Temporary eradication of acute attacks of migraine with or without aura and cluster headache.
Composition:
1 syringe (0.5 ml) contains 6 mg of Sumatriptan in the form of succinate.
Action:
Antimigraine drug - a selective agonist of 5-HT serotonin receptors1D. It does not affect other receptor subtypes (5-HT2 up to 5-HT7). The drug selectively narrows the blood vessels in the area of blood circulation of the carotid artery, not affecting the cerebral flow. In addition, the results of experimental studies suggest that it inhibits trigeminal nerve activity. Both mechanisms underlie the anti-migraine effect of sumatriptan. The effect of the drug after subcutaneous administration starts after 10-15 minutes. Bioavailability of sumatriptan after subcutaneous administration is 96%. The maximum concentration in the blood occurs after 25 minutes after administration. The degree of binding to plasma proteins is small (14-21%). It is metabolized mainly by monoamine oxidase A. The major transformation product - an indole acetic acid analogue is excreted in the urine, where it occurs in the form of free acid and glucuronides. Its action was not found on 5-HT receptors1 and 5-HT2. Non-renal excretion accounts for about 80% of total clearance. T0,5 in the blood is about 2 hours.
Contraindications:
Hypersensitivity to sumatriptan or any of the excipients. A history of myocardial infarction, ischemic heart disease, Prinzmetal angina, peripheral vascular disease or ischemic heart disease, moderate and severe symptoms, and mild uncontrolled hypertension. Patients after a stroke, brain or transient cerebral ischemic attack. Severe liver dysfunction. Simultaneous use with preparations containing ergotamine or its derivatives (including methy allergen) or any drug from the group of triptans or other 5-HT receptor agonists1. Co-administration with MAO inhibitors and 2 weeks from discontinuation. Do not use intravenously.
Precautions:
The preparation is not indicated for patients with hemiplegic migraine, basal or periportal migraine. In patients with previously diagnosed migraine, but with an unusual picture of a given headache and migraine-type headache, patients who have not previously been diagnosed with migraine should take measures to exclude potential other causes of the disorder (eg stroke or transient cerebral ischemic attack) ). Caution should be exercised in patients with mild controlled hypertension due to possible transient increases in blood pressure and peripheral vascular resistance. After administration of Sumatriptan, transient pain and tightness in the chest and throat may occur, sometimes severely; if these symptoms point to ischemic heart disease, the drug should be discontinued and appropriate diagnostic tests should be performed. The drug should be used with caution in patients who may be expected to change in absorption, metabolism or excretion of the drug, eg in hepatic impairment (Child-Pugh grade A or B) or kidney function. Special care should be taken in patients who have had seizures or risk factors lowering the seizure threshold and in patients with hypersensitivity to sulphonamides. The abuse of painkillers in the treatment of headache may be related to its severity (headache dependent on drug abuse - MOH), in these patients may need to stop treatment. In patients at risk for cardiovascular disease (heavy smokers, nicotine replacement therapy, postmenopausal women and men over 40 years of age), sumatriptan should only be used after appropriate testing. The preparation contains less than 1 mmol (23 mg) sodium per dose, ie it is considered to be "sodium-free".
Pregnancy and lactation:
It can only be used during pregnancy if the benefit to the mother outweighs the potential risk to the fetus. Sumatriptan is excreted in milk - breastfeeding should be avoided within 12 hours of admission.
Side effects:
Very common: temporary pain at the injection site, burning sensation, local swelling, redness, bruising, bleeding from the injection site. Common: dizziness, drowsiness, sensory disturbances (including paraesthesia and hypoaesthesia), transient increase in blood pressure soon after administration, sudden redness (especially of the face), shortness of breath, nausea and vomiting (the association with sumatriptan is not clear), pain , feeling hot or cold, heaviness, tension or pressure (these symptoms are usually transient, can be strong and occur in various parts of the body, including the chest and throat), feeling weak, tired, and aching muscles. Very rare: slight changes in liver function values. Not known: symptoms of hypersensitivity (from skin changes to anaphylactic shock), seizures (in patients with a history of seizures or co-existing factors that predispose to their occurrence, as well as in people without risk factors), tremor, dystonia, nystagmus, scotoma, flicker of light , double vision, changes in the field of vision, loss of vision, including permanent vision loss (visual disturbances may be a component of a migraine attack), bradycardia, tachycardia, palpitations, arrhythmia, transient ischemic changes in the ECG, coronary spasm, angina chest pain, myocardial infarction, hypotension, Raynaud's syndrome, ischemic colitis, diarrhea, stiff neck, joint pain, anxiety, excessive sweating.
Dosage:
subcutaneous. Adults aged 18-65. The preparation should be taken as soon as possible after the first symptoms of migraine or accompanying symptoms (nausea, vomiting, photophobia), however, the drug administered at any stage of the attack is equally effective. When starting treatment, the effectiveness of the preparation is independent of the duration of the seizure. The use of the drug in the migraine aura phase before the appearance of other symptoms may not prevent the occurrence of headache.Migraine: a single dose of the preparation is 6 mg. If the symptoms of a migraine attack do not improve after the first dose, taking a second dose during the same seizure is pointless; then treatment with acetaminophen, Acetylsalicylic acid or other NSAIDs may be used. The drug can be used during subsequent seizures. In case of recurrence of symptoms, the second dose of the preparation may be administered no earlier than after 1 hour from the first dose. The maximum dose within 24 hours is 2 injections of 6 mg.Cluster headache: a single dose of the preparation is 6 mg. The maximum dose within 24 hours is 2 injections of 6 mg with at least 1 hour interval between doses. The preparation should not be used prophylactically or a dose greater than the recommended dose.Special groups of patients. It is not recommended for use in children and adolescents below 18 years of age and over 65 years due to the lack of data on safety and efficacy.Way of giving. Subcutaneous injections are made using an autoinjector.
(C)
