01 Introduction to Basic

Principal of Pharmacology
Nomi made

 1.1 Which one of the following statements is correct?

A. Weak bases are absorbed efficiently across the
epithelial cells of the stomach.
B. Coadministration of atropine speeds the absorption
of a second drug.
C. Drugs showing a large V can be efficiently removed
by dialysis of the plasma.
D. Stressful emotions can lead to a slowing of drug
absorption.
E. If the V for a drug is small, most of the drug is in the
extraplasmic space.
d

 Which one of the following is true for a drug whose

elimination from plasma shows first-order kinetics?
A. The half-life of the drug is proportional to the drug
concentration in plasma.
B. The amount eliminated per unit of time is constant.
C. The rate of elimination is proportional to the plasma
concentration.
D. Elimination involves a rate-limiting enzymic reaction
operating at its maximal velocity (V ).
E. A plot of drug concentration versus time is a straight
line
m

 A patient is treated with drug A, which has a high affinity for albumin
and is administered in amounts that
do not exceed the binding capacity of albumin. A second drug, B, is
added to the treatment regimen. Drug B
also has a high affinity for albumin but is administered in amounts
that are 100 times the binding capacity of
albumin. Which of the following occurs after administration of drug
B?
A. An increase in the tissue concentrations of drug A.
B. A decrease in the tissue concentrations of drug A.
C. A decrease in the volume of distribution of drug A.
D. A decrease in the half-life of drug A.
E. Addition of more drug A significantly alters the serum concentration
of unbound drug B.

The addition of glucuronic acid to a drug:

A. Decreases its water solubility.
B. Usually leads to inactivation of the drug.
C. Is an example of a Phase I reaction.
D. Occurs at the same rate in adults and
newborns.
E. Involves cytochrome P450.

 Drugs showing zero-order kinetics of elimination:

A. Are more common than those showing firstorder kinetics.
B. Decrease in concentration exponentially with
time.
C. Have a half-life independent of dose.
D. Show a plot of drug concentration versus time
that is linear.
E. Show a constant fraction of the drug eliminated
per unit of time.

 A drug, given as a 100-mg single dose, results in a peak

plasma concentration of 20 Ag/mL. The apparent
volume of distribution is (assume a rapid distribution and
negligible elimination prior to measuring the peak
plasma level):
A. 0.5 L.
B. 1 L.
C. 2 L.
D. 5 L.
E. 10 L.

 A drug with a half-life of 12 hours is

administered by continuous IV infusion.
How long will it take for the
drug to reach ninety percent of its final
steady-state level?
A. 18 hours.
B. 24 hours.
C. 30 hours.
D. 40 hours.
E. 90 hours.

 Which of the following results in a

doubling of the steady-state
concentration of a drug?
A. Doubling the rate of infusion.
B. Maintaining the rate of infusion but
doubling the loading dose.
C. Doubling the rate of infusion and doubling
the concentration of the infused drug.
D. Tripling the rate of infusion.
E. Quadrupling the rate of infusion.

 Which of the following statements is correct?

A. If 10 mg of Drug A produces the same response as
100 mg of Drug B, Drug A is more efficacious than Drug
B.
B. The greater the efficacy, the greater the potency of a
drug.
C. In selecting a drug, potency is usually more
important than efficacy.
D. A competitive antagonist increases the ED50.
E. Variation in response to a drug among different
individuals is most likely to occur with a drug showing a
large therapeutic index.

