Term
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Definition
SLC22A6
pumps in penicillin, probenecid, and diuretics |
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Term
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Definition
SLC22A8
pumps in penicillin, probenecid, and diuretics |
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Term
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Definition
SLC22A1
Pumps in monoamines, cimetidine |
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Term
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Definition
SLC22A2
pumps in monoamines, cimetidine |
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Term
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Definition
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Term
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Definition
| (MRP1) vinca alkaloids, anthracyclines, (anti-cancer drugs) |
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Term
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Definition
| (MRP2 or cMOAT) vinca alkaloids, anthracyclines, cisplatin (anti-cancer drugs) |
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Term
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Definition
(p-gp or MDR)
vinca alkaloids, doxorubicin, taxol/paclitaxel (anti-cancer drugs) and cyclosporin A (CsA), digoxin |
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Term
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Definition
| rifambin, phenobarbital, verapamil, nifedipine, St John's Wort |
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Term
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Definition
| verapamil, ketoconazole, cyclosporin |
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Term
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Definition
| Phase I (oxidation, reduction) |
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Term
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Definition
| Phase I: oxidation, reduction (MFO=CYP) |
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Term
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Definition
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Term
| phase of metab: epoxide hydrolase |
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Definition
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Term
| phase of metab: transferases: |
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Definition
| Phase II (conjugation, synthetic) |
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Term
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Definition
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Term
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Definition
| lung and placenta (not liver!) |
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Term
| What is CYP1A1 and CYP1A2 activity? |
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Definition
| arylhydrocarbon hydroxylase (forms hydrocarbons) |
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Term
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Definition
| cigarette smoke and beta-carotene |
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Term
| which CYP has a polymorphism that causes intrauterine growth restriction? |
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Definition
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Term
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Definition
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Term
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Definition
| poor metabolism of substrate/drug |
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Term
| which drugs of 2C9 are affected by polymorphisms? |
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Definition
tolbutemide
phenytoin
warfarin (S)
(think substrates) |
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Term
| polymorphism of which CYP affects metabolism of mephenytoin? |
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Definition
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Term
| polymorphism of what CYP affects metabolism of clopidogrel? |
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Definition
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Term
| polymorphism of what CYP affects metabolism of S-warfarin? |
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Definition
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Term
| polymorphism of what CYP affects metabolism of codeine? |
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Definition
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Term
|
Definition
clopidogrel (2C19)
codeine (2D6)
tamoxifen (2D6) |
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Term
| polymorphism of what CYP affects metabolism of tomaxifen? |
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Definition
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Term
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Definition
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Term
| metabolism of acetaminophen is induced by: |
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Definition
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Term
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Definition
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Term
| substrates of UGT1 family |
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Definition
| bilirubin, phenols, amines, NSAIDS, coumarins |
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Term
| 2 diseases resulting from polymorphisms of UGT1 |
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Definition
Crigler-Najjer syndrome (can't conjugate bilirubin as well, so it won't get excreted>liver disease)
Gilbert's Disease: mild hyperbilirubinemia; decreased metabolism of drugs (because there is competitive inhibition between bilirubin and drug-APAP, lorazepam, and irinotecan |
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Term
|
Definition
| steroids, bile acids, morphine, oxazepam |
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Term
| cofactor of sulfonation reactions |
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Definition
| PAPS (3'-phosphoadenasine 5'-phosphosulfate) |
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
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Term
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Definition
| Dehydroepiandrosterone (DHEA) |
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Term
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Definition
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Term
| what kind of metabolism is NAT1 involved with? |
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Definition
| environmental/carcinogenic |
|
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Term
| what kind of metabolism is NAT2 involved with? |
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Definition
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Term
| If someone is a fast acetylator of NAT1, what are they at risk for? |
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Definition
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Term
| If someone is a slow acetylator of NAT1, what are they at risk for? |
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Definition
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Term
|
Definition
| widely distributed (think environment) |
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Term
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Definition
| liver and gi (think drug) |
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Term
| if you are a slow acetylator of NAT2, what are you at risk for? |
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Definition
| isoniazid neuropathy and hydralazine induced lupus |
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Term
| cofactor of glutathione conjugation |
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Definition
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Term
| If someone is missing a GSTM1, what are they at risk for? |
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Definition
| lung, colon, and bladder cancer from smoking |
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Term
| which enzyme is important in BBB? |
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Definition
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Term
| if you have a deleted gene for GSTT1, what is wrong? |
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Definition
| toxicity from cytostatic chemotherapy; low birth weights in mothers who smoke; toxicity from ethylene oxide |
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Term
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Definition
| either cytosol or microsome |
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Term
| what does gamma-glutamyltranspeptidasedo? |
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Definition
| cleaves off gamma glutamyl group |
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Term
| what does cysteinyl-glycinase do? |
|
Definition
| removes glycine to form pre-mercapturate |
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Term
| what does N-acetyltransferase do in glutathione conjugation? |
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Definition
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Term
| pharmacological toxicity? |
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Definition
| extension of therapeutic effect |
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Term
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Definition
| effect of drug that is unrelated to mechanism of therapeutic action |
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Term
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Definition
| causes mutation in person's DNA (avoid excpet cancer) |
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Term
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Definition
| person makes antibodies to drug |
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Term
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Definition
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Term
|
Definition
-pharmacological
-respiratory depression |
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Term
| calcium channel blockers toxicity |
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Definition
-pharmacological toxicity
-slows heart rate, hyperglycemia |
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Term
| alpha2-adrenergic receptor toxicity: |
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Definition
-pharmacological toxicity
-affects blood pressure |
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Term
|
Definition
-pharmacologic toxicity
-decreased heart rate and blood glucose |
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Term
| tricyclic antidepressants toxicity |
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Definition
-pharmacological toxicity
-arrhythmia |
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Term
| quinine/quinidine toxicity |
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Definition
-pharmacological toxicity
-arrhythmia |
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Term
|
Definition
-pharmacological toxicity
-kids don't show muscarinic (SLUD): they show nicotinic effects ("floppiness") |
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Term
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Definition
-pathological
-overheating, alkalosis and acidosis, pulmonary and cerebral edema |
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Term
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Definition
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Term
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Definition
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Term
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Definition
-pathological
-foamy lungs |
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Term
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Definition
-pathological
-kidney failure |
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Term
|
Definition
-pathological
-liver damage |
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|
Term
| what is the metabolite of CYP2E1 metabolism of APAP? |
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Definition
|
|
Term
|
Definition
From cysteine
N-acetylcysteine given as treatment for APAP toxicity to regenerate GSH |
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|
Term
| What is the purpose of Pentose shunt? |
|
Definition
| to recreate G6P from Fructose6-P |
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Term
| 2 routes of metabolism of APAP |
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Definition
| either conjugation (glucuronidation/sulfonation)to APAP-glucuronide or APAP-sulfate or CYP2E1 to NAPQI |
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Term
|
Definition
if GSH is present, it will bind to NAPQI to form a GSH-adduct.
