You are on page 1of 13

UNIT 1

● Absorption
INTRODUCTION TO PHARMACOLOGY ● Distribution
● Metabolism / Biotransformation
3 Phases Of Drug When Taken By Mouth Like ● Excretion / Elimination
Tablet or Capsule: Nursing responsibilities:

1. Pharmaceutic Phase ● The nurse applies knowledge of


pharmacokinetics when assessing the
2. Pharmacokinectic Phase patient for possible adverse drug
3. Pharmacodynamic Phase effects.
● The nurse communicates assessment
findings to members of the health care
team in a timely manner to promote
safe and effective drug therapy for the
patient.

The 4 Processes of Pharmacokinetic


PHARMACEUTIC PHASE 1. Absorption

 Drugs in liquid form are more rapidly available 1. the movement of drug particles from the GI tract to
for GI absorption than are solids. body fluids by passive absorption, active
absorption, or pinocytosis.
 Drugs are both disintegrated and absorbed
faster in acidic fluids with a pH of 1 or 2. 2. Most oral drugs are absorbed into the surface
area of the small intestine through the action of the
(Alkaline drugs would become ionized and extensive mucosal villi.
have difficulty crossing cell membrane
barriers.)
Mechanism of Absorption
 Drug absorption is generally slower for those
A. Passive absorption occurs mostly by diffusion
drugs absorbed primarily in the stomach.
(movement from higher concentration to lower
 Enteric-coated drugs resist disintegrated in the concentration)
gastric acid of the stomach, so disintegration B. Active absorption requires a carrier such as an
does not occur until the drug reaches the enzyme or protein to move the drug against a
concentration gradient. Energy is required for
alkaline environment of the small intestine.
active absorption.
o Enteric-coated tablets can remain in
C. Pinocytosis is a process by which cells carry a
the stomach for a long time; therefore, drug across their membrane by engulfing the drug
their effect may be delayed in onset. particles.
Enteric-coated tablets or capsules and
sustained-release (beaded) capsules
should not be crushed.
o Crushing would alter the place and
time of the absorption of the drug,
 Food in the GI tract may interfere with the
dissolution of certain drugs.

PHARMACOKINETIC PHASE

The four processes of pharmacokinetic


Factors Affecting Drug Absorption

1. pH portioning absorption – Weak acid drugs such


as aspirin are less ionized in the stomach, and they
pass through the stomach lining easily and rapidly.

Remember, drugs that are lipid soluble and nonionized


are absorbed faster than water-soluble and ionized
drugs.

2. Blood flow - Poor circulation to the stomach as a


result of shock, vasoconstrictor drugs, or disease
hampers absorption. Pain, stress, and foods that are
solid, hot, or high in fat can slow gastric emptying time,
so the drug remains in the stomach longer. Exercise Bioavailability- is a subcategory of absorption. It is
can decrease blood flow by causing more blood to flow the percentage of the administered drug dose that
reaches the systemic circulation.
to the peripheral muscle, thereby decreasing blood
circulation to the GI tract. The percentage of bioavailability for the oral route is
always less than 100%, but for the IV route it is
3. Surface area - Drugs given IM are absorbed faster 100%.

in muscles that have more blood vessels (e.g.,deltoids) Oral drugs that have a high first-pass hepatic
metabolism may have a bioavailability of only 20%
than in those that have fewer blood vessels (e.g.,
to 40% on entering systemic circulation.
gluteals). Subcutaneous tissue has fewer blood
To obtain the desired drug effect, the oral dose could
vessels, so absorption is slower in such tissue.
be higher than the drug dose for IV use.
4. Lipid Solubility - The GI membrane is composed
mostly of lipid (fat) and protein, so drugs that are lipid
soluble pass rapidly through the GI membrane. Water-
soluble drugs need a carrier, either enzyme or protein,
to pass through the membrane. Large particles pass
through the cell membrane if they are nonionized
(have no positive or negative charge).

