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12 Cards in this Set
- Front
- Back
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Which benzodiazepines are long lasting?
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Clonazepam
Diazepam Chlozepate Chlordiazepaxide Flurazepam |
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Clonazepam:
Onset of anxiolytic effect after an oral dose? T1/2 (hrs)? Usual dose range (mg/d)? Dose equivalent (mg)? 3H diazepam binding (nM)? Active metabolites? FDA indications? Clinical uses? |
Onset of anxiolytic effect after an oral dose: Intermediate
T1/2: 15-40 hrs Usual dose range (mg/d): 0.5-3.0 Dose equivalent (mg): 0.25 3H diazepam binding (nM):1.5 Active metabolites: - FDA indications: Panic disorder, seizure disorder Clinical uses: Longer t1/2 may facilitate tapering in panic disorder |
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Diazepam:
Onset of anxiolytic effect after an oral dose? T1/2 (hrs)? Usual dose range (mg/d)? Dose equivalent (mg)? 3H diazepam binding (nM)? Active metabolites? FDA indications? Clinical uses? |
Onset of anxiolytic effect after an oral dose: rapid
T1/2 (hrs): 30-100 Usual dose range (mg/d): 15-50 Dose equivalent (mg):5.0 3H diazepam binding (nM): 6.3 Active metabolites: + FDA indications: Anxiety, Alcohol Clinical uses: - |
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Chloazepate:
Onset of anxiolytic effect after an oral dose? T1/2 (hrs)? Usual dose range (mg/d)? Dose equivalent (mg)? 3H diazepam binding (nM)? Active metabolites? FDA indications? Clinical uses? |
Onset of anxiolytic effect after an oral dose: rapid
T1/2 (hrs): 30-100 Usual dose range (mg/d): 15-60 Dose equivalent (mg): 7.5 3H diazepam binding (nM): 41 Active metabolites: + FDA indications: Anxiety Clinical uses: - |
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Chlordiazepaxide:
Onset of anxiolytic effect after an oral dose? T1/2 (hrs)? Usual dose range (mg/d)? Dose equivalent (mg)? 3H diazepam binding (nM)? Active metabolites? FDA indications? Clinical uses? |
Onset of anxiolytic effect after an oral dose: intermediate
T1/2 (hrs): 30-100 Usual dose range (mg/d): 30-200 Dose equivalent (mg): 10.0 3H diazepam binding (nM): 220 Active metabolites: +++ FDA indications: Anxiety, Alcohol withdrawl Clinical uses: Accumulation of active metabolite, problem in elderly |
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Flurazepam:
Onset of anxiolytic effect after an oral dose? T1/2 (hrs)? Usual dose range (mg/d)? Dose equivalent (mg)? 3H diazepam binding (nM)? Active metabolites? FDA indications? Clinical uses? |
Onset of anxiolytic effect after an oral dose: intermediate
T1/2 (hrs): 100 Usual dose range (mg/d): 15-30 Dose equivalent (mg): - 3H diazepam binding (nM): - Active metabolites: ++ FDA indications: Hypnotic (sleep) Clinical uses: - |
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Alprazolam:
Onset of anxiolytic effect after an oral dose? T1/2 (hrs)? Usual dose range (mg/d)? Dose equivalent (mg)? 3H diazepam binding (nM)? Active metabolites? FDA indications? Clinical uses? |
Onset of anxiolytic effect after an oral dose: intermediate
T1/2 (hrs): 6-20 Usual dose range (mg/d): 1-6 Dose equivalent (mg):0.5 3H diazepam binding (nM): - Active metabolites: - FDA indications: Panic disorder, anxiety Clinical uses: Short t1/2 can lead to rebound anxiety and tapering difficulties |
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Lorazepam:
Onset of anxiolytic effect after an oral dose? T1/2 (hrs)? Usual dose range (mg/d)? Dose equivalent (mg)? 3H diazepam binding (nM)? Active metabolites? FDA indications? Clinical uses? |
Onset of anxiolytic effect after an oral dose: Intermediate
T1/2 (hrs): 10-20 Usual dose range (mg/d): 1.5-8.0 Dose equivalent (mg):1.0 3H diazepam binding (nM): 2.7 Active metabolites: - FDA indications: Anxiety Clinical uses: V&IMI preparations available for severe anxiety/agitation |
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Oxazepam:
Onset of anxiolytic effect after an oral dose? T1/2 (hrs)? Usual dose range (mg/d)? Dose equivalent (mg)? 3H diazepam binding (nM)? Active metabolites? FDA indications? Clinical uses? |
Onset of anxiolytic effect after an oral dose: intermediate-slow
T1/2 (hrs): 8-12 Usual dose range (mg/d): 30-120 Dose equivalent (mg): 15 3H diazepam binding (nM): 14 Active metabolites: - FDA indications: Anxiety, alcohol withdrawal Clinical uses: Not reinforcing due to slower onset. Indicated in pts with h/o substance abuse. |
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Describe the metabolism and elimination of diazepam
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Diazepam has a plasma half-life of >24 hours. The drug is metabolized by a process of desmethylation and hydroxylation to form several compounds. These metabolites do have antianxiety properties and almost certainly contribute to the overall therapeutic response to diazepam. The metabolites have even longer plasma half-lives than does the parent drug. Following the oral administration of a single dose of diazepam, 8-12 days are required for complete elimination of the drug and its metabolites.
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What are issues with short-acting compounds?
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The short-acting drugs must be given 2 or 3 times daily and inadvertent omission of a dose or abrupt discontinuation of therapy, may lead to rapid decline in blood levels with reappearance of anxiety symptoms or withdrawal syndrome.
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What SRIs are useful for anxiety disorders?
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Fluoxetine
Fluvoxamine Paroxetine Sertaline |
