Sumatriptan-LF tablets po 100mg №4×1

Name:
Sumatriptan-LF.
Description:
Round, biconvex, white film-coated tablets. Composition Each tablet contains: Active substance: sumatriptan (as sumatriptan succinate) – 50 mg or 100 mg. Excipients: croscarmellose sodium, talc, anhydrous colloidal silicon dioxide, lactose monohydrate, magnesium stearate, microcrystalline cellulose. Sheath composition: Opadray II 85F18422 white (polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc). Pharmacotherapeutic group Anti-migraine drugs, selective 5-HT1 receptor agonists. Code ATXN02CC01 Pharmacological properties Pharmacodynamics Sumatriptan is a specific selective 5-HT1D serotonin receptor agonist. It does not affect other subtypes of serotonin receptors (5-HT2 – 5-HT7). These receptors are predominantly located in the cranial blood vessels, and their stimulation causes vasoconstriction. In animals, sumatriptan selectively causes narrowing of the branches of the carotid artery, but does not affect cerebral blood flow. Branches of the carotid artery supply extracranial and intracranial tissues such as the meninges with blood. It is believed that the expansion of these vessels and / or swelling of their walls is the main mechanism for the onset of migraine in humans. In addition, animal data show that sumatriptan reduces trigeminal nerve activity. Both effects (cranial vasoconstriction and inhibition of trigeminal nerve activity) contribute to the anti-migraine effect of sumatriptan. Sumatriptan remains effective in the treatment of migraine associated with menstruation, that is, migraine without aura, which occurs in the period including 3 days before and 5 days after the start of the menstrual cycle. Sumatriptan should be taken as soon as possible when an attack starts. Pharmacokinetics Absorption of sumatriptan when taken orally occurs quickly: 70% of the maximum plasma concentration is reached after 45 minutes, and its average value after taking 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. Sumatriptan binds to plasma proteins to a small extent (14-21%). The average volume of distribution is 170 liters. The main metabolite is the indolacetic analogue of sumatriptan, which is excreted in the urine, where it is present as free acid and glucuronates. Its effect on 5-HT1 and 5-HT2 receptors was not noted. Metabolites present in smaller amounts have not been identified. The plasma elimination half-life of sumatriptan is approximately 2 hours. The total mean plasma clearance is 1160 ml/min and the mean renal plasma clearance is approximately 260 ml/min. Extrarenal excretion of the drug is approximately 80% of the total clearance. Sumatriptan is mainly biotransformed with the participation of monoamine oxidase A. The pharmacokinetics of sumatriptan after oral administration is not significantly affected by migraine attacks. Special Patient Populations Patients with Hepatic Impairment The pharmacokinetics of sumatriptan was studied after an oral dose (50 mg) or subcutaneous administration (6 mg) in 8 patients with mild to moderate hepatic impairment compared to 8 sex-, age-, and weight-matched healthy subjects. volunteers. After oral administration, the plasma exposure of sumatriptan (AUC and Cmax) was almost twice as high (increased by approximately 80%) in patients with hepatic insufficiency compared with the control group with normal liver function. After subcutaneous administration, no difference was observed between patients with impaired liver function and the control group. This indicates that mild to moderate hepatic impairment results in decreased presystemic clearance and increased bioavailability and exposure of sumatriptan compared to healthy subjects. After oral administration, presystemic clearance is reduced in patients with mild to moderate hepatic impairment and systemic exposure is almost doubled. Pharmacokinetics in patients with severe hepatic insufficiency has not been studied (see sections “Contraindications”, “Precautions and features of use”). Elderly patients (over 65 years of age) The kinetics in the elderly is not well understood to establish possible differences in kinetics between younger and older volunteers. Indications for use Relief of migraine attacks with or without aura in adults. Sumatriptan-LF should only be used if a definite diagnosis of migraine has been made. Dosage and Administration Sumatriptan should not be taken for prophylactic purposes. Sumatriptan is indicated for the treatment of migraine attacks as the sole drug and should not be taken concomitantly with ergotamine or ergotamine derivatives (including methyzergide). The drug should be taken immediately after the onset of