 Variation in the sensitivity of a

population of individuals to increasing
doses of a drug is best determined by
which of the following?
A. Efficacy.
B. Potency.
C. Therapeutic index.
D. Graded doseresponse curve.
E. Quantal doseresponse curve

 Which of the following statements most

accurately describes a system having spare
receptors?
A. The number of spare receptors determines the
maximum effect.
B. Spare receptors are sequestered in the cytosol.
C. A single drugreceptor interaction results in
many cellular response elements being activated.
D. Spare receptors are active even in the absence of
agonist.
E. Agonist affinity for spare receptors is less than
their affinity for nonspare receptors

 pharmakon means _____

Drugs

 The study of the interaction of

chemicals with living systems. Is
______
Pharmacology

 Is the scientific study of the origin,

nature, chemistry, effects, and uses
of drugs
Pharmacology

 Deals with how drugs interact within

biological systems to affect function
Pharmacology

 Branch of knowledge that has to do

with the chemicals that have
biological effect
Pharmacology

 is a scientist who specializes in the

study of pharmacodynamics,
employing all kinds of biochemical,
physiological and other techniques
Pharmacologist

 chemicals that act on living systems

at the molecular level
Drugs

 Which of the following are the xample of

drugs
Hormones
Neurotransmitters
Growth factors
Local autocrine factors
Drugs (Pharmaceuticals)
Toxic agents in the environment
All of above..ok

 the study of drugs used for the

diagnosis, prevention, and treatment
of disease
Medical pharmacology

 Area of pharmacology concerned

with unusual responses to drugs
caused by genetic differences
between individuals.
Pharmacogenomics

Just read.
Responses that are not found in the
general population, such as general
toxic effects, allergies, or side
effects, but due to an inherited
trait that produces a reduced or
enhanced response to a drug.
Pharmacogenomics

Responses that are not found in the general

population, such as general toxic effects,
allergies, or side effects, but due to an
inherited trait that produces a diminished
or enhanced response to a drug are due to
__________

Differences in Enzyme Activity

Example of enzymes activty are

Acetylation polymorphism
Butylcholinesterase alterations
Cytochrome P450 aberration

 study of the effect of drugs on

populations; particularly dealing
with the influence of genetics are
important
Pharmaco-epidemiology

 study of the cost effectiveness of

drug treatments; medications is of
worldwide concern, particularly
among certain groups such as the
elderly and AIDS
Pharmaco-economics -

 Medical science concerned with the

use of drugs in the treatment of
disease
Pharmaco-therapeutics

 Pharmacology provides a rational

basis for pharmacotherapeutics by:
a. explaining the mechanisms and effects
of drugs on the body
b. the relationship between dose and drug
response.

Both a and b ok

 Human studies are then used to

determine the efficacy and safety of
drug therapy
Clinical trials

 Study of poisons and organ toxicity

Toxicology

 Harmful effects of drugs and other

chemicals
Toxicology

 Mechanisms by which these agents

produce pathologic changes, disease,
and death
Toxicology

 Relationship between the dose and

the resulting tissue concentration
and biologic effects that the agent
produces
Toxicology

 Most drugs have toxic effects at high

enough doses and may have adverse
effects related to toxicity
at____________
therapeutic dose

 Is what the drug does to the body

Pharmacodynamic

 Interaction of drugs with cellular

proteins, such as receptors or
enzymes, to control changes in
physiological function of particular
organs.
Pharmacodynamic

 Drug-Receptor Interactions
Binding

 Dose-Response
Effect

 Mechanism of action, Pathways of

drugs is _____
Signal Transduction

 Is what the body does to the drug.

Pharmacokinetics

 The magnitude of the

pharmacological effect of a drug
depends on its ________
concentration at the site of action
Pharmacokinetics

 Relationship between the drug dose

and the plasma drug concentration
over time
Pharmacokinetics

 Study the fate(mustaqbil) of drugs

once ingested and the variability
(tabdili)of drug response in varying
patient populations
??????
Pharmacokinetics

 How the body absorbs, distributes,

metabolizes, and excretes drugs
(ADME)
Pharmacokinetics

 Calculation of various rates that

brings a quantitative component to
assessing drug action
Pharmacokinetics

 Drug dosage and integration is

_______
Pharmaceutical

 ADME is in _______
Pharmacokinetics

 Drug/ receptor interaction is ______

Pharmacodynamics

 Drug effect or response\ is _____

Pharmacotherapeutics

 morphine, cocaine, atropine, quinine

are from ______ source
Natural source/Plant Alkaloids-

 morphine, cocaine, atropine, quinine

are from ______ source

 The main source of antibiotic is

Microorganism

 The natural source of hormones is

______
Animal

 The natural source of lithium is ______

Minerals

 Aspirin, barbiturates, and local

anesthetics (e.g., procaine) are
_______
Synthetic Drugs

 morphine is a derivative of ______

oxycodone

 chemical agents that uniquely

interact with specific target
molecules in the body, thereby
producing a biological effect
Drugs

