Generic Stugeron ( Cinnarizine )

Buy Generic Stugeron (Cinnarizine) without prescription in Canada

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Stugeron (cinnarizine) is a piperazine derivative with antihistamine (H1‑receptor antagonist) and calcium‑channel‑blocking properties. It acts by reducing the excitability of the vestibular apparatus in the inner ear and inhibiting the flow of calcium into vascular smooth‑muscle cells. This dual action makes it effective for preventing and treating motion sickness and for managing peripheral vascular disorders and vestibular conditions such as vertigo, tinnitus, and Ménière’s disease. Its ability to selectively depress labyrinthine stimulation helps to restore balance and reduce nausea without heavily suppressing the central nervous system at therapeutic doses.

Usual adult dose: For motion sickness, 25 mg is taken 2 hours before travel, followed by 25 mg every 8 hours if needed during the journey. For vestibular disorders (e.g., vertigo, Ménière’s disease), the usual dose is 25 mg taken two or three times daily. The total daily dose should not exceed 75 mg for most indications. The lowest effective dose should be used, and therapy should be reassessed periodically in patients requiring prolonged treatment.

Dosage form: Oral tablets, 25 mg.

Onset of action: For motion sickness, the protective effect begins within 30 minutes to 2 hours after an oral dose. When used for vestibular disorders, symptomatic relief of vertigo may be noticeable within a few days of regular administration.

Duration of action: The anti‑motion sickness effect lasts approximately 8 hours after a single dose. The elimination half‑life is approximately 3 to 4 hours, but the drug’s antihistaminergic effects may persist longer due to tissue distribution.

Alcohol recommendation: Alcohol consumption should be avoided during treatment with Stugeron. Alcohol can potentiate the central nervous system depressant effects of cinnarizine, leading to increased drowsiness, dizziness, and impaired coordination.

Most common side effects: Drowsiness, fatigue, dry mouth, gastrointestinal discomfort (nausea, epigastric pain), and weight gain. Drowsiness is generally dose‑dependent and often diminishes with continued use or dose reduction. Prolonged use at high doses, particularly in the elderly, may rarely cause extrapyramidal symptoms such as tremor, rigidity, or involuntary movements.

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General Information about Stugeron (Cinnarizine)

• INN (International Nonproprietary Name): Cinnarizine
• Brand names available in Canada: Stugeron® is not an actively marketed brand in Canada. Cinnarizine is not available through regular Canadian pharmacy channels but can be accessed internationally as Stugeron® (Janssen Pharmaceutica) and generic cinnarizine tablets. The product is supplied to our pharmacy via the international supply chain for personal importation.
• ATC code: N07CA02 (antivertigo preparations)
• Dosage forms and strengths: Oral tablets: 25 mg. In some markets, 75 mg capsules are also available.
• Manufacturers in Canada: None. Cinnarizine is not manufactured or commercially distributed in Canada. Internationally, it is manufactured by Janssen (Stugeron) and various generic pharmaceutical companies.
• Registration status in Canada: Not marketed in Canada. Cinnarizine has not been issued a Notice of Compliance by Health Canada and is not listed in the Drug Product Database. It is, however, approved and widely available in many other countries, including the United Kingdom and several European nations.
• OTC / Rx classification: Prescription only (Rx). A valid prescription from a licensed Canadian healthcare professional is required for personal importation.

Mechanism of Action and Pharmacology

Cinnarizine is a piperazine derivative that exerts its therapeutic effects through a combination of antihistaminergic and calcium‑channel‑blocking activities. It acts as a potent and selective antagonist at histamine H1 receptors, which contributes to its anti‑emetic and sedative properties. In addition, cinnarizine inhibits the influx of extracellular calcium through L‑type voltage‑gated calcium channels in vascular smooth‑muscle cells and vestibular hair cells. By reducing calcium entry, it causes relaxation of vascular smooth muscle, leading to vasodilation and improved peripheral blood flow. In the vestibular system, cinnarizine suppresses the hyperexcitability of hair cells induced by angular and linear acceleration, thus preventing motion sickness and relieving vertigo. The drug is absorbed relatively slowly after oral administration, with peak plasma concentrations reached 2 to 4 hours after a dose. Cinnarizine is extensively metabolised in the liver, primarily via N‑desalkylation. Its elimination half‑life is approximately 3 to 4 hours. The drug is excreted mainly in the faeces and, to a lesser extent, in the urine.

Indications

• Motion sickness: Prevention and treatment of nausea, dizziness, and vomiting associated with travel by car, boat, train, or aircraft.
• Vestibular disorders: Symptomatic treatment of vertigo, tinnitus, and nystagmus associated with Ménière’s disease and other labyrinthine disorders.
• Peripheral vascular disorders: Symptomatic management of peripheral vascular disease, including Raynaud’s syndrome, intermittent claudication, and circulatory disturbances such as cold extremities and night cramps.

