GBP8 Flashcards
(14 cards)
How are water soluble drugs excreted
Liver or kidney
How are lipid soluble drugs excreted
Metabolised by the liver gut or blood then made water soluble ready for excretion by liver or kidney
How are volatile drugs excreted
Lungs
What can be the biological consequences of drug metabolism
inactivation- phenytoin, warfarin, suxamethonium
activation- clopidogrel, dabigatran, paracetamol, halothene
What is the toxic metabolite of paracetamol and what is it normally mopped up by
NAPQ1, mopped up by glutathine
What are the two phases in metabolism
phase 1 - introduction or unmasking of functional group, some increase in water solubility
phase 2 - conjugation with endogenous chemical at functional centre, great increase in water solubilty
What are oxidations done by in the liver
cytochrome p450
Why is cyto.p450 important in the liver
has many isoforms due to genetic variation or because they are inducible
How are alcohols oxidised in the liver
alcohol dehydrogenase
How are amines oxidised
monoamine oxidase`
What is beneficial about conjugation
makes the metabolite much more water soluble
What types of conjugation are there
glucuronidation, sulphation, glycine conjugation, acetylation
What is significant about age and metabolism
extreems of age both have reduced metabolism
What interaction mechanisms exist
inhibition, induction