Sumamigren®
Sumatriptan should only be prescribed if the diagnosis of migraine is certain and should be used as soon as possible after the onset of a migraine attack, although it is equally effective when used at any stage of the attack. The drug cannot be used for prophylactic purposes.
Sumatriptan should be taken with caution in controlled arterial hypertension of grade I, since in some cases a transient increase in blood pressure and peripheral vascular resistance was observed during administration; diseases in which the absorption, metabolism or excretion of the drug may be altered (for example, impaired renal or liver function).
There are very rare reports from post-marketing surveillance of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) as a result of concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. The development of serotonin syndrome has also been reported during concomitant use of triptans with selective serotonin norepinephrine reuptake inhibitors (SNRIs). In case of simultaneous administration with drugs from the SSRI/SNRI group, the patient's condition should be carefully monitored.
Sumatriptan should be used with caution in patients with epilepsy and a history of other risk factors accompanied by a decrease in the seizure threshold, since such patients may develop seizures while taking sumatriptan. Concomitant use of other triptans/5HT1 receptor agonists with sumatriptan is not recommended.
In patients with hypersensitivity to sulfonamides, the use of sumatriptan may cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis. Cross-sensitivity data are limited, but caution should be exercised when prescribing sumatriptan to such patients.
As with other antimigraine drugs, when prescribing sumatriptan in patients with previously undiagnosed migraine or in patients with atypical migraine, it is necessary to exclude other potentially serious neurological conditions. It should be noted that patients with migraine have an increased risk of developing certain cerebrovascular complications (stroke or transient ischemic attack).
Sumatriptan should not be prescribed to patients at risk of cardiovascular disease without prior examination to exclude cardiovascular pathology. These patients include postmenopausal women, men over 40 years of age, patients with risk factors for coronary artery disease, as well as smokers and those using nicotine replacement therapy. Although testing may not always detect heart disease in some patients, in very rare cases they develop cardiovascular side effects.
After taking sumatriptan, transient intense pain and tightness in the chest may occur, spreading to the neck area. If there is reason to believe that these symptoms are a manifestation of coronary heart disease, you should stop taking the drug and conduct an appropriate diagnostic examination.
Overuse of medications intended to treat migraine attacks is associated with increased headaches in sensitive patients (drug overuse headache). If you develop or suspect a headache associated with drug abuse, you should consult a doctor. In this case, the possibility of discontinuing the drug should be considered.
Undesirable effects may be more common when using triptans and herbal preparations containing St. John's wort ( Hypericum
perforatum
).
Do not exceed the recommended dose of sumatriptan.
Pharmacological properties of the drug Sumamigren
Pharmacodynamics . Sumatriptan is a specific selective agonist of 5-HT1D receptors and has no effect on other subtypes of serotonin receptors (5-HT2–5-HT7). These receptors are located primarily in the blood vessels of the carotid system. Acting on 5-HT1D receptors, sumatriptan selectively narrows the lumen of these arteries, but does not affect cerebral blood flow. According to the results of experimental studies, the drug also inhibits the activity of the trigeminal nerve. Both of these mechanisms determine the antimigraine effect of sumatriptan. The clinical effect develops 30 minutes after taking the drug. Pharmacokinetics . Absorption of sumatriptan after oral administration occurs quickly, 70% of the maximum concentration of sumatriptan in the blood plasma is achieved after 45 minutes, and its average value after taking the drug at a dose of 100 mg is 54 ng/ml. The average 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 l. The average total plasma clearance is 1160 ml/min, and the average renal clearance is about 260 ml/min. Removal . The half-life of sumatriptan from blood plasma is about 2 hours. The extrarenal route of elimination of the drug accounts for about 80% of the total clearance. Sumatriptan is metabolized primarily with the participation of monoamine oxidase A. The main metabolite, an analogue of indoleacetic acid, is excreted in the urine in the form of free acid and glucuronate. The effect on 5-HT1 and 5-HT2 receptors has not been established. Metabolites formed in smaller quantities have not been established. A migraine attack does not have a significant effect on the pharmacokinetics of sumatriptan after oral administration.
Contraindications to the use of Sumamigren
Hypersensitivity to sumatriptan or other components of the drug, coronary artery disease (angina pectoris, Prinzmetal angina, history of myocardial infarction) or other pathology of the cardiovascular system, cerebral disorders (stroke, history of transient ischemic attacks) and peripheral circulation (including intestinal ischemia), severe or uncontrolled hypertension (arterial hypertension), concomitant use of MAO inhibitors (Sumamigren can be taken 14 days after the last dose of MAO inhibitors), ergotamine or its derivatives (dihydroergotamine and methysergide), or other 5-HT1 receptor agonists (Sumamigren can be taken after 24 hours after the last use of these drugs), severe liver failure. Cluster headache (in older people).
