Arfendazam

Arfendazam is a drug which is a benzodiazepine derivative. Arfendazam is a 1,5-benzodiazepine, with the nitrogen atoms located at positions 1 and 5 of the diazepine ring, and so is most closely related to other 1,5-benzodiazepines such as clobazam.

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Arfendazam has sedative and anxiolytic effects similar to those produced by other benzodiazepine derivatives, but is a partial agonist at GABA_A receptors, so the sedative effects are relatively mild and it produces muscle relaxant effects only at very high doses.^[1][2]

Arfendazam produces an active metabolite lofendazam, which is thought to be responsible for part of its effects.^[3]

References

1. ^ Müller E. Benzodiazepine receptor interactions of arfendazam, a novel 1, 5-benzodiazepine. Pharmacopsychiatry 1985, (18):10-11.
2. ^ Müller WE, Groh B, Bub O. In vitro and in vivo studies of the mechanism of action of arfendazam, a novel 1, 5-benzodiazepine. Pharmacopsychiatry 1986, (10):314-315.
3. ^ J. Adrien, F. Albani, A. Baruzzi, M. Berger, E.O. Bixler, A.A. Borbeley, D.G. Dikeos, R. Drucker-Colin, R. Fritsch Montero, Y. Hishikawa, S. Inoue, A. Kales, E. Lugaresi, H. Merchant-Nancy, J.M. Monti. The Pharmacology of Sleep. Springer. ISBN 978-3540589617