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Pharmaco Midterm Compiled

The document outlines the pharmacokinetic and pharmacodynamic phases of drug action, detailing how medications are absorbed, metabolized, and excreted in the body. It emphasizes the importance of factors like drug form, route of administration, and physiological conditions on drug absorption and bioavailability. Additionally, it discusses the implications of drug interactions, especially in patients with liver or kidney issues, and the significance of understanding therapeutic and toxic doses for safe medication administration.

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angeladawnpanal
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0% found this document useful (0 votes)
18 views115 pages

Pharmaco Midterm Compiled

The document outlines the pharmacokinetic and pharmacodynamic phases of drug action, detailing how medications are absorbed, metabolized, and excreted in the body. It emphasizes the importance of factors like drug form, route of administration, and physiological conditions on drug absorption and bioavailability. Additionally, it discusses the implications of drug interactions, especially in patients with liver or kidney issues, and the significance of understanding therapeutic and toxic doses for safe medication administration.

Uploaded by

angeladawnpanal
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PDF, TXT or read online on Scribd

INTRODUCTION (PART 1 & 2)

Penicillin - poorly absorbed in the GI tract


HOW A MEDICATION TAKES EFFECT: because of gastric acid. It can be absorbed by
Tablets or capsules taken by mouth goes adding potassium or sodium salts.
Before a tablet is absorbed in the body, it has to
through two phases a drug of action occur:
be broken down into small particles called
Pharmacokinetic phase disintegration. its small particles must combine
Pharmacodynamic phase with the liquid to form a solution, a process
called dissolution. Then absorption happens in
The drug needs to be a solution first so that it the mucosal lining of the small intestine
can cross the biologic membrane of the cell. Absorption - this movement of drug into the
bloodstream after administration
When drug is administered parenterally like ❖Drugs are both disintegrated and dissolved
subcutaneous, or intramuscular, or intravenous faster in acidic fluids in a pH of one or two,
routes, there is no need for it to be converted than alkaline fluids. Because alkaline drugs
to solution. would become ionized and have difficulty
crossing the cell membrane barriers.
The pharmacokinetic phase is composed of four
processes: absorption, distribution, metabolism ❖The very young and older adults have less
or biotransformation, excretion or elimination. gastric acidity. Drug absorption is generally
slower for those drugs absorb in the stomach.
In pharmacodynamic phase, a biologic or
physiologic response results. ❖Enteric coated drugs are meant to be
absorbed in a small intestine.

= the process of drug movement throughout


the body that is necessary to achieve drug
action.
4 Processes:
➢ absorption (example of enteric coated medication)
➢ distribution
➢ metabolism or biotransformation
Nursing implication:
➢ excretion or elimination
You should not crash the medication.
ABSORPTION Otherwise, the medication will not be absorbed
solid form of drug: tablet in where the intended site is.
*Tablets are not 100% drugs. Fillers and inert
substances, such as simple syrup, vegetable
gums, and aromatic powders (excipients) are
used in drug preparation to allow the drug to
take a particular size and shape, and also to
enhance drug dissolution.
Some excipients such as the iron potassium in
penicillin potassium and sodium in penicillin
(example of an ordinary tablet)
sodium increase the absorbability of the drug.
Active transport requires a carrier such as an
enzyme or a protein to move drug against a
concentration medium. Energy is required for
Tablet is not entirely coated.
active absorption. (ATP is required)

Pinocytosis is a process by which cells carry a


Most oral drugs enter the bloodstream drug across your membrane by engulfing the
following absorption across the mucosal lining drug particles into a vesicle. (murag by batch
of the small intestine. ang pag sulod ug vesicle)
Mucus membrane that lines the GI tract is
The epithelial lining of the small intestine is composed of lipids or fats and protein such that
covered with villi finger-like protrusions that lipid soluble drugs can pass rapidly through the
increased the surface area available for mucous membrane.
absorption. Absorption is reduced if the villi are Water soluble drugs need a carrier, either an
decreased in number because of disease, drug enzyme or a protein to pass through the mucus
membrane. Large particles can pass through
effect, or the removal of some or all of the small
the mucous membrane if they are non-ionized.
intestine.
Drugs that are lipid soluble and non-ionized
Absorption happens in the mucosal lining of the are absorbed faster than water soluble and
small intestine through: ionized drugs.
➢ Drugs in liquid form are more rapidly
o passive transport (diffusion and facilitated absorbed than solid drugs.
diffusion)
➢ Pain, stress, and foods that are solid, hot or
o active transport (needs enzyme or protein) high in fat can cause drugs to remain in a
o pinocytosis. stomach longer. Because these causes slow
gastric emptying time.

= Poor circulation to stomach hampers


absorption. due to: shock vasoconstrictor drugs
or diseases.

= Drugs given rectally are absorbed slower


than drugs administered by mouth. the
composition of the suppository-based drug
Passive transport occurs in two processes: affects the absorption.
✓ diffusion (drug moves across the cell
membrane from an area of higher = There are drugs that do not past GIT due to
concentration to lower concentration) their route of administration. (Parenteral
routes, buccal, and inhalation). drugs given
✓ facilitated diffusion (relies in a carrier intramuscularly are absorbed faster in muscles
protein to move the drug from an area of higher that have increased blood flow, like deltoid,
concentration to lower concentration) than those that do not, like gluteus maximus.
Subcutaneous has decreased blood flow when
Passive transport does not required energy to compared with muscle. Thus, absorption rate is
move drugs across to membrane. (ATP is not slower in subcutaneous than in IM.
required)
Following absorption of oral drugs: from the GI = movement of drug from the circulation to
tract, they pass from the intestinal lumen to body tissues -- and is influenced by the rate of
deliver via the portal vein. in the liver, some the blood flow to the tissue.
drugs are metabolized to an inductive form and
are excreted. Thus, reducing the amount of = protein binding. as drugs are distributed in
the plasma, many bind with plasma proteins like
drug available to insert a pharmacologic effect.
albumin and lipoproteins.
Most oral drugs are affected to some degree by
➢ highly protein bound drugs - drugs that are
first pass metabolism. Lidocaine and some 90% bound to protein
nitroglycerines are examples which are not ➢ weakly protein bound drugs - drugs that
given orally because they have extensive first are less than 10% bound to protein
pass metabolism. And most of the drug is
inactivated. This medication is not given orally The portion of the drug that is bound to the
because if the lidocaine and nitroglycerine will protein is inactive because it is not available to
be given orally, nothing will be used by the interact with tissue receptors. It is not able to
body because it will be inactivated by exert a pharmacologic effect.
delivering. free active drug
= the portion that remains unbound
- percentage of administered = can exit blood vessel and reach their site of
drug available for activity action causing a pharmacologic response
For orally administered drugs, bioavailability is Patients with kidney or liver disease or those
affected by absorption and first pass who are malnourished may have significantly
metabolism. The bioavailability of oral drugs is lower albumin levels.
always less than 100% in varies based on the Nursing application: Check patient's protein and
rate of first pass metabolism. The bio albumin levels when administering drugs.
availability of intravenous or IV drugs is 100%.

If the medication is given orally, the


bioavailability is less than 100%, but if it is
intravenous, the bioavailability of the
medication is always 100%.
--
Factors that alter bioavailability:
o drug form
o route of administration
o gastric, mucosa, and motility
Blue = protein
o administration with food and other drugs
o changes in liver metabolism (caused by liver Green = drug (free drug) drug is not bound to
dysfunction or inadequate hepatic blood flow). protein.

A decrease in liver function or a decrease in Blue and green = protein bound drug (the drug
impacting blood flow can increase the bio has already attached to the protein. And when
availability of a drug, but only if the drug is the drug is already protein bound, that means
metabolized by the liver, less drug is destroyed that the drug is already inactivated. Why?
by hepatic metabolism in the presence of a liver Because the drug cannot interact with the
disorder. receptors anymore. Only the free drug can
interact with the receptors to take a A large percentage of drugs are lipid soluble,
pharmacologic effect.) thus the liver metabolizes the lipid soluble drug
substance to a water soluble substance for
When two highly protein bound drugs are renal excretion. However, some drugs are
administered together, they compete for transformed into active metabolites causing an
protein binding sites in which drug increased pharmacologic response
accumulation, may occur and toxicity will Liver diseases: cirrhosis and hepatitis altered
result. (The more highly protein bound drug drug metabolism by inhibiting drug
could displace the other from its binding site.) metabolizing, enzymes, and in the liver. When
drug metabolism rate is decreased, excess drug
accumulation can occur and can lead the
= decreases the number of available binding toxicity.
sites and can lead to an increase in the amount ✓ - time it takes for the amount of
of free drug available, resulting in drug drug into the body to be reduced by half the
accumulation and toxicity. amount of drug administered. The amount of
(Older adults are more likely to have drugs remaining in the body from the previous
hypoalbuminemia, particularly if they have dose metabolism and elimination affect half life
multiple chronic illnesses) of a drug.
Pregnancy- drugs crosses the placenta and
affects the mother and fetus ✓ Example: A 500 milligram paracetamol was
Drugs taken during: administered at 0800H. The medication has a
❖ first trimester - cause spontaneous half-life of four hours.
abortion
❖ second trimester - cause spontaneous By knowing half-life, the time it takes for a drug
abortion, teratogenesis, subtler defects to reach a steady state can be determined.
❖ third trimester - alter fetal growth and
development

The risk benefit ratio must be considered before


any drugs are given during pregnancy.
Breastfeeding - drugs can pass into breast milk,
which can affect nursing infant.
- Nurses must teach women who breastfeed to
consult their healthcare provider prior to taking
any drug, whether over the counter or
prescribed.
= occurs when the amount of drug being
DRUG METABOLISM administered is the same amount of drug being
= Metabolism or biotransformation: process by
eliminated
which the body chemically changes drugs into a
= necessary to achieve optimal therapeutic
form that can be excreted.
benefit
= The liver is a primary site of metabolism.
= cytochrome P450 system (Liver enzymes) or
P450 system of drug metabolizing convert drugs = administration of a large initial dose of a
to metabolites. medicine used to ensure quick therapeutic
response.
= usually given for a short period before therapy the problem is they outflow urine
continues with a lower maintenance dose from the kidneys

= This is applicable in the case of drugs with Pre-renal conditions:


long half-lifes - dehydration or hemorrhage: reduce blood
flow to the kidneys and results in reduced
Example: phenytoin glomerular filtration rate,

the half-life of phenytoin is approximately 22 Intrarenal conditions:


hours. If all doses of the drug will be the same, - glomerulonephritis and chronic kidney
steady state will not be achieved for about disease affect glomerular filtration and tubular
three and a half days. by giving a large initial secretion, and reabsorption
dose that is significantly higher than the
maintenance dose, therapeutic effects can be post renal conditions
obtained, while a steady state is reached. - obstruct urine flow: prostatic hyperthropy,
stones, and your urogenic bladder adversely
Loading dose can be used in order to achieve a affects glomerular filtration
quick therapeutic response
with any of these situations, drug accumulation,
RECAP: may occur resulting in adverse drug reactions.
- drugs are absorbed in the mucosal =Yes
lining of small intestine
– Creatinine and blood urea nitrogen, or B U N
- primary site for metabolism: liver are used to determine renal function between
the two. It is a creatinine which is more reliable
test for kidney function because it is not altered
= main route of drug excretion: through the by bodily processes. It is important for nurses to
kidneys know their patient's kidney function to ensure
correct dosage of the medication to better
= Drugs are also extracted through bile, lungs, understand the pharmacokinetic face.
saliva, sweat, and breastmilk.
Watch this video,
= urine pH influences, drug excretion
- acidic urine promotes elimination of weak A drug is a chemical or biological substance that
based drugs affects the body. And it's fun.
- alkaline urine promotes elimination of weak Drug absorption is when a drug enters the
acid drugs bloodstream, the level of absorption can affect
the speed and the quantity of the drug at the
site of action. This is termed bioavailability. If a
✓ Prerenal, intrarenal, and post renal tablet releases the drug quickly, blood levels
conditions affect drug excretion. may become too high. Whereas slow release
may result in low levels of absorption,
additional factors affecting absorption and
: the problem is a profusion of the
bioavailability include the properties of the drug
blood towards the kidney
and the physiology of the person such as pH
the problem is within the kidneys or levels in the stomach. And it speeds of
the formation of urine. emptying. Therefore, specific formulations are
used to release the drug at the desired speed.
Common formulations include tablets, capsules. - response relationship- body physiological
It's a positories transdermal patches and response to changes in drug concentration at
solutions. Drug metabolism is the process by the site of action
which the body breaks down drugs, which
mainly occurs by means of enzymes located in
the liver. Many factors, including intake of - the amount of drug needed to elicit specific
specific foods and other drugs can increase or physiologic response to a drug
decrease the speed at which drugs are broken
down and thus determine their levels within the - a drug with high potency produces significant
blood. A drug may be broken down to stop it therapeutic response at low concentration
from working. However, there are other drugs
that need to be broken down or modified - low potency produces minimal therapeutic
before they become active. These are known as response at low concentrations
pro drugs. Some drugs are directly eliminated
from the body, by the kidneys in urine for this - medications that are given at low
to happen. The drug must be water soluble concentration (5mg) can already elicit
drugs that are not water soluble, maybe therapeutic response whereas those medication
metabolized by the liver or enzymes in the that are given in 500mg is an example of low
blood into breakdown products that can be potency medication in which you need to
eliminated in urine diseases that affect the liver increase the dosage of the medication to feel
or the kidneys can cause blood levels of a drug the therapeutic effect
to increase

- point at which increasing the drug’s dosage no


PART 2 longer increases the desired therapeutic
Pharmacodynamic Phase response meaning even if you double the dose
of the medication, you can no longer increase
the effect
- study of the effect of drugs in the body, drugs
act within the body to mimic the body’s own
chemical messengers. - describes relationship between the
-drug response can cause primary and therapeutic dose of the drug (ED50) and the
secondary physiologic effect or both toxic dose of the drug (TD50)
Primary Effect: desirable response
Secondary Effect: maybe desirable or Abbrev:
undesirable

Example drug: Diphenhydramine dose that produces therapeutic response in


50% of the population
-antihistamine
Primary effect: for symptoms of allergies
Secondary Effect: central nervous depression dose of adrug that produces a toxic response
that causes drowsiness, the secondary effect is in 50% of the population
undesirable when patient drives a car but at Therapeutic index- difference between the toxic
bedtime it could be desirable because it cause and therapeutic doses
mild sedation.
REMEMBER: if the therapeutic and toxic doses With the first 3 receptor groups activation is
are close, the drug is said to have a narrow rapid
therapeutic index (require close monitoring) - drug molecule that binds to a receptor
- linked receptor- where ligand will bind
Onset, Peak , and Duration of Action
1. Agonist:
time it take for drug to reach the -drugs that activate receptors and produce a
minimum effective concentration after the desired response.
administration
drug reaches its highest concentration in 2.Antagonist:
blood -drugs that prevent receptor activation and
- length of time the drug block a response.
exerts a therapeutic effect
3.Nonspecific drug:
Receptor Theory -drugs that affect multiple receptor sites.

4 receptor families: 4. Nonselective drug:


-drugs that affect multiple receptors.
*difference between the 2: nonspecific only one
In cell membrane enzymes the ligand binding
type of receptor but a multiple receptor sites;
domain for drug is on the cell surface the drug
nonselective affects multiple types of receptors
activates the the enzyme inside the cell and the
response is initiated
5.Side effects:
-secondary effects of drug therapy
-can be desirable
channel crosses the cell membrane when the
-can be a reason for a client to stop taking the
channel opens ions flow into and out of the
medication
cells, primarily affects sodium and calcium ion
-Nursing implication: nurse must include health
teaching on side effects.
- needs 3 components: receptor, g- protein,
6. Adverse effects:
effector protein either an enzyme or ion
-are unintentional, unexpected reactions to
channel drug therapy that can occur at normal drug
- drug activates the receptor then g- protein will dosages.
affect the effector protein then response will be -can be mild to severe.
initiated -always undesirable.
* all receptor site is in the cell membrane
except the last*
7.Drug toxicity:
-Occurs when drug levels exceed the
therapeutic range.
- found inside the nucleus. Ligands that can -toxicity may occur secondary to overdose or
pass through the cellular membrane enter the drug accumulation.
cell after entering nucleus binds to intracellular
receptor, can alter the transcription of the cell 8.Tolerance:
- activation receptors through transcription -a decreased responsiveness to a drug over the
factors regulates protein synthesis and is course of therapy.
prolonged.
9.Tachyphylaxis: Part 3
-acute, rapid decrease in response to a drug. Over- The- Counter Drugs/ OTC drugs

10.Drug interaction: - drugs that have been found to be safe and


-altered or modified action or effect of a drug as appropriate for use without direct supervision
a result of interaction with one or multiple of a health care provider.
drugs.
-Available for purchase without a prescription in
11.Drug-nutrient interactions: many retail locations, other otc drugs just like
-food may increase, decrease or delay the Pseudoephedrine and emergency contraception
body’s pharmacokinetic response to drugs. are available with restrictions and must be kept
behind the pharmacy counter
12.Additive drug effect:
-response is increased beyond what either - prior to dispensing patient age and identity are
could be produce alone. verified and education is provided
-Ex: diuretic and antihypertensive.
Nursing implication: the nurse needs to
13.Synergistic drug effect or potentiation: emphasize that many of these drugs are potent
-the clinical effect of the 2 drugs given together and can cause moderate to severe side effects,
is substantially greater than that of either drug especially when taken with other drugs.
alone. Nursing considerations related to otc drugs
EX: Co-Amoxiclav (found in page 56 of PDF Pharmacology)

14.Antagonistic drug effect: Mechanisms of drug action- can either


-one drug reduces or blocks the effect of the stimulate, depress, or irritate cells ,can replace
other. certain chemicals, medications can also produce
EX:antidotes cytotoxic actions and antimicrobial actions, also
possible to modify immune status of the
15.Pharmacogenetics: person.
-is the study of genetic factors that influence an
individual’s response to specific drug. 1.Stimulation: enhances intrinsic activity
Example: adrenergic drugs(epinephrine)-
16.Placebo effect: increase heart rate, sweating and respiratory
-a drug response not attributed to the chemical rate
properties of a drug.
2.Depression: decrease neural activity and body
17.Ethnopharmacology: functions.
-a subdivision of ethnomedicine and focuses on Example: barbiturates- causes CNS depression
the use of herbs, powder, teas and animal
products as healing remedies. 3.Irritation: have noxious effect.
Example: Laxative (senocot and bisacodyl)-
considered as irritants, irritates sensory nerve
endings in the intestinal mucosa

4.Replacement: replace essential body


compounds.
Example: Insulin- replaces body compounds
5.Cytotoxic action: selectively kill invading become pregnant. (should not be taken because
parasites or cancers. it will cause fetal abnormalities
Example: Chemotherapeutic drugs or called as
antineoplastic medications *Refer to 5:33- 7:03 time in video*

6.Antimicrobial actions: prevent,inhibit,or kill


infections medications.
Example: Co-amoxiclav- an antibiotic Tablet (oral) – most common form of oral med

7.Modification of immune status:modify the Capsule- maybe liquid/Powder


immune status (modify,enhance, or depress the
immune system). Timed-release capsule or Spansule: with small
Example: corticosteroids (when it is taken for a beads, medication will be released in small
long it will make the person amounts over time
immunocompromise
Enteric-coated- don’t crush because the coating
is designed to hold the tablet together in the
During pregnancy, drugs can cross the placenta stomach and medication will be released in the
as much as it can cross other membranes that small intestine
affects the mother and fetus. Harmful abortion
can cause spontaneous abortion, congenital
defects and alter fetal growth and development
Oral- medication will be swallowed
PREGNANCY CATEGORIES OF DRUGS: to know
if the medication is safe for the pregnant Buccal- place the medication between cheek
woman or not and gum

CATEGORY A: controlled studies in women fail Sublingual- place under the tongue
to show a risk to the fetus and possibility to
fetal harm appears unlikely. (completely safe) *tablets are not only administered orally, but
can be intravaginally or rectally, read doctor’s
CATEGORY B: animal-production studies have order
not shown a fetal risk or adverse effect. Risks
have not been confirmed in controlled studies
in women.
Elixir- liquid containing a medicinal drug with
CATEGORY C: either studies in animals have
syrup, glycerin or alcohol added to mask its
revealed adverse effects on the fetus and there
unpleasant taste.
are no controlled studies in women or studies in
women and animals are not available.
Suspension- undissolved parts or 1 or more 2
medical agents mixed with a liquid vehicle for
CATEGORY D: there is confirmation of human oral administration (should shake before using)
fetal risk, but the benefits from use in pregnant
women may be acceptable despite the risk. Emulsion- mixture 2 or more liquids that are
normally immiscible or unmissable
CATEGORY X: animal and human studies have
shown fetal abnormalities, the drug is
contraindicated in women who are or may
Transdermal- patch is used, designed to Urethra
penetrate the skin layer and exert effects on - pencil shaped
deeper tissues -made from glycerinated gelatin or high
molecular weighted polyethylene glycols and
Topical- cream is used, topical in transdermal are common variety vehicles for drugs
compounds are applied in the skin, minimally - useful routes for babies
penetrate the skin layer which is its intent
Parenteral medication
Instillations/ Medical Insulation- - by injection, infusion, implantation or by some
administration of a medicine in liquid form, other route other than elementary canal
either drop by drop or with catheter into a body - length of needle and angle of insertion matter
space
Example: needle is in 10- 15 degree
Eye drops - 45 degrees but for insulin syringe-
Eye ointment the desired route 90 degrees
Nasal spray - 90 degrees
Ear drops

INSULIN:
Example: Old/Current system- insulin commonly
administered subcutaneously.
Metered-Dose Inhaler (MDI) Update- pain-free delivery of insulin through a
transdermal patch
MDI with spacer- spacer maybe attached to
metered- dose inhaler to facilitate inflow of
SERUM GLUCOSE:
medicine in lungs Old/Current system- monitoring of serum
glucose is done manually with the use of
Nebulizer- for asthma glucometer.
Update- insulin pups that deliver insulin based
Nasogastric and Gastrostomy Tube Routes – on monitoring of serum glucose level.
tube is inserted through the nose until the
stomach, medicines are administered in both
INFUSION PUMPS
tubes Old/Current system- programming of the
infusion pumps are done manually.
Gastrostomy Route- tube is inserted in the Update- intelligent infusion technology that
stomach through abdominal wall programs infusion based on the scanned
information.
Suppositories- solid medical preparation that is:
ANTIBIOTICS
Rectal- cone/spindle shaped Old/Current system- antibiotics are either
administered orally, parenterally or topically.
Vaginal- globular/egg shaped Update- aerosolized antibiotics
HERBAL PLANTS -Data from physician’s notes
Old/Current system- limited use of herbal plants -Measurement of vital signs
and without extensive research -The patient’s body language
Update- expanding use of medicinal plants in
medicine. 2.Diagnosis
-It is made based on the analysis of the
ANTENEOPLASTIC MEDICATION PREPARATION assessment data.
Old/Current system- the nurse or pharmacist -It determines the type of care the client will
personally prepares antineoplastic medication receive.
Update- robotic mixing of antineoplastic drugs.
3. Planning
PART 4 - the nurse uses the data collected to set goals
Nursing process: or expected outcomes and interventions
- patient-centered collaborative care
4. Implementation
-Nursing Process: -The nurse provides education, drug
I. Assessment administration, patient care, and other
II. Nursing Diagnosis interventions necessary to assist the patient in
III. Planning accomplishing established goals.
IV. Implementation Patient teachings:
V. Evaluation -Essential to the patient’s recovery.
-allows the patient to become informed in his or
1.Assessment her health problems.
-Principles:
Subjective data: -General
- Refers to the data that are covert or those you -Side-effects
couldn’t observe or know unless an interview is -Self-administration
conducted to the patient. -Diet
EX: -Cultural considerations
-Current health history including family history
-Dysphagia 5. Evaluation
-S/s of illness as verbalized by client -The nurse determines whether the goals and
-Current concerns about the patient teachings objectives are being met
-Allergies
-Financial barriers
-Use of tobacco, alcohol and caffeine -Five plus Five ‘rights of medication
-Cultural dietary barriers administration:
-Patient’s home safety needs 1. Right patient
-Care givers needs and supports system 2. Right drug
3. Right dose
Objective data: 4. Right time
-What the nurses directly observes about the 5. Right route
patient’s health status, it involves collecting the 6. Right assessment
patient’s health information by using the senses 7. Right documentation
seeing hearing,smelling,and touching. 8. Right education
EX: (Concerning medication administration)
9. Right evaluation
-Physical health assessment
10. Right to refuse
-Laboratory and diagnostic test results
-Counterfeit drugs: look like the desired drug,
1.Right to a complete and clear order but may have no active ingredient, the wrong
2.Right to have the correct drug route (form) active ingredient, or the wrong amount of
and dose dispensed active ingredient.
3. Right to have access to information -Report counterfeit products immediately.
4.Right to have policies to guide safe
medication administration
5.Right to administer medications safely and to -high alert drugs can cause significant harm to
identify problems in the system the patients.
6.Right to stop, think and be vigilant when -EX: epinephrine, oxytocin, promethazine,
administering medications. insulin, and etc

PART 5
1. Simplify the storage, preparation and
administration of high alert drugs
-ANA encourages the avoidance of punitive 2. Write policies concerning safe administration
approaches in reporting drug errors because Improve information and education
they focus on punishing individuals for 3. Limit access to high alert medication
reporting such errors. 4. Use labels and automated alerts
5. Use redundancies (automated or
-Just culture: does not hold individual independent double checks)
practitioners responsible for a failing system, 6.Closely monitor the patients response to the
although it does not tolerate disregard for a medication
patient or gross misconduct.

-An important component in the culture of


safety.
-The process of identifying the most accurate
list of all
medications that the patient is taking at 1.Patient and family-centered care: one must
transitions in care. recognize as the source of control and full
-Prevents discrepancies that can be used in drug partner in providing compassionate and
error coordinated care based on respect for patient
preferences, values, and needs

-National patient safety goals: 2. Collaboration and teamwork: the nurse must
-the 2 important goals that already become function effectively, in nursing, and inter
standards are the ‘do not use’ abbreviations professional teams, fostering open
and the the list of acceptable abbreviations communication, mutual respect, and shared
-Black box warning by the US FDA decision-making to achieve quality patient care.
(Page 89 and page 88 do not use/ ACCEPTABLE
ABBREVIATIONS) 3.Evidence-based practice: integrate best
current evidence with clinical expertise and
patient or family preferences and values for
-Sharps safety: tamper resistant container, delivery of optimal health care
syringes with safety features, jet-injector
4.Quality improvement: continuously improve 6. Niyog-inyo gna (Quisqualis indica L.)
the quality and safety of healthcare systems by -used to eliminate intestinal parasites
using data to monitor outcomes of care process
and improvement methods to design and test 7.Sambong (Blumea Balsamifera):
changes. -used to treat kidney stones, wounds, and cuts,
rheumatism, anti-diarrhea, anti spasms, colds,
5.Safety: minimize risk of harm to patients and and coughs, and hypertension
providers through both system effectiveness
and individual performance 8. Tsaang Gubat (Ehretia microphylla lam)
-Used to treat skin allergies including eczema,
6.Informatics: use information and technology scabies, and itchiness wounds in childbirth
to communicate, manage knowledge, mitigate
error, and support decision making. 9.Ulasimang Bato/Pansit-Pansitan (Peperomia
Pellucida):
-Used in treating arthritis

1. Akapulko (Cassia alata): 10.Yebra Buena (Clinopodium Douglasii)


-Used to treat tinea infections, insect bites, -as analgesic to relieve body aches and pain due
ringworms, eczema, scabies, and itchiness. to rheumatism and gout
-It is also used to treat coughs, cold and insect
2. Ampalaya (Momordica Charantia): bites
-found to be effective in the treatment of
diabetes (diabetes mellitus), hemorrhoids,
coughs, burns, and scalds, and being studied for 1.Astralagus:
anti-cancer properties. -used as an adjunct to boost immune system

3.Bawang or Garlic (Allium sativum): 2. Chamomile:


-Used to treat infection -for sleeplessness, anxiety, stomach, and
-With antibacterial, antiinflammatory, intestinal ailments
anticancer, and antihypertensive properties
-it is wildely used to reduce cholesterol level in 3.Cinnamon:
blood -Bronchitis, GI problems, anorexia, and diabetes

4. Bayabas or Guava (Psidium guajava): 4.Echnicaea:


-Used as antiseptic, antiinflammatory, -For colds, flue, and infection
antispasmodic, antioxidant hepatoprotective,
anti-allergy, antimicrobial, anti-plasmodial anti- 5.Garlic:
cough, antidiabetic, and antigentoxic in folkloric -used to lower cholesterol, blood pressure, and
medicine reduce heart disease

5.Lagundi (Vitex negundo): 6.Ginger:


-Used to treat cough, colds, and fever -Nausea, motion sickness, and diarrhea
-it is also used as a relief for asthma and
pharyngitis, rheumatism, dyspepsia, boils,a and 7.Gingko:
diarrhea -Asthma, bronchitis, fatigue and tinnitus
8. Ginseng: RA 9502 or Universally Accessible Cheaper
-used to boost the immune system, increase a And Quality Medicines Act of 2008
person’s sense of well-being and increase - a policy of the state publich health and when
asthma the public interest or circumstances of extreme
urgency so require
9. Hawthorn: - ensure access to affordable quality drugs
-For treatment of heart disease
RA 6675 or Generics Act of 1988
10.Licorice root: - to promote, require and ensure production of
-Used to treat stomach ulcer, bronchitis, sore an adequate supply, distribution, use and
throat and viral hepatitis acceptance of drugs by their generic names
INTERPRETING DRUG LABEL (pls. Follow the
11.Milk thistle: lines indicated to each label)
-Cirrhosis, chronic hepatitis, and gall bladder
disorders

12.Peppermint:
-Nausea, indigestion, irritable bowel syndrome,
colds , headaches muscle and nerve pain

13. St.john’s wort:


-mental disorders and nerve pain

14. Turmeric:
-heartburn, stomach ulcer, gallstones,
inflammation and cancer
Intepret Doctor’s Orders- to make sure that
nurses administered the correct medication to
15.Valerian:
the patients
-insomnia, anxiety headache, depression,
Example:
irregular

PART 6
Philippines National Drug Formulatory
-aims to make quality essential drugs available,
accessible, efficacious, safe and affordable
- provides the list of medicines registered with
FDA (pharmacopoeia)

RA 9711 or Food and Drug Administration Act


of 2009
- an act strengthening and rationalizing the
regulatory capacity of the BFAD by establishing
adequate testing laboratories and field offices,
upgrading its equipment
- Renaming it to FDA
Systems of Measurements
COMPUTATIONS IN AMOUNT TO ADMINISTER

COMPUTATION IN AMOUNT TO ADMINISTER considering BODY WEIGHT


COMPUTATION IN AMOUNT TO
ADMINISTER using BODY SURFACE
AREA
YOUNG’S RULE (refer to your
FUNDAMENTALS RLE NOTEBOOK)

- used to compute child’s dose (1-12 years


old)

FRIED’S RULE (refer to your


FUNDAMENTALS RLE NOTEBOOK)
- applicable for infants less than 1 years old.

