Cinarizine forte

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT CYNAZINE FORTE (CINNARIZINE FORTE)

Composition:

Active substance: cinnarizine;

One tablet contains 75 mg of cinnarizine calculated as 100% substance;

Excipients: lactose monohydrate; glycol montanic wax; ammonio-methacrylate copolymer (type A); ammonio-methacrylate copolymer dispersion; calcium stearate.

Pharmaceutical form. Tablets.

Main physicochemical properties: white to creamy, biconvex tablets with a score line.

Pharmacotherapeutic group.

Agents used in vestibular disorders. ATC code N07CA02.

Pharmacological properties.

Pharmacodynamics.

Cinnarizine inhibits smooth muscle cell contraction in blood vessels by blocking calcium channels. In addition to direct calcium antagonism, cinnarizine reduces the contractile effect of vasoactive substances such as norepinephrine and serotonin by blocking receptor-operated calcium channels. The blockade of calcium influx into cells is tissue-selective and results in reduced vasoconstriction without affecting arterial blood pressure and heart rate.

Cinnarizine may additionally improve impaired microcirculation by enhancing erythrocyte deformability and reducing blood viscosity. Its administration increases cellular resistance to hypoxia.

Cinnarizine suppresses stimulation of the vestibular system, thereby inhibiting nystagmus and other vegetative disturbances. Cinnarizine can prevent or alleviate acute episodes of vertigo.

Pharmacokinetics.

Maximum plasma concentrations of cinnarizine are reached within 1–3 hours after administration. The elimination half-life of cinnarizine from plasma ranges from 4 to 24 hours.

Cinnarizine is completely metabolized in the body and excreted as metabolites: approximately 1/3 in urine and 2/3 in feces.

Approximately 91% of the drug is bound to plasma proteins.

Clinical characteristics.

Indications.

Symptomatic treatment of:

• labyrinthine disorders including dizziness, tinnitus, nystagmus, nausea and vomiting;
• cerebrovascular disorders including dizziness, tinnitus, vascular headache, irritability, impaired memory and concentration;
• peripheral vascular disorders including Raynaud's disease, acrocyanosis, intermittent claudication, trophic disorders, trophic and varicose ulcers, paresthesia, nocturnal leg cramps, sensation of coldness in the extremities.

Contraindications.

Hypersensitivity to cinnarizine and/or to any of the other components of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

Alcohol/CNS depressants/tricyclic antidepressants: concomitant use may potentiate the sedative effect of any of these medicinal products or of Cinnarizine forte.

Diagnostic procedures: due to the antihistaminic effect, Cinnarizine forte may mask positive reactions to skin sensitivity factors during skin testing; therefore, its use should be discontinued 4 days prior to the procedure.

Special precautions for use.

Cinnarizine Forte may cause irritation in the epigastric region; taking the medication after meals can help reduce gastric mucosa irritation.

Cinnarizine Forte is recommended for patients with Parkinson's disease only if the benefits of treatment outweigh the potential risk of worsening the course of this disease.

Since Cinnarizine Forte may cause drowsiness, especially at the beginning of treatment, concomitant use of alcohol and administration of central nervous system depressants (CNS depressants) should be avoided.

Cinnarizine Forte should not be used in patients with porphyria.

Cinnarizine Forte should be used with caution in patients with hepatic and/or renal insufficiency.

The product contains lactose; therefore, patients with rare hereditary forms of galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption syndrome should not take this medicinal product.

Use during pregnancy or breastfeeding.

Although teratogenic effects of cinnarizine were not observed in animal studies, the drug is not recommended for use during pregnancy.

There is no information available regarding the passage of cinnarizine into breast milk. Therefore, treatment with Cinnarizine Forte should be avoided in women during breastfeeding.

Ability to affect reaction speed when driving or operating machinery.

Given that drowsiness may occur in sensitive patients during treatment with the drug (especially at the beginning of treatment), patients should refrain from driving vehicles and performing other tasks requiring concentration of attention during therapy.

Method of administration and dosage.

For adults, Cinnarizine Forte should be taken orally, preferably after meals.

For symptoms of cerebral circulation disorders: 1 tablet (75 mg) once daily;
for symptoms of peripheral vascular disorders: 2–3 tablets (150–225 mg) per day;
for symptoms of labyrinthine disorders: 1 tablet (75 mg) once daily.

The maximum daily dose should not exceed 225 mg (3 tablets). Since the effect in vertigo is dose-dependent, dosage should be gradually increased.

Children.

This medicinal formulation is not intended for use in children.

Overdose.

Symptoms. In isolated cases of acute overdose (from 90 mg to 2250 mg), the following manifestations were observed: altered consciousness ranging from drowsiness to stupor and coma; vomiting, extrapyramidal symptoms, arterial hypotension. Seizures were observed in a small number of children. In most cases, the clinical outcome was not severe, but fatal cases have been reported following overdose when used concomitantly with other medicinal products, including cinnarizine.

Treatment. There is no specific antidote. Gastric lavage should be performed within the first hour after ingestion. Activated charcoal may be administered if indicated.

Adverse reactions.

Somnolence and gastrointestinal disorders may occur. These symptoms are usually temporary and disappear with gradual attainment of the optimal dose. Rarely, symptoms such as headache, dry mouth, weight gain, sweating, or allergic reactions may develop. Very rarely, Wilson’s disease and lupus-like symptoms have been reported.

A single case of obstructive jaundice has been described in the medical literature. In elderly patients, prolonged treatment with cinnarizine has been associated with the onset or worsening of extrapyramidal symptoms, sometimes accompanied by depressive states. In such cases, the use of this drug should be discontinued.

The adverse reactions listed below were observed during clinical studies and in the post-marketing period with the use of cinnarizine. The frequency is defined as follows: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10,000 to <1/1000); very rare (<1/10,000); frequency not known (cannot be estimated from available data).

Additional cases of hypersensitivity reactions, headache, and dry mouth sensation have been reported.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 ºC.

Keep out of reach of children.

Packaging.

10 tablets in a blister, 2 blisters per pack.

Prescription status. Prescription only.

Manufacturer.

JSC "Kyivmedpreparat".

Manufacturer's address and place of business.

139 Saksaganskogo Street, Kyiv, 01032, Ukraine.