Instructions for Stopmigren film-coated tablets 100 mg No. 3
Composition
active ingredient: sumatriptan;
1 tablet contains sumatriptan succinate 140 mg, which is equivalent to sumatriptan 100 mg;
excipients: lactose monohydrate; magnesium stearate; croscarmellose sodium; microcrystalline cellulose; talc; colloidal anhydrous silicon dioxide;
shell: Opadry II Orange film-coating mixture (aluminum lakes sunset yellow FCF (E 110) and indigo carmine (E 132); hypromellose; lactose monohydrate; triacetin; polyethylene glycol; iron oxide yellow (E 172); titanium dioxide (E 171)).
Dosage form
Film-coated tablets.
Main physicochemical properties: round tablets with a biconvex surface, coated with an orange film coating.
Pharmacotherapeutic group
Drugs used to treat migraine. Selective serotonin 5HT1 receptor agonist. Sumatriptan. ATC code N02C C01.
Pharmacological properties
Pharmacodynamics
Sumatriptan is a selective agonist of 5HT1D receptors that does not affect other 5HT receptors. These receptors are mainly located in the craniocerebral blood vessels. Experimental studies have shown that sumatriptan has a selective vasoconstrictor effect on vessels in the carotid artery system, but does not affect cerebral blood flow. The carotid artery system supplies blood to extra- and intracranial tissues, such as the meninges. Migraine develops as a result of the expansion of these vessels. In addition, experimental data have shown that sumatriptan inhibits the activity of the trigeminal nerve. These are two possible mechanisms by which sumatriptan exerts its antimigraine activity.
The clinical effect is observed 30 minutes after oral administration of 100 mg of the drug.
Pharmacokinetics
After oral administration, sumatriptan is rapidly absorbed, reaching 70% of the maximum concentration after 45 minutes. After taking 100 mg, the average maximum plasma concentration is 45 ng/ml. The oral bioavailability is 14%, partly due to first-pass metabolism and partly to incomplete absorption. Plasma protein binding is low (14–21%), and the average volume of distribution is 17 l. The average total plasma clearance is approximately 1160 ml/min, and the average renal clearance is approximately 260 ml/min. Non-renal clearance accounts for approximately 80% of the total clearance, suggesting that sumatriptan is excreted mainly as metabolites. The main metabolite, the indoleacetic analogue of sumatriptan, is excreted in the urine, where it is found as the free acid and a glucuronide conjugate. It does not exhibit 5HT1 or 5HT2 activity. Other metabolites have not been identified. The pharmacokinetics of oral sumatriptan are not significantly altered during a migraine attack.
Indication
Stopmigraine tablets are prescribed for rapid relief of migraine attacks, with or without aura.
Contraindication
Hypersensitivity to any component of the drug. History of myocardial infarction, ischemic heart disease, Prinzmetal's angina, peripheral vascular disease or symptoms characteristic of ischemic heart disease. History of stroke or transient ischemic attack. Moderate or severe arterial hypertension and mild uncontrolled arterial hypertension. Severe hepatic insufficiency.
Concomitant use of ergotamine or its derivatives (including methysergide) (see section "Interaction with other medicinal products and other types of interactions").
Concomitant use of any triptan/5-hydroxytryptamine receptor (5-HT1) agonist (see section "Interaction with other medicinal products and other types of interactions").
Concurrent administration of monoamine oxidase inhibitors (MAOIs) and Stopmigren. Stopmigren should not be used within 2 weeks of discontinuation of MAOIs.
Interaction with other medicinal products and other types of interactions
There are no data on interactions with propranolol, flunarizine, pizotifen, or alcohol.
Data on concomitant use with medicinal products containing ergotamine or other triptan/5-HT1 receptor agonists are limited. Theoretically, prolonged vasospastic reactions are possible, therefore such concomitant use is contraindicated (see section 4.3).
The time interval that should be observed between taking sumatriptan and medicines containing ergotamine or other triptan/5-HT1 receptor agonists is unknown. It depends on the doses and types of medicines used. Since these effects may be potentiated by taking Stopmigren, a 24-hour interval should be observed between taking medicines containing ergotamine and other triptan/5-HT1 receptor agonists and the next dose of Stopmigren. Medicines containing ergotamine should not be used within 6 hours of taking Stopmigren, while medicines containing other triptan/5-HT1 receptor agonists should not be used within 24 hours of taking Stopmigren.
There have been isolated post-marketing reports of patients developing serotonin syndrome (including altered mental status, visceral instability, neuromuscular disorders) after taking selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. There have been reports of serotonin syndrome with the concomitant use of triptans and serotonin-norepinephrine reuptake inhibitors (SNRIs) (see section 4.4).
Application features
Stopmigren tablets are used only with a clearly established diagnosis of migraine.
Stopmigraine is not used to treat hemiplegic, basilar, and ophthalmoplegic migraine.
Before starting sumatriptan, the presence of another serious neurological pathology (e.g. stroke or transient ischemic attack) should be excluded if patients have atypical symptoms or do not have a diagnosis appropriate for sumatriptan.
The use of sumatriptan in some patients causes transient symptoms such as pain, tightness in the chest, which may be intense and extend to the larynx and pharynx (see section "Adverse reactions"). If such symptoms indicate ischemic heart disease, appropriate cardiac examination should be performed.
Sumatriptan should not be prescribed to patients with suspected heart disease without prior examination to detect cardiovascular pathology. Such patients include postmenopausal women, men over 40 years of age and patients with risk factors for coronary heart disease. However, such examination may not always detect the presence of heart disease, therefore, in rare cases, severe cardiac complications occur in patients with undiagnosed heart disease. Stopmigren should be prescribed with caution to patients under supervision for arterial hypertension, since a small number of patients may experience a transient increase in blood pressure and peripheral vascular resistance.