CLARK’S RULE (refer to your


FUNDAMENTALS RLE NOTEBOOK)
- used to compute pediatrics’ dose using child’s
weight
CALCULATING INTRAVENOUS FLOW RATE (refer to your
FN RLE NOTEBOOK)

DROP FACTOR

With needle

- most common in the area is 15-20 gtt/ml

- CDU-H: 20 gtt/ml

FLOW RATE per HOUR (refer to your FN RLE NOTEBOOK)


FLOW RATE per MINUTE (refer to your FN RLE
NOTEBOOK)
Special Considerations
Drug Classes that require dosage
adjustment in Chronic Kidney
Disease especially GERIATRIC
PATIENTS
PHARMACO- CNS

Central nervous system enough oxygen. This


condition prevents the
- Composed of brain and spinal cord
body organs from getting
- Regulates body functions
the oxygen they need to
- Stimulation of the CNS may either
function.
increase the neuron activity or block
nerve cell activity. MAJOR GROUPS OF CNS STIMULANTS:

Peripheral Nervous System 1. Amphetamines and Caffeine


- Will stimulate the cerebral cortex of the
- Consists of 2 divisions
brain
• Somatic Nervous System (SNS)
2. Anorexiants
➢ Voluntary
- Suppress appetite by stimulating the
➢ For locomotion and
satiety center of the hypothalamic and
respiration
limbic areas of the brain.
• Autonomic Nervous system 3. Analeptic and caffeine
➢ Involuntary - Which act in the brainstem and medulla
➢ For functioning of the to stimulate the respiration
heart, respiratory
system, gastrointestinal
system and glands.
1. AMPHETAMINES
STIMULANTS - Causes Euphoria and increased
alertness as well as insomnia,
Indications: restlessness, tremors, irritability, and
- Attention- Deficit/ Hyperactivity weight loss.
Disorder in children (ADHD) - Increased heart rate, palpitations,
➢ Also called as minimal brain cardiac dysrhythmia and increased
dysfunction hyperactivity in blood pressure can also result from
children, hyperkinesis, and cardiac stimulation and vasoconstriction
hyperkinetic syndrome with with continuous use of amphetamines
learning disorder. *TAKE NOTE: Excessive use may lead to
➢ Caused by dysregulation of the psychosis
transmitter’s serotonin,
norepinephrine and dopamine - Amphetamines have a half- life of 9-13
➢ May occur before 7 years of age hours
and may continue through
- Amphetamine and dextroamphetamine
teenage years.
are prescribed for narcolepsy and ADHD
➢ 3 to 7 times more common in
when amphetamine- like drugs are
boys than girls.
ineffective.
➢ Characteristics: inattentiveness,
inability to concentrate, - Amphetamine and amphetamine-like
restlessness, hyperactivity, drugs should not be administered in the
inability to complete tasks, and evening or before bedtime because
impulsivity insomnia may result.

- Nursing implication: It is best to


- Narcolepsy
administer amphetamines in the morning
➢ Characterized by falling asleep
so as not to interfere the sleep of the
during normal walking activities
patient
➢ Accompanied by sleep paralysis
and affects the voluntary
muscles. The patient with
narcolepsy is unable to move
and collapse.
- Reversal of respiratory distress
➢ Refers to a condition in
which the person is having
trouble breathing which Examples:
often show signs that they
are having to work harder ✓ Amphetamine sulfate
✓ Dextroamphetamine sulfate
breathe or are not getting

cns
PHARMACO- CNS

✓ Lisdexamfetamine dimesylate ➢ transdermal form of


medications may be worn for
- These medications stimulate the release nine hours.
of norepinephrine and dopamine from ➢ Symphathomimetics +
the brain and the nervous sympathetic methylphenidate
system and inhibit the reuptake of (ex.Pseudoephedrine)
these transmitters. Psychostimulants +
methylphenidate (ex. Caffeine)
*you may formulate a nursing diagnosis = result to irritability,
based on the side effects and adverse nervousness, tremors, and
reactions of the medication. insomnia.

Amphetamine-like Drug: Methylphenidate


example= seizure: Risks for injury
related to adverse reaction of the Monoamine Oxidase Inhibitors (MAOIs)
medication. + methylphenidate -> hypertensive
AMPHETAMINE-LIKE DRUGS crisis
Potentiates the action of the CNS
Examples: stimulants (Ex. Caffeine)
✓ Methylphenidate hydrochloride Inhibits the metabolism of some
✓ Modafinil barbiturates (Ex. Phenobarbital)
✓ Dexmethylphenidate
hydrochloride ❖ Side effects of methylphenidate
hydrochloride:
✓ Armodafinil
Anorexia Insomnia
- Used for ADHD and narcolepsy
Headache Dry mouth
- More effective in treating ADHD than Irritability Abdominal pain
amphetamines. Nausea Tremors
- Methylphenidate and Anemia Vomiting
dexmethylphenidate are given to Euphoria Dizziness
increase a child's attention span and Blurred vision
cognitive performance and to decrease
impulsiveness, hyperactivity, and ❖ Adverse reactions of
restlessness. methylphenidate hydrochloride:
Tachycardia Exfoliative dermatitis
- Methylphenidate is most frequently
Hypertension Seizure
prescribed drug in the treatment of
Growth suppression Hepatotoxicity
ADHD.
Palpitations Stroke
- Modafinil increases wakefulness in
Thrombocytopenia
patients with sleep disorders such as: Transient weight loss in children
narcolepsy.
- Amphetamine-like drugs are classified Nursing process in the care of clients who are
as Controlled Substance Schedule (CSS) taking Methylphenidate HCI (amphetamine-
II drug like drug)
➢ that this medication cannot be
purchased using ordinary Assessment:
prescriptions • Determine for history of heart disease,
➢ the physician who can only hypertension, hyperthyroidism, Parkinsonism,
prescribe these medications are or glaucoma:
only the physicians who have - In such cases, this drug is usually
CSS II licenses contraindicated.
➢ This medication is well • Assess vital signs:
absorbed for the GI mucosa
- To be used for further comparisons. Closely
➢ Usually administered to
monitor patients with cardiac disease, because
children twice a day before
these drugs may cause tachycardia,
breakfast and lunch hypertension, and stroke.
➢ food affects absorption rate =
given 30 to 45 minutes before • Assess mental status:
meals - Such as mood affect and aggressiveness.
➢ should be given at least six - You must also evaluate the height and weight
hours before sleep because it and growth of children.
can cause insomnia

cns
PHARMACO- CNS

- Assess also the complete blood count or CBC, • Teach nursing mothers to avoid foods that
differential white blood count or wbc,and contain caffeine (coffee, tea, chocolate, soft
platelets. Before and during drug therapy. drinks and energy drinks)

Nursing diagnosis: • Encourage children’s to provide children with


• Risk for health behavior that interfere with a nutritious breakfast because the drug may
peer relationships have anorexic effects.

• Interrupted family process related to • Teach patients about drug side effects, and
dysfunctional behavior the need to report tachycardia and palpitations.

Planning: • Monitor children for onset of Tourette


Objective: syndrome.
• Decrease the patient’s hyperactivity.
• Tourette Syndrome: this refers to a
• Increase the patient’s attention span. neurological disorder characterized by
repetitive, stereotyped involuntary movements
• This plan is for ADHD. and vocalizations called ticks (this is usually in
children)
Nursing Interventions:
• Monitor vital signs and report irregularities Evaluation:
• Evaluate height, weight and growth of • Evaluate the effectiveness of drug therapy,
children level of hyperactivity, and presence of adverse
• Especially, that one of the adverse effects of effects.
methylphenidate HCI is growth suppression. • Monitor weight, sleep pattern and mental
• Observe for withdrawal symptoms and side status.
effects.
Amphetamine-like drug: Modafinil
Patient teachings:
• Teach patients to take drug before meals - This drug is used to increase the
wakefulness in patients with sleep
• Advise patients to avoid alcohol consumption disorders such as narcolepsy.
• Use sugarless gum to relieve dry mouth
2. ANOREXIANTS
• Monitor weight 2x a week and report weight Examples of Anorexiants:
loss ✓ Benzphetamine
✓ Diethylproprion HCI
• Avoid driving and using hazardous equipment ✓ Phentermine
when experiencing tremors, nervousness, or ✓ HCI Phentermine topiramate
increased heart rate. ✓ Phendimetrazine
✓ Liraglutide
• Teach patients not to abruptly discontinue the
✓ Naltrexone HCI
drug the dose must be tapered to avoid
✓ Bupropion HCI
withdrawal symptoms.

• Consult a healthcare provider before - These medications cause a stimulant


modifying doses. effect on the hypothalamic and lambic
regions of the brain to suppress
• Encourage patients to read label of OTC appetite.
products,because they contain caffeine.a high - These medications do not have serious
plus macrophage level could be fatal. side effects, Associated with
amphetamines.
• Advice nursing mothers not to take drugs with - Reliance in appetite suppressants
cns stimulants because they are excreted in should be discouraged.
breast milk, and can cause hyperactivity or - Children younger than 12 years old
restlessness in infants. should not be given this medication.
- Long term use results to nervousness,
• Direct families to seek counseling for children
restlessness, irritability, insomnia,
with ADHD, drug therapy alone is not an
palpitation, and hypertension.
appropriate therapy program.

• Notify school nurse of drug therapy regime. 3. ANALEPTICS


Examples:
• Explain to patients and family that long-term ✓ Caffeine citrate
use may lead to drug abuse. ✓ Theophyllinne
✓ Doxapram

cns
PHARMACO- CNS

- Used to stimulate respiration • Avoid heavy meals or strenuous exercise


- One subgroup is the xanthines before bedtime.
(methylxanthines) of which caffeine • Take warm bath, listen to quiet music, or
and theophylline are the main drugs. perform other soothing activities before
- Caffeine stimulates the CNS,and take bedtime
note, large doses of caffeine will • Decrease exposure to loud noises
stimulate respiration. • Avoid drinking copious amount of fluids
- Theophylline on the other hand, is before sleep
mostly used to relax the bronchioles • Drink warm milk before bedtime.
and used to increase respiration in
newborn.
1. SEDATIVE- HYPNOTICS
Side effects of Analeptics: - Are commonly ordered for sleep
Nervousness Insomnia disorders
Restlessness Diuresis EXAMPLES:
Tremors GI traction ✓ Secobarbital sodium
Twitching Tinnitus (Rare) ✓ Butabarbital sodium
Palpitation ✓ Phenobarbital
✓ Pentobarbital
- Excessive caffeine can affect both the ✓ Mephobarbital
CNS and the heart of which may result
to convulsion (CNS) and dysrhythmia - Sedation is the mildest form of CNS
(heart) accordingly depression and take note, hypnotic
effect is a form of natural sleep.
RECALL: - Hypnotic drug therapy should be short
term, to prevent drug dependence and
STIMULANTS drug tolerance.
AMPHETAMINES - Interrupting drug therapy can decrease
& drug tolerance, but abrupt
ANOREXIANTS ANALEPTICS
AMPHETAMINE- discontinuation of a high dose of
(Used to (used to
LIKE DRUGS hypnotic medication: withdrawal
suppress stimulate
(used for symptoms.
appetite) respiration)
narcolepsy and
ADHD)
- Nursing implication: the medication
must be tapered. Meaning, the
medication should not be stopped
DEPRESSANTS
abruptly. In other words, if one person
• Drugs that are CNS depressants cause varying
is taking 500 mg of the medication, the
degree of depression or reduction of the
patient should not abruptly discontinue
functional activity within the CNS.
the medication. Instead, the medication
• The degree of depression depends primarily will be reduced gradually, until the
on the drug and the amount of drug taken. medication will not be taken anymore
by the patient
• The broad classification of CNS depressants:
✓ Sedative-hypnotics General rule:
✓ General Anesthetics - The lowest dose should be taken to
✓ Analgesics (opioid and nonopioid) achieve sleep.
✓ Anticonvulsants - And patients with severe respiratory
✓ Antipsychotic disorders should avoid hypnotics which
✓ Antidepressant could cause an increase in respiratory
✓ Antidepressants depression.
- Take note; that hypnotics are
Non-pharmacologic ways to promote sleep: contraindicated during pregnancy.
• Sedative-Hypnotics: Promote sleep to a - Ramelteon is the only major sedative-
person. hypnotic approved for long term use.
• Non-pharmacologic way: this is to make sure This drug may be used to treat chronic
that we will avoid drug dependence as well as insomnia.
drug tolerance.
Type of Sedative-hypnotics:
Ways: 1. Barbiturates:
• Arise at a specific hour in the morning
• Take few or no daytime naps - These medications are useful as sleep
• Avoid drinks that contain caffeine and alcohol sustainers for maintaining long periods
6 hours before bedtime of sleep.

cns
PHARMACO- CNS

• Classifications: • This drug is the antidote for overdosage of this


medications.
o Long acting: PHENOBARBITAL and
MEPHOBARBITAL • Increase anxiety can be the cause of insomnia
for some patients.
o Intermediate-acting: BUTABARBITAL
• Lorazepam and Diazepam can be used to
o Short-acting: SECOBARBITAL elevate the anxiety so that the person can have
a better sleep.
- Barbiturates should be restricted to
short-term use only. (Like two-weeks or • Benzodiazepines are effective for sleep
less; this is because of the numerous disorders for several weeks longer than other
side effects) sedative-hypnotics.
- Pentobarbital and Secobarbital are
used primarily to treat insomnia. • To prevent rapid eye movement rebound;
- The onset of action of pentobarbital is they should not be used longer than 3-4 weeks.
slower when administered IM than
when administered PO. • Adverse reaction: anterograde amnesia
- Whereas for pentobarbital, this (which refers to the impaired ability to recall
medication increases hepatic enzyme events after dosing) associated with the
action causing an increased anterograde amnesia are sleep related
metabolism and decreased effect of behaviors such as preparing and eating meals,
drugs such as anticoagulants, sleep driving, engaging in sex, or making phone
glucocorticoids, tricyclic anti- calls during sleep without any memory of the
depressants, and kinetine. event,
- Pentobarbital may cause • Alcohol, and CNS depressants increase the risk
hepatotoxicity If taken with large of sleep related behaviors.
doses of acetaminophen.
- do not confuse phenobarbital and Adverse
Side effects
pentobarbital. reactions
associated to
associated to
Alprazolam
Side effects and adverse Alprazolam
reactions of Barbiturates: - Lethargy - Depression
- Drowsiness - Tolerance
• Hangover - Dizziness - Dependence
• REM rebound - Headache - Withdrawal
• Dependence - Constipation - Hypotension
• Tolerance - Anterograde - Tachycardia
• Excessive (CNS) depression amnesia - Seizure
• Respiration depression
• Hypersensitivity
The Nursing Process for Patient’s taking
Benzodiazepines:
2. Benzodiazepines
- Benzodiazepines are used to induce Assessment:
sleeping. • Obtain a drug history
- This medication increase the action of • Assess baseline vital signs
the gamma-aminobutyric acid or GABA • Assess renal function
to the gaba receptors which in turn, will - Urine output should be 1500 ml per day. Renal
reduce the neuron excitability. impairment could prolong drug action by
increasing the half-life of the drug.
EXAMPLES:
✓ Alparazolam Nursing diagnosis:
✓ Extrasolar • Sleep deprivation related to adverse effect of
✓ Lorazepam insomnia.
✓ Temazepam • Ineffective breathing pattern related to CNS
✓ Triazolam depression.
✓ Quazepam
✓ Diazepam Planning:
• Patient will receive adequate sleep when
Antagonist: taking benzodiazepine.
Flumazenil: taken when the examples of Nursing interventions:
Benzodiazepines are taken with a large dose or • Monitor vital signs
an overdosage. • Use bed alarm
• Examine for skin rashes

cns
PHARMACO- CNS

Patient teaching: • Check for signs of respiratory depression like


• Avoid alcohol, antidepressants, antipsychotic slow irregular breathing patterns.
and opioid drugs while taking benzodiazepines. • Use bed alarm for older adults, or patients
• Do not drive a motor vehicle or operate receiving non-benzodiazepines for the first
machinery when using benzodiazepines. time, confusing may occur and injury may
• Benzodiazepines should be greatly withdrawn result.
• Observe patient for side effects of non-
Evaluation: benzodiazepines such as hangover, or residual
• Assess the effectiveness of benzodiazepine: If sedation, lightheadedness, dizziness, or
the patient has achieved better sleep or not. confusion.
• Evaluate respiratory status
Patient teaching:
3. Non- Benzodiapines • Teach non-pharmacologic methods to induce
- Non-benzodiazepines sleep
pharmacodynamics are almost entirely • Avoid alcohol, antidepressants,
the same as benzodiazepines drugs and antipsychotics, and narcotic drugs
therefore employ similar benefits, side • Take medication before bedtime.
effects, and risks.
- However, non-benzodiazepines have Evaluation:
dissimilar or entirely different chemical • Evaluate effectiveness of sedative-hypnotics
structures and therefore unrelated to in promoting sleep.
benzodiazepines on a molecular level. • Determine for development of side effects

Examples 4. Melatonin Agonist


✓ Zolpidem Tartrate: - Ramelteon is the newest category of
- used for short term treatment of sedative-hypnotics called melatonin
insomnia specifically its less than 10 agonist
days. This medication has a half-life of - Remelteon is the first hypnotic
1.4 to 6.73 hours. approved by the USFDA that is not
- This medication is metabolized in the classified as a controlled substance.
liver and is excreted in the bile, urine, - This drug acts by selectively targeting
and feces. melatonin receptors to regulate
- Dose should be decreased if circadian rhythm in the treatment of
prescribed in adults. insomnia.
✓ Eszopiclone - Remelteon has not been shown to
✓ Zaleplon decrease rapid eye movement sleep.
- This drug has a half-life of 1 to 2.6
Side Effects of hours
Adverse Reaction
Medication
• Drowsiness • Tolerance Adverse Effect Reactions
• Lethargy • Psychological or of Melatonin Agonist
• Headache physical dependence
• Hot flashes • Withdrawal
• Hangover •Drowsiness
•Dizziness
•Fatigue
Administering non-benzodiazepines to patients •Headache
we need to asses the following: •Nausea
•Suicidal Ideation
Assessment:
• Vital Signs and Laboratory tests (aspartame
aminotransferase, alanine aminotransferase, RECAP:
bilirubin) Depressants:
• Obtain a drug history • Under depressants: there are medications or
classifications called; Sedative-hypnotics,
Nursing Diagnosis: general anesthetics, Analgesics (opioid and non-
• Sleep deprivation related to anxiety opioid), antipsychotic, anticonvulsants ,
• Fatigue related to insomnia antidepressant.
Under Sedative-Hypnotics:
Planning: - Given to patients who have problems in
• Patient will remain asleep for 6-8 hours sleeping.
Nursing interventions: • This medications are used to promote better
• Monitor vital signs or quality sleep to the patients.
1. Barbiturates

cns
PHARMACO- CNS

2. Benzodiazepines b) Stage 2: Excitement or Delirium


3. Non-Benzodiazepines ✓ Produces a loss of consciousness caused
4. Melatonin Agonist by depression of the cerebral cortex
✓ Confusion, excitement or delirium occur
CNS PART 2 ✓ Induction time is short

ANESTHETICS c) Stage 3: Surgical


- substances that induces insensitivity to ✓ Surgical procedure is performed during
pain this stage
- classified as: ✓ There are 4 phases. Surgery is usually
✓ General performed in phase 2 and upper phase
✓ Local 3.
- Take note: you need to monitor vital ✓ As anesthesia deepens, respirations
signs following general and local become shallower and the respiratory
anesthesia because hypotension and rate is increased
respiratory depression may result.
d) Stage 4: Medullary Paralysis
BALANCED ANESTHESIA ✓ Considered as a toxic stage of
- a combination of several drugs each anesthesia in which respirations are
with a specific effect to achieve lost and circulatory collapse occurs
analgesia, muscle relaxation, ventilatory assistance is necessary in
unconsciousness and amnesia rather this stage.
than using one drug. ✓ The patient’s response to anesthesia
may differ according to variables
So why is this utilize? related to health status of the
- This is used to minimize cardiovascular individual.
problems, decreases the amount of ✓ These variables inlcude - age, a current
general anesthetic, used reduces health disorder, pregnancy, history of
possible post-anesthesia nausea and smoking and frequent use of alcohol
vomiting and this minimizes the and drugs. These problems must be
disturbance of organ function and identified before surgery because the
decreases pain. type and amount of anesthetic
required may need to be adjusted.
BALANCED ANESTHESIA
May include the following: Anesthetic agents can be administered
1. A hypnotic drug is given the night through:
before the operation a) Inhalation
2. There is premedication with an opioid b) Intravenous
analgesic or benzodiazepine plus an c) Topical
anticholinergic given about 1 hour d) Local infiltration
before surgery to decrease secretions e) Spinal route
3. The use of a short-acting non-
barbiturate medication such as propofol INHALATION ANESTHETICS
4. The use of an inhaled gas, often a - gas or volatile liquids administered as gas are
combination of an inhalation used to deliver general anesthesia
anesthetic, nitrous oxide and oxygen Examples of Volatile liquids:
5. The use of a muscle relaxant given as ✓ Halothane
needed. You can appreciate more of ✓ Methoxyflurane
this one, once that you will be rotated ✓ Fluorine
already in the operating room. ✓ Isoflurane
✓ Desflurane
Stages of Anesthesia: ✓ Sevoflurane

a) Stage 1: Analgesia Example of Gas anesthetic:


✓ this begins with consciousness and ends Nitrous oxide
with loss of consciousness - You’ll be familiar with this inhalation
✓ speech is difficult anesthetics when you will be exposed in
✓ sensations of smell and pain are lost the operating room. As you will be
✓ dreams and auditory & visual making also and operating room
hallucinations may occur requirements.
✓ This stage may be called the
“INDUCTION STAGE”

cns
PHARMACO- CNS

Adverse Reaction of Inhalation ⚫ Diagnostic procedures such as lumbar


Anesthetic puncture and thoracentesis
- Respiratory depression - EXAMPLES OF LOCAL ANESTHETICS:
- Hypotension ✓ Chloroprocaine hydrochloride
- Dysrhythmia ✓ Procaine hydrochloride
- Hepatic dysfunction ✓ Lidocaine hydrochloride
* Take note that these drugs may ✓ Mepivacaine hydrochloride
trigger malignant hyperthermia. ✓ Prilocaine hydrochloride
✓ Bupivacaine hydrochloride
*Malignant Hyperthermia ✓ Dibucaine hydrochloride
- a type of severe reaction that of course in ✓ Etidocaine hydrochloride
response to a particular medication used during ✓ Tetracaine hydrochloride
general anesthesia among those who are
susceptible. Lidocaine - has a rapid onset and a long
duration of action. This is more stable solution
Complications form and causes fewer hypersensitivity
Symptoms Include reactions than procaine
Include
• Muscle
• Muscle SPINAL ANESTHESIA
Rigidity
Breakdown - induction of spinal anesthesia requires that a
• High Fever
• High blood local anesthetic be injected into the
• Fast Heart
potassium subarachnoid space:
Rate
➢ Below the 1st lumbar space (L1) in
adults
INTRAVENOUS ANESTHETICS ➢ The 3rd lumbar space (L3) in children
- may be used for general anesthesia or for the - In a postdural puncture headache might result
induction stage of anesthesia following a spinal anesthesia possibly because
Examples of Intravenous anesthetics: of a decrease of cerebrospinal fluid pressure
✓ Propofol- Propofol - supports microbial caused by the leak of fluid at the needle
growth and may increase the risk of insertion point.
bacterial infection. Thus, discarding
open vials within 6 hours is a necessary Nursing intervention:
precaution in the prevention of sepsis - Encourage the patient to remain flat
✓ Droperidol following surgery
✓ Etomidate - Increase fluid intake usually decreases
✓ Ketamine hydrochloride the likelihood of leaking spinal fluid
* Which are also commonly used to provide a
Total Intravenous Anesthesia or TIVA. Various sides of the spinal column can be used
- these anesthetics have rapid onset and for a nerve block with a local anesthetic.
short duration of action
➢ Spinal block results from the penetration of
TOPICAL ANESTHETICS an anesthetic into the subarachnoid space
- used to decrease sensitivity of nerve which is the space between the pia mater
endings in the affected area. membrane and the arachnoid membrane.
- These can be in different forms:
 Solutions ➢ Epidural block is a placement of the local
 Liquid sprays anesthetic in the epidural space just posterior
 Ointments to the spinal cord or the dura mater. The
 Creams epidural space is located between the posterior
 Gels and powders longitudinal ligament on the anterior side and
the ligament of flavum posteriorly.
LOCAL ANESTHETICS
- are used to block the pain at the site ➢ Caudal block is an epidural block placed by
where the drug is administered by administering a local anesthetic through the
preventing the conduction of nerve sacral hiatus.
impulses
- these are useful in : ➢ Saddle block is given at the lower end of
⚫ dental procedures the spinal column to block the perineal area.
⚫ Suturing skin lacerations Blood pressure should be monitored of these
⚫ Short term surgery at a localized types of anesthesia because a decrease in blood
area pressure resulting from the drug and procedure
⚫ Block nerve impulses might occur.
⚫ Below the insertion of spinal
anesthetic

cns
PHARMACO- CNS

ANTI-SEIZURE DRUGS 1. Hydantoins


- these medications are used for epileptic
seizures these are also called as ✓act by inhibiting sodium influx, stabilizing cell
membranes, reduces repetitive neuronal firing
ANTICONVULSANTS or ANTI-EPILEPTIC
and limit seizures by increasing electrical
drugs.
stimulation threshold in the cardiac tissue.
- the medication acts by stabilizing nerve
cell membrane and suppress abnormal ✓it also acts as antidysrhythmic
electrical impulses in the cerebral
✓it has a slight effect on general sedation and it
cortex.
is non-addicting
- this type of medication prevents
seizures but do not eliminate the cause ✓Phenytoin - the first anti-seizure drug used to
or provide a cure treat seizures which is a hydantoin. It was
- Dosage of the medication usually starts discovered in 1938 and still commonly used for
low and gradually increases over a controlling seizures as of today.
period of weeks until the serum drug
✓Please take note that hydantoins should not
level is within therapeutic range or the
be used during pregnancy because it can have
seizure ceases.
the rhetogenic effect on the fetus. Meaning it
- The medication is usually taken
may cause birth defects or congenital
throughout the lifetime but it may be
anomalies.
discontinued if seizure has not occurred
in 3 to 5 years.
Hydantoin: Phenytoin
*These are the international classifications of - is used for the treatment of tonic-clonic
seizures. You may also refer to your textbook on seizure, partial seizures and status epilepticus
page 247. Please watch this video on epilepsy or
seizure. You may locate this one as one of the - this medication is slowly absorbed in the small
contents of the prerequisite for module 2M.* intestine

Antiseizure drugs act in 3 ways: - it has a half-life of 24 hours but it can range 7
1. By suppressing Sodium influx, through to 42 hours.
the drug binding to the sodium channel
when it is inactivated. This prolongs the - the drug is metabolized and excreted through
channel inactivation and thereby the urine.
prevents neuron firing. Examples of
medication with this mechanism of - it has a narrow therapeutic range which is 10-
action are - phenetoin, phosphanatoin, 20 mcg/mL which is generally considered as to
carbamazepine, oxcarbazepine, valproic 1-1.2mcg/mL, unbound or free phenytoin.
acid, superimate, zonasamite and
lamotrigine. Nurse application for these learners:
2. By suppressing the calcium influx, ⚫ You need to monitor the serum level of
which prevents the electric current phenytoin because again this medication has
generated by the calcium ion to the t- narrow therapeutic range if the medication will
type calcium channel. Examples of be or will exceed the 20mcg/mL then, it may
medications with this mechanism of cause toxic effects and if the medication is
action are - valproic acid and below 10mcg/mL then the medication will not
ethosoxoxymine. be render a desired effect or the patient will not
3. By increasing the action of Gamma- feel the desired effect of the medication
aminobutyric acid (GABA), which
inhibits neurotransmitters throughout So again if the medication is below the desired
the brain. Examples of medication with range the patient is not receiving the required
this mechanism of action are - drug dosage to control the seizure activity but if
barbiturates, benzodiazepines and the drug level is above the desired range drug
tiagobin. toxicity may result that is why again monitoring
the therapeutic serum drug range is of utmost
These are the antiseizure drugs we will importance.
discuss for this module:
✓ Hydantoins
✓ Barbiturates ➢Orally administered phenytoin has an onset
✓ Succinimides of action of 30 mins - 2 hrs with a peak of 1.5-
✓ Benzodiazepines 6hrs a steady state of serum concentration at 7-
✓ Iminostilbenes 10 days and a duration of action dependent on
✓ Valproate the half-life which could be up to 45hrs

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PHARMACO- CNS

➢IV infusion must be administered through by Hyperglycemia


a large vein by a central line or peripherally - results after hydantoin usage but this onky
inserted central catheter. The IV line should happens after a long period of hydantoin use.
always be flushed with saline solution before This happens because there is an increased
and after use to reduce venous irritation blood glucose due to the inhibition of the drug
on the release of insulin
➢This medication may be diluted with saline
solution and dextrose should be avoided
Less severe side effects of Hydantoin
because of drug precipitation.
➢IV Phenytoin 50 mg or a fraction thereof must ➢ Nausea and vomiting
be administered over one minute for adults and ➢ Gingival hyperplasia - overgrowth of gum
a rate of 25mg/min for older adults tissue
➢Infusion rates more than 50mg/min may ➢ Constipation
cause severe hypotension or cardiac
➢ Drowsiness
dysrhythmia. Especially for adults and
debilitated patients. ➢ Headaches

➢This medication must not be administered ➢ Slurred speech


through intramuscular or IM because the ➢ Confusion
absorption is erratic and irritate the tissues
which may cause damage. ➢ Alopecia

➢ Hirsutism - a condition in women that results


Take note: Cimetidine and Sulfonamides can
in excessive growth of dark or coarse hair in a
increase the action of hydantoins by inhibiting liver
male-like pattern which is usually very evident on
metabolism which is necessary for drug excretion
the face, chest and back
Nursing implication: ➢ Nystagmus- is a vision condition in which the
You need to monitor the serum level of eyes make repetitive, uncontrolled movements.
phenytoin as if it will not be excreted by the These movements often result in reduced vision
body the serum level might exceed the and depth perception and can affect balance and
20mcg/mL and so what are possibilities: coordination

✓The patient might experience toxic effects of


the medication
On the contrary, antacids, calcium
Before we administer the medication Phenytoin
preparations, sucralfate and antineoplastic
to our patients, what should be part of our
drugs decrease the absorption of hydantoins.
assessment?

