Pharmacology Flashcards
Combined P-GP and CYP3A4 inhibitors
Ketoconazole
Posa/voriconazole
Ritonavir
Combine P-GP and strong CYP3A4 inducers
Carbamazepine
Phenytoin
Rifampicin
St John’s Wort
Strong P-GP inhibitors and weak CYP3a4 inhibitors
Amiodarone
Calcium channel Blockers
Macrolides - erythro/azithromycin
Main determinant of maintenance dose
Clearance of dru
Clearance formula
Volume of blood cleared of drug per unit of time (volume/hr)
Elimination rate
clearance of drug (l/hr) x plasma drug concentration (mg/hr)
CYP3A4 inhibitors
Grape fruit juics Clarithromycin /erythromycin Diltiazem Fluconazole Ritonavir
Formula for constant steady state
Css = (DR x F) / CL - Vd
Competitive inhibitor Alcohol Dehydrogenase
fomepizole (a.k.a. 4-methylpyrazole)
Volume of distribution
Total amount of drug in body/plasma drug concentration
Loading dose
Volume of distribution x target plasma concentration
Steady state
Loading dose = Vd X CAS
HLA B5801
Allopurinol hypersensitivity syndrome
HLAB15:02
Cutaneous skin reactions
Carbamazepine, lamotrigine, phenytoin
Drugs that cause increased lithium concentration
Drugs that deplete Sodium ie diuretics
The two main determinants of hepatic clearance
hepatic extraction ratio and hepatic blood flow.
Hepatic extraction ratio is the fraction of the drug entering the liver in the blood which is irreversibly extracted during a pass through the liver.
The hepatic extraction ratio is determined largely by the free (unbound) fraction of the drug.