Janssen Products

Cinnarizine

Stugeron tablet/capsule

DESCRIPTION:
Cinnarizine (Stugeron*) is a selective calcium entry blocker, belonging to group IV of the calcium antagonists (WHO-classification).

Cinnarizine (Stugeron*) has an anti-histamine (H1)-effect.

Cinnarizine (Stugeron*) is available as oral tablets and red and yellow capsules containing 25 mg and 75 mg of cinnarizine respectively.

The inactive ingredients of the 25 mg tablets are: lactose, maize starch, sucrose, talc, hydrogenated vegetable oil, polyvidone (formulation F50). The inactive ingredients of the 75 mg capsules are: lactose, maize starch, magnesium stearate, talc, gelatin, erythrosine, titanium dioxide, orange yellow S, yellow ferric oxide (formulation F6).

PROPERTIES:
Pharmacodynamics
Cinnarizine (Stugeron*) inhibits contractions of vascular smooth muscle cells by blocking calcium channels. In addition to this direct calcium antagonism cinnarizine (Stugeron*) 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 (Stugeron*) may further improve deficient microcirculation by increasing erythrocyte deformability and decreasing blood viscosity. Cellular resistance to hypoxia is increased. Cinnarizine (Stugeron*) inhibits stimulation of the vestibular system, which results in suppression of nystagmus and other autonomic disturbances. Acute episodes of vertigo can be prevented or reduced by cinnarizine.

Pharmacokinetics
The peak plasma levels of cinnarizine are obtained 1 to 3 hours after intake. Cinnarizine (Stugeron*) disappears from plasma with a half-life of 4 hours. Cinnarizine (Stugeron*) 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%.

INDICATIONS:
Cerebral circulatory disorders

CONTRAINDICATIONS:
Cinnarizine (Stugeron*) is contraindicated in patients with known hypersensitivity to the drug.

WARNINGS AND PRECAUTIONS:
As with other antihistamines, Cinnarizine (Stugeron*) may cause epigastric distress; taking it after meals may diminish gastric irritation. In patients with Parkinson's disease Cinnarizine (Stugeron*) should only be given if the advantages outweigh the possible risk of aggravating this disease. Cinnarizine (Stugeron*) may cause somnolence, especially at the start of treatment. Therefore caution should be taken when alcohol or CNS depressants are used concomitantly.

INTERACTIONS:
Alcohol/CNS depressants/Tricyclic Antidepressants: Concurrent use may potentiate the sedative effects of either of these medications or of Cinnarizine (Stugeron*).

Diagnostic Interference: Because of its antihistamine effect, Cinnarizine (Stugeron*) may prevent otherwise positive reactions to dermal reactivity indicators if used up to 4 days prior to skin testing.

PREGNANCY AND LACTATION:
Although in animal studies, Cinnarizine (Stugeron*) has shown no teratogenic effects, as with all drugs, Cinnarizine (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 Cinnarizine (Stugeron*) in human breast milk: nursing should therefore be discouraged in women using Cinnarizine (Stugeron*).

EFFECTS ON DRIVING ABILITY AND OPERATION OF MACHINES:
Since somnolence may occur, especially at the start of treatment, caution should be taken during activities such as driving or operating machinery.

DOSAGE AND ADMINISTRATION:

Cinnarizine (Stugeron*) should preferably be taken after meals. The maximum recommended dosage should not exceed 225 mg (9 tablets or 3 capsules) daily. As the effect of Cinnarizine (Stugeron*) on vertigo is dose dependent, the dosage should be increased progressively.

ADVERSE REACTIONS:
Somnolence and gastrointestinal disturbance 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.

OVERDOSAGE:
In a single case of acute overdosage (2100 mg) in a 4-year old child, the following manifestations were observed: vomiting, drowsiness, coma, tremor, hypotonia. Recovery was uneventful.

There is no specific antidote, but in the event of overdosage, gastric lavage as well as the administration of activated charcoal may help.

HOW SUPPLIED:
Cinnarizine (Stugeron*):tablets:packs containing 100 tablets and 200 tablets of 25 mg of cinnarizine oer tablet;

Cinnarizine (Stugeron*) Forte: capsules:oacks containing 100 capsules of 75 mg of cinnarizine per capsule.

CAUTION:
Food, Drugs, Devices and Cosmetics Act prohibits dispensing without prescription.

STORAGE CONDITIONS:
Tablets: store in a dry place.
Tablets and capsules: protect from light
Store between 15°C and 25°C.
KEEP OUT OF REACH OF CHILDREN.

Manufactured by:
INTERPHIL LABORATORIES, INC.
Canlubang Industrial Estate
Bo. Pittland, Cabuyao, Laguna
For: Johnson & Johnson
Edison Road, Bo. Ibayo
Parañaque, Metro Manila
Under license from:
JANSSEN PHARMACEUTICA
Beerse, Belgium
Exclusively distributed by:
ZUELLIG PHARMA CORPORATION
Sen. Gil Puyat Avenue
Makati City