STUGERON Cinnarizine 25mg Tablet 1's
RXDRUG-DR-XY34825-1pc
Discreet Packaging
FDA-registered Products
FDA-licensed Pharmacies
Indications/Uses
Stugeron: Prophylaxis of migraine.
Disorders of balance: maintenance therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting.
Prophylaxis of motion sickness.
Stugeron Forte: Cerebral circulatory disorders: 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; Prophylaxis of migraine.
Disorders of balance: Maintenance therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting.
Peripheral circulatory disorders: 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.
Motion sickness: Prophylaxis of motion sickness.
Disorders of balance: maintenance therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting.
Prophylaxis of motion sickness.
Stugeron Forte: Cerebral circulatory disorders: 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; Prophylaxis of migraine.
Disorders of balance: Maintenance therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting.
Peripheral circulatory disorders: 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.
Motion sickness: Prophylaxis of motion sickness.
Dosage/Direction for Use
Stugeron: Dosage: Prophylaxis of migraine: Adults: 1 tablet three time a day.
Disorders of balance: Adults: 1 tablet three time a day.
Prophylaxis of motion sickness: Adults and adolescents aged 13 years and above: 1 tablet 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: Cinnarizine (Stugeron) should preferably be taken after meals.
Stugeron Forte: Cerebral Circulatory Disorders: Adult: 1 cap of 75 mg daily.
Peripheral Circulatory Disorders: Adult: 2-3 caps of 75 mg daily.
Disorders of Balance: Adults: 1 cap of 75 mg daily.
Stugeron Forte should preferably be taken after meals.
The maximum recommended dosage should not exceed 225 mg (9 tabs or 3 caps) daily.
Disorders of balance: Adults: 1 tablet three time a day.
Prophylaxis of motion sickness: Adults and adolescents aged 13 years and above: 1 tablet 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: Cinnarizine (Stugeron) should preferably be taken after meals.
Stugeron Forte: Cerebral Circulatory Disorders: Adult: 1 cap of 75 mg daily.
Peripheral Circulatory Disorders: Adult: 2-3 caps of 75 mg daily.
Disorders of Balance: Adults: 1 cap of 75 mg daily.
Stugeron Forte should preferably be taken after meals.
The maximum recommended dosage should not exceed 225 mg (9 tabs or 3 caps) daily.
Overdosage
Symptoms and Signs: Acute cinnarizine overdoses have been reported with doses ranging from 90 to 2250 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.
Stugeron: It is advisable to contact a poison control center to obtain the latest recommendations for the management of an overdose.
Stugeron Forte: Within the 1st hr after ingestion, gastric lavage may be performed.
Activated charcoal may be given if considered appropriate.
Treatment: There is no specific antidote. For any overdose, the treatment is symptomatic and supportive care.
Stugeron: It is advisable to contact a poison control center to obtain the latest recommendations for the management of an overdose.
Stugeron Forte: Within the 1st hr after ingestion, gastric lavage may be performed.
Activated charcoal may be given if considered appropriate.
Administration
Should be taken with food.
Contraindications
Patients with known hypersensitivity to cinnarizine.
Special Precautions
As with other antihistamines, cinnarizine may cause epigastric distress; taking it after meals may diminish gastric irritation.
In patients with Parkinson's disease, cinnarizine should only be given if the advantages outweigh the possible risk of aggravating this disease.
Cinnarizine 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 the Ability to Drive or Operate Machinery: Since somnolence may occur, especially at the start of the treatment, caution should be taken during activities such as driving or operating machinery.
Stugeron Forte: Use in Pregnancy & Lactation: Although in animal studies cinnarizine has shown no teratogenic effects, as with all drugs, it 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 in human breast milk; nursing should therefore be discouraged in women using Stugeron Forte.
In patients with Parkinson's disease, cinnarizine should only be given if the advantages outweigh the possible risk of aggravating this disease.
Cinnarizine 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 the Ability to Drive or Operate Machinery: Since somnolence may occur, especially at the start of the treatment, caution should be taken during activities such as driving or operating machinery.
Stugeron Forte: Use in Pregnancy & Lactation: Although in animal studies cinnarizine has shown no teratogenic effects, as with all drugs, it 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 in human breast milk; nursing should therefore be discouraged in women using Stugeron Forte.
Use In Pregnancy & Lactation
Pregnancy: Although in animal studies, cinnarizine (Stugeron/Stugeron Forte) has shown no teratogenic effects, as with all drugs, cinnarizine (Stugeron/Stugeron Forte) should be used during pregnancy only if the therapeutic benefits justify the potential risks for the fetus.