Adverse reactions of Hydantoins Assessment:


✓ Depression ✓Obtain a health history that includes current
✓ Suicidal ideation drugs and herbs the patient uses.
✓ Steven-Johnson’s
syndrome ✓Report and document any probable drug to
✓ Ventricular fibrillation drug or herb to drug interaction
✓ Blood dyscrasias ✓Assess the patient’s knowledge regarding the
✓ Purple glove syndrome medication regimen
✓ Hyperglycemia
✓Check urinary output to determine whether it
is adequate. The urine output of the patient
Steven-Johnson’s syndrome must be greater than 1500mL/day
- a rare serious disorder of the skin and the ✓Determine laboratory values related to renal
mucous membranes. and liver function if both BUN or blood urea
- it is usually a reaction to medications that start nitrogen and creatinine levels are elevated. A
with flu-like symptoms, followed by a painful renal disorder should be suspected. Elevated
rash that spreads and blisters then the top layer serum liver enzymes indicate a hepatic disorder.
of affected skin dies, sheds and begins to heal
after several days. Nursing Diagnosis:
✓ Risk for injury
Purple glove syndrome
- is an uncommon but dreaded complication of ✓ Risk for fall
intravenous phenytoin administration
characterized by pain, edema and purple blue Considering that Phenytoin has an adverse
discoloration of the limb distal to the injection effect of suicidal ideation and a side effect of
site. drowsiness.

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PHARMACO- CNS

Planning: ✓Coach patients to take anti-seizure drugs at


Phenytoin will be admistered to a patient in the same time every day with food and milk
order to diminish the patient’s frequency of
✓Tell patients that your reed may be harmless
seizure as well as to adhere to anti-seizure drug
pinkish red reddish brown in color
therapy
✓Advise patients to maintain good oral hygiene
Nursing interventions: and to use a soft bristled toothbrush to prevent
✓ Monitoring serum drug level of anti-seizure gum irritation and bleeding
medication to determine the therapeutic range.
✓Teach patients to report symptoms of sore
And again remember that the therapeutic of
throat, bruising and nose bleeds which my
Phenytoin is 10-20mcg/mL
indicate a blood dyscrasia.
✓Encourage patients compliance with
medication regimen. Monitor patients complete Evaluation:
blood count or CBC levels for early detection of ✓Evaluate effectiveness of drugs in controlling
blood discretion seizures
✓Use seizure precautions or environmental ✓Monitor serum phenytoin levels
protection from sharp objects such as table
✓Monitor patients for hydantoin overdose
corners for patients at risk for seizures
2. BARBITURATES
✓Determine whether the patient is receiving
- another classification of medication with an
adequate nutrients because phenytoin may
anti-seizure property
cause anorexia, nausea and vomiting
- we already tackled barbiturates under
✓Advise female patients who are taking oral sedative hypnotic
contraceptives and anti-seizure drugs to use an - example: Phenobarbital
additional contraceptive method
Phenobarbital
✓Patient teaching during phenytoin therapy
- used to treat tonic-clonic, partial and
must include:
myoclonic seizures as well as status epilepticus
◼Teaching patient to shake suspension form of or the rapid succession of epileptic seizures
medications thoroughly before using to - this medication reduces seizures by enhancing
adequately mix the medication to ensure the activity of the gamma-aminobutyric acid
adequate usage which is an inhibitory neurotransmitter.
- this medication has a therapeutic range of 20-
◼Advise patients not to drive or perform other 40mcg/mL
hazardous activities when initiating anti-seizure
therapy as drowsiness may occur 3. SUCCINIMIDE
◼Counsel female patients contemplating - used to treat seizure
pregnancy to consult with a health care - example: Ethosuximide
provider because phenytoin and valproic acid
may have a theratogenic effect Ethosuximide
- used to treat absence seizure
◼Monitor serum phenytoins level level closely - this medication acts by decreasing calcium
during pregnancy because seizures tend to influx through the t-type calcium channel
become more frequent due to increased - this medication has a therapeutic range of 40-
metabolic rates. 100mcg/mL
- if you have noticed the therapeutic range of
Patient teachings on client taking Phenytoin this medication is not as narrow as the
must include: therapeutic range of the Phenytoin (therapeutic
range is very narrow)
✓The avoidance of alcohol and other CNS Adverse Effects
depressants because they can cause an added
depressive effect on the body ➢ Blood dyscrasias
✓Teach patients not to abruptly stop drug ➢ Renal and liver impairment
therapy but rather to withdraw the prescribed ➢ Systemic lupus erythematosus
drug gradually under medical supervision. This
is to prevent seizure rebound or the recurrence
of seizures and status epilepticus Systemic lupus erythematosus- an autoimmune
disorder in which the immune system of the
✓Advise patients with Diabetes Mellitus to body mistakenly attacks healthy tissues.
monitor serum glucose levels more closely than
usual because phenytoin may inhibit insulin
release causing an increase in glucose level
4. BENZODIAZEPINES
- has an anti-seizure property

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PHARMACO- CNS

- example: ✓Valproic acid causes major malformations


⚫ Clonazepam
✓Antiseizure drugs tend to act as inhibitors of
⚫ Clorazepate dipotassium vitamin K this contribute to the hemorrhage in
infants shortly after birth
⚫ Lorazepam
⚫ Diazepam ✓Pregnant women taking anti-seizure drugs are
given an oral vitamin K supplement during the
Clonazepam - is effective in controlling absence last week or the last 10 days of the pregnancy
and myoclonic seizures but tolerance may or vitamin K is administered to the infant soon
develop 6 months after drug therapy starts after birth
Clorazepate dipotassium - administered for
✓Antiseizure drugs also increase the loss of
treating partial seizures
folate or folic acid in pregnant women. Thus,
Diazepam - administered through IV to treat
pregnant individuals should take daily folate
status epilepticus; has a short term effect; thus
supplements because folate is very important
phenytoin or phenobarbital must be given
during pregnancy as it will prevent neural tube
during or immediately after administration of
defects.
diazepam
Antiseizure drugs and Febrile seizures:
5. IMINOSTILBENES
✓Seizures associated to fever occur in children
- therapeutic serum range is 40-12mcg/mL
between 3 months and 5 years of age
- a potentially toxic interaction can occur when
grapefruit juice is taken with carbamazepine ✓Prophylactic antiseizure drug treatment such
and drug concentrations must be carefully as Phenobarbital or Diazepam may be indicated
monitored for high risk patients
Carbamazepine - an iminostilbene is used to ✓Valproic acid should not be given to children
control tonic-clonic and partial seizures younger than 2 years old because of
- also used for psychiatric disorders, trigeminal hepatotoxic effect
neurolgia and alcohol withdrawal.
Antiseizure drugs and Status epelipticus
6. VALPROATE OR VALPROIC ACID Status epilepticus
- is prescribed by tonic-clonic absence and mix - a continuous seizure state which is considered
type of seizures as a medical emergency
- Although the safety and efficacy of this drug
has not been established for children younger ✓If treatment is not started immediately, death
than 2 yrs of age could result
- care should be taken when giving this drug to
the very young children and to patients with ✓Drug of choice: Diazepam or Lorazepam via IV
liver disorders because Hepatotoxicity is one of followed by Phenytoin via IV
the possible adverse reactions ✓For continued seizures, Midazolam or
- liver enzymes should be monitored Propofol and then high-dose Barbiturates are
- therapeutic serum range is 50-100mcg/mL used
Anti-seizure drug dosages usually start low and
gradually increase over a period of weeks until ✓These drugs must be administered slowly to
the serum drug level is within the therapeutic avoid respiratory depression.
range or seizure seizes. Serum antiseizure drug
levels should be closely monitored to prevent
toxicity. EPILEPSY
• Epilepsy is a group of neurological diseases
Important aspects with regards to anti-seizure characterized by recurrent seizures.
drugs in Pregnancy: • Seizures happen as a result of a sudden surge
in the brain’s electrical activities.
✓During pregnancy, seizure episodes increase
• Depending on which part of the brain is
25% in women with epilepsy
affected, a seizure may manifest as:
✓Hypoxia may occur during seizure that is why
- Loss of awareness
as much as possible seizure should not occur
during pregnancy as it will pose a risk to the - Unusual behaviors/sensations
fetus
- Uncontrollable movements
✓Phenytoin and Carbamazepine are linked to
fetal anomalies that is why if a woman is if a • The brain is a complex network of billions of
woman is taking carbamazepine or phenytoin, neurons; neurons can be excitatory or
you need to consult your healthcare provider inhibitory.
immediately if you suspect of pregnancy

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PHARMACO- CNS

• Excitatory neurons stimulate others to fire - Complex partial seizures: involves a loss or
action potentials and transmit electrical changes in consciousness, awareness and
messages, while inhibitory neurons SUPPRESS responsiveness.
this process, preventing EXCESSIVE firing.
• A balance between excitation and inhibition is CAUSES:
essential for normal brain functions. • Epilepsy may developed as a result of a brain
injury, tumor, stroke, previous infection or a
• In epilepsy, there is an UP-regulation of
birth defect.
excitation and/or DOWN-regulation of
inhibition. • Generalized seizures that start in childhood
are likely to involved genetic factors.
• Causing lots of neurons to fire
SYNCHRONOUSLY at the same time.
• Epilepsy due to a single gene mutation is rare.
• If this abnormal electrical surge happens More often, an interaction of multiple genes
within a limited area of the brain, it causes and environmental factors is responsible.
PARTIAL or FOCAL seizures. Hundreds genes have been implicated.

DIFFERENCE BETWEEN PARTIAL OR FOCAL • Examples include genes encoding for GABA
SEIZURES receptors. Major components of the inhibitory
circuit and ion channels.
• Generalized Seizures: if the entire brain is
involved, generalized seizures will result. Many genetic disorders that cause brain
abnormalities or metabolic conditions have
• Generalized seizures subdivide further to: epilepsy as a primary symptom.
- Absence seizures: this type occurs most often
in children, and is characterized by a very brief The cause of epilepsy is unknown in about half
loss of awareness, commonly manifested as a of cases.
blank stare, with or without subtle body
movements such as eye blinks, lip smacking, DIAGNOSIS:
People with absence seizures may not be aware is based on:
that something is wrong for years. -Observations of symptoms,
- Tonic seizures: are associated with stiffening -Medical history, and
of muscles, and may cause the person to fall -Electroencephalogram (EEG) to look for
often backwards abnormal brain waves. An EEG may also help in
- Atonic seizures: are also known as drop differentiating between partial and generalized
attacks, are characterized by a sudden loss of seizures.
muscle tone, which cause the person to collapse -Genetic testing maybe helpful when genetic
or drop down. factors are suspected
- Clonic seizures: are associated with rhythmic
TREATMENTS:
jerking muscle movements.
There is no cure for epilepsy but various
Clonic seizures are rare.
treatments are available to control seizures.
- Myoclonic seizures: are brief jerks or twitches
of a muscle or a group of muscles. -MEDICATION: successfully controls seizures for
There can be one or many twitches occurring about 70% of cases. Many anti-epileptic drugs
within a couple of seconds. are available which target SODIUM CHANNELS,
- Tonic-clonic seizures: are also known as GABA RECEPTORS and other components
convulsive seizures which are combinations of involved in neural transmission. Different
muscle stiffening and jerking. medicines help with different ways of seizures.
This type is what most people relate to when
they think of a seizure. -DIETARY THERAPY: ketogenic diet has been
It also involves sudden loss of consciousness shown to reduce or prevent seizures in many
and sometimes loss of bladder control. children whose seizures could not be controlled
A tonic-clonic seizure that lasts longer than 5 with medication.
mins requires immediate medical treatment. Ketogenic diet is a special high-fat, low-
carbohydrate diet that must be prescribed and
• Partial seizures subdivide further to: followed strictly. With this diet the body uses
- Simple partial seizures: depending on the fat as the major source of energy instead of
affected brain area, patients may have unusual carbohydrates. The reason why this helps
feelings, strange sensations or uncontrollable control epilepsy is unclear.
jerky movements, but remain conscious and
aware of the surroundings. -NERVE STIMULATION THERAPY: such as vagus
nerve stimulation in which a device is placwd
under the skin programmed to stimulate the

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PHARMACO- CNS

vagus nerve at a certain rate. The device acts as -VR therapy ranges from treadmill training,
a pacemaker for the brain. The underlying balance and gait exercises to therapy tools that
mechanism is poorly understood but it has been provide excitement and prevent boredom.
shown to reduce seizures significantly.
As technology progress the training options for
-SURGERY: may be performed to remove part of improving motor functions will continue to
the brain that causes seizure. This is usually expand.
done when tests shows that seizures are
originated from a small area that does not have CNS 3
any vital function. DRUGS FOR PARKINSON’S DISEASE

UNDERSTANDING PARKINSONS DISEASE (PD) Parkinson’s Disease


Patients with Parkinson’s disease experience a - a chronic, progressive, neurologic disorder
loss of cells to a region of the brain called that affects the extrapyramidal motor tract that
Substantia nigra. controls posture, balance and locomotion
- most common form of Parkinsonism which is
Substantia nigra considered a syndrome or a combination of
-produces dopamine, a chemical messenger similar symptoms because of its major features:
responsible for transmitting signals within the
brain that allow for coordination of movement. • Rigidity (abnormal increased muscle tone)
-increases with movement, postural changes
-When dopamine levels decrease, it causes caused by rigidity and bradykinesia included
abnormal brain activity leaving patients less chest and hear thrust forward with the knees
able to direct or control their movement. and hips flexed, shuffling gait, arms swing, no
facial expressions, involuntary tremors with the
Patient with Parkinson’s will see a decline in head and neck, peel rolling motions of the
physical, psychological, and neurological hands
functions. The disease manifests in the form of • Bradykinesia (slow movement)
slowed movement known as BRADYKINESIA, • Gait disturbances
resulting in muscle tremors, gait problems, • Tremors
rigidity or stiffness, postural instability, and
cognitive impairment. NEUROTRANSMITTERS
• DOPAMINE (DA)
Since the disease is both chronic and - inhibitory neurotransmitter
progressive, patients gradually lose their ability -release from dopaminergic neurons
to perform even the simplest of tasks. - maintains and controls Ach and inhibits its
excitatory response
Although there is no cure for Parkinson’s a -places a part in controlling the movement a
number of treatments are available for the person makes as well as their emotional
management of motor and non-motor responses
symptoms to be used in combination with - right balance of dopamine is vital for both
medications. physical and mental well- being.
- vital brain function that affect mood, sleep,
Currently, the most popular surgical therapy memory, learning, concentration and motor
available for Parkinson’s disease is DEEP BRAIN control are influenced by the level of dopamine
STIMULATION (DBS). in a person’s body
-has a control in the locomotion or movement
of a person
DEEP BRAIN STIMULATION (DBS).
-delivers electrical pulses to brain cells to • ACETYLCHOLINE (Ach)
decrease the symptoms of Parkinson’s. - has an excitatory neurotransmitter
-DBS typically works best to lessen motor - releases from cholinergic neurons
symptoms like stiffness, slowness and tremors. - chief neurotransmitter of the parasympathetic
Targeted exercise that focuses on general nervous system that contracts smooth muscles,
mobility and dexterity may slow down the dilates blood vessels, increases watery
progression of the disease. secretions and slows heart rate
Lifestyle modifications, a balanced diet, and rest - essential for muscles to contract
may also slow down symptoms. An up and
coming form of treatment for Parkinson’s *this neurotransmitters need to work hand and
disease is VIRTUAL REALITY. hand in order to create a balance, others if one
is elevated there will be a chaos in the body
VIRTUAL REALITY (VR) system*
-is a fun way to practice motor skills, while also
combating depression in patients.

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PHARMACO- CNS
Side effects of Anticholinergics

HOW PARKINSON’S DISEASE DEVELOPS


• Dry mouth
- approximately 86,000 billion of neurons in the
brain •Dry secretions

- caused by an imbalance of the • Urinary tension


neurotransmitters: DA and Ach
• Constipation
- marked by the degeneration of dopaminergic • Blurred vision
neurons of the extrapyramital tract in the
midbrain reason is UNKNOWN (less DA is • Increase in HR
produced)

-excitatory response exceeds the inhibitory ASSESMENT:


response of the DA this is because the level of
Ach is beyond the level of the DA could handle ✓Obtain a health history – report history of
or inhibit... Why? Because only the DA glaucoma, GI dysfunction, Urinary tension,
production is affected but the production of the Angina
Ach continues thus there is more Ach than DA. ✓Obtain a drug history- report any probable
-excessive amount of Ach stimulate neurons drug to drug interaction such as phenothiozine,
that produce GABA (inhibits the activity of tricyclic anti depressants and antisimine (can
neuron) increase trihexyphenidyl hydrochloride)

-Gama amino buteric acid is considered an ✓Assess baseline vital signs for future
inhibitory neurotransmitter because it blocks comparison- HR may increase, assess patient’s
certain brain signals and decreases certain knowledge regarding the medication
activities in the Nervous system and when
certain brain signals are inhibited in NS ✓Assess usual urinary output- urinary
symptomatic movement disorders of retension may occur with continuous use of the
Parkinson’s disease occurs like: rigidity, tremors, medication
gait disturbance and bradykinesia
NURSING DIAGNOSES:
- 80% of DA has been depleted ✓Impaired mobility related to muscle rigidity
✓Impaired urinay elimination related to urinary
-dopamine is produced by the dopaminergic retention
neurons
PLANNING:
-symptoms of parkinson’s disease can be lessen ✓Decrease involuntary symptoms caused by
through the use of nonpharmarcologic measure Parkinson’s diseases or drug- induced
such as: parkinsonism
• Exercise- can improve mobility and
flexibility NURSING INTERVENTIONS:
• Nutrition- balance diet with fiber and ✓Monitor vital signs, urine output and bowel
fluids helps prevent constipation and sounds
weigh loss
• Group support- to help cope and ✓Observe for involuntary movements
understand the disorders
✓Patient- teachings:
- avoid alcohol, cigarette, caffeine,
DRUGS FOR PARKINSON’S DISEASES
aspirin (to decrease gastric acidity)
1. Anticholinergics
- encourage to relieve dry mouth with
- inhibits the release of acetylcholine
hard candy, ice chips, and sugarless
- 1 of the problems of Parkinson’s disease is the
gum
increased number of ACh so this inhibits the
- suggest usage of sunglasses in direct
ACh
sunlight because of photophobia
Example: benzotropine mesylate,
Advise patient to void before taking the
trihexyphenidyl hydrochloride
drug
REMEMBER: glaucoma is contraindicated !!!
- encourage patients to ingest foods high
why? Because this medication can actually
in fiber.
induce glaucoma and so if the patient has
already a glaucoma then the possibility is that
EVALUATION:
the glaucoma of the patient will worsen
✓Evaluate the response to the medication and
-block cholinergic receptors
determine whether symptoms are controlled.

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PHARMACO- CNS

ASSESSMENT:
2. Dopamine Replacements (dopaminergics) ✓Obtain vital signs- for future comparisons
Example: carbidopa and Levodopa
✓Assess for signs and symptoms- including
✓ LEVODOPA
stoop forward posture, shuffling gait, mask
- 1st drug of dopaminergic which was
facies and resting tremors
introduced in 1961 but no longer
available in US ✓Obtain patient history and contraindications-
- effective in diminishing parkinson’s glaucoma, heart disease, peptic ulcer, kidney/
disease and increasing the mobility liver disease and psychosis because severe
because the blood brain barrier admit cardiac renal are contraindications of levodopa
levodopa but not dopamine.
- the enzyme dopa decarboxylase ✓Obtain drug history- if the patient is taking
converts levodopa to dopamine in the monoamine oxidase inhibitor + cabidopa-
brain but it’s also found in the levodopa= HYPERTENSIVE CRISES- is a severe
peripheral nervous system and allows increase in the BP that may lead to stroke.
99% of levodopa to be converted to
dopamine before it reaches the brain NURSING DIAGNOSIS:
therefore only about 1% of levodopa ✓Impaired physical mobility related to dizziness
taken in is easy available to be
✓Risk for fall
converted to dopamine once it reaches
the brain and large doses are needed to
PLANNING:
achieve pharmacologic response.
✓Patient’s symptoms of parkinson’s disease will
- These high doses could cause many side
be decrease or absent after 1- 4 weeks of drug
effects including nausea, vomiting, etc.
therapy
Because the side effects and the fact
that so much levadopa is metabolized
NURSING INTERVENTIONS:
before it reaches the brain an
✓Monitoring vital signs and ECG- orthostatic
alternative drug carbidopa was
hypotension may occur
developed.
✓Observes for symptoms of syncope
✓ CARBIDOPA
- to inhibit dopa decarboxylase ✓Administer carbidopa- levodopa with LOW-
- by inhibiting the enzyme in the PROTEIN FOOD
peripheral nervous system more ✓Observe for symptoms of Parkinson’s disease
levodopa reaches the brain
- combined with levodopa in the ration of
1 carbidopa: 10 levodopa PATIENT TEACHING
Advantage Disadvantage - urge not to abruptly discontinue the
more dopamine more available medication
reaches the levodopa, more
basal ganglia side effects may - advise to avoid crushing the extended release
and smaller occur such as tablet
doses of nausea, vomiting,
levadopa are dystonic -suggest that taking carbidopa- levodopa with
required to movement, food may decrease GI upset but will slow the
achieve the psychotic rate of drug absorption
desired effect behavior
EVALUATION:
✓Evaluate effectiveness of drug therapy in
- The peripheral side effects are not as controlling symptoms of parkinson’s disease
prevalent but palpitations may occur ✓Determine if there is an absence of side
- GI disturbances are common who are effects
taking carbidopa- levodopa because ✓Determine if the patient and family have
dopamine stimulates the increased knowledge of drug regimen.
chemoreceptor trigger zone (CTZ) in
medulla which stimulate the vomiting
center 3. Dopamine Agonists
- taking it with food can decrease the - called dopaminergics
vomiting because it loses the -used to stimulate dopamine receptors
absorption rate of the medication Example:
- stimulate dopamine receptors Amantadine, bromocriptine, pramipexole,
ropinirole HCl

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PHARMACO- CNS

✓ AMANTADINE not enough considering that there is


- anti-viral drug that affects the dopamine degeneration of dopamic neurons
receptors - the produced dopamine has to be
- can be taken alone or combination with preserved
carbidopa- levodopa or anticholinergic - -MAO-B causes catabolism of the
-produces improvement in symptoms but drug dopamine- this enzyme will further
tolerance develops deplete/ decreases the number of
- can be used for drug-induced parkinsonism dopamine
-stimulates dopamine receptors - Selegiline will inhibit the MAO-B thus
Side Effects the dopamine will be preserved or the
• orthostatic dopamine will not be catabolized by the
• hypotension MAO-B.
• confusion - MAO-A (enzyme that promotes
• urinary retention metabolism of tyramine in the GI tract,
• constipation if tyramine is not metabolized it can
cause hypertensive crisis- severe
increase in the BP that may lead to
✓ BROMOCRIPTINE MESYLATE stroke
-more effective than amantadine and - large dose of selegiline, the MAO- B is
anticholinergics inhibited therefore the dopamine will
- not as effective as carbidopa- levodopa in not be catabolized by the MAO-B but
alleviating the symptoms this time the MAO-A will also be
- patients who cannot tolerate carbidopa- inhibited
levodopa are given with the medication
Side Effects NURSING INTERVENTION:
• nausea ✓Patient Teaching
• orthostatic hypotension - urge patients who take high doses of
• palpitation selegiline to avoid foods hign in
• chest pain tyramine such as aged cheese, red
• lower extremity edema wine, cream yoghurt, chocolate,
• nightmares bananas, and raisins to prevent
• delusion hypertensive crisis
• confusion -inform patient that severe drug
interaction may occur between
selegiline and various tricyclic
ASSESMENT, NURSING DIAGNOSIS, PLANNING antidepressant (TCA’s) or selective
- just the same with carbidopa- levodopa serotonin reuptake inhibitors (SSRI’s)
NURSING INTERVENTIONS:
✓ Patient- teaching 5. Catechol-O- methyltransferase (COMT)
- report any signs of skin lesion, seizures inhibitors
or depression Example: entacapone, tolcapone
- advise patients taking bromocriptine to REMEMBER: Dopaminergic neurons have
report symptoms of lightheadedness degenerated so the level of dopamine is
when changing positions decreased, there’s also a possibility that
- warn patients to avoid alcohol when dopamine will be inactivated because of COMT
taking bromocriptine -this enzyme inactivates the dopamine, WE
- teach patients to check their heart rate SHOULD SAVE DOPAMIN so use COMT
and report rate changes or irregularity inhibitors
- counsel patient not to abruptly stop the - entacapone/ tolcapone inhibits or stop COMT
drug w/o first notifying. from inactivating the dopamine
-inhibits COMT enzymes
4. Monoamine Oxidase B (MAO-B) inhibitors -COMT inhibitor + levodopa (increases the
Example: selegiline HCl and Rasagline amount of levodopa concentration in the brain
- inhibit MAO- B= prolongs the action of
levodopa ✓OLCAPONE
- inhibits MAO-B - 1st COMT inhibitor given with levodopa , can
REMEMBER: MAO- B (enzyme) causes affect the liver function ( can cause liver
catabolism or breakdown of dopamine damage)
Nursing Action: need to check the liver enzymes
to determine the liver function of the patient
✓SELEGILINE HCl- can delay the use of - Side effects: dark discoloration of urine,
carbidopa-levodopa by 1 year perspiration may be dark but harmless
REMEMBER: In parkinson’s disease, dopamine
is already depleted because the production is

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PHARMACO- CNS

Side Effects
✓ENTACAPONE • retroperitoneal fibrosis/
- does not affect liver function retropulmonary fibrosis,
- carbidopa- levodopa+ entacapone= provides • left side cardiac valve
greater dosing flexibility and individualization to dysfunction
the patient
REMEMBER: inform patient that urine can have PART 9
brownish orange discoloration DRUGS FOR ALZHEIMER'S DISEASE
- the use of the 2 inhibitors can intensify actions
of levodopa Alzheimer's Disease
-may lead to intense, uncontrollable urges (sex, • incurable dementia illness
gambling and spending money) in addition to • characterized by chronic progressive
suddenly falling asleep neurodegenerative conditions with
- warn patient to avoid driving and other marked cognitive dysfunction
potentially dangerous activities.
• 45 to 65 years of age
PART 8 Theories Related to the changes that cause
Drugs in Motion Alzheimer's Disease
• degeneration of the cholinergic neuron
Acetylcholinesterase Inhibitors and deficiency in acetylcholine
- patients with myasthenia gravis experienced a
• Neuritic plaques that form mainly
decreased ability of muscle movement
outside of the neurons and in the
cerebral cortex
NEUROLOGICAL COMPONENTS:
- nervous system is a group of neurons • Apolipoprotein E4 that promotes
with gaps in between formational plaques which binds the
- electrical signals pass between the gaps beta amyloid in the plaques
in one neuron to the next with the help • Beta-amyloid lipoprotein accumulation
of neurotransmitters in high levels that may contribute to
- when ACETYLCHOLINE binds to the neuronal injury
receptor it opens the receptor and • Presence of neurofibrillary tangles with
allows sodium to enter twists inside the neurons.
- when sodium enters the neuron, its
ionic charge allows electrical signal to Acetylcholinesterase/ Cholinesterase Inhibitor
move from the last neuron to the next - classification of medication that can be
neuron administered to a patient with Alzheimer’s
- with acetylcholine bound to the disease (one of the theories in Alzheimer’s
receptor, electrical signal fires until it disease = there is degeneration of the
reaches the muscle cholinergic neuron and there is deficiency in
- ACETYLCHOLINESTERASE, an enzyme acetylcholine)
that breaks down acetylcholine acetylcholinesterase or cholinesterase –
- breaking ACh will stop it from being breaks down acetylcholine, if this will
able to open the receptor happen, the level of acetylcholine will
- if the receptor remains closed, then the further deplete.
sodium cannot enter and the electrical to prevent such from happening, the
signals cannot be relayed to the next medications acetylcholinesterase or
nerve cholinesterase inhibitor will be administered
- Acetylcholinesterase inhibitors will bind which will then inhibit the cholinesterase and
to reseal cholinesterase and keep them preserve the acetylcholine.
from breaking down to acetylcholine Examples:
- since acetylcholine is not broken down, ✓ Donepazil
it can bind to the receptor and allows ✓ Galantamine
sodium to enter ✓ Memantine
- this allows electrical signal to continue ✓ Rivastagmin
to the next nerve
- with the nerve impulse continuing to its RIVASTIGMINE
destination, the muscles can contract ➢ increases the amount of ACh at the
and relax. cholinergic synapses (acetylcholinesterase
inhibitors increase cognitive functions for
ACETYLCHOLINE INHIBITORS for patients with mild to moderate Alzheimer’s
MYASTHENIA GRAVIS: disease. this medication is absorbed through
- ✓ PYRIDOSTIGMINE the GI tract without food)
➢ given twice a day (has a short half-life, and
the dose is gradually increased)

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PHARMACO- CNS

➢ contraindicated to patients with liver


disease because hepatotoxicity may occur
(cumulative drug effect is likely to occur in older
adults and in patients with liver and renal
dysfunction)

