by patients when applying creams is that they use too
much or do not rub them in fully. Generally, if the cream can be seen on the skin
after application, the patient has made one or both of these application mistakes (1).
6-Ointments are most useful on chronic lesions, relieving dryness, brittleness,
and protecting fissures owing to their occlusive properties. They should not be
used on acutely inflamed lesions. Ointments should not be applied to intertriginous
163
or hairy areas because they tend to trap heat and promote maceration. Ointments
are greasy and may be cosmetically unacceptable (1).
7-Collodions are painted on the skin and allowed to dry to leave a flexible film
over the site of application (2).
Table 13-2: Appropriate dermatologic vehicle selection across the range of
dermatologic lesions (1).

13.3-Anti-infective skin preparations


13.3.1-Antibacterial preparations
1- Some of the topical antibacterials used in superficial bacterial skin infections are
summarized in (Table 13-3) (3).
Table 14-3: Some topical antibacterials used in superficial bacterial skin
infections (3).
Drug Antibacterial activity
Framycetin Staphylococcus aureus, streptococci, gram-
1
(Aminoglycoside) negative organisms
2 Bacitracin Gram-positive organisms.
3 Fusidic acid Gram-positive organisms.
4 Mupirocin Gram-positive organisms.
Gram-positive cocci; anaerobic gram-positive
5 Clindamycin
organisms.
S. aureus, gram-negative organisms,
6 Silver sulfadiazine
Pseudomonas.
polymyxin B (gram-negative organisms);
Polymyxin B/
7 gramicidin (gram-positive organisms); bacitracin
gramicidin/ bacitracin
(gram-positive organisms).
2-Cellulitis, erysipelas, and leg ulcer infections require systemic antibacterial
treatment. Impetigo requires topical antiseptic/antibacterial or systemic
antibacterial treatment (2).
3-To minimize the development of resistant organisms it is advisable to limit the
choice of antibacterials applied topically to those not used systemically (2).
4- Silver sulfadiazine is used in the treatment of infected burns (2).
5-Metronidazole is used topically for rosacea and to reduce the odor associated
with anaerobic infections (2).
164
Topical antibacterials
Scientific name Trade names Dosage form
1

Any extra notes:

13.3.2-Antifungal preparations
1-Most localized fungal infections are treated with topical preparations.
Systemic therapy is necessary for scalp infection or if the skin infection is
widespread, disseminated, or intractable; although topical therapy may be used to
treat some nail infections, systemic therapy is more effective (2).
2-Important: To prevent relapse, local antifungal treatment should be continued
for 1–2 weeks after the disappearance of all signs of infection (2).
3-Topical antifungal include: The imidazole antifungals (clotrimazole, econazole,
ketoconazole, miconazole and tioconazole), Terbinafine, tolnaftate, nystatin,
griseofulvin, amorolfine, and compound benzoic acid ointment (Whitfield‘s
ointment).
4-Cutaneous antifungals are available as ointments, creams, powders, and aerosols.
Creams or solutions are the most efficient and effective dosage forms for
delivery of the active ingredient to the epidermis. Sprays and powders are less
effective because often they are not rubbed into the skin. They are probably more
useful as adjuncts to a cream or a solution or as prophylactic agents in preventing
new or recurrent infections (4).
5-Pityriasis versicolor can be treated with ketoconazole shampoo (apply once
daily for maximum 5 days, leave preparation on for 3–5 minutes before rinsing) (2).
6-Antifungal treatment may not be necessary in asymptomatic patients with
tinea infection of the nails. If treatment is necessary, a systemic antifungal is
more effective than topical therapy (2).
7-Combination products of an antifungals and corticosteroids are available to
treat used to control used to control symptoms of redness and itch (5) (in the first
few days only) (2).
165
Antifungal preparations (including Combination products)
Scientific name Trade names Dosage form
1

Any extra notes:

13.3.3-Antiviral preparations
1-Aciclovir cream can be used for the treatment of initial and recurrent labial
herpes simplex infections (cold sores) (2).
Important: Aciclovir is best applied at the earliest possible stage (Apply 5 times a
day for 5–10 days, to be applied to lesions approximately every 4 hours), usually
when prodromal changes of sensation are felt in the lip and before vesicles
appear (2).
2-Penciclovir cream is also licensed for the treatment of herpes labialis; it needs to
be applied more frequently than aciclovir cream (2).
3-Systemic treatment is necessary for buccal or vaginal infections and for herpes
zoster (shingles) (2).
Antiviral preparations
Scientific name Trade names Dosage form

Any extra notes:

166
13.3.4-Parasiticidal preparations
13.3.4.1-Scabies
1-Permethrin is used for the treatment of scabies (apply 5% preparation over
whole body then wash off after 8–12 hours); malathion can be used if permethrin
is inappropriate (apply preparation over whole body, and wash off after 24 hours)
(2)
.
2-Benzyl benzoate is an irritant and should be avoided in children; it is less
effective than malathion and permethrin (2).
3-Ivermectin by mouth has been used, in combination with topical drugs, for the
treatment of hyperkeratotic (crusted) scabies that does not respond to topical
treatment alone; further doses may be required (2).
4-All members of the affected household should be treated simultaneously.
Treatment should be applied to the whole body including the scalp, neck, face, and
ears. Particular attention should be paid to the webs of the fingers and toes and
lotion brushed under the ends of nails (2).
5-It is now recommended that malathion and permethrin should be applied
twice, one week apart; in the case of benzyl benzoate in adults, up to 3
applications on consecutive days may be needed. It is important to warn users to
reapply treatment to the hands if they are washed (2).
6-The itch and eczema of scabies persists for some weeks after the infestation has
been eliminated and treatment for pruritus and eczema may be required.
Application of crotamiton can be used to control itching after treatment with more
effective acaricides (2).
7-A topical corticosteroid may help to reduce itch and inflammation after scabies
has been treated successfully; however, persistent symptoms suggest that scabies
eradication was not successful. Oral administration of a sedating antihistamine
at night may also be useful (2).
Preparations for scabies
Scientific name Trade names Dosage form
1

Any extra notes:

13.3.4.2-Head lice
1-Head lice infestation (pediculosis) should be treated using lotion or liquid
formulations (shampoos are diluted too much in use to be effective) (2).
167
2-A contact time of 8–12 hours or overnight treatment is recommended for lotions
and liquids (2).
3-In general, a course of treatment for head lice should be 2 applications of
product 7 days apart to kill lice emerging from any eggs that survive the first
application. All affected household members should be treated simultaneously (2).
4-Dimeticone is effective against head lice; it is less active against eggs and
treatment should be repeated after 7 days. Malathion, an organophosphorus
insecticide, is an alternative, but resistance has been reported (2).
Drugs for Head lice
Scientific Trade Dosage Application
name names form
1

Any extra notes:

13.4-Preparations for minor cuts and abrasions


Cetrimide is used to treat minor cuts and abrasions. The effervescent effect of
hydrogen peroxide is used to clean minor cuts and abrasions (2).
Scientific name Trade names Dosage form

Any extra notes:

13.5-Skin cleansers, and antiseptics


1-Wound cleansing is required to remove any dirt or foreign bodies and to remove
exudate and slough (pus and necrotic tissue). This helps to prevent infection and
aids healing. Commonly used cleansing solutions are sodium chloride 0.9%,
hypochlorite, hydrogen peroxide, povidone-iodine, and chlorhexidine (6).
2-Hydrogen peroxide, an oxidising agent, can be used in solutions of up to 6% for
skin disinfection, such as cleansing and deodorizing wounds and ulcers (2).
3-For irrigating ulcers or wounds, lukewarm sterile sodium chloride 0.9% solution
is used (2).