 Drugs, as well as hormones,

neurotransmitter, autocoids and
toxins can make possible the transfer
of information to cells by interaction
with specific receptive molecules
called _____________
receptors

 ________can be stimulatory or
inhibitory
Drugs

 _______interact with biological

systems in ways that mimic,
resemble or otherwise affect the
natural chemicals of the body
Drugs

 Protamine act by its _______ property

acidic or basic properties

 Amphotericin act by its _____

properties
surfactant properties

 Astringents has the ability to _____

denature proteins

 laxatives, diuretics has the properties

of ____
osmotic properties

 Which of the following drugs have

osmotic properties
Laxatives, Diutetics

 Drugs has physicochemical

interactions with membrane lipids is
_____
general and local anesthetics

 Most drugs combine (bind) with

specific receptors to produce ________
response

 Drugs binding takes place by precise

physicochemical and steric
interactions between specific groups
of the drug and the _______
receptor.

 ______is the tendency of drug to bind

with a receptor
Affinity

 The maximal effect produce by a

drug is called _______
Efficacy

 The power of a drug to produce the

desired effect is called_______
Potency

 It drugs bind to receptors and

activate them is _______
Agonist

 produce a lower response, at full receptor

occupancy

partial agonists

 produce full response_____

Full agonist

 ________bind to receptors but do not

activate them
Antagonist

 The primary action of _________is to

prevent agonists (other drugs or
endogenous regulatory molecules)
from activating receptors.
Antagonist

 Sometimes also called inverse

agonists
antagonists

 In the presence of a fixed

concentration of agonist, increasing
concentrations of a reversible
________progressively inhibit the
agonist response
competitive antagonist

 counteract the effects of

heparin_____
Or antidote of heparin is ____
Protamine

 sometimes used to oppose the

hyperglycemic effects of a
glucocorticoid hormone
Insulin

 actions of the ________hormones lead

to increased blood sugar, an effect
that is physiologically opposed by
insulin.
glucocorticoid

 Insulin, Norepinephrine, estrogen are

____classification receptor
Pharmacological

 Which of the following are the

example of biological and
biochemical receptor
cAMP

 ____ is a molecular and structural

classification of receptor
5HT1A

 mediate the actions of endogenous

chemical signals, neurotransmitters,
autacoids, and hormones
Regulatory proteins

 Na + /K + -ATPase, the membrane

receptor for cardioactive digitalis
glycosides are the example of ____
protein receptor
Transport proteins

 tubulin, the receptor for colchicine,

an anti-inflammatory agent
Structural proteins

 Which of the following are the

example of G-Protein-linked receptors
Serotonin
Muscarinic
Dopaminergic
Noradrenergic
All of above/Except

 Tyrosine kinase
Enzyme receptors

Ligand-gated ion channel receptors

Nicotinic
GABA
glutamate

 INTRACELLULAR AND NUCLEAR

RECEPTORS are
Hormone receptors
Autocoid receptors
Growth factors receptors
Insulin receptors
All of above/Except one.

 _____Cross the plasma membrane

and act on intracellular receptors
Binding to specific DNA sequences
(response elements) near the gene
whose expression is to be regulated
Lipid-soluble ligands/Agent

 WHY BE CONCERNED ABOUT HOW

DRUGS WORK?
FDA Approved and Unapproved Uses
Interactions with Other Drugs
Adverse Effects and Contraindications
All of Above..or Except oneok

 WHY BE CONCERNED ABOUT HOW

DRUGS WORK?
new modalities for using drugs
new indications for drugs
new concerns regarding risk-benefit

 Causes of Variability in Drug Response

related to the biological system
1. Body weight and size
2. Age and Sex
3. Genetics - pharmacogenetics
4. Condition of health
5. Placebo effect
All of Above..Except one..ok

 Causes of Variability in Drug

Response related to the conditions of
administration are ______
1. Dose, formulation, route of
administration.
2. Resulting from repeated
administration of drug
3. Drug interactions

Drug interactions???
chemical or physical;
GI absorption;
protein binding/distribution;
metabolism (stimulation/inhibition);
excretion (pH/transport processes);
receptor (potentiation/antagonism);
changes in pH or electrolytes.

