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