Breastfeeding: There are no data on the excretion of cinnarizine (Stugeron/Stugeron Forte) in human breast milk: nursing should therefore be discouraged in women using cinnarizine (Stugeron/Stugeron Forte).
Breastfeeding: There are no data on the excretion of cinnarizine (Stugeron/Stugeron Forte) in human breast milk: nursing should therefore be discouraged in women using cinnarizine (Stugeron/Stugeron Forte).
Adverse Reactions
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 affect the rates observed in clinical practice.
Clinical Trial Data: Placebo-Controlled Double-Blind Data - Adverse Drug Reactions Reported at ≥ 1% Incidence: The safety of cinnarizine (Stugeron) (30 to 225 mg/day) was evaluated in 601 subjects (of which 303 were treated with cinnarizine (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 cinnarizine (Stugeron)-treated subjects noted in the double-blind clinical trials are shown in Table 1. (See Table 1.)
Clinical Trial Data: Placebo-Controlled Double-Blind Data - Adverse Drug Reactions Reported at ≥ 1% Incidence: The safety of cinnarizine (Stugeron) (30 to 225 mg/day) was evaluated in 601 subjects (of which 303 were treated with cinnarizine (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 cinnarizine (Stugeron)-treated subjects noted in the double-blind clinical trials are shown in Table 1. (See Table 1.)
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 cinnarizine (Stugeron), in the treatment of peripheral circulatory disorders, cerebral circulatory disorders, and vertigo.
Adverse reactions reported by ≥ 1% of cinnarizine (Stugeron)-treated subjects noted in the comparator and open label clinical trials are shown in Table 2. (See Table 2.)
Adverse reactions reported by ≥ 1% of cinnarizine (Stugeron)-treated subjects noted in the comparator and open label clinical trials are shown in Table 2. (See Table 2.)
Placebo, Comparator, and Open-Label Data - Adverse Reactions Reported at < 1% Incidence: Additional adverse reactions that occurred in < 1% of cinnarizine (Stugeron)-treated subjects in the previously mentioned 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.)
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. Frequencies In the table are provided according to the following convention: Very common ≥ 1/10; Common ≥ 1/100 and < 1/10; Uncommon ≥ 1/1000 and < 1/100; Rare ≥ 1/10000 and < 1/1000; Very rare < 1/10000, including isolated reports; Not known Cannot be estimated from the available data. (See Table 4.)
Stugeron Forte: Somnolence and GI 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 depression, have been described during prolonged therapy. The treatment should be discontinued in such cases.
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 depression, have been described during prolonged therapy. The treatment should be discontinued in such cases.
Drug Interactions
Alcohol, CNS Depressants, Tricyclic Antidepressants: The sedative effects of Cinnarizine (Stugeron) and of any of the following may be potentiated when used concomitantly: alcohol, CNS depressants, or tricyclic antidepressants.
Diagnostic Interference: Because of its antihistaminic effect, cinnarizine may prevent otherwise positive reactions to dermal reactivity indicators if used up to 4 days prior to skin testing.
Diagnostic Interference: Because of its antihistaminic effect, cinnarizine may prevent otherwise positive reactions to dermal reactivity indicators if used up to 4 days prior to skin testing.
Caution For Usage
Stugeron: Incompatibilities: None Known.
Storage
Store at temperature not exceeding 30°C.
Action
Cinnarizine is a selective calcium-entry blocker belonging to group IV of the calcium antagonists (WHO classification). It has an antihistamine (H1)-effect (Stugeron Forte).
Pharmacology: Pharmacodynamics: Mechanism of action: 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: Stugeron: 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.
Stugeron Forte: The peak plasma levels of cinnarizine are obtained 1-3 hrs after intake. It disappears from plasma with a t½ of 4 hrs. It 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%.
Toxicology: Non-Clinical Information: Stugeron: 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.
Single dose Lethal Dose50 (LD50) values in various animal models show a large margin of safety on a mg/kg basis when compared to the maximum recommended human dose (MRHD) of 100 mg/day or 2 mg/kg as based on a 50 kg person. LD50 values were > 1000 mg/kg in the mouse following oral, subcutaneous and intraperitoneal administrations. Similarly, the LD50 values in the rat and dog were > 640 mg/kg and > 160 mg/kg, respectively, for all three routes of administration. The LD50 following intravenous administration in the mouse and rat were 22 mg/kg and 24 mg/kg, respectively. The LD50 in the guinea pig was > 40 mg/kg following oral and subcutaneous administrations. Results from acute oral subcutaneous and intraperitoneal toxicity in the mouse or rat with dihydrochloride salt were similar to the results of the parent compound.
