pharmachologic effect
Antimigraine drug. A specific selective agonist of serotonin 5HT1D receptors, does not affect other subtypes of 5HT serotonin receptors. Serotonin 5HT1D receptors are located predominantly in the blood vessels of the brain, their stimulation leads to a narrowing of these vessels. Sumatriptan reduces the sensitivity of the trigeminal nerve. Both of these effects underlie the anti-migraine effect of the drug. The clinical effect is observed 30 minutes after taking the drug orally.
Sumamigren's analogues
The following drugs are analogues of Sumamigren based on the active substance:
- Amigrenin;
- Imigran;
- Migrepam;
- Sumatriptan;
- Sumatriptan Adifarm;
- Sumatriptan Pfizer;
- Sumig;
- Sumitran;
- Trimigraine;
- Sumatriptan-Teva;
- Ramimed;
- Sumarin.
According to the mechanism of action and belonging to the same pharmacological group, analogues of Sumamigren include the following medications:
- Zomig;
- Zomig Rapimelt;
- Naramig;
- Relpax;
- Frovamigran.
Pharmacokinetics
Suction
When taking the drug orally, sumatriptan is quickly absorbed from the gastrointestinal tract, and after 45 minutes 70% of Cmax is reached in plasma. When taking the drug at a dose of 100 mg, Cmax averages 54 ng/ml. Bioavailability when taken orally averages 14% due to first-pass metabolism and incomplete absorption.
Distribution
Plasma protein binding is 14-21%.
Metabolism
Biotransformed under the influence of MAO type A. The main metabolite is an indoleacetic analogue of sumatriptan, which has no activity against serotonin 5HT1 and 5HT2 receptors.
Removal
T1/2 is 2 hours. The main metabolite of sumatriptan is excreted primarily in the urine in the form of a free acid or glucuronide conjugate. Migraine attacks do not have a significant effect on the pharmacokinetics of sumatriptan taken orally.
Release form
According to the instructions, Sumamigren is released in the form of:
- film-coated, biconvex, oblong, light pink and white at the break, 50 mg tablets, with a score line on one side, 2 pcs. in blisters, in cardboard packs;
- film-coated, biconvex, oblong, white tablets 100 mg, 2 pcs. in blisters in cardboard boxes.
One tablet of Sumamigren contains 70 mg or 140 mg of sumatriptan succinate, 100 mg or 200 mg of microcrystalline cellulose, 123.5 mg or 247 mg of lactose monohydrate, 1.5 mg or 3 mg of croscarmellose sodium, 3 mg or 6 mg of magnesium stearate, 1. 5 mg or 3 mg talc and 500 mcg or 1 mg colloidal silicon dioxide.
The film shell of Sumamigren tablets contains 3.07 mg or 4.1 mg of hypromellose, 1.2 mg or 1.6 mg of macrogol 6000, 1.31 mg or 1.8 mg of talc, 900 mcg or 1.2 mg of titanium dioxide , 980 mcg or 1.3 mg of triethyl citrate and 40 mcg of crimson dye (for light pink tablets).
Dosage regimen
The tablets are taken orally whole with water.
The recommended single dose is 50 mg (1 tablet), in some cases it may be necessary to use the drug at a higher dose of 100 mg. If migraine symptoms do not disappear or improve after the first dose, the drug should not be re-prescribed to relieve an ongoing attack. The drug can be used to relieve subsequent migraine attacks.
If symptoms have decreased or resolved and then returned, a second dose may be taken within the next 24 hours. The maximum dose of the drug is 300 mg over 24 hours.
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.
Side effect
From the body as a whole:
pain, sensations of heat, tingling, tightness or heaviness (usually transient, but can be intense and occur in various parts of the body, including in the chest or throat); Hot flashes, dizziness, a feeling of weakness, a feeling of fatigue, drowsiness are also possible (usually mild or moderate and transient).
From the cardiovascular system:
decreased blood pressure, bradycardia, tachycardia, transient increase in blood pressure; rarely - rhythm disturbances, transient ischemic ECG changes, coronary artery spasm, myocardial infarction; in isolated cases - Raynaud's syndrome.
From the digestive system:
nausea, vomiting, ischemic colitis (the connection between these phenomena and the use of sumatriptan has not been clearly established); feeling of abdominal discomfort, dysphagia, increased activity of liver transaminases.
From the side of the central nervous system:
dizziness; rarely - seizures (in some cases observed in patients with a history of seizures or with conditions predisposing to the development of seizures); sometimes - diplopia, scotoma, nystagmus, decreased visual acuity; extremely rarely - partial transient loss of vision (it should be borne in mind that visual impairment may be associated with a migraine attack).