First-pass effect, or hepatic first pass

The process in which the drug passes to the liver first: Factors that alter bioavailability include:
• Some drugs do not go directly into the systemic (1) the drug form (e.g., tablet, capsule, sustained
circulation following oral absorption but pass from release, liquid, transdermal patch, rectal
the intestinal lumen to the liver via the portal vein. suppository, inhalation)
• In the liver, some drugs may be metabolized to an (2) route of administration (e.g., oral, rectal, topical,
inactive form that may then be excreted, thus parenteral)
reducing the amount of active drug.
(3) GI mucosa and motility
• Some drugs do not undergo metabolism at all in the
liver, and others may be metabolized to drug (4) food and other drugs, and
metabolite, which may be equally or more active
(5) changes in liver metabolism caused by liver
than the original drug
dysfunction or inadequate hepatic blood flow.
Rapid absorption - increases the bioavailability of the patient’s plasma protein and albumin levels, because a
drug and can cause an increase in drug decrease in plasma protein (albumin) decreases
concentration. Drug toxicity may result.
protein-binding sites, permitting more free drug in the
Slow absorption - can limit the bioavailability of the
circulation.
drug, thus causing a decrease in drug serum
concentration.

2. Distribution - is the process by which the drug


becomes available to body fluids and body tissues.

Drug distribution is influenced by:

1. blood flow

2. the drug’s affinity to the tissue

3. the protein-binding effect

Volume of drug distribution (Vd) is dependent on drug ➢ Abscesses, exudates, body glands, and tumors
dose and its concentration in the body. Drugs with a
hinder drug distribution. Antibiotics do not distribute
larger volume of drug distribution have a longer
well at abscess and exudate sites
half-life and stay in the body longer.
➢ some drugs accumulate in particular tissues such
Protein-binding effect- As drugs are distributed in the
as fat, bone, liver, muscle, and eye tissues.
plasma, many are bound to varying degrees
(percentages) with protein (primarily albumin).
The (blood-brain barrier (BBB) is a
semipermeable membrane in the central
nervous system (CNS) that protects the
brain from foreign substances. Highly
lipid-soluble drugs are able to cross the
BBB. Drugs that are not bound to proteins
and are not lipid soluble are not able to
cross the BBB, which makes it difficult to
distribute the drug.
During pregnancy, both lipid-soluble and
❖ The portion of the drug that is bound is inactive lipid-insoluble drugs are able to cross the
placental barrier, which can affect the
because it is not available to receptors, and the portion fetus and the mother. The risk-benefit
that remains unbound is free, active drug. ratio should be considered before drugs
are given during pregnancy
❖ Only free drugs (drugs not bound to protein) are During lactation, drugs can be secreted into
active and can cause a pharmacologic response. breast milk, which could affect the nursing
infant. The nurse needs to check which
drugs may cross into breast milk before
❖ As the free drug in the circulation decreases, more administering to a lactating patient
bound drug is released from the protein to maintain the
balance of free drug. Drugs bound to proteins cannot
leave the systemic circulation to get to the site of 3. Metabolism (or Biotransformation)
action. This is why only free drug is active.
❑ is the process by which the body inactivates or
❖ A low serum protein level decreases the number of biotransforms drugs. Drugs can be metabolized in
protein-binding sites and can cause an increase in the several organs; however, the liver is the primary site of
amount of free drug in the plasma. Drug toxicity may metabolism.
then result.
❑ Most drugs are inactivated by liver enzymes and are
❖ To avoid possible drug toxicity, checking the protein then converted or transformed by hepatic enzymes to
binding percentage of all drugs administered to a
patient is important. The nurse should also check the
inactive metabolites or water-soluble substances for ✓ breast milk
excretion.
➢The kidneys filter free unbound drugs, watersoluble
❑ a large percentage of drugs are lipid soluble; thus drugs, and drugs that are unchanged.
the liver metabolizes the lipid-soluble drug substance
➢The lungs eliminate volatile drug substances and
to a watersoluble substance for renal excretion
products metabolized to carbon dioxide (CO2) and
❑ When the drug metabolism rate is decreased, water (H2O).
excess drug accumulation can occur and lead to
➢The urine pH influences drug excretion. Urine pH
toxicity.
varies from 4.5 to 8.
The half-life (t 1/2 ) of a drug is the time it takes for
one half of the drug concentration to be eliminated. ➢Acidic urine promotes elimination of weak base

Metabolism and elimination affect the half-life of a drugs, and alkaline urine promotes elimination of weak

drug. acid drugs.

