Drug(s) with high extraction by the liver:
Drugs poorly extracted by the liver:
First pass pulmonary uptake > 65% of dose
Factors that affect first pass pulmonary effect magnitude
Large volumes of distribution:
Factor(s) influencing the volume of distribution:
Factor(s) influencing clearance (CL):
Most important organ for unchanged drug/drug metabolite elimination
Glomerular filtration:important factors
Passive renal tubular reabsorption:
Factor(s) influencing renal clearance:
Factor(s) affecting hepatic clearance:
Drugs which exhibit clearances > 6 ml/min./kg
Factor(s) which may change intrinsic drug clearance:
Capacity-limited elimination
Half-life = time required to decrease in other drug in the body by 50% during elimination. Assumption(s):
Factor(s) influencing drug half-life:
The definition of "context-sensitive" halftime is the length of time required for drug plasma concentration to fall 50% after continuous infusion
Number of half-lives required to go from one steady-state to another:
Bioavailability < 100% following oral dose administration:
Absorption rate proportional to the drug concentration dissolved in the gastrointestinal tract
Termination drug action
Drug-plasma protein binding
Renal clearance
Biotransformation: tends to convert a drug to a more hydrophobic (lipophilic) metabolite
Parent drug is altered by introducing or exposing a functional group such as -OH or NH2
Phase II characteristics: parent compound functional group linkages with
Property/properties of phase II conjugates:
Principal organ for biotransformation of drugs:
Factor/factors which may reduce drug bioavailability:
Localization of mixed function oxidase system:
Important microsomal enzyme/enzymes for drug biotransformation
Drug mechanism/mechanisms which may increase the amount of cytochrome P450 enzyme:
glucuronidation: