Drug intelligence / Profile preview

cinnarizine

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Oral
01

Overview

Cinnarizine is a small molecule antihistamine and selective calcium channel blocker of the diphenylmethylpiperazine group. It is primarily used to manage symptoms associated with vestibular (inner ear) disorders, including vertigo, tinnitus, nystagmus, nausea, and vomiting. Cinnarizine works by antagonizing histamine H1 receptor in the brain to reduce nausea and vomiting (antiemetic effect), as well as blocking T-type and L-type voltage-gated calcium channels to inhibit smooth muscle contraction in blood vessels and improve blood flow in the inner ear. It also exhibits antiserotonergic (Serotonin 5-HT2 receptor antagonist) and antidopaminergic (Dopamine D2 receptor antagonist) properties. The drug was first synthesized by Janssen Pharmaceuticals in 1955. Its main indications are for travel sickness (motion sickness), Ménière’s disease, vertigo, tinnitus, and other balance or movement disorders[1][2][4][8].

Brand names
Stugeron
02

Targets

5-HT2 (5-HT2 receptor family)LTCC (Voltage-gated calcium channel (L-type))HRH1 (Histamine H1 Receptor)CaV3 (Caveolin-3)DRD2 (Dopamine D2 Receptor)

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