A drug goes through several half-lives before more ➢ With a kidney disease that results in decreased
than 90% of the drug is eliminated. If the patient takes glomerular filtration rate (GFR) or decreased renal
650 mg of aspirin and the half-life is 3 hours, it takes 3 tubular secretion, drug excretion is slowed or impaired.
hours for the first half-life to eliminate 325 mg, 6 hours
➢ A decrease in GFR results in an increase in serum
for the second half-life to eliminate an additional 162
creatinine level and a decrease in urine creatinine
mg, and so on until the sixth half-life (or 18 hours),
clearance.
when 10 mg of aspirin is left in the body.
➢ Urea nitrogen is a waste product that your kidneys
remove from your blood. Higher than normal BUN
levels may be a sign that your kidneys aren't working
well. People with early kidney disease may not have
any symptoms. A BUN test can help uncover kidney
problems at an early stage when treatment can be
more effective

➢ Common tests used to determine renal function are


creatinine clearance (CLcr) and blood urea nitrogen
(BUN).
4. Excretion (or Elimination)
➢ Creatinine is a metabolic by-product of muscle that
The main route of drug elimination is through the is excreted by the kidneys.
kidneys (urine).
➢ The creatinine clearance test compares the level of
Other routes include:
creatinine in the urine with the level of creatinine in the

✓Bile blood. Creatinine clearance varies with age and


gender.
✓Feces
Lower values are expected in older adult and female
✓Lungs patients because of their decreased muscle mass.

✓Saliva

✓Sweat PHARMACODYNAMIC PHASE


- is the study of the way drugs affect the body.

- Drug response can cause a primary or secondary


physiologic effect or both.

- The primary effect is desirable, and the secondary


effect may be desirable or undesirable.

- An example of a drug with a primary and secondary


effect is diphenhydramine (Benadryl), an antihistamine.

RECEPTOR THEORY

➢Drugs act through receptors by binding to the


receptor to produce (initiate) a response or to block
(prevent) a response. The activity of many drugs is

\ determined by the ability of the drug to bind to a


specific receptor. The better the drug fits at the
receptor site, the more biologically active the drug is. It
The primary effect of diphenhydramine is to treat the
is similar to the fit of the right key in a lock.
symptoms of allergy, and the secondary effect is a
central nervous system depression that causes
Most receptors, which are protein in nature, are found
drowsiness. The secondary effect is undesirable when
the patient drives a car, but at bedtime it could be in cell membranes.
desirable because it causes mild sedation.
Drug-binding sites are primarily on:

ONSET, PEAK, AND DURATION OF ACTION ❖Proteins

➢ Onset of action is the time it takes to reach the ❖Glycoproteins


minimum effective concentration (MEC) after a drug is
administered. ❖Proteolipids

➢ Peak action occurs when the drug reaches its ❖Enzymes.


highest blood or plasma concentration.

➢ Duration of action is the length of time the drug has


a pharmacologic effect.

