01.2 Pharmacokinetics Flashcards
Define bioavailability
The fraction of the dose that enters circulation
What is the bioavailability of an IV drug?
100%
How is oral bioavailability calculted from a plasma concentration against time graph?
The area under the curve is the bioavailability
What factors alter bioavailability?
First pass effect
Age
Drug formulation
What factors affect drug distribution?
Lipophilicity
Plasma protein binding
Tissue protein binding
Density of bind sites on tissues
How is volume of distribution calculated from a Vd time graph?
By extrapolating the curve back to time 0
What is Vd when the drug is only in the plasma?
~5L
What is Vd when the drug is in the ECF and ICF?
10-30L
What is Vd when the drug is very lipophillic and bound to tissue proteins?
100+ L
What are some cytochrome P450 inducers?
Carbamazepine Rifampicin Barbituates Phenytoin St Johns Wort
What are some cytochrome P450 inhibitors?
Sodium valproate Ciprofloxacin Sulphonamide Cimetidine Antifungals Amiodarone Isoniazid Erythromycin Clarythromycin Grapefruit juice
What is clearance of drugs dependant on?
Hepatic clearance
Renal clearance
Heart maintaining output so renal perfusion is maintained
How is half life associated with clearance?
Half life is inversely propoertional to clearance
What is 1st order kinetics?
Rate of elimination proportional to drug level
What is 0 order kinetics?
Rate of elimination is constant