UNIT 1 INTRODUCTION TO Enteric-coated tablets can remain in the
PHARMACOLOGY stomach for a long time; therefore,
3 Phases Of Drug When Drug Taken By
Mouth Like Tablet Or Capsule
1. Pharmaceutic Phase
2. Pharmacokinetic Phase
3. Pharmacodynamic Phase
PHARMACEUTIC PHASE
• The pharmaceutic phase (dissolution) is
the first phase of drug action.
• A drug in solid form (tablet or capsule)
must disintegrate into small particles to
dissolve into a liquid, a process known
as dissolution.
• Drugs in liquid form are already in
solution.
• Excipients Fillers and inert substances
that are used in drug preparation to
allow the drug to take on a particular
size and shape and to enhance drug
dissolution.
• Disintegration is the breakdown of a
tablet into smaller particles.
• Dissolution is the dissolving of the
smaller particles in the GI fluid before
absorption
• Drugs in liquid form are more rapidly
available for GI absorption than are
solids.
• Drugs are both disintegrated and
absorbed faster in acidic fluids with a pH
of 1 or 2. (Alkaline drugs would become
ionized and have difficulty crossing cell
membrane barriers.)
• Drug absorption is generally slower for
those drugs absorbed primarily in the
stomach.
• Enteric-coated drugs resist disintegration
in the gastric acid of the stomach, so
disintegration does not occur until the
drug reaches the alkaline environment
of the small intestine.
Lauro, VKV | Pharmacology
their effect may be delayed in onset.
Enteric-coated tablets or capsules and
sustained-release (beaded) capsules
should not be crushed.
Crushing would alter the place and time
of absorption of the drug.
• Food in the GI tract may interfere with
the dissolution of certain drugs.
PHARMACOKINETIC PHASE
The four processes of
pharmacokinetic
● Absorption
● Distribution
● Metabolism / Biotransformation
● Excretion / Elimination
Nursing responsibilities:
● The nurse applies knowledge of
pharmacokinetics when assessing
the patient for possible adverse
drug 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
1. Absorption
1. the movement of drug particles from
the GI tract to body fluids by passive
absorption, active absorption, or
pinocytosis.
2. Most oral drugs are absorbed into the
surface area of the small intestine
through the action of the extensive
mucosal villi.
MECHANISM OF ABSORPTION
A. Passive absorption occurs mostly
by diffusion (movement from higher
concentration to lower concentration)
B. Active absorption requires a carrier
such as an enzyme or protein to move
the drug against a concentration
gradient. Energy is required for active
absorption.
C. Pinocytosis is a process by which
cells carry a drug across their
1
 membrane by engulfing the drug are nonionized (have no positive or
particles. negative charge)
First-Pass Effect, Or Hepatic First Pass
The process in which the drug passes to
the liver first:
• Some drugs do not go directly into the
systemic circulation following oral
absorption but pass from the intestinal
lumen to the liver via the portal vein.
• In the liver, some drugs may be
metabolized to an inactive form that
may then be excreted, thus reducing
the amount of active drug.
• Some drugs do not undergo metabolism
at all in the liver, and others may be
metabolized to drug metabolite, which
may be equally or more active than the
Factors Affecting Drug Absorption
original drug
1. pH partitioning 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
Bioavailability
hampers absorption. Pain, stress, and
is a subcategory of absorption. It is the
foods that are solid, hot, or high in fat
percentage of the administered drug
can slow gastric emptying time, so the
dose that reaches the systemic
drug remains in the stomach longer.
circulation.
Exercise can decrease blood flow by
The percentage of bioavailability for the
causing more blood to flow to the
oral route is always less than 100%,
peripheral muscle, thereby decreasing
but for the IV route it is 100%.
blood circulation to the GI tract.
Oral drugs that have a high first-pass
3. Surface area- Drugs given IM are
hepatic metabolism may have a
absorbed faster in muscles that have
bioavailability of only 20% to 40% on
more blood vessels (e.g., deltoids) than
entering systemic circulation.
in those that have fewer blood vessels
To obtain the desired drug effect, the oral
(e.g., gluteals). Subcutaneous tissue
dose could be higher than the drug
has fewer blood vessels, so absorption
dose for IV use
is slower in such tissue.
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