ASSESSMENT
✓Assess the patient’s mental and physical
abilities
✓Obtain a history that includes any liver or
renal disease or dysfunction ❖Because antibodies attack the receptor sites
✓Assess for memory and judgment loss for the acetylcholine, there will be less or
(memory loss, declining interest in people or reduced acetylcholine receptor sites.
home, difficulty in following through with ❖The acetylcholine molecules are prevented
simple activities, and a tendency to wander from binding to the receptors.
from home)
❖The stimulation of normal neuromuscular
✓Observe for signs of behavioral disturbances transmission is inhibited.
(hyperactivity, hostility, and wondering)
❖There is ineffective muscular contraction and
✓Examine the patient for signs of aphasia (or weakness.
difficulty in speech: motor function) Your acetylcholine is important
✓Determine family member’s ability to cope neurotransmitter for your muscles to contract. If
with a patient's mental and physical changes there is a problem with the transmission, later
there will be also a problem in relation to
NURSING DIAGNOSES muscle contraction.
✓Self-care deficit related to memory loss
✓Chronic confusion related to memory loss MANIFESTATIONS
▪ Ptosis
PLANNING ▪ Diplopia
✓Patient’s memory will be ▪ Dysphagia
✓Patient will maintain self-care body functions ▪ Dysarthria
with assistance. ▪ Respiratory Muscle Weakness
INTERVENTIONS (maintain consistency in care) (Problem is not actually primarily on the level of
✓ Assist the patient in ambulation and activity acetylcholine, but the acetylcholine receptor
✓ Monitor for side effects (related to site. However, acetylcholine may also be
continuous use of acetylcholinesterase depleted because of the enzyme
inhibitors) acetylcholinesterase (AChE)/ Cholinesterase.
✓ Record vital signs periodically (note signs of This enzyme is responsible for the breakdown of
bradycardia and hypotension) acetylcholine.
✓ Observe any patient behavioral changes To stop that, Acetylcholinesterase/
(note any improvement or decline) Cholinesterase inhibitor will be administered to
✓ Patient Teaching: inhibit the action of the Acetylcholinesterase or
 Teach family members about safety Cholinesterase. And it will prevent the
measures (removing obstacles in the patient's breakdown of the Acetylcholine. Thus,
path to avoid injury when the patient wanders) preserving acetylcholine (there is more
 Patient should rise slowly to avoid dizziness acetylcholine available to activate the
and loss of balance cholinergic receptors and promote muscle
 Monitor liver function tests (because contraction)
hepatotoxicity is an adverse effect) Example
❖ Neostigmine
EVALUATION ❖ pyridostigmine
• Effectiveness of drug regimen (look if
the manifestations of the patients have Neostigmine (first drug used to manage
improved) myasthenia gravis)
o short-acting Acetylcholinesterase inhibitor
DRUGS FOR MYASTHENIA GRAVIS with a half-life of 0.5 to 1 hour
o the drug must be given on time to prevent
Myasthenia Gravis muscle weakness
• Chronic autoimmune neuromuscular
disease that affects approximately 20 in Pyridostigmine (poorly absorbed from the GI
every 100, 000 people) tract)

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PHARMACO- CNS

o has a short half-life (must be administered If ptosis is immediately corrected after


several times a day) the half-life of oral administration of this drug, the diagnosis is
pyridostigmine is three to seven hours, and it is most likely myasthenia gravis.
two to three hours for iv
o sometimes given every four to six hours IF UNRESPOSIVE TO AChE INHIBITORS:
Prednisone
This medication increases muscle strength. Plasma exchange
Overdosing or underdosing of IV immune globulin
Acetylcholinesterase inhibitors has an effect. Immunosuppressive drugs
 Myasthenic Crisis (underdosage of the
acetylcholinesterase inhibitor) Prednisone
 Cholinergic (overdosage of the ➢drug of choice, it reduces the presence of
acetylcholinesterase inhibitor) antibodies
➢corticosteroids do not produce permanent
Myasthenic Crisis remission
▪ severe complication manifested as
➢long-term side effects are significant
generalized muscle weakness that may involve
Side Effects
the muscles of respiration.
Adverse reactions
▪Triggered by infection, emotional stress, • Nausea
menses, pregnancy, surgery, trauma, • Vomiting
hypokalemia, temperature extremes, and • Diarrhea
alcohol intake • Abdominal Cramps
▪occur three to four hours after taking certain • Increased Salivation
medications (aminoglycosides, phenytoin, • Tearinng
macrolides, fluoroquinolones, quinine, quinidine, • Miosis
lidocaine, magnesium salt, psychotropic • Blurred vision
medications, and neuromuscular blocking • Tachycardia
agents) • Hypotension

Cholinergic Crisis ASSESSMENT


▪accurate exacerbation of symptoms Obtain a drug history (all current medications)
▪usually occurs within 30 to 60 minutes after Observe the patient's drug profile (for
taking anticholinergic drugs possible drug interactions, patients should avoid
▪complication due to continuous depolarization atropine, atropine-like drugs, and muscle
of postsynaptic membranes that creates a relaxants)
neuromuscular blockade Record baseline vital signs
▪patient with cholinergic crisis often has severe Assess patient for signs and symptoms of
muscle weakness that can lead to respiratory myasthenic crisis (muscle weakness with
paralysis and arrest difficulty breathing and swallowing)
▪accompanying symptoms: miosis or abnormal
pupil constriction, sweating, vertigo excessive NURSING DIAGNOSIS
salivation, nausea, vomiting, abdominal ➢Ineffective breathing pattern related to weak
cramping, diarrhea, bradycardia and respiratory muscle
fasciculations or involuntary muscle twitching ➢Activity intolerance related to fatigue

Similar Major Symptoms: severe muscle PLANNING


weakness: Patient’s symptoms of muscle weakness,
Edrophonium = ultra-short acting difficulty in breathing, and difficulty in
cholinesterase inhibitor used to distinguish swallowing caused by MG will be eliminated
between the myasthenic crisis from cholinergic or reduced in 2-3 days
crisis.
✓myasthenic crisis: if the symptoms are NURSING INTERVENTIONS
elevated because of an increase in acetylcholine Monitor effectiveness of drug therapy
✓cholinergic crisis: if the muscle weakness (muscle strength should be increased
becomes more severe – due to drug overdosing both depth and rate of respirations
should be assessed and maintained
EDROPHONIUM within normal range)
o used to diagnose myasthenia gravis Administer prescribed AChE inhibitor
o its ultra-short duration of 5 to 30 minutes following dosage recommendations
increases muscle strength immediately (and nursing guidelines)
Observe patients for signs and
symptoms of cholinergic crisis (caused

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PHARMACO- CNS

by overdosing such as muscle weakness,


respiratory failure, increased salivation, Other Medications for Multiple Sclerosis:
sweating, and bronchial secretions
along with miosis) Alemtuzumab
Have an antidote for cholinergic crisis ✓monoclonal antibody – are laboratory-
ready: ATROPINE SULFATE produced molecules engineered to serve as
Patient Teaching: substitute antibodies that can restore, enhance,
Teach patients to take drugs as ordered or mimic the immune system's attack in cancer
(to avoid recurrence of symptoms) cells.
encourage patients to wear a medical ✓they are designed to bind to antigens that are
ID or necklace that indicates health generally more numerous in the surface of
problem cancer cells than healthy cells
teach patients about side effects corticosteroids
(medication and when to notify the ✓classification of medication that lowers
health care provider. advise patient to inflammation in the body
report recurrence of symptoms of
✓reduce immune system activity
myasthenia gravis to the health care
provider)
Beta-1b and Glatiramer Acetate
inform patients to take the drug before • administered subcutaneously either
meals for best absorption (if gastric once daily or three times a week
irritation occur, take the drug with food) depending on the healthcare provider's
order
EVALUATION
✓Evaluate effectiveness of drug therapy Teriflunomide
✓Determine the absence of respiratory • oral drug
distress • administered daily
✓Evaluate the correct use of drug by
the patient Alemtuzumab
• requires a daily IV dose of 12 mg for five
DRUGS FOR MULTIPLE SCLEROSIS consecutive days and in 12 months, an
Multiple Sclerosis additional 12-mg dose for three
consecutive days
autoimmune disorder that attacks the myelin
sheath of the nerve fibers in the brain and the Corticosteroid
spinal cord which results in the lesions called • used to manage exacerbation of
plaques multiple sclerosis – the condition has
worsened, or there is an increase in the
Although the cause of multiple sclerosis is severity of a disease or its signs and
unknown, disease develops in a genetically symptoms
susceptible person as a result of environmental
exposure like an infection. The onset of multiple PART 10
sclerosis is usually slow. It is a condition in
which there are remissions and exacerbations ANTIPSYCHOTIC AGENTS
of multiple symptoms • Antipsychotic agents are also known as
neuroleptics/psychotropics. But the preferred
common manifestations: motor, sensory, name for this group is either antipsychotics or
neurologic, cerebellar, and emotional neuroleptics.
problems
• The term ‘neuroleptic’ refers to any drug that
Immunomodulators modifies psychotic behavior and exerts an
▪are disease modifying drugs antipsychotic effect.
▪also called as disease modifying therapies
▪and they are the first line of treatment for Psychosis:
patients with multiple sclerosis • Is defined as the loss of contact with reality.
▪disease modifying drugs can slow the • Manifestations, or s/s of psychosis include the
progression of the disease and prevent relapses following:
Examples:
- Difficulty processing information
• beta-interferon
interferon beta- 1a - Disorganized thought
interferon beta- 1b - Distortion of reality
• glatiramer acetate
• teriflunomide - Delusion

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PHARMACO- CNS

- Hallucination • All antipsychotic agents block the D2 or the


dopaminergic receptor which in turn, promotes
- Catatonia the presence of extrapyramidal symptoms.
- Aggressive or violent behavior
• Extrapyramidal symptoms include, shoulda
Schizophrenia: Parkinsonism, akathesia, dystonia, and tardive
• A chronic psychotic disorder is a major dyskinesia.
category of psychosis, in which many of the
mentioned symptoms are manifested. • On the other hand, atypical antipsychotics,
have a weak affinity to D2 receptors.and a
ANTIPSYCHOTIC AGENTS stronger affinity for D4 receptors and they block
(are divided into two categories: ) the serotonin receptor.

• Typical • This agents cause fewer extra pyramidal


- The typical antipsychotic agents are effective symptoms than typical antipsychotic agents
in treating positive symptoms of schizophrenia. which has strong affinity to D2 receptors
- Typical antipsychotic agents have specific TYPICAL ANTIPSYCHOTIC AGENTS:
subclassifications which include:
1. Phenothiazines:
- Phenothiazines:
• Alipathic
-Alipathic= This agents cause fewer extra
pyramidal symptoms than typical antipsychotic - Produce a strong sedative effect, decreased
agents which has strong affinity to D2 receptors blood pressure and may cause moderate
- Piperazine extrapyramidal symptoms (EPS).
- Piperidine DRUG EXAMPLE:
Non-phenothiazines: ✓ Chlorpromazine
✓ hydrochloride (Thorazine)
- Butyrophenones
- Dibenzoxazepines • Piperazine
- Dihydroindolones - Produce more extrapyramidal symptoms
- Thioxanthenes (EPS), dry mouth, urinary retention and
agranulocytosis
• Atypical DRUG EXAMPLE:
- The atypical antipsychotic agents these are ✓ fluphenazine (Prolixin)
effective in treating both the negative and ✓ Perphenazine (Trilafon)
positive symptoms of schizophrenia.
• Examples of medications for the atypical • Piperidine
classification include: - Have a strong sedative effect, a few
- Clozapine (Clozaril) extrapyramidal symptoms (EPS), have a low to
- Olanzapine (Zyprexia) moderate effect on blood pressure and have no
- Risperidone (Risperdal) antiemetic effect.
DRUG EXAMPLE:
- Quetiapine (Seroquel)
✓ thioridazine (Mellaril)
- Ziprasidone (Geodon) - Most antipsychotics can be given orally in a
- Aripiprazole (Abilify) form of tablet or liquid it can also be given
intramuscularly or intravenously.
• Antipsychotic agents block the action of
- For oral use; the liquid form might be
dopamine and thus may be classified as
preferred because some patients may hide
dopaminergic antagonists.
tablets in their cheek or under their tongue to
avoid taking them.
• Specifically, it blocks the dopamine receptors.
- Mouth checks are necessary for non compliant
• there are five subtypes of dopamine receptors patients
numbered as: - Phenothiazine metabolites may cause a
- D1 harmless pink to red brown urine color. The full
- D2 -> antipsychotic agents block this therapeutic effect of oral antipsychotics may
- D3 not be evident for 3-6 weeks following initiation
- D4 of their therapy. But, an observable therapeutic
- D5 response may be apparent after 7-10 days

2. Non-Phenothiazines:
• Butyrophenone

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PHARMACO- CNS

- A frequently prescribed nonphenothiazine - Extra Pyramidal Symptoms


specifically under butyrophenone is: - Pseudoparkinsonism
DRUG EXAMPLE: - Akathisia
✓ Haloperidol (Haldol)
- Dystonia
- Tardive Dyskinesia
- Haloperidol’s pharmacologic behavior is
similar to that of a the phenothiazines it is a
Pseudoparkinsonism
potent antipsychotic drug in which the
is characterized by:
equivalent prescribed dose is smaller than that
of drugs of lower potency. - Stooped posture
- Shuffling gait
- Rigidity
- The drug dose for haloperidol is 0.5-5 - Bradykinesia
milligrams (mg) administration precautions
- Tremors at rest
should be taken to prevent soreness and
- Pill-rolling motion of the hand
inflammation at the injection site that is if, the
medication is administered intramuscularly.
Akathisia
is characterized by:
- Because the medication is a viscous liquid, a - Restless
large gauge needle such as gauge 21, should be - Trouble standing still
used with a Z-track method administration in a - Paces the floor
deep muscle. - Feet in constant motion, rocking back and
forth
- The injection site, should not be massaged and
sites should be rotated these medications
should not remain in a plastic syringe longer
than 15 minutes. Acute Dystonia
is characterized by:
- Take note; this is true if the medication is Facial grimacing
administered intramuscularly. There are also - Involuntary upward eye movement
capsules or tablet forms of haloperidol. - Muscle spasms of the tongue, face, neck,
and back (back muscle spasms cause trunk
• Dibenzoxapine to arch forward)
- This classification of medication has moderate - Laryngeal spasms
sedative and orthostatic hypotensive effects
DRUG EXAMPLE:
✓ Loxapine (Loxitane)
Tardive Dyskinesia
• Dihydroindolone is characterized by:
- This medication has a low sedative and - Protrusion and rolling of the tongue
orthostatic hypotensive effect. - Sucking and smacking movement of the
DRUG EXAMPLE: lips
✓ molindone HCI (Moban) - Chewing motion
- Facial dyskinesia
• Thioxanthene - Involuntary movements of the body and
extremities
- This type of antipsychotic medication
produces a low sedative and orthostatic
Neuroleptics Malignant Syndrome
hypotensive effect
• Is a rare but potentially fatal condition
✓ DRUG EXAMPLE: thiothixene (Navane)
associated with antipsychotic drugs
predisposing factors include:
Side Effects and Adverse Reactions
- Excess agitation
- Dry mouth - Exhaustion
- Increased heart rate - Dehydration
- Urinary retention Neuroleptics S/S
- Constipation - Muscle rigidity
- Decreased blood pressure - Hyperthermia
- Blood dycrasias - Altered mental status
- Photosensitivity - Profuse diapered is
- Blood pressure fluctuation
- Tachycardia

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PHARMACO- CNS

- Dysrhythmia • It is to check the blood sugar level of your


- Seizures patient.
- Rhabdomyolysis • So you see, if you know the adverse effects,
- Acute renal failure and the side effects of the medication, it will
- Respiratory failure guide you again, on what specific nursing
- Coma intervention you’re going to apply.

Treatment of Neuroleptic Malignant DRUG INTERACTIONS


Syndrome: • Phenothiazines decreases the effects of
- Immediate withdrawal antipsychotics anticonvulsants, thus, an adjustment on the
dosage of the anticonvulsant may be necessary.
- Adequate hydration
But take note; it has to be prescribed by the
- Hypothermic blankets physician. So you as a nurse, your responsibility
- Administration of antipyretic here if when the patient has seizure and is
- Benzodiazepines taking an anti-seizure medication is that you
- Muscle relaxant (Such as dendrolene) need to inform the physician right away. So that
the physician can adjust the dosage of the
ATYPICAL ANTIPSYCHOTIC AGENTS medication.
• These are effective in treating both positive • Potentiates the effect of antipsychotic:
and negative symptoms of schizophrenia. alcohol, hypnotics, sedatives, narcotics,
benzodiazepines, and atropine
• These are not likely to cause extrapyramidal
syndrome • Antihypertensives can cause additive
hypotensive effects
• DRUG EXAMPLES:
- NURSING IMPLICATION: you need to
✓ Clozapine (Clozaril) monitor the vital signs of the patient,
✓ Olanzapine (Zyprexia) particularly the blood pressure.
✓ Risperidone (Risperdal)
ASSESSMENT:
✓ Quetiapine (Seroquel) • What would compromise your assessment for
✓ Ziprasidone (Geodon) a patient who is taking a phenothiazine or a
non-phenothiazine medication? Or in general,
✓ Aripiprazole (Abilify)
an antipsychotic?
Common Side effects of Atypical - You must assess baseline vital signs. For use in
Antipsychotic Agents future comparisons.
- Weight gain - Obtain a health history from client of present
- Drowsiness drug therapy. If the patient is taking an
- Unsteady gait anticonvulsant, the drug dose might need to be
- Headache increased because antipsychotics tend to lower
- Insomnia the seizure threshold.
- Depression - You need to assess mental status, cardiac, eye
- Diabetes Mellitus and respiratory disorders before the start of
- Dyslipidemia drug therapy and continue daily assessment.

NURSING DIAGNOSIS:
• Knowing the side effects and the adverse • Ineffective relationship to social withdrawal.
effects of a medication will guide you on what • Risk for loneliness.
specific nursing diagnosis you’re going to
formulate. PLANNING:
• Further,it will also guide you, On what specific • To improve patient’s psychotic behavior with
nursing interventions you’re going to apply. medication, psychotherapy, and adjunct
therapies.
• For example; if the side effect of the
medication is drowsiness, and unsteady Gait,
NURSING INTERVENTIONS:
what nursing intervention should you apply to
• Monitor vital signs because orthostatic
your patient?
hypotension is likely to occur.
• It may include assisting the patient in • Remain with patient while medication is
ambulation, checking your patient from time to taken and swallowed, because some
time especially that your patient will be at risk patients hide antipsychotic medications
for fall. in the mouth to avoid taking them.
• in the case of diabetes mellitus, what nursing • Avoid skin contact with liquid
intervention should you apply? concentrates to prevent contact
dermatitis.

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PHARMACO- CNS

• Administer oral doses with food or milk S/S of severe anxiety attack:
to decrease gastric irritation. • Dyspnea
• Dilute oral solution of Fluphenazine in • Choking
fruit juices, water, or milk avoid apple • Chest pain
juice and caffeinated drinks • Heart palpitation
• Administer medication deep into • Dizziness
muscle because drug irritates fatty • Faintness
tissue. Do not administer intravenously. • Sweating
You also need to check blood pressure, • Trembling
for marked decrease or increase 30 • Shaking
minutes after drug is injected. Do not • Fear of losing control
mix in same syringe, with heparin,
pentobarbital, cimetidine, or diamond • Before giving anxiolytics, non-pharmacologic
hydranate. You also need to observe for measures should be used for decreasing
extrapyramidal symptoms; such as anxiety.
acute dystonia akathesia,
pseudoparkinsonism ,and target • These measures might include:
dyskinesia. You also need to assess for - Relaxation technique
presence of neuroleptic malignant
syndrome. - Psychotherapy
• Record urine output because urinary - Support groups
retention may result.
• Monitor serum glucose level • The medication used to treat anxiety is
• Inform patients that medication may BENZODIAZEPINES.
take 6 weeks or longer to achieve full
clinical effects • Benzodiazepines, has multiple uses; such as
• Caution patients not to consume anticonvulsant, sedative-hypnotic, pre-
alcohol or any other CNS depressants operative drug, substance abuse
such as narcotics because these drugs withdrawal,and anxiolytic.
intensify the depressant effect on the
body. • Most of the benzodiazepines are used mainly
• Teach smoking cessation because for severe or prolonged anxiety.
smoking increases the metabolism of
some antipsychotics. • Examples of benzodiazepines include:
• Guide patients to maintain oral ✓ Chlordiazepoxide
hygiene by frequently brushing and ✓ Diazepam
flossing teeth. ✓ Clorazepate dipotassium
• Instruct pt. To promptly report ✓ Lorazepam
symptoms of EPS ✓ Alprazolam
• Instruct pt. To wear sunglasses, limit
exposure to direct sunlight, and use • The most frequently described
sunscreen benzodiazepine is lorazepam. Many of the
• Suggest lozenges or hard candy if benzodiazepines are used for more than one
mouth dryness occurs purpose.
• Advise patient to rise slowly. From
sitting or lying, to standing to prevent a
sudden decrease in blood pressure ASSESSMENT:
• For a patient who is taking benzodiazepines
EVALUATION: and is experiencing anxiety should be assessed
• Evaluate the effectiveness of the drug for:
and whether the patient has acceptably
- Assess for suicidal ideation obtain a patient’s
reduced psychotic symptoms at the
drug anxiety reaction.
lowest dose possible. Ascertain whether
the patient can cope with everyday - Determine the patient’s support system such
living situations and attend to activities as family, friends, and groups.
of daily living. - Obtain a drug history. Report possible drug to
• Determine whether any side effects or drug interaction.
adverse reactions to the drug have
occurred. NURSING DIAGNOSIS:
• Anxiety related to situational crisis.
ANXIOLYTICS:
• Are primarily used to treat anxiety and
insomnia.
PLANNING:

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PHARMACO- CNS

• Aim to reduce the patient’s anxiety and stress ✓ Monoamine Oxidase Inhibitors
through no pharmacologic method, anxiolytics (MAOIs)
drugs, or support/ group therapy.
1. Tricyclic Antidepressants (TCA):
NURSING INTERVENTIONS: • Are used to treat major depression. This
• Observe patients for side effects recognize blocks the uptake of neurotransmitter
that drug tolerance and physical and norepinephrine and serotonin in the brain.
psychological dependency can occur with most
anxiolytics. • Clinical response is after 2-4 weeks of drug
• Monitor vital signs especially blood pressure therapy. Meaning, that’s the time the patient
and pulse, because orthostatic hypotension will feel the therapeutic effect of the
may occur. medication.
Side Effects and Adverse Reaction
• Encourage family to be supportive to patient - Orthostatic hypotension
• Advise patient not to drive a motor vehicle or - Sedation
operating dangerous equipment when taking - Anticholinergic effects
anxiolytics because sedation is a common side - Cardiotoxicity seizures
effect.
• Warn patient not to consume alcohol or CND • Most common anticholinergic effect is urinary
depressants such as narcotics, while taking retention.
anxiolytics. Drug Examples:
✓ Amitriptyline HCl
• Inform patients that an effective response
✓ Imipramine
may take 1-2 weeks.
✓ Trimipramine
• Advise pt. To rise slowly from sitting to ✓ Doxepin
standing position. To avoid dizziness from ✓ Clomipramine HCl
orthostatic hypotension.
• Alcohol, hypnotics, sedatives, and
EVALUATION: barbiturates Potentiates CNS depression when
• Evaluate the effectiveness of drug therapy. By taken with TCA.
determining whether the patient is less anxious • That is why, it is essential that you educate
and more able to cope with stresses and your patient to avoid this substances or
anxieties. classifications of medications when the patient
• Determine whether the patient is taking the is still taking TCA.
anxiolytic drug as prescribed.
2. Selective Serotonin Reuptake Inhibitors
ANTIDEPRESSANT AGENTS: (SSRIs):
• Antidepressant agents are types of • This group of antidepressants block the
medications that are used to treat clinical reuptake of serotonin in the nerve terminals of
the CNS.
depression, or prevent it from recurring.
• This is used for major depressive disorders.
DEPRESSION: Drug Examples:
• Is the most common mental illness affecting ✓ Fluoxetine
approximately 14.8 million Americans. ✓ Fluovoxamine
✓ Sertraline
• This is characterized primarily by mood
✓ Paroxetine
changes and loss of interest in normal activities.
✓ Citalopram
✓ Escitalopram
TYPES OF DEPRESSION:
• Reactive
• Take note that many SSRI’s have an
• Major depression interaction with grapefruit juice that can lead to
• Bipolar disorder possible toxicity.
•NURSING IMPLICATION: you need to educate
ANTIDEPRESSANT AGENTS ARE DIVIDED INTO your patient to avoid grapefruit juice when
5 GROUPS: taking SSRIs.
✓ Tricyclic antidepressants (TCA) or Side Effects
tricyclics - Dry mouth
✓ Selective Serotonin Reuptake - Blurred vision
Inhibitors (SSRIs) - Insomnia
- Headache
✓ Serotonin Norepinephrine Reuptake - Nervousness
Inhibitors (SNRIs) - Anorexia
✓ Atypical antidepressants - Nausea

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PHARMACO- CNS

- Diarrhea • This is used for mild, reactive, and atypical


- Suicidal ideation depression.
Drug Example:
3. Serotonin Norepinephrine Reuptake ✓ Tranylcypromine sulfate
Inhibitors SNRIs) ✓ Isocarboxazid
• It is called serotonin Norepinephrine reuptake ✓ Selegiline HCl
inhibitors because this group of medication ✓ Phenlzine sulfate
inhibits the reuptake of serotonin and • Take note; that when MAOI is concurrently
norepinephrine. administered with a CNS stimulant (MAOI + CNS
This is used for major depression stimulants or sympathomimetics ->
DRUG EXAMPLES: hypertensive crisis it may result to a
hypertensive crisis
✓ Venlafaxine • Hypertensive crisis: it is a severe increase in
✓ Duloxetine blood pressure that can lead to stroke.
✓ Desvenlafaxine • MAOI +tyramine rich foods -> hypertensive
Side Effects of SNRIS crisis if MAOI is taken and the patient eats
tyramine rich foods, it could also result to
- Drowsiness
hypertensive crisis.
- Dizziness
- Insomnia
- Headache EXAMPLES OF TYRAMINE RICH FOODS:
- Euphoria - Aged cheese
- Amnesia - Cream
- Blurred vision - Yogurt
- Ejaculatory dysfunction - Coffee
- Chocolate
NURSING IMPLICATION: if one of the side
effects is insomnia, the nursing implication is it
- Bananas
is best to administer in the morning. - Raisins
- Italian green beans
Adverse Effects of SNRIS - Liver
- Hypertension - Pickled foods
- Tachycardia - Sausage
- Angiodema
- Seizures
- Soy sauce
- Suicidal ideation - Yeast
- Beer
4. Atypical antidepressants - Red wines
• This is the ‘second-generation’ anti-
depressants. NURSING IMPLICATION: You need to monitor
• This is used for major depression,reactive the blood pressure of the patient.
depression, and anxiety.
Side Effects
• It affects one or two of the three
- Agitation
neurotransmitters which are serotonin
- Restlessness
Norepinephrine, and dopamine.
- Insomnia
- Orthostatic hypotension
Drug Examples:
- Anticholinergic effects
✓ Amoxapine
✓ Nefazodone
✓ Maprotiline MOOD STABILIZERS:
✓ Trazodone • Are used to treat bipolar affective disorder.
• This is a psychological illness,that involves
severe mood swings.
• This group of antidepressants should not be • This mood swings take the form of depression
taken with MAOIs and should not be used or mania, and may last at several months at a
within 14 days after discontinuing MAOIs time.
• During the time of the depression, patients
5.Monoamine Oxidase Inhibitors (MAOIs)
often have a great sadness, guilt,no appetite,
• This group inhibits MAO-A and MAO-B.
poor sleep, and cannot enjoy themselves.
• MAO-A: inactivates dopamine in the brain.
• Mania is the opposite of this, with patients
experiencing erratic, and excited behavior.
• MAO-B: inactivates norepinephrine and
DRUG EXAMPLES:
serotonin.
✓ Lithium

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PHARMACO- CNS

✓ Carbamazepine impulses but also suppress respiration


✓ Valproic acid and coughing.
✓ Divalproex -
✓ Lamotrigine TAKE NOTE: this medication suppress pain
• These drugs are considered as the first impulses and coughing.
line drugs for bipolar disorder.
Side effects and Adverse Reaction
- drowsiness
1. Lithium: - respiratory depression
• Lithium is an inexpensive drug that must be - sedation
closely monitored because it has a narrow - euphoria
therapeutic serum range of 0.8-1.2 mEq/L (ml - hallucination
equivalent per liter) - headache
- palpitation
• Serum lithium levels greater than 1.5 mEq/L - orthostatic hypotension
may produce early signs of toxicity. - physiologic dependence
- urinary retention
• The serum lithium level should be monitored - constipation
by weekly, until the therapeutic level has been
obtained. And then, it must be monitored at - All of these are serious. Thus, the
least 1-2 months on the maintenance dose. nurses should monitor the patient
closely
• Serum sodium levels have to be monitored. - An overdosage of morphine sulfate will
Because lithium tends to deplete sodium. require an antidote:NALOXONE.( In
Side Effects of Lithium general the antidote of opioid analgesic
- Dry mouth overdosage is naloxone).
- Thirst
- Increased urination NURSING ASSESSMENT
- Weight gain (receiving opioid analgesic)
- Bloated feeling
- Metallic taste obtain the medical history - ( contraindication
- Edema on the hands and ankle for morphine sulfate includes severe respiratory
orders, increase intracranial pressure and
severe renal disease. Morphine may cause
CNS 6 seizures.)
If you have a mild headache,or muscle ache, an
over the counter painreliever will usually make Determine the drug history and check for drug
you feel better. But if your pain is more severe, allergies - (report if a drug to drug interaction
your doctor may recommend you with probable.Morphine increases the effects of
something stronger. alcohol, sedatives and hepnotics, antisectory
drugs, and muscle relaxens and it can cause
A prescription opioid or what is called as opioid respiratory depression)
analgesic, these type of analgesic are recotic
type of medications. Assess vital signs - (noting the rate and depth of
respirations as well as pupil size for future
Example of Opioid analgesics are: comparisons because opioid commonly
decrease respiration and systolic blood pressure
and may cause meiosis.
• Morphine Sulfate ( Duramorph)
MEIOSIS- constriction of pupil.
-Suppress pain impulses but also suppress
respiration and coughing.
Monitor urinary output -(because morphine
can cause urinary retention and assess the type
Indication Contraindication
of pain, location, and duration before giving
-Relief of moderate -head injury
opioids.
to severe pain. -shock or very low
-pre-operative blood pressure
NURSING DIAGNOSIS for a patient who will
medication.
receive opioid analgesics:
-as supplement to
-Acute pain related to surgical tissue injury.
anesthesia
-Ineffective breathing pattern related to excess
- This medication can causes placental
morphine dosage.
and blood brain barrier to bind the CNS
optate receptors and inhibits ascending
pain pathway. They suppress pain
PLAN:
-The patient’s pain will be reduced or alleviated.