Isolated cases of serotonin syndrome (including altered mental status, visceral instability, neuromuscular disorders) have been described in patients after taking selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. There are reports of the development of serotonin syndrome with the simultaneous appointment of triptans and serotonin and noradrenaline reuptake inhibitors (SNRIs). If the simultaneous use of Stopmigren and SSRI/SNRI is clinically justified, it is advisable to conduct a preliminary examination of the patients (see section "Interaction with other medicinal products and other types of interactions"). It is not recommended to use sumatriptan simultaneously with any triptan/5HT1-agonist.
Stopmigren should be prescribed with caution to patients with significant impairment of drug absorption, metabolism, or excretion, such as renal or hepatic insufficiency (Child-Pugh A or B).
Stopmigren should be prescribed with caution to patients with a history of seizures or with risk factors that lower the seizure threshold.
Patients with hypersensitivity to sulfonamides may experience allergic reactions ranging from skin hypersensitivity to anaphylaxis after using Stopmigren. Cross-sensitivity is limited, but caution should be exercised when prescribing the drug to such patients.
The recommended doses of Stopmigren should not be exceeded.
Intensive treatment of acute migraine attacks is associated with exacerbation of headache (intensive treatment headache) in susceptible patients. Treatment may need to be discontinued.
Adverse reactions may occur more frequently when triptans are used concomitantly with herbal preparations containing St. John's wort (Hypericum perforatum).
Prolonged use of any type of painkiller may worsen headaches. If this occurs or is suspected, consult a doctor and discontinue treatment. Patients who experience frequent or daily headaches due to regular use of headache medications may be diagnosed with headache due to painkiller overuse.
The medicinal product contains lactose, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the medicinal product.
Due to the content of the medicinal product in the form of yellow FCF (E 110), allergic reactions are possible.
Ability to influence reaction speed when driving vehicles or other mechanisms
Drowsiness can be a consequence of both migraine and its treatment with Stopmigren, so you should avoid driving or operating other mechanisms.
Use during pregnancy or breastfeeding
The expected benefit to the woman and the risk to the fetus should be weighed.
Sumatriptan has been shown to be excreted in breast milk following subcutaneous administration. Exposure to the infant can be minimized by avoiding breastfeeding for 12 hours after administration of the drug.
Method of administration and doses
The recommended doses of Stopmigren should not be exceeded.
Stopmigraine is recommended to be used as early as possible after the onset of a migraine attack, although it is equally effective at each stage.
The recommended dose of Stopmigren for adults is 50 mg. In some cases, the dose can be increased to 100 mg.
If a dose of the medicine is ineffective, there is no need to take another dose during the same attack. The next dose of Stopmigren can be taken during subsequent attacks.
If the patient has responded to the first dose but symptoms recur, a second dose may be administered within the next 24 hours, with a minimum interval of 2 hours between doses. The total daily dose in any 24-hour period should not exceed 300 mg.
The tablets should be swallowed whole with water.
Elderly patients (over 65 years of age).
There is insufficient experience with sumatriptan in patients over 65 years of age. Although the pharmacokinetics of the drug do not differ from those in younger individuals, until additional clinical data are available, the use of Stopmigren in elderly patients is not recommended.
Children
Use is not recommended, as the efficacy and safety of sumatriptan for the treatment of children and adolescents have not yet been established.
Overdose
Doses exceeding 400 mg (oral) did not cause any side effects other than those listed below.
If overdose occurs, the patient should be observed for at least 10 hours and the usual supportive measures should be taken.
The effect of hemodialysis or peritoneal dialysis on the plasma levels of Stopmigren has not been established.
Adverse reactions
Nervous system: dizziness, drowsiness, sensory disturbances (including paresthesia and hypoesthesia); convulsions (although some of these cases were observed in patients with a history of convulsions or conditions that may lead to them; there are cases of convulsions in patients without any predisposition to them); tremor, dystonia, nystagmus, scotoma.
From the cardiovascular system: transient increase in blood pressure immediately after taking the drug, blood flow; bradycardia, tachycardia, palpitations, arrhythmia, transient ischemic changes on the ECG, coronary artery spasm, angina pectoris, myocardial infarction, hypotension, Raynaud's disease.
Respiratory system: shortness of breath.
On the part of the digestive system: nausea and vomiting, which occur in some patients, but their relationship with the use of Stopmigren has not been fully clarified; ischemic colitis, diarrhea.
Musculoskeletal and connective tissue disorders: feeling of heaviness, myalgia; neck stiffness, arthralgia.
The above symptoms are usually transient, can be intense, and affect any part of the body, including the chest and throat.
On the part of the immune system: hypersensitivity reactions - from skin hypersensitivity to cases of anaphylaxis.
On the part of the organs of vision: flickering in the eyes, diplopia, decreased visual acuity; loss of vision (usually transient). However, visual disturbances may be a consequence of the migraine attack itself.
General disorders: pain, sensations of heat or cold, tightness or tightness (usually transient, may be intense and affect any part of the body, including the chest and throat); feeling weak, tired (mostly mild or moderate and transient).
Laboratory data: minor changes in liver function tests were observed.
Mental disorders: agitation.
Skin and subcutaneous tissue disorders: hyperhidrosis.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
3 tablets in a blister; 1 blister in a pack.
Vacation category
According to the recipe.
Producer
JSC "KYIV VITAMIN FACTORY".
Location of the manufacturer and its business address
04073, Ukraine, Kyiv, Kopylivska St., 38.
