Expiration date: 10/2028
Release form
Film-coated tablets 100 mg - 10 pcs with instructions for medical use (package insert) in a pack.
Dosage form
Round, biconvex, film-coated tablets are white or off-white, scored on one side. A cross-section of the tablet, regardless of dosage, reveals two layers: an off-white core and a film coating.
Composition
Film-coated tablet 100.0 mg contains:
Active ingredient: sumatriptan succinate - 140.0 mg, in terms of sumatriptan - 100.0 mg;
Excipients: lactose monohydrate (milk sugar) - 102.4 mg, microcrystalline cellulose (MCC-101) - 90.0 mg, sodium croscarmellose - 12.0 mg, povidone-K25 - 12.0 mg, magnesium stearate - 3.6 mg.
Shell composition: hypromellose - 5.8 mg, macrogol-4000 - 1.2 mg, titanium dioxide - 3.0 mg.
Pharmacotherapeutic group
anti-migraine drug
Pharmacodynamics
Sumatriptan is a selective 5-hydroxytryptamine-1 receptor (5-HT?D) agonist that does not affect other 5-HT receptor subtypes (5-HT?-5-HT?). 5-HT?D receptors are located primarily in the cranial blood vessels of the brain, and their stimulation leads to vasoconstriction.
In animals, sumatriptan selectively acts by vasoconstricting branches of the carotid artery without affecting cerebral blood flow. The carotid artery vascular bed supplies extracranial and intracranial tissues (including the meninges), and dilation and/or swelling of these vessels is believed to be the primary mechanism for migraine in humans. Furthermore, preclinical data suggest that sumatriptan reduces trigeminal nerve sensitivity. Both of these effects may underlie sumatriptan's antimigraine activity. Sumatriptan is effective in the treatment of menstrual migraine, i.e., migraine without aura that occurs 3 days before and 5 days after the menstrual cycle. The clinical effect is usually observed 30 minutes after oral administration of 100 mg. Although the recommended oral dose is 50 mg, migraine attacks vary in severity both within and between patients. Doses of 25 mg to 100 mg have shown greater efficacy than placebo in clinical trials, but 25 mg is statistically significantly less effective than 50 mg and 100 mg.
Pharmacokinetics
Migraine attacks do not significantly affect the pharmacokinetics of orally administered sumatriptan.
Suction
After oral administration, sumatriptan is rapidly absorbed, reaching 70% of its maximum plasma concentration within 45 minutes. After a 100 mg dose, the mean maximum plasma concentration is 54 ng/mL. The mean absolute bioavailability is 14%, partly due to first-pass metabolism and partly due to incomplete absorption.
Distribution
Sumatriptan binds to plasma proteins to a small extent (14-21%), the average total volume of distribution is 170 L.
Metabolism
The major metabolite, the indoleacetic acid analogue of sumatriptan, is excreted primarily in the urine as the free acid and glucuronide. This metabolite is inactive at 5-HT? and 5-HT? serotonin receptors. No minor metabolites of sumatriptan have been detected.
Withdrawal
The half-life is approximately 2 hours. The mean total plasma clearance is approximately 1160 ml/min, the mean renal clearance is approximately 260 ml/min, and extrarenal clearance is approximately 80% of the total clearance.
Sumatriptan is metabolized by monoamine oxidase A.
Special patient groups
Patients with impaired liver function
Due to a decrease in presystemic clearance of sumatriptan in patients with impaired liver function, the level of sumatriptan in blood plasma increases.
Elderly patients
Pharmacokinetics in patients over 65 years of age does not differ significantly from that in younger patients.
Indications
Relief of acute migraine attacks with or without aura, including attacks of menstruation-associated migraine.
Sumatriptan should only be used in patients with a confirmed diagnosis of migraine.
Contraindications
- Hypersensitivity to sumatriptan or any of the excipients of the drug;
- Hemiplegic, basilar and ophthalmoplegic forms of migraine.
- History of myocardial infarction, ischemic heart disease, coronary vasospasm (Prinzmetal's angina), peripheral vascular disease, patients with symptoms and signs of ischemic heart disease;
- History of stroke or transient ischemic attack;
- Severe liver dysfunction;
- Moderate and severe arterial hypertension, uncontrolled mild arterial hypertension;
- Concomitant use of ergotamine or ergotamine derivatives (including methysergide), any triptans/5-hydroxytryptamine? (5-HT?) receptor agonists (see section “Interaction with other medicinal products”);
- Concomitant use with monoamine oxidase inhibitors (MAO), as well as within two weeks after discontinuation of therapy with MAO inhibitors;
- Age up to 18 years and over 65 years;
- Lactase deficiency, galactose intolerance and glucose-galactose malabsorption (due to the presence of lactose in the drug).
Precautionary measures
With caution
- controlled mild arterial hypertension;
- diseases that may alter the absorption, metabolism or excretion of this drug (eg, impaired renal or hepatic function);
- epilepsy (including any conditions with a decrease in the seizure threshold);
- in patients with hypersensitivity to sulfonamides (taking sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis). Data on cross-sensitivity are limited, but caution should be exercised when prescribing sumatriptan to such patients.
