Term
Phase two metabolites are usually what at phys pH?
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Definition
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Term
| These Phase II metabolites are not an ANION at physiological pH |
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Definition
Methylated
Fatty acid
&
Acetylated metabolites |
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Term
| Acetaminophen metabolized by which CYPS? |
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Definition
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Term
| CYP2D6 ASSOCIATED WITH WHAT OLD DRUG ANTI htn MED? |
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Definition
DEBRISOQUINE
[NO ACTIVE CYP2D6 MADE PEOPLES BP LOWER WAY TOO MUCH] |
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Term
| CODEINE IS A PRODRUG. THE ALTERED FUNCTION OF _____________ CAUSES CODEINE NOT TO WRK IN SOME PEOPLE |
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Definition
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Term
CYP2C19 FIRST SHOWN WITH WHAT DRUG_____
AFFECTS WHAT POP?_____ |
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Definition
MEPHENYTOIN
asian/japanese (20-30%)
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Term
| NEWBORNS HAVE LOW LEVELS OF _________ |
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Definition
ugt
[HARD FOR BABIES TO EXCRETE/METAABOLIZE BILLIRUBIN SO THEY DEVELOP JAUNDICE] |
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Term
SlOW ACETYLATORS (can cause toxicity)
ASIANS
SWEDISH
GENERAL US |
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Definition
ASIANS [0-30%]
SWEDISH [70%]
GENERAL US [50%] |
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Term
isoniazid treats___________
isoniazid uses wat enzyme to become inactive?___ |
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Definition
TUBERCULOSIS
NAT-2[N-acetyltransferase 2] (CAN USE CYP2E1 TOO) |
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Term
SOME PEOPLE EXPRESS UNSTABLE CYP2D6 THEY ARE ___________
soME HAV EXTRA COPIES
_____________ |
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Definition
SLOW-noN
ULTRA-RAPID METABOLIZERS (hIGH IN ARAB/AFRICAN) |
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Term
WHICH CYPS ARE INDUCED BY
TOBACCO,CHARCOAL
ETHANOL
ST. JOHNS WORT |
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Definition
TOBACCO,CHARCOAL [CYP1A2]
ETHANOL [CYP2E1]
ST. JOHNS WORT [CYP3A4] |
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Term
| rIFAMPIN CONTRAINDICATED WITH OCs WHY? |
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Definition
CYP3A4 INDUCED BY RIFAMPIN
OCs METABOLIZED TO FAST AND YOU GET UNPLANNED PREGNANCY |
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Term
| tHEOPHYLLINE CONTRAINDICATED WITH CHARCOAL BROILED FOODS WHY? |
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Definition
BOTH USE CYP1A2
[MAKES THEOPHYLLINE NO LONGER EFFECTIVE]
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Term
| EETHANOL REDUCES ______ AND ______ CONCENTRATION LEADING TO POOR ___&&___ |
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Definition
nadph & udpga
monooxygenation & glucuronidation |
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Term
| AIDS medication use __________ to bind ritonavir and avoid first pass of indinavir and saquinavir |
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Definition
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Term
| KETOCONAZOLE AND CIMETIDINE INHIBIT SEVERAL FORM S OF CYP BY _______________ |
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Definition
| BINDING /OCCUPYING HEMOGOLOBIN BINDING SITE OF CYP |
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Term
| ERYTHROMYCIN INHIBITS _______BY BINDING TIGHTLY AND PREVENTING METABOLISM OF OTHER RX |
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Definition
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Term
| THE LONE PAIR ON __________CONTAINING DRUGS OCCUPY O2 BINDING SITE ON CYP450 & PREVENT OXYGENATION OF OTHER DRUGS |
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Definition
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Term
GRAPEFRUIT INTERXN OCCUR WHERE
W/ WHAT ENZYMES |
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Definition
Enterocytes
CYP3A4 &
OR W/ DRUGS THAT ARE SUBSTRATE FOR P-GLYCOPROTEIN [MDR1] |
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Term
| HYDROPHILLIC METABOLITES ARE USUALLY |
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Definition
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Term
EXAMPLE OF :
ACTIVE RX>ACTIVE METABOLITE
ACTIVE RX > INACTIVE METABOLITE
iNACTIVE RX > ACTIVE METABOLITE |
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Definition
ACT RX>ACT [DIAZEPAM TO N-DESMEHTL,...]