Lauro, VKV | Pharmacology 2


Factors that alter bioavailability
include:
(1) the drug form (e.g., tablet, capsule,
sustained release, liquid, transdermal
patch, rectal suppository, inhalation)
(2) route of administration (e.g., oral,
rectal, topical, parenteral)
(3) GI mucosa and motility
(4) food and other drugs, and
(5) changes in liver metabolism caused by
liver dysfunction or inadequate hepatic
blood flow.
Rapid absorption increases
bioavailability of the drug and can
cause an increase in
concentration. Drug toxicity may result.
Slow absorption can limit
bioavailability of the 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 dose and its
concentration in the body. Drugs with a
larger volume of drug distribution have a
longer half-life and stay in the body longer.
Protein-binding effect- As drugs
are distributed in the plasma, many are
bound to varying degrees (percentages)
with protein (primarily albumin)
Lauro, VKV | Pharmacology
❖ The portion of the drug that is bound is
inactive because it is not available to
receptors, and the portion that remains
unbound is free, active drug.
❖ Only free drugs (drugs not bound to
protein) are active and can cause a
pharmacologic response.
❖ As the free drug in the circulation
decreases, more 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 action. This is why only free drug is
active.
❖ a low serum protein level decreases the
number of protein-binding sites and can cause
an increase in the amount of free drug in the
plasma. Drug toxicity may then result.
❖ To avoid possible drug toxicity, checking
the protein binding percentage of all drugs
administered to a patient is important. The
nurse should also check the patient’s plasma
protein and albumin levels, because a decrease
the in plasma protein (albumin) decreases protein-
binding sites, permitting more free drug in the
drug circulation.
the
➢ Abscesses, exudates, body glands, and
tumors hinder drug distribution. Antibiotics
do not distribute well at abscess and
exudate sites
➢ some drugs accumulate in particular tissues
such as fat, bone, liver, muscle, and eye
tissues.
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
lipid-insoluble drugs are able to cross
3
 Other routes include: ✓Bile ✓Feces
the placental barrier, which can affect
the fetus and the mother. The risk- ✓Lungs ✓Saliva ✓Sweat ✓ breast milk
benefit ratio should be considered ➢The kidneys filter free unbound drugs,
before drugs are given during watersoluble drugs, and drugs that are
pregnancy unchanged.
During lactation, drugs can be secreted ➢The lungs eliminate volatile drug substances
into breast milk, which could affect the and products metabolized to carbon dioxide
nursing infant. The nurse needs to
(CO2) and water (H2O).
check which drugs may cross into
breast milk before administering to a ➢The urine pH influences drug excretion.
lactating patient Urine pH varies from 4.5 to 8.
➢Acidic urine promotes elimination of weak
3. METABOLISM/BIOTRANSFORMATION
base drugs, and alkaline urine promotes
❑ is the process by which the body inactivates
elimination of weak acid drugs
or biotransforms drugs. Drugs can be
➢ With a kidney disease that results in
metabolized in several organs; however, the
decreased glomerular filtration rate (GFR)
liver is the primary site of metabolism.
or decreased renal tubular secretion, drug
❑ Most drugs are inactivated by liver enzymes
excretion is slowed or impaired.
and are then converted or transformed by
➢ A decrease in GFR results in an increase in
hepatic enzymes to inactive metabolites or
serum creatinine level and a decrease in
water-soluble substances for excretion.
urine creatinine clearance.
❑ a large percentage of drugs are lipid
➢ Urea nitrogen is a waste product that
soluble; thus the liver metabolizes the lipid-
soluble drug substance to a watersoluble your kidneys remove from your blood.
substance for renal excretion Higher than normal BUN levels may be
❑ When the drug metabolism rate is a sign that your kidneys aren't working
decreased, excess drug accumulation can well. People with early kidney disease
may not have any symptoms. A BUN
occur and lead to toxicity.
test can help uncover kidney problems
The half-life (t 1/2 ) of a drug is
at an early stage when treatment can
the time it takes for one half of the drug
be more effective
concentration to be eliminated.
➢ Common tests used to determine renal
Metabolism and elimination affect the half-
function are creatinine clearance (CLcr)
life of a drug.
and blood urea nitrogen (BUN).
A drug goes through several half-
➢ Creatinine is a metabolic by-product of
lives before more than 90% of the drug is
muscle that is excreted by the kidneys.
eliminated. If the patient takes 650 mg of
➢ The creatinine clearance test compares
aspirin and the half-life is 3 hours, it takes
the level of creatinine in the urine with
3 hours for the first half-life to eliminate
the level of creatinine in the blood.
325 mg, 6 hours for the second half-life to
Creatinine clearance varies with age
eliminate an additional 162 mg, and so on
and gender.
until the sixth half-life (or 18 hours), when
Lower values are expected in older adult
10 mg of aspirin is left in the body.
and female patients because of their
decreased muscle mass.

