Pharmacology of Diazonamide

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Questions and Answers

What is the resulting functional group from the oxidation of a primary alcohol?

  • Carboxylic acid (correct)
  • Ketone
  • Ester
  • Aldehyde

Which of the following reactions does not involve the formation of a NH2 group?

  • Reduction of azo compounds
  • Oxidation of primary alcohols (correct)
  • Reduction of nitro compounds
  • Hydrolysis of amides

What is the product of the hydrolysis of an ester?

  • Carboxylic acid and an alcohol (correct)
  • Amide and an alcohol
  • Carboxylic acid and an aldehyde
  • Amide and a carboxylic acid

Which of the following compounds cannot be reduced to form a NH2 group?

<p>Ester (A)</p> Signup and view all the answers

What is the byproduct of the hydrolysis of an amide?

<p>H2O (D)</p> Signup and view all the answers

What is the primary reason the liver is the most important organ in drug metabolism and detoxification?

<p>It contains almost all the necessary enzymes for biotransformation (A)</p> Signup and view all the answers

What types of compounds does the liver metabolize and detoxify?

<p>Both endogenous and exogenous compounds (A)</p> Signup and view all the answers

Why is the liver considered a critical organ in the body?

<p>It has a high concentration of enzymes for biotransformation (B)</p> Signup and view all the answers

What is the significance of the liver's dual blood supply system in drug metabolism?

<p>It provides the liver with a constant supply of substrates for biotransformation (A)</p> Signup and view all the answers

What is a unique feature of the liver that enables it to perform its functions in drug metabolism?

<p>It has the ability to regenerate itself (C)</p> Signup and view all the answers

What is the first part of a cytochrome's classification?

<p>A number specifying the cytochrome family (C)</p> Signup and view all the answers

Which of the following is an example of a cytochrome subfamily?

<p>CYP1A (A)</p> Signup and view all the answers

What is the purpose of the capital letter in a cytochrome's classification?

<p>To denote the subfamily (C)</p> Signup and view all the answers

What is the correct order of a cytochrome's classification?

<p>Family, subfamily, gene name (D)</p> Signup and view all the answers

Which part of a cytochrome's classification is not mentioned in the passage?

<p>The enzyme function (A)</p> Signup and view all the answers

What is the purpose of the number at the end of the cytochrome name?

<p>To specify the subfamily of enzymes (C)</p> Signup and view all the answers

What is the general term for the enzymes denoted by the 'CYP' prefix?

<p>Cytochrome P450 oxidases (B)</p> Signup and view all the answers

What is the major distinction between different cytochrome P450 enzymes?

<p>Substrate specificity (A)</p> Signup and view all the answers

What is the purpose of the 'CYP' prefix in enzyme names?

<p>To identify the enzyme as a member of the cytochrome P450 family (D)</p> Signup and view all the answers

What is the significance of the 'CYP' prefix in understanding enzyme function?

<p>It identifies the enzyme as a cytochrome P450 oxidase (B)</p> Signup and view all the answers

What is the primary mechanism of action of Diazepam in the liver?

<p>Deesterification (D)</p> Signup and view all the answers

What is the result of demethylation of the amine group in Diazepam?

<p>Inactivation of the compound (A)</p> Signup and view all the answers

What is the purpose of adding an acetyl group to the active compound?

<p>To inactivate it (D)</p> Signup and view all the answers

What is the result of hydroxylation of the third position of the compound?

<p>Increased activity of the compound (D)</p> Signup and view all the answers

What is the role of the liver in the metabolism of Diazepam?

<p>Conversion to an active form (C)</p> Signup and view all the answers

What is the effect of deesterification on the compound?

<p>Conversion to a more active form (D)</p> Signup and view all the answers

What is the purpose of administering Diazepam in ester form?

<p>To delay its onset of action (B)</p> Signup and view all the answers

What is the result of converting the active compound to an inactive form?

<p>Decreased potency of the compound (C)</p> Signup and view all the answers

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Study Notes

Drug Metabolism

  • Diazepam is taken in ester form and undergoes several steps of metabolism to produce an inactive compound when it reaches the liver.
  • Deesterification occurs in the liver, converting the ester form to its active form.

Enzymatic Reactions

  • Addition of acetyl groups to the active compound to inactivate it (e.g., acetylation of isoniazid)
  • Hydroxylation of the third position of the compound (e.g., diazepam)
  • Demethylation of amine groups
  • Oxidation of alcohols to acids
  • Hydrolysis of esters and amides to yield COOH, NH2, and OH groups
  • Reduction of azo and nitro compounds to give NH2 moieties

Sites of Drug Biotransformation

  • The liver is the most important organ in drug metabolism and detoxification of endogenous and exogenous compounds.
  • The liver contains a wide range of enzymes, including cytochrome P450 (CYP) enzymes.

Cytochrome P450 (CYP) Enzymes

  • CYP enzymes are a superfamily of enzymes responsible for various drug metabolism reactions.
  • The CYP enzyme name is composed of:
    • A number specifying the cytochrome family (CYP1, CYP2, CYP3, etc.)
    • A capital letter representing the subfamily (CYP1A, CYP1B, CYP2A, CYP2B, CYP3B, etc.)
    • A number specifying the specific enzyme responsible for a particular reaction (CYP1A2, CYP2C9, CYP2C19, etc.)

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