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PHARMACO- CNS

- for relief of moderate and severe pain


NURSING INTERVENTIONS: - when given IV, dilution of each dose with 5mL
-Administer morphine sulfate before pai sterile water or normal saline solution or NSS is
reaches its peak (to maximizes effectiveness of preferred
the drug) - Direct administration of 2mg or less should be
given over 2-3 minutes and when this
-Monitor vital signs- fewer than 10 respirations/ medication is administered respirations should
min can indicate respiratory distress. (At be monitored closely and adequate hydration
frequent intervals to detect respiratory must be provided.
changes)
Treatment of Migraine Headaches
-Record the patients urine outputs- should be
atleast 600mL/day (because urinary retention Migraine Headache
is the side effect of morphine.) - is characterized by unilateral throbbing head
pain accompanied by nausea, vomiting and
-Check bowel sounds for decrease peristalsis photophobia
(because constipation is the side effect of
morphine. A dietary change or mild daxative For migraine attacks:
may be needed. Opioid Analgesics

-Check for pupil changes and reaction. Take Ergot alkaloids (ex. Dihydroergotamine
note for pinpoint pupils as these indicates mesylate)
morphine overdosage.
Selective serotonin receptor agonists
-have nalaxone available (triptan)
(as an antidote to reverse respiratory
depression if morphine overdose occurs) Example of triptans:
✓ Sumatriptan
-Suggest and encourage patients not to use ✓ Naratriptan
alcohol or CNS depressants with any opioid ✓ Almotriptan
analgesics such as morphine cause respiratory
depression can result, as well as dizziness and - For mild migraine attacks:
the potential of fall risk. ✓ Aspirin
✓ acetaminophen,
- Suggest non-pharmacologic measures to ✓ NSAIDs (ibuprofen and naproxen)
relieve pain as the patient recuperates from
surgery. As recovery progresses a non- opioid Remember:
analgesics may be prescribed. Anti-migraine medication should be taken early
during migraine attack.
-Alert patient that continuous use of morphine
sulfate can be addicting. VID 7
EVALUATION
NONOPIOID ANALGESIC
-Evaluate the effectiveness of morphine in
Such as:
lessening or alleviating pain in using consistent
pain scale. ● Aspirin
-Determine stability of vital signs of the patient ● Acetaminophen
especially the respiration ● Ibuprofen
● Naproxen
• Meperidine -less potent than opted analgesics and are used
- can be given orally, IM, or Iv, routes to treat mild to moderate pain
-Primarily effective in GI procedures
-Preferred during pregnancies because it does
Examples:
not diminished contractions and causes less
neonatal respiratory depression ❖ Nonsteroidal Anti-inflammatory Drugs/
-This is not indicated to patients with chronic NSAID
pain severe liver dysfunction, sickle cell disease ❖ Acetaminophen
history of seizure severe CAD and cardiac
dysrhythmia
*REVIEW*
Inflammation
• Hydromorphone - A response to tissue injury and infection
- is a semi synthetic opioid like morphine 6x - Cardinal signs of inflammation:
more potent than morphine

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PHARMACO- CNS

➔ Redness inflammatory drugs usually inhibit or


➔ Swelling (edema) block both cox-1 and cops2
➔ Heat ▪ inhibition of cox-1 produces the
desirable effect of decreasing plated
➔ Pain
aggregation, but it also has an
➔ Loss of function
undesirable effect of decreasing
protection to the stomach lining;
NSAID (Nonsteroidal anti-
therefore stomach bleeding and ulcers
inflammatory Drug)
may occur with aspirin and ancient
agents.
- Has 4 therapeutic effects based on its
▪ when cox 2 is inhibited pain and fever
name:
are reduced and inflammation is
❖ Anti-inflammatory
suppressed.
❖ Analgesic- can alleviate pain
❖ Antipyretic - used to reduce the TAKE NOTE:
body temperature of a person ▪ take note that this mechanism of action
❖ Anticoagulant- Can decrease or this illustration of the mechanism of
platelet aggregation action of the salicylate or aspirin is the
- 7 groups of NSAID same on the mechanism actions of
1. Salicylates propionic acid derivative, phenyl acetic
2. Para-chlorobenzoic acid acid derivative, fenamates, para-
derivatives, or indoles chlorobenzoic acid derivatives and
3. Phenylacetic acid derivatives oxycams.
4. Propionic acid derivatives ▪ these six groups of nsaids have the
5. Fenamates same mechanism of action in which
6. Oxicams they block or inhibit both cox-1 and
7. Cyclooxygenase-2 (COX-2) cox-2.
Inhibitors
Yellow- 1st gen NSAID
Green- 2nd gen NSAID
1. SALICYLATES
1. SALICYLATES Aspirin
- Derived from Salicylic Acid
- Should not be taken during the last
Drug Examples:
trimester of pregnancy
● Aspirin
● Diflunisal ❖ Because it can cause premature
● Olsalazine sodium closure of the ductus arteriosus
● Sulfasalazine when premature closure of the
ductus arteriosus happens it
ASPIRIN leads to volume overload on
▪ Aspirin and other non-steroidal anti- the fetus, eventually, it will lead
inflammatory drugs relieve pain by to persistent pulmonary
inhibiting your cox 1 or your cyclo hypertension and in some cases
oxygenase 1 as well as cox2 or death.
cyclooxygenase 2 which are needed for
the biosynthesis of prostaglandins - Should not be taken by children with flu

NOTE: take note that the two enzymes cox-1 ❖ Reye Syndrome will develop
and cox-2 serve different purposes ❖ Reye Syndrome is a rare but serious
▪ the cox one is the one that protects the condition that causes swelling in the
stomach lining and regulates blood liver and the brain. It often affects
platelets which promotes blood children and teenagers recovering from
clotting. a viral infection most commonly from
▪ whereas cox2 it is the enzyme that flu and chickenpox.
triggers pain and inflammation at the
injured site non-steroidal anti-

cns
PHARMACO- CNS

-Aspirin overdose/ hypersensitivity s/s:

When aspirin is taken excessively the person 4. PROPIONIC ACID DERIVATIVES


may manifest the following:
Examples:
● Tinnitus (ringing of ears)
▪ Fenoprofen Ca
● Vertigo (dizziness)
▪ Flurbipofen Na
● bronchospasm
▪ Ibuprofen
▪ Ketoprofen
2. PARA-CHLOROBENZOIC ACID ▪ Naproxen
▪ Oxaprozin
Examples:

▪ Indomethacin
NOTICE THAT:
▪ Sulindac
▪ tolmetin ibuprofen is a most commonly prescribed

propionic acid derivative


NOTE:

▪ are used for rheumatoid arthritis gouty


NOTE:
arthritis and osteoarthritis.
▪ take note that indomethacin is very ▪ propionic acid derivatives are aspirin
irritating to the stomach and should be like but have stronger effects and
taken with food creates less GI irritation
▪ this group of non-steroidal anti- ▪ its effect is decreased when taken with
inflammatory drugs may cause sodium aspirin thus the two classifications of
retention and water retention as well medications should not be taken
thus blood pressure may increase together
▪ take note that hypoglycemia may result
when ibuprofen is taken with insulin or
NURSING IMPLICATION:
oral hypoglycemic drug
▪ for this one you need to monitor the ▪ and the risk of toxicity is high when
vital signs of the patient closely taken with calcium channel blocker
particularly the blood pressure

5. FENAMTES

Example:

▪ Meclofenomate sodium monohydrate


3. PHENYL ACETIC ACID DERIVATIVES ▪ mefenamic acid
NOICE THAT:
Examples:
▪ Maybe you have heard of the
▪ diclofenac sodium
mefenamic acid already before as you
▪ ketorolac tromethamine
have taken this one because mefenamic
▪ etodolac
acid is a very common over-the-counter
medication
KETOROLAC

▪is recommended for short-term NOTE:


management of pain
▪ fenamates are used for acute and
▪ for surgical pain it has shown efficacy
chronic arthritic conditions
equal or superior to that of opioid
▪ Gastric irritation is a common side
analgesics
effect for this. Take note if gastric
NOTE: so it means that this medication is very
irritation is a common side effect, then
potent and is very effective in elevating pain you need to encourage the patient to
of the patient take the medication with food
▪ contraindication for fenamates would
be peptic ulcer, because take note

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PHARMACO- CNS

phenomens just like other nsaids except COX- 1


your cox-2 inhibitor will inhibit bothcox-
▪ protects the stomach lining and
1 and cox-2 and
regulates blood platelet to promote
▪ take note the cox-1 will protect the gi
coagulation
lining so if that will be inhibited it may
make he peptic ulcer worse.
COX-2

6. OXICAMS ▪ cox2 it triggers pain and inflammation


and again

is the last group of non-steroidal anti-
inflammatory drugs which inhibits both
cox-1 and cox2. TAKE NOTE:
EXAMPLES:
▪ Both cox-1 and cox-2 are being
▪ Piroxicam inhibited by the first generation non-
▪ Meloxicam steroidal anti-inflammatory drug.
NOTE:

▪ may be used for long-term rheumatoid What happens when cox-1 is blocked?
arthritis or and osteoarthritis
▪ stomach bleeding and ulcer may occur
▪ it can also cause gi problems like
as well as there will be decreased
ulceration and epigastric distress
platelet aggregation
▪ take note that oxycontin should not be
What happens if COX-2 is blocked?
taken with aspirin
▪ pain and fever are reduced
▪ inflammation is suppressed

NOTE:so again, these are the actions of the first


With 1st Generation NSAIDS
generation nonsteroidal, antiinflammatory
other nsis general side effects and adverse drug.
reactions in the intake of first-generation non-
steroidal anti-inflammatory drugs include: now, what about the second generation of the
non-steroidal anti-inflammatory drug?
▪ zits action is it will only block the COX-2.
▪ gastric irritation which is a common so meaning, the cox-2 inhibitor or the
side effect when non-steroidal anti- second generation of the non-steroidal
inflammatory drug is taken without anti-inflammatory drug can reduce pain
food and fever and suppress inflammation
▪ another is sodium and water retention without causing a decrease in platelet
which may increase the blood pressure aggregation as well as stomach bleeding
of the patient. Thus, as a nurse we need and development of ulcer.
to monitor the vital signs of the patient ▪ okay again the second generation of
particularly the blood pressure non-steroidal, anti-inflammatory drug is
▪ take note that gastric irritation may called cox2 inhibitor because again it
also develop due to the intake of will only inhibit or it will only block COX-
alcoholic beverages thus alcoholic 2.
beverages must be avoided. ▪ Thus, it can reduce pain and fever and
suppress inflammation without causing
stomach bleeding or ulcer as well as
decreasing platelet aggregation.
FIRST GENERATION OF NSAIDS

▪ it is comprised by salicylates para 7. COX- 2 INHIBITORS CELECOXIB


chlorobenzoic acid derivatives phenyl ▪ is the only COX-2 inhibitor
acetic acid derivatives propionic acid ▪ Indications:
derivatives fenimates and oxycons and ▪ osteoarthritis
take note that first generation nsaids ▪ rheumatoid arthritis
block both cox-1 and cox-2 ▪ dysmenorrhea

cns
PHARMACO- CNS

▪ moderate to severe pain will not be under treated. thus, we need


▪ ankylosing spondylitis to assess the level of pain accurately.)

Side Effects Nursing Diagnosis:


▪ headache ▪ risk for injury
▪ dizziness ▪ acute pain related to edema from the
▪ sinusitis surgical incision
▪ abdominal pain
▪ nausea Planning:
▪ flatulence ▪ the patient's pain will be relieved or
▪ diarrhea diminished
▪ rash
Nursing interventions:
Adverse Reactions ▪ checking hepatic enzyme tests
▪ peripheral edema ▪ teach patient to keep acetaminophen
▪ bleeding out of children's reach
▪ hypertension ▪ advise patients not to self-medicate
▪ stroke with acetaminophen for more that 10
days
▪ teaching patients to check
acetaminophen dosages on the label of
(another classification of drug that is non-opioid OTC drugs (do not exceed
but still an analgesic is Acetaminophen) recommended dosage which is 4g/day
for adults to avoid hepatic damage)
ACETAMINOPHEN ▪ avoid alcohol ingestion while taking
▪ analgesic and antipyretic drug (used for acetaminophen
muscular aches and pains and for fever ▪ antidote for acetaminophen is
caused by viral infections in infants, Acetylcysteine (antagonist of
children, adults, and older adults. It is a acetaminophen)
popular non-prescription drug which
constitutes 25% of all OTC drugs sold.) Evaluation:
▪ this medication is a non-opioid drug but ▪ evaluate the effectiveness of
not an NSAID. acetaminophen in relieving pain using
▪ causes little to no gastric distress and consistent pain scale (whatever pain
does not interfere with platelet scale you use during the assessment will
aggregation still be the same assessment pain scale
▪ overdosage of acetaminophen can be you're going to use during the
extremely toxic to liver cells; death evaluation phase of the drug therapy)
occur in 1-4 days from hepatic necrosis ▪ determine whether the patient is taking
▪ early symptoms of hepatic damage: the recommended dosage
Nausea, vomiting, diarrhea, and
abdominal pain Anti-inflammatory
1. NSAIDs (nonsteroidal anti-inflammatory
Assessment: drugs) ALREADY DISCUSSED SO WE'LL
▪ obtain a medical history of liver PROCEED TO CORTICOSTEROIDS
dysfunction (because overdosing or 2. corticosteroids
extremely high doses of acetaminophen 3. disease-modifying antirheumatic drugs
can cause hepatotoxicity, hepatic 4. antigout drugs
failure, and death)
▪ ascertain the severity of pain (non-
opioid non-steroidal anti-inflammatory CORTICOSTEROIDS
drugs such as ibuprofen or an opioid ▪ Used as anti-inflammatory agents
may be necessary to relieve pain and ▪ controls inflammation by suppressing or
not acetaminophen because it is very preventing many of the components of
important that the pain of the patient the inflammatory process at the injured
site

cns
PHARMACO- CNS

inhibiting it from binding to interleukin


drug examples: receptors located in cartilage in bone.
▪ prednisolone o Example: Anakinra
▪ prednisone o Tumor necrosis factor (TNF) blockers –
▪ dexamethasone binds to TNF and blocks it from
attaching to the TNF receptors on the
synovial cell surfaces.
CORTICOSTEROIDS o Examples: Etanercept,
Drug Examples: Infliximab, Adalimumab,
▪ Prednisolone Leflunomide
▪ Prednisone Antimalarials :
▪ Dexamethasone o May be used to treat RA when other
methods fail.
NOTE: o The exact mechanism of action in this
▪ Used as anti-inflammatory agents medication is unclear.
▪ Controls inflammation by suppressing o The effect may take 4-12 weeks to
or preventing many of the components become apparent.
of the inflammatory process at the o Used in combination with other NSAIDs
injured site Gout
– is an inflammatory condition that
DISEASE-MODIFYING ANTIRHEUMATIC DRUGS attacks joints, tendons, and other
(DMARDS) tissues.
Includes: – May be called gouty arthritis
o Immunosuppressive agents – Most common side of acute gouty
o Immunomodulators inflammation is at the joint of the big
o Antimalarials toe.
– Characterized by: uric acid metabolism
DMARDs are used for Rheumatoid Arthritis disorder (Increase in urates, uric acid)
(RA), osteoarthritis, psoriatic arthritis, severe and a defect in purine metabolism
psoriasis, ankylosing spondylitis, Crohn’s (Accumulation of uric acid,
disease and ulcerative colitis. hyperuricemia) or an ineffective
clearance of uric acid by the kidneys.
Immunosuppressive agents – are used to treat
refractory rheumatoid arthritis or to arthritis To promote uric acid excretion and to prevent
that does not respond to anti-inflammatory renal calculi:
drugs. o Fluid intake should be increased while
In low doses selected immunosuppressive taking anti gout drugs
agents have been effective in the treatment of o Foods high in purine such as organ
rheumatoid arthritis drugs, such as: meats, sardines, salmon, gravy, herring,
Drug examples: liver, and meat soups as well as alcohol
o Azathioprine especially beer should be avoided.
o Cyclophosphamide o Take note: Alcohol causes both an
o Methotrexate – primarily used to overproduction and under excretion of
suppress cancer growth and uric acid.
proliferation might be used to suppress
the inflammatory process of ANTIGOUT DRUGS:
rheumatoid arthritis when other Anti-inflammatory Gout Drug – acts by
treatment fails. inhibiting the migration of leukocytes to the
inflamed site
Immunomodulators – are used to treat Example: Colchicine
moderate to severe rheumatoid arthritis (RA) by
disrupting the inflammatory process and Uric Acid Biosynthesis Inhibitors – inhibits the
delaying disease progression. final step of uric acid biosynthesis
Immunomodulators: Ex: Allopurinol
o Interleukin-1 or IL1 receptor antagonist
– blocks the activity of interleukin 1 by

cns
PHARMACO- CNS

Uricosurics – increase the rate of uric acid inhibiting uric acid reabsorption. Small
excretion by inhibiting it’s reabsorption doses of colchicine should be given
Ex: Probenecid and Sulfinpyrazone before adding probenecid.
Anti-inflammatory Gout Drug: Colchicine • Should be taken with meals if gastric
Colchicine – inhibits the migration of leukocytes irritation occurs
to the inflamed site.
o It is effective in alleviating acute ANOTHER URICOSURICS: SULFINYRAZONE
symptoms of gout but is not effective Sulfinyrazone – this drug is a metabolite of
for decreasing inflammation that phenylbutazone.
occurs with other inflammatory • More potent than probenecid
disorders. • Should be taken with meals or with
o It does not inhibit uric acid synthesis antacids, to prevent gastric irritation
and does not promote uric acid • Severe blood dyscrasias might occur,
excretion and should not be used if the especially with patients with a history of
patient has severe renal, cardiac, GI blood dyscrasias.
problem. Remember: for patients who experience gouty
o Gastric irritation is a common problem, arthritis is that ASPIRIN SHOULD BE AVOIDED BY
so colchicine should be taken with PATIENTS WITH GOUTY ARTHTRITIS, because
food. With high does nausea, vomiting, this causes uric acid retention
diarrhea or abdominal pain occurs in
approximately 75% of patients taking
this drug.

URIC ACID BIOSYNTHESIS INHIBITORS:


ALLOPURINOL
Allopurinol – is not an anti-inflammatory drug
instead it inhibits the final step of uric acid
biosynthesis and therefore lower serum uric
acid levels, preventing the precipitation of an
attack.
• Frequently used as prophylactic to
prevent gout, a drug choice for patients
with chronic to facetious gout
• Allopurinol is also indicated for gout
patients with renal impairment.
• Useful for patients who have renal
obstructions caused by uric acid stones
and for patients with blood disorders
such as: leukemia and polycythemia
vera
• Also given to patients who do not
respond well to uricosuric drugs such as
probenecid

Uricosurics: Probenecid
Take note: uricosurics increase the rate of uric
acid excretion by inhibiting its absorption
• Probenecid is effective in alleviating
chronic gout
• should not be used during acute attacks
this medication blocks the reabsorption
of uric acid and promotes its excretion.
• Probenecid can be taken with
Colchicine, to begin initial therapy of
relieving symptoms of gout and

cns
 This has two subdivisions:
o Symphatetic nervous
system and
parasympathetic

Autonomic Nervous system

Nervous System

- Is composed of all nerve tissues, the brain,


spinal cord, nerves and ganglia
- The purpose of the nervous system is to  Also called as the visceral system
receive stimuli and transmit information to  Because this acts on smooth muscles and
nerve centers for an appropriate response glands, its functions include control and
regulation of the heart, respiratory system,
2 types of nervous systems: gastrointestinal tract, bladder, eyes and
glands
1. Central nervous system
 Involuntary nervous system over which we
 Interprets information sent by impulse from have little or no control
the peripheral nervous system and returns  There are two sets of neurons of autonomic
the instruction through the peripheral component of the peripheral nervous
nervous system for appropriate cellular system which are the afferent or the
actions sensory neuron and the efferent or the
motor neuron- with 2 pathways.
2. Peripheral Nervous System
1. Afferent or sensory
 Consist of two divisions:  Sends impulse to the cns and
1. Somatic nervous system the efferent neuron receives
 Voluntary and acts on impulses from the brain and
skeletal muscle to produce transmit these impulses
locomotion and respiration through the spinal cord to
2. Autonomic nervous system the effector organ
 Controls and regulate the 2. Efferent or motor
functioning of the heart,  take note that the efferent
respiratory system, pathways in the ANS are
gastrointestinal system and divided into 2 branches:
the glands sympathetic and
 Large nervous system that parasympathetic nerves
functions without our collectively these two
conscious control branches are called the
sympathetic nervous
system and the
parasympathetic nervous
system so take note that
each organ is innervated by
both sympathetic and
parasympathetic nervous
system

A. Sympathetic Nervous System

 also called as the adrenergic system


 norepinephrine is the neurotransmitter that
innervates smooth muscle on the other Drugs affecting Sympathetic Nervous
hand System
 has 4 types of adrenergic receptors on an STIMULATE DEPRESS/BLOCK
organ cell which are: (the adrenergic
1. alpha₁ neruotransmitters)
2. alpha₂ Adrenergic Agonist/ Adrenergic
3. beta ₁ Adrenergics/Sympathomi Antagonists/Adrener
4. beta₂ metics gic
Blockers/Sympathol
B. Parasympathetic Nervous system ytics
 also called as cholinergic system because it
is the neurotransmitter acetylcholine which Adrenergic Agonists
stimulates the receptor cells to produce the
response
 acerylcholine
 has cholinergic receptors at organ cells
which are either nicotinic or muscarinic

Drugs act on sympathetic or parasymphatetic


nervous system by either stimulating or  refers to drugs that stimulate the
depressing responses. sympathetic nervous system
 these drugs are also called adrenergics
or sympathomimetics
 it is called sympathomimetics because it
mimics the neurotransmitters epinephrine
and norepinephrine which act on the four
main receptors of the effector cells
 4 main receptors of effector cells:
1. alpha₁
2. alpha₂
3. beta₁
4. beta₂
 If these neurotransmitters act on the the blood vessels and the smooth muscle of
receptors, a response is produced. gastrointestinal tract for the blood vessels, it leads
to a decrease in vasoconstriction which then leads to
Alpha₁ receptor decreased blood pressure because there is
vasodilation.

For the smooth muscle it leads to the decreased


gastrointestinal tone and motility.

Beta₁ receptor

Alpha₁ receptors are located in the blood vessels in


the eye, the bladder and the prostate. Stimulation of
the alpha-1 receptor in the blood vessel causes
vasoconstriction which leads to increased blood
pressure and increased contractibility of the For the heart:
heart activation of the alpha-1 receptor in the eye  Beta-1 receptors are located primarily in the
leads to mydriasis or pupil dilation for the heart but are also found in the kidneys.
bladder its relaxation, and for the prostate its
 Stimulation of the beta-1 receptor in the
contraction.
heart leads to increased heart contraction
Alpha₂ receptor thus there is increased heart rate.
For the kidneys:
 It increases the renin secretion which leads
to increased angiotensin and later on
increases the blood pressure.

Beta₂ receptors

Unlike alpha-1 receptors which are located on Beta-2 receptors are found mostly in the smooth
specific organs. Alpha-2 receptors are located in the muscle of the gastrointestinal tract, the lungs, in the
post-ganglionic sympathetic nerve endings uterus, and in the liver and the activation of beta-2
receptors in these organs lead to decreased
when stimulated they inhibit the release of
gastrointestinal tone and motility, bronchodilation,
norepinephrine and such change has an effect on
relaxation of the uterine smooth muscle and 3. Mixed-acting
activation of the glycogenolysis which leads to the  The sympathomimetic medication stimulate
increase of blood sugar. the adrenergic receptor sites and also
stimulate the release of the norepinephrine
After the neurotransmitter has performed its from the terminal nerve endings. Again, as
function, the action must be stopped to prevent you can see in the illustration, the D
prolonging the effect and it is possible through represents the sympathomimetic drug so it’s
neurotransmitter inactivation. considered, to be mixed acting and if it will
activate the receptor site and also stimulate
Neurotransmitters are inactivated by: the release of the norepinephrine so that the
1. reuptake of the transmitter back into the norepinephrine can bind on the receptor site
neuron (nerve cell terminal) after stimulating this receptor, a response is
2. enzymatic transformation or degradation produced.
3. Diffussion away from the receptor  Take note that aside from norepinephrine ,
epinephrine and dopamine can also produce
sympathomimetic response.
The mechanism of norepinephrine reuptake plays
a more important role in an activation than does
Catecholamines
the enzymatic action after the reuptake of the
 Chemical structures of a substance,
transmitter in the neuron, the transmitter may be
endogenous or synthetic, that can produce
degraded or reused.
sympathomimetic response
2 enzymes that inactivate norepinephrine: Endogenous Catecholamines: Epinephrine,
1. Monoamine Oxidase – located inside the neuron norepinephrine and dopamine
2. Catechol-O-Methyltransferase (COMT) –
located outside the neuron Examples of Synthetic Catecholamines:
 Isoproterenol
3 categories of sympathomimetic drugs:  Dobutamine

Examples of Noncatecholamines:
 Phenylephrine
 Metaproteronol
 Albuterol

Noncatecholamines
1. Direct- acting  Stimulate the adrenergic receptors and
 If it directly stimulates the adrenergic produce sympathomimetic response
receptor
 For example, in this illustration, this letter D What’s the difference between catecholamines
is the drug. This is the sympathomimetic and noncatecholamines especially the synthetic
drug. This is considered to be direct acting if ones?
this one directly binds or activates the
receptor and then a response is produced.
 The key difference between catecholamines
2. Indirect-acting and non-catecholamines is that
 A sympathomimetic drug is considered to be catecholamines are mainly direct acting
indirect acting if it stimulates the release of adrenergic drugs that have catechol while
norepinephrine from the terminal nerve non-catecholamines can be direct acting,
endings so that the norepinephrine can indirect acting or dual acting adrenergic
activate or stimulate the adrenergic receptor drugs that do not have catechol.
and then once done, a response id produced.
Adrenergic Agonist:  Drug to drug interaction in the administration
1. Pseudoephedrine of epinephrine when epinephrine is
 Stimulates the release of norepinephrine administered concurrently with digoxin
from the nerve terminals and acts directly on cardiac dysrhythmia may occur, the nursing
the alpha-1 and beta-1 receptors intervention for this one is to monitor the
 Over-the-counter drug but controlled patient with the use of ecg or
however this is controlled because this electrocardiogram
medication can be used in the illegal  Beta blockers can antagonize the action of
production of amphetamine and epinephrine
methamphetamine  Tricyclic Antidepressants and Monoamine
 This medication is helpful in relieving nasal Oxidase Inhibitors intensify and prolong
and sinus congestion without rebound epinephrine’s effects
congestion
 Used with caution to people with diabetes It is important to know the side effects and
mellitus because this medication can adverse reactions of epinephrine for us to render
increase blood glucose level the appropriate nursing care.

Contraindications: hypertension, closed-angle Side effects and Adverse Reactions:


glaucoma, bronchitis, emphysema and urinary 1. Hypertension 7.Dizziness
retention 2. Tachycardia 8. Urinary Retention
3. Palpitations 9. Nausea
2. Epinephrine 4. Restlessness 10. Vomiting
 Epinephrine’s action is non-selective which 5. Tremors 11. Dyspnea
means it stimulates more than one 6. Dysrhythmia 12. Pulmonary Edema
adrenergic receptor
 Acts on alpha-1 , beta-1, beta-2 adrenergic
receptor sites  Unlike epinephrine which is non-selective,
 Is frequently used in emergencies to treat albuterol is a selective beta-2 agonist which
anaphylaxis or anaphylactic reaction which means this medication stimulates beta-2
means a life-threatening allergic response receptor sites
 A potent inotropic drug which means this  This medication relaxes bronchial smooth
medication can strengthen the myocardial muscle and promotes bronchodilation thus
contraction this medication is therapeutic to condition
 Administered through / Administration: like asthma
subcutaneous/ly, IM  Again take note: Albuterol is a selective
(intramuscular/ly),IV(intravenous/ly), beta-2 agonist however when administered
inhaled/ inhalation this is not given orally in high doses it can also affect beta-1 and
because it is rapidly metabolized in the remember beta-1 is found in the heart and
gastrointestinal tract and the liver which when beta-1 receptor site is activated it can
results in unstable serum level increase heart rate thus with the
 Increases cardiac output, promotes administration of high doses of albuterol it
vasoconstriction, and systolic blood pressure can also increase the heart rate
elevation, increases heart rate , and  Most common SE of oral/inhalation albuterol;
produces bronchodilation tremors, nervousness and restlessness
 Take note: high doses of epinephrine can  Take note: When albuterol is taken
cause cardiac dysrhythmia thus an concurrently with monoamine oxidase
electrocardiogram monitoring is important inhibitor -> hypertensive crisis may occur
 Can cause renal vasoconstriction which leads  Take note: Beta antagonist or beta blocker
to renal perfusion and output with this being may inhibit the action of albuterol because
said, it is important to monitor the urine albuterol is a beta-2 agonist which is a direct
output of the patient opposite of beta antagonist
Adrenergic Agonists  Determine baseline glucose level.

Patient Problems (In a client who need to receive


Drug Target Indications adrenergic agonists include):
receptor  Hypotension
s  Decreased gas exchange
Epinephrine alpha₁,  Dyspnea
beta₁,  Hypoxemia
beta₂
Epinephrine alpha₁, Hypotensive Planning (Agonists are administered in order to):
HCI beta₁, states,  Patient’s vital signs will be within acceptable
beta₂ bronchoshospas ranges.
m, asthma  Patients will experience therapeutic effects
Norepinephrine alpha₁, Acute by improved blood pressure, breathing
bitartrate beta₁ Hypotension, pattern and cardiac output
cardiogenic and
septic shock Nursing Interventions:
Dopamine HCI alpha₁, Hypotension,  Administer epinephrine 1mg for cardiac
beta₁ Heart Failure, resuscitation; may repeat every 3-5 minutes.
septic and Follow each does with 20-mL saline flush to
cardiogenic shock ensure proper delivery. Normally,
Midodrine HCI alpha₁ Orthostatic epinephrine is administered 1mg IV over 1
hypotension minute or more.
Phenylephrine alpha₁ Sinus and nasal  Monitor IV site frequently when
HCI congestion, administering norepinephrine bitartrate or
hypotension/shoc dopamine this is because extravasation of
k, PSVT, these drugs cause tissue damage and
glaucoma, necrosis within 12 hours. These drugs should
pupillary dilation be diluted sufficiently in IV fluids.
Pseudoephedri alpha₁, Nasal congestion  To administer the antidote, phentolamine
ne HCI alpha₂, mesylate, 5-10 milligrams diluted in 10-15
beta₁ mL of normal saline infiltrated into the area
Albuterol beta₂ for IV extravasation of norepinephrine and
dopamine.
Metaproterenol beta₂ Acute
 Check blood pressure every 3-5 minutes if
sulfate bronchospasm,
alpha-adrenergic agonist is administered IV
asthma and
and monitor ECG.
COPD
 Cold medications by spray or drops must be
Dobutamine beta₁ Heart failure,
administered with the head in upright
HCI cardiogenic shock
position.
and for cardiac
 Encourage patient to have an EpiPen readily
surgery
available at all times and to store in cool,
Terbutaline beta₂ Asthma, COPD,
dark place. Refrigeration of epipen is not
sulfate and prophylaxis
recommended.
and treatment of
 Teach patient and family that EpiPen must be
bronchospasm
used immediately upon the initial occurrence
of difficulty breathing, wheezing,
Adrenergic Agonist hoarseness, hives, itching, or swelling of the
Assessment: lips and tongue.
 Record baseline vital signs for future  Do not use Epipen if particles are pink to
comparisons brown. In the administration of epinephrine
 Determine patient’s health history. through the use of epipen take care to inject
subcutaneously and not intradermally and pressure. Adrenergic agonist are centrally acting
be sure to apply sufficient pressure to or those that activate or stimulate the alpha-2
activate the epipen while holding the device receptors.
in place for 5-10 seconds. The epipen should
be inserted into the outer thigh after the Central – Acting Alpha Agonists
administration, massage the injection site for  These medications are used to control
10 seconds to promote absorption and hypertension
reduce vasoconstriction and tissue irritation.  Take note: That high doses of clonidine and
 Again before using the epipen check for pink methyldopa can cause sodium and water
to round particles of the epinephrine retention; frequently administered with
through this part of the EpiPen diuretics. These medications must not be
abruptly discontinued because rebound
hypertensive crisis may result however that
is less likely to happen with the use of
guanfacine
Examples:
 Clonidine
 Methyldopa
 Guanfacine

Clonidine
 For hypertension / hypertensive medication
 Alpha-2 adrenergic agonist that’s why its
considered a central acting alpha agonist
 Do not administer the epinephrine if  This medication is available in oral tablet or
particles are pink to brown in color. transdermal patch form which is replaced
every 7 days; skin irritation may occur with
Pseudoephedrine this route of aministration.
 Alpha-1 and beta1  This medication is not used if pregnant or the
Epinephrine woman is contemplating of pregnancy
 Alpha-1, beta-1 and bet-2 because clonidine is considered as pregnancy
Albuterol category C which means that this medication
 Beta-2 may pose a risk to the fetus
Alpha-2 receptor is located in the post-ganglionic  This medication may produce bradycardia,
sympathetic nerve ending and when stimulated hypotension, sedation and dry mouth at very
they inhibit the release of norepinephrine which low doses
leads to the decrease in vasoconstriction which
then results in vasodilation and decrease in blood Methyldopa
 Another example of central acting alpha
agonist
 This is used for chronic or pregnancy induced
hypertension.
 This medication must not be used in patients
with impaired liver function.