a migraine attack. The drug is also effective in any stage of a migraine attack. Adults The recommended oral dose of sumatriptan is 50 mg. Some patients require a dose of 100 mg. If after taking a single dose of the drug the symptoms do not disappear, you should not take the next dose during the same migraine attack. Taking the next dose of the drug is possible during the next attack. If the patient feels better after taking the first dose, but the symptoms recur, then a second dose of the drug can be taken, provided that the interval between two doses is at least two hours. During any 24-hour period, the total dose should not exceed 300 mg. Tablets should be swallowed whole with water. Children and adolescents (under 18 years of age) Sumatriptan should not be used in children and adolescents due to the lack of sufficient data on the efficacy and safety of the use. Elderly patients (over 65 years) Data on the use of sumatriptan tablets in patients over 65 years of age are limited. There were no significant differences in pharmacokinetics between this age group of patients and younger people. Until detailed clinical data are collected, the use of sumatriptan in this group of patients is not recommended. Patients with impaired liver and kidney function Sumatriptan should be administered with caution to patients with impaired liver function (Child-Pugh class A or B) and kidney function (see sections “Pharmacokinetics”, “Precautions”). If treatment with sumatriptan is necessary in patients with mild or moderate hepatic insufficiency, the daily dose should not exceed 50 mg. Sumatriptan is contraindicated in severe hepatic impairment. Adverse reactions Adverse reactions were grouped according to the frequency of their occurrence, defined as follows: very often (> 1/10); often (>1/100 to <1/10); infrequently (>1/1000 to <1/100); rarely (>1/10,000 to <1/1000); very rare (<1/10,000), unknown (frequency cannot be determined based on available data). Some of these adverse reactions may be migraine symptoms. Immune system disorders Not known: hypersensitivity symptoms ranging from skin changes (eg, urticaria) to rare cases of anaphylactic shock. Nervous system disorders Common: dizziness, drowsiness, sensory disturbances, including paresthesia and hypoesthesia. Not known: Seizures that have occurred in people who have had seizures in the past or with factors that predispose them to occurrence, as well as in people without risk factors. Muscular trembling, dystonia, nystagmus, scotoma. On the part of the organ of vision Not known: flickering light, diplopia, changes in the visual field, including irreversible visual impairment. Visual disturbances can be part of a migraine attack. Cardiac disorders Not known: bradycardia, tachycardia, palpitations, cardiac arrhythmias, transient ischemic ECG changes, coronary artery spasm, angina pectoris, myocardial infarction. Vascular disorders Often: transient increase in blood pressure immediately after taking the drug, sudden redness, especially of the skin of the face. Not known: hypotension, Raynaud's syndrome. Respiratory, thoracic and mediastinal disorders Common: suffocation. Gastrointestinal disorders Common: some patients experience nausea and vomiting, but their relationship with sumatriptan is not obvious. Not known: ischemic colitis, diarrhea. Musculoskeletal and connective tissue disorders Common: A feeling of pressure or heaviness (symptoms are usually transient, but may be intense and occur anywhere in the body, including the chest and throat). Muscle pain. Not known: muscle tension in the back of the neck, joint pain. General disorders and disorders at the injection site Common: pain, feeling hot or cold, tension or heaviness (symptoms are usually transient, but can be intense and occur in any part of the body, including the chest and throat). Feeling of weakness, fatigue (these symptoms are most often of mild to moderate intensity and are transient). Influence on the results of laboratory and instrumental studies Very rarely: slight changes in the values of liver activity parameters. Psychiatric disorders Not known: fear. Skin and subcutaneous tissue disorders Not known: increased sweating. In case of occurrence of the listed adverse reactions, as well as reactions not listed in this leaflet, you should consult a doctor. Contraindications- Hypersensitivity to sumatriptan or to any of the excipients of the drug. - Do not use to prevent migraine attacks. - Do not use in children under 18 years of age or in patients over 65 years of age. - Ischemic heart disease or related symptoms, spasm of the coronary vessels (Prinzmetal's angina), previous myocardial