168
4-Potassium permanganate solution 1 in 10000, a mild antiseptic with astringent
properties, can be used for exudative eczematous areas; treatment should be
stopped when the skin becomes dry (2).
5-Alcohol (indications: skin preparation before injection). (cautions : flammable;
avoid broken skin) (2).
6-Wound dressings and packing preparations help to protect the wound and
provide the correct environment for wound healing. Some also help by absorbing
exudates (6). (e.g. sofra-tulle®).
Skin cleansers, and antiseptics
Scientific name Trade names Dosage form
1

Any extra notes:

13.6-Emollients and barrier preparations


1-Emollients (like soft paraffin) soothe, smooth and hydrate the skin and are
indicated for all dry or scaling disorders (like eczema) (2).
2-Barrier preparations often contain water-repellent (e.g. zinc oxide, castor oil).
They are used on the skin around stomas, bedsores, and pressure areas in the
elderly where the skin is intact (2).
3-Notes concerning napkin rash (2) :
A-The first line of treatment is to ensure that nappies are changed frequently.
The rash may clear when left exposed to the air and a barrier preparation can be
helpful.
B-If the rash is associated with a fungal infection, an antifungal cream such
as clotrimazole cream is useful.
C-Mild corticosteroid such as hydrocortisone 0.5%or 1% can be used if
inflammation is causing discomfort, but it should be avoided in neonates.

169
D-Preparations containing hydrocortisone should be applied for no more
than a week. The hydrocortisone should be discontinued as soon as the
inflammation subsides.
Emollients and Barrier preparations (including preparations for napkin
rash)
Scientific name Trade names Dosage form
1 Zinc oxide

2 Zinc and castor oil

Any extra notes:

13.7-Topical local anaesthetics and antipruritics


1-An emollient may be of value where the pruritus is associated with dry skin (2).
2-Preparations containing crotamiton are sometimes used but are of uncertain
value. Preparations containing calamine are often ineffective (2).
3-Topical antihistamines and local anaesthetics are only marginally effective and
occasionally cause sensitization. For insect stings and insect bites, a short
course of a topical corticosteroid is appropriate. Short-term treatment with an
oral sedating antihistamine may help in insect stings where sedation is desirable
(2)
.
4-Calamine preparations are of little value for the treatment of insect stings or
bites (2).
5-Topical preparation containing doxepin 5%p is licensed for the relief of pruritus
in eczema; it can cause drowsiness [may affect performance of skilled tasks (e.g.
driving)] and there may be a risk of sensitization (2).
Topical local anaesthetics and antipruritics
Scientific name Trade names Dosage form
1

171
Any extra notes:

13.8-Topical corticosteroids
1-Topical corticosteroids are used for the treatment of inflammatory conditions
of the skin (other than those arising from an infection), in particular eczema,
contact dermatitis, insect stings (2).
2-Topical corticosteroids are not recommended in the routine treatment of urticaria
(2)
.
3-Application:
A-Topical corticosteroids should be applied no more than twice daily.
Increasing the application from twice daily to four times daily does not produce
superior responses, and may lead to increased frequency of topical and systemic
adverse effects (1).
B-One fingertip unit (approximately 500 mg) is sufficient to
cover an area that is twice that of the flat adult handprint
(palm and fingers) (2).
4-Preparations should be rubbed thoroughly and, when possible, applied while the
skin is moist (e.g., after bathing and drying off). Hydration of the skin increases
percutaneous absorption and the resultant therapeutic effect of topical steroids (1).
5-Children, especially infants, are particularly susceptible to side-effects. A
mild corticosteroid such as hydrocortisone 1% ointment or cream is useful for
treating nappy rash and for atopic eczema in childhood. A moderately potent
or potent corticosteroid may be appropriate for severe atopic eczema on the limbs,
for 1–2 weeks only, switching to a less potent preparation as the condition
improves (2).
6-Thinning of
the skin,
telangiectasia
(a visible
permanent
dilatation of
small cutaneous
blood vessels),
localized fine
hair growth, hypopigmentation, and striae (pink, red or purple lines or bands)
can result from repeated application of topical corticosteroids (1).
7-Mild corticosteroids are generally used on the face. Potent corticosteroids should
generally be avoided on the face and skin flexures (2).
8-When topical treatment has failed, intralesional corticosteroid injections may be
used (2).
171
9-Topical corticosteroid preparation potencies (Table 13-4) (6).
Table 13-4: potencies of topical corticosteroid (6).

Topical Corticosteroids (including Combination products)


Scientific name Trade names Dosage form potencies
1

Any extra notes:

13.9-Preparations for psoriasis


1-Psoriasis is a chronic inflammatory skin disorder characterized by enhanced
epidermal proliferation leading to erythema, scaling, and thickening of the skin
(6)
.

172
2-There are several types of psoriasis including guttate, flexural, pustular, and
erythrodermic, but chronic plaque psoriasis (psoriasis vulgaris) is the most
common form. In chronic plaque psoriasis; the areas most commonly affected are
the extensor sides of the knees, elbows, and hands, and the scalp and sacrum (6).
3-There is no cure and treatment is designed to induce a remission or suppress
disease to a tolerable level (6).
4-Drug therapy for psoriasis are summarized in (Table 13-5) (1, 2, 7, 8).

Table 13-5: Drug therapy for psoriasis (1, 2, 7, 8)