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
4. EXCRETION / ELIMINATION the secondary effect may be desirable
The main route of drug elimination or undesirable.
is through the kidneys (urine). - An example of a drug with a primary
and secondary effect is

Lauro, VKV | Pharmacology 4

 diphenhydramine (Benadryl), an
antihistamine.
The primary effect of diphenhydramine is to treat
the symptoms of allergy, and the secondary
effect is a central nervous system depression
that causes drowsiness. The secondary effect is
undesirable when the patient drives a car, but at
bedtime it could be desirable because it causes
mild sedation.
Onset, Peak, and Duration of Action
➢ Onset of action is the time it takes to
reach the minimum effective concentration
(MEC) after a drug is administered.
➢ Peak action occurs when the drug
reaches its 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
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 is similar to the fit of
the right key in a lock.
Lauro, VKV | Pharmacology
Most receptors, which are protein in
nature, are found in cell membranes.
Drug-binding sites are primarily on: ❖Proteins
❖Glycoproteins ❖Proteolipids ❖enzymes.
There are four receptor families:
a) kinase-linked receptors
b) ligand-gated ion channels
c) G protein–coupled receptor systems
d) nuclear receptors.
The ligand-binding domain is
the site on the receptor at which drugs
bind.
I. Kinase-linked receptors. The ligand-
binding domain for drug binding is on the
cell surface. The drug activates the
enzyme (inside the cell), and a response
is initiated.
II. Ligand-gated ion channels. The
channel spans 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:
IV. Nuclear receptors. Found in the cell
nucleus (not on the surface) of the cell
membrane. Activation of receptors
through the transcription factors is
prolonged. first three receptor groups,
activation of the receptors is rapid
Agonists and Antagonists
Drugs that produce a response are
called agonists
5
Example:Epinephrine (Adrenalin)
stimulates beta1 and beta2 receptors, so it
is an agonist.
Drugs that block a response are called
antagonists.
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
Nonspecific and Nonselective Drug
Effects
A receptor produces a variety of
physiologic responses, depending on
where in the body the receptor is located.
Cholinergic receptors are located in the
bladder, heart, blood vessels, stomach,
bronchi, and eyes. A drug that stimulates
or blocks the cholinergic receptors affects
all anatomic sites of location. Drugs that
affect various sites are nonspecific
drugs and have properties of
nonspecificity.
Drugs may act at different receptors.
Drugs that affect various receptors are
nonselective drugs or have properties of
nonselectivity.
Drugs that produce a response but do not
act on a receptor may act by stimulating or
inhibiting enzyme activity or hormone
production.
Four Categories of Drug Action
Lauro, VKV | Pharmacology
1. STIMULATION the rate of cell activity
or the secretion from a gland
increases depression- cell activity and
function of a specific organ are
reduced
2. REPLACEMENT drugs such as insulin
replace essential body compounds
3. INHIBITION OR KILLING OF
ORGANISMS Drugs that inhibit or kill
organisms interfere with bacterial cell
growth (e.g., penicillin exerts its
bactericidal effects by blocking the
synthesis of the bacterial cell wall)
4. IRRITATION Drugs also can act by
the mechanism of irritation (e.g.,
laxatives irritate the inner wall of the
colon, thus increasing peristalsis and
defecation)
Therapeutic Index and Therapeutic
Range (Therapeutic Window)
The safety of drugs is a major concern.
The 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 (ED50) and the lethal
