Cinitapride Explained

Cinitapride (trade names Cintapro, Pemix) is a gastroprokinetic agent and antiemetic agent of the benzamide class which is marketed in India, Mexico, Pakistan and Spain.[1] [2] It acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors.[3] [4]

Uses

It is indicated for the treatment of gastrointestinal disorders associated with motility disturbances such as gastroesophageal reflux disease, non-ulcer dyspepsia and delayed gastric emptying. It may be also used in the management of nausea and vomiting.

Synthesis

Cinitapride is the amide formed by reacting methyl 4-amino-2-ethoxy-5-nitrobenzoate (1) with the 4-aminopiperidine derivative (2).[5] [6]

Notes and References

  1. Robert M, Salvà M, Segarra R . The prokinetic cinitapride has no clinically relevant pharmacokinetic interaction and effect on QT during coadministration with ketoconazole . Drug Metabolism and Disposition . 35 . 7 . 1149–56 . July 2007 . 17437965 . 10.1124/dmd.106.010835 . 1284844 . etal.
  2. Fernández AG, Massingham R . Peripheral receptor populations involved in the regulation of gastrointestinal motility and the pharmacological actions of metoclopramide-like drugs . Life Sciences . 36 . 1 . 1–14 . January 1985 . 2981378 . 10.1016/0024-3205(85)90280-2.
  3. Alarcón-de-la-Lastra Romero C, López A, Martín MJ, la Casa C, Motilva V . Cinitapride protects against ethanol-induced gastric mucosal injury in rats: role of 5-hydroxytryptamine, prostaglandins and sulfhydryl compounds . Pharmacology . 54 . 4 . 193–202 . April 1997 . 9211565 . 10.1159/000139487.
  4. Alarcón de la Lastra C, La Casa C, Martin MJ, Motilva V . Effects of cinitapride on gastric ulceration and secretion in rats . Inflammation Research . 47 . 3 . 131–6 . March 1998 . 9562338 . 10.1007/s000110050301 . 25620004 . 2010-02-27 . https://web.archive.org/web/19990827033745/http://link.springer-ny.com/link/service/journals/00011/bibs/8047003/80470131.htm . 1999-08-27 . dead .
  5. GB . 1574419 . Piperidine compounds . Inglesias, J.B; Soto, J.P; Noverola, A.V; Mauri, J.M . patent . 1980-09-03 . 1977-11-11 . 1977-11-11 . Anphar SA .
  6. Web site: Cinitapride . Thieme . 2024-07-02.

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