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Pharmacology Guide

Sleep

Date Created
Date Modified

Temazepam (Restoril) | Triazolam (Halcion) | Zolpidem (Ambien)

 

Temazepam

Restoril

Mechanism of Action

Like other benzodiazepines such as diazepam it enhances the inhibitory action of GABA.

Therapeutic Use

Treatment of insomnia (disturbed sleep).

Absorption

Peak effect, 2-4 hours. Well absorbed.

Metabolism

Metabolized by conjugation with glucuronic acid in the liver.

Half-life

11 Hours.

Average Daily Dose (adult)

15 mg before retiring.

Adverse Effects

Drowsiness, dizziness, headache, fatigue, dependence and loss of memory.

Drug Interaction

Can cause excessive sedation when combined with other CNS depressants.

Contraindication

Pregnancy. Use with caution in severely depressed individuals.
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Triazolam

Halcion

Mechanism of Action

Like other benzodiazepines such as diazepam it enhances the inhibitory action of GABA.

Therapeutic Use

Short term treatment of insomnia (disturbed sleep).

Absorption

Well absorbed. Time for Peak effect, .5-2 hours following oral administration.

Metabolism

Metabolized in the liver by P-450 enzymes.

Half-life

1.5-5.5 hours.

Average Daily Dose (adult)

0.125-0.25 mg before retiring.

Adverse Effects

Rebound insomnia, amnesia (loss of memory), headache, ataxia (muscular incoordination) and dependence.

Drug Interaction

Triazolam produces additive CNS depressant effects when coadministered with other CNS depressants Should not be taken with other drugs that inhibit CYP 3A such as; ketoconazole, itraconazole and nefazodone.

Contraindication

Pregnancy. Hypersensitivity to benzodiazepines.
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Zolpidem

Ambien

Mechanism of Action

Binds to the benzodiazepine receptor and enhances the inhibitory action of GABA.

Therapeutic Use

Short term treatment of insomnia (disturbed sleep).

Absorption

Rapid absorption from the GI tract. Peak effect, 1.6 hours.

Metabolism

Metabolized in the liver and metabolites are eliminated in the urine.

Half-life

1.4-3.8 hours.

Average Daily Dose (adult)

10 mg before bedtime.

Adverse Effects

Headache, daytime drowsiness, lethargy and dizziness.

Drug Interaction

Use with caution in patients using other CNS depressants. No significant drug interactions have been observed.

Contraindication

Use with caution in patients with liver disease.
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These brief pharmaceutical summaries do not include all information important for patient use and should not be used as a substitute for professional medical advice. Consult the prescribing doctor and read package inserts before using these or any other medications or supplements.


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