Side effects and Adverse Reactions:


 Drowsiness
 Dry mouth
 Dizziness
 Slow heart rate (bradycardia)
 Headache
 Nasal congestion
 Nightmares bladder, neck and
 Constipation prostate gland
 Edema Beta₁ Decreases Heart rate,
reduces force of
Adrenergic Antagonist (Adrenergic Blocker) contraction
 Drugs that block the effect of adrenergic Beta₂ Constricts bronchioles,
neurotransmitters contracts uterus;
 Also called as adrenergic blockers or inhibits glycogenolysis
symoatholytics which can decrease
 Most adrenergic antagonost block either the blood glucose
alpha receptor or the beta receptor
 These medications block the effect of Alpha- Adrenergic Antagonist
neurotransmitters either by :  Drugs that block or inhibit a response at the
 Directly occupying the receptors or alpha-adrenergic receptor site
 Indirectly by inhibiting the release of  They are also called adrenergic blocker or
the neurotransmitters norepinephrine alpha blocker and this group of medication
and epinephrine is divided into two subgroups:
1. selective alpha blockers(which
Remember that receptor sites in the adrenergic blocks only the alpha-1)
system are: 2. nonselective alpha blockers
(which blocks both alpha-1 and
Alpha₁ Alpha-adrenergic alpha-2 receptor sites )
antagonist  Can promote vasodilation causing a
Alpha₂ Adrenergic Neuron decrease in blood pressure (promote
Antagonist vasodilation -> dec. BP)
Beta₁ Beta- Adrenergic  If vasodilation is long-standing,
Antagonist hypotension may result (long-standing
Beta₂ Beta- Adrenergic vasodilation -> orthostatic hypotension)
Antagonist  Dizziness may be a symptom of decrease in
blood pressure as blood pressure decreases,
Drugs that block the effect of the adrenergic pulse rate usually increase to compensate
neurotransmitters are collectively called as for the low blood pressure and inadequate
adrenergic antagonists. Those adrenergic blood flow.
antagonists that block alph-1 and alpha-2 are  Alpha antagonist can be used to treat
called alpha-adrenergic antagonists and peripheral vascular disease such as
those that specifically block alpha-2 are called Raynaud disease this is because
adrenergic antagonists. Adrenergic antagonist vasodilation occurs permitting more blood
that block beta-1 and beta -2 are beta – flow to the extremities.
adrenergic antagonist.  Also helpful in decreasing symptoms of
Benign Prostatic Hyperplasia (BPH)
Take note: That the following receptors
Drug Target Indications
happen when alpha-1 receptor site is blocked.
Receptors
Receptor Responses
Phentolamine Alpha₁ Antidote for
Alpha₁ *Vasodilation:
mesylate dopamine,
decreases BP; reflex
dobutamine,
tachycardia might
phenylephrine,
result;
epinephrine,
*mydriasis (dilation of
NE, and
pupils),
catecholamine
*suppresses ejaculation
extravasation
*reduces contraction of
smooth muscle in
Doxazosin Alpha₁ Hypertension
mesylate and BPH
Prazosin HCL Alpha₁ Hypertension
Terazosin Alpha₁ Hypertension
HCI and BPH

Another example of alpha blockers however


these medications are nonselective because
these medications do not only target alpha-1 but
also target beta receptors.

Drug Target Indications


Receptors
 Or the adrenergic antagonists that target
Carvedilol Alpha₁ and Antidote for
beta-1 and beta-2
beta₁ and dopamine,
 These medications are also called as beta
beta₂ dobutamine,
blockers
phenylephrine,
 Decrease heart rate and decrease in blood
epinephrine,
pressure usually follows
NE, and
 Useful in treating mild to moderate
catecholamine
hypertension, angina, heart failure, and
extravasation
myocardial infarction
Labetalol Alpha₁ and Acute/chronic  You need to remember that beta blockers
beta₁ and hypertension should not be abruptly discontinued instead
beta₂ it must be tapered off over 1-2 weeks.
Because if not it can lead to tachycardia,
hypertension myocardial infarction.
2. Beta- Adrenergic Antagonist  Could be selective and non-selective
 Nonselective beta blockers block both beta-
1 (decrease heart rate) and beta-2 (leads to
bronchoconstriction) receptors
 This beta blocker is contraindicated in
asthma also non selective beta blockers are
used with extreme caution in patient with
Chronic Obstructive Pulmonary Disorder
(COPD)
 Remember that electrolyte imbalances such
as hypomagnesemia and hypokalemia
should be corrected before initiating beta
blocker therapy

Drug Examples of Nonselective Beta


Adrenergic Antagonist
 This medications block beta-1 and beta -2
 Bet-2 receptors are mostly located in the
lungs
 Can cause bronchoconstriction

Drug Target Indications


Receptors
Propanol beta₁ and beta Hypertension,
₂ angina, MI,
HF,  Onset of action for oral preparation is 1
dysrhythmia hour, peak time is 2-1 hours and duration of
and migraine action is 24 hrs.
prophylaxis  Effective for once-daily dosing
Nadolol beta₁ and beta Hypertension  Contraindication: Bradycardia, heart block,
₂ and angina cardiogenuc shock, acute heart failure,
Pindolol beta₁ and beta Hypertension asthma and sick sinus syndrome
₂  NSAIDS decrease the hypotensive effect of
Sotalol beta₁ and beta For ventricular atenolol
₂ dysrhythmia,  Hypotension can be potentiated when taken
atrial flutter concurrently with another antihypertensive
and atrial medication
fibrillation  When atenolol is administered concurrently
Timolol beta₁ and beta Hypertension, with atropine or other anticholinergics that
maleate ₂ glaucoma leads to increased absorption of atenolol
treatment, and
for migraine Side effects and adverse reactions:
prophylaxis 1. Bradycardia 7. Cardiac dysrhythmia
2. Hypotension 8. Flushing
Selective Beta – Adrenergic Antagonist 3. Headache 9. Fatigue
 Only target one type of beta receptor 4. Dizziness 10. Erectile dysfunction
5. Cold extremities 11. Depression
Drug Target Indications 6. Bronchospasm
Receptors
Metoprolol beta₁ Hypertension, 3. Adrenergic Neuron Antagonist
tartate angina. HF, and  Adrenergic neuron blockers
acute MI  Block the release of NE from the
Atenolol beta₁ sympathetic terminal neurons
Acebutolol beta₁ Hypertension and  Used to decrease blood pressure
HCI dysrhythmia Ex. Reserpine
Betaxolol beta₁ Hypertension and  Resembles alpha and beta adrenergic
glaucoma blockers
 Reduces the serotonin and catecholamine
Bisoprolol beta₁ Hypertension
transmitters, depletion of which may lead to
fumarate
severe mental depression
Esmolol HCI beta₁ Supraventricular
 Withhold the administration of reserpine if
tachydysrhythmia
heart rate (HR) of the patient is 60
and hypertension
beats/min
 Advise the patient that the therapeutic
Atenolol
effects of adrenergic neuron antagonist may
 Selective beta-1 blocker
not occur for two to three weeks after
 This medication decreases the sympathetic
initiation of therapy
outflow to the periphery and suppresses the
renin- angiotensin- aldosterone system
Autonomic Nervous system
(RAAS) response
1. Sympathetic Nervous System
 Blocks beta-1 receptors -> decreases heart
 Also called as the adrenergic system
rate peripheral vascular resistance, force of
 Norepinephrine
cardiac contraction and cardiac output and
 4 types of adrenergic receptors on organ
reduces both systolic and diastolic blood
cells:
pressure
1. alpha₁
 This medication is available in tablets and in
2. alpha₂
parenteral form for IV administration
3. beta₁
4. beta₂ 2 types of cholinergic receptors:
1. Muscarinic receptors
 (stimulate the smooth muscle and slow
the heart rate)
2. Nicotinic receptors
 (neuromuscular, affects the skeletal
muscles)

2 types of cholinergic agonists:


1. Direct-acting
2. Parsympathetic Nervous System  act on the receptors to activate a tissue
 also called as cholinergic system response
 acetylcholine 2. Indirect acting
 Cholinergic receptors at organ cells:  inhibit the action of the enzyme
nicotinic or muscarinic cholinesterase/ acetylcholinesterase and
 Acetylcholinesterase enzyme may inactivate by forming a chemical complex that
acetylcholine before it reaches allows acetylcholine to persist and attach
to the receptor

Drugs affecting Parasympathetic Nervous


system
STIMULATE DEPRESS/BLOCK
Cholinergic Agonist Cholinergic Antagonist

Cholinergic Agonists
 Drugs that stimulate parasympathetic
nervous system
 Also called as parasympathomimetics
1. Direct-Acting Cholinergic Agonist
 They are called parasympathomimetics
 Many drugs classified as direct-acting
because they mimic the parasympathetic
cholinergic agonists are primarily
neurotransmitter acetylcholine, the
selective to the muscarinic receptors but
neurotransmitter located at the ganglions
are nonspecific because the muscarinic
and the parasympathetic terminal nerve
receptors are located in the smooth
endings is acetylcholine
muscle of the gastrointestinal tract, the
 Stimulate the parasympathetic nervous
genital urinary tract, the glands and the
system by mimicking the parasympathetic
heart.
neurotransmitter acetylcholine
 Drug examples of direct-acting
 This neurotransmitter innervates
cholinergic agonists which acts on the
cholinergic receptors in the organs, tissues
muscarinic receptors:
and glands
o Bethanecol
o Metaclopramide Hydrochloride (HCI)
 What you need to remember in of possible problems in a client who need to receive
administering these medications are the bethanecol include :
following: Patient Problems
o Should be prescribed cautiously to  Urinary Retention
patients with low blood pressure and  Hypotension
chronic obstructive pulmonary
disease or COPD
 Take note: Muscarinic agonists are
contraindicated for patients with intestinal of Planning:
urinary tract obstruction, severe bradycardia  The objective of administering bethanecol
or active asthma such as methanical and to the client is to promote voiding (patient
methylclopramide are contraindicated to will void more frequently after taking
patients with intestinal or urinary tract cholinergic agonists)
obstruction, severe bradycardia or active
asthma Nursing Interventions:
A. Bethanecol That the nurse must carry out an administering
 This medication is direct-acting cholinergic bethanecol will include the following:
agonist  Monitor the vital signs (heart rate, blood
 Acts on the muscarinic receptor pressure decrease when large doses of
 This medication is used in a treatment of cholinergics are taken)
urinary retention and neurogenic bladder  orthostatic hypotension is a side effect of
 Principal use is to promote urination by cholinergic agonists such as mechanical
stimulating the muscarinic cholinergic record fluid intake and output decreased
receptors in the detrusor muscle to contract urinary should be reported because it may
the bladder and produce urine output be related to urinary obstruction
 This medication can also increase peristalsis  Give cholinergic agonists 1 hour before or 2
in the gastrointestinal tract (GIT) and hrs after meals to minimize nausea and
increase gastric emptying time vomiting
 This drug should be taken on an empty  If a patient complains of gastric pain the
stomach 1-2 hours before meals to minimize drug may be given with meals
nausea and vomiting  Check serum amylase, lipase, aspartate
aminotransferase (AST), and bilirubin levels
Side effects and adverse reactions  These laboratory values may increase
1. Hypotension slightly in a patient taking cholinergic
2. Tachycardia agonists
3. Excessive salivation  The nurse must also auscultate breath
4. Increased gastric acid secretion sounds for rails, crackling sounds or rhonchi
5. Abdominal cramps because cholinergic agonists can increase
6. Diarrhea bronchial secretions.
7. bronchospasm  Have (IV) atropine sulfate (0.6 – 1.2 mg)
available as an antidote for cholinergic
Cholinergic Agonist, Direct Acting: Bethanecol overdose
Assessment:  Early signs of overdosing includes flushing,
 Assess baseline vital signs salivation, sweating, nausea and abdominal
 Assess urine output (should be> 1500 cramps
mL/day)  Increase bathing frequency and linen
 Obtain patient history of health problems change when needed because diaphoresis
such as peptic ulcer, urinary obstruction or or excessive perspiration may occur
asthma  Monitor for possible cholinergic crisis of
Cholinergic Agonist such as methanical can which symptoms will include muscular
aggravate symptoms of these conditions examples weakness and increased salivation
Evaluation:  The function of the enzyme cholinesterase is
 Determine effectiveness of the cholinergic to break down acetylcholine into choline and
agonist or anticholinesterase acetic acid.
 A small amount of cholinesterase can break
B. Metoclopramide HCI down a large amount of acetylcholine in a
 Also an example of direct-acting cholinergic short period.
agonist  A cholinesterase inhibitor binds with
 Acts on muscarinic receptor cholinesterase allowing acetylcholine to
 This medication is usually prescribed to activate muscarinic and nicotinic cholinergic
treat gastroparesis, nausea and receptors.
gastroesophageal reflux disease (GERD)  This action permits skeletal muscle
 In low doses, metoclopramide enhances stimulation which increases the force of
gastric motility and thus accelerates gastric muscular contraction because of this action,
emptying time the cholinesterase inhibitors are useful to
increase muscle tone for patients with
Direct-Acting Cholinergic Agonist but this myasthenia gravis by increasing
time acts on nicotinic receptor acetylcholine additional effects occur such as
increase in GI motility bradycardia, miosis, or
Drug examples of these medications: constriction of the pupils, bronchial
 Pilocarpine constriction and increased micturition
 Carbachol
Reversible Cholinesterase Inhibitors
Pilocarpine  Primary use: to treat myasthenia gravis
 Direct-acting cholinergic agonist: eye  This medications are used to produce
 Used to treat glaucoma by relieving pupillary constriction in the treatment of
(intraocular) fluid pressure in the eye and to glaucoma and to increase muscle strength
promote miosis (dilation) in eye surgery and in patients with myasthenia gravis
examinations  Drug effects persist for several hours
 Constricts the pupils of the eyes which leads
to the opening of the Schlemm canal to Drug examples:
promote drainage of aqueous humor Neostigmine
 Oral form of pilocarpine is used to relieve Pyridostigmine bromide
xerostomia (dry mouth) Ambenonium Chloride
Edrophonium Chloride
Indirect Cholinergic Agonists Physostigmine
 Which have an interaction with either – antidote for atropine, for
nicotinic or muscarinic receptors, the anticholinergic toxicity
indirect cholinergic agonists do not act on
cholinergic receptors Contraindications:
 Do not have an interaction on the Asthma
cholinergic receptors Diabetes
 Inhibit or inactivate the enzyme Cardiovascular disease
cholinesterase -> permitting acetylcholine Intestinal/ urinary obstruction
to accumulate at the receptor sites
 This action gives them the name Must be used with Caution:
cholinesterase (CHE) inhibitors or Bradycardia
acetylcholine inhibitors (acetylcholinesterase Peptic ulcer
(AChE) inhibitors ) or anticholinesterase Seizure
o Reversible Dysrhythmia
o Irriversible Side effects:
Hypotension
Bradycardia
Sweating
Hypersalivation
GI distress (can be manifested: anorexia,
nausea, vomiting, abdominal pain, and
diarrhea)

Irreversible Cholinesterase Inhibitors


 Indirect Cholinergic Agonists:
Cholinesterase Inhibitors
 Primary clinical indication : glaucoma
 This medication is used to produce
pupillary constriction.
 Irreversible cholinesterase inhibitors are
potent agents because of their long-
lasting effects
 Take note that pralidoxime chloride –
antidote for irreversible and reversible
cholinesterase inhibitors
NCM 106: Pharmacology

Module 3M: ANS Part 3 → Drug examples:


• Atropine Sulfate
• Scopolamine
CHOLINERGIC Atropine Sulfate
ANTAGONISTS → First derived from a belladonna plant
→ Drugs that inhibit the action of → Atropine sulfate acts on muscarinic
acetylcholine by occupying the receptors and have little effect on
acetylcholine receptors nicotinic receptors except in high doses
→ These medications are also → Atropine sulfate is useful primarily in
pre-operative medication to decrease
called as muscarinic salivary secretions
antagonists, anticholinergics, → This medication also acts as an agent
cholinergic blocking agents, to increase heart rate when bradycardia
antispasmodics, or is present
parasympatholytics → This medication is also used as an
antidote for miscarriage agonist
→ These medications affect the
poisoning caused by overdose of
heart, respiratory tract, GI tract, cholinesterase inhibitor of a muscarinic
urinary bladder, eyes and drug such as bethanechol
exocrine glands → Atropine sulfate blocks acetylcholine
→ Major Responses: by occupying muscarinic receptor
➢ Decrease in GI motility → This medication increases the heart
rate by blocking vagus stimulation and
➢ Decrease salivation promotes dilation of the pupils by
➢ Promote mydriasis paralyzing the iris sphincter
➢ Increase in pulse rate → Two most frequent uses of
→ Other Effects: Atropine Sulfate
➢ Decrease bladder 1. To decrease salivation and
respiratory secretions
contraction (results to
preoperatively
urinary retention) 2. To treat sinus bradycardia by
➢ Decrease rigidity and increasing the heart rate
tremors related to the → Atropine sulfate is also useful
neuromuscular ophthalmically because of its property to
excitement cause mydriasis or dilation of the pupils
→ This medication can also cause
→ NOTE: Anticholinergics and
cycloplegia or paralysis of the
adrenergic agonists produce ciliary muscle of the eye which
many of the same responses are necessary before an eye
→ A cholinergic antagonist can act examination and in the treatment
as an antidote to the toxicity of the iris (iritis) and uveal tract
caused by cholinesterase Common Side Effects:
• Xerostomia (dry mouth)
inhibitors and organophosphate
• Nasal dryness
➢ Organophosphate is an • Blurred vision
example of an irreversible • Tachycardia
cholinesterase inhibitor • Constipation
→ May also block the effect of the • Urinary retention
direct-acting and indirect-acting Other Side Effects and Adverse
parasympathomimetics Reactions:
• Nausea
• Headache
• Dehydration

Yuson, Drea
NCM 106: Pharmacology

• Seizure CHOLINERGIC ANTAGONIST:


• Hypotension or hypertension Antiparkinson
• Photophobia (intolerance to Anticholinergics
bright light) → Affect the CNS by suppressing
• Coma the tremors and muscular rigidity
of parkinsonism but has little
CHOLINERGIC AGONIST, DIRECT
ACTING: ATROPINE effect on mobility and muscle
weakness
Assessment: → As a result, several
Before administering atropine sulfate, anticholinergic drugs were
the nurse must: developed for the treatment of
✓ Assess baseline vital signs
parkinsonism such as (drug
✓ Assess urine output
Patient Problems: examples):
❖ Urinary retention • Trihexyphenidyl
❖ Hypertension hydrochloride (HCl)
Planning: • Biperiden
Atropine sulfate is administered to the
• Benztropine
client in order:
✓ To decrease secretions before Benztropine
surgery
→ Decreases the involuntary and
✓ To increase heart rate will be
diminishes the signs and symptoms of
increased
tremors and muscle rigidity that occur
Nursing Interventions:
with parkinsonism and
✓ Monitor vital signs
pseuoparkinsonism
✓ Determine fluid intake and output
→ Available as oral tablet and as
✓ Assess bowel sounds
parenteral IM and IV injections
✓ Teach patient with narrow-angle
→ NOTE: Alcohol and other CNS
glaucoma to avoid atropine-like
depressants potentiate sedation
drugs
→ Anticholinergics, phenothiazines and
Evaluation:
tricyclic antidepressants may increase
✓ Evaluate response to
the anticholinergic effect
anticholinergic medications
→ Side effects of benztropine are similar
to anticholinergic drugs
Cholinergic Antagonists are also used as
Antiparkinson / Anti-parkinson
medications
CHOLINERGIC ANTAGONIST:
Studies indicate that anticholinergics affect
Motion Sickness
the central nervous system as well as the
parasympathetic nervous system.
→ The effect of anticholinergics on
the CNS benefit patients who are
prone to motion sickness
→ Drug Examples:
(antihistamines)
• Scopolamine
• Dimenhydrinate
• Cyclizine
• Meclizine Hydrochloride
(HCl)
→ Most of the mentioned drugs can
be purchased over-the-counter

Yuson, Drea
NCM 106: Pharmacology

with the exception of


scopolamine
→ NOTE: Cholinergic antagonists
are contraindicated to glaucoma
Scopolamine
→ Available topically as a skin patch;
placed behind the ear
→ Scopolamine is frequently prescribed
for activities such as flying, cruising on
the water and bus for automobile trips
→ Side Effects and Adverse
Reactions:
• Xerostomia
• Drowsiness
• Visual disturbances
• Constipation
• Tachycardia (when taken in
large doses)
• Hypotension
• Dysphagia
• Anhidrosis
• Flushing

Yuson, Drea
Nursing Care of Clients with Drugs related to the Endocrine System, Women and Men’s Health

Mr. Jetier T. Pinote


Gland Hormone Targ Function Testes Testosteron Many Male
et e characteristics
Orga
n
Pineal Secretes Many Responsible for Pituitary Gland
Gland Melatonin the Biological 1. Anterior lobe
clock meaning  Aka adenohypophysis
they regulate  Secretes the ff hormones that target
the sleep and glands and tissues:
wake cycle of a  Growth hormone (GH)
person  Thyroid stimulating hormone (TSH)
Pituita FSH/LH Ovari Both hormones
 Adrenocorticotropic hormone (ACTH)
ry (follicle es regulate the
 Gonadotropins follicle stimulating
Gland stimulating Menstrual
hormone cycle hormone (FSH) & luteinizing hormone
and (LH)
luteinizing
hormone)

ADH Kidne Which is


(antidiuretic ys responsible for
hormone) the fluid
regulation in the
body(Osmoregul
ation)

GH(growth Many Growth &


hormone) division
Growth hormone
Oxytocin Uteru Birth  Regulated by two hypothalamic
s contractions hormones: (1) GH releasing hormone
(somatropin) and (2)GH inhibiting
Prolactin Milk production hormone (somatostatin)
Breas  Are given via SUBQ (subcutaneous) or
t IM (intramuscular) ONLY
tissue  Growth hormone drugs cannot be
Thyroi Thyroxin Liver Metabolic rate given orally because they are
d
inactivated by GI enzymes
Gland
 Should be administered before the
Adren Adrenaline Many Fight or flight
al Cortisol Many anti-stress fusion of epiphyses because they act
Gland only on newly forming bones
Pancr Insulin/gluc Liver Blood sugar  The prolonged use leads to the
eas agon levels increase of blood sugar level this is
Ovarie Estrogen/ Uteru Menstrual cycle because of the antagonization of
s Progesteron s insulin.
e  When we say of growth hormone, this
talks about the deficiency or the
Nursing Care of Clients with Drugs related to the Endocrine System, Women and Men’s Health

Mr. Jetier T. Pinote


decrease level and the increase level or
the extra circulatory growth hormone.

Growth Hormone Analogue


SOMATROPIN
 MOA: stimulates growth of essentially
all tissues of the body mostly the bone
 Drug of choice for a child with growth
failure due to inadequate secretion of
endogenous growth hormone &
dwarfism Growth Hormone Suppressant Drugs
 If a person is deficient with growth  Indications: patients with excess
hormone we will be providing growth secretion of growth hormone,
hormone analogue. gigantism, acromegaly
 Tyrion Lannister, a very famous actor 1. GH receptor antagonist
diagnosed with dwarfism 2. Somatostatin analogues
 Drug example for growth hormone 3. Dopamine agonists
analogue: Somatropin
 Contraindicated to pediatric patients
with Prader-Willi Syndrome, those with
severe respiratory impairment, those
patients taking corticosteroids,
because this inhibits the effect of
somatropin, those patients taking
antidiabetic drugs because your
somatropin enhances the efficacy of
antidiabetic drugs which leads to 1. GH Receptor Antagonist
hypogylycemia Pegvisomant
 Take note: once final height is  MOA: blocks GH receptor site
achieved therapy should be  Side effects (s/e): hyperhydorsis,
discontinued cephalgia, fatigue
 Side effects (s/e): arthralgia,  Adverse effects(a/e): chest pain,
myalgia, peripheral edema, weakness hypertension, elevated hepatic
paresthesia, cephalgia transaminase
 Adverse effects (a/e): seizures,
intracranial hypertension, and
leukemia
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 Growth hormone drugs should not be
given orally however for bromocriptine
mesylate since it does not entirely
focus on the growth hormone and
only has an effect on it that is why
this medication can be given oral
formulation.
 Side effects(s/e): nausea, anorexia,
dyspepsia, serostomia
Growth Hormone Suppressant Drugs  Adverse Effects (a/e):
2. Somatostatin Analogues hypertension, myocardial infarction,
stroke seizure
Lanreotide Acetate
 MOA: prevents pituitary gland secrete
growth hormone
 The effect is dependent on the dose
given
 The dose will be calculated by the
physicians
 Depot formulation (meaning it is a
slow release form of medication to
permit less frequent administration of
medication)
 Last for 28 days after deep
subcutaneous injection
Thyroid-Stmulating Hormone
 For the same reason that this
 MOA: stimulates thyroid gland to
medication is given every 4 weeks.
release T3 (triiodothyronine) and T4
 Side effects(s/e): Diarrhea,
(thyroxine)
abdominal pain, nausea & vomiting,
 Used as diagnostic agent to
constipation, weight loss, and
differentiate between primary and
flatulence
secondary hypothyroidism
 Indicated to patients with thyroid
cancer
 0.9 mg IM (intramuscular) gluteus
maximum, and 2nd dose is given after
24 hrs
 This medication is given to the patient
and then lab works will be done.
Growth Hormone Suppressant Drugs  Primary Hypothyroidism: If there is
an increase of your TSH level.
Dopamine Agonists
 Secondary Hypothyroidism: If
Bromocriptine mesylate
there is still a very low TSH.
 MOA: inhibits the secretion of GH
 This is indicated to patients with
caused by tumor in pituitary gland
thyroid cancer.
 Available in oral formulation
Nursing Care of Clients with Drugs related to the Endocrine System, Women and Men’s Health

Mr. Jetier T. Pinote

Pituitary Gland
2. Posterior Lobe
 Aka neurohypophysis
Secretes the following hormones:
 Antidiuretic hormone(ADH)/
vasopressin
Adrenocorticotropic Hormone  Oxytocin
 A hormone released by pituitary
corticotrophs
 Stimulates the release of
glucocorticoids (cortisol), Antidiuretic Hormone
mineralocorticoids (aldosterone), and  Decrease of your ADH or which with
androgen term as the diabetes insipidus as the
 Secretion follows a diurnal rhythm disorder or the increase of the ADH or
(meaning the secretion is higher in the your SIADH or the syndrome of
morning and decreases throughout the inappropriate antidiuretic hormone or
day) an increase level of your ADH.
1. Cosyntropin Diabetes Insipidus
 A synthetic ACTH  Decreased amount of circulating
 MOA: stimulates production of and Antidiuretic Hormone
release of cortisol, corticosterone, and  Excessive urination which leads to
androgens severe dehydration and electrolyte loss
 Used for diagnostic purposes to  Kidney tubules fail to reabsorb water
differentiate between pituitary and  S/S: Excretion of large amounts of
adrenal cause of adrenal insufficiency dilute urine, polydipsia, dehydration,
 Given via IM (intramuscular) or IV inability to concentrate urine which
(intravenous) routes again is manifested with dilute urine,
 CAUTION: patients receiving diuretics low urine specific gravity
Antidiuretic Hormone Therapy Drugs
since this medication increases
 MOA: promotes water reabsorption from
electrolyte loss the renal tubules
 S/e: Peripheral edema  Contraindication: Patients with renal
 A/e: bradycardia, hypertension, sinus, disease
tachycardia  Drug Ex. Vasopressin, Desmopressin
acetate
1. Desmopressin
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Mr. Jetier T. Pinote


 Administered via oral, or intranasal, or by  S/e: thirst, dry mouth, constipation,
injection IV or Subcutaneous route hyperglycemia, dizziness, weakness
 Given to patients with Hemophilia A or von
Willebrand Disease Type 1
2. Vasopressin Nursing Interventions
 Administered IM or IV and intranasally
 Introduce the release of
adrenocorticotropic hormone which
increases the serum cortisol level
1. Monitor Vital Signs.
3. Demeclocycline
 Increased heart rate and decreased
 MOA: induces nephrogenic Diabetes
Insipidus with side(?) systolic pressure can indicate fluid
 A tetracycline antibiotic volume loss resulting from the
 Given orally decrease of your ADH production with
 Common complaint: photosensitivity less secretion more water is excreted
 S/E: Dental discoloration, enamel decreasing the vascular fluid which
hypoplasia leads to hypoglycemia
 It induce nephrogenic diabetes insipidus 2. Record urinary output.
this only last 5 days starting treatment  Increased output could indicate fluid
usually reversed to 2-6 days following the loss caused by the disease of your
cessation of treatment ADH.
3. Obtain daily weight using the same
Vaptans (Vasopressin Receptor weighing scale and clothing.
Antagonist) 4. Assess abdominal girth.
 MOA: increase serum sodium and free
water clearance
 Contraindicated with patients that have 1. Monitor blood glucose.
hypovolemia because these further  Because hypoglycemia can occur in
decreases the water level in the body high doses of this medication
 Ex. Conivaptan and Tolvaptan 2. Monitor serum electrolyte level
1. Conivaptan
 Contraindication: patients with corn
allergy
 Should be administered IV in large
veins and rotated every 24 hours
 Therefore you need multiple IV site for
this medication.
 Injections site complications: Phlebitis,
pain, edema, pruritus because of the
strong potency of the medication.
 A/e: Orthostatic hypotension,
syncope, hypertension, atrial
fibrillation, electrolyte imbalance
2. Tolvaptan  Secretes the following hormones:
 Given orally  Triiodothyronine (T3)
Nursing Care of Clients with Drugs related to the Endocrine System, Women and Men’s Health