Use during pregnancy and breastfeeding
Pregnancy
Post-marketing use of sumatriptan-containing medications has been described in over 1,000 women during the first trimester of pregnancy. Although the data are insufficient to draw a definitive conclusion, the data do not suggest an increased risk of congenital malformations.
Experience with the use of sumatriptan in the second and third trimesters of pregnancy is limited.
Animal studies have shown no direct teratogenic or adverse effects on prenatal or postnatal development. However, effects on embryo-fetal viability were observed in rabbits. Sumatriptan should only be used if the expected benefit to the mother outweighs the potential risk to the fetus.
Breastfeeding period
Sumatriptan has been shown to be excreted into breast milk following subcutaneous administration. To avoid adverse effects on the infant, breastfeeding should be discontinued during treatment with sumatriptan and for 12 hours after discontinuation. Breast milk should be pumped promptly during this period.
Use by children
The drug is contraindicated for use by children under 18 years of age.
The efficacy and safety of sumatriptan in children under 10 years of age have not been studied. No clinical data are available for this age group.
The efficacy and safety of sumatriptan in children aged 10 to 17 years have not been established.
demonstrated in clinical studies conducted in this age group. Therefore, the use of sumatriptan in children aged 10 to 17 years is not recommended.
Method of administration and dosage
The tablet should be swallowed whole with water.
Adults
Sumatriptan is used for the intermittent treatment of migraine attacks. The drug should not be used prophylactically.
Treatment with sumatriptan should be started as soon as possible after the onset of a migraine attack, but the drug is equally effective at any stage of the attack.
The recommended dose of Sumatriptan is 50 mg, in some cases the dose may be increased to 100 mg.
The maximum dose of Sumatriptan should not exceed 300 mg during any 24-hour period.
If the patient feels better after the first dose and then symptoms return, a second dose can be taken within the next 24 hours, provided that a minimum time interval of two hours is observed between the two doses.
If the first dose of sumatriptan is ineffective, a second dose should not be used to relieve the same migraine attack. In this case, paracetamol, aspirin, or nonsteroidal anti-inflammatory drugs may be used. Sumatriptan may be used to relieve subsequent attacks.
Sumatriptan is recommended for use as monotherapy for migraine; sumatriptan should not be used concomitantly with ergotamine or its derivatives (including methysergide).
For patients with impaired liver function: the recommended dose is 50 mg.
Children
The efficacy and safety of sumatriptan in children under 10 years of age have not been studied. No clinical data are available for this age group.
The efficacy and safety of sumatriptan in children aged 10 to 17 years have not been established.
demonstrated in clinical studies conducted in this age group. Therefore, the use of sumatriptan in children aged 10 to 17 years is not recommended.
Elderly patients (over 65 years old)
Experience with the use of sumatriptan in patients over 65 years of age is limited.
Pharmacokinetics are not significantly different from those in younger patients, but until appropriate clinical data are obtained, the use of sumatriptan in patients over 65 years of age is not recommended.
Side effects
Adverse reactions are listed below according to anatomical and physiological classification and frequency of occurrence.
Frequency is defined as follows: very common (>1/10); common (>1/100 and <1/10); uncommon (>1/1,000 and <1/100); rare (>1/10,000 and <1/1,000); very rare (<1/10,000), frequency not known (frequency cannot be estimated from the available data). Some of the symptoms that have been described as adverse reactions may be symptoms associated with migraine.
Clinical trial data:
From the nervous system: often - dizziness, drowsiness, sensory disturbances, including paresthesia and decreased sensitivity.
From the vascular system: often - transient increase in blood pressure (shortly after taking the drug), hot flashes.
From the respiratory system and chest organs: often - shortness of breath.
From the gastrointestinal tract: often - nausea, vomiting (a causal relationship between the occurrence of adverse reactions and taking the drug has not been proven).
From the musculoskeletal and connective tissue: often - a feeling of heaviness (usually transient, can be intense and occur in any part of the body, including the chest and throat), myalgia.
General disorders and administration site conditions: Common - pain, feeling of cold or heat, feeling of pressure or tightness (usually transient, can be intense and occur in any part of the body, including the chest and throat), weakness, fatigue (usually mild to moderate, transient).
Laboratory and instrumental data: very rarely - minor deviations in liver function tests.
Post-registration data
From the immune system: frequency unknown - hypersensitivity reactions that range from cutaneous manifestations of hypersensitivity to anaphylaxis.
From the nervous system: frequency unknown - seizures (in some cases observed in patients with a history of seizures or with concomitant conditions predisposing to the occurrence of seizures; in some patients, risk factors were not identified), tremor, dystonia, nystagmus, scotoma.
Eye disorders: frequency unknown - flickering, diplopia, decreased visual acuity. Vision loss (usually transient). However, visual disturbances may be caused by the migraine attack itself.
From the heart: frequency unknown - bradycardia, tachycardia, palpitations, arrhythmia, ECG signs of transient myocardial ischemia, coronary vasospasm, angina pectoris, myocardial infarction.
