:Lecture 15

.Other therapies

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 I. Ophthalmic preparations
:Anatomy*

Eyelids)1
External eye: lacrimal apparatus + cul-de-sac)2

N.B * the capacity of eye for instilled ophthalmic drops: 0.01- 0.05 ml
less than 0.02 ml of ophthalmic solution can be placed successfully in eye  but *
this volume is less than 0.05 ml [ /drop] that commonly prescribed. Explain
A portion of the dose is lost through drainage over the cheek

:Internal eye )3
conjunctiva: mucous membrane that lines eyelids-
sclera: outer coating of the eye ball-
Iris: colored membrane that regulate color entrance through pupil-
lens: transparent membrane that focus rays on retina-
retina: receive image formed by lens-
Trabecular meshwork and schlemm's canal  exit pathway for aqueous *-
.humor

:N.B Cornea is composed of 3 layers

Epithelium [outer layer], Stroma [least lipophilic], Endothelium [inner layer]
So cornea "lipophilic+ hydrophilic layers" drug to pass through it must exist
.in both ionized and un ionized form at physiological pH
:Some eye disorders & ttt

Disorder .How to know it ttt

A) conjunctivitis
.Viral-1
.Allergic-2
Bacterial & Chlamydial-3
B)Insufficient tearing
e.g. Sjogren's syndrome
.Pink eye Artificial tears
Topical decongestant
.Eye itching Topical decongestant
Anti histaminic
Cromolyn Na 4%
--------------- ttt é prescription AB
----------------- artificial tears

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 :imp*ophthalmic products contain the following agents

Antioxidants and -1 e.g. Na bisulfite

stabilizers
: Buffers-2 Keep product pH between 6-8 eg. Boric à, acetic à
:preservatives-3 Combination between Benzalkonium chloride (0.01%) + Edeta (0.01%)*
the most effective for ophthalmic use
phenyl mercuric nitrate 0.002% (bacteriostatic & sporocidal)*

N.B phenyl group in phenyl mercuric nitrate: leads to less solubility than
.other inorganic salts
:Bactericidal preservatives to eye drops
benzalkonium chloride 0.01%-1
2chlorohexidine acetate 0.01%

:Effectiveness of preservatives depend on

conc. of preservative : increase in conc.increase in effectiveness but too*1
high conc. tearing and irritation
degree of contamination & MOs strains*2
Preservative is considered effective if it will re-sterilize the eye solution *
within 1 hr. Explain
>---‫> تلوث‬-----‫ بعد ما افتح القطرة‬Preservative re-sterilize it before next dose
Clarifying or )4 reduce surface tension of the lens e.g. Polysorbate 20 & Polysorbate 80
:wetting agent
Viscosity )5 Examples [hydroxy Propyl methyl cellulose - polyvinyl alc - polyvinyl *
:increasing agents pyrolidine - methyl cellulose]

Use: increase ocular contact time between drug and cornea to increase *
amount of drug absorption

:some terms*
a)Liquifilm: it is used when the ophthalmic solution contains polyvinyl alc
.b)Isopto: ophthalmic solution contain hydroxy propyl methyl cellulose

:put right or wrong

veegum is the best viscosity builder for ophthalmic preparation. [x]
it is a clay
Tonicity ) 6 .....e.g dextrose, glycerin, KCl, NaCl
:adjusters Increase or decrease tonicity eye irritation
e.g a) purified H2Ohypertonic irritation
b)Na sulfacetamide30% hypertonic irritation
‫اوكيوسول‬
any solution of Na Sulfacetamide stronger than 12% will irritate and *
.sting the eye so the patient should be warned to expect this

N.B NaCl conc. from 0.5% 2% can be put into either normal or inflamed
.eye without causing pain

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 :Sterilization of eye drops*
Membrane filtration through 0.22 u porosity-1
Autoclave 115 Celsius for 30 min-2
.Heating with bactericidal at 100 Celsius for 30 min-3

:M.O that contaminate eye products

pseudomonas .1 imp1- Fluorescein sodium if contaminated é pseudomonas aeruginosa

aeruginosa ?and soln applied to the eye blindness. Why
Fluorescein Na is diagnostic agent that is used to determine corneal
damage so contaminated solu with p. aeruginosa pass easily
.through damaged corneainterior of eye ball blindness
Pharmaceutical manufacturer supply it as unit dose solution or ∴
.individual paper strip
Acanthamoeba-2  its microorganism that cause ophthalmic keratitis in patients using
.contact lens soln
Acanthamoeba removed by thermal disinfection

:Color code for some ophthalmic products *

Red top: Mydriatic e.g Atropine
Green Top: Miotic e.g Pilocarpine

:Storage conditions for some ophthalmic products*

Chloramphenicol & 1% Epinephrine refrigeration 0.5% -
N.B 1%epinephrine is used in ttt of glaucoma (open angle)
Na Sulfacetamide cool place : +15 Celsius no need for refrigeration but if -
.no problem

