Stopmigren
Ukraine
Table of Contents
INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT SТОPМIGREN (STOPMIGREN)
Composition:
Active substance: sumatriptan;
50 mg tablets: 1 tablet contains 70 mg of sumatriptan succinate, equivalent to 50 mg of sumatriptan;
Excipients: lactose monohydrate; magnesium stearate; sodium croscarmellose; microcrystalline cellulose; talc; colloidal anhydrous silicon dioxide;
coating: Opadry II Pink film-coating mixture (aluminum lakes of brilliant red (E 129) and indigo carmine (E 132); hypromellose; lactose monohydrate; triacetin; polyethylene glycol; titanium dioxide (E 171));
100 mg tablets: 1 tablet contains 140 mg of sumatriptan succinate, equivalent to 100 mg of sumatriptan;
Excipients: lactose monohydrate; magnesium stearate; sodium croscarmellose; microcrystalline cellulose; talc; colloidal anhydrous silicon dioxide;
coating: Opadry II Orange film-coating mixture (aluminum lakes of yellow FCF (E 110) and indigo carmine (E 132); hypromellose; lactose monohydrate; triacetin; polyethylene glycol; yellow iron oxide (E 172); titanium dioxide (E 171)).
Pharmaceutical form. Film-coated tablets.
Main physicochemical properties:
50 mg tablets: round, biconvex tablets, film-coated, pink in color;
100 mg tablets: round, biconvex tablets, film-coated, orange in color.
Pharmacotherapeutic group. Medicinal products used for migraine treatment. Selective 5-HT1 serotonin receptor agonist. Sumatriptan. ATC code N02C C01.
Pharmacological Properties
Pharmacodynamics
Sumatriptan is a selective 5HT1D receptor agonist that does not affect other 5HT receptors. These receptors are primarily located in cerebral blood vessels. Experimental studies have demonstrated that sumatriptan exerts a selective vasoconstrictor effect on vessels within the carotid arterial system without affecting cerebral blood flow. The carotid arterial system supplies blood to extracranial and intracranial tissues, such as the meninges. Dilation of these vessels is associated with the development of migraine. Additionally, experimental data have shown that sumatriptan inhibits the activity of the trigeminal nerve. These two mechanisms are considered responsible for the antimigraine activity of sumatriptan.
Clinical effect is observed within 30 minutes after oral administration of 100 mg of the drug.
Pharmacokinetics
After oral administration, sumatriptan is rapidly absorbed, reaching 70% of its maximum concentration within 45 minutes. Following a 100 mg dose, the mean peak plasma concentration is 45 ng/mL. The bioavailability after oral administration is 14%, partly due to presystemic metabolism and partly due to incomplete absorption. Plasma protein binding is low (14–21%), and the mean volume of distribution is 17 L. Mean total plasma clearance is approximately 1160 mL/min, and mean renal clearance is approximately 260 mL/min. Non-renal clearance accounts for approximately 80% of total clearance, indicating that sumatriptan is primarily eliminated in the form of metabolites. The main metabolite, an indole acetic acid analogue of sumatriptan, is excreted in urine as free acid and as glucuronide conjugate. This metabolite lacks 5HT1 and 5HT2 activity. Other metabolites have not been identified. The pharmacokinetics of oral sumatriptan are not significantly altered during a migraine attack.
Clinical characteristics.
Indications.
Stopmigren tablets are indicated for the rapid relief of migraine attacks, with or without aura.
Contraindications.
- Hypersensitivity to any component of the medicinal product.
- Myocardial infarction in medical history, ischemic heart disease, Prinzmetal's angina, peripheral vascular disease, or symptoms characteristic of ischemic heart disease.
- Stroke or transient ischemic attack (TIA) in medical history.
- Moderate or severe arterial hypertension, and mild uncontrolled arterial hypertension.
- Severe hepatic impairment.
- Concomitant use of ergotamine or its derivatives (including methysergide) (see section "Interaction with other medicinal products and other forms of interaction").
- Concomitant use of any agonist of triptan/5-hydroxytryptamine receptors (5-HT1) (see section "Interaction with other medicinal products and other forms of interaction").
- Concurrent administration of monoamine oxidase inhibitors (MAOIs) and Stopmigren. Stopmigren must not be used within 2 weeks of discontinuing MAOIs.