Topical Agents for the Agents for the Treatment of
Treatment of Psoriasis Severe Psoriasis
1 Emollients 1 Psoralens plus UVA (PUVA)
2 Keratolytics (salicylic acid, urea, Acitretin, Alitretinoin
α-hydroxy acids [i.e., glycolic and 2
lactic acids])
3 Topical corticosteroids 3 Methotrexate, ciclosporin,
4 Coal tar 4 mycophenolate, tofacitinib
5 Anthralin Immunomodulators (etanercept,
6 Calcipotriene and calcitriol 5 infliximab, adalimumab, golimumab,
7 Retinoids (Tazarotene) secukinumab, ixekizumab)
8 Ultraviolet B (UVB)
9 Calcineurin inhibitor
(Tacrolimus and Pimecrolimus)
5-Topical drugs are the treatment of first choice for chronic plaque psoriasis (6).
A-Different dosage forms are available such as creams, lotions, gels, foams,
ointments, shampoos, oil solutions, tapes, and sprays. Ointments are
recommended for dry and thick lesions to enhance absorption and reduce loss
of skin moisture (8).
B-Creams are indicated for acute, but moist appearing, lesions that do not
require ointment-based products. Solutions/shampoos and gels are
recommended for scalp lesions and foams and sprays are usually used for
lesions in genital areas (8).
C-Ointments are the most occlusive and most potent formulations because of
enhanced penetration into the dermis. Patients may prefer the less greasy creams
or lotions for daytime use (7).
6-Corticosteroids are the topical first-line treatment for mild to moderate
psoriasis. Additionally, topical corticosteroids can be combined with other topicals
or systemic/biologic agents to enhance therapy (8).
7-Calcipotriene and calcitriol are vitamin D3 analogs that bind to vitamin D
receptors, which inhibit keratinocyte proliferation. These agents can be used as
first-line monotherapy or in combination with a topical corticosteroid for mild
plaque psoriasis (7).
173
8-Retinoids: Tazarotene is a topical retinoid. It may be combined with a topical
corticosteroid to enhance efficacy and reduce irritation. Tazarotene is
contraindicated in pregnancy and should not be used in women of childbearing
potential unless effective contraception is being used (7).
9-Coal tar is used infrequently due to limited efficacy and poor patient
adherence and acceptance (it has an unpleasant odor, and stains clothing) (7).
10-Salicylic acid has keratolytic properties and has been used in shampoos or bath
oils for scalp psoriasis. It enhances penetration of topical corticosteroids,
thereby increasing corticosteroid efficacy (7).
11-Topical tacrolimus and pimecrolimus have a role in the treatment of psoriasis.
They are indicated also for atopic eczema (2).
12-Phototherapy and photochemotherapy: Phototherapy consists of either
ultraviolet A (UVA) or ultraviolet B (UVB), as light therapy for psoriatic lesions
(4)
. Phototherapy and photochemotherapy are generally used in the management
of moderate to severe disease (8). UVA is generally given with a photosensitizer
such as an oral psoralen to enhance efficacy; this regimen is called PUVA
(psoralen + UVA treatment) (7).
13-Psoriasis refractory to topical therapy may respond to systemic drugs
(acitretin, methotrexate, ciclosporin, mycophenolate , and tofacitinib and
Biologic agents ) (6-8).
14-Biologic agents are considered for moderate-to-severe psoriasis when other
systemic agents are inadequate or contraindicated or when comorbidities exist.
Cost considerations tend to limit their use as first-line therapy (1).
15-Acitretin;
A-It is a metabolite of etretinate, is a retinoid (vitamin A derivative) (2).
B-Acitretin is teratogenic. In women with a potential for child-bearing, the
possibility of pregnancy must be excluded before treatment and effective
contraception must be used during treatment and for at least 3 years afterwards
(2)
.
C-Monitor serum-triglyceride, serum-cholesterol, and liver function before
and during treatment (2).
D-Taken with or just after meal. Patient should protect the skin from
sunlight—even on a bright but cloudy day (2).
E-Abstinence from alcoholic beverages should be observed during therapy
and for at least 2 months after acitretin is discontinued (9).

174
Preparations for psoriasis (including both topical and systemic products)
Scientific name Trade names Dosage form
1

Any extra notes:

13.10-Acne and rosacea


13.10.1-Acne
1-Mild to moderate acne is generally treated with topical preparations. Systemic
treatment with oral antibacterials is generally used for moderate to severe acne or
where topical preparations are not tolerated or are ineffective or where application
to the site is difficult (2).
2-Severe acne is usually treated with oral isotretinoin (2).
3-Concerning topical preparations:
A-Topical preparations for acne include: Benzoyl peroxide, azelaic acid,
topical retinoid and topical antibacterials (2).
B- It is usual to start with a lower strength and to increase the concentration of
benzoyl peroxide gradually (to minimize skin irritation) (2).
C-Benzoyl peroxide can bleach clothing and bedding. If it is applied at night,
white sheets and pillowcases are best used and patients can be advised to wear
an old T-shirt or shirt to minimize damage to good clothes (9).
D-Topical tretinoin, its isomer isotretinoin, and adapalene (a retinoid-like
drug), are useful for treating mild to moderate acne. Several months of
treatment may be needed to achieve an optimal response and the treatment
should be continued until no new lesions develop. Patients should be warned
that some redness and skin peeling can occur initially but settles with time (2).
E-Topical retinoids should be applied at night, a half hour after cleansing (7).
F-Important: Topical retinoids are contra-indicated in pregnancy; women
of child-bearing age must use effective contraception (2).

175
G-Topical antibacterials are probably best reserved for patients who wish to
avoid oral antibacterials or who cannot tolerate them. Topical preparations of
erythromycin and clindamycin are effective for inflammatory acne (2).
Clindamycin is currently the preferred topical antibiotic for acne therapy (8).
4-Oral antibiotics are indicated for use in patients with moderate to severe acne and
forms of inflammatory acne that are resistant to topical therapy. Tetracycline,
doxycycline, and minocycline are the most commonly prescribed oral
antibiotics for acne. Erythromycin, azithromycin, and trimethoprim (±
sulfamethoxazole) are appropriate second-line agents for use when patients
cannot tolerate or have developed resistance to tetracycline or its derivatives (8).
5-Topical antibiotics and oral antibiotics should never be used as monotherapy
or as long-term maintenance therapy. Additionally, the use of topical antibiotics
in combination with oral antibiotics should be avoided due to increased risk of
bacterial resistance (8).
6-Cyprindiol (cyproterone acetate with ethinylestradiol) contains an anti-
androgen. It is licensed for use in women with moderate to severe acne that has not
responded to topical therapy or oral antibacterials, and for moderately severe
hirsutism (although it is an effective hormonal contraceptive, it should not be used
solely for contraception) (2).
7-Oral retinoid for acne:
A-The retinoid isotretinoin reduces sebum secretion. It is used for the systemic
treatment of severe acne (such as nodular acne or acne at risk of permanent
scarring) resistant to adequate courses of standard therapy with systemic
antibacterials and topical therapy (2).
B-Isotretinoin is a toxic. It is given for at least 16 weeks; repeat courses are not
normally required (2).
C-Side-effects of isotretinoin include severe dryness of the skin and mucous
membranes, nose bleeds, and joint pains (2).
D-The drug is teratogenic. Women must practise effective contraception for at
least 1 month before starting treatment, during treatment, and for at least 1
month after stopping treatment. They should be advised to use at least
1 method of contraception, but ideally they should use 2 methods of
contraception (2).
8-Spironolactone in higher doses is an
antiandrogenic compound. Doses of 50 to 200 mg
have been shown to be effective in acne in select
women (7).
9-Corticosteroids :
A-Oral corticosteroids in high doses used for
short courses may provide temporary benefit in
patients with severe inflammatory acne. Low-
176
dose prednisone (5–15 mg daily) given alone or with high estrogen-containing
combination oral contraceptives has shown efficacy for acne and seborrhea.
Long-term adverse effects preclude oral corticosteroid use as a primary therapy
for acne (7).
B-Intralesional triamcinolone injections are effective for large individual
inflammatory nodules (7).
13.10.2-Rosacea
1-The pustules and papules of rosacea respond to topical azelaic acid, topical
ivermectin or to topical metronidazole (2).
2-Alternatively oral administration of oxytetracycline or tetracycline, or
erythromycin , can be used; courses usually last 6–12 weeks and are repeated
intermittently. Doxycycline can be used [unlicensed indication] if oxytetracycline
or tetracycline is inappropriate (e.g. in renal impairment) (2).
3-Topical brimonidine tartrate is licensed for the treatment of facial erythema in
rosacea (2).
Topical and oral preparations for acne and Rosacea
Scientific name Trade names Dosage form
1

