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Traumatic Brain Injury Pharmacology Guide: Sleep

Pharmacology Guide


Sleep

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



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.



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.



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.

References:



General References:

Zafonte, R., Mann, N., & Fichtenberg, N. (1996). Sleep disturbance in traumatic brain injury: pharmacologic options. Neurorehabilitation. 7(3), 189-196.