Caroverine is a quinoxaline derivative with dual pharmacological properties: it acts as a spasmolytic agent on smooth muscle and as a glutamate receptor antagonist in the central nervous system. In the Indian market, it is primarily utilized for its smooth muscle relaxant effects in the treatment of gastrointestinal and biliary spasms. Its unique mechanism provides relief from spasmodic pain without significant CNS depression.
Adult: 20mg to 40mg, three to four times daily. The 20mg tablet is typically administered as 1-2 tablets per dose, not exceeding 160mg (8 tablets) in 24 hours.
Note: Oral administration. Tablet should be swallowed whole with a glass of water, preferably after meals to reduce gastric irritation. Do not crush or chew.
Caroverine exerts its primary therapeutic effect through a dual mechanism. 1) It acts as a non-selective calcium channel blocker, inhibiting the influx of extracellular calcium ions into smooth muscle cells, leading to muscle relaxation. 2) It functions as a non-competitive antagonist at glutamate receptors (NMDA and AMPA subtypes) in the central nervous system, though this action is more relevant to its investigational use in conditions like tinnitus and not its primary GI indication in India.
Pregnancy: Category C: Animal studies have shown adverse effects on the fetus. There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus. Avoid in the first trimester.
Driving: May cause dizziness, blurred vision, or drowsiness. Patients should be cautioned against driving or operating machinery until they know how the drug affects them.
| Other Anticholinergics (e.g., Atropine, Dicyclomine, Tricyclic Antidepressants) | Additive anticholinergic side effects (dry mouth, constipation, urinary retention, blurred vision). | Major |
| CNS Depressants (e.g., Alcohol, Benzodiazepines, Opioids) | Enhanced sedative effect and dizziness. Increased risk of accidents. | Moderate |
| Calcium Channel Blockers (e.g., Verapamil, Diltiazem, Nifedipine) | Additive cardiovascular effects (hypotension, bradycardia). | Moderate |
| CYP3A4 Inhibitors (e.g., Ketoconazole, Clarithromycin, Ritonavir) | Increased plasma concentration of Caroverine, leading to enhanced effects and toxicity. | Moderate |
| CYP3A4 Inducers (e.g., Rifampicin, Carbamazepine, Phenytoin) | Decreased plasma concentration of Caroverine, leading to reduced efficacy. | Moderate |
| Levodopa | Caroverine may reduce the absorption and efficacy of Levodopa. | Moderate |
Same composition (Caroverine (20mg)), different brands: