Beruflich Dokumente
Kultur Dokumente
Pharmacokinetics
What the body does to the drug
Dr Baba Sule Mahamma
Objectives
Define Pharmacology and its branches
Define what a drug is
State the different types of drug names
Define Pharmacokinetics (PK)
Explain
Absorption
Distribution
Natural
Plant (digitalis, belladonna, cinchona)
Animal (dry skin of toad adrenaline; insulin,
Cod liver oil -Vitamin A)
Mineral (Kaolin, Iron, Aluminium hydroxide)
Distribution
Metabolism
Elimination
Excretion
Toxicity
Absorption
Absorption is defined as the process
by which a drug proceeds from the
site of administration to the site of
measurement (?) (usually blood,
plasma or serum).
Parameters
Rate of absorption
Area under the concentration curve
(AUC)
Membranes and
Absorption
Hydrophilic
Lipid Bilayer
Heads Hydrophobic
Tails
Small, H2O, urea,
uncharged Swoosh!
CO2, O2, N2
to
Dose systemic
circulation
.
The absolute bioavailability
is the area under curve (AUC)
non-intravenous divided by
AUC intravenous
Distribution
The movement of drug from the blood
to and from the tissues
Distribution
The process of reversible transfer of
drug to and from the site of
measurement (usually blood or
plasma).
Rate and Extent of drug distribution is
determined by:
1. how well the tissues and/or organs are
perfused with blood
2. the binding of drug to plasma proteins
and tissue components
3. the permeability of tissue membranes
to the drug molecule (BBB, placenta).
Physicochemical properties of the drug
Characterised by volume of
distribution (Vd)
Volume of distribution (Vd)
Volume within which drug appears to be distributed
(Apparent Vd), if the concentration throughout the
body were equal to that in plasma (assuming single
compartment)
Determinants
Plasma protein binding (bounded and unbounded
drugs)
Albumin, lipoprotein, 1-acid glycoprotein,
globulins
Result in small Vd
Tissue binding
Protein
Fat
Result in large Vd
Protein Binding
Conjugation reactions
Condensation reactions
Metabolism contd.
Liver disease
Slows metabolism
Prolongs effects
Dose
adjustment/contraindications
Excretion
Defined as the irreversible loss of a
drug in a chemically unchanged or
unaltered form
Primary site kidney (liver important,
lungs, milk, faecal matter)
Renal excretion
Glomerular filtration (MW less than 10,
000, ie almost all drugs)
Renal tubular excretion cells of
proximal tubule actively transport (eg
OATs and OCTs)
Renal tubular reabsorption
Excretion contd.
Renal disease
Slows excretion
Prolongs effects
Time Amount
0 sec 6 mg
10 sec 3 mg
20 sec 1.5 mg
30 sec 0.75 mg