Questions and Answers
What is an anxiolytic?
Antianxiety and anti-panic disorder drug.
What is the chemical name for Xanax?
Alprazolam
What is the half-life of Xanax?
11-15 hours
What is the chemical name for Librium?
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What is the half-life of Librium?
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What is the chemical name for Valium?
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What is the half-life of Valium?
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What is the chemical name for Ativan?
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What is the half-life of Ativan?
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What is the general benzodiazepine structure derived from?
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The advantages of benzodiazepines over barbiturates include fewer side effects and being much safer in _____.
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What can develop within a week of initiating benzodiazepine therapy?
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Tolerance to the anxiolytic effects develops quickly and to a greater degree than sedative effects.
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What neurotransmitter do benzodiazepines mainly act on?
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What is one of the therapeutic uses of benzodiazepines?
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Which of the following are classified as long-acting benzodiazepines? (Select all that apply)
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Benzodiazepines have a high risk of dependence with extended use.
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Study Notes
Benzodiazepines Overview
- Anxiolytics are drugs used to treat anxiety and panic disorders.
Specific Benzodiazepines and Their Properties
- Alprazolam (Xanax): Half-life of 11-15 hours.
- Chlordiazepoxide (Librium): Half-life of 5-30 hours.
- Diazepam (Valium): Longer half-lives, exceeding 24 hours.
- Lorazepam (Ativan): Half-lives range from 20-50 hours.
Structural Characteristics
- Benzodiazepines consist of a benzene ring and a seven-member diazepine ring, plus a phenyl group at the 5-position essential for activity.
- Electron-withdrawing groups at the R7 position, like chlorine or nitro groups, enhance activity.
Potency and Duration Modifications
- Smaller substituents on position N1 can decrease potency.
- Larger substituents on position N1 may increase potency.
- Adding an additional ring to positions 1 and 2 of the diazepine ring results in higher potency.
Advantages Over Barbiturates
- Benzodiazepines have fewer side effects and a larger safety margin in overdose compared to barbiturates.
Therapeutic Uses and Mechanism
- Commonly used to treat anxiety; notable examples include diazepam and alprazolam from the 1970s and 1980s, respectively.
- Anxiolytic effects arise from inhibitory actions in the brain related to anxiety induction, primarily via GABAa receptors.
Enhanced Potency Variants
- Imidazo- and triazolo-benzodiazepines are highly potent due to additional rings at the diazepine positions 1 and 2.
Illicit Drug Interaction
- Combining benzodiazepines with opiates enhances the euphoric effects.
- Cocaine can lower the seizure threshold and provides calming effects after binge use.
- Benzodiazepines are utilized in treating alcohol withdrawal to prevent seizures during detoxification.
Tolerance and Dependence
- Rapid tolerance to sedative effects can develop within a week, while tolerance to anxiolytic effects develops more slowly.
- Long-term use can lead to dependence; 35% of users for over four weeks may experience withdrawal symptoms after stopping.
- Higher potency and shorter half-life benzodiazepines are linked to an increased risk of dependence.
Pharmacokinetics
- Benzodiazepines are metabolized in the liver through Phase I (hydroxylation, dealkylation, etc.) and Phase II reactions (conjugation with glucuronic acid), with hydroxy metabolites being major urinary products.
Benzodiazepine Duration Classification
- Short-acting: Elimination half-lives of a few hours (e.g., midazolam, triazolam).
- Intermediate-acting: Half-lives of 6-24 hours (e.g., alprazolam, lorazepam).
- Long-acting: Half-lives greater than 24 hours (e.g., diazepam, quazepam).
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Description
This quiz covers essential terms and definitions related to benzodiazepines, including their chemical names and half-lives. Study key anxiolytic medications like Xanax, Librium, and Valium. Perfect for pharmacology students looking to enhance their understanding of these important drugs.
