Antimigren-zdorovya
Ukraine
Table of Contents
INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT ANTIMIGREN-ZDOROVYE (ANTIMIGREN-ZDOROVYE)
Composition:
Active substance: sumatriptan;
One tablet contains 50 mg or 100 mg of sumatriptan;
Excipients: lactose monohydrate; povidone; microcrystalline cellulose; calcium stearate; sodium croscarmellose; colloidal anhydrous silicon dioxide; titanium dioxide (E 171); hypromellose.
Dosage form. Film-coated tablets.
Main physicochemical properties: film-coated tablets of white color with a yellowish tint.
Pharmacotherapeutic group. Medicinal products used for the treatment of migraine. Selective 5-HT1 serotonin receptor agonists. Sumatriptan. ATC code N02C C01.
Pharmacological properties.
Pharmacodynamics.
Sumatriptan is a selective 5HT1-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 vasoconstrictive 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 involved in 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 effects are 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 oral bioavailability 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. The mean total plasma clearance is approximately 1160 mL/min, and the 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 a glucuronide conjugate. This metabolite lacks 5HT1- and 5HT2-receptor activity. Other metabolites have not been identified. The pharmacokinetics of oral sumatriptan are not significantly altered during a migraine attack.
Clinical characteristics.
Indications.
Antimigren-Zdorovya tablets are indicated for the rapid relief of migraine attacks, with or without aura. Antimigren-Zdorovya tablets should be used only when migraine has been clearly diagnosed.
Contraindications.
Hypersensitivity to any component of the medicinal product.
History of myocardial infarction, 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 types of interactions").
Concomitant use of any triptan/5-hydroxytryptamine receptor agonist (5-HT1) (see section "Interaction with other medicinal products and other types of interactions").
Concomitant use of monoamine oxidase inhibitors (MAOIs) and Antimigren-Zdorovya. Antimigren-Zdorovya should not be administered within 2 weeks after discontinuation of MAO inhibitors.
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. 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 interval depends on the doses and type of medicinal products used. Since these effects may be potentiated by sumatriptan, a 24-hour interval should be observed between administration of ergotamine-containing products and other triptan/5-HT1-receptor agonists, and administration of sumatriptan. Accordingly, medicinal products containing ergotamine or other triptan/5-HT1-receptor agonists should not be used within 6 hours after sumatriptan administration.
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 receiving selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Cases of serotonin syndrome have also been reported with concomitant use of triptans and serotonin-norepinephrine reuptake inhibitors (SNRIs) (see section "Special precautions for use").
Special precautions for use.
Antimigren-Zdorovya tablets are used only when migraine has been clearly diagnosed.
Antimigren-Zdorovya is not used for the treatment of hemiplegic, basilar, or ophthalmoplegic migraine.
Before initiating treatment with sumatriptan, serious neurological disorders (e.g., stroke, transient ischemic attack) should be ruled out, especially if the patient presents with atypical symptoms or if the diagnosis of migraine has not been established.
Administration of sumatriptan in some patients may cause transient symptoms such as pain and sensations of pressure or tightness in the chest, which may be intense and radiate to the throat (see section "Adverse reactions"). If such symptoms suggest ischemic heart disease, appropriate cardiological evaluation should be performed.
Sumatriptan must not be prescribed to patients suspected of having cardiovascular disease without prior evaluation for cardiovascular pathology. This group includes postmenopausal women, men aged 40 years and older, and patients with risk factors for ischemic heart disease. However, such evaluation does not always detect underlying heart disease, and in rare cases, severe cardiovascular complications have occurred in patients with undiagnosed heart disease. Antimigren-Zdorovya should be prescribed with caution to patients under monitoring 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 receiving selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Cases of serotonin syndrome have also been reported with concomitant use of triptans and serotonin-norepinephrine reuptake inhibitors (SNRIs). If concomitant use of Antimigren-Zdorovya and SSRIs/SNRIs is clinically justified, prior patient evaluation is recommended (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.
Antimigren-Zdorovya should be used with caution in patients with significant impairment in drug absorption, metabolism, or elimination, such as in renal or hepatic impairment (Child–Pugh class A or B).
Antimigren-Zdorovya should be prescribed with caution to patients with a history of seizures or risk factors that lower the seizure threshold.
Allergic reactions may occur in patients hypersensitive to sulfonamides after administration of Antimigren-Zdorovya. Reactions may range from skin hypersensitivity to anaphylaxis. Cross-sensitivity is limited, but caution should be exercised when prescribing the drug to such patients.
Recommended doses of Antimigren-Zdorovya must not be exceeded.
Frequent or intensive treatment of acute migraine attacks may lead to worsening of headache (medication-overuse headache) in susceptible patients. Discontinuation of treatment may become necessary.
