Caroverine

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Caroverine
Clinical data
Routes of
administration		Oral
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 InfoCard100.164.389 Edit this at Wikidata
Chemical and physical data
FormulaC22H27N3O2
Molar mass365.47 g/mol 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 checkY
  • Key:MSPRUJDUTKRMLM-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Caroverine (Spasmium, Spadon, Tinnex) is a drug used in Tinnitus treatment improves mechanosensitivity and mechanotransduction phenomenon and otoneuroprotective (inner ear protective) agent in some countries.[1] It acts as an N-type calcium channel blocker, competitive AMPA receptor antagonist, and non-competitive NMDA receptor antagonist.[1] It also has potent antioxidant effects.[1][2]

Caroverine [1-(diethylaminoethyl) -3 – (p-methoxybenzyl) – 1, 2 – hydroquinoxaline-2-one] is a quinoxaline derivative developed in the 1960s. Caroverine, an N-methyl-D-aspartate and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist together with antioxidant activity, has been shown to protect the inner ear from excitotoxicity and to be effective in the treatment of tinnitus, sudden hearing loss and speech discrimination disorders in presbyacusis.

In recent years, it is on grounds of its quinoxline-dione structure, glutamate antagonism of him excitatory, afferent synapses of the cochlear inner hair cells and its neuroprotective properties that caroverine has been investigated as a new drug in the pharmacological treatment of tinnitus.

Caroverine also acts as a reversible glutamate antagonist in afferent cochlear synapse. Theoretical justification for the introduction of caroverine in the pharmacotherapy of tinnitus is that glutamate, as a key neurotransmitter in the central nervous system, is the most likely transmitter-substance in the afferent cochlear synapse (Ehrenberger-K eta al., 1992; Ehrenberger-K et al., 1995a; Ehrenberger-K et al., 1995b).

Application

Caroverine has been demonstrated to have a high rate of efficacy in the treatment of cochlear-synaptic tinnitus.[3]

Caroverine is available in Injection and Capsule form.

See also

References

  1. ^ a b c Udilova N, Kozlov AV, Bieberschulte W, Frei K, Ehrenberger K, Nohl H (2003). "The Antioxidant Activity of Caroverine". Biochemical Pharmacology. 65 (1): 59–65. doi:10.1016/S0006-2952(02)01452-1. PMID 12473379.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  2. ^ Nohl H, Bieberschulte W, Dietrich B, Udilova N, Kozlov AV (2003). "Caroverine, a Multifunctional Drug with Antioxidant Functions". BioFactors. 19 (1–2): 79–85. doi:10.1002/biof.5520190110. PMID 14757980.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  3. ^ Denk DM, Heinzl H, Franz P, Ehrenberger K. (Nov 1997). "Caroverine in tinnitus treatment. A placebo-controlled blind study". Acta Oto-Laryngologica. 117: 825–30. doi:10.3109/00016489709114208. PMID 9442821.{{cite journal}}: CS1 maint: multiple names: authors list (link)


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