Delving into the Latest Updates on Caroverine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Caroverine (INN), Spasmium, Tinnex

Target

AMPA receptor x NMDA receptor

Action

antagonists

Mechanism

AMPA receptor antagonists(Glutamate receptor ionotropic AMPA antagonists), NMDA receptor antagonists(Glutamate [NMDA] receptor antagonists)

Therapeutic Areas

Nervous System Diseases

Active Indication

PainSpasm

Inactive Indication

Labyrinth DiseasesTinnitus

Originator Organization-

Active Organization-

Inactive Organization

Phafag AG

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC22H27N3O2

InChIKeyMSPRUJDUTKRMLM-UHFFFAOYSA-N

CAS Registry23465-76-1

The sound sensation that is experienced in the ears or brain and is unrelated to any external sources of stimulus is known as tinnitus. Tinnitus Functional Index (TFI) is used to establish the presence of the condition and determine symptom severity, its impact on the patient's quality of life, thus in this study, we aim to compare the efficacy of caroverine and Ginkgo Biloba in the management of idiopathic tinnitus using TFI.

Methods:

This clinical study was conducted in at a tertiary care hospital in North India, for a duration of one year, among patients with chronic tinnitus. The sample size for this study consisted of 60 patients in each of three groups (caroverine, gingko biloba, and multivitamin). Assessments of TFI and pure-tone audiometry were performed to evaluate the efficacy of the two medications. The information pertaining to the subjects was kept anonymous and confidential. During data analysis, an association was significant for p value < 0.05.

Results:

The patients in three groups were matched for the age, gender and duration of tinnitus. At 6 months of medication with Ginkgo Biloba, patients experienced a significant (p < 0.0001) decrease of 50.0% in tinnitus of moderate severity, and a complete resolution of severe tinnitus symptoms with a percentage change of -100.0%.

Conclusion:

In our study, Ginkgo Biloba Group has significantly improved the severity of idiopathic tinnitus. Tinnitus has diverse underlying mechanisms, can be a symptom of various underlying diseases, and is challenging to measure. Further research is warranted to validate and explore these treatment options further.

01 Oct 2024·Journal of Family Medicine and Primary Care

Effect of oral caroverine in the treatment of tinnitus: A quasi-experimental study

Article

Author: Panda, Abinash ; Satpathy, Manas R. ; Barik, Prasanjit A. ; Dash, Anil K. ; Prusty, Nilamadhaba ; Bisoyi, Sasmita K.

Objective::

Caroverine is an antagonist of non-NMDA and NMDA glutamate receptors. Cochlear synaptic tinnitus arises from a synaptic disturbance of NMDA or non-NMDA receptors on the afferent dendrites of spiral ganglion neurons. This forms a basis for the use of caroverine in the treatment of tinnitus. Hence, the present study was carried out to find the effect of oral caroverine in the treatment of tinnitus.

Methodology::

This quasi-experimental study was carried out on sixty consecutive patients of tinnitus. Thirty patients were given the usual standard of care consisting of Tab. Cinnarizine 25mg twice daily along with fixed dose combination Cap. B-complex and Ginkgo biloba once daily for ninety days and thirty patients were given Cap. Caroverine 40mg, twice daily for ninety days. Outcome assessment was done using the tinnitus case history questionnaire, tinnitus handicap inventory score, and VAS. The data were analyzed using GraphPad Prism Trial Version. A P value ≤ 0.05 was taken as statistically significant.

Results::

There was a significant improvement in the tinnitus case history questionnaire score at 90 days in patients suffering from mild tinnitus when treated with caroverine. There was a larger decrease in the tinnitus handicap inventory score at 90 days of treatment in the caroverine-treated patients. The median VAS showed an improvement in the caroverine-treated group. The overall reduction in tinnitus in the caroverine-treated group was 53.3% with an odds ratio, 95% CI of 0.375 (0.12-1.08).

Conclusion::

Oral caroverine was found to be better than the usual standard of care in reducing mild cochlear synaptic tinnitus. It also improved sensory–neural hearing loss during the treatment period.

16 Dec 2022·ACS Catalysis

Cobalt(II)-Catalyzed C–H Alkylation of N-Heterocycles with 1,4-Dihydropyridines

Author: Park, Jung Su ; Kim, In Su ; Mishra, Neeraj Kumar ; Ghosh, Prithwish ; Byun, Youjung ; Kwon, Na Yeon

Reported the cobalt(II)-catalyzed C-H alkylation and acylation of N-heterocycles with 1,4-dihydropyridines (DHPs) as alkylating and acylating agents.Notably, a combination of KBrO₃ and a Co(II) catalyst were successfully employed for the generation of alkyl and acyl radicals from DHPs.A series of heterocycles, including azauracils, quinoxalinones, pyrazinones, pyridones, quinolones, quinazolinones, xanthines, chromones and azine N-oxides, were compatible under the developed conditions.The applicability of the developed protocol in challenging contexts is highlighted by the selective modification of drug candidates as well as the gram-scale synthesis of bioactive mols.Combined mechanistic investigations aided the elucidation of a plausible reaction mechanism.

100 Deals associated with Caroverine

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