Any extra notes:

13.11-Preparations for warts and calluses


1-Warts (verrucas) are caused by a human papillomavirus, which most
frequently affects the hands, feet (plantar warts), and the anogenital region (2).
2-Salicylic acid is a useful keratolytic which may be considered first-line for wart
(Apply daily, treatment may need to be continued for up to 3 months); it is also
suitable for the removal of corns and calluses (2).
3-Lactic acid is included in some preparations with salicylic acid. However, there
is no evidence to support greater efficacy when lactic acid is added (5).
177
4-Advise patient to apply carefully to wart and to protect surrounding skin (e.g.
with soft paraffin or specially designed plaster); rub wart surface gently with file or
pumice stone once weekly (2).
5-Other treatment options for wart are formaldehyde, glutaraldehyde,
cryotherapy (cryotherapy causes pain, swelling, and blistering) silver nitrate (2).
6-The treatment of external anogenital warts is by topical application of
podophyllin or imiquimod (It is also licensed for the treatment of superficial basal
cell carcinoma) (2).
(ALDARA ®: imiquimod cream): Manufacturer advises cream should be rubbed
in and allowed to stay on the treated area for 6–10 hours for warts or for 8 hours
for basal cell carcinoma, then washed off with mild soap and water. The cream
should be washed off before sexual contact (2).
Preparations for warts and calluses
Scientific name Trade names Dosage form
1

Any extra notes:

13.12-Sunscreen preparations
1-Sunscreen preparations contain substances that protect the skin against UVA
and UVB radiation, but they are no substitute for covering the skin and avoiding
sunlight (2).
2-The sun protection factor (SPF) provides guidance on the degree of protection
offered against UVB; for example, a SPF of 8 should enable a person to remain 8
times longer in the sun without burning (2).
3-For optimum photoprotection, sunscreen preparations should be applied thickly
and frequently. As maximum protection from sunlight is desirable, preparations
with the highest SPF should be prescribed (2).
4-All products should be applied 20 to 30 minutes before exposure to the sun,
reapplied after 30 minutes and then every 2 hours (5).
5-Sunscreen must be applied to all exposed areas of the body including the nose
ad lips but avoid contact with eye (4).

178
Sunscreen preparations
Scientific name Trade names Dosage form SPF
1

Any extra notes:

13.13-Hair conditions
13.13.1-Androgenetic alopecia
1-Finasteride is licensed for the treatment of androgenetic alopecia in men.
Continuous use for 3–6 months is required before benefit is seen, and effects are
reversed 6–12 months after treatment is discontinued (2).
2-Topical application of minoxidil (1mL twice daily to be applied to the affected
areas of scalp) may stimulate limited hair growth in a small proportion of adults
but only for as long as it is used. Ensure hair and scalp dry before application.
Patients and their carers should be advised to wash hands after application of liquid
or foam (2).
3-Minoxidil is available in 2% and 5% concentrations (5). The 2% and 5%
products are approved for use in both men and women (4).
Preparations for androgenetic alopecia
Scientific name Trade names Dosage form
1

Any extra notes:

13.13.2-Hirsutism
1-Hirsutism may result from hormonal disorders or as a side effect of drugs.
Topical eflornithine can be used as an adjunct to laser therapy for facial hirsutism
in women (2).
2-Co-cyprindiol (cyproterone with ethinylestradiol) may be effective for
moderately severe hirsutism. Metformin is an alternative in women with polycystic
ovary syndrome. Systemic treatment is required for 6–12 months before benefit is
seen (2).

179
Preparations for hirsutism
Scientific name Trade names Dosage form
1

Any extra notes:

13.13.3-Dandruff and seborrhoeic dermatitis


1-Seborrhoeic dermatitis (seborrhoeic eczema) is associated with species of the
yeast Malassezia and affects the scalp, paranasal areas, and eyebrows. Dandruff is
considered to be a mild form of seborrhoeic dermatitis (2).
2-Ketoconazole shampoo is used for seborrhoeic dermatitis and dandruff (leave
preparation on for 3–5 minutes before rinsing ) (treatment: apply twice weekly for
2–4 weeks) (prophylaxis: apply every 1–2 weeks). Selenium sulfide shampoo is
also used (apply twice weekly for 2 weeks, then apply once weekly for 2 weeks,
then apply as required) (2).
3-Cradle cap in infants may be treated with olive oil applications overnight,
followed by using a baby shampoo the next morning. Selenium and etoconazole
should be used for resistant or more moderate disease) (5).
Preparations for dandruff and seborrhoeic dermatitis
Scientific name Trade names Dosage form
1

Any extra notes:

13.14-Antiperspirants
1-Hyperhidrosis (excessive sweating) can be generalized or focal, affecting the
palms of the hands, soles of the feet, or axillae (6).
2-Drug therapy should be tried initially but is often ineffective in severe cases.
Aluminium salts, such as aluminium chloride or aluminium chlorohydrate in
alcoholic solvents applied topically, may be successful in milder forms of focal
hyperhidrosis (6).

181
Antiperspirants (if available )
Scientific name Trade names Dosage form
1

Any extra notes:

References
1-Zeind, Caroline S and Carvalho, Michael G. Applied Therapeutics: The clinical
use of drugs, 11th ed., 2018.
2-BNF-81(2021).
3-Canadian pharmacists association. Therapeutic choices. 2019.
4-American pharmacists association. Handbook of Non-prescription drugs: An
Interactive Approach to Self-Care. 18th edition. 2016.
5-Paul Rutter. Community Pharmacy. Symptoms, Diagnosis and Treatment. 5th
edition. 2021
6-Martindale: The Complete Drug Reference, 38th Edition. Pharmaceutical Press
2014.
7-Joseph T. DiPiro, Robert L. Pharmacotherapy: A Pathophysiologic Approach,
11th Edition. 2021.
8-Marie A. Chisholm-Burns .Pharmacotherapy Principles & Practice. 5th edition.
2019.
9-Alison Blenkinsopp, Paul Paxton and John Blenkinsopp. Symptoms in the
pharmacy . A guide to the managements of common illness. 8th edition. 2018.