Adverse reactions may occur more frequently during concomitant use of triptans and 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 suspected, 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 product contains lactose; therefore, if the patient has known intolerance to certain sugars, medical advice should be sought before taking this medicinal product.
Use during pregnancy or breastfeeding.
Pregnancy
Post-marketing data are available from over 1000 women who used sumatriptan during the first trimester of pregnancy. Although these data are insufficient to draw definitive conclusions, they do not indicate an increased risk of congenital malformations. Experience with sumatriptan use during the second and third trimesters is limited.
In animal studies, no direct teratogenic or adverse effects on perinatal and postnatal development were observed; however, data indicate impaired embryo-fetal viability in rabbits.
Sumatriptan should be used only if the expected benefit to the mother outweighs any potential risk to the fetus.
Breastfeeding
Sumatriptan is excreted in breast milk, with a mean relative infant dose of < 4% after a single dose of sumatriptan. The effect on the breastfed infant can be minimized by withholding breastfeeding for 12 hours after drug administration. Breast milk expressed during this period should be discarded.
Cases of breast pain and/or nipple pain have been reported after sumatriptan use in breastfeeding women (see section "Adverse reactions"). The pain is usually transient and resolves within 3–12 hours.
Effects on ability to drive and use machines.
Somnolence may result from both migraine itself and its treatment with Antimigren-Zdorovya; therefore, driving or operating machinery should be avoided.
Method of Administration and Dosage
Antimigren-Zdorovya tablets must not be used for the prevention of migraine attacks.
The recommended doses of Antimigren-Zdorovya must not be exceeded.
Antimigren-Zdorovya should be taken as early as possible after the onset of a migraine attack, although it remains equally effective at any stage.
The recommended dose of Antimigren-Zdorovya for adults is 50 mg. In individual cases, the dose may be increased to 100 mg.
If the administered dose proves ineffective, a second dose must not be taken during the same attack. In such cases, paracetamol, acetylsalicylic acid, or other nonsteroidal anti-inflammatory drugs may be used. The next dose of Antimigren-Zdorovya may be taken during subsequent attacks.
If the patient responds to the first dose but symptoms recur, a second dose may be administered within the following 24 hours, with a minimum interval of 2 hours between doses. The total daily dose within any 24-hour period must not exceed 300 mg.
Antimigren-Zdorovya is indicated as monotherapy for the rapid relief of migraine attacks and must not be used concomitantly with ergotamine or its derivatives (including methysergide) (see section "Contraindications").
Tablets should be swallowed whole with water.
Geriatric patients (over 65 years of age)
Experience with the use of sumatriptan in patients aged 65 years and older is limited. Although the pharmacokinetics of the drug do not differ significantly from those in younger individuals, until additional clinical data become available, the use of Antimigren-Zdorovya 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 been established.
Overdose.
Doses exceeding 400 mg (oral) have not resulted in adverse reactions 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 Antimigren-Zdorovya has not been established.
Adverse reactions.
Nervous system disorders: dizziness, somnolence, sensory disturbances including paraesthesia and hypoaesthesia; 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); tremor, dystonia, nystagmus, scotoma.
Cardiovascular system disorders: 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 phenomenon.
Respiratory system disorders: dyspnea.
Gastrointestinal disorders: nausea and vomiting occurring in some patients, although the association with the use of the drug has not been fully established; ischemic colitis, diarrhea, dysphagia.
Musculoskeletal and connective tissue disorders: sensation of heaviness, myalgia (these symptoms are usually transient, may be intense, and may affect any part of the body, including the chest and throat), neck muscle rigidity, arthralgia.
Reproductive system and breast disorders: breast pain – reported with "rare" frequency.
General disorders: pain, increased pain following trauma, increased pain during inflammation, sensation of warmth or cold, tightness or pressure (these symptoms are usually transient, may be intense, and may affect any part of the body, including the chest and throat), feeling of weakness, fatigue (these symptoms are mainly mild or moderate in severity and are transient).
Laboratory findings: minor changes in liver function tests have been observed.
Immune system disorders: hypersensitivity reactions – ranging from skin hypersensitivity to cases of anaphylaxis.
Eye disorders: flickering, diplopia, decreased visual acuity, vision loss (usually transient). However, visual disturbances may be a consequence of the migraine attack itself.
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: 1 tablet, 1×3, or 3 tablets in a blister pack in a carton.
Prescription status. Prescription only.
Manufacturer.
LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".
LIMITED LIABILITY COMPANY "FARMEKS GROUP".
Manufacturer's location and address of business activity.
Ukraine, 61013, Kharkiv region, Kharkiv, Shevchenka Street, 22.
(LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA")
Ukraine, 08301, Kyiv region, Boryspil, Shevchenka Street, 100.
(Limited liability company "Farmeks Group")
Date of last review.