Prazepam

Pronunciation: PRAY-zee-pam (also pronounced PRAZ-eh-pam)

Chemical Abstracts Service Registry Number: 2955-38-6

Formal Names: Centrax, Demetrin, Verstran

Type: Depressant (benzodiazepine class). See page 21

Federal Schedule Listing: Schedule IV (DEA no. 2764)

USA Availability: Prescription

Pregnancy Category: None

Uses. In the human body this long-acting drug converts into desmethyldi-azepam, which is called a metabolite. Desmethyldiazepam is the major metabolite of diazepam and also a metabolite of clorazepate dipotassium and chlordiazepoxide. Some researchers believe this metabolite produces the main drug effects of prazepam and that prazepam should therefore be considered a prodrug (meaning the substance itself has little drug value but that within the body it converts into another substance that is beneficial). Prazepam resembles oxazepam both in chemistry and in its effects.

Prazepam is used medically to relieve anxiety and is considered as effective as alprazolam and lorazepam for that purpose even though they are much stronger drugs than prazepam. One study found prazepam to work better than diazepam for treating anxiety, although diazepam is about twice as potent. A comparison with chlordiazepoxide showed mixed results; chlordiaze-poxide produced faster general betterment of anxiety, but prazepam was more effective at improving particular symptoms. Prazepam has also been used successfully for treatment of depression and crankiness. One clinical trial produced weight gain in patients using the drug, but perhaps this was due to better appetite resulting from better mood, rather than an inherent weight-promoting quality of the drug. Some scientists have wondered if the drug improves mood simply by helping patients to get better sleep; researchers investigating that question concluded that the drug does have antianxiety qualities causing the improvement. In evaluating results of a rat experiment, researchers concluded that prazepam may be useful for treating high blood pressure. Animal studies also find the drug to be a muscle relaxant and to reduce convulsions.

The drug has been used to help alcoholics withdraw from alcohol. In one study group several patients had experienced delirium tremens when with drawing from alcohol in the past, but no one suffered the affliction while receiving prazepam. A subsequent study of alcohol withdrawal management rated prazepam as better than placebo but not as good as chlordiazepoxide. The latter study also found that benefits declined with time; after 14 days the placebo, chlordiazepoxide, and prazepam groups of alcoholics were all faring the same. Also during the latter study, in comparison to placebo, about three times as many patients receiving prazepam broke sobriety—a curious and discouraging finding.

Drawbacks. Volunteers taking prazepam showed little sedation and little difference in mental ability tests when compared to performance before taking the drug. Prazepam has been praised for having fewer unwanted effects than diazepam, and for being better absorbed by the body than clorazepate dipo-tassium. In one experiment a single large dose at night produced less dizziness than taking three divided doses during the day, a factor relevant to the potential of falls (especially among the elderly). Unwanted effects can include dry mouth, weakness, and sleepiness. Tests comparing equivalent-strength oral doses of the drug in liquid and solid formats find the liquid version to be a more potent sedative, a difference ascribed to quicker absorption by the body. In an experiment testing the drug on people of various ages, a dose seemed to last longer in older men, but that change was not seen in older women. An experiment found the drug's effect on movement was similar to that of chlordiazepoxide, suggesting that operating an automobile might be dangerous when using prazepam.

Abuse factors. Not enough scientific information to report about prazepam's specific characteristics, but they should be consistent with general characteristics of the benzodiazepine class of depressants.

Drug interactions. The antacid remedy cimetidine probably slows the body's metabolism of prazepam. Scores on tests of reaction time and mental ability can become worse when alcohol is used along with prazepam.

Cancer. Two experiments, one with rats and one with mice, failed to demonstrate potential for causing cancer. Potential for causing human cancer is unknown.

Pregnancy. A small amount of the drug passes from a nursing mother into her milk.

Additional scientific information may be found in:

Daniel, J.T., and W.W.K. Zung. "Double Blind Clinical Comparison of Prazepam, Lor-azepam, Diazepam, and Placebo in the Treatment of Anxiety in a Private Surgical Outpatient Practice." Current Therapeutic Research: Clinical and Experimental 30 (1981): 417-26.

Dorman, T. "Multicenter Comparison of Prazepam and Diazepam in the Treatment of

Anxiety." Pharmatherapeutica 3 (1983): 433-40. Greenblatt, D.J., and R.I. Shader. "Prazepam and Lorazepam, Two New Benzodiazepines." New England Journal of Medicine 299 (1978): 1342-44. Guelfi, J.D., S. Lancrenon, and V. Millet. "Etude Comparative en Double Insu du Bro-mazepam versus Prazepam dans l'anxiete Non Psychotique [Comparative Double-Blind Study of Bromazepam versus Prazepam in Non-Psychotic Anxiety]." L'Encephale 19 (1993): 547-52. Abstract in English. Kingstone, E., A. Villeneuve, and I. Kossatz. "Double-Blind Evaluation of Prazepam,

Chlordiazepoxide and Placebo in Non-Psychotic Patients with Anxiety and Tension: Some Methodological Considerations." Current Therapeutic Research: Clinical and Experimental 11 (1969): 106-14.

"Prazepam." IARC Monographs on the Evaluation of the Carcinogenic Risk of Chemicals to Humans 66 (1996): 143-55.

Shaffer, J.W., et al. "A Comparison of the Effects of Prazepam, Chlordiazepoxide, and Placebo in the Short-Term Treatment of Convalescing Alcoholics." Journal of Clinical Pharmacology and the Journal of New Drugs 8 (1968): 392-99.

Zung, W.W.K., et al. "Comparison of the Incidence of Sedation in Anxious Outpatients Treated with Diazepam and Prazepam." Current Therapeutic Research: Clinical and Experimental 39 (1986): 480-89.

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