2.6 - Metabolism Flashcards
1
Q
Biotransformation/ Chemical Change
A
Metabolism
2
Q
Goal:
To convertdrugs into the following forms:
A
– Inactive
– Polar
– Non-toxic/ Less Toxic
– Easily excreted
3
Q
Exceptions
A
- Prodrug
- Formation of Toxic Metabolites
- Active ➡️ Active
4
Q
Inactive parent molecule metabolized to become active
A
Prodrug
5
Q
Ex: Prodrugs
A
• ACEIs — EXCEPT - Captopril – Lisinopril – Enalaprilat IV • Clopidogrel • Dipivefrinn (EPI)
6
Q
Formation of Toxic Metabolites
A
APAP ➡️ NAPQI
7
Q
Active ➡️ Active
A
Diazepam ➡️ Oxazepam
8
Q
Organs
A
- Liver — dominant
- Kidneys
- Plasma
- GIT
- Placenta
9
Q
– For PO drugs
– Initial metabolism of drugs before enterig the syatemic circulation
A
First Pass Effect/ Pre-systemic Metabolism
10
Q
GIT ➡️ Portal Circulation ➡️ Liver
A
Effect: ⬇️Oral Bioavailability
11
Q
Ex: First Pass Metabolism
A
- Propranolol
- Opioids
- Catecholamines
- Felodipine
- Lidocaine
12
Q
2 Phases of Metabolism
A
- Phase 1
* Phase 2
13
Q
– Functionalizariin/ Asynthetic
A
Phase 1
14
Q
Goal of Phase 1:
A
To add/ unmask FUNCTIONAL groups
15
Q
Phase 1
A
- Oxidation
- Reduction
- Hydrolysis
16
Q
– Dominant Phase 1
– 2 enzymes
A
Oxidation
17
Q
2 Enzymes
A
- CYP Mediated
* Non CYP Mediated
18
Q
CYP1A2
A
- Caffeine
- Acetaminophen
- Theophylline
19
Q
CYP2C19
A
- PPIs
- Propranolol
- Clopidogrel
