Sumatriptan Teva pills coated 50mg N2
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Active ingredients
Sumatriptan
Release form
Pills
Composition
1 tab. Sumatriptan 50 mg. Excipients: lactose monohydrate 70.
Pharmacological effect
Sumatriptan is a specific selective 5HT1D-serotonin receptor agonist (5-hydroxytryptamine-1-like), located mainly in the blood vessels of the brain. Stimulation of 5HT1D serotonin receptors leads to vasoconstriction. The drug does not affect other subtypes of 5HT-serotonin receptors (5HT2-5HT7). Experimental studies have shown that sumatriptan causes a selective narrowing of the carotid arteries that supply extracranial and intracranial tissues with blood, including the meninges (expansion of these vessels and / or their edema is the main mechanism for the development of migraine in humans), without having a significant effect on the cerebral blood flow. It has also been established experimentally that sumatriptan inhibits the activity of receptors for the endings of the trigeminal afferent fibers. Eliminates nausea and photophobia associated with migraine attack.
Pharmacokinetics
Absorption: After oral administration, sumatriptan is rapidly absorbed, after 45 minutes its concentration in the blood plasma reaches 70% of the maximum value. After oral administration, sumatriptan at a dose of 100 mg Cmax in plasma is reached in 2-2 / 5 hours and averages 54 ng / ml. Absolute bioavailability when administered orally averages 14% due to presystemic metabolism and incomplete absorption. Distribution: Plasma protein binding is 14–21%, with a total Vd of 170 liters on average (2.4 L / kg). Metabolism: Sumatriptan is metabolized by oxidation with the participation of MAO (mainly isoenzyme A) with the formation of metabolites, the main of which is the indole-analogue of sumatriptan, which does not have pharmacological activity against 5HT1- and 5HT2-serotonin receptors, and its glucuronide. Withdrawal: T1 / 2 is 2-2.5 hours. On average, plasma clearance is 1160 ml / min, renal clearance is 260 ml / min. Extrarenal clearance is 40% after ingestion. Excreted by the kidneys, mainly in the form of metabolites (97% after ingestion) of free acid or glucuronide, the rest is excreted by the intestines.
Indications
- migraine (for relief of attacks, with or without aura).
Contraindications
- hemiplegic, basilar and ophthalmoplegic forms of migraine - ischemic heart disease (including myocardial infarction, post-infarction cardiosclerosis, Prinzmetal stenocardia) - patients who have risk factors for developing coronary heart disease - stroke or transient violation of cerebral circulation (including in vein of heart failure (including in veins of cerebral ischemic heart disease or stroke) or transient cerebral circulation (including in vein of heart failure (including in vein of heart failure), or transient cerebral circulation (including in vema, including in heart arteries (including in heart arteries) peripheral vascular occlusive diseases - uncontrolled arterial hypertension - severe hepatic and / or renal failure - simultaneous use with ergot alkaloids and their derivatives (including metizergid) or other triptans and / 5HT1-serotonin receptor agonists - simultaneous administration of MAO inhibitors and a period of up to 14 days after their discontinuation - up to 18 years old, patients over 65 years old - lactose intolerance, lactase deficiency, glucose-galactose malabsorption - hypersensitivity to sumatriptan or other components of the drug . With care Epilepsy (including any condition, accompanied by a decrease in the convulsive readiness threshold in history), organic brain damage, controlled arterial hypertension, impaired renal function and / or impaired liver function of mild to moderate severity, pregnancy.
Use during pregnancy and lactation
Despite the fact that the safety data obtained when using sumatriptan in 1000 women in the first trimester of pregnancy do not contain sufficient information, there is no reason to draw definitive conclusions about the risk of congenital defects in the fetus. Experience with sumatriptan II and III trimester of pregnancy is limited. The use of sumatriptan during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. Breastfeeding should be discontinued during the administration of sumatriptan and within 24 hours after the end of its administration.
Dosage and administration
Inside (pill is swallowed whole with water). The initial single dose of 50 mg, if necessary, the dose can be increased to 100 mg. If the symptoms of migraine do not disappear and do not decrease after taking the first dose, then the second dose is not prescribed to relieve the continuing attack.For relief of subsequent attacks (with the reduction or disappearance of symptoms, and then resumption), you can take a second dose over the next 24 hours, provided that the interval between doses is at least 2 hours. The maximum daily dose for ingestion is 300 mg.