From the vascular side: frequency unknown - decreased blood pressure, Raynaud's syndrome.
From the gastrointestinal tract: frequency unknown - ischemic colitis, diarrhea.
From the musculoskeletal and connective tissue: frequency unknown - neck stiffness, arthralgia.
From the psyche: frequency unknown - anxiety.
From the skin and subcutaneous tissues: frequency unknown - hyperhidrosis.
Overdose
Oral administration of sumatriptan at doses greater than 400 mg did not cause any adverse reactions other than those listed above.
In case of sumatriptan overdose, patients should be observed for at least 10 hours and symptomatic therapy should be administered if necessary. There are no data on the effect of hemodialysis or peritoneal dialysis on plasma sumatriptan concentrations.
Drug interactions
No interactions were observed between sumatriptan and propranolol, flunarizine, pizotifen and ethyl alcohol in healthy volunteers.
Concomitant use of sumatriptan and ergotamine or other triptans/5-HT?-serotonin receptor agonists is contraindicated. A theoretically increased risk of coronary vasospasm is possible, and concomitant use of these drugs is contraindicated (see Contraindications).
The time interval between the use of sumatriptan and ergotamine-containing products or another triptan/5-HT? receptor agonist is unknown. It will depend, among other things, on the dose and type of medication prescribed. The effect may be additive. It is recommended to wait at least 24 hours after the use of ergotamine-containing products or another triptan/5-HT? receptor agonist before using sumatriptan. Conversely, it is recommended to wait at least 6 hours after the use of sumatriptan before using ergotamine-containing products and at least 24 hours before using another triptan/5-HT? receptor agonist.
An interaction between sumatriptan and MAO inhibitors is possible; their concomitant use is contraindicated (see section “Contraindications”).
There have been rare reports of serotonin syndrome (including mental disorders, autonomic instability, and neuromuscular disturbances) following the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Serotonin syndrome has also been reported with the concomitant use of triptans and selective serotonin and norepinephrine reuptake inhibitors (SNRIs).
Side effects are more common when triptans are used concomitantly with medications containing St. John's wort.
Special instructions
Sumatriptan should only be used in patients with a confirmed diagnosis of migraine.
Sumatriptan is not indicated for use in hemiplegic, basilar, and ophthalmoplegic migraine.
The recommended dose of sumatriptan should not be exceeded. As with other medications for the treatment of acute migraine attacks, other potentially serious neurological conditions should be excluded before treating a headache attack in patients previously undiagnosed with migraine or in patients with atypical migraine.
It should be noted that patients with migraine have an increased risk of developing certain cerebrovascular disorders (eg, stroke or transient ischemic attacks (TIA)).
After taking Sumatriptan, transient symptoms such as chest pain and pressure may occur. These symptoms may be intense and may extend to the neck. If there is reason to believe these symptoms are a manifestation of coronary artery disease (CAD), further use of sumatriptan should be discontinued and appropriate diagnostic testing should be performed.
Patients with risk factors for coronary heart disease, including heavy smokers or those using nicotine replacement therapy, should not be prescribed sumatriptan without prior cardiovascular evaluation. Particular care should be taken in postmenopausal women and men over 40 years of age with these risk factors. However, testing does not always detect heart disease, and in very rare cases, serious cardiac complications have occurred in patients without underlying cardiovascular disease.
Sumatriptan should be used with caution in patients with controlled mild hypertension, as transient increases in blood pressure and peripheral vascular resistance have been observed in a small number of patients.
There have been rare postmarketing reports of serotonin syndrome (including mental status changes, autonomic instability, and neuromuscular disturbances) following the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Serotonin syndrome has also been reported with the concomitant use of sumatriptan with triptans and selective serotonin-norepinephrine reuptake inhibitors (SNRIs).
If concomitant use of SSRIs and/or SNRIs is clinically warranted in a patient, the patient's condition should be closely monitored.
Sumatriptan should be used with caution in patients who may have significantly altered absorption, metabolism, or excretion of sumatriptan, such as those with liver or renal impairment. In patients with liver impairment, the initial dose should be 50 mg.
Sumatriptan should be used with caution in patients with a history of seizures or other risk factors for lowering the seizure threshold, as seizures have been reported with sumatriptan.
In patients with known hypersensitivity to sulfonamides, sumatriptan may cause allergic reactions, ranging from cutaneous hypersensitivity reactions to anaphylaxis. Data on cross-sensitivity are limited, so caution should be exercised before administering sumatriptan to these patients.
Side effects may be more common with the simultaneous use of triptans and medications containing St. John's wort.
Long-term use of any type of painkiller for headaches can lead to worsening headaches. If this occurs or is suspected, discontinue therapy and undergo further evaluation. Medication overuse headache may be suspected in patients who experience recurrent or daily headaches despite regularly taking headache medications.
Patients with rare hereditary problems of lactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take Sumatriptan because it contains lactose.
Impact on control of vehicles and mechanisms
Migraine patients may experience drowsiness, both related to the migraine itself and to the use of sumatriptan. Patients should exercise particular caution when driving or operating machinery.
Storage temperature
from 2℃ to 25℃