Mr. Jetier T. Pinote


 Thyroxine (T4)
 Calcitonin  A decrease in thyroid hormone
Thyroid drugs secretion
1. Levothyroxine sodium  Causes:
 MOA : increases T4 meaning it also a. Primary – thyroid gland disorder
increases its metabolic rate and its b. Secondary – pituitary gland disorder
oxygen consumption, the utilization which results to lack of TSH secretion
and mobilization of glycogen source c. Tertiary – hypothalamus disorder which
and metabolically is deiodinated to T3 results to lack of TSH secretion
 T3 now acts on the target itself.  (Signs and symptoms) s/s:
 Also considered to be the drug of fatigues, weight gain, feeling cold,
choice (DOC) for replacement therapy itchy and dry skin
for the treatment of primary
hypothyroidism
 Given orally
 Contraindication: Thyrotoxicosis,
mycocardial Infarction

2. Liothyronine Sodium
 A synthetic T3
 Biologic half life of 2.5 days with a rapid
onset of action  Once hypothyroidism is no longer
 Given PO or IV controlled
 Used as a replacement or supplemental  Severe hypothyroidism in adult
treatment for hypothyroidism and as  S/S: Lethargy, apathy, memory
an initial therapy for myxedema this is impairment, emotional changes, slow
because of its short half life speech, edema on the eyelids and face,
 Unlike Levothyroxine, does not need to dry skin, a deep and coarse voice, cold
be deiodinated which increases the intolerance, sloe pulse, constipation,
availability for use by the body tissues weight gain and abnormal menses
3. Desiccated Thyroid  Photo below: Women affected by
 Contains both Levothyroxine and myxedema.
Liothyronine
 Given PO (per orem)
 Used to treat hyperthyroidism due to
thyroid atrophy, hormone deficiency,
goiter
4. Liotrix
 Mixture of Levothyroxine sodium and
Liothyronine, 4:1
 Given PO
Nursing Care of Clients with Drugs related to the Endocrine System, Women and Men’s Health

Mr. Jetier T. Pinote


 Congenital hypothyroidism in children  Euthyroid is achieved in 2 to 4 months
which causes delayed physical and of treatment
mental growth  Preferred due to its lesser side effects
compared to PTU

1. Monitor Vital signs


2. Weigh patient daily using the same
weighing scale and clothing.
3. Instruct patient to take the medication at
 For patients who underwent total
the same time each day.
thyroidectomy or the removal of
4. Monitor for thyroid function before and
the thyroid gland, lifetime treatment
after therapy.
of thyroid medication is observed.
5. Monitor for adverse reactions.
 From the day they were operated until
the last day here on earth they should
be taking the medication.
 This gland secretes parathyroid
hormones or parathormone.
 Regulates serum calcium levels
 Promotes calcium absorption from the
GI tract
 Promotes calcium reabsorption from
the renal tubules
 Activated Vitamin D

Thiourea Derivatives / Thioamides


Propylthiouracil (PTU)
 MOA: block thyroid action reducing
hormones
 Enhances anticoagulant effect when Hypoparathyroidism
taken with warfarin  Decrease functioning of the
parathyroid gland leading to low level
Methimazole of PTH
 10 times more potent than PTU  Causes: Damage to parathyroid gland,
 Given PO hypomagnesemia, hypocalcemia, renal
 Longer half life impairment, diuretic therapy
Nursing Care of Clients with Drugs related to the Endocrine System, Women and Men’s Health

Mr. Jetier T. Pinote


 S/S: Paresthesia, muscle pains,
fatigue, twitching of facial muscles

Calcitriol
 MOA: promotes calcium absorption
from the GI tract and secretion of
calcium from bone to the bloodstream
 Given orally
 Contraindication: Hypersensitivity,
hypercalcemia, hypevitamosis D
 S/e: Fatigue, weakness, somnolence,  MOA: increases bone density
cephalgia, nausea, vomiting, diarrhea,  Used primarily to prevent bone loss
cramps, drowsiness, dizziness, vertigo, and fractures
metallic taste, lethargy, constipation,  Contraindications: patients with fish
xerostomia allergy
 A/e: anorexia, photophobia,  Given IM or SQ
dehydration, cardiac arrhythmias,  S/e: nausea, vomiting dephalgia
decreased libido, hypertension,  A/e: Severe hypocalcemia, Tetany,
sensory disturbances, hypercalciuria, seizure
hypercalcemia, hyperphosphatemia

Cinacalcet
 Increased circulating parathyroid
 MOA: increases the sensitivity of the
hormone
calcium sensing receptors of the cells
 Causes: lung cancer, hyperthyroidism
of the thyroid gland, thereby reducing
 S/s: Enuresis, polydipsia, muscle
PTH
weakness, loss of concentration,
 This action causes a decrease in serum
fatigue, loss of appetite, osteoporosis,
calcium and slow the progression of
bone and joint pain
bone disease
 Used for patient with
hyperparathyroidism due to chronic
renal disease and parathyroid cancer
 Given PO
Nursing Care of Clients with Drugs related to the Endocrine System, Women and Men’s Health

Mr. Jetier T. Pinote

1. Monitor serum calcium level. Normal 8 to


10 mg/dL  Dexamethasone
2.Monitor for hypersensitivity reactions  Given PO, IM or IV
3. Assist activities of daily living.  Given to patients with adrenocortical
4. Instruct patient to adhere to medication insufficiency
regimen.  Betamethasone (PO)
5. Monitor for untorward reactions.  Betamethasone sodium phosphate /
betamethasone acetate susp (IM)

1. Monitor vital signs


2. Weigh patient daily.
3. Obtain Abdominal girth
 Consist of adrenal medulla and adrenal 4. Monitor serum electrolyte level specifically
cortex potassium and sodium.
 Adrenal medulla secretes epinephrine 5. Monitor for glucose level.
and norepinephrine 6. Watch signs and symptoms of hypokalemia
 Adrenal cortex secretes androgen, 7. Avoid abruptly stopping the medication.
estrogen, and steroid hormones: 8. Monitor older adults for signs and
glucocorticoids (cortisol), considered to symptoms of osteoporosis.
be the most potent natural cortisol and 9. Instruct to avoid large crowds and persons
mineralocorticoids (aldosterone), with respiratory infection
promotes sodium retention, potassium
and hydrogen excretion

 Frequently called cortisone  Cortisone Acetate


 Usually ends with the suffix-one - Given with foods
 MOA: suppresses inflammation,  Hydrocortisone cypionate (PO)
humoral immune response and adrenal  Hydrocortisone sodium
function phosphate(IM/IV)
 May be administered: orally,  Hydrocortisone acetate sodium
parenterally, topical and aerosol suspension (IM)
 Used to treat Addison’s disease,
inflammation, allergic reaction,
 A/e: Increased blood glucose, moon
debilitating conditions, autoimmune
face, buffalo hump, decreased
disorders, ulcerative colitis,
extremity size, muscle waisting,
glomerulonephritis, shock, ocular and
edema, sodium and water retention,
vascular inflammation, polyarteritis
hypertension, euphoria or psychosis,
nodosa, hepatitis, organ transplant
thinned skin with purpura, glaucoma,
recipients to prevent organ rejection
peptic ulcers, growth retardation
 For the buffalo hump: this is usually
situated at the nape.
Nursing Care of Clients with Drugs related to the Endocrine System, Women and Men’s Health

Mr. Jetier T. Pinote


 Drug interactions:
- Increases the potency of drugs
taken concurrently, including
aspirin and NSAIDs, thus increasing
the risk of bleeding
- Use of K-wasting diuretic increases
potassium loss

 Administration of glucocorticoid drugs


 Indications: Trauma, surgery,
inflammation, emotional upsets,
anxiety
 When therapy is discontinued, the dose
should be tapered to allow the adrenal
cortex to produce cortisol and other
corticosteroids.
 Abrupt withdrawal of the drug can
result in severe adrenocortical
deficiency.

Fludrocortisone
 MOA: promotes reabsorption of sodium
from the renal tubules
 Given orally with a glucocorticoids
 A/e: fluid overload, hypertension
 Mineralocorticoid deficiency usually
occurs with glucocorticoid deficiency,
called corticosteroid deficiency.
Endocrine System, Women and Men’s 4. Gestation  Is because of
Health al the increasing
Diabetes level of
Diabetes Mellitus progesterone,
cortisol, and
Normally when we eat carbohydrates your
human
body turns into a sugar called your glucose,
placental
and sends that to your blood stream. Your lactogen to
pancreas releases insulin, it is a hormone check her
that helps move glucose from your blood into during the
your cell and then the cell uses that glucose second to third
for energy. trimester.
 The increase of
When you have diabetes and don’t get the the hormones
proper treatment, your body doesn’t use leads to the
insulin like it should. Too much glucose stays inhibition of
in your blood a condition called your high insulin usage.
blood pressure or your hyperglycemia. To
define Diabetes Mellitus simply:
Differentiation of a healthy Type 1 DM
 Chronic Disease of the pancreas that and type 2 DM
results from deficient glucose
metabolism.
 Caused by insulin secretion
insufficiency
 Can’t be cured but, it can be
controlled

Types of Diabetes
1. Type 1
2. Type 2
3. Secondar  Highly
y influenced by
Diabetes the use of Healthy; the moment the body receives the
medications
glucose the pancreas secretes insulin; the
Example:
insulin will now attach itself to the receptor
- With the use of
glucocorticoids sites opening the gates of the cell for the
, cortisol, or glucose to enter.
prednisone. Type 1; the pancreases fails to produce
- With the use of
insulin therefore the cell couldn’t be opened
thiazide
because the insulin is not present, again, the
diuretics,
hydrochlorothi insulin receptor sites open the cell with the
azide and with use of the insulin.
the use of Type 2; There is presence of insulin
epinephrine.
however, there is a defective insulin receptor
site no matter how many insulins are present

M.L.
it could still not open the cell since the Hemoglobin A1c (HbA1c) or
receptor site is defective glycerated hemoglobin test
Description & - Measure the
preparation amount of
glucose
attached to
hemoglobin
- Provides
Type 1 Type 2 average
Also called- Insulin Also called Non- blood
Dependent Insulin Dependent/ glucose level
Diabetes/ Juvenile Adult-Onset over the past
Onset Diabetes Diabetes two to three
months.
The pancreas is For the past 20 Normal - Less than
damaged and years, the type 2 5.7%
doesn’t make DM is more Prediabetes - 5.7 to 6.4%
insulin common in children
Diabetes - 6.5% and
and teens; this is
higher
because more
- Goal for
young people are
diabetic
overweight and
patient:
obese.
<7%
About 90% of the
people diagnosed
with diabetes have Fasting Plasma Glucose (FPG)
type 2 diabetes.
Description & - 8 hours
Pancreas creates preparation fasting is
some insulin bit it’s required
either not enough before the
or your body exam.
doesn’t use it like it - Usually done
should. first thing in
the morning
Insulin resistant- before
when cells don’t breakfast.
respond to insulin. Normal - Less than
100 mg/dl
Milder than type 1 Prediabetes - 100 to 125
but can still cause mg/dl
major health Diabetes - 126 mg/dl or
complication, higher
especially in the tiny
blood vessels of the
Oral Glucose Test (OGTT)
kidneys, eyes and
nerves. Description & - A two hour
preparation test that

M.L.
checks blood - Are modifications of human insulin
sugar levels with alterations in onset and duration
before and of action
two hours - Ex. Insulin lispro & Insulin aspart.
after
drinking a Insulins are currently manufactured
special biosynthetically using recombinant DNA
sweet drink. technology, because before in the past; big
Normal - Less than pancreas tissue were used to extract insulin
140 mg/dl since it is structurally closer to humans.
Prediabetes - 140 to 199
mg/dl Set of terms needed to master when
Diabetes - 200 mg/dl studying about Insulin.

Onset
- The length of time before insulin
Random (Casual) Plasma Glucose
reaches the bloodstream and
Test
begins lowering blood sugar.
Description & - Test blood
Peak
preparation glucose any
- The time during which insulin is at
time of the
maximum strength in terms of
day
lowering blood sugar.
Normal
Duration
Prediabetes - Is how long insulin continuing to
Diabetes - 200 mg/dl lower blood glucose.
and higher

FOUR TYPES OF INSULIN


Insulin 1. Rapid Acting
- MOA: promotes the uptake off 2. Short Acting
glucose, amino acids, and fatty acids 3. Intermediate Acting
and coverts them to substances that 4. Long Acting
are stored in the body cells. Rapid Onset Peak Duration
Insulin is also available in a Commercially Acting
Prepared Insulin Insulin
(clear)
1. Human Insulin Insulin 15-30 30-90 3-5
- Duplicates insulin produced by the lispro mins mins hours
pancreas of the human body. (Humalog)
- Advantage: low incidence of allergic Insulin 10-20 40-50 3-5
effect and insulin resistance aspart mins mins hours
- Ex. Humulin R & Novolin N (Novolog)
Insulin 20-30 55 mins 1-2.5
gluisine mins hours
2. Human Insulin Analogues
(apidra)
Oral 12-15 53 mins 2.5
Inhilation mins hours

M.L.
Insulin Insulin
(Afrezza) glargine 1-1.5 None 24 hours
Should be administered 10 to 15 minutes (Lantus) hours
before meal time Insulin
detemir 1-2 6-8 24 hours
(Levemir) hours hours
Afrezza- is an inhaled insulin, and should Insulin
not be injected. The previously mention deludec 1 hour 12 hours 42 hours
insulins except Afrezza are given (Tresiba)
subcutaneously.

 Rapid is the first type of insulin.


Under rapid insulin we have
Humalog, Apidra and Novolog. Short
acting insulin are your regular
insulins so basically those insulins
Cartridge- Where the load of insulin will be
ending with R.
placed
 Humulin-N ph (Intermediate acting
Short Onset Peak Duration insulin) Long, Levemir and Lantus.
Acting
Insulin
(clear) Mixing of Insulin
Insulin Subcu: Subcu: Subcu: 4-
Regular 30 mins 2.5-5 12 hours Steps to manually mixing Insulin
(Humulin hours 1. Wash hands
R; 2. Gently rotate NPH insulin bottle
Novolin IV: 15 IV: 15 IV: 30-60 3. Wipe off tops of insulin cials with
R) mins mins alcohol swab.
Should be administered 30 to 60 mins before 4. Draw back amount of air into the
meals syringe that equals total dose.
5. Inject Air equal to NPH dose into
Intermediate Onset Peak Duration NPH vial. Remove syringe from
Acting vial taking care not to touch
Insulin needle tip to fluid (example
(cloudy) picture for *36 units*)
Insulin 1-2 4-12 14-24
isophane hours hours hours
(NPH)
(Humulin N;
Novolin N)

Long Onset Peak Duration


Acting
Insulin 6. Inject air equal to regular dose
into regular vial.

M.L.
Note: For the air, you need to inject first the
cloudy then clear; Upon drawing remember
7. Invert regular insulin bottle and
R->N. The regular (R) comes first before the
withdraw regular insulin dose.
NPH (H) or the Intermediate.

8. Without adding more air to NPH


vial, carefully withdraw NPH dose
taking care not to push fluid back
into container as this will
contaminate NPH insulin with
regular insulin. Storage of Insulin

 Should not be placed inside the


freezer, nor under direct sunlight.
 Unopened vials are refrigerated until
needed.
 Unopened vials are refrigerated until
needed.

Insulin Administration
Example 2:  Administered via Subcutaneous route
in the abdominal area. They are
administered in the abdominal area
because they are absorbed faster
than those at other body sites and
have been found to be more
consistent.

M.L.
 Using insulin syringe in a 90-degree 1. 8 day rotation schedule
angle. 2. Insulin be injected daily at a chosen
 Only regular insulin can be injected site for 1 week.
intravenously - 1.5 inches apart
 Increases subcutaneous absorption;
heat and massage. Insulin Syringe
 Slows down absorption; cooling or - injected subcutaneously in a 90-
application of cold packs. degree angle. -disadvantages;
painful, injection site reactions.

- Insulin site should be rotated to Insulin Pen


prevent lipodystrophy - resembles a fountain pen but
contains a disposable needle and
disposable insulin-filled cartridge.
- -injected subcutaneously in a 90-
degree angle.
- allows more simple, accurate, and
convenient delivery than using a vial
syringe.
 Lipodystrophy; this involves your
- Types: prefilled and reusable
lipoatrophy it is depression under
- Capacity: 150-300 units
skin surfaces that primarily affect
women and children Insulin Pumps
 Lipohypertrophy, on the other
hand erase lump or not on skin - used in association with blood
surface that is more common in men, glucose monitoring and carbohydrate
but in general lipodystrophy is caused counting.
by the repeated injection into the - this device has an insulin reservoir
same site. and programming capacity to deliver
continuous rapid-acting insulin in
 To prevent this complication, varying amounts at different times
we have Insulin Rotation throughout a 24-hour period.
Program:
Insulin Jet Injectors
- Shoots insulin without a needle
directly through the skin into the fatty
tissue.
- s/e; stinging, pain, burning, bruising-
since insulin is delivered in high
pressure.

M.L.
result being that the liver rapidly
Insulin Syringe breaks down fat into ketones to
employ as a fuel sources.
- S/s; extreme thirst, polyuria, fruity
breath odor, kussmaul breathing,
rapid and thready pulse, blood
Insulin Jet Injector glucose > 250 mg/dl.

 These are given to patients with


Type 2 diabetes
Insulin Pump Sulfonylureas

MOA: stimulate pancreatic beta


cells to secrete insulin; because of
this, it increases the insulin
receptor cells which increases the
ability of the cell to bind insulin for
Adverse Reactions glucose metabolism.
Insulin Shock  chemically related to sulfonamides
but lack antibacterial activity
- occurs when too much insulin is  Types: 1.) 1st Generation
administered. 2.) 2nd Generation
- -s/s; nervousness, trembling, lack of 1st Generation
coordination, cold and clammy skin, Short acting Sulfonylureas
headache.
- -provide orally or IV Tolbutamide
 Administered PO
Somogyi Effect  s/e: headache, dysgeusia, pyrosis,
hypoglycemia, weight gain,
- a hypoglycemic effect that occurs weakness, dizziness, fatigue,
between 2:00am to 4:00am blurred vision.
- reducing bed time insulin dosage.
- S/s; early morning headache, night Long Acting Sulfonylureas
sweats and nightmares.
Chlopropamide
Dawn Phenomena  administered PO with breakfast
 avoid administering to older adults.
- hyperglycemia on awakening.  Because long half-life and duration
- increase bedtime dose of insulin. of action and its increased risk of
prolonged and serious
Diabetic Ketoacidosis hypoglycemia with symptoms
- occurs when absolute or relative including tachycardia, palpitation,
irritability, headache hypothermia
insulin deficiency inhibits the ability
visual disturbances and lethargy.
of glucose to enter cells for
 Chlorpropamide is sold under
utilization as metabolic fuel, the brand name DIABINESE.

M.L.
 Ex. Metformin
Taken with meals
Does not produce
hypolycemia or
2nd Generation hyperglycemia
 greater hypoglycemic potency Absorbed in the small
than first generation intestine
 longer duration of action and Does not undergo
fewer side effects hepatic metabolicm
 Effective doses are lowered and eliminated
compared to first generation unchanged in the urine
 Less displacement potential Most effective in
from protein binding sites monatherapy
 Contraindicated to patients with Useful to oral
liver or kidney dysfunction antidiabetic resistant
patients if combines
with sulfonylureas
S/e: Dizziness,
headache, flushing,
2ND Generation weakness
Glipizide, Glyburide, Glimepiride
 S/e: Hypoglycemia
 A/e: Aplastic anemia, 2. Alpha-Glucosidase Inhibitors
leukopenia, thrombocytopenia,  MOA: inhibits digestive
weight gain, seizure enzymes in the small intestine
 Ex. Acarbose
Is not absorbed in the
GI tract
Non-sulfonylureas Intended for patients
1. Biguanides who do not achieve
2. Alpha-Glucosidase Inhibitors results with diet
3. Thiazolidenidiones (Insulin  Miglitor
Enhancing Agents) Absorbed in the GI
4. Meglitinides tract
5. Incretin Modifiers/ Dipeptidyl 3. Meglitinides
Peptidase 4 Inhibitors/ Gliptins  MOA: stimulate beta cells to
releaase insulin
 Contraindicared to patients with
liver dysfunction because of a
1. Biguanides possible decreased liver
 MOA: increase binding to metabolism rate
insulin to receptors and Ex. Repaglinide, nateglinide
improved tissue to sensitivity to  S/e: headache, diarrhea, back
insulin pain, dizziness, infection

M.L.
4. Gliptins emptying, modulate appetite by
 MOA: increase the level of inducing satiety
incretin hormones, increase  Administered via SubQ before
insulin secretions, and decrease meals in either abdomen or
glucagon production thigh
 Used as an adjunct therapy  Can be given to patients with
treatment with exercise and diet Type 1 and Type 2 DM
 Ex. Sitagliptin phosphate,  Ex. Pramlintide
linapliptin, aloglipton,  S/e: dizziness, nausea, vomiting
saxagliptin fatigue
 S/e: headache, nasopharyngitis,
arthralgia, peripheral edema
Guidelines:
1. Onset of Diabetes Mellitus at age 40
years or older Glucagon
2. Diagnosis of diabetes within the past  MOA: increases blood glucose
5 years by stimulating glycogenolysis
3. Normal or overweight  Used to treat insulin-induced –
4. Fasting blood sugar of 200 mg/dL or hypoglycemia when other
less means of providing glucose are
5. Fewer than 40 units of insulin not available
required per day  Administered via SubQ, IM and
6. Normal renal and hepatic function IV oroute

Incretin Mimetics/ Glucagon-like


Peptide
 MOA: acts on beta cell to
improve its responsiveness
 Given via subcutaneous route
 NOT SUBSTITUTE FOR INSULIN
 Ex. Exenatide, Liraglutide,
Dulaglatide, Albiglutide
 S/e: Headache, restlessness,
fatigue, GI distress, injection
site reactions
Amylin Analogues
 MOA: suppress glucagon
secretions, slows gastruc

M.L.
NCM 106: Pharmacology

Module 4M: Endocrine System Progestin MOA


(Mechanism of Action)
→ Suppresses the LH surge
WOMEN’S REPRODUCTIVE → Ovulation is prevented when LH
surge is suppressed. Pregnancy will
HEALTH
not occur

Combined Hormonal Progestin Effects


Contraceptives (endometrial changes which
(CHCs) creates a less favorable place for
→ Contains synthetic version of implantation)
❖ Endometrial changes
estrogen and progestin
❖ Creates thick and hostile
→ Causes drug-induced cervical mucus
anovulatory cycles - prevents the sperm to
- A cycle which ovulation swim through and
does not occur survive
→ Can be given orally, ❖ Alters movement of the
transvaginally, transdermally, fallopian tube and cilia
intramuscularly - impeding the
movement of the ovum
Estrogen MOA through the tube
(Mechanism of Action)
→ Inhibits ovulation by preventing
the formation of a dominant follicle Examples of Estrogens:
→ When a dominant follicle does not
mature, estrogen remains at a 1. Esterified Estrogens
consistent level and is unable to 2. Estradiol
reach the peak level needed to
stimulate the luteinizing hormone 3. Conjugated estrogens

Estrogen Effects: 4. Ethinyl Estradiol


❖ Stabilize uterine endometrium Examples of Progestins:
❖ Inhibits proliferation and
secretory changes 1. Norethindrone
❖ Decreases the occurrence of
2. Norethindrone acetate
heavy or irregular bleeding
3. Ethynodiol diacetate
4. Norgestrel
5. Levonorgestrel
6. Desogestrel
7. Norgestimate
8. Drospirenone

Yuson, Drea
NCM 106: Pharmacology

Side Effects Withdrawal Bleeding


❖ Nausea
❖ Vomiting → Aka pseudomenstruation
→ Scheduled monthly to mimic
❖ Menstrual changes
normal 28-day menstrual cycle
❖ Breast tenderness
❖ Malaise Guidelines for Missed Dose
❖ Weight gain (missed taking your CHCs)
One Tablet
Adverse Effects
❖ Breakthrough bleeding ► Take the tablet as soon as the
- Episode of bleeding that missed dose is realized
occurs during the active ► Take the next tablet as
pill cycle of CHC scheduled
❖ Excessive cervical mucus
Two Tablets
formation
❖ Hypertension ► Take 2 tablets as soon as the
CHCs are available in 21 days missed dose is realized 2
tablet pack and 28 days tablet tablets the next day
pack ► Use a back up contraception
→ In the 21-day active box, 21 plan for the rest of the cycle
days active pills that contain Three Tablets
estrogen and progestin are
followed by a seven day pill-free ► Discontinue the present pack
period and allow for withdrawal
→ In a 28-day tablet pack, 21 days bleeding
of active pills are followed by ► Start a new package of tablets
seven days of inert pills or for 7 days after last tablet is
coldure (?) counters taken
→ You can identify there the ► Use another form of
counter pills which is at the contraception until tablets have
bottom part since they are the been taken for 7 contraceptive
only ones that are in color days
green. The active pills are in Ethinyl Estradiol and
color white Norelgestromin Transdermal
→ During the hormone-free Patch
periods or the counter days or → Another example of CHC
the 7-day pill-free for the 21 → It is a weekly form of CHC patch
days tablet pack, this result of given transdermally
the decreased level of estrogen → It delivers 20 mcg of your ethinyl
and progestin which allows estrogen and 150 mcg of your
breakdowns of endometrial norelgestromin every 24 hours or 35
lining. So this is somehow mcg of EE and 150 mcg of N every
called your withdrawal bleeding 24 hours
→ Placed on a clean and dry skin,
once a week for 3 weeks in a row
→ 4th week is patch-free to allow
withdrawal bleeding

Yuson, Drea
NCM 106: Pharmacology

Sites of Patch Application: 3. Once inserted, keep the ring in


❖ Buttocks place as long as checked by your
❖ Abdomen healthcare provider
❖ Upper arm or upper torso → For this case, that should be
left there for 3 weeks

NURSING INTERVENTIONS
1. Monitor vital signs and weight
2. Instruct the client in the
administration of the medication.
Ethinyl Estradiol and Etonogestrel
Transvaginal Contraception → It may take up to 1 week for full
→ In a form of a 2-inch flexible contraceptive effect to occur
indwelling vaginal ring when medication is begun
→ Non-biodegradable, transparent,
3. Assist the client with DM in
colorless
→ Releases 15 mcg of EE (ethinyl monitoring blood glucose level
estradiol) and 120 mcg of E 4. Instruct the client to contact
(etonogestrel) healthcare provider if vaginal bleeding
→ The vaginal ring is placed during
or menstrual irregularities occur or if
the first 5 days of menstruation and
pregnancy is suspected
left in place for 3 weeks and
removed for 1 week to allow 5. Advise the client to use an
withdrawal bleeding alternative method of birth control
when taking antibiotics because these
may decrease absorption of oral
contraceptives
Specific to Contraceptive Patches:
1. Instruct the client to peel away half
of the backing on a patch, apply the
How to Insert the Vaginal Ring: sticky surface to the skin, remove the
other half of the backing, and then
press down on the patch with the palm
for 10 seconds.
2. Encourage the client to change the
patch weekly, using a new location for
1. Hold the ring between your thumb each patch.
and index finger and press the
opposite sides of the ring together. 3. If the patch falls off and remains off
2. Gently push the folded ring up into for less than 24 hours, it can be
the vagina as far as possible. Don’t reapplied if still sticky, or it can be
worry that you will push the ring so replaced with a new patch
that it will not get lost.