infarction, Wolff-Parkinson-White syndrome, or arrhythmias associated with other accessory pathways of the heart. - Ischemic bowel disease. - A stroke or transient cerebrovascular accident. - Diseases of the peripheral vascular system. - Moderate and severe forms of arterial hypertension, as well as poorly controlled mild hypertension. - Use simultaneously with monoamine oxidase inhibitors (sumatriptan should not be used within 2 weeks after the end of treatment with monoamine oxidase inhibitors). - Simultaneous use with drugs containing ergotamine or its derivatives, for example, metizergide or other drugs from the group of 5-HT1 receptor agonists. - Severe liver failure. - Use during pregnancy and lactation - see the appropriate section. Overdose Oral doses of sumatriptan greater than 400 mg and subcutaneous administration of 16 mg did not cause any other side effects other than those indicated above. In patients, after administration of 12 mg of the drug subcutaneously, no significant side effects were noted. In case of an overdose of sumatriptan, the patient should be observed for at least 10 hours. Depending on the situation, symptomatic treatment should be carried out. The effect of hemodialysis or peritoneal dialysis on the change in plasma sumatriptan concentration is unknown. Use during pregnancy and lactation Pregnancy Based on post-marketing data in more than 1000 women who took sumatriptan in the first trimester of pregnancy, there was no increase in the incidence of congenital malformations in children, however, these data are insufficient to draw final conclusions. Data on the use of sumatriptan in the second and third trimester of pregnancy are limited. Evaluation of studies conducted on animals did not reveal a teratogenic effect and a detrimental effect in the pre- and postnatal period. However, in rabbits, the survival of embryos and (or) fetuses was impaired. Sumatriptan-LF should only be used during pregnancy when the potential benefit to the mother outweighs any potential risk to the fetus. Lactation After subcutaneous administration, sumatriptan has been found to be excreted in breast milk. Therefore, in order to minimize the effect of the drug on the nursing child, breastfeeding should be avoided for 12 hours after taking sumatriptan, and breast milk expressed during this period should be discarded. Precautions and features of the application Sumatriptan should be used only in patients after a thorough diagnosis of migraine. Sumatriptan is not recommended in patients with hemiplegic, basilar or ophthalmoplegic migraine. Sumatriptan should not be taken in patients at risk for developing coronary heart disease, including patients who smoke or use nicotine substitutes, without first assessing the condition of the circulatory system. Special care should be taken in postmenopausal women, as well as in men over the age of 40, who are also at risk. However, it should be borne in mind that not in every case the examinations carried out allow the correct diagnosis of heart disease, and that in very rare cases, severe symptoms of heart disease can occur without the presence of a disease of the cardiovascular system. After taking sumatriptan, transient pain and a feeling of heaviness in the chest and throat, sometimes significantly pronounced, may appear. Based on these symptoms, coronary artery disease can be suspected. In case of their occurrence, it is recommended to stop taking the drug and undergo an appropriate examination. Life-threatening cardiac arrhythmias, including ventricular tachycardia and fatal ventricular fibrillation, have been reported within hours of administration of 5-HT1 agonists. If heart rhythm disturbances occur, sumatriptan tablets should be discontinued. Sumatriptan is contraindicated in patients with Wolff-Parkinson-White syndrome or arrhythmias associated with other accessory pathways of the heart. Sumatriptan may cause a transient increase in blood pressure and an increase in peripheral vascular resistance. Sumatriptan-LF should be used with extreme caution in hypertensive patients. In patients with migraine status who have not previously been diagnosed with migraine, as well as in patients with previously diagnosed migraine, but with an atypical picture of this attack of headaches, another cause of malaise, a neurological origin, should be taken into account. It should be remembered that patients who suffer from migraine may be at risk of developing vascular damage to the brain, such as transient ischemic attack or stroke. Sumatriptan can lead to non-coronary vasospastic reactions such as peripheral vascular ischemia, intestinal ischemia, splenic infarction and Raynaud's syndrome. In