Cinnarazine

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Cinnarizine is an antihistamine and calcium channel blocker of the diphenylmethylpiperazine group.[1]

Potential uses[edit | edit source]

Cinnarizine is typically used for vertigo/Ménière's disease, vestibular conditions, tinnitus, nystagmus, motion sickness, nausea and vomiting.[1] Cinnarizine relaxes the blood vessels; when used together with a nootropic, such as piracetam, it improves blood flow to the brain.[1]

Pharmacodynamics[edit | edit source]

Cinnarizine has also known to have antiserotoninergic and antidopaminergic effects.[1][2] Cinnarizine blocks muscarinic acetylcholine receptors, meaning it acts against vomiting.[1]

The half-maximal inhibitory concentration of cinnarizine for smooth muscle contraction inhibition is 60mM.[3][4]

Action of cinnarizine Target of action
Calcium ion channel antagonist T-type calcium channels
Antihistaminic H1 receptors
Antiserotinergic 5-HT2 receptors[5]
Antidopaminergic D2 receptors

Costs and availability[edit | edit source]

It is not available in the United States or Canada.[citation needed]

See also[edit | edit source]

Learn more[edit | edit source]

References[edit | edit source]

  1. 1.0 1.1 1.2 1.3 1.4 "Cinnarizine". DrugBank Online. Retrieved April 13, 2022.
  2. Kariya S, Isozaki S, Masubuchi Y, Suzuki T, Narimatsu S (November 1995). "Possible pharmacokinetic and pharmacodynamic factors affecting parkinsonism inducement by cinnarizine and flunarizine". Biochemical Pharmacology. 50 (10): 1645–50. doi:10.1016/0006-2952(95)02057-8. PMID 7503767.
  3. Silver PJ, Dachiw J, Ambrose JM, Pinto PB (September 1985). "Effects of the calcium antagonists perhexiline and cinnarizine on vascular and cardiac contractile protein function". The Journal of Pharmacology and Experimental Therapeutics. 234 (3): 629–35. PMID 3162016.
  4. López MG, Moro MA, Castillo CF, Artalejo CR, García AG (March 1989). "Variable, voltage-dependent, blocking effects of nitrendipine, verapamil, diltiazem, cinnarizine and cadmium on adrenomedullary secretion". British Journal of Pharmacology. 96 (3): 725–31. doi:10.1111/j.1476-5381.1989.tb11874.x. PMC 1854390. PMID 2720300.
  5. Pukhal'skaya TG, Kolosova OA, Men'shikov MY, Vein AM (July 2000). "Effects of calcium antagonists on serotonin-dependent aggregation and serotonin transport in platelets of patients with migraine". Bulletin of Experimental Biology and Medicine. 130 (7): 633–5. doi:10.1007/BF02682090. PMID 11140571.