dose (LD) in 50% of people (LD50).
The closer the ratio is to 1, the greater the
danger of toxicity.
Drug dosage might need adjustment, and
plasma (serum) drug levels need to be
monitored because of the small safety
range between the ED and LD.
Drugs with a high therapeutic index have
a wide margin of safety and less
danger of producing toxic effects
The therapeutic range (therapeutic
window) of a drug concentration in
plasma is the level of drug between the
minimum effective concentration in the
plasma for obtaining desired drug
action and the minimum toxic
concentration (the toxic effect).
When the therapeutic range is given, it
includes both protein-bound and
unbound portions of the drug.
6
 Peak and Trough Drug Levels
aspirin.
Peak drug level is the highest plasma Paradoxical Reaction
concentration of drug at a specific time. Are reactions that are opposite of
Peak drug levels indicate the rate of what would be expected.
absorption. Allergic Response
If the drug is given orally, the peak Is an antigen-antibody reaction.
time might be 1 to 3 hours after drug The body develops hives, rashes,
itching, or swelling of the skin. A
administration.
rash or shortness of breath is
If the drug is given IV, the peak time occasionally seen in patients
might occur in 10 minutes. allergic to aspirin.
If a peak drug level is ordered, a Anaphylactic Response
blood sample should be drawn at the Is a severe form of allergic
proposed peak time, according to the reaction that is life threatening.
route of administration. The patient develops severe
shortness of breath, may stop
The trough drug level is the lowest breathing, or may have cardiac
plasma concentration of a drug, and it collapse.
measures the rate at which the drug is
eliminated. Trough levels are drawn
TOXIC EFFECTS / TOXICITY
immediately before the next dose of
• identified by monitoring the plasma
drug is given, regardless of route of
(serum) therapeutic range of the drug.
administration.
However, for drugs that have a wide
therapeutic index, the therapeutic
Loading Dose
ranges are seldom given.
When immediate drug response is
• When the drug level exceeds the
desired, a large initial dose, known as
therapeutic range, toxic effects are
the loading dose, of drug is given to
likely to occur from overdosing or drug
achieve a rapid minimum effective
accumulation.
concentration in the plasma. After a
large initial dose, a prescribed dosage Common Drug interactions
per day is ordered.
Additive Effect
Digitalization is the process by which the
When two drugs are given
minimum effective concentration level together, the combined effect of
for digoxin is achieved in the plasma the drugs is equal to that of the
within a short time single more active component of
the mixture or to the sum of the
Side Effects, Adverse Reactions
effects of the individual drugs.
Common response to Medications. Antagonistic Effect
Effect takes place when one drug
Desired Effect interferes with the action of
The therapeutic goal is achieved. another drug.
The drug does what is supposed Displacement
to do. Takes place when one drug
Side Effect replaces another at the drug
Are mild but annoying response to receptor site, increasing the effect
medication. Ex nausea and of the first drug.
drowsiness. Incompatibility
Adverse Effect Occurs when two drugs mixed
Are more severe symptoms or together in a syringe produce a
problems that arise because of the chemical reaction, so they cannot
medication. Ex gastric bleeding or be given.
edema Interference
Idiosyncratic Response Occurs when one drug promotes
Are strange, unique, or the rapid excretion of another, thus
unpredicted reactions. Ex blood in reducing its activity.
the urine a rare case for taking

