EXAM QUESTION 2

PHARMACOKINETIC PROCESSES
1. absorption- movement of drug from from it s site of administration in to the
circulation
2. Distribution when a drug gained access to blood stream, gets distributed to other
tissues that initially has no drug.
3. Biotransformation- chemical alteration of the drug in the body
4. Excretion- passage out of systemically absorbed drug.
MECHANISM OF DRUG TRANSPORT ACROSS THE MEMBRANE
1. passive diffusion- drug diffuses across membrane in the direction of its
concentrated gradient, the membrane plays no role. Lipid soluble drugs diffuses
by dissolving in the lipoidal matrix of the membrane
2. specialized transport-can be carrier mediated or pinocytosis
carriers- drug combine with carrier present in the membrane and the complex
then translocates from one face of the membrane to the other. It can be active
transport movement(movement against concentration gradient, needs energy and
metabolic poison) and passive diffusion ( more rapid but along concentration
gradient and does not need energy)
pinocytosis- transport across cell in form by formation of vesicles. For proteins and
other big molecules
3. filtration- passage of drug through aqueous pores n the membrane or through para
cellular spaces.
ABSORPTION
Movement of drug from site of administration in to circulation
FACTORS AFFECTING ABSORPTION
1. Solubility-suspension of colloidal preparation are absorbed more slowly han
aqueous solution
2. Dosage- the larger the dose, greater the effect , until a maximum effect is
achieved.
3. route of drug administration- more quieckly from large surfaces areas
4. blood flow- high vascularized organs (small intestine) have greatest absorption
ability
DISTRIBUTION
When a drug access to blood stream, it gets distributed to other tisses that initially have
no drug, concentration gradient being in the direction of the plasma to tissue
FACTORS EFFECTING DISTRIBUTION
1. Blood flow
2. capillary permeability

3.
4.
5.
6.

binding to plasma proteins(limits access to cellular compartments)

drug structure (small lipophilic molecules easier to distribute)
blood brain barrier (lipid soluble drugs cross all barriers but not water-soluble)
cellular binding of drugs

EXCREATION
Passage out pf systemically absorbed drug eliminated from the body .
FACTORS EFFECTING EXCRETION
1. ionization of drug ( unionized drug are well reabsorbed so decrease excretion)
2. concentration of drug increase- excretion increase
3. pH of drug acidic drug excretion increase in alkali urine and vice versa
4. rate of metabolism and excretion
5. glomerular filtration rate
6. active renal tubular secretion and reabsorption
7. renal blood flow increase- excretion increase
PHARMACOKINETICS PARAMETERS
BIOAVAILABILITY
VOLUME OF DISTRIBUTION (Vd)
Volume of distribution is a quantitative estimate of the tissue localization of the drug
Vd = total amount of drug in body
Plasma drug concentration
CLEARANCES:
Its the theoretical volume of plasma from which the drug is completely removed in unit
time
CL = rate oof eliminantion
Plasma drug concentration
PLAMA HALF LIFE (t1/2)
It is the time taken for its plasma concentration to be reduced to half of its original value.
The time when the concentration of the drug becomes exactly half of the peak volume.
T1/2=0.693 V
CL
Measurement of t1/2 allows circulation of the elimination rate constant (K el) from the
formula
K el = 0.693
t
K el is the fraction of drug present at any time that would be eliminated in unit time