Metabolism Flashcards by lourize lanuza

Is the chemical transformation of the drug by the biological environment to form metabolites

Drug metabolism or biotransformation

How well did you know this?

Not at all

Perfectly

Objective of drug metab is to convert xenobiotics to a (4)

less active
less toxic
polar
readily excretable form

How well did you know this?

Not at all

Perfectly

Exception of drug metab (3)

Inactive (prodrug) to active form
Active to active metabolites
Non-toxic to toxic form

How well did you know this?

Not at all

Perfectly

What is the active form of chloral hydrate

Trichloroethanol

How well did you know this?

Not at all

Perfectly

Active metabolites of amitriptyline

Nortriptyline

How well did you know this?

Not at all

Perfectly

Hepatotoxic metabolite of paracetamol

NAPQI
N-acetyl-p-benzo-quinone imine

How well did you know this?

Not at all

Perfectly

Detoxification of paracetamol convert by glutathione into

Mercapturic acid

How well did you know this?

Not at all

Perfectly

initial metabolism that happens before a drug reaches the systemic circulation
• These are drugs with high extraction ratio (ER) in the liver.

First-Pass Metabolism

How well did you know this?

Not at all

Perfectly

drugs with high extraction ratio (ER) - significant portion will metabolize (5)

(PCMMP)
Propranolol
Catecholamines
Meperidine
Morphine
Pentazocine

How well did you know this?

Not at all

Perfectly

Phase 1 reaction also called (2)

Functionalization
Asynthetic

How well did you know this?

Not at all

Perfectly

Conversion of drugs to active form by
addition or unmasking of a functional group.
Attach small polar grp to drug structure

Phase 1

How well did you know this?

Not at all

Perfectly

3 Chemical Reactions

Oxidation
Reduction
Hydrolysis

How well did you know this?

Not at all

Perfectly

Redox reaction
(GEROA) (LEORA)

Oxidation-reduction
Gain electron = reduction, oxidizing agent
Lose electron = oxidation, reducing agent

How well did you know this?

Not at all

Perfectly

Most common reaction in all metabolic process (phase 1 & 2 )

Oxidation

How well did you know this?

Not at all

Perfectly

What do you call the family of oxidative enzyme

Mixed function oxidases (MFO)

How well did you know this?

Not at all

Perfectly

Cytochrome P-450 subfamily that is predominant in pediatrics

CYP3A7

How well did you know this?

Not at all

Perfectly

Cytochrome P-450 subfamily that is predominant to adults

CYP3A4

How well did you know this?

Not at all

Perfectly

Cytochrome P-450 subfamily that metabolizes antidepressants

CYP2D6

How well did you know this?

Not at all

Perfectly

Cytochrome P-450 substrate (drugs) with 1A2 subfamily (4)
Induced by (2)

Acetaminophen
Theophylline
Warfarin
Caffeine

Induced by:
Omeprazole
benzopyrene (charred meat)

How well did you know this?

Not at all

Perfectly

Cytochrome P-450 substrate (drugs) with 2C9 subfamily (3)

Phenytoin
Tolbutamide
Warfarin

How well did you know this?

Not at all

Perfectly

Cytochrome P-450 substrate (drugs) with 2C19 subfamily (2)

Propranolol
Omeprazole

Cytochrome P-450 substrate (drugs) with 2D6 subfamily (4D)

Debrisoquin
Thioridazine
Haloperidol
Dextrometorphan

Cytochrome P-450 substrate (drugs) with 3A4 subfamily (8)

(MATAGA CD)
50% of drugs:
Acetaminophen
Astemizole
Macrolides
Terfenadine
Grapefruite juice
Amiodarone
Cortisol
Diazepam

Subject to enzyme inhibition/induction

MAO A selective metabolizes what (2)
Tx for _____
Give ex of drugs: (2)

Norepi
Serotonin

Antidepressants

Florgiline
Meclobemide

MAO B selective metabolizes what (1) Tx for _____ Give ex of drugs: (2)

Dopamine Parkinstons Disease Selegiline Rosagiline

MAO nonselective drug ex (3)

(TIP) Tranylcypromine Phenelzine Isocarboxazid

Alcohol dehydrogenase inbitor ex(drug)

Fomepizole

Aldehyde dehydrogenase inhibitor drug ex

Disulfiram (Antabuse)

Drug that undego nitro reduction DOC for typhoid fever

Chloramphenicol

Drug that undego carbonyl reduction It is antidote for opioid toxicity

Naloxone

(4) ester drug that undergo hydrolysis It stays at_____

(PACE) Procaince Aspirin Cocaine Enalapril Plasma

(3) amide drug that undergo hydrolysis It stays at_____

(LIP) Lidocaine Indomethacin Procainamide

DOC for Patent Ductus Arteriosus (PDA) in premature infants

Indomethacin

Reactions generally involved in the inactivation of a drug and formation of its polar form Collect complex molar grp

Phase 2

Phase 2 also called (2)

Conjugation Synthetic

Most abundant process in phase 2 Most abundant in adult Least abundant in Neonates

Glucuronidation

Enzyme of Glucuronidation

UDP-glucuronosyltransferase

Most abundant process in neonates

Sulfate conjugation

Enzyme involved in Sulfate conjugation

Sulfotransferase

Enzyme involved in glycine conjugation

N-acyltransferase

Tripeptide involve in glutathione conjugation

Glutamine Cysteine Glycine

Enzyme involve in glutathione conjugation

Glutathione-S-transferase

Enzyme involve in acetylation ____ Give (4) ex of drug

N-acetyltransferase (HIPS) Hydralazine Isoniazid Procainamide Sulfonamide

Enzyme involve in metylation ____ Give ex (1)

Methyltransferase Catecholamines

ENZYME INDUCERS

( CrOP GPSs) Carbamazepine Chronic Alcoholism Rifampicin Omeprazole Phenobarbital Griseofulvin Phenytoin Smoking St. John’s Wort

ENZYME INHIBITORS

(SIiCK FACES 3D CGV) Sodium Valproate Isoniazid Indinavir Cimetidine Ketoconazole Fluconazole Alcoholism Chloramphenicol Erythromycin Sulfonamides Diltiazem Disulfiram Diphenhydramine Ciprofloxacin Grapefruit juice Verapamil

Genetic polymorphism- enzyme expression that produce normal/adequate amount of enzymes

EM: Extensive Metabolizers

Genetic polymorphism- enzyme expression that produce more than the normal amount of enzymes

UM: Ultra-rapid metabolizers

Genetic polymorphism- enzyme expression produce less than the normal amount of enzymes

PM: Poor metabolizers

Races that has fast metabolism

Filipinos Orientals Eskimos

Races that has slow metabolism

Africans Americans Caucasians