patients with symptoms or signs suggestive of non-coronary vasospastic reactions after the use of any 5-HT1 agonist, vasospastic reactions should be ruled out until the next dose of sumatriptan tablets. Cases of transient or permanent blindness, significant partial loss of vision have been reported with the use of 5-HT1 agonists. Since visual disturbances can be part of a migraine attack, a causal relationship between these events and the use of 5-HT1 agonists has not been clearly established. During the simultaneous use of sumatriptan and selective serotonin reuptake inhibitors (SSRIs), the appearance of serotonin syndrome (including mental status changes, autonomic instability, and neuromuscular disorders) has been noted. The appearance of serotonin syndrome was also noted with the simultaneous use of triptans with serotonin and norepinephrine reuptake inhibitors (SNRIs). If concomitant treatment with sumatriptan and SSRI/SNRI drugs is clinically warranted, appropriate monitoring of the patient is recommended. Sumatriptan should be used with caution in patients in whom changes in drug absorption, metabolism, or excretion can be expected, such as those with hepatic or renal insufficiency. Sumatriptan should be used with extreme caution in patients who have been diagnosed with seizures or factors that lower the seizure threshold. In patients allergic to sulfonamides, allergic symptoms of varying intensity, from skin changes to anaphylactic shock, may occur after taking sumatriptan. Information on this topic is limited, however, caution should be exercised in these patients. Prolonged use of any pain reliever may cause headaches to worsen. If the patient is diagnosed or suspected of such a cause of headaches, he should stop taking the drug and consult a doctor. In patients suffering from frequent or daily headaches, despite the regular use of painkillers (or in connection with their use), the diagnosis of headaches due to the continuous use of these drugs should be considered. With the simultaneous use of sumatriptan and drugs containing St. John's wort (Hypericum perforatum), undesirable effects may occur more often. Do not take more than the recommended dosage. Due to the lactose content, the medicinal product should not be used in patients with rare hereditary galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption syndrome. The safety of treating an average of more than 4 episodes of headaches within 30 days has not been established. Influence on the ability to drive vehicles or potentially dangerous mechanisms Studies on the effect on the ability to drive a car and maintain mechanisms have not been conducted. Drowsiness may occur during treatment with sumatriptan. This may affect the ability to drive and operate machinery. Interactions with other medicinal products: Studies have not revealed interactions of sumatriptan with ethyl alcohol, as well as with such drugs as propranolol, flunarizine and pizotifen. Limited data are available on the interaction of medicinal products containing ergotamine with triptans and other 5-HT1 receptor agonists. The concomitant use of ergotamine and sumatriptan is contraindicated, since there is a theoretical possibility of an increased risk of vasospasm. The period that must elapse between taking sumatriptan and medicinal products containing ergotamine or other triptans and other 5-HT1 receptor agonists is unknown. It also depends on the dose taken and the form of the drug. Their impact can be cumulative. Before taking sumatriptan, it is recommended to wait at least 24 hours after using any drug containing ergotamine or other triptans and other 5-HT1 receptor agonists. Medicinal products containing ergotamine can be taken as early as 6 hours, and medicinal products containing other triptans and other 5-HT1 receptor agonists 24 hours after taking sumatriptan. Sumatriptan should not be taken simultaneously with MAO inhibitors and 2 weeks after the end of therapy with this drug due to possible interactions. During the simultaneous use of sumatriptan and selective serotonin reuptake inhibitors (SSRIs), the appearance of serotonin syndrome (including changes in mental state, instability of the autonomic system, and impaired coordination of movements) was noted. The appearance of serotonin syndrome was also noted with the simultaneous use of triptans with serotonin and norepinephrine reuptake inhibitors (SNRIs). Storage conditions In a place protected from moisture and light at a temperature not exceeding 25 ° C. Keep out of the reach of children. Shelf life 2 years. Do not use after the expiration date indicated on the package. Buy Sumatriptan-LF tablets po 100mg No. 4x1