181
Index
Abatacept .................... 745 Angiotensin II receptor Benzyl benzoate .......... 761
Abciximab ...................... 27 blockers ..................... 72 Benzylpenicillin ............. 17
Acarbose .................. 82 ,99 Angiotensin receptor– Beta-blockers ................ 71
Aceclofenac ................. 711 neprilysin inhibitor .... 72 Betahistine .................... 61
Acetaminophen ....... 67 ,25 Angiotensin-converting Betamethasone ..... 741 ,89
Acetazolamide ....... 772 ,77 enzyme inhibitors ...... 77 Betrixaban ..................... 22
Acetic acid 2%.............. 774 Anidulafungin ................ 97 Bevacizumab ................. 86
Aciclovir . 766 ,746 ,777 ,97 Antacids ................... 11 ,12 Bezafibrate .............. 79 ,71
Acipimox ........................ 71 Anthelmintics ................ 92 Biguanides ............... 98 ,99
Acitretin ............... 714 ,711 Anti-arrhythmic drugs ... 24 Bilastine ......................... 75
Acrivastine ..................... 75 Antiepileptic drug .......... 76 Bile acid sequestrants ... 71
Adalimumab .. 711 ,745 ,21 Antifungal766 ,767 ,746 ,97 Biosimilars ................... 745
Adefovir ......................... 94 Antihistamine ,748 ,71 ,18 Bisacodyl ....................... 14
Adsorbents .................... 11 771, 715 ,761,, ,61 77 ,75 Bismuth ......................... 15
Aflibercept ..................... 86 749 Bisphosphonates ......... 755
Agomelatine .................. 78 Antiplatelet drugs.... 27 ,25 Botulinum toxin type A . 66
Alafenamide .................. 94 Antipsychotics ......... 79 ,77 Bran ............................... 14
Albendazole ................... 92 Antispasmodics ............. 19 Brexpiprazole ................ 79
Albuterol ........................ 44 Antithyroid drugs .... 89 ,81 Brimonidine......... 711 ,772
Alendronic acid ............ 755 Antituberculosis ...... 95 ,18 Brinzolamide ............... 772
Alfacalcidol .................. 728 Apixaban.................. 21 ,22 Brivaracetam ................. 76
Alginates ........................ 11 Apraclonidine .............. 772 Bromocriptine ..... 757 ,754
Allopurinol ................... 742 Aripiprazole ................... 79 Brompheniramine ......... 77
Almotriptan ................... 67 Ascorbic acid ....... 728 ,722 Buclizine ........................ 75
Alogliptin ....................... 99 Asenapine ...................... 79 Budesonide .. 44,776,46,41
Alphagan-P .................. 772 Aspirin ,711 ,86 ,67 ,64 ,27 Bulk-forming laxative17 ,14
Alpha-glucosidase inhibitor 741 ,747, 727 Bumetanide ................... 77
................................... 99 Atenolol ......................... 71 Bupropion ............... 69 ,78
Alprazolam..................... 71 Atorvastatin............. 79 ,71 Caffeine ....................... 717
Alteplase ........................ 27 Atosiban ...................... 776 Calamine ..................... 715
Alverine ......................... 19 Atropine ........................ 16 Calciferol ..................... 728
Amantadine ............. 61 ,62 Avibactam...................... 12 Calcipotriene ............... 711
Amikacin .................. 18 ,15 Azelaic acid .......... 711 ,717 Calcitriol .............. 711 ,728
Amiloride ....................... 77 Azilsartan ....................... 72 Calcium carbonate ,755 ,11
Aminoglycosides .... 746 ,15 Azithromycin ..... 14,16,746 726
Aminophylline ... 48 ,44 ,41 Aztreonam ..................... 14 Calcium gluconate ....... 726
Aminosalicylates ...... 29 ,21 Bacitracin ..................... 764 Calcium-channel blockers74
Amiodarone ................... 24 Baclofen....................... 744 Canagliflozin .................. 99
Amitriptyline............ 66 ,78 Balsalazide ................ 21,29 Candesartan ............ 66 ,72
Amlodipine .............. 77 ,74 Baricitinib .................... 714 Cangrelor ....................... 27
Amorolfine................... 767 Beclometasone.............. 44 Capsaicin ......... 714 ,86 ,67
Amoxicillin777 ,16 ,17 ,17 ,15 Benzalkonium chloride ,748 Captopril........................ 77
Amoxicillin–clavulanate16,777 772 Carbamazepine . 86 ,67 ,76
Amphotericin B.............. 97 Benzathine penicillin G.. 16 61
Ampicillin ......... 17, 142, 16 Benzhexol ...................... 61 Carbapenems .......... 17 ,15
Anakinra ...................... 745 Benzodiazepine ....... 71 ,19 Carbidopa/Levodopa..... 62
Benzoyl peroxide ......... 717

182
Carbimazole ................... 81 Clindamycin716 ,764 ,777 ,11 Dasabuvir ...................... 94
Carbomers ................... 748 Clomifene .................... 752 Degludec ....................... 81
Carboprost ................... 771 Clonazepam ................... 76 Dehydroepiandrosterone,
Cariprazine..................... 79 Clopidogrel .............. 28 ,27 better ...................... 712
Caspofungin ................... 97 Clotrimazole ,767 ,774 ,774 Delafloxacin ................... 11
Cefadroxil ...................... 17 768 Desipramine .................. 78
Cefalexin ........................ 17 Clozapine ....................... 79 Desloratadine ................ 75
Cefepime ....................... 17 Coal tar ................ 714 ,711 Desmopressin...... 777 ,754
Cefixime .................... 17,12 Cobalamins .................. 728 Desvenlafaxine .............. 78
Cefotaxime .................... 17 Coconut oil .................. 717 Detemir ......................... 81
Cefpodoxime ............ 17,12 Co-cyprindiol ............... 718 Dexamethasone741 ,89 ,18
Ceftaroline ..................... 17 Codeine ......................... 72 Dextromethorphan .. 72,77
Ceftazidime............... 17,12 Colchicine ............ 742 ,747 Diazepam .............. 744 ,71
Ceftriaxone ............... 17,12 Colecalciferol ............... 728 Diclofenac778 ,741 ,711 ,716
Cefuroxime ............ 746 ,17 Colesevelam .................. 71 Digoxin .......................... 24
Celecoxib ..................... 711 Colestipol....................... 71 Dihydroergotamine ....... 66
Cephalosporins 746 ,12 ,17 Colestyramine ............... 71 Diloxanide furoate ........ 91
Certolizumab ......... 745 ,21 Colloids ........................ 717 Diltiazem ....................... 74
Cerumunolytics............ 777 Combined oral contraceptives Dimethindene ............... 75
Cetirizine........................ 75 ................................. 779 Dimeticone .................. 769
Cetrimide ..................... 769 Co-phenotrope .............. 16 Dinoprostone .............. 776
Chamomile .................. 717 Coq-10 ......................... 717 Dipeptidyl peptidase-4 (DPP-
Chloramphenicol ......... 746 Corticosteroids ,46 ,41 ,47 ,21 4) inhibitors .......... 87,99
Chlordiazepoxide ........... 71 ,747 ,717 ,714 ,88 ,89 ,41 Diphenhydramine765 ,77 ,75
Chlorhexidine769 ,765 ,778 ,771 ,776 ,749 ,741 ,741 Diphenoxylate ............... 16
Chloroquine ................. 727 ,717 ,767 ,765 ,778 ,779 Dipyridamole ................. 27
Chlorphenamine ...... 77 ,75 716 ,714 ,711 Direct Oral Anticoagulants22
Chlorpromazine ............. 79 Cortisone Acetate.......... 89 Docusate ..................... 777
Chlortalidone ................. 77 Co-trimoxazole .............. 19 Domperidone ... 754 ,18,67
Chondroitin.. 718 ,714 ,717 Cranberry .................... 712 Donepezil ...................... 77
Ciclosporin 711,714,775,21 Creatine ....................... 712 Dopamine ........ 754 ,62 ,78
Cilastatin .................. 17 ,15 Crotamiton .......... 715 ,761 Dorzolamide ................ 772
Cilostazol ................. 86 ,27 Cryotherapy................. 719 Dosulepin ...................... 78
Cimetidine ..................... 28 Crystalloids .......... 717 ,715 Doxazosin .................... 756
Cinnamon .................... 717 Cyprindiol .................... 716 Doxepin .................. 715,78
Cinnarizine ........... 75,61,18 Cyproheptadine............. 75 Doxycycline711 ,765 ,86 ,19
Ciprofibrate ................... 71 Dabigatran ................ 21,22 Doxylamine .............. 77,18
Ciprofloxacin746 ,727 ,11 ,21 Daclatasvir ..................... 94 Dulaglutide .................... 87
Citalopram ..................... 78 Dalteparin ...................... 22 Duloxetine714 ,775 ,86 ,78
Clarithromycin747 ,14 ,17 ,15 Dantrolene .................. 744 Dutasteride ................. 751
Clarithromycin ......... 14 ,15 Dapagliflozin .................. 99 Echinacea .................... 712
Clavulanic acid ......... 16 ,17 Dapoxetine .................. 772 Echinocandin ................. 97
Clemastine ..................... 75 Dapsone ...................... 727
Darbepoetin ................ 724
Darifenacin .......... 775 ,759