:Put (T) or (F)*

Cortisone eye drops should be stored between 2- 8 Celsius [false]-
Phosphoiodine I2 drops between 2 - 8 Celsius [ true]
ttt glaucoma

:Medical agents
there is no FDA approved anti infective products available for OTC ophthalmic *
.use
:OTC products

:Astringents )1 the only FDA approved astringent is zinc sulfate [0.25%] relief eye
irritation
:Demulcents )2 e.g all viscosity increasing agents
Decongestants & )3 ]Naphazoline HCl, tetrazoline HCl & Phenylephrine[
vasoconstrictors Rebound congestion occur é long duration of use*
C.I patients é narrow angle glaucoma*
Hypertonic agents)4 e.g NaCl 2-5% ---> ttt of corneal swelling
Artificial tears )5 for Sjogren's síndrome
N.B If more than one ophthalmic product is usedseparate by 5 mins
Ophthalmic ointment :may blur vision if used during waking hours *
‫المرهم دايما قبل النوم‬

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 after instillation of eye dropgently squeeze inner corner of eye near nose for 1*
min, that will reduce amount of drug lost through tear duct to the nose B.

:Contact lenses
: Types
1)Daily wear soft lenses removed and cleaned nightly & require once weekly enzymatic
cleaning by contact lenses cleanser tabs
2) Daily wear disposable soft single use
lenses: ‫مرة وتترمي‬
3) Extended wear soft lens: designed to warm continuously for up to 6 nights
4)Frequent replacement of
soft lenses
5) Rigid gas permeable hard lens available as daily and extended wear versions
[RGP] lenses:
N.B Cleanser tabs:
may contain one of the following [papain-subtilisin-pancreatin]
they are proteolytic enzymes that aids in removal of proteinocous residues that
slowly build up on soft lenses during wear.

*Which one of the following products isn't needed by wearer of

flexible hydrophilic lenses:
a)cleaning products b)disinfection system
c)wetting products d)Rejuvenation system
Answer is (c) bcz the lens is already hydrophilic & the use of wetting products is
to change lens surface from hydrophobic to hydrophilic

*Disinfection :for hygiene storage of soft lenses by killing. m.o E.g hydrogen
peroxide

*Rejuvenation System: remove heavy residues that slowly build up in soft lenses

N.B Tetracaine HCL is useful for topical eye anesthesia why??

1)5-8 times more potent than cocaine
2) doesn't cause mydriasis, cycloplegia or intraocular HTN

Sterilization of contact lenses:

1-soaking in saline &heat for 15 min
2-soaking in soln [preservative]

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 C. Glaucoma (Ocular HTN):
*It is the increase in IOP
Normal IOP 10-20 mmHg.

*Types of Glaucoma:
1. Acute closed angle glaucoma:
This is a rare ophthalmic emergency; treatment is by peripheral laser iridotomy.
Oral, IV, and topical medication is necessary to stabilize the eye and lower the
pressure before laser iridotomy; IV Acetazolamide, topical Pilocarpine, a topical
beta-blocker, mannitol or oral glycerol may be used; seek specialist advice.

2. Chronic (primary) open angle glaucoma:

The conventional approach is to use topical drugs (usually one, occasionally 2 or
more) as first line, followed by laser trabeculoplasty or filtration surgery
(trabeculectomy).
Drugs used to treat open angle glaucoma are :

A) decrease aqueous humor production B) increase in aqueous humor drainage

B-antagonist e.g. Timolol, levbulol, )1 Prostaglandin analogues: Latanoprost
Betaxolol
Sympathomimetics e.g. Epinephrine)2 Parasympathomimetics: Pilocarpine
Carbonic anhydrase inhibitors: )3
.Acetazolamide, Brinzolamide, Dorzolamide
:The only agent that works by both mechanisms
i.e. decrease in aqueous humor production and increase in aqueous humor drainage is alpha 2
agonists Brimonidine (alphagan)

N.B Loteprednol: corticosteroid for allergic conjunctivitis.

*For emergency ttt of Acute closed angle glaucoma unresponsive to
conventional treatment we give Mannitol.

