Name:
Sumatriptan tablets 100 mg in a cell. cell No. 2×1
Description:
Film-coated tablets are blue, round, with a biconvex surface, a dosage of 100 mg – with a score. The cross section shows the core of an almost white color. The main active ingredient Sumatriptan Form of release coated tablets Dosage 100 mg Pharmacological properties Pharmacodynamics Sumatriptan is a specific selective agonist of vascular 5-hydroxytryptamine-1 receptors (5HT1D), does not affect other subtypes of 5HT receptors (5HT2 – 5HT7). 5HT1 receptors are located mainly in the blood vessels of the brain, and their stimulation leads to constriction of these vessels. Reduces the sensitivity of the trigeminal nerve. Both of these effects may underlie the anti-migraine effect of sumatriptan. The clinical effect is usually observed 30 minutes after oral administration of the drug (LS). Weakens the pulsation of the cerebral vessels and the associated headache. The drug also reduces the release of neuropeptides and other inflammatory mediators. It has no pronounced effect on adrenergic, dopaminergic, muscarinic and benzodiazepine receptors. It does not have a direct analgesic effect. Pharmacokinetics Absorption of sumatriptan after oral administration is fast, 70% Cmax of sumatriptan in plasma is reached after 45 minutes, and its average value after taking the drug at a dose of 100 mg is 54 ng / ml. The mean oral bioavailability of sumatriptan is 14%, partly due to metabolism and partly due to incomplete absorption. Distribution. To a small extent, sumatriptan binds to plasma proteins (14-21%). The average volume of distribution is 170 liters. The mean total plasma clearance is 1160 ml/min and the mean renal clearance is about 260 ml/min. Withdrawal. T? sumatriptan from plasma is about 2 hours. The extrarenal route of excretion of the drug is about 80% of the total clearance. Sumatriptan is metabolized mainly with the participation of monoamine oxidase A. The main metabolite, the indolacetic analogue of sumatriptan, is excreted in the urine as a free acid and a glucuronide conjugate. This metabolite has no activity in relation to 5-HT1 and 5-HT2 serotonin receptors. Metabolites formed in smaller quantities have not been established. A migraine attack does not significantly affect the pharmacokinetics of sumatriptan after oral administration. Indications for use Relief of migraine attacks with and without aura. Dosage and administration Inside, swallowing the tablet whole and drinking water. The recommended dose is one 50 mg tablet. Some patients may require a higher dose of 100 mg. If the symptoms of migraine do not disappear and do not decrease after taking the first dose of Sumatriptan, then the drug should not be taken again to stop the same attack. However, sumatriptan can be taken to relieve subsequent migraine attacks. If the patient feels better after the first dose and then symptoms recur, a second dose can be taken within the next 24 hours, while the total daily dose should not exceed 300 mg. Elderly patients (over 65 years of age). There is insufficient experience with the use of sumatriptan in patients over 65 years of age. Although the pharmacokinetics of the drug does not differ from that in young people, the use of Sumatriptan in patients over 65 years of age is not recommended until additional clinical data are obtained. The recommended daily dose for patients with hepatic insufficiency is 50 mg. Application during pregnancy and lactation In animal experiments (rats and rabbits), the use of sumatriptan was accompanied by embryotoxic effects, developmental anomalies and death of newborns. There are no data from adequate and well-controlled clinical studies on the safety of use during pregnancy. Drug Sumatriptan during pregnancy can be prescribed only if the expected therapeutic effect for the mother outweighs the potential risk to the fetus. Use with caution during lactation. Do not recommend breastfeeding for 24 hours after the use of drugs. Precautions: Sumatriptan should only be used if the diagnosis of migraine is beyond doubt. HP Sumatriptan can not be used for prophylactic purposes. In patients with previously undiagnosed migraine or in patients with atypical migraine, other neurological pathology must be excluded. It should be noted that patients with migraine have an increased risk of developing certain cerebrovascular disorders (eg, stroke or transient ischemic attacks). After taking sumatriptan, transient pain and tightness in the chest may occur, extending to the neck. If there is reason to believe that these symptoms are a manifestation of coronary heart disease, it is necessary to conduct an appropriate diagnostic examination. Sumatriptan should not be administered to patients at risk of cardiovascular disease without prior examination to exclude it (women in the post-menopausal period, men over the age of 40 years and patients with risk factors for coronary heart disease). The examination performed does not always reveal heart disease in some patients. In very rare cases, patients may experience serious adverse reactions from the cardiovascular system, in the anamnesis of which there was no cardiovascular pathology. It should be administered with caution to patients with controlled arterial hypertension, since in some cases there was a transient increase in blood pressure and peripheral vascular resistance; in patients suffering from diseases in which the absorption, metabolism or excretion of this drug may significantly change (for example, impaired renal or hepatic function). There are very rare post-marketing reports of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) as a result of the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. The development of serotonin syndrome has also been reported against the background of the simultaneous administration of triptans with selective serotonin and norepinephrine reuptake inhibitors. Children Do not recommend the use of the drug in children due to