183
Econazole............. 767 ,774 Fibrates.................... 79 ,71 Glucagon-like peptide-1
Edoxaban ................. 21 ,22 Finasteride............ 751,718 receptor agonists ...... 87
Eflornithine .................. 718 Flaxseed oil .................. 712 Glucosamine ,719 ,714 ,712
Elbasvir .......................... 94 Flucloxacillin ............. 16,17 718
Eletriptan ....................... 67 Fluconazole ................... 97 Glutaraldehyde ........... 719
Emergency hormonal Flucytosine .................... 97 Glycerin ........... 772 ,17 ,14
contraception .......... 778 Fludrocortisone ............. 86 Glyceryl trinitrate ...... 78 ,9
Emollients .... 711 ,715 ,768 Fluoride ............... 767 ,765 Glycopeptide ................. 11
Empagliflozin ................. 99 Fluoroquinolones ,18 ,11 ,17 Golimumab.... 711 ,745 ,21
Enalapril ......................... 77 721 Golimumab.................. 747
Enoxaparin..................... 22 Fluoxetine ................ 65 ,78 Gonadotrophins .......... 751
Entacapone.................... 62 Fluphenazine ................. 79 Gramicidin ................... 764
Entecavir ........................ 94 Flurbiprofen......... 765 ,741 Granisetron ................... 18
Ephedrine .............. 776 ,77 Fluticasone ........ 44,776,41 Grazoprevir ................... 94
Epinephrine ................... 75 Fluvastatin ..................... 71 Griseofulvin767 ,778 ,779 ,97
Epoetins ............... 727 ,724 Fluvoxamine .................. 78 Griseofulvin ................... 97
Eprosartan ..................... 72 Folic acid ...................... 726 Growth hormone 754 ,751
Eptifibatide .................... 27 Folinic acid ................... 717 Guaifenesin ............. 72 ,77
Erenumab ...................... 66 Follicle-stimulating hormone Haloperidol.................... 79
Ergometrine................. 771 ................................. 751 Histamine-2 receptor
Ergotamine tartrate....... 66 Formaldehyde ............. 719 antagonists ................ 28
Ertapenem ............... 17 ,15 Formoterol .. 41 ,46 ,47 ,44 Hormone replacement
Ertugliflozin.................... 99 Foscarnet ....................... 97 therapy .................... 757
Erythromycin711 ,716 ,86 ,14 Fosfomycin .................... 95 Hyaluronic acid derivatives
Escitalopram .................. 78 Fosinopril ....................... 77 ......................... 718 ,714
Eslicarbazepine .............. 76 Framycetin............ 774,764 Hydrochlorothiazide ..... 77
Esomeprazole .......... 28 ,29 Fremanezumab ............. 66 Hydrocortisone768 ,89 ,44,
Etanercept ................... 745 Frovatriptan................... 67 715,717,741 ,89
Ethambutol .................... 18 Furosemide.................... 77 Hydrogen peroxide769 ,778
Ethosuximide ................. 76 Fusidic acid .... 764 ,746 ,95 Hydroxychloroquine717 ,714
Etodolac ....................... 711 Gabapentin ......... 67,86 ,76 Hydroxyzine................... 75
Etoricoxib..................... 711 Galantamine .................. 77 Hypochlorite................ 769
Exenatide ....................... 87 Galcanezumab ............... 66 Hypromellose .............. 748
Ezetimibe ................. 79 ,71 Garlic ........................... 712 Ibandronic acid............ 755
Ezogabine ...................... 76 Gatifloxacin ................... 11 Ibuprofen .................... 711
Famciclovir ............ 777 ,97 Gemeprost................... 776 Iloperidone .................... 79
Famotidine .............. 15 ,28 Gemfibrozil .................... 71 Imidapril ........................ 77
Febuxostat ................... 742 Gemifloxacin ................. 11 Imidazole ..................... 767
Felbamate ...................... 76 Gentamicin .... 774 ,746 ,15 Imipenem ................. 15,17
Felodipine ................ 77 ,74 Ginger .......................... 712 Imipramine ............. 777,78
Fenofibrate .................... 71 Ginkgo biloba .............. 712 Imiquimod ................... 719
Fenticonazole .............. 774 Ginseng........................ 712 Indometacin ................ 711
Ferric citrate ................ 721 Glargine ......................... 81 Infliximab.. 21,745,711,747
Fesoterodine ............... 775 Glibenclamide ......... 98 ,99
Feverfew ...................... 712 Gliclazide ....................... 99
Fexofenadine ................. 75 Glimepiride .............. 98 ,99
Glipizide .................... 98,99

