Alpidem

drugbox
IUPAC_name = "2- [3-chloro-8-(4-chlorophenyl)-1,7-diazabicyclo [4.3.0]
nona-2,4,6,8-tetraen-9-yl] -N,N-dipropyl-acetamide"

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width = 160
CAS_number = 82626-01-5
ATC_prefix =
ATC_suffix =
PubChem = 54897
DrugBank =
C = 21 | H = 23 | Cl = 2 | N = 3 | O = 1
molecular_weight = 404.332 g/mol
bioavailability =
metabolism =
elimination_half-life =
excretion = Renal
pregnancy_category =
routes_of_administration = Oral
formulations =

Alpidem (Ananxyl) is an anxiolytic drug from the imidazopyridine family, related to the more well known sleeping medication zolpidem. Unlike zolpidem however, alpidem does not produce sedative effects at normal doses, and is instead used specifically for the treatment of anxiety. [Zivkovic B, Morel E, Joly D, Perrault G, Sanger DJ, Lloyd KG. Pharmacological and behavioral profile of alpidem as an anxiolytic. "Synthelabo Recherche", L.E.R.S., Bagneux, France. 1990 May;23 Suppl 3:108-13. PMID 1974069] [Sanger DJ, Zivkovic B. Discriminative stimulus effects of alpidem, a new imidazopyridine anxiolytic. "Synthelabo Recherche", Bagneux, France. 1994 Jan;113(3-4):395-403. PMID 7862851]

Alpidem is a fairly recently introduced drug, and is not widely used. Alpidem acts selectively on the α3 receptor subtype and to a lesser extent at the α1 subtype (Kd of 0.33nM and 1.67nM respectively), of the benzodiazepine receptor. [ Langer SZ, Arbilla S, Benavides J, Scatton B. Zolpidem and alpidem: two imidazopyridines with selectivity for omega 1- and omega 3-receptor subtypes. "Advances in Biochememical Psychopharmacology". 1990;46:61-72.] [Langer SZ, Arbilla S, Tan S, Lloyd KG, George P, Allen J, Wick AE. Selectivity for omega-receptor subtypes as a strategy for the development of anxiolytic drugs. "Pharmacopsychiatry". 1990 May;23 Suppl 3:103-7.] However the chemical structure of alpidem is not related to that of the benzodiazepines, and alpidem is thus sometimes referred to as a nonbenzodiazepine. [Diamond BI, Nguyen H, O'Neal E, Ochs R, Kaffeman M, Borison RL. A comparative study of alpidem, a nonbenzodiazepine, and lorazepam in patients with nonpsychotic anxiety. "Psychopharmacology Bulletin". 1991;27(1):67-71.]

Indications

Alpidem is generally prescribed to patients with moderate to severe anxiety. [ Kunovac JL, Stahl SM. Future directions in anxiolytic pharmacotherapy. "Psychiatric Clinics of North America". 1995 Dec;18(4):895-909.] Most of these patients have exhibited either sensitivity or resistance to benzodiazepine therapy, and therefore switched to a non-benzodiazepine medication due to the reduced incidence of side effects relative to benzodiazepine drugs. [Morton S, Lader M. Studies with alpidem in normal volunteers and anxious patients. "Pharmacopsychiatry". 1990 May;23 Suppl 3:120-3.] [Frattola L, Garreau M, Piolti R, Bassi S, Albizzati MG, Borghi C, Morselli PL. Comparison of the efficacy, safety and withdrawal of alpidem and alprazolam in anxious patients. "British Journal of Psychiatry". 1994 Jul;165(2):94-100.] Alpidem produces little or no sedative or hypnotic action at normal doses but may produce sedation when used at a high dose, and only has anticonvulsant actions at much higher doses than those used clinically for the treatment of anxiety. [Zivkovic B, Morel E, Joly D, Perrault G, Sanger DJ, Lloyd KG. Pharmacological and behavioral profile of alpidem as an anxiolytic. "Pharmacopsychiatry". 1990 May;23 Suppl 3:108-13.]

Dangers

Alpidem was withdrawn from the market in most of the world following reports of severe liver damage caused by Ananxyl, [Baty V, Denis B, Goudot C, Bas V, Renkes P, Bigard MA, Boissel P, Gaucher P. Hepatitis induced by alpidem (Ananxyl). Four cases, one of them fatal. "Gastroenterologie Clinique et Biologique". 1994;18(12):1129-31. (French).] [Ausset P, Malavialle P, Vallet A, Miremont G, Le Bail B, Dumas F, Saric J, Winnock S. Subfulminant hepatitis caused by alpidem and treated by liver transplantation. "Gastroenterologie Clinique et Biologique". 1995 Feb;19(2):222-3. (French).] although other brands of alpidem may still be on sale in some countries.

ee also

* Zolpidem
* Anxiolytic
* Benzodiazepine (receptor)
* Imidazopyridines

References