PHARMACOKINETICS
Prof. Erejuwa O. Omotayo
Department of Pharmacology & Therapeutics
Faculty of Basic Clinical Sciences
Ebonyi State University
LECTURE OBJECTIVES
You should be able to:
Differentiate between pharmacokinetics and
pharmacodynamics
Mention and define the various pharmacokinetic
processes or parameters
Mention and define the various pharmacokinetic
variables
Explain briefly the various transport mechanisms
of drugs in the body
Discuss the factors that affect absorption
INTRODUCTION
Pharmacokinetics: 2 Greek words – ‘Kinesis’
(which means movement) and ‘Pharmacon’
(which means drug).
That is, the movement of drug in the body.
Pharmacokinetics can, therefore, be defined as
the movement of the drug in and alteration of the
drug by the body.
It refers to what the body does to the drug or the
effect of the body on the drug.
PHARMACOKINETIC PROCESSES /
PARAMETERS
(ADME)
1.Absorption
2.Distribution
3.Metabolism
4.Excretion
PHARMACOKINETIC VARIABLES
1.Bioavailability Absorption
2.Volume of distribution
Distribution
3.Half life Metabolism
4.Clearance Excretion
ABSORPTION
Movement or passage of drug
from its site of administration into
the systemic/general circulation.
FACTORS AFFECTING
ABSORPTION
1. Biological membranes
2. Lipid-water solubility
3. Physical/dosage forms
(Disintegration and dissolution)
4. Molecular and particle sizes
5. Concentration
FACTORS AFFECTING ABSORPTION CONT.
6. Chemical nature and route of drug
administration
7. Area of absorptive surface
8. Vascularity of the absorbing surface
9. Presence of other substances
10. GI mobility/Diseases
FACTORS AFFECTING
ABSORPTION
1. BIOLOGICAL MEMBRANES
Transport mechanisms across
biological membranes
(a) Filtration
(b) Passive/Simple diffusion
(c) Facilitated diffusion
(d) Active transport
PROCESS OF FACILITATED DIFFUSION
FACTORS AFFECTING
ABSORPTION CONT.
2. Lipid water solubility
3. Physical/dosage forms
(Disintegration and dissolution)
4. Molecular and particle sizes
5. Concentration
FACTORS AFFECTING ABSORPTION CONT.
6. Chemical nature and route of drug
administration
7. Area of absorptive surface
8. Vascularity of the absorbing surface
9. Presence of other substances
10. GI mobility/Diseases
PHARMACOKINETIC VARIABLE FOR
ABSORPTION
The pharmacokinetic variable for
absorption is bioavailability.
Bioavailability: percentage or fraction or
proportion of the administered dose of the
drug that reaches systemic circulation in an
unchanged form irrespective of the route of
drug administration.
DISTRIBUTION
Distribution refers to the passage of the
drug from systemic circulation to other
tissues that initially had no drug.
Redistribution (Heart, kidney and brain)
Plasma protein binding
Localization/tissue binding
PHARMACOKINETIC VARIABLE FOR
DISTRIBUTION
The pharmacokinetic variable for
distribution is volume of distribution (Vd).
Vd: Apparent volume into which the drug is
distributed to provide the same
concentration as it is currently in blood
plasma.
Vd = amount of the drug in the
body/amount of drug in the plasma
concentration.
PRACTICE
QUESTIONS
PRACTICE QUESTION 1
The following is not a pharmacokinetic
parameter
(a) Distribution
(b) Metabolism
(c) Absorption
(d) Excretion
(e) Bioavailability
PRACTICE QUESTION 2
Distribution refers to:
(A). Process that defines the drug entrance
into the systemic circulation from the site
of administration or application
(B). An abstract concept which determines
where is a drug distributed
(C). Chemical processing of drugs before
they will leave an organism
(D). Disposition of a drug throughout the
body from the general circulation
(E). Elimination of drugs from the body
PRACTICE QUESTION 3
The rate of absorption of a drug is affected
by the following EXCEPT
(a)Route of drug administration
(b)Solubility of the drug
(c)Site of administration
(d)Patient’s gender
(e)Presence of other substances
PRACTICE QUESTION 4
Pharmacokinetics is the effect of the ------
and pharmacodynamics is the effect of the
…...
(a) Drug on a drug; Body on the drug
(b) Body on the drug; Drug on a drug
(c) Drug on the body; Body on the drug
(d) Body on the drug; Drug on the body
(e) Drug on a drug; Drug on a drug
PRACTICE QUESTION 5
What does pharmacokinetics include?
(A)Complications of drug therapy
(B)Drug biotransformation in the organism
(C)Influence of drugs on metabolism
processes
(D)Effects of drugs on genes
(E)None of the above
PRACTICE QUESTION 5
Pharmacokinetics include EXCEPT
(a) Deals with the physical and biochemical
effect of drugs and their mechanisms
of action
(b) Examines how drugs are eliminated
from the body
(c) Is the study of how drugs are handled
in the body including absorption,
distribution, metabolism and excretion
(d) Is concerned with how drugs reaches
various organs of the body
(e) What the body does to the drug
PRACTICE QUESTION 6
The main mechanism of most drugs
absorption in GIT is
(A). Active transport
(B). Filtration
(C). Endocytosis
(D). Facilitated diffusion
(E). Passive diffusion
PRACTICE QUESTION 7
The following are pharmacokinetic
parameters except
(a) Distribution
(b) Excretion
(c) Metabolism
(d) Clearance
(e) Absorption
PRACTICE QUESTION 8
The following are pharmacokinetic
variables except
(a) Half-life
(b) Biotransformation
(c) Bioavailability
(d) Volume of distribution
(e) Clearance
PRACTICE QUESTION 9
The subjects of pharmacokinetics include
EXCEPT
(A). Route of administration of the drug.
(B). Biotransformation of active
substance.
(C). Distribution of active substance within
the organism.
(D). Binding of the active substance with
plasma albumins.
(E). Adverse effects of the drug
PRACTICE QUESTION 10
Drugs mostly cross biological membranes
by
(a). Active diffusion
(b). Passive diffusion
(c). Active transport
(d). Carrier mediated transport
(e). All of the above
PRACTICE QUESTION 11
Which of the following transport system is
saturable?
(a). Passive diffusion
(b). Aqueous diffusion
(c). Lipid diffusion
(d). Active transport
(e). None of the above
PRACTICE QUESTION 12
Which of the following is NOT a
pharmacokinetic process?
(a) Alteration of the drug by liver enzymes
(b) Drug metabolites are removed
in the urine
(c) Movement of drug from the gut into
general circulation
(d) The drug causes dilation of coronary
vessels
(e) The drug is readily deposited in fat
tissue
