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Pharmacology > METABOLISM > Flashcards

METABOLISM Flashcards

1
Q

How can the drug be eliminated:

A
  • Metabolism
  • Excretion
  • Redistribution
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2
Q

Metabolism synonyms

A

Biotransformation

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3
Q

Metabolism definition

A

Chemical alteration of the drug in the body. It is needed to inactivate the drug by making it ionized, water-soluble

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4
Q

Sites of metabolism

A
  • Liver
  • Lung
  • Kidney and skin
  • GIT
  • Plasma cholinesterase (ChE)
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5
Q

Which drug is metabolised in the lung:

A

Nicotine

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6
Q

Which drug is metabolised in the kidney and skin

A

Vitamin D

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7
Q

Which drug is metabolised in the GIT:

A

Tyramine

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8
Q

Which drug is metabolised by the plasma cholinesterase

A

Succinylcholine

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9
Q

Types of metabolism in the liver

A 
Phase I (non-synthetic)
Phase II (Synthetic, conjucation)
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10
Q

What reactions happen in phase I

A
  • Oxidation
  • Reduction
  • Hydrolysis
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11
Q

What reactions happen in phase II

A
  • Glucuronic acid
  • Acetylation
  • Methylation
  • Glycine
  • Sulfation
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12
Q

Example of oxidation reaction

A

Ethyl alcohol —> acetaldehyde —-> acetic acid + H2O + CO2 + water

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13
Q

Example of reduction reaction

A

Chloral hydrate —-> trichloroethanol

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14
Q

Example of hydrolysis

A

Acetylcholine —-> acetic acid + choline

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15
Q

Example of drugs metabolised by glucuronic acid:

A

Asprin
Morphine
Chloramphenicol

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16
Q

Example of drugs metabolised by acetylation

A

Isoniazid
Procainamide
Hydralazine

17
Q

Example of drugs metabolised by methylation

A

Noradrenaline

18
Q

Example of drugs metabolised by addition of glycine

A

Asprin

19
Q

Example of drugs metabolised by sulfation

A

Steroids

20
Q

Results of phase I metabolism:

A
  • Inactivation of drug
  • Activation of inactive drug (prodrug)
  • Maintain activation of the drug
  • Toxication
21
Q

Results of phase II metabolism

A

Usually inactivation except morphine-6-glucuronide

22
Q

Most drugs enter Phase I then phase II while some drugs enter phase II directy like …..

A

Isoniazide

23
Q

Types of cellular enzymes

A
  • Microsomal enzymes

- Non-microsomal enzymes

24
Q

Site of microsomal enzymes

A

In the sER or liver, kidney, lung and intestinal mucosa

25
Q

Sites of non-microsomal enzymes

A

Cytoplasm and mitochondria in all tissue

26
Q

Example of microsomal enzymes:

A

Monooxygenases, cytochrome P450, UGTs, epoxide hydrolases

27
Q

Examples of non-microsomal enzymes

A

The esterases, amidases, some flavoprotein oxidases and most conjugases

28
Q

What reactions does microsomal enzymes do?

A

Catalyze oxidation, reduction (phase I) and glucuronidation only (phase II)

29
Q

What reactions does non-microsomal enzymes do?

A

Oxidation, reduction, hydrolysis (phase I)

All phase II except glucuronidation

30
Q

Microsomal enzymes are inducible by ……..

A

drugs, diet and genetics

31
Q

Non-microsomal enzymes are not inducible but

A

shows genitic variation

32
Q

Factors affecting hepatic microsomal enzymes

A
  • Hepatic microsomal enzyme inducers
  • Hepatic microsomal enzyme inhibitors
  • Age
  • Disease
  • Genetic defect
  • Sex
33
Q

Hepatic microsomal enzyme inducers action

A

Increase metabolism of other drugs , decrease their action

Increase their own metabolism, causes tolerance

34
Q

Hepatic microsomal enzyme inducers examples

A

Phenobarbitone, phenytoin, carbamazepine, rifampicin, androgen and tobacco smoke

35
Q

Hepatic microsomal enzyme inhibitors types

A

Specific/Direct

Non-specific/ Indirect

36
Q

Specific hepatic microsomal enzyme inhibitors examples

A

Estrogen, cimetidine (ramitidine), valproic acid, erythromycin, ciprofloxacin, chloramphenicol.

37
Q

Non-specific hepatic microsomal enzyme inhibitors examples

A

Hepatotoxic drugs and drugs decreasing hepatic blood flow as propranolol and cimetidine.

Pharmacology (11 decks)

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