Drug metabolism Flashcards
drug metabolism/biotransformaton is the CHEMICAL modification of lipophilic agents to produce more polar/hydrophilic product
T or F
T
drug metabolism can sometimes lead to chemical activation of inactive agents/drugs
give two examples of such drugs and their active form
Codeine(inactive form)- morphine
enalapril(inactive form) - enalaprilat
biotransformaton occurs only in the liver and involves both microsomal and non microsomal organs
T or F
F
it occurs in all cells of the body not just liver(main location)
other locations include
lungs, kidney, GIT, skin
during drug metabolism phase 1 must occur before phase 2
T or F
F
it could occur in any order
if present, phase 3 reactions involves
removal of drugs that have undergone phase 1 and 2 by P-glycoprotein transporters
phase 1 reactions are also called
Functionalization/non-synthetic
the mechanism of phase 1 reaction is via
addition or removal of functional groups from the drug
list 5 examples of phase 1 reaction
oxidation
reduction
hydrolysis
cyclization
decyclization
after phase 1 reaction drugs may be sufficiently polar for excretion
T or F
T
phase 1 is the true detoxification step in drug metabolism
T or F
F
phase 2
list 5 compounds used for conjugation in phase 2
glucoronide
sulfate
acetate
amino acid
glycine
microsomal enzymes are involved in phase 1 reactions only
T or F
F
1 and 2
microsomal enzymes are located where
on sEr
list 4 microsomal enzymes
Monooxygenases
CYP450
UDP - glucoronyl transferase
epoxide hydroxylase
non microsomal enzyme are found in
Plasma
cytoplasm
mitochondria
