Pronunciation: ess-TA-zoh-lam

Chemical Abstracts Service Registry Number: 29975-16-4 Formal Names: ProSom

Type: Depressant (benzodiazepine class). See page 21 Federal Schedule Listing: Schedule IV (DEA no. 2756) USA Availability: Prescription Pregnancy Category: X

Uses. Estazolam's main medical uses are for relaxing muscles, fighting convulsions, and inducing sleep. The compound can also reduce anxiety in insomniacs but is not intended for long-term use against insomnia. Estazolam has been used successfully to treat auditory hallucinations and to improve the general mental state of schizophrenics. The drug is considered more potent than diazepam. Insomnia studies show estazolam to be about 15 times stronger than flurazepam.

Drawbacks. Estazolam may, at inappropriate times, make people lightheaded or sleepy and interfere with movement. Constipation and dry mouth are common. Even at high doses the drug's hindrance of respiration is of no concern in persons who breathe normally but might be troublesome for persons who have impaired breathing—although experimental results have been reassuring even for that population. A rebound effect can occur when people stop taking the drug for insomnia, meaning that sleep disturbance temporarily becomes worse than it was before treatment. In one study the most common adverse effect was feeling tired the day after using the drug. Other volunteers have experienced lower mental acuity and pulse rate 10 hours after taking the drug, even after getting a good night's sleep.

Abuse factors. Withdrawal symptoms are usually minor if a person takes estazolam long enough to produce dependence, but unusual reports exist of delirium and dangerous seizures during withdrawal.

Drug interactions. Estazolam actions can be boosted by alcohol, barbiturates, opiates, antihistamines, and monoamine oxidase inhibitors (MAOIs— found in some antidepressants). Cigarette smoking can shorten the time that an estazolam dose lasts.

Cancer. Long-term experiments with rats and mice found no sign that es-tazolam causes cancer. Potential for causing human cancer is unknown.

Pregnancy. A rat experiment produced no change in fertility. Estazolam is known to cause human birth defects, and pregnant women are never supposed to take the drug. Analysis of milk from nursing rats shows that esta-zolam and its breakdown products can pass into milk.

Additional scientific information may be found in:

Astrup, C., and L. Vatten. "Effect of the Benzodiazepine Derivative Estazolam in

Schizophrenia." Biological Psychiatry 19 (1984): 85-88. Cohn, J.B. "Hypnotic Efficacy of Estazolam Compared with Flurazepam in Outpatients with Insomnia." Journal of Clinical Pharmacology 31 (1991): 747-50. "Estazolam—A New Benzodiazepine Hypnotic." Medical Letter on Drugs and Therapeutics 33 (1991): 91-92.

Lingjaerde, O. "Effect of the Benzodiazepine Derivative Estazolam in Patients with Auditory Hallucinations. A Multicentre Double-Blind, Cross-Over Study." Acta Psychiatrica Scandinavica 65 (1982): 339-54. Pierce, M.W., V.S. Shu, and L.J. Groves. "Safety of Estazolam. The United States Clinical

Experience." American Journal of Medicine 88, no. 3A (1990): 12S-17S. Rosen, R.C., et al. "Psychophysiological Insomnia: Combined Effects of Pharmacotherapy and Relaxation-Based Treatments." Sleep Medicine 1 (2000): 279-88. Vogel, G.W., and D. Morris. "The Effects of Estazolam on Sleep, Performance, and Memory: Long-term Sleep Laboratory Study of Elderly Insomniacs." Journal of Clinical Pharmacology 32 (1992): 647-51.

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