 ________is the study of drug

absorption, distribution within body,
and drug elimination over time.
Pharmacokinetics

 ______depends on the route of

administration
Absorption

 ______depends on how soluble the

drug molecule is in fat (to pass
through membranes) and on the
extent to which the drug binds to
blood proteins (albumin)
Drug distribution

 _______is accomplished by excretion

into urine and/or by inactivation by
enzymes in the liver
Drug elimination

 This barrier is permeable to many drug

molecules but not to others, depending on
their lipid solubility.
Cell Membranes:

 Small pores, 8 angstroms, permit small molecules

such as alcohol and water to pass through.
Cell Membranes:

 Pores between the cells are larger

than most drug molecules, allowing
them to pass freely, without lipid
solubility being a factor.
Walls of Capillaries:

 This barrier provides a protective

environment for the brain.
Blood/Brain Barrier:

 Speed of transport across this barrier

is limited by the lipid solubility of the
psychoactive molecule.
Blood/Brain Barrier:

 ________ barrier separates two

distinct human beings but is very
permeable to lipid soluble drugs.
Placental Barrier

 Dependent upon its route of

administration and target area
Drugs distribution

 Cell membranes, consisting of 3

layers,
2 layers of water-soluble
complex lipid molecules
(phospholipid) and
a layer of liquid lipid, sandwiched
within these layers

 The permeability of a cell membrane,

for a specific drug, depends on a
ratio of its_____
water to lipid solubility

 drugs may exist as a mixture of two

interchangeable forms, either ______
or ______
water (ionized-charged)
lipid (non-ionized) soluble

 In water soluble form, drugs cannot

pass through________
lipid membranes

 Majority f the drugs is excreted

through kidney _____
Glomerulus and tubular

 Minor drug is excreted through

kidney _____
Metabolism

 Majority of drug is eliminated though

liver is by _____
Metabolism

 Help to convert a lipid soluble to

more water soluble molecule to
excrete in kidney
Liver

 Possibility of active metabolites with

same or different properties as
parent molecule
Liver

 Is the drug metabolized via a specific

hepatic isoenzyme?
Substrate

 Does a specific drug inhibit a specific

hepatic isoenzyme?
Inhibitor

 Would expect this to interfere with

drug inactivation
Inhibitor

 does a specific drug enhance a

specific hepatic isoenzyme?
Inducer

 Would expect this to speed up drug

inactivation
Inducer

 1.1 Which one of the following statements is

correct?
A. Weak bases are absorbed efficiently across the
epithelial cells of the stomach.
B. Coadministration of atropine speeds the absorption of
a second drug.
C. Drugs showing a large Vd can be efficiently removed
by dialysis of the plasma.
D. Stressful emotions can lead to a slowing of drug
absorption.
E. If the Vd for a drug is small, most of the drug is in the
extraplasmic space.
View Answer

 P.24
1.2 Which one of the following is true for a drug whose
elimination from plasma shows first-order kinetics?
A. The half-life of the drug is proportional to the drug
concentration in plasma.
B. The amount eliminated per unit of time is constant.
C. The rate of elimination is proportional to the plasma
concentration.
D. Elimination involves a rate-limiting enzymic reaction
operating at its maximal velocity (Vm).
E. A plot of drug concentration versus time is a straight line.
.