It is necessary to understand the time response in


relationship to drug administration. If the drug plasma
or serum level decreases below threshold or MEC,
adequate drug dosing is not achieved; too high a drug
level above the minimum toxic concentration (MTC)
can result in toxicity

There are four receptor families:

a) kinase-linked receptors
b) ligand-gated ion channels

c) G protein–coupled receptor systems NONSPECIFIC AND NONSELECTIVE DRUG


EFFECTS
d) nuclear receptors
A receptor produces a variety of physiologic
The ligand-binding domain is the site on the receptor at
responses, depending on where in the body the
which drugs bind.
receptor is located. Cholinergic receptors are located
I. Kinase-linked receptors. The ligand-binding in the bladder, heart, blood vessels, stomach, bronchi,
domain for drug binding is on the cell surface. The and eyes. A drug that stimulates or blocks the
drug activates the enzyme (inside the cell), and a cholinergic receptors affects all anatomic sites of
response is initiated. location. Drugs that affect various sites are
nonspecific drugs and have properties of
II. Ligand-gated ion channels. The channel spans
nonspecificity.
the cell membrane and, with this type of receptor, the
channel opens, allowing for the flow of ions into and
out of the cells. The ions are primarily sodium and
calcium.

III. G protein–coupled receptor systems. There are


three components to this receptor response: (1) the
receptor, (2) the G protein that binds with guanosine
triphosphate (GTP), and (3) the effector that is either
an enzyme or an ion channel. The system works as
follows:

Drugs may act at different receptors. Drugs that affect


various receptors are nonselective drugs or have
IV. Nuclear receptors. Found in the cell nucleus (not
properties of nonselectivity.
on the surface) of the cell membrane. Activation of
Drugs that produce a response but do not act on a
receptors through the transcription factors is receptor may act by stimulating or inhibiting enzyme
prolonged. first three receptor groups, activation of the activity or hormone production.
receptors is rapid.

AGONISTS AND ANTAGONISTS

Agonists – drug that produce a response

Example: Epinephrine (Adrenalin) stimulates beta1


and beta2 receptors, so it is an agonist.

Antagonists – drugs that block a response

Example: Atropine, an antagonist, blocks the histamine


(H2) receptor, thus preventing excessive gastric acid
secretion. The effects of an antagonist can be
determined by the inhibitory (I) action of the drug
concentration on the receptor site.
Four Categories of Drug Action

1. STIMULATION - the rate of cell activity or the


secretion from a gland increases depression- cell PEAK AND TROUGH DRUG LEVELS
activity and function of a specific organ are reduced
Peak drug level is the highest plasma concentration of
2. REPLACEMENT - drugs such as insulin replace drug at a specific time. Peak drug levels indicate the
essential body compounds rate of absorption.

3. INHIBITION OR KILLING OF ORGANISMS - Drugs If the drug is given orally, the peak time might be 1 to 3
that inhibit or kill organisms interfere with bacterial cell hours after drug administration.
growth (e.g., penicillin exerts its bactericidal effects by
If the drug is given IV, the peak time might occur in 10
blocking the synthesis of the bacterial cell wall)
minutes.
4. IRRITATION - Drugs also can act by the mechanism
If a peak drug level is ordered, a blood sample should
of irritation (e.g., laxatives irritate the inner wall of the
be drawn at the proposed peak time, according to the
colon, thus increasing peristalsis and defecation).
route of administration.

Trough drug level is the lowest plasma concentration


THERAPEUTIC INDEX AND THERAPEUTIC RANGE of a drug, and it measures the rate at which the drug is
(THERAAPEUTIC WINDOW) eliminated. Trough levels are drawn immediately
before the next dose of drug is given, regardless of
The safety of drugs is a major concern. The
route of administration.
therapeutic index (TI) estimates the margin of safety of
a drug through the use of a ratio that measures the
effective (therapeutic) dose (ED) in 50% of people
LOADING DOSE
(ED50) and the lethal dose (LD) in 50% of people
(LD50). When immediate drug response is desired, a large
initial dose, known as the loading dose, of drug is
The closer the ratio is to 1, the greater the danger of
given to achieve a rapid minimum effective
toxicity.
concentration in the plasma. After a large initial dose, a
Drug dosage might need adjustment, and plasma prescribed dosage per day is ordered.
(serum) drug levels need to be monitored because of
Digitalization is the process by which the minimum
the small safety range between the ED and LD.
effective concentration level for digoxin is achieved in
Drugs with a high therapeutic index have a wide the plasma within a short time.
margin of safety and less danger of producing toxic
effects Side Effects, Adverse Reactions