Side effects
The frequency of side effects is classified according to the recommendations of the World Health Organization: very often - at least 10%; often not less than 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01% (including isolated cases). Since the cardiovascular system: very rarely - bradycardia, tachycardia, arrhythmia, transient increase in blood pressure (BP) (immediately after the start of treatment), transient signs of myocardial ischemia on ECG, coronary spasm, myocardial infarction, Raynaud's syndrome, decrease in blood pressure "flushes" of blood to the face. On the part of the respiratory system: often - shortness of breath, transient irritation of the mucous membrane or burning sensation in the nasal cavity or throat. On the part of the digestive system: often - nausea, vomiting; a slight increase in the activity of liver enzymes; very rarely - ischemic colitis, diarrhea, a feeling of discomfort in the abdomen. On the part of the nervous system: often - dizziness, drowsiness, impaired sensitivity, including paresthesia, hypesthesia; very seldom - convulsions (usually in the presence of convulsions in the anamnesis); unknown frequency - tremor, dystonia, anxiety. On the part of the organ of vision: infrequently - diplopia, flickering of "flies" before the eyes, nystagmus, scotoma, decrease in visual acuity; very rarely - partial transient loss of vision (it should be borne in mind that visual impairment may be associated with the migraine attack itself). From the musculoskeletal system: often - myalgia; unknown frequency -regidity of the occipital muscles, arthralgia. Allergic reactions: very rarely - skin rash, urticaria, pruritus, erythema, anaphylaxis. Other: often - pain, tingling, feeling hot, feeling weak and / or tired, nose bleeding, feeling of pressure or heaviness (these symptoms are usually transient, but can be intense and occur in any part of the body, including the chest and neck); unknown frequency - increased sweating.
Overdose
With a single subcutaneous dose of 12 mg, sumatriptan did not cause any side effects. When administered subcutaneously at a dose of more than 16 mg or when administered more than 400 mg, sumatriptan did not cause any unforeseen side effects other than those listed above. Treatment: gastric lavage, taking activated charcoal, monitoring the condition of patients for at least 10 hours, if necessary - symptomatic therapy. There is no data on the effect of hemodialysis and peritoneal dialysis on the concentration of sumatriptan in plasma.
Interaction with other drugs
Sumatriptan does not interact with propranolol, flunarisine, pizothiphene and ethyl alcohol. The simultaneous use of sumatriptan with ergot alkaloids and their derivatives (including metisergide) or other triptans / agonists of 5HT1-serotonin receptors is accompanied by an increased risk of developing prolonged vasospasm and ischemia. Sumatriptan can be used no earlier than 24 hours after administration of ergot alkaloids and their derivatives or other triptans / 5HT1-serotonin receptor agonists, in turn, preparations containing ergot alkaloids can be taken no earlier than 6 hours after administration of sumatriptan, other triptans / agonists of 5HT1-serotonin receptors can be taken no earlier than 24 hours after administration of sumatriptan. Interaction between sumatriptan and MAO inhibitors is possible, their simultaneous use is contraindicated. There are very rare reports from postmarketing observations on the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders), while using sumatriptan with selective serotonin reuptake inhibitors (SSRIs). The development of serotonin syndrome has also been reported with the simultaneous use of triptans with selective serotonin and norepinephrine reuptake inhibitors (NRIs). Isolated reports have been received of a more pronounced manifestation of adverse reactions on the part of sumatriptan with simultaneous use with herbal preparations containing St. John's wort perforated.
special instructions
Sumatriptan is not intended for the prevention of migraine.Sumatriptan should be taken only if the diagnosis of migraine is beyond doubt. Sumatriptan should be used as early as possible after the onset of a migraine attack, however, the drug is equally effective at any stage of the attack. In the absence of the effect of the first dose, the diagnosis should be clarified. When sumatriptan is used to relieve headaches in patients with previously untreated migraine or in migraines with atypical symptoms, other potentially dangerous neurological diseases should be excluded. It must be borne in mind that in patients with migraine there is a risk of cerebrovascular complications (including stroke or transient cerebral circulatory disorders). Sumatriptan should be used with caution in epilepsy and any other conditions accompanied by a decrease in the convulsive readiness threshold. In the case of simultaneous use with SSRIs / SNRIs, the patient’s condition should be carefully monitored (see section “Interaction with Other Medicines”). Before using sumatriptan in patients, cardiovascular disease should be excluded, especially in patients at risk. These patients are women in the postmenopausal period, men over the age of 40 years and patients with risk factors for developing coronary artery disease.The survey does not always reveal cardiovascular disease in some patients. In very rare cases, after taking sumatriptan, transient side effects such as pain and chest tightness may occur. The pain can be intense and radiate to the neck (throat) area. If there is reason to believe that these symptoms may be a manifestation of IHD , it is necessary to stop taking the drug and make a diagnostic examination.Treatment with sumatriptan in patients with controlled arterial hypertension should be carried out with caution, because in some cases sya increased blood pressure and peripheral vascular resistance. Sumatriptan should be used with caution in patients with diseases in which significant changes in the absorption, metabolism or excretion of sumatriptan are possible, for example, in cases of impaired renal or liver function.Patients with hypersensitivity to sulfonamides with sumatriptan may develop allergic reactions that range from skin manifestations to anaphylactic shock. Data on cross-sensitivity is limited, but caution is needed when using sumatriptan in such patients. The abuse of drugs intended to relieve migraine attacks is associated with an increase in headaches in sensitive patients (a headache associated with the abuse of drugs). In this case, the possibility of drug withdrawal should be considered. Influence on the ability to drive vehicles and control equipment With migraine, as well as during therapy with sumatriptan, drowsiness may develop. Therefore, during the period of use of sumatriptan, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and quickness of psychomotor reactions.