 1.3 A patient is treated with drug A, which has a high

affinity for albumin and is administered in amounts that
do not exceed the binding capacity of albumin. A second
drug, B, is added to the treatment regimen. Drug B
also has a high affinity for albumin but is administered
in amounts that are 100 times the binding capacity of
albumin. Which of the following occurs after
administration of drug B?
A. An increase in the tissue concentrations of drug A.
B. A decrease in the tissue concentrations of drug A.
C. A decrease in the volume of distribution of drug A.
D. A decrease in the half-life of drug A.

 1.4 The addition of glucuronic acid to a

drug:
A. Decreases its water solubility.
B. Usually leads to inactivation of the
drug.
C. Is an example of a Phase I reaction.
D. Occurs at the same rate in adults and
newborns.
E. Involves cytochrome P450.

SAQs Introduction to
Pharmacology
Nomi made.

SAQ
What is the relationship between Pharmacokinetic and
Pharmacodynamics

SAQs
Enlist the source of drug
1. Natural product
2. Synthetic drugs
3. Pharmaceutical preparation

SAQs
List the type of receptor made of
protiesn

i. G protein-linked
ii.Ligand gated channels
iii.Intracellular

SAQs
What is pharmacology?

The study of the interaction of

chemicals with living systems.

S.A.Qs
What is Drugs
chemicals that act on living systems
at the molecular level

SAQs
Drug name ( Proprietary and Non-proprietary)
acidic or basic properties (e.g. antacids,
protamine),
surfactant properties (amphotericin),
ability to denature proteins (astringents),
osmotic properties (laxatives, diuretics), or
physicochemical interactions with membrane
lipids (general and local anesthetics).
Not confirm Answer?????

SAQs
List Pharmacology classification
1. Medical pharmacology
2. Pharmacogenomics
3. Pharmacoepidemiology
4. Pharmacoeconomics
5. Pharmacotherapeutics
6. Toxicology
7. Pharmacodynamic
8. Pharmacokinetics

SAQs
List the Drugs and their sources
Natural product
Plant Alkaloids- morphine, cocaine, atropine, quinine
Microorganisms- Antibiotics
Animals- Hormones
Minerals- lithium

Synthetic drugs
Aspirin, barbiturates, and local anesthetics (e.g.,
procaine)
Semisynthetic derivatives, e.g., morphine derivative
oxycodone

Pharmaceutical preparation

SAQs
List the Classification of receptor with
example
1. Pharmacological

Mediator (i.e. Insulin, Norepinephrine, estrogen)

2. Biophysical and Biochemical

Second messenger system (i,.e. cAMP, PLC, PLA)

3. Molecular or Structural

Subunit composition (i.e. 5HT1A )

4. Anatomical

5.

Tissue (i.e muscle vs ganglionic nAChRs)

Cellular (i.e. Membrane bound vs

Intracellular)

Formula: Pha-Bio-Mol_Ana_Cel

Jis ka akir main ..ase aye wo effeter honga

 a transmembrane receptor protein

whose intracellular enzymatic
activity is regulated by
a ligand that
a ligandbinds toatransmembra
a site aon thegated
proteins
transme
a
ne receptor
mbrane
transmembran
transme
extracellular
protein whosedomain
ion
a lipidsoluble
ligand
that
crosses
the
membran
e and
acts on
an
intracellu

intracellular
enzymatic
activity is
regulated by
a ligand that
binds to a site
on the
proteins
extracellular
domain

mbrane
receptor
that
binds
and
stimulate
sa
protein
tyrosine
kinase

channel
that can
be
induced
to open
or close
by the
binding
of a

e receptor
protein that
stimulates a
GTP-binding
signal
transducer
protein (G
protein), which
in turn
modulates

SAQ Pharmacokinetic

SAQ: List the route of administration

of drugs

SAQs: Drug Delivery

Systems
Tablets
Injections
(Syringe)
Cigarettes
Beverages
Patches
Suppositories

Candy
Gum
Implants
Gas
Creams
Others?

SAQ: Enlist the types of membrane

from where the drugs are transported

Cell Membranes
Walls of Capillaries
Blood/Brain Barrier
Placental Barrier