Caroverine

Last updated
Caroverine
Caroverine.png
Clinical data
Trade names Spasmium, Tinnitin, Tinnex
Routes of
administration 		By mouth
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 1-[2-(diethylamino)ethyl]- 3-(4-methoxybenzyl)quinoxalin- 2(1H)-one
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.164.389 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C22H27N3O2
Molar mass 365.477 g·mol−1
3D model (JSmol)
  • O=C/1N(c3c(\N=C\1Cc2ccc(OC)cc2)cccc3)CCN(CC)CC
  • 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 Yes check.svgY
  • Key:MSPRUJDUTKRMLM-UHFFFAOYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Caroverine is an antispasmodic drug used in Austria and Switzerland to relieve spasms in smooth muscles, as well as to treat cerebrovascular diseases and tinnitus. [1]

Contents

Chemically, it is a quinoxalineone [2] and is available in both a base and hydrochloric acid forms. [1]

Pharmacology

Pharmacologically, it has been described as a nonspecific calcium channel blocker and as an antagonist of the NMDA receptor and other receptors. [3] [4]

History

It was discovered in Austria in the 1950s [3] and was developed by Austrian company Phafag AG. [3]

Its international nonproprietary name (INN), caroverine, was proposed in 1972. [5]

Society and culture

Brand names

As of 2018, it was marketed under the brand names Spasmium and Tinnitin in Austria, and under the brand Tinnex in India. [6]

Research

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. [7]

In 2010 Phafag licensed rights to caroverine to the Indian company, Lincoln Pharmaceuticals, to develop the drug for tinnitus in India. [8] Lincoln first marketed it for that purpose in India in 2011. [9]

As of 2016 it had been studied in a small clinical trial in people with loss of the sense of smell. [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): 1202–1211. 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. ↑ "Caroverine International Brands". Drugs.com. Retrieved 14 July 2018.
  7. ↑ Darlington CL, Smith PF (2007). "Drug treatments for tinnitus". Tinnitus: Pathophysiology and Treatment. Progress in Brain Research. Vol. 166. pp. 249–262. doi:10.1016/S0079-6123(07)66023-3. ISBN   9780444531674. PMID   17956789.
  8. ↑ "Press release: Lincoln Pharma ties up with Swiss Phafag for Tinnitin injections". Lincoln via Business Standard India. 17 November 2010.
  9. ↑ "Press Release: Lincoln Pharma launches Tinnex Injection". Lincoln via Business Standard India. 14 April 2011.
  10. ↑ Harless L, Liang J (July 2016). "Pharmacologic treatment for postviral olfactory dysfunction: a systematic review". International Forum of Allergy & Rhinology. 6 (7): 760–767. doi:10.1002/alr.21727. PMID   26879592. S2CID   29620152.
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