Pharmacology: In vitro and in vivo experiments have shown cinnarizine to reduce smooth muscle contractions induced by various vasoactive agents (histamine, angiotensin, bradykinin, nicotine, acetylcholine, adrenaline, noradrenaline, BaCl2) and by KCl depolarization. Specific anticonstrictor activities were observed when vascular smooth muscles were used. Cinnarizine acts on the contractile response of depolarized smooth muscle fibres by selectively inhibiting the calcium influx into depolarized cells and thereby reducing the availability of free Ca++ ions for the induction and maintenance of contraction. Cinnarizine is almost non-toxic and does not impede any of the important physiological functions (CNS, respiratory and circulatory function).
Pharmacokinetics: Isotope-labelled cinnarizine given to rats was found to be rapidly absorbed from the gastrointestinal tract and within 1-hr peak radioactivity levels were found in the blood, liver, kidneys, heart, spleen, lungs and brain. Extensive metabolization occurred within ½ hr of treatment and after 32 hrs, tissue drug levels were negligible. The drug was metabolized, especially by N-dealkylation. Approximately 2/3 of the radioactive metabolites were excreted in the faeces, and 1/3 in the urine. Excretion was virtually accomplished within 5 days following administration.
Cerebral Circulatory Disorders: Maintenance therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting.
Prophylaxis of motion sickness and migraine.
Maintenance therapy for symptoms of cerebrovascular origin, including dizziness, ear buzzing (tinnitus), vascular headache, unsociability and irritability disorders, loss of memory and lack of concentration.
Maintenance therapy for symptoms of peripheral circulatory disorders, including Raynaud's phenomenon, acrocyanosis, intermittent claudication, trophic disturbances, trophic and varicose ulcers, paraesthesia, nocturnal cramps and cold extremities.
Patients with known hypersensitivity to Stugeron.
Use in pregnancy: Although cinnarizine gives no evidence of embryotoxic or teratogenic properties in animals, potential hazards of prescribing drugs during pregnancy should always be weighed against expected therapeutic benefits.
In patients with Parkinson's disease, Stugeron should only be given if the advantages outweigh the possible risk of aggravating this disease.
Use in pregnancy: Although cinnarizine gives no evidence of embryotoxic or teratogenic properties in animals, potential hazards of prescribing drugs during pregnancy should always be weighed against expected therapeutic benefits.
Slight somnolence or gastrointestinal disorders may occur at high dosages. In most cases, these side effects disappear spontaneously after a few days. In sensitive patients, it is advisable to start the treatment with 1 tab 3 times a day and to increase the dosage progressively.
Aggravation and appearance of extrapyramidal symptoms may also occur.
Alcohol/CNS Depressant/Tricyclic Antidepressants: Concurrent use may potentiate the sedative effects of these medications or of Stugeron.
N07CA02 - cinnarizine ; Belongs to the class of antivertigo preparations.
Tab 25 mg x 25 x 10's, 100 x 10's.
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