The therapeutic range (therapeutic window) of a drug Common response to medications


concentration in plasma is the level of drug between
the minimum effective concentration in the plasma for Desired Effect
obtaining desired drug action and the minimum toxic The therapeutic goal is achieved. The
drug does what is supposed to do.
concentration (the toxic effect).
Side Effect
When the therapeutic range is given, it includes both
Are mild but annoying response to
protein-bound and unbound portions of the drug. medication. Ex nausea and
drowsiness. Takes place when one drug replaces
another at the drug receptor site,
Adverse Effect increasing the effect of the first drug.
Are more severe symptoms or Incompatibility
problems that arise because of the
medication. Ex gastric bleeding or Occurs when two drugs mixed
edema together in a syringe produce a
chemical reaction, so they cannot be
Idiosyncratic Response given.
Are strange, unique, or unpredicted Interference
reactions. Ex blood in the urine a rare
case for taking aspirin. Occurs when one drug promotes the
rapid excretion of another, thus
Paradoxical Reaction reducing its activity.
Are reactions that are opposite of
what would be expected.
Allergic Response PHARMACOGENETICS
Is an antigen-antibody reaction. The
body develops hives, rashes, itching, - is the scientific discipline studying how the effect of a
or swelling of the skin. A rash or drug action varies from a predicted drug response
shortness of breath is occasionally
seen in patients allergic to aspirin. because of genetic factors or hereditary influence.

Anaphylactic Response Because people have different genetic makeup,


they do not always respond identically to a drug
Is a severe form of allergic reaction
that is life threatening. The patient dosage or planned drug therapy.
develops severe shortness of breath,
may stop breathing, or may have
cardiac collapse.
Tolerance and Tachyphylaxis

Tolerance – refers to a decreased responsiveness


TOXIC EFFECTS, OR TOXICITY
over the course of theraphy.
• Identified by monitoring the plasma (serum)
Tachyphylaxis – refers to a rapid decrease in
therapeutic range of the drug. However, for drugs
that have a wide therapeutic index, the therapeutic response to the drug. Tachyphylaxis is an “acute
ranges are seldom given. tolerance”.
• When the drug level exceeds the therapeutic range,
toxic effects are likely to occur from overdosing or ● Drug categories that can cause tachyphylaxis
drug accumulation. include narcotics, barbiturates, laxatives, and
psychotropic agents.
Common Drug interactions
Placebo Effect
Additive Effect
- is a psychological benefit from a compound that may
When two drugs are given together,
the combined effect of the drugs is not have the chemical structure of a drug effect. The
equal to that of the single more active placebo is effective in approximately one third of
component of the mixture or to the
sum of the effects of the individual persons who take a placebo compound.
drugs.
Antagonistic Effect
Effect takes place when one drug
interferes with the action of another
drug.
Displacement
Malfeasance. Giving the correct drug but by the wrong
route that results in the patient’s death.

INITIATIVES TO COMBAT DRUG


COUNTERFEITING

1. The role of the nurse is critical in consumer


CHAPTER 2: education.
THE DRUG APPROVAL PROCESS
2. The nurse must advise patients to report any
differences in taste or appearance of a drug or in its
packaging.

3. Patients should be alert to slight variations in


packaging or labeling (e.g., color, package seal);

4. Should note any unexpected side effects; and


should buy drugs from reputable sources.

