Sumatriptan-OBL pills p o. 50mg N2
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Sumatriptan
Release form
Pills
Composition
1 tablet contains: sumatriptan (in the form of succinate) 50 mg.
Pharmacological effect
Remedy for the treatment of migraine; serotonin 5-HT1 receptor agonist. The therapeutic effect of sumatriptan appears to be due to two mechanisms: the substance excites serotonin 5-HT1 receptors of vascular smooth muscle of the carotid artery system and causes their narrowing. The carotid arteries supply blood to the head tissue, incl. meninges; with the expansion of the vessels of the brain membranes associated with the occurrence of migraine attacks. In addition, sumatriptan activates the receptors of the endings of the afferent fibers of the trigeminal nerve in the dura mater; as a result, the secretion of sensory neuropeptides is reduced. Sumatriptan does not penetrate well through the BBB and, according to experimental data, does not possess the actual analgesic properties. The effect of sumatriptan usually occurs 30 minutes after ingestion and 10-15 minutes after s / c administration.
Pharmacokinetics
After ingestion is rapidly absorbed. 70% of the maximum plasma concentration is reached after 45 minutes. Cmax in plasma is 54 ng / ml. Bioavailability - 14% (due to presystemic metabolism and incomplete absorption). Plasma protein binding is 14–21%. Metabolized by oxidation with the participation of monoamine oxylase (predominantly isoenzyme A) to form metabolites, the main ones being the indole acetic analog of sumatriptan, which does not have pharmacological activity against 5-HT1-serotonin receptors, and its glucuronide. Excreted by the kidneys, mainly in the form of metabolites.
Indications
Migraine (relief of attacks, with or without aura).
Contraindications
Hypersensitivity, hemiplegic, basilar or ophthalmoplegic forms of migraine, coronary heart disease (CHD), (including suspicion of it), angina (including Prinzmetal angina), myocardial infarction (including in history) , arterial hypertension (uncontrolled), occlusive peripheral arterial disease, stroke or transient cerebral circulation (including history), hepatic and / or renal failure.
Use during pregnancy and lactation
Clinical experience with sumatriptan during pregnancy is limited, and therefore is contraindicated for use. Caution should be used during lactation. It is not recommended to breastfeed for 24 hours after taking sumatriptan.
Dosage and administration
Inside Begin treatment as soon as possible after the onset of a migraine attack (although the drug is equally effective at any stage of the attack). For the relief of acute migraine attacks in adults - 50 mg. if necessary, 100 mg (the pill should be swallowed whole with water). If the symptoms of migraine do not disappear and do not decrease after the first dose, then again for the relief of an ongoing attack is not prescribed. 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 intake is at least 2 hours. For any 24 hours, the maximum dose is 300 mg / day .
Side effects
Since the cardiovascular system: a decrease in blood pressure (BP), a transient increase in blood pressure (observed soon after admission), bradycardia. palpitations, tachycardia (including ventricular); in some cases - severe cardiac arrhythmias (up to ventricular fibrillation), transient ECG changes of the ischemic type, myocardial infarction, in rare cases Raynaud's syndrome. From the alimentary system: nausea and vomiting; in some cases, a slight increase in the activity of liver transaminases. feeling of abdominal discomfort, dysphagia, ischemic colitis. From the nervous system: dizziness, weakness (usually mild or moderately pronounced and transient); rarely - drowsiness, feeling tired (more often when taken orally); in some cases - epileptic seizures (usually with a history of epilepsy). From the senses: sometimes - diplopia, flashing flies before the eyes, nystagmus, scotoma, reduced visual acuity, very rarely - partial loss of vision (may be associated with the attack itself migraine). Allergic reactions: skin rash (including - urticaria and erythematous rash), itching of the skin, anaphylactic reactions. Other: myalgia. "Flushes" of blood to the face.
Overdose
Symptoms: when administered to 400 mg, no other adverse reactions other than those listed above are observed. Treatment: gastric lavage, observation of the patient for 10 hours, symptomatic therapy.
Interaction with other drugs
With simultaneous use with lithium salts, cases of the development of the serotonin syndrome are described. With simultaneous use with moclobemide, the bioavailability of moclobemide increases in the absence of clinical manifestations. If used simultaneously with Rizatriptan, there is a risk of additive hyper-stimulation of serotonin 5-HT1 receptors; with ergotamine - the development of vasospasm is possible. In case of simultaneous use of preparations of the herb St. John's wort, serotonergic effects may increase and side effects may develop.
special instructions
Sumatriptan is not used to prevent migraine attacks. It is used with caution in disorders of the liver and kidneys, as well as in patients with epilepsy or other disorders of brain function. When treating attacks, it is advisable to start treatment as early as possible, however, the introduction of sumatriptan during the aura period other symptoms may not prevent the occurrence of headache. When treating with sumatriptan, symptoms sometimes appear that resemble angina attacks - pain, a feeling of constriction in the chest. In this regard, sumatriptan should not be used in case of suspected undiagnosed cardiovascular disease, before conducting an appropriate examination. If there is no effect on the administration of the first dose of sumatriptan, it is necessary to verify the diagnosis. The safety and efficacy of use in children and adolescents under the age of 18 years has not been established Influence on the ability to drive motor vehicles and control mechanisms. During migraine, as well as during therapy with sumatriptan, drowsiness may develop. Therefore, during the period of use, patients should be extremely careful to drive a car and engage in other potentially hazardous activities that require a high rate of psychomotor reactions.