Chemistry:Caroverine
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| Routes of administration | Oral |
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| Formula | C22H27N3O2 |
| Molar mass | 365.477 g·mol−1 |
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Caroverine (Spasmium, Tinnitin, Tinnex) is a muscle-relaxing drug used in Austria and Switzerland to relieve spasms in smooth muscles (which include intestines, arteries, and other organs), and the use in those countries was extended to aid with cerebrovascular diseases there, and eventually to treat tinnitus.[1] It is also used to treat tinnitus in India.
Chemically, it is a quinoxalineone[2] and is available in both a base and hydrochloric acid forms.[1]
Pharmacologically, it has been described as a nonspecific calcium channel blocker and as an antagonist of both non-NMDA and NMDA glutamate receptors.[3][4]
It was discovered in Austria in the 1950s[3] and was developed by Austrian company Phafag AG.[3]
Its INN name, caroverine, was proposed in 1972.[5]
An intravenous formulation was tested in a single-blinded study in tinnitus that published in 1997 and had positive results; an effort to replicate those results failed to show any effect,[4] and more people had their condition worsen than experienced benefit.[3] Pilot studies using a spray formulation for tinnitus published in 2005.[6]
In 2010 Phafag licensed rights to caroverine to the Indian company, Lincoln Pharmaceuticals, to develop the drug for tinnitus in India.[7] Lincoln first marketed it for that purpose in India in 2011.[8]
As of 2016 it had been studied in a small clinical trial in people with loss of the sense of smell.[9]
As of 2018 it was marketed under the brand names Spasmium and Tinnitin in Austria, and under the brand Tinnex in India.[10]
References
- ↑ 1.0 1.1 Martindale (36th ed.). Pharmaceutical Press. 2009. p. 2277. ISBN 9780853698401.
- ↑ "Spasmolytics". Ullmann's Encyclopedia of Industrial Chemistry. Wiley. 15 June 2000. p. 11. doi:10.1002/14356007.a24_515. ISBN 978-3527306732.
- ↑ 3.0 3.1 3.2 3.3 "A review of randomized clinical trials in tinnitus". The Laryngoscope 109 (8): 1202–1211. August 1999. doi:10.1097/00005537-199908000-00004. PMID 10443820.
- ↑ 4.0 4.1 "Emerging pharmacotherapy of tinnitus". Expert Opinion on Emerging Drugs 14 (4): 687–702. December 2009. doi:10.1517/14728210903206975. PMID 19712015.
- ↑ "Proposed INNs List 28". WHO Chronicle 26 (9). 1972. https://www.who.int/medicines/publications/druginformation/innlists/PL28.pdf.
- ↑ "Drug treatments for tinnitus". Tinnitus: Pathophysiology and Treatment. Progress in Brain Research. 166. 2007. pp. 249–262. doi:10.1016/S0079-6123(07)66023-3. ISBN 9780444531674.
- ↑ "Press release: Lincoln Pharma ties up with Swiss Phafag for Tinnitin injections". Lincoln via Business Standard India. 17 November 2010. https://www.business-standard.com/article/companies/lincoln-pharma-ties-up-with-swiss-phafag-for-tinnitin-injections-110111700044_1.html.
- ↑ "Press Release: Lincoln Pharma launches Tinnex Injection". Lincoln via Business Standard India. 14 April 2011. https://www.business-standard.com/article/press-releases/lincoln-pharma-launches-tinnex-injection-111041400145_1.html.
- ↑ "Pharmacologic treatment for postviral olfactory dysfunction: a systematic review". International Forum of Allergy & Rhinology 6 (7): 760–767. July 2016. doi:10.1002/alr.21727. PMID 26879592.
- ↑ "Caroverine International Brands". Drugs.com. https://www.drugs.com/international/caroverine.html.
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