184
Insulin ,81 ,82 ,87 ,85 ,98 ,99 Lixisenatide.................... 87 Miconazole .. 767 ,779 ,774
87 ,84 Lofepramine .................. 78 Midodrine...................... 86
Insulin aspart ........... 84 ,81 Loop diuretics ................ 76 Mifepristone ........ 771,776
Insulin glulisine ........ 84 ,81 Loperamide ............. 19 ,16 Milk thistle .................. 712
Insulin lispro ............ 84 ,81 Loprazolam .................... 71 Minoxidil ..................... 718
Interferon ...................... 94 Loratadine ..................... 75 Mirabegron ......... 775 ,759
Ipratropium ....... 41,779,44 Lorazepam ................ 18,71 Mirtazapine ................... 78
Irbesartan ...................... 72 Lormetazepam .............. 71 Misoprostol ......... 771 ,776
Iron dextran ................. 721 Losartan ......................... 72 Mizolastine .................... 75
Isavuconazole ................ 97 Low molecular weight Mometasone ... 776 ,41 ,44
Isoniazid ............ 18,728,I95 heparins ..................... 22 Monoamine oxidase inhibitors
Isosorbide dinitrate ....... 25 Loxapine ........................ 79 ................................... 78
Isosorbide mononitrate. 25 Lurasidone ..................... 79 Monobactam................. 14
Isotretinoin .......... 716 ,717 Luteinizing hormone ... 751 Monovisc ..................... 718
Ispaghula ....................... 14 Macrolides ............. 746 ,14 Montelukast ............ 49 ,44
Isradipine ....................... 74 Magnesium...... 765 ,11 ,12 Moxifloxacin746 ,727 ,18 ,11
Itraconazole ................... 97 Magnesium.................. 721 Multivitamin preparations715
Ivermectin ............. 761 ,92 Malathion ............. 761,769 Mupirocin .................... 764
Kaolin ............................. 11 Mannitol ............ 772,77,76 Mycophenolate714 ,711 ,721
Ketoconazole ........ 767,795 Mast cell stabilizers ....... 48 Nalidixic acid ................. 11
Ketoprofen .................. 711 Mebendazole ................ 92 Naphazoline ................ 776
Ketotifen ................ 741 ,75 Mebeverine ................... 19 Naphazoline-Antazoline.)748
Lacosamide .................... 76 Mefenamic acid ........... 711 Naproxen ..................... 711
Lactic acid .................... 711 Meglitinides ............. 85 ,99 Naratriptan .................... 67
Lactulose.............. 17,19,14 Melatonin ........ 712 ,78 ,71 Natalizumab .................. 21
Lamivudine .................... 94 Meloxicam ................... 711 Nateglinide .............. 85 ,99
Lamotrigine ................... 76 Memantine .................... 77 Nefazodone ................... 78
Lansoprazole ........... 28 ,29 Menadione .................. 727 Nefopam ....................... 67
Lanthanum .................. 721 Mepolizumab ................ 44 Neomycin ...... 774 ,746 ,15
Latanoprost ................. 777 Meropenem ............. 15,17 Nicardipine .................... 74
Ledipasvir ...................... 94 Mesalamine ................... 21 Nicotinic acid ................. 71
Leflunomide......... 717 ,714 Mesterolone ................ 752 Nifedipine .............. 776 ,74
Leukotriene Receptor Metformin ....... 718 ,98 ,99 Nimodipine.................... 74
Antagonists .......... 49 ,44 Methimazole ................. 81 Nisoldipine .................... 74
Levamisole ..................... 92 Methotrexate ,714 ,726 ,21 Nitrates.................... 25 ,78
Levetiracetam ................ 76 717,714,711 Nitrofurantoin ....... 727 ,97
Levocetirizine ................ 75 Methoxy polyethylene glycol- Nitroglycerin.................. 78
Levodopa ....................... 62 epoetin beta ............ 724 Nizatidine ................ 15 ,28
Levofloxacin746 ,18 ,11 ,17 Methylcellulose ............. 14 Nonoxynol-8-............... 725
Levonorgestrel............. 778 Methyldopa ................... 27
Levothyroxine ................ 81 Methylprednisolone741 ,89
Linagliptin ...................... 99 Metoclopramide 86 ,67 ,18
Lincomycin ..................... 11 Metronidazole . ,17 ,15 ,21
Liraglutide .......... 87 ,47 ,45 17.711 ,777 ,86 ,91,764
Lisinopril ........................ 77 Mianserin ...................... 78
Lithium........................... 61 Micafungin .................... 97

185
Non-steroidal anti- Paritaprevir.................... 94 Pridinol ........................ 744
inflammatory drugs . ,61 Paroxetine ............... 65 ,78 Primaquine .................. 727
714, 777 ,741 ,747 716, Pectin............................. 11 Primidone ...................... 76
765, ,716 ,714 ,67 ,61,64 Penciclovir ................... 766 Probiotics .............. 712 ,11
,741 ,742 ,747 ,719 ,711 Penicillins................. 16 ,17 Prochlorperazine61 ,67 ,18
749 Pentoxifylline................. 27 Procyclidine ................... 61
Noradrenaline reuptake Peppermint oil ............... 19 Progestogen . 778,752 ,757
inhibitors ................... 78 Perampanel ................... 76 Promethazine ................ 77
Norfloxacin .................. 727 Perindopril ..................... 77 Propranolol ....... 89 ,66 ,71
Nortriptyline ............ 86 ,78 Permethrin ........... 761,761 Propylthiouracil ............. 81
NPH .......................... 81 ,82 Perphenazine ................ 79 Protamine sulfate.......... 22
Nystatin .... 779,765,767,97 Phenazopyridine.......... 771 Proton pump inhibitors . 29
Octreotide ..................... 86 Phenelzine ..................... 78 Pseudoephedrine .... 71 ,77
Ofloxacin........ 746 ,727 ,18 Phenobarbital ................ 76 Psoralen ...................... 714
Ofloxacin........................ 11 Phenothiazine ............... 19 Pyrazinamide................. 18
Olanzapine ................ 61,79 Phenoxymethylpenicillin17 Pyridoxine ....... 728 ,18 ,18
Olmesartan .................... 72 Phenylephrine ........ 776,77 Pyridoxine ................... 728
Olopatadine ................. 741 Phenytoin ...................... 76 Quetiapine .......... 61,71,79
Olsalazine ................. 21,29 Pholcodeine.............. 72,77 Quinapril ....................... 77
Omalizumab .................. 44 Phosphate-binding agents721 Quinidine ..................... 727
Ombitasvir ..................... 94 Phosphodiesterase inhibitors Quinolones .... 746 ,727 ,11
Omega-3 fatty acid ........ 71 .................... 756,759,44 Rabeprazole ............ 28 ,29
Omeprazole ............. 28 ,29 Pimecrolimus ............... 714 Ranibizumab.................. 86
Ondansetron.................. 18 Pioglitazone .............. 85,99 Ranitidine ...................... 28
Opioid analgesics ........... 64 Piperacillin ..................... 17 Rasagiline ...................... 62
Oral iron............... 721 ,722 Piroxicam ..................... 711 Rasburicase ................. 727
Oral progestogen-only Podophyllin ................. 719 Reboxetine .................... 78
contraceptives ......... 778 Polyene .......................... 97 Relebactam ................... 17
Oral rehydration solution11 Polymyxin B ......... 764 ,746 Repaglinide............... 85,99
Orlistat ..................... 47 ,45 Polymyxins .................. 774 Reslizumab .................... 44
Oseltamivir .................... 96 Polyvinyl alcohol.......... 748 Reteplase....................... 27
Osmotic laxative ............ 14 Posaconazole................. 97 Riboflavin .................... 728
Oxcarbazepine ............... 76 Potassium ,721 ,771 ,76 ,77 Rifampicin ................ 18,95
Oxybutynin .......... 775 ,759 768 Risedronate sodium .... 755
Oxymetazoline....... 776 ,77 Potassium permanganate768 Risperidone .............. 61,79
Oxytocin............... 771 ,776 Potassium-sparing diuretics Ritonavir ........................ 94
Paliperidone .................. 79 ................................... 76 Rituximab ............. 745,747
Palonosetron ................. 18 Povidone-iodine .......... 769 Rivaroxaban .................. 22
Pamaquin..................... 727 Pramipexole .................. 62 Rivastigmine .................. 77
Pamidronate disodium 755 Prasugrel ....................... 27 Rizatriptan ..................... 67
Pantoprazole ........... 28 ,29 Pravastatin .................... 71 Roflumilast .................... 44
Paracetamol ............ 64 ,61 Praziquantel .................. 92 Ropinirole ...................... 62
Parecoxib ..................... 711 Prednisolone ... 741 ,89 ,44 Rosiglitazone ................. 85
Parenteral iron .... 724 ,721 Prednisone .............. 89 ,46 Rosuvastatin ............ 79 ,71
Parenteral progestogen-only Pregabalin....... 67,86,76,71 Rowatinex ................... 771
contraceptives ......... 778 Rufinamide .................... 76
Rupatadine .................... 75

