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Pharmacology > 2.6 - Metabolism > Flashcards

2.6 - Metabolism Flashcards

1
Q

Biotransformation/ Chemical Change

A

Metabolism

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2
Q

Goal:

To convertdrugs into the following forms:

A

– Inactive
– Polar
– Non-toxic/ Less Toxic
– Easily excreted

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3
Q

Exceptions

A
  • Prodrug
  • Formation of Toxic Metabolites
  • Active ➡️ Active
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4
Q

Inactive parent molecule metabolized to become active

A

Prodrug

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5
Q

Ex: Prodrugs

A 
• ACEIs — EXCEPT 
 - Captopril
 – Lisinopril
 – Enalaprilat IV
• Clopidogrel
• Dipivefrinn (EPI)
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6
Q

Formation of Toxic Metabolites

A

APAP ➡️ NAPQI

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7
Q

Active ➡️ Active

A

Diazepam ➡️ Oxazepam

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8
Q

Organs

A
  • Liver — dominant
  • Kidneys
  • Plasma
  • GIT
  • Placenta
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9
Q

– For PO drugs

– Initial metabolism of drugs before enterig the syatemic circulation

A

First Pass Effect/ Pre-systemic Metabolism

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10
Q

GIT ➡️ Portal Circulation ➡️ Liver

A

Effect: ⬇️Oral Bioavailability

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11
Q

Ex: First Pass Metabolism

A
  • Propranolol
  • Opioids
  • Catecholamines
  • Felodipine
  • Lidocaine
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12
Q

2 Phases of Metabolism

A
  • Phase 1

* Phase 2

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13
Q

– Functionalizariin/ Asynthetic

A

Phase 1

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14
Q

Goal of Phase 1:

A

To add/ unmask FUNCTIONAL groups

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15
Q

Phase 1

A
  • Oxidation
  • Reduction
  • Hydrolysis
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16
Q

– Dominant Phase 1

– 2 enzymes

A

Oxidation

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17
Q

2 Enzymes

A
  • CYP Mediated

* Non CYP Mediated

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18
Q

CYP1A2

A
  • Caffeine
  • Acetaminophen
  • Theophylline
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19
Q

CYP2C19

A
  • PPIs
  • Propranolol
  • Clopidogrel
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20
Q

CYP2C9

A
  • S-Warfarin

* Phenytoin

21
Q

CYP2D6

A
  • Codeine
  • Antidepressants
  • Antipsychotics
22
Q

CYP3A4,5,7

– responsible for metabolism > 50% of commercial drugs

A
  • CCBs
  • Azoles
  • Macrolides
  • Anti-HIV
  • Antineoplastics
23
Q

Non CYP mediated

A
  • MAO
  • Alcohol Dehydrogenase
  • Aldehyde Dehydrogenase
24
Q

Reduction

A
  • Nitroreduction
  • Carbonyl reduction
  • Azo reduction
25
Q

Nitroreduction

A

Chloramphenicol

26
Q

Carbonyl reduction

A
  • Methadone

* Naloxone

27
Q

Azo reduction

28
Q

Hydrolysis

A
  • Ester

* Amide

29
Q

Ester

A
  • ASA
  • ACEIs
  • Ester-tyoe local anesthetics
30
Q

Amide

A
  • Procainamide

* Lidocaine

31
Q

Conjugation/ Synthetic

32
Q

Phase 2

A
  • Glucuronidation
  • Acetylation
  • Muscellaneous
33
Q

Goal:

A

Addition of a POLAR Conjugate

34
Q

– dominant Phase 2 (adults)
– Uridine-5’-diphosphoglucuronosyl transferase
– Poorly expressed in neonates

A

Glucuronidation

35
Q 
– N-acetyltransferase
– Substrates:
 - Hydralazine
 - Isoniazid
 - Procainamide
A

Acetylation

36
Q

Miscellaneous

A
  • Glycine Conjugation
  • Methylation
  • Sulfation — dominant Phase 2 (neonates)
37
Q

Enzyme Induction/ Inhibition

A
  • Enzyme Induction

* Enzyme Inhibition

38
Q

Stimulates activity of enzymes

A

Enzyme Induction

39
Q

GOSPRC

A
  • Griseofulvin
  • Omeprazole
  • St. John’s Wort
  • Phenytoin, Phenobarbital
  • Rifampicin
  • Cigarette, Chronic Alcoholism
40
Q

Consequences

A
  • Prodrug
  • Toxic Metabolite
  • Inactive Metabolite
41
Q

Prodrug

A

⬆️Efficacy; ⬆️Toxicity

42
Q

Formation of Toxic Metabolites

A

⬆️Toxicity

43
Q

Inactive Metabolites

A

⬇️Efficacy

44
Q

Reduce Enzyme Activity

A

Enzyme Inhibition

45
Q

MEDVICKGA

A
  • Metronidazole
  • Erythromycin
  • Disulfiram, Diphen, Diltiazem
  • Valproic Acid, Verapamil
  • Isoniazid, Indinavir
  • Cimetidine, Cipro, Chloram
  • Ketoconazole
  • Grapefruit
  • Acute Alcoholism
46
Q

Consequences

A
  • Prodrug

* Active Parent — Inactive

47
Q

Prodrug

A

⬇️Efficacy

48
Q

Active Parent — Inactive

A

⬆️Efficacy; ⬆️Toxicity

Pharmacology (21 decks)

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