Metabolism

Question 1

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

Answer 1

Drug metabolism or biotransformation

Question 2

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

Answer 2

less active
less toxic
polar
readily excretable form

Question 3

Exception of drug metab (3)

Answer 3

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

Question 4

What is the active form of chloral hydrate

Answer 4

Trichloroethanol

Question 5

Active metabolites of amitriptyline

Answer 5

Nortriptyline

Question 6

Hepatotoxic metabolite of paracetamol

Answer 6

NAPQI
N-acetyl-p-benzo-quinone imine

Question 7

Detoxification of paracetamol convert by glutathione into

Answer 7

Mercapturic acid

Question 8

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

Answer 8

First-Pass Metabolism

Question 9

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

Answer 9

(PCMMP)
Propranolol
Catecholamines
Meperidine
Morphine
Pentazocine

Question 10

Phase 1 reaction also called (2)

Answer 10

Functionalization
Asynthetic

Question 11

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

Answer 11

Phase 1

Question 12

3 Chemical Reactions

Answer 12

Oxidation
Reduction
Hydrolysis

Question 13

Redox reaction
(GEROA) (LEORA)

Answer 13

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

Question 14

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

Answer 14

Oxidation

Question 15

What do you call the family of oxidative enzyme

Answer 15

Mixed function oxidases (MFO)

Question 16

Cytochrome P-450 subfamily that is predominant in pediatrics

Answer 16

CYP3A7

Question 17

Cytochrome P-450 subfamily that is predominant to adults

Answer 17

CYP3A4

Question 18

Cytochrome P-450 subfamily that metabolizes antidepressants

Answer 18

CYP2D6

Question 19

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

Answer 19

Acetaminophen
Theophylline
Warfarin
Caffeine

Induced by:
Omeprazole
benzopyrene (charred meat)

Question 20

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

Answer 20

Phenytoin
Tolbutamide
Warfarin

Question 21

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

Answer 21

Propranolol
Omeprazole

Question 22

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

Answer 22

Debrisoquin
Thioridazine
Haloperidol
Dextrometorphan

Question 23

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

Answer 23

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

Subject to enzyme inhibition/induction

Question 24

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

Answer 24

Norepi
Serotonin

Antidepressants

Florgiline
Meclobemide

Question 25

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

Answer 25

Dopamine Parkinstons Disease Selegiline Rosagiline

Question 26

MAO nonselective drug ex (3)

Answer 26

(TIP) Tranylcypromine Phenelzine Isocarboxazid

Question 27

Alcohol dehydrogenase inbitor ex(drug)

Answer 27

Fomepizole

Question 28

Aldehyde dehydrogenase inhibitor drug ex

Answer 28

Disulfiram (Antabuse)

Question 29

Drug that undego nitro reduction DOC for typhoid fever

Answer 29

Chloramphenicol

Question 30

Drug that undego carbonyl reduction It is antidote for opioid toxicity

Answer 30

Naloxone

Question 31

(4) ester drug that undergo hydrolysis It stays at_____

Answer 31

(PACE) Procaince Aspirin Cocaine Enalapril Plasma

Question 32

(3) amide drug that undergo hydrolysis It stays at_____

Answer 32

(LIP) Lidocaine Indomethacin Procainamide

Question 33

DOC for Patent Ductus Arteriosus (PDA) in premature infants

Answer 33

Indomethacin

Question 34

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

Answer 34

Phase 2

Question 35

Phase 2 also called (2)

Answer 35

Conjugation Synthetic

Question 36

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

Answer 36

Glucuronidation

Question 37

Enzyme of Glucuronidation

Answer 37

UDP-glucuronosyltransferase

Question 38

Most abundant process in neonates

Answer 38

Sulfate conjugation

Question 39

Enzyme involved in Sulfate conjugation

Answer 39

Sulfotransferase

Question 40

Enzyme involved in glycine conjugation

Answer 40

N-acyltransferase

Question 41

Tripeptide involve in glutathione conjugation

Answer 41

Glutamine Cysteine Glycine

Question 42

Enzyme involve in glutathione conjugation

Answer 42

Glutathione-S-transferase

Question 43

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

Answer 43

N-acetyltransferase (HIPS) Hydralazine Isoniazid Procainamide Sulfonamide

Question 44

Enzyme involve in metylation ____ Give ex (1)

Answer 44

Methyltransferase Catecholamines

Question 45

ENZYME INDUCERS

Answer 45

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

Question 46

ENZYME INHIBITORS

Answer 46

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

Question 47

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

Answer 47

EM: Extensive Metabolizers

Question 48

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

Answer 48

UM: Ultra-rapid metabolizers

Question 49

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

Answer 49

PM: Poor metabolizers

Question 50

Races that has fast metabolism

Answer 50

Filipinos Orientals Eskimos

Question 51

Races that has slow metabolism

Answer 51

Africans Americans Caucasians