Podcast
Questions and Answers
Which benzodiazepine has the fastest onset of action?
Which benzodiazepine has the fastest onset of action?
Which benzodiazepine has the longest half-life?
Which benzodiazepine has the longest half-life?
Which benzodiazepine is most likely to interact with tricyclic antidepressants (TCAs)?
Which benzodiazepine is most likely to interact with tricyclic antidepressants (TCAs)?
Which benzodiazepine is contraindicated for concurrent use with ketoconazole?
Which benzodiazepine is contraindicated for concurrent use with ketoconazole?
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Which benzodiazepine is most likely to have decreased clinical effect when taken with phenytoin?
Which benzodiazepine is most likely to have decreased clinical effect when taken with phenytoin?
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Which patient education recommendation is most important for benzodiazepine users?
Which patient education recommendation is most important for benzodiazepine users?
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Which statement about the use of benzodiazepines in geriatric patients is true?
Which statement about the use of benzodiazepines in geriatric patients is true?
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Which of the following is NOT a major adverse effect of benzodiazepines?
Which of the following is NOT a major adverse effect of benzodiazepines?
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Which of the following is a common side effect of benzodiazepines?
Which of the following is a common side effect of benzodiazepines?
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Which drug interaction is of greatest concern with benzodiazepines?
Which drug interaction is of greatest concern with benzodiazepines?
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Which benzodiazepine is the treatment of choice for status epilepticus?
Which benzodiazepine is the treatment of choice for status epilepticus?
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Which benzodiazepine is preferred for long-term treatment of anxiety?
Which benzodiazepine is preferred for long-term treatment of anxiety?
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How do benzodiazepines exert their anxiolytic and sedative effects?
How do benzodiazepines exert their anxiolytic and sedative effects?
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Which drug is less likely to cause dependence due to its long action?
Which drug is less likely to cause dependence due to its long action?
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What is the primary concern related to benzodiazepine use?
What is the primary concern related to benzodiazepine use?
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How should the use of benzodiazepines be discontinued to avoid severe withdrawal symptoms?
How should the use of benzodiazepines be discontinued to avoid severe withdrawal symptoms?
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In what type of disease condition should benzodiazepines be avoided?
In what type of disease condition should benzodiazepines be avoided?
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Which benzodiazepine is metabolized by conjugation and is better tolerated by patients with impaired liver function?
Which benzodiazepine is metabolized by conjugation and is better tolerated by patients with impaired liver function?
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What distinguishes alprazolam (Xanax) and lorazepam (Ativan) from clonazepam (Klonopin) regarding dependence risk?
What distinguishes alprazolam (Xanax) and lorazepam (Ativan) from clonazepam (Klonopin) regarding dependence risk?
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Which factor influences the duration of effect of benzodiazepines more than the parent drug?
Which factor influences the duration of effect of benzodiazepines more than the parent drug?
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What should be done regarding benzodiazepine usage for children younger than 6 years?
What should be done regarding benzodiazepine usage for children younger than 6 years?
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What should be done to avoid withdrawal symptoms when discontinuing benzodiazepine use?
What should be done to avoid withdrawal symptoms when discontinuing benzodiazepine use?
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According to the passage, which of the following is NOT a class of drugs used to treat anxiety?
According to the passage, which of the following is NOT a class of drugs used to treat anxiety?
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How do benzodiazepines, such as diazepam or alprazolam, differ from other gaba-ergic drugs in their mechanism of action?
How do benzodiazepines, such as diazepam or alprazolam, differ from other gaba-ergic drugs in their mechanism of action?
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What is the net effect of inhibiting GABA, according to the passage?
What is the net effect of inhibiting GABA, according to the passage?
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What is the primary reason the prescriber needs to select a specific drug to treat anxiety?
What is the primary reason the prescriber needs to select a specific drug to treat anxiety?
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What is the primary reason benzodiazepines have been frequently prescribed to treat anxiety and insomnia, according to the passage?
What is the primary reason benzodiazepines have been frequently prescribed to treat anxiety and insomnia, according to the passage?
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Study Notes
Benzodiazepines
- Benzodiazepines are a class of drugs that are thought to exert their anxiolytic and sedative effects by increasing the action of GABA, an inhibitory neurotransmitter, thereby decreasing the effect of neuronal excitation.
- Within the GABA receptor is an area that the benzodiazepines bind to, referred to as the benzodiazepine receptor.
Pharmacokinetics
- Benzodiazepines are rapidly and widely distributed after oral administration and reach their peak levels within 30 minutes to 6 to 8 hours.
- Chlordiazepoxide (Librium) and diazepam (Valium) are slowly and inconsistently absorbed after intramuscular administration, but lorazepam (Ativan) and midazolam are rapidly absorbed and widely distributed after IM injection.
- These drugs are lipid-soluble and highly protein-bound, which means that they may have prolonged activity in obese people and compete with other protein-bound drugs for receptor sites.
Metabolism and Excretion
- Benzodiazepines are metabolized in the liver and biotransformed by oxidation or conjugation.
- Lorazepam and temazepam are biotransformed by conjugation and are better tolerated by patients with impaired liver function, are elderly, or are smokers.
- Benzodiazepines metabolized by oxidation may have a prolonged effect in older adults.
- Duration of effect is influenced by the lipid-solubility and the half-life of the active metabolites more than the parent drug.
Pharmacotherapeutics
- Precautions and contraindications include the development of dependence, which can be psychological as well as physical, and is of concern with the benzodiazepines.
- Dependence is less likely with clonazepam (Klonopin) because of its long action.
- Symptoms of withdrawal, which usually occur 1 to 2 days after the last dose of short-acting benzodiazepines and 5 to 10 days after the last dose of the long-acting compounds, resemble withdrawal symptoms of other CNS depressants.
- Use of the drug should be gradually tapered rather than abruptly discontinued because of the risk of severe withdrawal symptoms.
Drug Interactions
- Benzodiazepines can interact with other CNS depressants, such as barbiturates, alcohol, antihistamines, and neuroleptics, because of their additive effects.
- Benzodiazepines also increase the blood levels of TCAs and digitalis preparations.
- Concurrent administration with other CNS depressants should be avoided.
Clinical Use and Dosing
- Benzodiazepines are indicated for the short-term treatment of anxiety and anxiety-related disorders.
- Additional uses include muscle relaxants, emergency treatment of status epilepticus, irritable bowel syndrome, chemotherapy-induced nausea and vomiting, and restless legs syndrome.
- Diazepam is the treatment of choice for status epilepticus, administered by a parenteral route (preferably IV), because of the rapidity of absorption and effect.
Rational Drug Selection
- All of the benzodiazepines are equally efficacious, and drug selection depends on the patient’s and prescriber’s preference and the patient’s side-effect profile.
- For long-term treatment of anxiety, other classes of drugs should be considered first (e.g., buspirone or SSRIs); and if the benzodiazepine is necessary, then clonazepam is preferred due to its long half-life and daily dosing ability.
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Description
Test your knowledge on drugs used to treat anxiety, focusing on the pharmacological actions of anxiolytics and hypnotics. Learn about serotonergics, gaba-ergics, dopaminergics, and benzodiazepines like diazepam and alprazolam.