Important Warnings and Precautions

At‑risk groups

• Pregnancy: Cinnarizine should be avoided during pregnancy, particularly in the first trimester, unless the potential benefit clearly outweighs the possible risk to the foetus. Limited data are available on the safety of cinnarizine in human pregnancy, and animal studies have shown evidence of teratogenicity at high doses. Women of childbearing potential should use effective contraception.
• Breastfeeding: It is not known whether cinnarizine is excreted in human breast milk. Because of the potential for adverse effects in the nursing infant, breastfeeding is not recommended during treatment.
• Paediatrics (< 5 years): Safety and efficacy in children under 5 years of age have not been established. Cinnarizine should not be administered to children in this age group.
• Elderly: Elderly patients are more susceptible to the sedative, anticholinergic, and extrapyramidal side effects of cinnarizine. Cinnarizine is included in the Beers Criteria as a potentially inappropriate medication for older adults due to its anticholinergic properties and the risk of exacerbating Parkinson’s disease. If used, the lowest effective dose should be employed for the shortest possible duration. Prolonged use in the elderly is associated with an increased risk of drug‑induced parkinsonism and tardive dyskinesia.
• Parkinson’s disease: Cinnarizine can block postsynaptic D2 dopamine receptors and may induce or worsen parkinsonian symptoms. It is contraindicated in patients with established Parkinson’s disease and should be used with extreme caution in patients with a family history or early signs of the disorder.
• Hepatic impairment: Cinnarizine is extensively metabolised by the liver. Use with caution, and consider dose reduction in patients with significant hepatic insufficiency.
• Renal impairment: Use with caution in patients with moderate to severe renal impairment, as drug clearance may be reduced.
• Hypotension: Due to its calcium‑channel‑blocking effects, cinnarizine may cause a modest reduction in blood pressure. Use with caution in patients with pre‑existing hypotension or those taking antihypertensive medications.
• Allergy: Do not take Stugeron if you have a known hypersensitivity to cinnarizine, other piperazine derivatives, or any excipient in the formulation.

Driving and alcohol

Stugeron can cause significant drowsiness, dizziness, and fatigue, particularly at the start of therapy and at higher doses. Patients should not drive, operate heavy machinery, or engage in activities requiring mental alertness until they have determined how the medication affects them. The risk of sedation is heightened when cinnarizine is combined with alcohol. Alcohol should be avoided entirely during treatment to prevent dangerous additive drowsiness and psychomotor impairment.

Dosage Instructions

• Motion sickness: Adults and children over 12 years: 25 mg taken 2 hours before the start of travel. If necessary, a further 25 mg may be taken 8 hours later. For children aged 5 to 12 years, half of the adult dose (12.5 mg) is recommended.
• Vestibular disorders: Adults: 25 mg two or three times daily. The dose may be adjusted according to clinical response, but the total daily dose should not exceed 75 mg.
• Peripheral vascular disorders: Adults: 25 mg two or three times daily, depending on the severity of symptoms.
• Elderly patients: A starting dose of 25 mg once or twice daily is recommended, with cautious upward titration only if tolerated.
• Administration: The tablets should be swallowed whole with a glass of water, preferably after a meal to minimise gastric irritation. For motion sickness, the first dose must be taken at least 2 hours before departure to ensure full protective effect.
• Missed dose: If a dose is missed, take it as soon as remembered unless it is close to the time of the next dose. Do not double the dose to make up for a missed one.

Side Effects and Contraindications

• Very common side effects (≥ 10%): Drowsiness and fatigue. These are generally dose‑dependent and often resolve with continued treatment or dose reduction.
• Common side effects (1‑10%): Dry mouth, gastrointestinal disturbances (nausea, epigastric pain, dyspepsia), headache, and weight gain.
• Rare but serious side effects: Extrapyramidal symptoms, including parkinsonism (tremor, rigidity, akinesia), orofacial dyskinesia, and tardive dyskinesia, particularly in the elderly and with prolonged use at higher doses. Allergic skin reactions, including rash and urticaria, have also been reported. Rare cases of cholestatic jaundice have been documented.
• Contraindications: Known hypersensitivity to cinnarizine, other piperazine derivatives, or any excipient in the formulation. Established Parkinson’s disease. Children under 5 years of age. Pregnancy (first trimester) and breastfeeding.

Drug Interactions

• CNS depressants: Alcohol, benzodiazepines, barbiturates, opioids, sedating antihistamines, and other central nervous system depressants may potentiate the sedative effects of cinnarizine, leading to excessive drowsiness and psychomotor impairment.
• Anticholinergic drugs: Concomitant use with tricyclic antidepressants, antipsychotics, and other drugs with anticholinergic properties may increase the risk of dry mouth, constipation, blurred vision, and urinary retention.
• Dopamine receptor antagonists: Because cinnarizine may block dopamine D2 receptors, co‑administration with antipsychotic drugs or metoclopramide can theoretically increase the risk of extrapyramidal side effects.
• Antihypertensives: Cinnarizine may exert additive hypotensive effects when used with antihypertensive medications. Blood pressure should be monitored in patients on concurrent therapy.
• Diagnostic skin testing: Antihistamines such as cinnarizine can mask the cutaneous histamine response and produce false‑negative results in allergy skin tests. Cinnarizine should be discontinued at least 72 hours before such testing.