Lauro, VKV | Pharmacology 7

 Pharmacogenetics CHAPTER 2: THE DRUG APPROVAL
is the scientific discipline studying PROCESS
how the effect of a drug action varies from Federal Legislation
a predicted drug response because of Through federal legislation, the
genetic factors or hereditary influence. public is protected from drugs that are
Because people have different genetic impure, toxic, ineffective, or not tested
makeup, they do not always respond before public sale. The primary purpose of
identically to a drug dosage or planned the legislation is to ensure safety.
drug therapy. NURSE PRACTICE ACTS
● TOLERANCE AND - Nurses are responsible for knowing
TACHYPHYLAXIS their state’s law and administrative
Tolerance refers to a decreased code. Nurses who administer a drug
responsiveness over the course of without a licensed health care
therapy. provider’s order are in violation of the
Tachyphylaxis refers to a rapid nurse practice act and can have their
decrease in response to the drug. licenses revoked.
tachyphylaxis is an “acute - the nurse can be prosecuted for giving
tolerance.” the wrong drug or dosage, omitting a
● Drug categories that can cause drug dose, or giving the drug by the
tachyphylaxis include narcotics, wrong route. The legal terms for these
barbiturates, laxatives, and offenses are as follows:
psychotropic agents. Misfeasance. Negligence; giving
● PLACEBO EFFECT the wrong drug or drug dose that
A placebo effect is a results in the patient’s death
psychological benefit from a Nonfeasance. Omission; omitting
compound that may not have the a drug dose that results in the
chemical structure of a drug effect. patient’s death
The placebo is effective in Malfeasance. Giving the correct
approximately one third of persons drug but by the wrong route that
who take a placebo compound. results in the patient’s death
INITIATIVES TO COMBAT DRUG
COUNTERFEITING
1. The role of the nurse is critical in
consumer education.
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

Chemical Name

constitutes a description of a drug using

a nomenclature of chemistry.

Generic Name

known as the nonproprietary name;

known also the most common drug

Lauro, VKV | Pharmacology 8

 ✓ The nurse must obtain a thorough health
name where the drug manufacturer
uses for a drug. history to determine all the
pharmacotherapeutic agents the patient is
Brand Name using.
Healers play a role in traditional health
known as the proprietary or trade name
practices in about 80% of the population
or the name for the drug manufactured
by one of the company often by the worldwide. Traditional healers usually
symbol have some practical knowledge of human
anatomy and physiology, pharmacology,
and pharmaceutical substances.
Chapter 3: Cultural and
Assimilation occurs when a less powerful
Pharmacogenetic Considerations
group changes its ways to blend in with
ETHNOPHARMACOLOGY
the dominant cultural group. Adults who
- is the study of drug responses that
immigrate to a new region usually take
may be unique to an individual owing
longer to assimilate than do younger
to social, cultural, and biologic
people.
phenomena.
Acculturation is the process by which a
- highlights the need for nurses to use
group adjusts to living within a dominant
knowledge and research from the
culture while at the same time maintaining
social sciences as well as the biologic
its original identity.
and physical sciences to provide
Complementary Health Practices that
holistic nursing care
combine traditional beliefs and
PHARMACOGENETICS
mainstream health practices.
- integrates the study of
Alternative Health Practices it is called
pharmacokinetics,
when a dominant group adopts health
pharmacodynamics, and variations of
practices from a nondominant group.
the predicted response to a drug due
Pharmacogenomics refers to the general
to genetic factors. The nurse must
study of all the different genes that
integrate knowledge of
determine drug behavior.
pharmacogenetics within patients’
cultural contexts.
Culture is defined as sets of learned
behavior and ideas that human beings
acquire as members of a 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 Chapter 3: Drug Interactions and Over-
Numerous cultural groups engage the-Counter Drugs
in the use of traditional health practices, Drug Interaction
which may include use of: teas, herbs, is defined as an altered or modified
spices, and special foods as well as action or effect of a drug as a result of
homeopathic remedies, poultices, and interaction with one or multiple drugs.
ointments. - It should not be confused with adverse
These practices can have neutral, drug reaction or drug incompatibility.
beneficial, or deleterious effects on a - An adverse drug reaction is an
patient’s health. undesirable drug effect that ranges
from mild untoward effects to severe