Repeat dose oral (administered in the diet) toxicity studies in the rat showed some decrease in food consumption and changes in serum chemistry (decrease in inorganic phosphorus, increase in calcium/phosphor ratio), organ weight (decrease in spleen and heart, increase in liver, kidney and brain) and histopathology (chronic centrilobular degeneration and pancreatic modifications).
These observations were generally in the high dose group (320 mg/kg or 160 x MRHD) and were more pronounced after 18-months of treatment. After 3- or 12-months oral dosing in the dog, all observations were similar to controls except for some decreased body weight (after 3 months at 80 mg/kg or 40 x MRHD) or some limited histopathological findings (focal nuclear vacuolation and satellitosis in the CNS, hydropic aspect in the liver, pancreatic modifications, lymphoid depletion, inhibition of spermatogenesis and atrophy of female genital tract) after 12 months at the high dose of 20 mg/kg (10 x MRHD).
In reproductive studies in the rat, rabbit, and dog, there were no effects on fertility and no teratogenicity. At very high doses (80 to 320 mg/kg, 40 to 160 x MRHD) in the rat, maternal toxicity resulted in decreased litter size, an increase in the percent of resorptions and a decrease in fetal birth weight.
In vitro mutagenicity study with Salmonella typhimurium indicated that the parent compound is not mutagenic up to 10 μmol/plate. However, after reacting with nitrite and forming the nitrosation product, a weak mutagenic activity was observed. Carcinogenicity has not been specifically evaluated. However, no pre-neoplastic changes were evident during chronic 18-month oral administration in rats up to a dose of 160 times the maximum human dose level.
Pharmacology: Pharmacodynamics: Mechanism of action: 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: Stugeron: 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.
Stugeron Forte: The peak plasma levels of cinnarizine are obtained 1-3 hrs after intake. It disappears from plasma with a t½ of 4 hrs. It 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%.
Toxicology: Non-Clinical Information: Stugeron: 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.
Single dose Lethal Dose50 (LD50) values in various animal models show a large margin of safety on a mg/kg basis when compared to the maximum recommended human dose (MRHD) of 100 mg/day or 2 mg/kg as based on a 50 kg person. LD50 values were > 1000 mg/kg in the mouse following oral, subcutaneous and intraperitoneal administrations. Similarly, the LD50 values in the rat and dog were > 640 mg/kg and > 160 mg/kg, respectively, for all three routes of administration. The LD50 following intravenous administration in the mouse and rat were 22 mg/kg and 24 mg/kg, respectively. The LD50 in the guinea pig was > 40 mg/kg following oral and subcutaneous administrations. Results from acute oral subcutaneous and intraperitoneal toxicity in the mouse or rat with dihydrochloride salt were similar to the results of the parent compound.
Repeat dose oral (administered in the diet) toxicity studies in the rat showed some decrease in food consumption and changes in serum chemistry (decrease in inorganic phosphorus, increase in calcium/phosphor ratio), organ weight (decrease in spleen and heart, increase in liver, kidney and brain) and histopathology (chronic centrilobular degeneration and pancreatic modifications).
These observations were generally in the high dose group (320 mg/kg or 160 x MRHD) and were more pronounced after 18-months of treatment. After 3- or 12-months oral dosing in the dog, all observations were similar to controls except for some decreased body weight (after 3 months at 80 mg/kg or 40 x MRHD) or some limited histopathological findings (focal nuclear vacuolation and satellitosis in the CNS, hydropic aspect in the liver, pancreatic modifications, lymphoid depletion, inhibition of spermatogenesis and atrophy of female genital tract) after 12 months at the high dose of 20 mg/kg (10 x MRHD).
In reproductive studies in the rat, rabbit, and dog, there were no effects on fertility and no teratogenicity. At very high doses (80 to 320 mg/kg, 40 to 160 x MRHD) in the rat, maternal toxicity resulted in decreased litter size, an increase in the percent of resorptions and a decrease in fetal birth weight.
In vitro mutagenicity study with Salmonella typhimurium indicated that the parent compound is not mutagenic up to 10 μmol/plate. However, after reacting with nitrite and forming the nitrosation product, a weak mutagenic activity was observed. Carcinogenicity has not been specifically evaluated. However, no pre-neoplastic changes were evident during chronic 18-month oral administration in rats up to a dose of 160 times the maximum human dose level.
MedsGo Class
Antivertigo Drugs / Peripheral Vasodilators & Cerebral Activators
Features
Brand
Stugeron
Full Details
Dosage Strength
25mg
Drug Ingredients
- Cinnarizine
Drug Packaging
Tablet 1's
Generic Name
Cinnarizine
Dosage Form
Tablet
Registration Number
DR-XY34825
Drug Classification
Prescription Drug (RX)
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