Chemistry:Cinepazide
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| Formula | C22H31N3O5 |
| Molar mass | 417.49864 g·mol−1 |
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Cinepazide or cinepazide maleate[1] (Kelinao or Anjieli in China[2][3]) is a vasodilator used in China for the treatment of cardiovascular and cerebrovascular diseases, and peripheral vascular diseases.[4] It appears to work by potentiating A2 adenosine receptors.[5]
History
Cinepazide was discovered by scientists at Laboratoires Delalande (now part of Sanofi) in 1969 in an effort to explore useful substituted cinnamoyl-piperazine compounds.[6][7] The drug, in the form of a pill taken orally, was launched by Delalande in 1976 under the tradename Vasodistal, for treatment of heart failure, balance disorders, cerebrovascular disease, and vascular complications of diabetes.[6][8] In 1988 the drug was withdrawn from the market in Spain due to risk of agranulocytosis; other countries where the drug was available added warnings to the label.[9][10] It was withdrawn from the market in France in 1992.[11] The drug had also been marketed in Japan by Daiichi Pharmeceutical Company under the brand name "Brindel"[2] for dementia, but was withdrawn in 1999, following a review by the Japanese regulatory authorities of dementia drugs after a drug, calcium hopantenate, that had been considered the standard of care and against which cinepazide and other dementia drugs had been compared, had failed to demonstrate efficacy in a re-evaluation.[12]
In 2002 Sihuan Pharmaceutical brought an injectable form of the drug to market in China;[13] Sihuan had acquired the drug from a military hospital in China that had developed the formulation.[14] In 2010 it was the highest selling drug in China, with about 1 billion RMB in sales in the 3rd quarter, outselling Plavix in China.[13][3] This made Sihuan Pharm the largest company in China in the cardio-cerebral vascular drug market in 2010.[3] In 2014 it was the tenth highest-selling drug in China.[14]
References
- ↑ "Anjieli, Kelinao, cinepazide maleate - Product Profile - BioCentury". http://www.biocentury.com/products/anjieli.
- ↑ 2.0 2.1 Drugs.com Drugs.com International listings for cinepazide Page accessed Aug 3, 2015
- ↑ 3.0 3.1 3.2 20 Oct 2010 Sihuan Pharm – China's leading player in cardio-cerebral vascular drug – IPO Report
- ↑ Sihuan Pharmaceutical Kelinao/Anjieli official site Page accessed Aug 3, 2015
- ↑ "Drug receptors and control of the cardiovascular system: recent advances". Progress in Drug Research. Fortschritte der Arzneimittelforschung. Progrès des Recherches Pharmaceutiques 36: 117–360. 1991. doi:10.1007/978-3-0348-7136-5_4. ISBN 978-3-0348-7138-9. PMID 1876708. https://books.google.com/books?id=tWT0BwAAQBAJ&pg=PA304.
- ↑ 6.0 6.1 Johnson Sun for Guotai Junan International. Sept 28, 2011. Company Report: Sihuan Pharmaceuticals
- ↑ "The metabolic fate of the coronary vasodilator 4-(3,4,5-Trimethoxycinnamoyl)-1-(N-pyrrolidinocarbonylmethyl)piperazine (cinepazide) in the rat, dog and man". Xenobiotica; the Fate of Foreign Compounds in Biological Systems 6 (7): 441–55. July 1976. doi:10.3109/00498257609151657. PMID 997590.
- ↑ Reactions Weekly 305(1):1. June 1990 Cinepazide-related agranulocytosis
- ↑ "Agranulocytosis induced by cinepazide". European Journal of Clinical Pharmacology 38 (4): 387–8. 1990. doi:10.1007/bf00315580. PMID 2344862.
- ↑ Department of Economic and Social Affairs of the United Nations Secretariat Consolidated List of Products Whose Consumption and/or Sale Have Been Banned, Withdrawn, Severely Restricted or not Approved by Governments Twelfth Issue: Pharmaceuticals United Nations – New York, 2005
- ↑ Sidney M. Wolfe, M.D. for the Public Citizen's Health Research Group. February 2, 1995. Differences in the Number of Drug Safety Withdrawals: United States, United Kingdom, Germany and France 1970-1992
- ↑ "New drugs for Alzheimer's disease in Japan". Psychiatry and Clinical Neurosciences 65 (5): 399–404. August 2011. doi:10.1111/j.1440-1819.2011.02253.x. PMID 21851448.
- ↑ 13.0 13.1 Lefei Sun, Jinsong Du, and Iris Wang for Credit Suisse. October 6, 2011 China Pharma Sector
- ↑ 14.0 14.1 Su Zhang for Standard Chartered Bank (HK) Limited. June 27, 2014 China health care: Pharma sector comes of age
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