Pharmacokinetics Flashcards
Absorption
Process by which unchanged drug proceeds from the site of administration to the site of measurement
Bioavailability
Fraction of unchanged drug reaching the systemic circulation following administration by any route
Bioequivalence
90% confidence interval of the ratios of the population average estimates of AUC, Cmax and Tmax for the test and reference formulations lie within a pre established bioequivalence limit, usually 80-125%
Therapeutic equivalence
Comparable clinical effectiveness and safety between related products
First pass effect
To reach general circulation, a drug given orally must pass through the liver via the portal system
Distribution
Reversible transfer of drug from one location to another within the body
Volume of Distribution
Fluid volume that would be required to contain all of the drug in the body at the same concentration in the blood or plasma.
Vd = amt. of drug in body/plasma drug conc. = X/Cp
Phase I Reactions
Convert the parent drug to a more polar metabolite by introducing or unmasking a functional group
Inducer
Decrease the conc. Of drug, decrease efficacy and increase metabolism
Inhibitor
Increase conc. Of drug, increase toxicity and decrease metabolism
Phase II Biotransformation
Conjugation reaction
Metabolized by covalent addition of an endogenous species such as sugar or amino acid
Converts a lipophilic drug into a more polar product
Conjugation reactions
Glucoronidation by UDP glucuronosyltransferases
Sulfation/sulfonation by STs
Acetylation by acetyltransferases
Clearance
Volume of blood from which all drug would appear to be removed per unit time
Half-Life
Time required for the drug concentration to fall by half
First order kinetics
Constant fraction of a drug is eliminated per unit time
Zero order kinetics
Constant amount of drug eliminated per unit time
ER:F
Inverse
Cl:t1/2
Inverse
fu(p):Vd
Direct
fu(t):Vd
Inverse
t1/2:Vd
Direct
ER:First pass
Direct
Css:t1/2
No relationship
Time to Css:t1/2
Direct
Absorption
Process by which unchanged drug proceeds from the site of administration to the site of measurement
Bioavailability
Fraction of unchanged drug reaching the systemic circulation following administration by any route
Bioequivalence
90% confidence interval of the ratios of the population average estimates of AUC, Cmax and Tmax for the test and reference formulations lie within a pre established bioequivalence limit, usually 80-125%
Therapeutic equivalence
Comparable clinical effectiveness and safety between related products