Allergic reactions:
rash, itching, erythema, urticaria; in isolated cases - anaphylactic reactions.
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.
Contraindications to the use of SUMAMIGREN®
- hemiplegic, basilar and ophthalmoplegic forms of migraine;
— IHD (including Prinzmetal’s angina, myocardial infarction, post-infarction cardiosclerosis), as well as the presence of symptoms suggesting IHD;
- occlusive diseases of peripheral arteries;
— stroke or transient cerebrovascular accident (including history);
- uncontrolled arterial hypertension;
- severe liver dysfunction;
- severe renal dysfunction;
- simultaneous use of drugs containing ergotamine or its derivatives (including metisegride);
- simultaneous use of MAO inhibitors and a period of up to 14 days after their discontinuation;
- pregnancy;
- lactation period (breastfeeding);
— age of patients under 18 years and over 65 years;
- hypersensitivity to the drug.
Carefully _
the drug is prescribed to patients with controlled arterial hypertension, with diseases in which the absorption, metabolism or excretion of sumatriptan may be altered (impaired liver or kidney function), with epilepsy (including any conditions with a decrease in the seizure threshold), with increased sensitivity to sulfonamides (the use of sumatriptan can cause allergic reactions of varying severity; from skin to anaphylactic reactions.
Indications and restrictions
Prescribed to alleviate the condition of patients during periods of migraine attacks with or without aura.
The medication should not be used in the following cases:
- Known intolerance to one or more components of the drug, including sumatriptan.
- Impaired delivery of nutrition and oxygen to organs and tissues due to a history of ischemia (coronary heart disease, myocardial infarction, vasospastic angina, stroke, TIA, impaired abdominal circulation, etc.)
- PAD leading to arterial occlusion.
Heart rhythm disturbances.- History of epilepsy.
- Hepatargy.
- Essential or secondary hypertension, uncontrolled or untreatable.
- Parallel use of drugs - derivatives of ergotamine or ergotamine itself, as well as monoamine oxidase enzyme blockers, including a 2-week period after their discontinuation.
- In the treatment of cluster cephalgia in the elderly.
Pregnancy is a contraindication for the use of this substance. It is recommended to breastfeed only 12 hours after the last dose of sumatriptan.
Studies were conducted in which about 800 children and adolescents aged 10 to 17 years suffering from migraine participated, where one group took a placebo and the other took Sumamigren. This study found no significant difference in effects between placebo and drug. The number and frequency of undesirable effects is the same in both adolescents and adults.
special instructions
Sumamigren ® should be prescribed only when the diagnosis of migraine is beyond doubt. The drug should be used as soon as possible after the onset of the attack, although it is equally effective when used at any stage of the attack.
The drug is not intended for the prevention of migraine attacks.
When prescribing Sumamigren to patients with previously undiagnosed migraine or to patients with atypical migraine, other potentially serious neurological conditions must be excluded. It should be noted that patients with migraine have an increased risk of developing cerebrovascular complications (stroke or transient cerebrovascular accident).
Sumamigren ® should not be prescribed to patients with suspected heart disease without prior examination. This category of patients includes postmenopausal women, men over 40 years of age, and patients with risk factors for developing coronary artery disease. The use of the drug is possible only after excluding diseases of the cardiovascular system. If, while using the drug, such patients develop symptoms from the cardiovascular system and there is reason to suspect coronary heart disease, then it is necessary to conduct an appropriate examination.
Do not exceed the recommended doses of the drug.
Impact on the ability to drive vehicles and operate machinery
During therapy with sumatriptan, drowsiness may develop (both associated with the disease itself and with taking the drug). Therefore, during the period of use of the drug, patients should be especially careful when driving a car and engaging in other potentially hazardous activities that require a high speed of psychomotor reactions.
Drug interactions
There were no drug interactions between sumatriptan and propranolol, flunarizine, pizotifen and ethanol.
When taken simultaneously with ergotamine, prolonged vasospasm was observed. Sumatriptan can be prescribed no earlier than 24 hours after taking drugs containing ergotamine, and drugs containing ergotamine can be prescribed no earlier than 6 hours after taking sumatriptan.
Interaction between sumatriptan and MAO inhibitors is possible; their simultaneous use is contraindicated.
There are isolated reports of the development of weakness, hyperreflexia and loss of coordination in patients after concomitant use of sumatriptan and selective serotonin reuptake inhibitors (this combination is not recommended, and if the use of such a combination is necessary, the patient's condition should be carefully monitored).
