Pharmacodynamics
Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities including contraction of airway and gastrointestinal smooth muscle, vasodilation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release, and chemotaxis of eosinophils and mast cells. Cinnarizine also blocks muscarinic acetylcholine receptors. Cinnarizine also inhibits calcium channels through its action resulting in a relaxing effect on vascular smooth muscle.
Pharmacokinetics
Cinnarizine is most commonly taken orally in tablet form. After ingestion, the substance is absorbed quite rapidly and reaches maximum plasma concentration within 1-3 hours after administration. Cinnarizine is CNS-responsive due to its high lipophilicity, which is why it can have a sedative effect on patients. Cinnarizine is metabolized in the liver, after which one-third is excreted in the urine and two-thirds in the stool. The elimination half-life varies between 3.4-60 hours depending on the age of the patient.