Source: Υπουργείο Υγείας (CY) Revision Year: 2019 Publisher: Remedica Ltd, Aharnon Street, Limassol Industrial Estate, 3056 Limassol, Cyprus
Pharmacotherapeutic group: Other nervous system drugs, antivertigo preparations
ATC code: N07CA02
Cinnarizine’s actions in the treatment of peripheral vascular disease are due to its anti-vasoconstrictor properties, its action on blood hyperviscosity and its anti-ischaemic effect. Anti-vasoconstriction is thought to be through a calcium blocker mechanism and is evident selectively in vascular smooth muscle. Increased peripheral muscle blood flow may be mediated by prevention of calcium entry into ischaemic erythrocytes, thereby preserving flexibility.
The peak plasma levels of cinnarizine are obtained 1 to 3 hours after intake.
The plasma protein binding of cinnarizine is 91%.
Cinnarizine is extensively metabolised mainly via CYP2D6 in the liver.
The reported elimination half-life for cinnarizine ranges from 4 to 24 hours. The elimination of metabolites occurs as follows: about one third in the urine and two thirds in the faeces. Plasma elimination half life is 3 to 4 hours.
Nonclinical safety studies showed that effects were observed only after chronic exposures from approximately 5 to 72 times, on a mg/kg basis when compared to the maximum recommended human dose of 225 mg/day, calculated as 4.5 mg/kg as based on a 50 kg person.
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