Yuson, Drea
NCM 106: Pharmacology

4. If the patch is off for more than 24 Disadvantages:


hours, a new 4-week cycle must be
• Higher incidence of irregular
started immediately.
bleeding and spotting
Specific to Vaginal Ring: • Mood changes
• Depression
1. Instruct client that a back up
contraception is needed during the first • Decreased libido
seven days after the ring is placed. Start Date and Dosing Schedule
When are you supposed to start taking
2. Insert the ring into the middle or
the medications?
upper third of vagina.
3. Instruct the client that the ring First-day Start Method
remains in place during sex, tampon → Initiated on the first day a
use or administration of intravaginal woman experiences bleeding
drugs → Days are counted then
4. If the ring slips out for less than 3 2,3,4,5,6 and so on until the
first-day bleeding begins again
hours, instruct the client to rinse with
→ So, if you started your
lukewarm water and should be
reinserted. menstruation or your bleeding
on September 22, then you will
5. If the ring slips out for more than 3 be taking your pill on
hours, reinsert ring and have an September 22 as well
additional contraceptive for 7 days.
Sunday Start Method
6. Removed rings should be wrapped
→ Starts the tablet or patch on a
in a foil pouch and discarded, not
flushed down the toilet. Sunday after the first day of
menstruation
PROGESTIN CONTRACEPTIVES → If menstruation starts on a
→ Contains only progestin Sunday, the woman starts her
→ Available in oral, intramuscular tablet/patch on that day
(IM), subcutaneous and → It aids a woman in remembering
implantable routes the first days of her
contraception
Advantages:
→ For example, the bleeding
• Relatively safe started on September 17, you
• Easy to use will be taking or applying the
• Spontaneity of sexual patch, taking the tablet and
intercourse but less effective applying the patch on a Sunday
than CHCs on September 19
- since they do not → If the woman starts
suppress the release of contraception later than 5 days
FSH and LH as same as of her menstrual cycle, a
degree as CHCs backup contraception should be
used for 7 days

Yuson, Drea
NCM 106: Pharmacology

Quick Start Method Natural Androgens:


→ Starts on the day the patient ❖ Testosterone Nasal
receives the prescription ❖ Transdermal testosterone patch
regardless where she might be ❖ Testosterone topical gel
in her menstrual cycle ❖ Buccal testosterone
→ Increases adherence and ❖ Testosterone pellet
resolves risk for becoming ❖ Testosterone cypionate
pregnant while waiting for
Synthetic Androgens:
menstruation to start the
contraceptive ❖ Fluoxymesterone
→ So, if you receive your ❖ Methyltestosterone
prescription on September 20,
MOA: binds to androgen receptors,
you will also be staring to take
producing multiple anabolic and
the prescribed medication on
androgenic effects
September 20.
→ If used after the first 5 days of Antiandrogens/Androgen
menstruation, a backup Antagonist
contraception is needed for 7 → Drugs used to treat BPH, advanced
days prostatic cancer, hormonal therapy for
patients with endometriosis
MEN’S REPRODUCTIVE
HEALTH DRUG EXAMPLES:
ANDROGENS
Goserelin Acetate and Leuprolide
→ Male sex hormones
Acetate
→ Control the development and
maintenance of sexual process, → MOA: elevates GnRH
accessory organs, cellular
Ketoconazole
metabolism, and bone & muscle
growth → An antifungal drug but with
→ Used to replace deficient testosterone suppressing
hormones such as your effects
hypogonadism → MOA: inhibits testosterone
release
Side Effects:
→ Given at higher doses 400 mg
Masculine secondary sexual PO q8h as opposed to its 200 to
characteristics: 400 mg daily for the treatment
of fungal infection
❖ Body hair growth
❖ Lowered voice Flutamide,
❖ Muscle growth Bicalutmide/Bicalutamide
❖ Breast tenderness
→ MOA: inhibits receptor sites
❖ Gynecomastia
→ It competes with androgens at
❖ Priapism
receptor sites in the prostate
gland blocking the conversion of
testosterone to
dihydrotestosterone

Yuson, Drea
NCM 106: Pharmacology

→ By doing so, this prevents the Depot Medroxyprogesterone


androgens from stimulating the Acetate (DMPA)
prostate cancer cells to grow [Progestin Contraceptive]
→ Also highly effective, long acting
Spironolactone injectable progestin
→ A weak Potassium-Sparing (K- → MOA: thickens cervical mucus,
thins uterine endometrium,
sparing) diuretics
decreases fallopian tube motility
→ MOA: inhibits androgen
→ Administration Dose: 150 mg/mL
receptor sites deep IM ventral gluteus or deltoid
Finasteride every 1 to 13 weeks
→ Causes anovulation and
→ MOA: Blocks conversion of amenorrhea because it inhibits both
testosterone to FSH and LH secretion
dihydrotestosterone → Higher circulating level than
CHCs and POPs
NURSING INTERVENTIONS
Specific to DMPA:
Progestin Implant
1. Instruct the client that the injection → A single-rod device that contains
site should not be massaged after 68 mg of estonogestrel /
administration. etonogestrel
→ Implanted in the inner side of the
2. Document the injection site and the
upper non-dominant arm
injection site reaction.
→ Should be removed not later than
3. Instruct the client to return within 11 3 years after date of implantation
to 13 weeks. though it may be replaced with a
new implant at the time of removal
→ If the client fails to return after → Contains barium, a radio peak
13 weeks, for example three substance that can help locate the
weeks and one day, pregnancy device on a 2-dimensional
should be ruled out first before radiography ultrasound, MRI and CT
the client receives another scan, may not be effective in women
injection with a BMI greater than 30 or your
obese women
4. Include calcium and vitamin D How Progestin Implant is Placed:
supplements in the diet.
→ Because bone resorption
exceeds bone formation

Yuson, Drea
NCM 106: Pharmacology

Progestin Only Oral Contraceptive


Pills (POPs)
→ Also called minipill
→ MOA:
1. Alters cervical mucus making
it thick and viscous blocking
sperm penetration
2. Interferes endometrial lining
making implantation difficult
3. Decreases fallopian tube
peristalsis slowing down the
transport of ovum
4. Interferes with LH surge
which inhibits ovulation
→ Unlike CHCs, all 28 pills contain
active hormone with 0.35 mg of
norethidone / norethindrone each
→ Should be taken continuously
without a break within a 3-hour
window
→ Because it takes 4 to 6 hours
for progestin to thicken the
cervical mucus to prevent
penetration
→ The duration of the progestin
and cervical mucus lasts for
just 24 hours
→ If the minipill is taken more
than 3 hours late, a back-up
contraceptive method should
be used for 48 hours

GUIDELINES FOR MISSED DOSE:


One or More Tablets
❖ Take the tablet as soon as
the missed dose is realized,
and follow with the next tablet
at a regular time
❖ Use a backup method of
contraception for 48 hours

Yuson, Drea
5M- NURSING CARE OF CLIENTS WITH DRUGS PEPTIC ULCER
RELATED TO THE DIGESTIVE SYSTEM ▪ Another digestive problem when there
Mr. Jetier T. Pinote is a hypersecretion of hydrochloric acid
and pepsin, which later one erode the
Nausea and Vomiting GI mucosal lining this is your PEPTIC
▪ An area in your brain called the medulla ULCER.
oblongata where we find the vomiting
center. Now, close to the vomiting
center is the Chemoreceptor Trigger NURSING PROBLEMS
Zone (CTZ). 1. Nausea
2. Diarrhea
Vomiting center and CTZ- 3. Constipation
▪ both are responsible for vomiting. 4. Risk for Deficient Fluid Volume
5. Pain
The CTZ 6. Imbalanced Nutrition: Less than Body
▪ Receive most of the impulses of the Requirements
drugs, toxins, and the vestibular center 7. Anxiety
in your ear and transmits them in to the 8. Deficient Knowledge
vomiting center.

Dopamine DIGESTIVE SYSTEM DRUGS


▪ a neurotransmitter 1. Antiemetics
▪ stimulates the CTZ which in turn ▪ from word itself "anti" which means
stimulates the vomiting center, which opposing or contrary
now causes your VOMITING. ▪ "emetics" which means vomiting
▪ these are drugs used to prevent and
treat nausea, vomiting, vertigo, and
DIARRHEA motion sickness.
▪ The moment your GI is exposed to a ▪ NOTE: Antiemetics are not
bacteria or a virus, this disrupts the recommended during pregnancy,
epithelium of the intestine including the however, if the vomiting worsen and
absorptive epithelium. threatens the well-being of the mother,
▪ Because of this disruption, the water thus TRIMETHOBENZAMIDE (Tigan) is
cannot be absorbed effectively by the given.
system leading to diarrhea.
TRIMETHOBENZAMIDE(Tigan)
Diarrhea ▪ Although, this drug if classified as
▪ defined as loose, watery stool and pregnancy category C
possibly more frequent bowel
movements. 2 MAJOR CLASSIFICATION UNDER
NOTE: The opposite of diarrhea is constipation. ANTIEMETICS
1. No prescription/ OTC
2. Prescription
CONSTIPATION
▪ accumulation of hard fecal material in
the large intestine.

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
NONPRESCRIPTION ANTIEMETICS NON PRESCRIPTION ANTIEMETIC: Bismuth
1. Antihistamine Subsalicylate (Pepto Bismol)
2. Bismuth Subsalicylate ▪ act directly on the gastric mucosa to
3. Phosphorated Carbohydrate Solution suppress vomiting
▪ marketed in liquid and chewable tablet
forms and can be taken for gastric
PRESCRIPTION ANTIEMETICS discomfort or diarrhea.
1. Antihistamine
2. Dopamine Antagonist NON PRESCRIPTION ANTIEMETIC: Phosporated
3. Benzodiazepines Carbohydrate Solution (Emetrol)
4. Serotonin Antagonists ▪ act by changing the pH of the stomach
5. Glucocorticoids and it also decreases it's smooth muscle
6. Cannabinoids contraction.
7. Miscellaneous Antiemetics ▪ it's effectiveness as an antiemetic has
not been verified.
1. ANTIHISTAMINE
▪ Moa: Block h1 receptor sites, therefore NOTE: Patients with Diabetes Miletus should
inhibiting the stimulation of CTZ and the avoid this drug because of its high sugar
vestibular pathways. content.
▪ can be OTC or prescribed medication
▪ NOTE: More or less your
nonprescription and your prescribed PRESCRIPTION ANTIEMETICS: Antihistamines
antihistamines have the same ▪ acts with the same mechanism of action
mechanism of action but they differ on with the nonprescribed antihistamine.
how they regulated with regard to their ▪ this type of antihistamine is used for
length of treatment, side and adverse postoperative nausea and vomiting, and
effects. vertigo.
EXAMPLES:
NONPRESCRIPTION ANTIEMETICS 1. Hydroxyzine (Vistaril)
▪ frequently used to prevent motion 2. Promethazine (Phenergan)
sickness but have minimal effects on
controlling the severe vomiting ▪ administer preoperatively with
resulting from anticancer agents, NARCOTICS to decrease nausea
radiation and toxins. ▪ give hydroxyzine intramuscular
EXAMPLES:
1. Cyclizine HCL (Marexine) SIDE EFFECTS OF ANTIHISTAMINE
2. Dimenhydrinate (Dramamine) 1. drowsiness
3. Meclizine HCL (Antivert) 2. Dry mouth
3. Blurred vision
NOTE: 4. Constipation
▪ Administer these drugs 30-60 minutes 5. Hypertension
before the travel because these drug 6. Transient leukopenia
are not effective in motion sickness if 7. Urinary retention
this is taken after vomiting has 8. Photosensitivity
occurred.
▪ These drugs should be taken after
meals

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
Anticholinergics Promethazine (Phenergan)
Chlorpromazine (Thorazine)
MOA: Act primarily on the vomiting center of
the brain and also act by decreasing stimulation
of the CTZ and vestibular pathways.
 BUTYROPHENONE
Scopolamine (Transderm-Scop) MOA: Blocks the dopamine2 receptors
in the CTZ.
- 3 days efficacy
- Used in prevention of nausea and
- Apply behind ear at least 4 hours before
vomiting during surgical and diagnostic
antiemetic effect is required.
procedures.
- Alternate ears if using for longer than 3
days DRUG EXAMPLES:
- Wash hands after applying patch
Droperidol (Inapsine)
- Apply no more than one patch at a
Haloperidol (Haldol)
time.

Dopamine Antagonists

MOA: Block dopamine 2 receptors in the CTZ  Benzodiazepines


leading to the suppression of vomiting. - For prevention of nausea and vomiting
resulting from cancer chemotherapy.
CATEGORIES: - Administered together with
METOCLOPRAMIDE
PHENOTHIAZINES
DRUG EXAMPLES:
BUTYROPHENONES
LORAZEPAM (ATIVAN)
BENZODIAZEPINES
- This effectively provides emesis control,
sedation, anxiety reduction, and
 PHENOTHIAZINES amnesia.
MOA: Inhibition of the Chemoreceptor DID YOU NOTICE: DOPAMINE ANTAGONIST
trigger zone (CTZ). INVOLVED ANTIPSYCHOTICS?
2 USES: 1. Phenothiazines
PRIMARY- treatment of severe nausea and 2. Butyrophenones
vomiting ANXIOLYTICS
SECONDARY: Reduce anxiety, tension and 1. Benzodiazepines
for psychosis. - These drugs act primarily on the brain
- When phenothiazine is prescribed for which also has an effect on the
vomiting, the dosage is usually smaller dopamine activity. However, In the
than when use for psychiatric disorders. discussion we are more focus on the
ANTIEMETIC effects of each drug
DRUG EXAMPLES: classification
Prochlorperazine Maleate (Compazine)

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
ADVERSE EFFECT OF DOPAMINE ANTAGONIST: SEROTONIN (5-HT3) RECEPTOR ANTAGONISTS

SPECIFICALLY ON TYPICAL ANTIPSYCHOTIC: MOA: Block the serotonin receptors in the CTZ;
block afferent vagal nerve terminals in the
- ( EPS) Extrapyramidal Symptoms upper GI tract. Therefore, it cannot send signals
- Antiemetic doses, ex. Phenothiazines to the brain which causes vomiting.
and butyrophenones relatively DOES
NOT CAUSE EPS. However, is use for - Most effective of all antiemetics in
suppressing nausea and vomiting
extended time, this may now result to
caused by cancer chemotherapy.
EPS
- Drug usually end with suffix -setron
EXTRAPYRAMIDAL SYMPTOMS (DRUG
DRUG EXAMPLES:
INDUCED MOVEMENT DISORDER)
ONDANSETRON (ZOFRAN)
Involves: GRANISETRON (KYTRIL)
Dystonia – continuous spasm and DOLASETRON (ANZEMET)
muscle contraction. These movements PALONOSETRON (ALOXI)
are often repetitive and might include
- These drugs don’t block the dopamine
eye spasm or blinking, twisting head,
receptors. Therefore, they DO NOT
protruding tongue, and extended neck CAUSE EPS.
among others.

Akathisia- May manifest motor Side Effects


restlessness. Patient might twitch their Headache
legs, rocking of their feet or rubbing Diarrhea
their face. Dizziness
Fatigue
Parkinsonism- Symptoms that are
similar to those of Parkinson’s disease.
For oral and IV route
Such as rigidity.
- Administer 30-60 BEFORE
Tardive Dyskinesia- Irregular jerky chemotherapy (ORAL OR IV) and 12
movements. Involves repetitive hours AFTER chemotherapy
involuntary facial movements, such as
tongue twisting, chewing motions, lip
smacking, cheek puffing , and grimacing Glucocorticoids (corticosteroids)

- CNS EFFECTS - Suppress emesis associated with cancer


- Includes: restlessness, weakness, chemotherapy with MINIMIZED SIDE
agitation, EFFECTS because they are administered
- HYPOTENSION only for a short while via IV route.

DRUG EXAMPLES:

DEXAMETHASONE (DECADRON)
METHYLPREDNISOLONE (SOLUMEDROL)

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
CANNABINOIDS xiii. Orthostatic
hypotension/hypertensi
- Act as agonist antiemetics via the on
activation of cannabinoid receptors in xiv. Psychologic problems
both the brainstem and the Enteric are really common
Nervous System.
- For Alleviation of nausea and vomiting
resulting from cancer treatment Miscellaneous antiemetics

CANNABINOIDS - Called as such because they do not act


as strictly as antihistamines,
- Acts as agonist antiemetics via the anticholinergics or phenothiazines
activation of cannabinoid receptors in - MOA – suppress impulses to the CTZ
both the brainstem and the enteric and inhibiting impulses to the vestibul
nervous system area
- Alleviation of nausea and vomiting from - Drugs
cancer treatment o Diphenidol (Ventrol)
- When antiemetics fail, this is prescribed o Trimethobenzamide (Tigan)
to people receiving therapy o Aprepitant (Emened)
- Last resort of antiemetic because this is o Metoclopramide HCl (Regland)
highly addictive
Examples
Metoclopramide HCl
1. Dronabinol (Marinol) CSS III
a. Administer before and for 24 - MOA – blocks dopamine receptors in
hours after chemotherapy the CTZ
b. Make sure patient s not - Used in the treatment of postoperative
suffering from any psychiatric emesis, cancer chemotherapy, and
disorder radiation therapy
i. Because SE are on the - High doses → sedation and diarrhea
CNS affectations → will - Contraindications – pts with GI
worsen if person has obstruction, hemorrhage, proliferation
psychiatric disorder
c. Side effects Side/Adverse effects
i. Mood changes
ii. Euphoria - Drowsiness
iii. Drowsiness - Anticholinergic symptoms
iv. Dizziness - Hypotension
v. Headaches - Diarrhea
vi. Depersonalization - EPS
vii. Nightmares
viii. Confusion Instruct the patients to avoid alcohol and CNS depressant
ix. Incoordination → these will interfere the drug action and potency →
x. Memory lapse severe AE
xi. Dry mouth
xii. Tachycardia

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
EMETICS ANTIDIARRHEALS

- MOA – induce vomiting by stimulating - Treats diarrhea and decreasing


the CTZ in the medulla and acting hypermotility (increased peristalsis)
directly on the gastric mucosa - Should not be used for more than 2
o Putting back part of throat – days and if ever is present (as this might
can induce vomiting not be just simple diarrhea, but a
- Why do we induce vomiting? symptom of another GI disease)
o This is for patients who aspired - Categorized as
a poisonous substance that we o Opiates and opiate-related
have to extract through agents
vomiting o Adsorbents
- Applicable if aspired substance is non-
corrosive
o Since the action of emetic OPIATES AND OPIATE RELATED AGENTS
causes vomiting, the ingested - MOA – decrease intestinal motility →
corrosive substance will flow decreasing peristalsis
back out of the body which will - Drugs
only add up to the injury as it o Deodorized opium tincture
passed to the GI tract o Difenoxin and atropine
o Example of corrosive substance (motofen)
▪ Ammonia o Diphenoxylate with atropine
▪ Chlorine bleach (Lomotil)
▪ Lie o Loperamide HCl (Imodium)
▪ Toilet cleaners - Can cause CNS depression when taken
▪ Battery acid with alcohol, edative, or tranquilizers

(Under emetics) Diphenoxylate with atropine (Lomotil)


Ipecac syrup - Less potential for causing drug
- Taken with glass of water dependence
- Should be taken within 60 minutes of - For traveler’s diarrhea
poisoning
- Vitim should be alert and conscious Ditenoxin and atropine (Motofen)
o Give med to unconscious
person → they will aspirate the - Active metabolite of phenoxylate
vomited gastric contents - More potent than diphenoxylate
- Treatment for non-speicifc and chronic
Patient teaching diarrhea

1. Instruct the guardian to keep ipecac from


children’s reach

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
Both Diphenoxylate and Ditenoxin are combined
with Atropine because this decreases abdominal LAXATIVES AND CATAHRTICS
- Used to treat constipation by
cramping, intestinal motility, and hypersecretion
eliminating fecal matter
Loperamide (Imodium) - The two differ from the area of their
- Diatabs in the PH action
- Structurally related to diphenoxylate - But save same purpose which is
- Causes less CNS depression than elimination of fecal matter
diphenoxylate and detenoxin
- Most common OTC and protects against
diarreha, decreases fecal volume, and Laxative Cathartic
decreases intestinal fluid and electrolye - Promote soft - Result in a
losses. stool watery stool
- Drugs help with some
SIDE EFFECTS: evacuation of cramping
formed fecal - Drugs help
- Constipation matter from evacuation of
- Drowsiness the rectum unformed
- Dizziness usually
- Dry mouth watery fecal
- Weakness material
- Flush from the
- Rash entire colon
- Blurred Vision
5 TYPES OF LAXATIVES

ADSORBENTS C – hloride Channel Activators


- MOA- coat the wall of the GI tract and E- mollients (stool softeners)
adsorb bacteria or toxins that cause B- ulk- forming
diarrhea O- smotics (saline)
- Used in combination of OTC S- timulants (contact or irritant)
antidiarrheals
- Examples:
o Bismuth subsalicylate (Pepto- Chloride Channel Activators (Selective Chloride
Bismol) Channel Activator)
o Kaolin-pectin (Kaolin with
Pectin) - New category of laxatives
- MOA – activate chloride channels in the
lining of the small intestine leading to
Nursing Management increase in intestinal fluid secretion and
motility because of that, it enhances
1. Continuous monitoring of the passage of stools and relieves
loose bowel movement constipation and accompanying
2. Administer every after loose stool symptoms including pain
- used for idiopathic constipation in
adults
- Example:

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
o Lubiprostone (Amitiza)
Nursing Management
EMOLLIENTS (STOOL SOFTENERS)
- Instruct the px taking powdered laxative that it
- Lubricants should be mixed with water or juice and must be
- Surface acting consumed immediately and should be followed by
- Lubricants like mineral oil increase the a half to full glass of water because this
retention of water in the stool medication solidifies with insufficient water
- Used to prevent constipation intake which can result in intestinal obstruction.
- MOA: work by lowering surface tension
and promoting water accumulation in - After taking this medication it may take
the intestine and stool meaning they 8-24 hours to take effect however, it
draw the water to the stool making the may take up to 3 days after drug
hard stool soft. Because of that action, therapy has started for the stool to be
this now decreases straining during soft and well-formed
defecation
- Examples:
o Docusate Calcium (Surfak) OSTMOTIC (SALINE) LAXATIVE
o Docusate Sodium (Colace)
o Docusate Sodium with senna Hyperosmolar laxative
-
(peri-Colace) Include salt or saline product , lactose,
-
Contraindicated to: and glycerine
• Children - MOA: pull and retain water into the
• Older adults colon through osmotic activity. Because
of the retention of water in the colon
• Patients with debilitating diseases
and the increase of fecal bulk size, this
- Because they may aspirate the mineral
stimulates peristalsis which promotes
oil resulting in lipid pneumonia
bowel movement to a semi-formed to
watery stool
BULK – FORMING LAXATIVES
TAKE NOTE:
- This laxative contains salt and because
- Natural fibrous substance that are non-
of that salt content, good renal function
absorbable
is a must to excrete these salts. Due to
- They promote large, bulk stools
this, it is contraindicated to patients
- MOA: by absorbing water into the
with heart failure
intestine. As the water accumulates in
- Examples:
the intestine, the fecal matter absorbs
o Glycerin
this water making it increase in size.
o Lactulose (Cephulac, Chronulac,
Because of the increase in size of the
Duphalac)
fecal matter this dispense the GI Tract
o Magnesium Citrate (Citroma)
which then stimulates the increase of
o Magnesium Hydroxide (Milk of
peristaltic movement
magnesia)
- Examples:
o Magnesium Oxide (Mag-Ox)
o Polycarbophil (FiberCon)
o Sodium Biphosphate (Fleet
o Polyethylene glycol (MiraLax)
Phopho-Soda)
o Methylcellulose (Citrucel)
o Polyethylene Glycol with
o Psyllium (Metamucil)
electrolytes (GoLYTELY)

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
Polyethylene Glycol with electrolytes action is quick. Within
(GoLYTELY) 2-6 hours of
- Used for bowel preparation administration.
- Requires ingestion of large volume of ▪ This shouldn’t be given
the solution to early pregnancy
- Approximately 3-4 liters over 3 hours because it stimulates
- To make the Polyethylene glycol uterine contractions
palapable patients are required to store which may result to
this medication inside the refrigerator spontaneous abortion.
- The good thing about GoLYTELY is that o Senna (Senokot)
this is an isotonic non absorbable ▪ Long time use of Senna
osmotic substance that contains sodium injures the nerves in the
salts and potassium chloride. colon.
- This is non absorbable can be used for ▪ May result into the loss
patients with renal impairment/with of intestinal muscular
cardiac disorders tone.
▪ Side Effects: Reddish
Lactulose (Duphalac) brown urine. This is
- A very common laxative that is found in because of the
the area. excretion of
- Decreases the serum ammonia level phenolphthalein,
- Used for patients with liver cirrhosis senna/cascara.
- Contains glucose and fructose o Bisacodyl (Dulcolax)
- Diabetic patients should avoid these ▪ Most frequently used
laxatives. and abused laxatives
- TAKE NOTE: Patients taking with that can be purchased
osmotic laxative should continuously be over the counter.
monitored for serum electrolyte levels ▪ The abuse usage may
this is to avoid electrolyte imbalance lead to fluid and
because this contains electrolyte imbalance
sodium/magnesium and small amount specially one’s
is systematically absorb. potassium and calcium.
Stimulant (Contact) Laxatives ▪ Although, absorption of
- It contacts and stimulates Bisacodyl is minimal
- MOA: the drug comes into contact with there might still be
the colon and then it stimulates sensory minimal side effects.
nerve endings in the intestinal mucosa, Side Effects of all the laxatives:
leading to increase peristaltic o Diarrhea
movement. o Abdominal cramping
- These drugs are used to empty the o Nausea
bowel before diagnostic test such as: o Vomiting
barium enema. o Weakness
- Drug Examples: - One serious and dangerous problem the
world is facing is laxative abuse and
o Castor Oil (Neoloid, Purge) dependence.
▪ Should not be given - Since laxative can be purchased OTC,
during bedtime since its most older adults incorporate laxative

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
in their diet to eliminate, unwanted - The impulses releases Ach on the
calories and to double their weight loss. endings of vigous fibers in the endings
- After eating, the individual usually takes of the stomach walls.
laxatives thinking that these laxatives - Transmission of the nervous impulse to
will work to rush out food and calories the acid producing cells in the stomach.
before they can be absorbed by the - Ex: cholridiazepoxide (Librium) and
body. However, what they don’t know clidinium bromide (Quarzan)
is that laxative abuse leads to - Adverse Effects: edema, ataxia,
dependence. confusion, extrapyramidal syndrome,
- Prolong use of laxative can lead to and agranulocytosis.
electrolyte imbalance, dehydration, Anticholinergics
mineral deficiency and even serious - a.k.a. antimuscarinics /
permanent damage to the digestive parasympatholytic
system: including chronic constipation, - MOA: inhibit acetylcholine (activation
damage to the nerves and muscles of of the release of histamine)
the colon. - blocking of histamine and hydrochloric
Nurse Roles: acid
- Provide health teachings about proper - decrease GI mutility and and secretion
use of laxatives. - delays the gastric emptying time
- Correct misconception on using - frequently used for duodenal ulcers
laxatives than for gastric ulcers
Anti ulcers - DOC: peptic ulcers with ANTACIDS
- These are drugs used to prevent and - Should be used as an ADJUNCTIVE
treat ulcers THERAPY
- There are groups under anti ulcers - Ex: clidinium bromide and
these are: chlordiazepoxide HCl (Robinul) and
o Tranquilizers propantheline bromide (Pro-Bantine)
o Anticholinergics - Administer Anticholinergic before meals
▪ These two are used in In order to decrease acid secretion that
frequently due to occurs within
potential adverse - to be followed by antacids 2 hours after
effects. to slow the absorption of
o Antacids anticholinergics.
o Histamine 2 blockers Side effects
o Proton pump inhibitors
o Pepsin inhibitor • Anticholinergic effects
o Prostaglandin analogue

Tranquilizers
- Have minimal effect in
preventing/treating ulcers.
- MOA: they work in reducing vagal
stimulation.
- The relationship of vagal stimulation
and ulcers: the vagus nerves
- Vagus nerve: aroused by sight odor and
taste of palatable food.

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
Antacids magnesium (magnesium hydroxide and
magnesium trisiclicate).
• MOA: Neutralize HCl and reduce pepsin
activity Magnesium hydroxide- has greater neutralizing
power than aluminum hydroxide. This is not
given to patients with impaired renal function
There are 2 types of antacids: because of the risk of hypermagnesemia since
magnesium is primarily excreted in the kidneys.
1. Systemic (effect) antacids
however, hypermagnesemia is usually not a
2. Non-Systemic (effect) antacids problem unless a patient with renal
insufficiency is ingesting magnesium.

Aluminum has a small degree of absorption and


Systemic Antacids
it may cause hypophosphatemia (decreased
Drug example: level of phosphorous in the blood since
aluminum absorbs phosphorous)
1. Sodium bicarbonate (Alka-Seltzer)- One
of the first antiulcer drugs but It is now • Long term use of magnesium causes
seldomly used due to many side effects diarrhea (remember= MAGnesium=
such as: Sodium excess causing MAGtatae)
hypernatremia and water retention
• Long term use of aluminum causes
(because where sodium goes, water
constipation (ALUMINUM is hard=
follows), Metabolic alkalosis caused by
Constipation)
the excess of bicarbonate, and acid
rebound. • Magnesium + Aluminum neutralizes
gastric acid without causing severe
2. Calcium carbonate- most effective in
diarrhea or constipation. Since the
neutralizing acid under systemic
action of the drug is to neutralize the
antacids. However, can cause acid
hydrochloric acid, this is best given 1-3
rebound because 1/3 to 1/2 of the drug
hours after meals and at bedtime.
can be absorbed systemically.

-Excessive use may


cause Burnett's syndrome (milk alkali Histamine 2 blockers
syndrome)
MOA: Block the histamine to receptors of the
parietal cells in the stomach thus reducing
gastric acid secretion and concentration
Non-systemic antacids
Drugs under Histamine 2 blockers usually ends
• composed of alkaline salts such as
with -tidine:
aluminum (aluminum hydroxide) and
1. Cimetidine (tagamet)
BSN 2E (R.N. 2024/ 2025 cutie)
Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
2. Famotidine (pepcid) • There are fewer side effects and drug
interaction compared to cimetidine
3. Nizatidine (Axid)- relieves nocturnal
gastric acid secretion for 12 hours and
since they block H2 receptor, which is
responsible for the stimulation of Sife effects and adverse reactions
gastric acid secretion, This is best given -headache
before meals and at bedtime. -dizziness
Remember= Provide 1 hour interval -constipation
with antacid to maintain efficacy of the -pruritis skin
drug -skin rash
-gynecomastia
4. Ranitidine (Zantac)- 5x more potent -decreased libido
than cimetidine but less potent than -impotence
*Ranitidine and Famotidine have fewer side
famotidine
effects than cimetidine

Cimetidine (tagamet)
Proton pump inhibitors also termed as gastric
• First histamine blocker made. acid secretion inhibitors and gastric pump
inhibitors.
• short half life and duration of action.
• MOA: they block the final step of acid
• only blocks 70% of acid secretion for 4 production through inhibiting the
hours stimulation of the enzyme system,
• good kidney function is needed because hydrogen/potassium adenosine
50% to 80% of the drug is excreted triphosphate located in gastric parietal
unchanged in the urine cells

• Cimetidine + antacids= effectiveness is • they inhibit gastric acid secretion up to


decreased 90% than Histamine 2 blockers

• Proton pump inhibitors are also


considered to be the drug of choice for
Famotidine (pepcid) & Nizatidine (Axid) & GastroEsophageal Reflux Disease
Ranitidine (Zantac) (GERD)

• More potent that cimetidine. • since the action of the drug is to block
the final step of acid production, this is
• Promote ulcer healing
best administered before meal and at
• Duration of action is longer= decrease bedtime
of frequency of dosing.

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.
Drugs under proton pump inhibitors usually
ends with the suffix -prazole:

-omeprazole (prilosec)
-lansoprazole (prevacid)
-Rabeprazole (aciphex)
-Pantoprazole (protonix)
-Esomeprazole (nexium)
-Dexansoprazole (doxilant)

Pepsin inhibitor or also called as mucosal


protective drug

• MOA: form a viscous substance that


covers the ulcer and protects it from
acid and pepsin

• pepsin inhibitor DOES NOT neutralize or


decrease acid secretions

ex: Sucralfate (Carafate) -administered before


meal and at bedtime

Last classification under anti ulcer:

Prostaglandin Analogue Antiulcer Drug

• MOA: Increase cytoprotective mucus in


the GI tract leading to suppression of
gastric acid secretion and moderate
decrease of pepsin secretion

Drug example:

-Misoprostol (cytotec)- contraindicated to


pregnant woman because this causes abortion

BSN 2E (R.N. 2024/ 2025 cutie)


Alfafara, Betonio, Castillano,
Lim, Mabalot, and Tabar.

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