DRUG NAMES
FEDERAL LEGISLATION - Through federal
legislation, the public is protected from drugs that are Chemical Name

impure, toxic, ineffective, or not tested before public


constitutes a description of a drug using a
sale. The primary purpose of the legislation is to nomenclature of chemistry.
ensure safety.
Generic Name

NURSE PRACTICE ACTS known as the nonproprietary name; known


also the most common drug name where
the drug manufacturer uses for a drug.
- Nurses are responsible for knowing their state’s law
and administrative code. Nurses who administer a drug
Brand Name
without a licensed health care provider’s order are in
violation of the nurse practice act and can have their known as the proprietary or trade name or
licenses revoked. the name for the drug manufactured by one
of the company often by the symbol
- The nurse can be prosecuted for giving the wrong
drug or dosage, omitting a drug dose, or giving the
drug by the wrong route. The legal terms for these
offenses are as follows:

Misfeasance. Negligence; giving the wrong drug or


drug dose that results in the patient’s death

Nonfeasance. Omission; omitting a drug dose that


results in the patient’s death
These practices can have neutral, beneficial, or
deleterious effects on a patient’s health.

✓ The nurse must obtain a thorough health history to


CHAPTER 3:
determine all the pharmacotherapeutic agents the
CULTURAL AND PHARMACOGENETIC
patient is using.
CONSIDERATIONS
Healers play a role in traditional health practices in
ETNOPHARMACOLOGY
about 80% of the population worldwide. Traditional
- is the study of drug responses that may be unique to healers usually have some practical knowledge of
an individual owing to social, cultural, and biologic human anatomy and physiology, pharmacology, and
phenomena. pharmaceutical substances.

- highlights the need for nurses to use knowledge and Assimilation occurs when a less powerful group
research from the social sciences as well as the changes its ways to blend in with the dominant cultural
biologic and physical sciences to provide holistic group. Adults who immigrate to a new region usually
nursing care take longer to assimilate than do younger people.

Acculturation is the process by which a group adjusts

PHARMACOGENETICS to living within a dominant culture while at the same


time maintaining its original identity.
- integrates the study of pharmacokinetics,
pharmacodynamics, and variations of the predicted Complementary Health Practices that combine

response to a drug due to genetic factors. The nurse traditional beliefs and mainstream health practices.

must integrate knowledge of pharmacogenetics within Alternative Health Practices it is called when a
patients’ cultural contexts. dominant group adopts health practices from a
nondominant group.

Culture is defined as sets of learned behavior and Pharmacogenomics refers to the general study of all

ideas that human beings acquire as members of a the different genes that determine drug behavior.

community.

Community is a cluster of individuals who function as


a group to attain cultural universals.

Cultural universals are designed to meet the


community’s survival needs and common goals such
as the obtainment of food and other practices that
maintain the group.

TRANSCULTURAL NURSING

Numerous cultural groups engage in the use of


traditional health practices, which may include use of:
teas, herbs, spices, and special foods as well as CHAPTER 4:
homeopathic remedies, poultices, and ointments. DRUG INTERACTION AND OVER-THE-COUNTER
DRUGS
Drug Interaction

- is defined as an altered or modified action or effect of Drug-induced Photosensitivity


a drug as a result of interaction with one or multiple
- Reaction is a skin reaction caused by exposure to
drugs.
sunlight. It is caused by the interaction of a drug and
- It should not be confused with adverse drug reaction exposure to ultraviolet A (UVA) light, which can cause
or drug incompatibility. cellular damage. Usually the skin area that is exposed
is affected.
- An adverse drug reaction is an undesirable drug
effect that ranges from mild untoward effects to severe 2 types of photosensitivity reactions
toxic effects, including hypersensitivity reaction and
1. Photoallergy
anaphylaxis.
- Occurs when a drug (e.g., sulfonamide) undergoes
activation in the skin by ultraviolet light to a compound
Drug incompatibility that is more allergenic than the parent compound.
Because it takes time to develop antibodies,
- is a chemical or physical reaction that occurs among
photoallergenic reactions are a type of delayed
two or more drugs in vitro. In other words, the reaction
hypersensitivity reaction.
occurs between two or more drugs within a syringe, IV
bag, or other artificial environment outside of the body. 2. Phototoxicity

- Photosensitive drug undergoes photochemical


reactions within the skin to cause damage. This type of
Drug interactions can be divided into two categories:
reaction is different from photoallergy in that it is not
● Pharmacokinetic Interactions immune-mediated. The onset of phototoxicity with
erythema can be rapid, occurring within 2 to 6 hours of
● Pharmacodynamic Interactions
sunlight exposure.