the fact that at present the efficacy and safety of sumatriptan in children have not been established. Interaction with other drugs No interactions of sumatriptan with propranolol, flunarizine, pizotifen and ethyl alcohol were noted. When taken simultaneously with ergotamine, a prolonged vasospasm was noted. Sumatriptan can be prescribed no earlier than 24 hours after taking drugs containing ergotamine; conversely, preparations containing ergotamine can be administered no earlier than 6 hours after taking sumatriptan. An interaction between sumatriptan and MAO inhibitors is possible, their simultaneous use is contraindicated. There are very rare post-marketing reports of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) as a result of the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. The development of serotonin syndrome has also been reported against the background of the simultaneous appointment of triptans with selective serotonin and norepinephrine reuptake inhibitors (SNRIs). Contraindications hypersensitivity to sumatriptan or other components of the drug; hemiplegic, basilar and ophthalmoplegic form of migraine; coronary heart disease (CHD) (including myocardial infarction, postinfarction cardiosclerosis, angina pectoris, Prinzmetal’s angina pectoris), as well as the presence of symptoms suggesting the presence of coronary artery disease; occlusive peripheral vascular disease; cerebrovascular accident (cerebrovascular accident, transient ischemia of the brain); uncontrolled hypertension, moderate and severe arterial hypertension; simultaneous use with monoamine oxidase inhibitors (drug Sumatriptan can be used after 14 days after treatment with monoamine oxidase inhibitors); simultaneous use with medicinal drugs containing ergotamine or its derivatives, such as dihydroergotamine and methysergide, or other drugs from the group of 5-HT1 receptor agonists (drug Sumatriptan can be used after 24 hours after le treatment with drugs containing ergotamine or its derivatives); severe liver failure; epilepsy; childhood and adolescence up to 18 years; pregnancy and lactation; age over 65 years excipients: talc, croscarmellose sodium, anhydrous colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, lactose monohydrate, opadra II (blue) (partially hydrolyzed polyvinyl alcohol, talc, macrogol 3350, titanium dioxide E 171, aluminum varnish based on indigo carmine E 132 , aluminum lacquer based on quinoline yellow E 104) . Overdosing The intake of drugs Sumatriptan orally at a dose of more than 400 mg did not cause any side effects, in addition to those listed above. In case of an overdose of Sumatriptan, the condition of patients should be observed for at least 10 hours and, if necessary, symptomatic therapy should be carried out. There are no data on the effect of hemodialysis or peritoneal dialysis on the plasma concentration of sumatriptan. Symptoms: increased severity of side effects. In case of overdose, it is necessary to cancel the drug. Treatment: symptomatic. Side effects Undesirable reactions are listed below depending on the anatomical and physiological classification and frequency of occurrence. The frequency is defined as follows: very frequent 1/10; frequent? 1/10; infrequent 1/1000 and <1/100; rare 1/10,000 and <1/1000; very rare <1/10,000, including isolated cases. The data of clinical studies were evaluated, while it must be remembered that the frequency of adverse reactions against the background of taking comparison drugs was not taken into account. Clinical studies: From the nervous system: often - dizziness, drowsiness, sensory disturbances, including paresthesia and decreased sensitivity. Since the cardiovascular system: often - a transient increase in blood pressure (shortly after taking the drug), hot flashes. From the respiratory system and chest organs: often - shortness of breath; mild, transient mucosal irritation or burning sensation in the nasal cavity or throat, epistaxis. From the gastrointestinal tract: often - nausea, vomiting (causal relationship has not been proven). From the musculoskeletal system and connective tissue: often - a feeling of heaviness (usually transient, can be intense and occur in any part of the body, including the chest and throat). General and local reactions: often - pain, a feeling of cold or heat, a feeling of pressure or tightness (usually transient, can be intense and occur in any part of the body, including the chest and throat). Often - weakness, fatigue (usually mild or moderate, transient). Laboratory indicators: very rarely - slight deviations in liver function tests. Post-marketing surveillance From the immune system: very rarely - hypersensitivity reactions, including skin manifestations, as well as anaphylaxis. On the part of the nervous system: very rarely - convulsive seizures (in some cases observed in patients with a history of convulsive seizures or with concomitant conditions predisposing to seizures; in some patients, no risk factors were identified), tremor, dystonia, nystagmus, scotoma. On the part of the organ of vision: very rarely - flickering, diplopia, decreased visual acuity. Blindness (usually transient). However, visual disturbances can be caused by the migraine attack itself. From the side of the cardiovascular system: very rarely - bradycardia, tachycardia, flutter, arrhythmias, transient ECG changes, coronary vasospasm, angina pectoris, myocardial infarction. Very rarely - hypotension, Raynaud's syndrome. From the gastrointestinal tract: very rarely - ischemic colitis, dysphagia, discomfort in the abdomen. Storage conditions In a place protected from light and moisture, at a temperature not exceeding 25 ° C. Keep out of the reach of children. Buy Sumatriptan tablets p/o 100mg No. 2x1
INN | SUMATRIPTAN |
---|---|
The code | 89 806 |
Barcode | 4 810 201 014 715 |
Dosage | 100mg |
Active substance | Sumatriptan |
Manufacturer | Borisovsky ZMP, Belarus |
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