Makes drug more hydrophilic and easy for excretion
Patient who are _____ will not receive analgesic effects from codeine (prodrug of morphine).
Poor/ intermediate metabolizers
This means none of the codeine gets metabolized into morphine, which is the active form of the drug
People who are ______ of drug will be susceptible to that drug’s severe adverse effects
Ultra metabolizers
Codeine is a substrate of ____
CYP 2D6 (phase 1 enzyme)
Which phase 1 enzyme preferentially metabolizes acidic drugs?
CYP2C19
Clopidogrel’s phase 1 enzyme is _____
CYP 2C19
Poor metabolizing CYP2C19, would result in ______ when on clopidogrel
Platelet aggregation
Which enzyme is the rate-limiting step in pyrimidine catabolism, which is important in getting rid of chemotherapy agents such as 5-FU and capecitabine?
Dihydropyrimidine Dehydrogenase (DPD)
Non-functioning DPD, as a result of a mutation lacking_____, would lead to ______
Exon 14
Increased chemotherapeutic toxicity
Phase II of drug metabolism involves _______, and enzymes include _____, _____
Conjugation
UGT1A1
TPMT
What is UGT1A1?
A phase 2 enzyme, responsible for inactivation of active metabolites of irinotecan, a prodrug for 1st line chemotherapy used alongside 5-FU and leucovorin for metastatic carcinoma
What is TPMT?
Phase 2 enzyme important in the metabolism of Azathioprine, 6-mercaptopurine, 6-thioguanine
T/F: Slow metabolizer in phase 2 enzymes would result in more ADR toxic effects
True
What is contraindicated in patients with G6PD deficiency?
Rasburicase
Which combination of nonsensical numbers and alphabet, if in deficiency, would expose the body to statin leading to myopathy?
OATP1B1 (organic anion transporter)
What is OATP1B1?
responsible for uptake of mainly weak acid drug like statins
T/F: Abacavir is an HIV drug, which can result in drug induced hypersensitivity, this is due to HLA polymorphism
True
Reduced expression of _____ and _____ could lead to excessive anti-coagulation and bleeding, respectivelya. This is seen with warfarin use
