Term
| Drugs/mnenomic associated with 3A4? |
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Definition
Substrates: benzos, CCBs, cyclosporine, macrolide abx, immunosuppressants
Inducers: Rifampin, Dexamethasone, Phenytoin, St. John’s wort
Inhibitor: Ritonavir |
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Term
| Drugs/mnenomic associated with 3A5? |
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Definition
| Tacrolimus. In nonexpressors of 3A5, drug levels are 1.5-2x higher |
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Term
| Drugs/mnenomic associated with 3A7? |
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Definition
| clinical impact is unclear |
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Term
| Drugs/mnenomic associated with Amplichip? |
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Definition
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Term
| Drugs/mnenomic associated with 1A2? |
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Definition
Lots of C's associated with the '1'!
1 (customer), Chris, gets Clozapine and Caffeine. (substrates)
Inducers: He Smokes and eats Chargrilled and Cruciferous vegetables. |
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Term
| Drugs/mnenomic associated with 2B6? |
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Definition
BICE.
Substrates: Bupropion, Ifosfamide (prodrug), Cyclophosphamide (prodrug), Efavirenz (mostly 2B6, but also 3A4 which is minor)
60% of Papua New Guineans have decreased activity of 2B6. |
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Term
| Drugs/mnenomic associated with 2C9? |
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Definition
War? Funny you SAID we would Lose.
Warfarin, Phenytoin, NSAIDs, losartan (prodrug)
Warfarin: patients with *3/*3 variant need lowest dose. Wild allele (*1) needs highest dose.
Phenytoin: if homozygous for *2 or *3 variants, also need dose reduction.
NSAIDs: inc GI bleeding and inc CV risk
Losartan: prodrug, so dec CYP2C9 activity will decrease therapeutic benefit. |
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Term
| Drugs/mnenomic associated with 2C19? |
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Definition
Funny that Vori is 19 and now needs Clopidogrel, PPIs, SSRIs.
Phenytoin (but more activity with 2C9), Voriconazole, clopidogrel (prodrug), omeprazole, citalopram/escitalopram.
PM (non-func), EM (inc activity), RM (wild).
Vori is asian, 14% Chinese and 70% pacific islanders are PM! |
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Term
| Drugs/mnenomic associated with 2D6? |
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Definition
2 D ('to the') BAHA CAT.
B-blockers, Antipsychotics (Haloperidol), Antidepressants, Codeine (prodrug), Atomoxetine, Tamoxifen (prodrug)
PM (lacking), IM (dec activity), EM (wild), UM (2-13 gene copies)
Effects of PM:
BB: inc SE hypotension
Antidepressants: inc SE (extrapyridimal, parkinson-like)
Codeine: cant convert to morphine so stays in pain
Atomoxetine: inc SE
Tamoxifen: prodrug, so PM sees dec therap benefit and increased cancer recurrence :( |
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Term
| Drugs/mnenomic associated with 2E1? |
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Definition
Lots of A's
Substrates: APAP, alcohol, (halogenated) anesthetics
Inducers: Obesity!, alcohol, nicotine (not smoking), organic solvents,
*1D means enzyme is highly inducible by obesity, alcohol, and isoniazid! |
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Term
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Definition
p-amonibenzoic/salicylic acid
Not many polymorphic alleles |
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Term
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Definition
isoniazid, dapsone, sulfonamides.
Slow acetylators: less metabolism so higher drug conc. |
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Term
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Definition
Irinotecan (prodrug?) whose active metabolite is SN-38.
UGTA1*28: polymorphism where TA repeats are inserted into the TATA (promoter region) and leads to decreased expression of UGT1. Thus, less metabolism and higher conc in blood and increased ADRs such as DIARRHEA!
Gilberts Syndrome is worsened by defects in UGT1 and other UGT enzymes. Person already doesnt have enough UGT activity so more susceptible to hyperbilirubinemia when given drugs Atazanavir and Indinavir (which compete for UGT and worsen jaundice)
Also, more susceptible to APAP! |
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Term
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Definition
| deletions in these enzymes lead to inability to produce enough glutathione to combat oxidative stress and cancer. But having less of the enzymes means that the cancer drug substrates won't get metabolized as much and will be more beneficial because higher conc (less drug resistance) |
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Term
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Definition
CA CODE
Carboplatin, APAP, Cisplatin, Oxiplatin, Doxorubicin, and Etoposide.
Variants (*A and *B) increased conc, inc therapeutic effect, and inc toxicity :/
Minor alleles (Val 105): Asthma risk in children whose mothers took APAP while pregnant, since fetus doesnt have GST to conjugate/metabolize the NAPQI produced by APAP. NAPQI will be free to damage lungs and later lead to asthma |
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Term
| Which enzyme is involved with APAP and NAPQI? What diease can it cause? |
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Definition
| GST P1. Can cause asthma in children. Especially if defective GST. But I think babies dont have GST to even produce glutathione. |
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Term
| 60% of Papua New Guineans have defect in which CYP? |
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Definition
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Term
| 14% Chinese and 70% Pacific islanders are PM with which CYP? |
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Definition
| 2C19 (think: i look like im 19 and im Chinese) |
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Term
| Many asians and blacks are IM for which CYP? |
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Definition
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Term
| North African and Mediterranean people are UM for which CYP? |
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Definition
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Term
| Which population have 50% slow acetylators? What enzyme is this? |
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Definition
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Term
| What population has about 30% and 50% defect in their UGT1? What drug is affected? |
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Definition
| white people (30%) and black people (50%). Irinotecan (prodrug) whose metabolite is SN-38. Once SN-38 formed, it should be metab by UGT, but if there is low expression of UGT, then more ADRs (DIARRHEA) |
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Term
| Which enzyme is found in hispanics and blacks commonly? |
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Definition
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