Interaction with other medicinal products and other forms of interaction.
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. Prolonged vasospastic reactions are theoretically possible; therefore, such concomitant use is contraindicated (see section "Contraindications").
The required time interval between administration of sumatriptan and medicinal products containing ergotamine or other triptan/5-HT1-receptor agonists is unknown. This depends on the doses and types of medicinal products used. Since these effects may be potentiated by taking Stopmigren, a 24-hour interval should be maintained between taking products containing ergotamine or other triptan/5-HT1-receptor agonists and the next dose of Stopmigren. Medicinal products containing ergotamine must not be used within 6 hours after taking Stopmigren, whereas products containing other triptan/5-HT1-receptor agonists must not be used within 24 hours after taking Stopmigren.
An interaction may occur between sumatriptan and MAO inhibitors; therefore, their concomitant use is contraindicated (see section "Contraindications").
There have been isolated post-marketing reports of serotonin syndrome (including altered mental status, autonomic instability, and neuromuscular abnormalities) in patients taking selective serotonin reuptake inhibitors (SSRIs) together with sumatriptan. Cases of serotonin syndrome have also been reported with concomitant use of triptans and serotonin-norepinephrine reuptake inhibitors (SNRIs) (see section "Special warnings and precautions for use").
Special precautions for use
Stopmigraine tablets should be used only when migraine has been clearly diagnosed.
Stopmigraine is not indicated for the treatment of hemiplegic, basilar, or ophthalmoplegic migraine.
Before initiating sumatriptan therapy, the presence of other serious neurological disorders (e.g., stroke or transient ischemic attack) should be ruled out in patients who present with atypical symptoms or who do not have a confirmed diagnosis appropriate for sumatriptan use.
Sumatriptan use may cause transient symptoms such as pain or a sensation of chest tightness in some patients, which may be intense and radiate to the throat and pharynx (see section "Adverse reactions"). If such symptoms suggest ischemic heart disease, appropriate cardiological evaluation should be performed.
Sumatriptan must not be administered to patients with suspected cardiovascular disease without prior evaluation for cardiac and vascular pathology. This includes postmenopausal women, men over 40 years of age, and patients with risk factors for ischemic heart disease. However, such evaluation does not always detect underlying heart disease, and severe cardiovascular complications have been reported in isolated cases in patients with undiagnosed cardiac conditions. Stopmigraine should be used with caution in patients under medical supervision for arterial hypertension, as transient increases in blood pressure and peripheral vascular resistance may occur in a small number of patients.
Isolated cases of serotonin syndrome (including altered mental status, autonomic instability, and neuromuscular abnormalities) have been reported in patients taking selective serotonin reuptake inhibitors (SSRIs) together with sumatriptan. There have also been reports of serotonin syndrome developing with concomitant use of triptans and serotonin-norepinephrine reuptake inhibitors (SNRIs). If concomitant use of Stopmigraine and SSRIs/SNRIs is clinically justified, preliminary patient evaluation is advisable (see section "Interaction with other medicinal products and other forms of interaction"). Concomitant use of sumatriptan with any other triptan or 5-HT1 agonist is not recommended.
Stopmigraine should be administered with caution to patients with significant impairment in drug absorption, metabolism, or excretion, such as those with renal or hepatic impairment (Child–Pugh class A or B).
Stopmigraine should be used with caution in patients with a history of seizures or with risk factors that lower the seizure threshold.
Allergic reactions ranging from skin hypersensitivity to anaphylaxis may occur in patients hypersensitive to sulfonamides after administration of Stopmigraine. Cross-sensitivity is limited, but caution should be exercised when prescribing the drug to such patients.
The recommended doses of Stopmigraine must not be exceeded.
Frequent treatment of acute migraine attacks may be associated with worsening of headache (medication-overuse headache) in susceptible individuals. Discontinuation of treatment may become necessary.
Adverse reactions may occur more frequently when triptans are used concomitantly with herbal products containing St. John's wort (Hypericum perforatum).
Prolonged use of any type of analgesic may exacerbate headache. If such a situation occurs or is imminent, medical advice should be sought and treatment discontinued. Patients who experience frequent or daily headaches due to regular use of headache medications may be diagnosed with medication-overuse headache.
The medicinal product contains lactose; therefore, patients with rare hereditary forms of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption should not take this medicine.
