Stugeron

White, circular, halfscored tablet with the inscription "JANSSEN" on one side and "S/25" on the other side. Each tablet contains 25 mg cinnarizine.
Excipients/Inactive Ingredients: 25 mg tablets: Cotton seed oil hydrogenated, lactose monohydrate, maize starch, polyvidone, sucrose, talc.

Pharmacotherapeutic group: antivertigo preparations. ATC code: N07CA02.
Pharmacology: Pharmacodynamics: Cinnarizine has an anti-histamine (H1)-effect. 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 anti-vasoconstrictor 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 vestibular system, which results in suppression of nystagmus and other autonomic disturbances. Acute episodes of vertigo can be prevented or reduced by cinnarizine.
Pharmacokinetics: Absorption: The peak plasma levels of cinnarizine are obtained 1 to 3 hours after intake.
Distribution: The plasma protein binding of cinnarizine is 91%.
Metabolism: Cinnarizine is extensively metabolized mainly via CYP2D6.
Elimination: The reported elimination half-life for cinnarizine ranges from 4 to 24 hours. The elimination of metabolites is about 1/3 in the urine and 2/3 in the feces.
Toxicology: Non-Clinical Information: A comprehensive battery of nonclinical safety studies showed that effects were observed only after chronic exposures that were 10 to 160 times (on a mg/kg basis) those at the maximum recommended human dose of 100 mg/day, calculated as 2 mg/kg as based on a 50 kg person.

Disorders of balance - maintenance therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting.
Prophylaxis of motion sickness.

Dosage: Disorders of balance - Adult: 1 tablet of 25 mg three times a day.
Prophylaxis of motion sickness: Adults and adolescents aged 13 years and above: 1 tablet of 25 mg at least half an hour before travelling; to be repeated every 6 hours.
Children aged 6 to 12 years: half of the adult dose is recommended.
Administration: STUGERON should preferably be taken after meals. It is for oral administration.

Symptoms and signs: Acute cinnarizine overdoses have been reported with doses ranging from 90 to 2,250 mg. The most commonly reported signs and symptoms associated with overdose of cinnarizine include: alterations in consciousness ranging from somnolence to stupor and coma, vomiting, extrapyramidal symptoms, and hypotonia. In a small number of young children, seizures developed. Clinical consequences were not severe in most cases, but deaths have been reported after single and polydrug overdoses involving cinnarizine.
Treatment: There is no specific antidote. For any overdose, the treatment is symptomatic and supportive care. It is advisable to contact a poison control center to obtain the latest recommendations for the management of an overdose.

STUGERON is contraindicated in patients with known hypersensitivity to the drug.

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, central nervous system (CNS) depressants or tricyclic antidepressants are used concomitantly.
Effects on Ability to Drive and Use Machines: Since somnolence may occur, especially at the start of treatment, caution should be taken during activities such as driving or operating machinery.

Pregnancy: 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.
Breast-feeding: There are no data on the excretion of STUGERON in human breast milk: nursing should therefore be discouraged in women using STUGERON.

Throughout this section, adverse reactions are presented. Adverse reactions are adverse events that were considered to be reasonably associated with the use of cinnarizine based on the comprehensive assessment of the available adverse event information. A causal relationship with cinnarizine cannot be reliably established in individual cases. Further, because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
Clinical trial data: Placebo-controlled double-blind data - adverse reactions reported at ≥1% incidence: The safety of STUGERON (30 to 225 mg/day) was evaluated in 601 subjects (of which 303 were treated with STUGERON, 298 were given placebo) who participated in 6 placebo-controlled, double-blind clinical trials: 2 in the treatment of peripheral circulatory disorders, 1 in the treatment of cerebral circulatory disorders, 1 in the treatment of vertigo, 1 in the prevention of motion sickness, and 1 in the treatment of both vertigo and cerebral circulatory disorders.
Adverse reactions reported by ≥1% of STUGERON-treated subjects noted in the double-blind clinical trials are shown in Table 1. (See Table 1.)

Click on icon to see table/diagram/image

Comparator and open-label data - adverse reactions reported at ≥1% incidence: Six comparator trials and 13 open label trials were selected to determine the incidence of adverse reactions. In these 19 studies, 937 subjects were treated with doses ranging from 25 to 450 mg/day STUGERON, in the treatment of peripheral circulatory disorders, cerebral circulatory disorders, and vertigo.
Adverse reactions reported by ≥1% of STUGERON-treated subjects noted in the comparator and open label clinical trials are shown in Table 2. (See Table 2.)

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Placebo, comparator, and open-label data - adverse reactions reported at <1% incidence: Additional adverse reactions that occurred in <1% of STUGERON-treated subjects in the above 2 clinical datasets (25 studies with a total of 1240 subjects treated with doses ranging from 25 to 450 mg/day) are listed as follows in Table 3. (See Table 3.)

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Postmarketing data: Adverse events first identified as adverse reactions during postmarketing experience with cinnarizine are included in Table 4. The postmarketing review was based on review of all cases where there was a use of cinnarizine. In Table 4, adverse reactions are presented by frequency category based on spontaneous reporting rates, with frequencies provided according to the following convention: Very common ≥1/10 (≥10%); Common ≥1/100 and <1/10 (≥1% and <10%); Uncommon ≥1/1000 and <1/100 ( (≥0.1% and <1%); Rare ≥1/10000 and <1/1000 (≥0.01 and <0.1%); Very rare <1/10000 including isolated reports (<0.01%); Not known Cannot be estimated from the available data. (See Table 4.)

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Alcohol/CNS Depressants and tricyclic antidepressants: The sedative effects of STUGERON and of any of the following may be potentiated when used concomitantly: alcohol, CNS depressants, or tricyclic antidepressants.
Diagnostic interference: 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.

Incompatibilities: None known.
Instructions for Disposal: Any unused product or waste material should be disposed of in accordance with local requirements.

Store below 30°C.
Protect from light.
Shelf Life: 3 years.

Peripheral Vasodilators & Cerebral Activators / Antivertigo Drugs

N07CA02 - cinnarizine ; Belongs to the class of antivertigo preparations.

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