Drug Metabolism Flashcards

1
Q

Mention 5 consequence of metabolism ?

A
  1. Pharmacological inactivation
  2. Bioactivation or toxicological activation
  3. Pharmacological activation
  4. Change in pharmacological activity
  5. Lethal synthesis
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2
Q

Major organ of drug bio transformation?

A

Liver

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3
Q

Give an example of a drug that undergoes non enzymatic metabolism and explain how ?

A

Atracurium : through molecular re-arrangement

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4
Q

Microsomal enzymes activity requires?

A

NADPH and oxygen

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5
Q

Microsomal enzymes are located where ?

A

Smooth endoplasmic reticulum

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6
Q

Non Microsomal enzymes undergoes all phase 2 reactions except?

A

Glucoronidation

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7
Q

Functionalization reaction is what phase of metabolism ?

A

Phase 1

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8
Q

How many p450 enzymes are identified in human liver microsomes ?

A

15

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9
Q

Mention 2 examples of drugs that undergoes auto induction?

A

Carbamazepine and rifampicin

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10
Q

Mention 5 clinical importance of enzyme induction?

A
  1. Decease plasma level and therapeutic effect of a drug
  2. Reduce half life of a drug
  3. Reduce potency and efficacy of a drug
  4. Increase change of drug interactions
    5.enhance drug tolerance
  5. Increase drug toxicity
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11
Q

How does propranolol reduce the rate of metabolism of lignocaine ?

A

By reducing hepatic blood flow

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12
Q

Mention the 3 major factors affecting drug metabolism ?

A
  1. Physicochemical properties of drugs
  2. Chemical factors
  3. Biological factors
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13
Q

Explain how sex affect drug metabolism ?

A

Metabolism is higher in males due to high GFR

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14
Q

Explain the effect of of age in drug metabolism ?

A

Metabolism reduce with age cause of reduction in liver mass and liver blood flow which leads to reduction in first pass metabolism which lead to higher absorption but lower metabolism

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15
Q

Mention two properties of non Microsomal enzymes ?

A
  1. Non inducible
  2. May show genetic variation
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