28 Questions
What is the resulting functional group from the oxidation of a primary alcohol?
Carboxylic acid
Which of the following reactions does not involve the formation of a NH2 group?
Oxidation of primary alcohols
What is the product of the hydrolysis of an ester?
Carboxylic acid and an alcohol
Which of the following compounds cannot be reduced to form a NH2 group?
Ester
What is the byproduct of the hydrolysis of an amide?
H2O
What is the primary reason the liver is the most important organ in drug metabolism and detoxification?
It contains almost all the necessary enzymes for biotransformation
What types of compounds does the liver metabolize and detoxify?
Both endogenous and exogenous compounds
Why is the liver considered a critical organ in the body?
It has a high concentration of enzymes for biotransformation
What is the significance of the liver's dual blood supply system in drug metabolism?
It provides the liver with a constant supply of substrates for biotransformation
What is a unique feature of the liver that enables it to perform its functions in drug metabolism?
It has the ability to regenerate itself
What is the first part of a cytochrome's classification?
A number specifying the cytochrome family
Which of the following is an example of a cytochrome subfamily?
CYP1A
What is the purpose of the capital letter in a cytochrome's classification?
To denote the subfamily
What is the correct order of a cytochrome's classification?
Family, subfamily, gene name
Which part of a cytochrome's classification is not mentioned in the passage?
The enzyme function
What is the purpose of the number at the end of the cytochrome name?
To specify the subfamily of enzymes
What is the general term for the enzymes denoted by the 'CYP' prefix?
Cytochrome P450 oxidases
What is the major distinction between different cytochrome P450 enzymes?
Substrate specificity
What is the purpose of the 'CYP' prefix in enzyme names?
To identify the enzyme as a member of the cytochrome P450 family
What is the significance of the 'CYP' prefix in understanding enzyme function?
It identifies the enzyme as a cytochrome P450 oxidase
What is the primary mechanism of action of Diazepam in the liver?
Deesterification
What is the result of demethylation of the amine group in Diazepam?
Inactivation of the compound
What is the purpose of adding an acetyl group to the active compound?
To inactivate it
What is the result of hydroxylation of the third position of the compound?
Increased activity of the compound
What is the role of the liver in the metabolism of Diazepam?
Conversion to an active form
What is the effect of deesterification on the compound?
Conversion to a more active form
What is the purpose of administering Diazepam in ester form?
To delay its onset of action
What is the result of converting the active compound to an inactive form?
Decreased potency of the compound
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.)
This quiz covers the metabolism of Diazonamide, a drug used to treat epilepsy, and its deesterification in the liver to produce an active compound.
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