Caroverine

Caroverine
Clinical data
Routes of
administration		Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
IUPAC name
  • 1-[2-(diethylamino)ethyl]- 3-(4-methoxybenzyl)quinoxalin- 2(1H)-one
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.164.389
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Chemical and physical data
FormulaC22H27N3O2
Molar mass365.477 g·mol−1
3D model (JSmol)
SMILES
  • O=C/1N(c3c(\N=C\1Cc2ccc(OC)cc2)cccc3)CCN(CC)CC
InChI
  • InChI=1S/C22H27N3O2/c1-4-24(5-2)14-15-25-21-9-7-6-8-19(21)23-20(22(25)26)16-17-10-12-18(27-3)13-11-17/h6-13H,4-5,14-16H2,1-3H3 checkY
  • Key:MSPRUJDUTKRMLM-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

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 quinoxalinedione[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. 1 2 Sweetman SC, ed. (2009). Martindale (36th ed.). Pharmaceutical Press. p. 2277. ISBN 9780853698401.
  2. ↑ Bungardt E, Mutschler E (15 June 2000). "Spasmolytics". Ullmann's Encyclopedia of Industrial Chemistry. Wiley. p. 11. doi:10.1002/14356007.a24_515. ISBN 978-3527306732.
  3. 1 2 3 4 Dobie RA (August 1999). "A review of randomized clinical trials in tinnitus". The Laryngoscope. 109 (8): 1202–11. doi:10.1097/00005537-199908000-00004. PMID 10443820. S2CID 21409406.
  4. 1 2 Langguth B, Salvi R, Elgoyhen AB (December 2009). "Emerging pharmacotherapy of tinnitus". Expert Opinion on Emerging Drugs. 14 (4): 687–702. doi:10.1517/14728210903206975. PMC 2832848. PMID 19712015.
  5. ↑ "Proposed INNs List 28" (PDF). WHO Chronicle. 26 (9). 1972.
  6. ↑ Darlington, CL; Smith, PF (2007). Drug treatments for tinnitus. Progress in Brain Research. Vol. 166. pp. 249–62. doi:10.1016/S0079-6123(07)66023-3. ISBN 9780444531674. PMID 17956789.
  7. ↑ "Press release: Lincoln Pharma ties up with Swiss Phafag for Tinnitin injections". Lincoln via Business Standard India. 17 November 2010.
  8. ↑ "Press Release: Lincoln Pharma launches Tinnex Injection". Lincoln via Business Standard India. 14 April 2011.
  9. ↑ Harless L, Liang J (July 2016). "Pharmacologic treatment for postviral olfactory dysfunction: a systematic review". International Forum of Allergy & Rhinology. 6 (7): 760–7. doi:10.1002/alr.21727. PMID 26879592. S2CID 29620152.
  10. ↑ "Caroverine International Brands". Drugs.com. Retrieved 14 July 2018.
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