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Pharmacodynamics Drugs/ Enzymes - Coggle Diagram
Pharmacodynamics Drugs/ Enzymes
N-Acetyltransferase (NAT2)
Slow Acetylators
isoniazid drug predisposed side-effects
peripheral neuropathy
Fast Acetylators
amonafide drug predisposed side-effects
myelosuppression
colorectal cancers from dietary carcinogens
Thiopurine-S-Methyltransferase (TMPMT) Polymorphism
Polymorphism catalyzes the deactivation of anticancer and anti-inflammatory drugs (eg.
mercaptopurine
, 6-thioguanine, azathioprine
variant enzyme has reduced stability/ activity; deficiency causes severe
hematopoietic toxicity
CYP Enzymes
Catalyze Oxidation
2C19
catalyzes oxidation of
clopidogrel
(also proton pump inhibitors, & selective serotonin re-uptake inhibitors)
2D6
Polymorphism in Oxidative metabolism leads to
accumulation of parent drugs including beta-blockers, anti-arrhythmics, antidepressants, neuroleptics
Poor metabolizers
less sensitive to drugs requiring CYP2D6 activation: codeine --> morphine; tamoxifen --> endoxifen
mnemonic:
D
if you are
d
epressed you go on opioids. or
D
for Co
D
eine
2C9 & VKORC1
Genetic polymorphisms affect
warfarin
metabolism/ clearance ---> homozygous variants have
inc... bleeding risk
Mnemonic: Think War-9
Uridine Diphosphate Glucuronosyltransferase (UGT)
Normal Enzyme Function
Glucoronidation of bilirubin, drugs, xenobiotics
UGT1A128 variant (7 TA repetes in promoter) results in
increased risk for neutropenia
following initiation of irinotecan treatment (CAMPTOSAR); also inc. risk for Gilbert's syndrome --> increased toxicity, myelosuppression, diarrhea