If GSH is depleted, NAPQI will bind to tissue protein and cause damage to hepatocytes. |
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Term
|
Definition
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Term
| What can FAva beans cause ? |
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Definition
| if patient has G6Pase deficiency, can cause hemolytic anemia |
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|
Term
| which drugs which cause hemolytic anemia in g6pase deficient patients |
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Definition
|
|
Term
| what does G6P dehydrogenase do? |
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Definition
|
|
Term
| What does GSH reductase do? |
|
Definition
| Reduces GSSG (glutathione disulfide) to GSH |
|
|
Term
| What does GSH reductase need as a cofactor? |
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Definition
|
|
Term
| What does GSH peroxidase do? |
|
Definition
| degrades hydrogen peroxide into water |
|
|
Term
| what does GSH peroxidase need as a cofactor? |
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Definition
|
|
Term
| how does hemolytic anemia happen? |
|
Definition
| accumulation of hydrogen peroxide causes ppt of Hb>hemolysis |
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Term
| what is the benefit of having slight G6Pase deficiency |
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Definition
| elevated hydrogen peroxide levels kill of malaria parasites |
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Term
| drug-induced hemolytic anemia in pts with G6Pase deficiency is example of what kind of toxicity |
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Definition
|
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Term
|
Definition
| damage to hepatocytes surrounding bile ducts (decreased bile flow) |
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Term
| what causes toxicity in kidneys that impairs renal blood flow? |
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Definition
|
|
Term
| what causes toxicity in the kidney that causes tubular damage? |
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Definition
|
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Term
| describe toxicity of gentamicin |
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Definition
| get a little bit of toxicity from gentamicin, it is eliminated by the kidney so less is eliminated, more accumulates, becomes more toxic, spirals |
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Term
| genotoxicity of thalidomide in pregnant women |
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Definition
| limb reduction (phocomelia) |
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Term
| genotoxicity of angiotensin converting enzyme inhibitors in pregnant women |
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Definition
|
|
Term
| genotoxicity of ethanol in pregnant women |
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Definition
|
|
Term
| genotoxicity retinoic acid in pregnant women |
|
Definition
| anomalies of head and face, heart, CNS (functional deficits) |
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Term
| genotoxicity of phenytoin in pregnant women |
|
Definition
fetal hydantoin syndrome
abnormalities of skull and facial features, fingers, nails, lower hairline
neural tube closure |
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Term
| genotoxicity of carbamazepine in pregnant women |
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Definition
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|
Term
| genotoxicity during fetal period |
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Definition
| low birth rate, intrauterine growth reduction |
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|
Term
| how does smoking cause tumors? |
|
Definition
| smoking mutates p53 tumor suppressor gene >>> uncontrolled cell growth and tumor prolifs |
|
|
Term
| what does bisphenol A do? |
|
Definition
| suppresses methylation, which controls gene expression |
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|
Term
| what is phenoxybenzamine? |
|
Definition
alpha-adrenergic blocker: brings BP down for surgery and controls adrenaline release
irreversible competitive antagonist |
|
|
Term
| what is an example of an inverse agonist? |
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Definition
|
|
Term
| describe binding of an antagonist |
|
Definition
| binds to both active and inactive receptors. the binding to the inactive receptor prevents binding of an agonist |
|
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Term
| what kinds of antagonists are surmountable and which aren't? |
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Definition
| reversible competitive antagonists are surrmountable irreversible competitive antagonists and non-competitive antagonists aren't |
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Term
| who are poor metabolizers of 2C9? |
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Definition
|
|
Term
| who are poor metabolizers of 2C19 |
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Definition
|
|
Term
| what parameter does bioavailability influence? |
|
Definition
|
|
Term
| what parameters does absorption rate influence? |
|
Definition
|
|
Term
| which cyp: debrisoquine sensitivity? |
|
Definition
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