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PK - Metabolism
Pharm I - Block 1
26
Pharmacology
Not Applicable
05/25/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
What is Biotransformation?
Definition

The chemical alteration of a drug eirther

1. Drug - - Inactive metabolite - Morphine

 

2. Drug - - Active metabolite - imipramine – desipramine (much more active than parent compound)

 

3. Prodrug - Drug -

Levodopa - dopamine

codeine - morphine

Term
Phase 1 Biotransformaion
Definition
Reduction, Oxidation or Hydrolysis of the drug in the liver
Term
Oxidation
Definition
Phase 1 - Acetomiophen
Term
Reduction
Definition
Phase 1 - Halothane
Term
Hydrolysis
Definition

Phase 1 - –Local Ansthetic ..procaine..psudocholinesterase

 

Term
Deamination
Definition
anphetamine
Term
Dealkalyation
Definition
Codeine
Term

Phase II biotransformation

Definition

 

Conjugation of a drug or Phase I metabolite which is easily excreted in urine 

 

Term

Glucuronidation

Definition
Phase II  - chloramphenicol
Term

Acetylation 

Definition
Phas II - Isoniazid, hydrallazine, procainamide
Term

Methylation

Definition
Phase II - epinephrine
Term

Sulfate conjugation

 

Definition
Phase II  - methyldopa
Term

Glycine conjugation

 

Definition
Phase II - aspirin
Term

Gluathione(GSH) conjugation

Definition
Phase II - acetaminophen 
Term

Pseudocholineesterase deficiency

1. Defect?

1. Test

2.results in

Definition

1. Cannot metabolise Succinyl CoA 

2. Dibucaine number - identifies people with defect

3.Succinyle CoA apnea - Prolonged neuromuscular paralysis

 

Term

Slow Acelyators

1. Defect

2. Drugs

Definition

1.drug induces SLE (butterfly rash)

2. Isoniazide , procainamide, hydralazine

Term
WHat drugs increase synthesis of CYP450 in liver?
Definition

1. Phenobarbitone

2. carbamezapine

3.phenytoin

4.rifampine

5. aromatic hydrocarbons (smoking)

Term

Give an example of a drug that decreases duration and intensity of another drugs action

 

Definition

phenytoin with oral contraceptives

failure of contraception

Term

Example of a drug which demonstrates tolerance (the requirement of a higher dose to elicit the given response)

Definition
  Ex: carbamazepine
Term

CYP 450 enzyme inhibitors

examples...

Definition

 

cimetidine,grapefruit juice, erythromycin, azole antifungals- ketoconazole, HIV protease inhibitors

... leads to less enzyme thus it wont be metabolised and eliminated it accumilates thus more toxicity of drugs

 

Term

CYP 1A1

1. Drug substrate

2.Inducers

3.Inhibitors

Definition

1. Theophylline & Acetaminophen

2. Smoke (aromatic hydrocarbons)

3. Quinolones & Macrolides

Term

CYP 2C9

1. Drug substrate

2. Inducer

Definition

1.Phenytoin & Warfarin

2. Phenobarbitone, Phenytoin & Rifampin

Term

CYP 2D6

1.Drug substrates

3. Inhibitors

Definition

1. CVS & CNS drugs

2. Haloperidol & Quinidine

Term

CYP 3A4

1. Drug substrates

2. Inducers

Definition

1. 60% of drugs

2. Anticonvulsants & Rifampin

 

Term

Toxic Metabolism

give an example

Definition

•Some drugs can be converted to its active/toxic forms after metabolism leading to tissue injury
•Eg:  acetaminophen is converted to a reactive metabolite N-acetyl-p-benzoquinoneimine which is conjugated with glutathione (GSH)
•In overdoses the glutathione gets depleted, so the reactive metabolite combines with essential hepatic cell proteins- leads to cell death
•Rx: Administration of acetylcycteine which replenishes the glutathione

Term

Acetaminophen OD.. what happens?

how is it treated?

 

Definition

Toxic metabolism (hepatotoxicity)

 - glutathione stores are depleted which conjugates it

 

-Administration of acetylcycteine which replenishes the glutathione

 
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