Phase II Metabolism
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UGT transfers ___________ to substrate
What is UDPGA and what isoforms utilize it?
- Uridine-5-diphosphate-a-D-glucuronic acid
- UGT1, UGT2A and UGT2B
What are UGT GI forms? What are they important for?
- UGT1A7, 1A8, 1A10
- 1st pass metabolism and affects bioavailability
___________ is the major enzyme for codeine glucuronidation
What disease is associated with mutation of UGT1A1 gene?
Mutation in UGT1A1 gene will cause what biological effect(ie.HTN is a biological effect)?
UGT1A1 mutation causes __________ which produces ___________ in the serum.
- Crigler-Najjar syndrome
- High bilirubin
Mutation in UGT1A1 (increase/decrease) in glucuronidation acivity that leads to ____ and ___?
- congenital nonhemolytic jaundice
- unconjugated hyperbilirubinemia
UGT1A1*28 allege mutation is associated with what disease?
Glibert syndrome causes __________ in blood serum due to mutation in _________ allele.
- increase in unconjugated bilirubin
Glibert syndrom is a mutation in what region of the gene?
Treating UGT1A1*28 mutation with _______ drug leads to severe delayed diarrhea and _________.
House cats have lots their ability to glucuronidate certain agents due to what characteristic?
Due to hypercarnivorous characteristic of house cats, they have lost _______ enzyme.
Loss of _________, cats can not glucuronidate ___&___ due to its increase in toxicity and slow clearance.
- APAP & acetysalicylic acid
During fetal development, __________ is the enzyme that is responsible for biotransformation of retinol?
Sulfotransferases are responsible for biotransfering what anticoagulant drug?
________ SULTs are located in the Golgi.
________ SULTs are mainly responsible for biotransfering sulfonate xenobiotics, bile acids.
What subfamily of GST is responsible for metabolism of inflammatory agents such as protaglandins.
Which isoform of GST causes a null mutation that leads to colon cancer.
Null mutation (GSTM1*0)
Which null mutation of GST subfamily leads to increase in chemotherapy side effects
Increase in incidence of asthma is associated with what polymorphism?
Null GST polymorphism
Overexpression ___________ leads to increase in resistance to nitrogen mustards binding to DNA.
______&______ isoforms of are known as fast acetylators which is responsible for ________ drug used for tuberculosis.
- NAT2*12 and NAT2*13
Slow acetylators can do lead to what when hydralazine is given?
tachycardia or hypotension
Poor metabolism of what drug by NAT lead to severe cadiogenic effects?
Inactivation of neurotransmittors is associated with what enzyme?
Polymorphisms in the enzyme resposible for metabolizing neurotransmittor can lead to what disease. (Name one)
What enzyme metabolizes antineoplastic and immunosupressive agents?
activation of _______ drug by ___________ into 6-MP.
- Glutathione S-transferase
6-MP is metabolized by ___________.
Polymorphisms in TPMT leads to what severe pathophysiologic effect, due to increased concentration of drug that are metabolized by TPMT.(Name one)
- life-threatening myelosuppression
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