wk6 metabolsim and excretion Flashcards
phase 1 metabolsim
addition of polar groups through oxidation, reduction or hydrolysis, makes the drug more polar and prepares it for phase 2
phase 2 metabolism
conjugation with ionic groups. glutathione, acetyl, methyl. makes drug more water soluble
metabolsim of morphine
primary pathway is phase 2 metabolism. udp glucuronosyl transferase (ugt) is the enzyyme responsible. it conjugates glucuronic acid and makes glucuronide morphine metabolites.
metabolsim of praracetamol
primary pathway phase 2. and metabolites are paracetamol glucuronide/sulfate. however, in overdose, the metabolism shifts to phase 1 and produces the toxic metablite napqi by enzyme cyp2e1.. risks liver damage
what are prodrugs
drugs that need to be metabolized to become active like codeine to morphine by cyp2d6
two main routes of excretion
renal excretion (the major route) - glomerular filtration > active tubular secretion > tubular reabsorption
biliary - large polar molecules reabsorbed from intestine and reenter bloodstream