Due to the presence of yellow sunset FCF (E 110) in the formulation, allergic reactions are possible.
Use during pregnancy or breastfeeding
The potential benefit to the mother and the potential risk to the fetus should be carefully weighed.
After subcutaneous administration, sumatriptan has been shown to be excreted in breast milk. Infant exposure can be minimized by avoiding breastfeeding for 12 hours after drug administration.
Effect on ability to drive or operate machinery
Somnolence may result either from migraine itself or from its treatment with Stopmigraine. Therefore, driving or operating machinery should be avoided.
Method of administration and dosage.
Stopmigraine tablets must not be used for migraine attack prevention.
Recommended doses of Stopmigraine must not be exceeded.
Stopmigraine should be used as early as possible after the onset of a migraine attack, although it is equally effective at any stage.
The recommended dose of Stopmigraine for adults is 50 mg. In individual cases, the dose may be increased to 100 mg.
If the administered dose proves ineffective, another dose should not be taken during the same attack. The next dose of Stopmigraine may be taken during subsequent attacks.
If the patient responded to the first dose but symptoms recur, a second dose may be administered within the following 24 hours; the minimum interval between doses must be at least 2 hours. The total daily dose within any 24-hour period must not exceed 300 mg.
Tablets should be swallowed whole with water.
Elderly patients (over 65 years of age).
There is insufficient experience with the use of sumatriptan for the treatment of patients aged 65 years and older. Although the pharmacokinetics of the drug do not differ from those in younger individuals, until additional clinical data are obtained, the use of Stopmigraine in elderly patients is not recommended.
Children. Not recommended for use, as the efficacy and safety of sumatriptan for the treatment of children and adolescents have not been established to date.
Overdose.
Doses exceeding 400 mg (orally) have not caused any adverse effects other than those listed below.
In case of overdose, the patient should be observed for at least 10 hours, and standard supportive measures should be applied.
The effect of hemodialysis or peritoneal dialysis on plasma levels of Stopmigraine has not been established.
Adverse reactions.
Central and peripheral nervous system: dizziness, somnolence, sensory disturbances (including paraesthesia and hypaesthesia); seizures (although some of these cases occurred in patients with a history of seizures or conditions that may lead to seizures; there have been cases of seizures developing in patients without any predisposition to them); tremor, dystonia, nystagmus, scotoma.
Cardiovascular system: transient increase in blood pressure immediately after taking the medication, flushing; bradycardia, tachycardia, palpitations, arrhythmia, transient ischemic changes on ECG, coronary artery spasm, angina pectoris, myocardial infarction, hypotension, Raynaud's disease.
Respiratory system: dyspnea.
Gastrointestinal system: nausea and vomiting occurring in some patients, although their relationship to the use of Stopmigren is not fully established; ischemic colitis, diarrhea; dysphagia (frequency unknown).
Musculoskeletal and connective tissue disorders: sensation of heaviness, myalgia; neck muscle rigidity, arthralgia.
The above symptoms are usually transient, may be intense in nature, and may affect any part of the body, including the chest and throat.
Immune system: hypersensitivity reactions – from skin hypersensitivity to cases of anaphylaxis.
Eye disorders: visual flickering, diplopia, decreased visual acuity; vision loss (usually transient). However, visual disturbances may also be caused by the migraine attack itself.
General disorders: pain, sensation of warmth or cold, tightness or pressure (usually transient, may be intense, and may affect any part of the body, including the chest and throat); feeling of weakness, fatigue (mainly mild or moderate in severity and transient).
Cases of increased pain following trauma and increased pain during inflammation have been reported – frequency unknown.
Laboratory findings: minor changes in liver function tests have been observed.
Psychiatric disorders: excitement.
Skin and subcutaneous tissue disorders: hyperhidrosis.
Shelf life. 3 years.
Storage conditions.
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging.
Tablets 50 mg: 6 tablets in a blister; 1 blister per carton.
Tablets 100 mg: 3 tablets in a blister; 1 blister per carton.
Prescription status. Prescription only.
Manufacturer. JSC "KYIV VITAMIN PLANT".
Manufacturer's address and location of business activity.
38 Kopilivska Street, Kyiv, 04073, Ukraine.
Web-site: www.vitamin.com.ua.