Practical Advice

• Administration: To prevent motion sickness, take the first dose 2 hours before departure, followed by a dose every 8 hours during the journey if necessary. When taken for vertigo or circulatory disorders, doses should be taken after meals to reduce stomach upset. Swallow the tablet whole with water; do not crush or chew.
• Monitoring: No specific routine laboratory monitoring is required. However, patients on long‑term therapy, particularly the elderly, should be monitored for signs of extrapyramidal effects, such as tremor, stiffness, or abnormal facial movements. If these symptoms appear, the drug should be discontinued promptly.
• Storage: Store at room temperature (15‑30 °C) in a dry place, protected from moisture and light. Keep out of the reach and sight of children.
• Lifestyle: Cinnarizine may cause drowsiness, so avoid activities that require full mental alertness until individual sensitivity is known. Alcohol should be avoided throughout treatment. If you are prone to motion sickness, additional preventative measures—such as focusing on a stable horizon, avoiding large meals before travel, and ensuring good ventilation—can improve the overall anti‑sickness effect.
• When to seek medical review: Contact your doctor if symptoms of vertigo, tinnitus, or peripheral vascular disease do not improve after several weeks of treatment. Seek emergency medical attention if you experience signs of an allergic reaction (such as difficulty breathing, hives, or swelling of the face, lips, or throat) or if you develop severe stiffness, tremor, or uncontrollable movements.
• Disposal: Return unused or expired medication to a pharmacy for safe disposal. Do not flush down the toilet or discard in household waste.

Alternative Medications

• Dimenhydrinate (Gravol®): An over‑the‑counter antihistamine widely available in Canada for motion sickness. It is generally more sedating than cinnarizine and has a shorter duration of action.
• Meclizine (Antivert®, Bonamine®): A piperazine antihistamine chemically related to cinnarizine, available by prescription in Canada. It is effective for vertigo and motion sickness, usually with a longer duration of action than dimenhydrinate.
• Betahistine (Serc®): A first‑line prescription medication for Ménière’s disease and vertigo in Canada. It works as a histamine H3‑receptor antagonist and H1‑agonist, reducing labyrinthine pressure, and does not cause sedation.
• Scopolamine (Transderm‑V®): A prescription transdermal patch applied behind the ear for motion sickness prevention. It provides 72 hours of anti‑emetic activity and is an alternative for patients who cannot tolerate oral medications.
• Prochlorperazine (Stemetil®): A phenothiazine antipsychotic used as an anti‑emetic and for the treatment of vertigo. It carries a higher risk of extrapyramidal side effects than cinnarizine.
• Non‑pharmacological alternatives: For benign positional vertigo, the Epley manoeuvre (canalith repositioning procedure) is the recommended first‑line treatment. For motion sickness, behavioural strategies such as gaze stabilisation and habituation exercises can be helpful adjuncts.

Clinical Efficacy

Cinnarizine has a long history of clinical use for motion sickness and vestibular disorders, with efficacy established in numerous controlled trials. In motion sickness studies, cinnarizine 25 mg consistently demonstrates a significant reduction in nausea, dizziness, and vomiting compared with placebo, while producing less drowsiness than dimenhydrinate or scopolamine. In the management of vertigo associated with Ménière’s disease, cinnarizine has been shown to reduce both the frequency and severity of vertiginous attacks. A randomised controlled trial comparing cinnarizine with betahistine found similar improvements in vertigo control, with cinnarizine offering additional benefit for patients who also experience significant nausea. For peripheral vascular disorders, cinnarizine improves walking distance in patients with intermittent claudication and reduces the frequency and severity of vasospastic attacks in Raynaud’s phenomenon. The drug’s dual mechanism of action as both an antihistamine and a calcium‑channel blocker makes it a versatile option for vestibular and circulatory indications; however, its use is limited in Canada due to its non‑marketed status and the availability of other agents with a more favourable safety profile in the elderly, such as betahistine and meclizine.

Important:

Stugeron (cinnarizine) is a prescription medication that has not been approved for marketing by Health Canada. It should only be used under the close supervision of a qualified healthcare professional. This medication can cause significant drowsiness and may impair your ability to drive or operate machinery; do not engage in such activities until you know how the drug affects you. Alcohol must be strictly avoided. Cinnarizine can cause extrapyramidal symptoms, including drug‑induced parkinsonism, particularly in elderly patients and with prolonged use at higher doses. If you experience tremor, muscle stiffness, slowness of movement, or involuntary movements of the face or tongue, discontinue the medication immediately and seek medical advice. This drug is contraindicated in patients with Parkinson’s disease, during the first trimester of pregnancy, and while breastfeeding. This information is not a substitute for professional medical advice, diagnosis, or treatment.

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