Cinnarizine
Brand name:- Stugeron, vertigon, vertin, Dizikind , DIZI, Convert.
Cinnarizine is an antihistamine that stops you feeling or being sick (nausea or vomiting). It works by blocking the effects of histamine in your brain to reduce the symptoms of travel sickness (motion sickness). It also helps to improve blood flow in the inner ear.
Pharmacodynamic:-
Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system.
Mechanism of action:-
Cinnarizine, developed as an anti-histamine, subsequently manifested a number of pharmacological effects, most significantly: labyrinthine suppressant action and peripheral anti-vasoconstrictive effects . Cinnarizine inhibits smooth muscle cell contraction in the vasculature by blocking L-and T-type voltage-gated calcium channel. It is also known to bind to histamine H1 receptors, muscarinic (acetyl choline) receptors and dopamine D2 receptors. Thus, the mechanism of action of cinnarizine is multimodal . Insufficient cerebral blood circulation has been hypothesized to cause ‘vertiginous symptoms’ like tinnitus, dizziness, nausea and vomiting in a range of conditions including transient ischemic attacks. Cinnarizine’s anti-vasoconstrictive and protective action against hyperviscosity of blood along with its peripheral anti-ischemic action may be helpful in improving blood flow thus playing an important role in various therapeutic indications .
Used:-
Used in the treatment of motion sickness, vertigo and Meniere's disease.
Side Effects:-
Sleepiness, Nausea, Weight gain.
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