Alpidem
| Clinical data | |
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| Trade names | Ananxyl |
| Other names | SL 80.0342; SL800342; SL-800342 |
| Routes of administration | Oral administration |
| Drug class | Nonbenzodiazepine; GABAA receptor positive allosteric modulator; Anxiolytic |
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| Pharmacokinetic data | |
| Bioavailability | 32–35% (estimated)[1][2] |
| Protein binding | 99.4%[1] |
| Metabolism | Extensive (hydroxylation, dealkylation, conjugation)[1] |
| Metabolites | Many (some active)[1] |
| Onset of action | 1.0–2.5 hours (Cmax)[1] |
| Elimination half-life | Young adults: 19 hours (7–44 hours)[1] Elderly: 22.6 ± 2.3 hours[1] Children: 11.4 ± 1.9 hours[1] |
| Excretion | Mainly feces[1] |
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| ECHA InfoCard | 100.216.305 |
| Chemical and physical data | |
| Formula | C21H23Cl2N3O |
| Molar mass | 404.34 g·mol−1 |
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Alpidem, sold under the brand name Ananxyl, is a nonbenzodiazepine anxiolytic medication which was briefly used to treat anxiety disorders but is no longer marketed.[3] It was previously marketed in France, but was discontinued due to liver toxicity.[3] Alpidem is taken by mouth.[1]
Side effects of alpidem include sedation, fatigue, dizziness, and headache, among others.[3][2][4] It has much less to no impact on cognition, memory, and psychomotor function relative to benzodiazepines.[3][5] Similarly, no rebound anxiety or withdrawal symptoms have been observed with alpidem.[3][2] Rarely, alpidem can cause serious liver toxicity, including liver failure and death.[3] Alpidem is a nonbenzodiazepine of the imidazopyridine family, structurally related to the Z-drug zolpidem,[1] and acts as a GABAA receptor positive allosteric modulator of the benzodiazepine site of the receptor complex.[3] In contrast to zolpidem however, alpidem has anxiolytic effects rather than sedative or hypnotic effects at normal therapeutic doses.[3]
Alpidem was first described by 1982[6][7] and was introduced for medical use in France in 1991.[3][8][9] It was also under development for use in other countries in the 1990s, but development was discontinued and the drug was never marketed in any other country.[8][9] Alpidem was withdrawn from the market in France in 1993 due to liver toxicity.[10][11][12][13][3]
- ^ a b c d e f g h i j k Durand A, Thénot JP, Bianchetti G, Morselli PL (1992). "Comparative pharmacokinetic profile of two imidazopyridine drugs: zolpidem and alpidem". Drug Metabolism Reviews. 24 (2): 239–266. doi:10.3109/03602539208996294. PMID 1576937.
- ^ a b c Morselli PL (May 1990). "On the therapeutic action of alpidem in anxiety disorders: an overview of the European data". Pharmacopsychiatry. 23 (Suppl 3): 129–134. doi:10.1055/s-2007-1014549. PMID 1974073.
- ^ a b c d e f g h i j Skolnick P (November 2012). "Anxioselective anxiolytics: on a quest for the Holy Grail". Trends in Pharmacological Sciences. 33 (11): 611–620. doi:10.1016/j.tips.2012.08.003. PMC 3482271. PMID 22981367.
- ^ Cite error: The named reference
pmid1974071was invoked but never defined (see the help page). - ^ Cite error: The named reference
pmid1974069was invoked but never defined (see the help page). - ^ Cite error: The named reference
Elks2014was invoked but never defined (see the help page). - ^ Saletu B, Grünberger J, Linzmayer L (April 1986). "Pharmacokinetic and dynamic studies with a new anxiolytic imidazo-pyridine alpidem utilizing pharmaco-EEG and psychometry". International Clinical Psychopharmacology. 1 (2): 145–164. doi:10.1097/00004850-198604000-00006. PMID 2883214.
- ^ a b Cite error: The named reference
AdisInsightwas invoked but never defined (see the help page). - ^ a b Cite error: The named reference
Micromedexwas invoked but never defined (see the help page). - ^ Guengerich FP (2011). "Mechanisms of drug toxicity and relevance to pharmaceutical development". Drug Metabolism and Pharmacokinetics. 26 (1): 3–14. doi:10.2133/dmpk.dmpk-10-rv-062. PMC 4707670. PMID 20978361.
- ^ "ANANXYL WITHDRAWN FROM MARKET IN FRANCE - Pharmaceutical industry news".
- ^ "La commercialisation de l'Ananxyl est suspendue pour un an". Le Monde.fr. 26 October 1993.
- ^ WHO Drug Information Vol. 8, No. 2, 1994, page 64