Side effects of the drug Sumamigren
Data from clinical studies From the nervous system: phono- and photophobia, dizziness, drowsiness, sensitivity disorders (including paresthesia and hypoesthesia), increased thermal sensitivity, a feeling of constriction in the head, depression, disturbances in concentration, smell, euphoria, pain in the face, lacrimation, sleep disturbances, tremor, aggressiveness, apathy, headache, convulsions, loss of appetite, hallucinations, paralysis of facial muscles, feeling of hunger, hysteria, memory impairment. From the cardiovascular system: transient increase in blood pressure soon after taking the drug, flushing of the face, fainting, decreased blood pressure, arrhythmia, ECG changes, pallor of the skin, tachycardia, angina pectoris, atherosclerosis, bradycardia, cerebral ischemia, cardiac conduction disorders of varying degrees. , peripheral cyanosis, transient myocardial ischemia. From the ENT organs: sinusitis, tinnitus, allergic rhinitis, inflammation of the upper respiratory tract, ear, nose and laryngeal bleeding, otitis media, hearing impairment, rhinitis, feeling of stuffiness in the ears. From the endocrine system and metabolism: thirst, increased TSH levels, galactorrhea, hyperglycemia, hypoglycemia, hypothyroidism, polydipsia, increase or decrease in body weight, electrolyte imbalance, formation of cysts in the endocrine glands, skin nodules, increased sensitivity of the mammary glands. From the organ of vision: changes in the sclera, mydriasis, blurred vision, itching, eye irritation and burning sensation, accommodation disturbances, eye pain, keratitis and conjunctivitis. From the gastrointestinal tract: nausea and vomiting that occur in some patients, but their connection with the use of Sumamigren has not been definitively established, diarrhea, dyspepsia, constipation, gastroesophageal reflux, gastrointestinal bleeding, melena, peptic ulcer, abdominal pain, dental pain, hypersalivation, irritation of the oral mucosa. From the musculoskeletal system: a feeling of heaviness (symptoms are usually transient in nature, can be pronounced and of different localization, including the chest and larynx), myalgia, convulsions. From the respiratory system: shortness of breath, dyspnea, bronchospasm, sneezing, cough, bronchitis. From the skin and subcutaneous tissue: sweating, itching, rash, dry skin, seborrheic dermatitis. From the urogenital system: polyuria, intermenstrual bleeding. General disorders: pain, sensation of warmth or cold, squeezing or tension (can be severe and of different locations, including the chest and larynx), feeling of weakness, fatigue. Laboratory values: minor changes in liver function tests were noted. Allergic reactions: common - anaphylaxis or anaphylactoid reactions have occurred rarely, more often in patients with a history of allergies, but can be life-threatening. Other: infrequently - fever, fluid retention in the body, rarely - hyperhidrosis, lymphadenopathy, speech disorders and voice changes, ecchymosis. Post-marketing data From the immune system: hypersensitivity reactions from skin hypersensitivity to anaphylaxis in isolated cases. From the nervous system: seizures, and, in some cases, noted in patients with seizures or with a history of conditions that can lead to seizures, and there have also been cases of seizures in patients without an increased risk of developing a seizure syndrome; tremor, dystonia, nystagmus, scotoma, stiff neck. On the part of the organ of vision: flickering “fly spots” before the eyes, diplopia, decreased visual acuity, loss of vision (usually transient). However, visual disturbances can be a consequence of a migraine attack. From the cardiovascular system: bradycardia, tachycardia, palpitations, arrhythmia, transient ischemia on the ECG, coronary artery spasm, angina pectoris, myocardial infarction, arterial hypotension, Raynaud's phenomenon. From the gastrointestinal tract: ischemic colitis.
Overdose of Sumamigren, symptoms and treatment
No side effects were detected in 670 patients who took the drug at a single dose of 140–300 mg orally. In 174 healthy volunteers who took the drug at a single dose of 140–400 mg orally, no severe side effects other than those described were noted. Overdose in animals was accompanied by convulsions, tremor, paralysis, inertia, mydriasis, hypersalivation, lacrimation and led to death. The half-life of sumatriptan is 2.5 hours, however, in case of overdose, patients must be monitored for at least 12 hours or the entire period of clinical manifestations of intoxication. The effect of hemodialysis or peritoneal dialysis on the level of Sumamigren in the blood plasma has not been established.