186
Sacubitril ........................ 72 Spiramycin ............... 91 ,14 Tinidazole .. 777 ,91 ,17 ,15
Salbutamol............. 776 ,47 Spironolactone 716 ,76 ,77 Tinzaparin ...................... 22
Salbutamol..................... 44 St. John’s wort ............. 712 Tiotropium .............. 41 ,44
Salicylic acid ......... 711 ,714 Statins ...................... 79 ,71 Tirofiban ........................ 27
Salmeterol ............... 41 ,44 Sterculia......................... 14 Tizanidine .................... 744
Sarilumab..................... 745 Stimulant laxative.......... 14 Tobramycin ........... 746 ,15
Saw palmetto ...... 712 ,758 Stiripentol ...................... 76 Tocilizumab ................. 745
Saxagliptin ..................... 99 Streptomycin ................. 15 Tocolytics .................... 776
Secukinumab ............... 745 Sucroferric oxyhydroxide721 Tofacitinib714 ,711 ,714 ,21
Selective serotonin reuptake Sulfamethoxazole .......... 19 Tolbutamide .................. 99
inhibitor ........... 19,78,65 Sulfasalazine .... 714 ,29 ,21 Tolcapone ...................... 62
Selegiline ................. 62 ,78 Sulfonamides ,85 19,727,98 Tolnaftate .................... 767
Selenium .............. 795 ,729 Sulindac ....................... 711 Tolterodine ........... 759,775
Semaglutide ................... 87 Sulphonylureas .............. 99 Topiramate ............... 66,76
Senna ............................. 14 Sumatriptan................... 67 Torasemide ................... 77
Serotonin and noradrenaline Sunscreen ............ 718 ,719 Tramadol ............... 714 ,64
re-uptake inhibitors ... 78 Tacrolimus ....... 21,714,711 Trandolapril ................... 77
Serotonin and α2-adrenergic Tadalafil ......... 772 ,759 ,86 Tranylcypromine ........... 78
antagonist .................. 78 Tafluprost .................... 777 Trazodone ..................... 78
Sertraline ....................... 78 Tamoxifen.................... 751 Tretinoin ...................... 717
Sevelamer .................... 721 Tamsulosin .......... 751 ,756 Triamcinolone741 776,711,89
Sildenafil ................ 772 ,86 Tazarotene .......... 714 ,711 Triamterene .................. 77
Silodosin ...................... 756 Tazobactam ............. 17 ,12 Triazole .......................... 97
Silver nitrate ................ 719 Teicoplanin .................... 11 Tricyclic antidepressant ,19
Silver sulfadiazine ........ 764 Telavancin ..................... 11 777 ,66 ,65 ,67,78
Simeprevir ..................... 94 Telbivudine .................... 94 Trifluoperazine .............. 79
Simeticone ..................... 11 Telmisartan.................... 72 Trihexyphenidyl............. 61
Simvastatin .............. 79 ,71 Temazepam ................... 71 Trimethoprim ........ 716 ,19
Sitagliptin ....................... 99 Temocillin ...................... 17 Trimipramine................. 78
Sodium bicarbonate778 ,777 Tenecteplase ................. 27 Triprolidine .................... 77
Sodium chloride 0.9%, . 769 Tenofovir ....................... 94 Trospium ..................... 775
Sodium clodronate ...... 755 Tenoxicam ................... 711 Tryptophan .................... 78
Sodium cromoglicate ,48 ,44 Terazosin ..................... 756 Ulipristal ...................... 752
771 ,749 Terbinafine .................. 767 Ulipristale .................... 778
Sodium hyaluronate .... 775 Terbutaline ...... 776 ,47 ,44
Sodium picosulfate ........ 14 Testosterone751 ,756 ,752 ,9
Sodium-glucose cotransporter Tetracycline711 ,716 ,19 ,15
............................. 87 ,99 Tetracycline ........... 716 ,19
Sofosbuvir ...................... 94 Tetracyclines ........... 18 ,19
Soft Paraffin ................. 768 Theophylline ...... ,28,48,44
Solifenacin ........... 759,775 Thiamine...................... 728
Spermicidal contraceptives
................................. 725

187
Unfractionated Heparin 22
Upadacitinib ................ 714
Ustekinumab .......... 21,745
Vaborbactam ................. 17
Valaciclovir ............ 777 ,97
Valerian ....................... 712
Valproate ................. 61 ,76
Valsartan........................ 72
Vancomycin ................... 11
Vardenafil .............. 772 ,86
Vasopressin ................. 754
Vedolizumab .................. 21
Velpatasvir ..................... 94
Venlafaxine .................... 78
Verapamil .......... 24 ,77 ,74
Vigabatrin ...................... 76
Vilazodone ..................... 78
Vildagliptin..................... 99
Vitamin A ..................... 729
Vitamin B Substances .. 729
Vitamin C ..................... 728
Vitamin D ..................... 728
Vitamin E ..................... 728
Vitamin K ............... 728 ,21
Voriconazole .................. 97
Vortioxetine ................... 78
Voxilaprevir ................... 94
Warfarin ............. 21,28,22
Xylometazoline ...... 776 ,77
Zafirlukast ................ 49 ,44
Zaleplon ......................... 71
Zanamivir ....................... 96
Zileuton.......................... 49
Zileuton.................... 49 ,44
Zinc .................. 721 ,11 ,11
715 ,768
Ziprasidone .................... 79
Zoledronic .................... 755
Zoledronic acid ............ 755
Zolmitriptan ................... 67
Zolpidem ........................ 71
Zonisamide .................... 76
Zopiclone ....................... 71

188
‫الدكتور ضيـــــــــاء جبـــــار كاظـــــــــم‬
‫تولــــــــــــــــــد‪ :‬بغداد ‪ 4797‬م‪.‬‬
‫بكالوريوس علوم صيدلة‪ :‬كلية الصيدلــــــة ‪ -‬جامعة بغــــــــداد ‪ 4779/‬م‪.‬‬
‫ماجستير صيدلة سريرية‪ :‬كلية الصيدلــــــة ‪ -‬جامعة بغــــــــداد ‪ 5008/‬م‪.‬‬
‫دكتوراه صيدلة سريرية‪ :‬كلية الصيدلــــــة ‪ -‬جامعة بغــــــــداد ‪ 5046/‬م‪.‬‬
‫تدريسي في فرع الصيدلة السريرية ‪ /‬كلية الصيدلــــــة ‪ -‬جامعة بغــــــــداد‪.‬‬

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