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 :II. Pediculicides
Pediculus capitis: head lice transmitted head to head contact
.Pediculus pubis: pubic lice transmitted by sexual contact

A. OTC products ttt

Pyrethrin é piperonyl butoxide)1 Pyrethrin: parasitc neurotoxin*
]head &pubic lice[ Piperonyl butoxide: enhance effect of pyrethrin by *
.suppressing oxidative degradation mechanisms of the lice
Premethrin [Head lice only] )2 It is a synthetic derivative of pyrethrin
Method of use*
pyrethrin : apply to dry hair*)1
Premethrin: apply to hair after the hair has been shampooed, rinsed and towel dried *
leave the product on head for 10 minutes)2
rinse é warm H2O)3
dry é disposable cloth)4
comb hair é fine toothed comb to remove dead lice & eggs )5
Re ttt may occur after 7 days)6

N.B pyrethrin containing products should be avoided by people é roge weed allergy because
pyrethrin are plant derivative
B. Prescription products
:Malathion -1 organophosphate cholinesterase inhibitor
Mode of action: sulfur atoms in Malathion bind é sulfur
gps on hair  residual protective effect against
reinfestation

N.B it should be left on dry hair for 8-12 hrs before

rinsing
:Lindane-2 Mode of action: neurotoxic to the parasite
S.E 1- shampoo (4 min) mild S.E
lotion CNS toxicity in infants' é seizures & reported -2
.no of deaths

.N.B Pediculicides *Shouldn't be used around eye

For ttt of eye lash pubic lice infestation  petrolatum
.applied 5 times/day asphyxiates lice
:Crotamiton [Eurax]-3 prescription only
N.B ttt of scabies as Pediculus

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 .III. Acne vulgaris ttt: Caused by propionibacterium acne

A) Cleansing recommendations *Gentle cleansing 3 times/day to remove excess oil

Use mild facial soaps e.g Dove, Neutrogena*
B) OTC products
:Benzoyl peroxide )1 Mode of action*
10% &5% benzoyl peroxide decomposesO2lethal to p. acne  -1
‫هام جدا‬ .desquamation &antiseptic effect
as irritant.  increase turnover of epithelial cells-2
.Benefit: within 2 weeks*
S.Es: 1-burning & stinging sensation which gradually disappear s*
.bleach hair & clothes-2
.shouldn't come into contact é eye or mucus membrane-3
Combination é Erythromycin or Clindamycin [prescription only]*
Salicylic à, Sulfur & )2 .All: Keratolytic*
Resorcinol .Sulfur: has antibacterial action *
:C) Prescription products
:I) Topical agents
:Tretinoin )1 .M.O.A: Increase turnover of epithelial cells*
.S.Es: 1-Erythema, peeling*
.Increase risk of severe sunburn-2
.There may be initial exacerbation of acne so ttt course 12 week-3
:Adapalene )2 It is a retinoid like compound which cause less irritation & is more
.effective than Tretinoin
:Trazarotene )3 .Retinoid prodrug*
used also for psoriasis*
:Azelaic à)4 M.O.A: as Benzoyl peroxide as effective as it*
cream % 20 it is less irritating than Benzoyl peroxide or Tretinoin*
:II) Systemic agents
Oral antibiotics )1 Erythromycin- Clindamycin- Tetracycline
Doxycycline- Minocycline- Azithromycin-

Minocycline: mainly used in ttt of acne vulgaris

S.E 1-Epigastric distress
Vestibular toxicity such as dizziness -2
‫] دوار‬giddiness *[
:Isotretinoin )2
:Others )3 .a) Estrogens - Spironolactone - Anti androgens
b) Corticosteroids
intralesional injection of Triamcinolone-1
oral prednisone 20 mg/day-2

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 .IV. Psoriasis shiny silver scales
ttt
Methotrexate-1
"Coal tar "LCD-2
Calcipotriol Topical keratolytic-3
Salicylic à-4
.Tazarolene  prodrug of Retinol-5

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 :V. Some OTC drugs

: A-Melatonin it is an endogenous hormone produced by pineal gland )1

taken 1-2 hrs before sleep aids sleep)2
also tryptophan aids sleep )3

:B]Some herbal products

:Standard Methods For Extracting Active ingredient from crude herbals are
maceration-1
Percolation-2
:Echinacea* Reduce severity of cold or virus infection
)N.B no effect on coagulation(
: Ginkgo Biloba* .Improve memory by increasing blood perfusion
C.I é anticoagulant
: St. John's wart* .Active ingredient is Hypericin mild sedative
S.E photosensitivity
:Saw palmetto* Improves urine flow so used in treatment of BPH
:Valerian* Mild tranquilizer /sedative é no residual effect
:Cranberry juice* oz/day: For urinary tract infections (UTI) 10
:Ginger roots* ttt of N, V & motion sickness
:Garlic* mg counteracts hyperlipidemia 600-900
 for relieving. HTN
:Black Cohosh* . ttt of hot flushes for post menopausal woman
:Fever few*  Prevent migraine
:Eleuthero* )Adaptogen increase non specific resistance & stress
)Siberian ginseng(
Milk thistle: * Hepato protective effect for liver
(Silymarin)

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