Lauro, VKV | Pharmacology 9

 toxic effects, including hypersensitivity reaction is different from photoallergy
reaction and anaphylaxis. in that it is not immune-mediated. The
Drug incompatibility onset of phototoxicity with erythema
is a chemical or physical reaction can be rapid, occurring within 2 to 6
that occurs among two or more drugs in hours of sunlight exposure.
vitro. In other words, the reaction occurs Pediatric and Geriatric
between two or more drugs within a Pharmacokinetic
syringe, IV bag, or other artificial
Geriatric Distribution
environment outside of the body.
Drug interactions can be divided into two
categories:
● Pharmacokinetic Interactions
● Pharmacodynamic Interactions
DRUG INTERACTIONS
Drug-Food
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.
Drug-induced Photosensitivity
reaction is a skin reaction caused
by exposure to sunlight. It is caused by
the interaction of a drug and exposure to
ultraviolet A (UVA) light, which can cause
cellular damage. Usually the skin area that
is exposed is affected.
2 types of photosensitivity reactions
1. Photoallergy
occurs when a drug (e.g.,
sulfonamide) undergoes activation in
the skin by ultraviolet light to a
compound that is more allergenic than
the parent compound. Because it
takes time to develop antibodies, Pediatric Distribution
photoallergenic reactions are a type of • GI absorption slower in infancy,
delayed hypersensitivity reaction. but absorption from intra-
2. Phototoxicity muscular injection is faster.
• In neonates common practice to
photosensitive drug undergoes
use IV preparations
photochemical reactions within the • Infant skin is thin and
skin to cause damage. This type of percutaneous absorption can
Lauro, VKV | Pharmacology
10

cause systemic toxicity (ex. If
potent steroids are applied too
extensively)
• Body fat content in infants low,
water content is high
• Lower Vd of fat soluble drugs
(diazepam) in infants
• Decrease plasma protein binding
of drugs in neonates (kernicterus
due to displacement of bilirubin
by sulfonamides)
• Blood-brain barrier is more
permeable in neonates and
young children, leading to and
increase risks of CNS adverse
effects
• At birth, the heaptic microsomal
enzyme system is relative
immature particularly in preterm
infant but after first four weeks it
matures rapidly
• Conversely hepatic drug
metabolism 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.
- Chloramphenicol can produce
grey baby syndrome in neonates.
GERIATRIC
Golden rule for drug therapy in
elderly
- Smallest number of drugs
- In lowest possible doses
- For shortest possible time
- In simplest regimen
PEDIATRIC PHARMODYNAMIC
Important Adverse Effects in Children
● With a few notable exceptions, drugs
in children generally have a similar
adverse effect profile to those in
adults.
Examples of Some Specific ADR
1. Chronic corticosteroid use: inhibit
growth
2. Tetracyclines: staining and
occasionally dental hypoplasia
3. Fluoroquinolone (ciprofloxacin):
damage growing cartilage
4. Metoclopramide: Dystonias more
frequently than in adults
5. Valproate: Hepatotoxicity is increase in
young children
6. Aspirin: Reye’s syndrome
GERIATRIC PHARMACODYNAMIC
Pharmacodynamic Changes:
● 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
● Avoid drugs with negligible or doubtful
benefits
● Think about the dose
● Think about drug formulation
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● Assume any new symptoms may be
due to drug side-effects
● Take a careful drug history
● Used fixed combinations of drugs
rarely
● Check compliance
● Think before adding a new drug to the
regimen
● Stopping is as important as Starting.

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