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BIOPHARM > Metabolism > Flashcards

Metabolism Flashcards

1
Q

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

A

Drug metabolism or biotransformation

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2
Q

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

A

less active
less toxic
polar
readily excretable form

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3
Q

Exception of drug metab (3)

A

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

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4
Q

What is the active form of chloral hydrate

A

Trichloroethanol

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5
Q

Active metabolites of amitriptyline

A

Nortriptyline

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6
Q

Hepatotoxic metabolite of paracetamol

A

NAPQI
N-acetyl-p-benzo-quinone imine

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7
Q

Detoxification of paracetamol convert by glutathione into

A

Mercapturic acid

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8
Q

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

A

First-Pass Metabolism

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9
Q

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

A

(PCMMP)
Propranolol
Catecholamines
Meperidine
Morphine
Pentazocine

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10
Q

Phase 1 reaction also called (2)

A

Functionalization
Asynthetic

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11
Q

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

A

Phase 1

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12
Q

3 Chemical Reactions

A

Oxidation
Reduction
Hydrolysis

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13
Q

Redox reaction
(GEROA) (LEORA)

A

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

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14
Q

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

A

Oxidation

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15
Q

What do you call the family of oxidative enzyme

A

Mixed function oxidases (MFO)

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16
Q

Cytochrome P-450 subfamily that is predominant in pediatrics

A

CYP3A7

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17
Q

Cytochrome P-450 subfamily that is predominant to adults

A

CYP3A4

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18
Q

Cytochrome P-450 subfamily that metabolizes antidepressants

A

CYP2D6

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19
Q

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

A

Acetaminophen
Theophylline
Warfarin
Caffeine

Induced by:
Omeprazole
benzopyrene (charred meat)

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20
Q

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

A

Phenytoin
Tolbutamide
Warfarin

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21
Q

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

A

Propranolol
Omeprazole

22
Q

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

A

Debrisoquin
Thioridazine
Haloperidol
Dextrometorphan

23
Q

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

A

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

Subject to enzyme inhibition/induction

24
Q

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

A

Norepi
Serotonin

Antidepressants

Florgiline
Meclobemide

25
Q

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

A

Dopamine

Parkinstons Disease

Selegiline
Rosagiline

26
Q

MAO nonselective drug ex (3)

A

(TIP)
Tranylcypromine
Phenelzine
Isocarboxazid

27
Q

Alcohol dehydrogenase inbitor ex(drug)

A

Fomepizole

28
Q

Aldehyde dehydrogenase inhibitor drug ex

A

Disulfiram (Antabuse)

29
Q

Drug that undego nitro reduction
DOC for typhoid fever

A

Chloramphenicol

30
Q

Drug that undego carbonyl reduction
It is antidote for opioid toxicity

A

Naloxone

31
Q

(4) ester drug that undergo hydrolysis
It stays at_____

A

(PACE)
Procaince
Aspirin
Cocaine
Enalapril

Plasma

32
Q

(3) amide drug that undergo hydrolysis
It stays at_____

A

(LIP)
Lidocaine
Indomethacin
Procainamide

33
Q

DOC for Patent Ductus Arteriosus (PDA) in premature infants

A

Indomethacin

34
Q

Reactions generally involved in the inactivation of a drug and formation of its polar form

Collect complex molar grp

A

Phase 2

35
Q

Phase 2 also called (2)

A

Conjugation
Synthetic

36
Q

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

A

Glucuronidation

37
Q

Enzyme of Glucuronidation

A

UDP-glucuronosyltransferase

38
Q

Most abundant process in neonates

A

Sulfate conjugation

39
Q

Enzyme involved in Sulfate conjugation

A

Sulfotransferase

40
Q

Enzyme involved in glycine conjugation

A

N-acyltransferase

41
Q

Tripeptide involve in glutathione conjugation

A

Glutamine
Cysteine
Glycine

42
Q

Enzyme involve in glutathione conjugation

A

Glutathione-S-transferase

43
Q

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

A

N-acetyltransferase

(HIPS)
Hydralazine
Isoniazid
Procainamide
Sulfonamide

44
Q

Enzyme involve in metylation ____
Give ex (1)

A

Methyltransferase

Catecholamines

45
Q

ENZYME INDUCERS

A

( CrOP GPSs)

Carbamazepine
Chronic Alcoholism
Rifampicin
Omeprazole
Phenobarbital
Griseofulvin
Phenytoin
Smoking
St. John’s Wort

46
Q

ENZYME INHIBITORS

A

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

47
Q

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

A

EM: Extensive Metabolizers

48
Q

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

A

UM: Ultra-rapid metabolizers

49
Q

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

A

PM: Poor metabolizers

50
Q

Races that has fast metabolism

A

Filipinos
Orientals
Eskimos

51
Q

Races that has slow metabolism

A

Africans
Americans
Caucasians

BIOPHARM (3 decks)

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