DRUG INTERACTIONS
PEDIATRIC AND GERIATRIC PHARMACOKINETIC
Drug-Food
Geriatric Distribution
- interaction is known to increase, decrease, or delay
drug absorption. Food can bind with drugs, causing
less or slower drug absorption. An example of food
binding with a drug is the interaction of tetracycline and
dairy products. The result is a decrease in the plasma
concentration of tetracycline. Because of the binding
effect, tetracycline should be taken 1 hour before or 2
hours after meals and should not be taken with dairy
products

Drug-Laboratory interaction

- Abnormal plasma or serum electrolyte concentrations


can affect certain drug therapies.
increased in older infants and
children
• Phenobarbitone metabolism faster in
children than adults
• Drug administered to the mother can
induce neonatal enzyme activity
(ex.barbiturate)
• All renal mechanisms (filtration,
secretion and reabsorption) are
reduced in neonates
• Renal excretion of drugs relatively
reduced in new born

Clinical Significance

PEDIATRIC
- Phenobarbital, when given to
pregnant women near term, can
induce fetal hepatic enzymes
responsible for the glucuronidation of
bilirubin.
Pediatric Distribution - Chloramphenicol can produce grey
• GI absorption slower in infancy, but baby syndrome in neonates.
absorption from intra-muscular
injection is faster. GERIATRIC

• In neonates common practice to use Golden rule for drug therapy in elderly
IV preparations - Smallest number of drugs
• Infant skin is thin and percutaneous - In lowest possible doses
absorption can cause systemic - For shortest possible time
toxicity (ex. If potent steroids are - In simplest regimen
applied too extensively)
• Body fat content in infants low, water
content is high Pediatric Pharmodynamic

• Lower Vd of fat soluble drugs Important Adverse Effects in Children


(diazepam) in infants
• Decrease plasma protein binding of ● With a few notable exceptions, drugs in children
drugs in neonates (kernicterus due to generally have a similar adverse effect profile to those
displacement of bilirubin by
sulfonamides) in adults.

• Blood-brain barrier is more permeable


in neonates and young children,
leading to and increase risks of CNS Examples of Some Specific ADR:
adverse effects
• At birth, the heaptic microsomal 1. Chronic corticosteroid use: inhibit growth
enzyme system is relative immature
particularly in preterm infant but after 2. Tetracyclines: staining and occasionally dental
first four weeks it matures rapidly
hypoplasia
• Conversely hepatic drug metabolism
3. Fluoroquinolone (ciprofloxacin): damage growing ● Avoid drugs with negligible or doubtful benefits
cartilage
● Think about the dose
4. Metoclopramide: Dystonias more frequently than in
● Think about drug formulation
adults
● Assume any new symptoms may be due to drug
5. Valproate: Hepatotoxicity is increase in young
side-effects
children
● Take a careful drug history
6. Aspirin: Reye’s syndrome
● Used fixed combinations of drugs rarely

● Check compliance
GERIATRIC PHARMODYNAMIC
● Think before adding a new drug to the regimen
Pharmacodynamic Changes:
● Stopping is as important as Starting.
● Greater sensitivity to medications affecting the CNS
(benzodiazepines and opioids)

● More confusion with cimetidine

● Increased incidence of postural hypotension

● Reduced clotting factor synthesis: require reduced


dose of warfarin

● Increased toxicity from NSAIDS

● Increased incidence of allergic reactions

Principles of Prescribing in Children

● Calculate doses for drugs based on weight of


patients

● Use well established drugs

● Give proper instructions to parents

● Keep all drugs out of reach of children

● Use antibiotics sparingly ad only when required

● Avoid prolonged treatment with drugs that have


delayed complications (Steroids)

● Use suitable dosage forms

● Keep in mind PK & PD differences

General Principles for Prescribing in Elderly

● Think about the necessity for drugs

You might also like