ACT RX > INACT [ISONIAIZD TO N ACETYL,....]
iNACT RX > ACT [IRINOTECAN TO 2N-38] |
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Term
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Definition
Hydrolysis
Oxydation
Reduction |
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Term
|
Definition
Amino acid Conjugation
Glutathione Conjugation
Glucuronidation
Acetylation
Sulfonation |
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Term
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Definition
Fatty acid conjugation
Methylation
Cholesterol Conjugation |
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Term
|
Definition
-Phase I (H2O catalyse)
-Peptidase
-Epoxide
-Amide Hydrolyses
-Ester hydrolyses |
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Term
|
Definition
-Phase I []
-Flavin monooxygenase[NADPH, O2]
-Alcohol & Aldehyde Dehydrogenase[NADPH,NADH,O2]
-Monoamine Oxidase[NADH,O2]
-CYP[NADPH,O2]
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Term
|
Definition
phase I [*DAAD NONE*]
-Desaturation
-Aromatic ring hydroxylation
-Aliphatic hydroxylation
-Dehalogenation
-N & S Oxidation
-O Dealkylation
-N Dealkylation
-Epoxidation |
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Term
|
Definition
-Phase I
(NADPH)
-Nitrogrp to amino grp[nitroreductase enzyme]
-Azo group to amino grp |
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Term
|
Definition
PHASE II
Catalyzed: NAT
Co-Substrate: ACETYL-COA
NOT ANIONIC METABOLITES |
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Term
|
Definition
PHASE II
Catalyzed: UGT
Co-Substrate: UDPGA
GROUPS-(*ATACH*)----Amine,Thiol,Acidic carbons,Carboxylic acids,Hydroxyl |
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Term
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Definition
PHASE II
Catalyzed: GST
Co-Substrate: GSH(glutathione)
GROUPS----alkyl halides,aryl halides,alpha-beta unsat ketones,epoxides
DETOXIFYING AGENT |
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Term
| AMINO ACID CONJUGATION(Hippuric acid) |
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Definition
PHASE II
Catalyzed: ACYL COA LIGASE, then ACYL COA N-ACETYLTRANSFERASE
Co-Substrate: GLYCINE, SOMETIMES GLUTAMINE OR TAURINE
GROUPS----carb acids |
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Term
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Definition
PHASE II
Catalyzed:SULT
Co-Substrate:PAPS
GROUPS---hydroxyls, amines |
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Term
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Definition
OTHER PHASE II
Catalyzed: AMIDASE OR ESTERASE
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Term
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Definition
OTHER PHASE II
Catalyzed: S-ADENOSINE METHYL TRANSFERASE
Co-Substrate: SAM |
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Term
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Definition
OTHER PHASE II
CATALYSE: HYDROLASE |
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Term
| REACTIVITY [least to most reactive func. grps] |
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Definition
CAEKA
carb acid, amide, ester, ketone,aldehyde |
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Term
UGT1A1
substrate:_____
gene deletion:______
reduced expression:_______
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Definition
substrate: billirubin
gene deletion: Crigler-Nager syndrome
(severe unconjugated bilirubemia)
reduced expression: Gilberts Syndrome
[1.common variant UGT1A1*28]
[2.IRINOTECAN Tx for Colon Cancer] |
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Term
| THESE PHASE II METABOLITESARE NOT WATER SOLUBLE |
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Definition
[*FMC*]
FATTY ACID CONJUGATION, CHOLESTEROL CONJUGATION, METHYLATION |
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Term
THESE METABOLITES INCLUDE PROTEIN AIDED REMOVAL OF DRUGS FROM THE CELL
[termed by scientists] |
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Definition
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Term
|
Definition
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