WHO Expert Committee on Drug Dependence – WHO Technical Report Series, No. 915 – Thirty-third Report
(2003; 31 pages) [French] [Spanish] View the PDF document
Table of Contents
View the document1. Introduction
View the document2. Scheduling criteria
Open this folder and view contents3. Critical review of psychoactive substances
Close this folder4. Pre-review of psychoactive substances
View the document4.1 Ketamine (INN)
View the document4.2 Zaleplon (INN)
View the document4.3 Zopiclone (INN)
View the document4.4 Butorphanol (INN)
View the document4.5 Oripavine
View the document4.6 Khat
View the document5. Terminology used in reporting abuse-related adverse drug reactions
View the document6. Other matters
View the documentAcknowledgements
View the documentReferences
View the documentAnnex Terminology used in reporting abuse-related adverse drug reactions

4.2 Zaleplon (INN)

Zaleplon, chemical name 3’-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)-N-ethylacetanilide, has not previously been reviewed by WHO. Zaleplon selectively binds to the brain alpha subunit of the GABAA omega-1 receptor. Its pharmacological properties are similar to those of zolpidem, and it is indicated for the short-term (2 to 4 weeks) management of insomnia. It produces a benzodiazepine-type withdrawal syndrome upon discontinuation of long-term use and studies on subjective effects show its similarity to triazolam. Zaleplon has been on the market for only a short time and the number of reports of abuse-related adverse drug reactions received by the international drug monitoring programme are as yet very few.


Although the abuse potential of this substance is considered to be similar to that of zolpidem and triazolam, critical review was not recommended at this stage as the information on actual abuse available to the Committee was insufficient to confirm the existence of significant public health and social problems in more than one country. However, the Committee recommended that WHO continue the surveillance of zaleplon1.

1 One Member of the Committee (Professor M.S. Bourin) expressed his concern regarding the potential for abuse of and dependence on zaleplon and felt that a critical review was warranted.

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