Class: Central Nervous System
Dosage Form: Tablets
Description: Selective calcium entry blocker
Lactose, maize starch, sucrose, talc, hydrogenated vegetable oil, polyvidone
Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking calcium channels.In addition to this direct calcium antagonism cinnarizine decreases the contractile activity of vasoactive substances, such as norepinephrine and serotonin, by blocking receptor-operated calcium channels. Blockade of the cellular influx of calcium is tissue-selective, and results in antivasoconstrictor properties without effect on blood pressure and heart rate. Cinnarizine may further improve deficient microcirculation by increasing erythrocyte deformability and decreasing blood viscosity Cellular resistance to hypoxia is increased. Cinnarizine inhibits stimulation of the veslibular system, which results in suppression of nystagmus and other autonomic disturbances. Acute episodes of vertigo can be prevented or reduced by cinnarizine.
The peak plasma levels of cinnarizine are obtained 1 to 3 hours after intake. Cinnarizine disappears from plasma with an half-life of 4 hours. Cinnarizine is thoroughly metabolized. The elimination of these metabolites occurs for about 1/3 in the urine and for 2/3 with the feces. The plasma protein binding of cinnarizine is 91%.
Stugeron is indicated in:
- Maintenance therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting
- Prophylaxis of motion sickness
- Prophylaxis of 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, paresthesia, nocturnal cramps, cold extremities
Stugeron is contraindicated in patients with known hypersensitivity to the drug.
Concurrent use of of alcohol, CNS depressants, and tricyclic antidepressants may potentiate the sedative effects of either of these medications or of Sutgeron.
Somnolence and gastrointestinal disturbances may occur. They are usually transient and may often be prevented by achieving the optimum dosage gradually.
In rare cases, headache, dry mouth, weight gain, perspiration or allergic reactions may be observed.
Similarly, very rare cases of lichen planus and lupus-like symptoms have been reported.
In the medical literature an isolated case of cholestatic jaundice has been reported.
In elderly people, cases of aggravation or appearance of extrapyramidal symptoms, sometimes associated with depressive feelings, have been described during prolonged therapy The treatment should be discontinued in such cases.
Dosage and Administration:
The following is generally recommended:
- Cerebral circulatory disorders: 1 tablet of 25 mg t.i.d.
- Peripheral circulatory disorders: 2-3 tablets of 25 mg t.i.d.
- Disorders of balance: 1 tablet of 25 mg t.i.d.
- Motion sickness:
- In adults: 1 tablet of 25 mg half an hour before traveling; to be repeated every 6 hours
- In children: half of the adult dose is recommended
Stugeron should preferably be taken after meals. The maximum recommended dosage should not exceed 225 mg (9 tablets) daily.
As the effect of Stugeron on vertigo is dose dependent, the dosage should be increased progressively.
In a single case of acute overdose (2100 mg) in a 4-year old child, the following manifestations were observed: vomiting, drowsiness, coma, tremor, hypotonia.
There is no specific antidote. Within the first hour after ingestion, gastric lavage may be performed. Activated charcoal may be given if considered appropriate.
Pregnancy and Lactation:
Although in animal studies, Stugeron has shown no teratogenic effects, as with all drugs, Stugeron should be used during pregnancy only if the therapeutic benefits justify the potential risks for the fetus.
There are no data on the excretion of Stugeron in human breast milk; nursing should therefore be discouraged in women using Stugeron.
As with other antihistamines Stugeron may cause epigastric distress; taking it after meals may diminish gastric irritation.
In patients with Parkinson’s disease Stugeron should only be given if the advantages outweigh the possible risk of aggravating this disease.
Stugeron may cause somnolence, especially at the start of treatment. Therefore caution should be taken when alcohol or CNS depressants are used concomitantly.
Because of its antihistamine effect, Stugeron may prevent otherwise positive reactions to dermal reactivity indicators if used up to 4 days prior to skin testing.
Pack of 3 strips of 10 tablets each.
Store at room temperature, below 25°C.