Sumamigren, 50 mg 2 pcs

Pharmacological action – serotoninergic, antimigraine.

Sumatriptan is a specific selective agonist of vascular 5-hydroxytryptamine-1 receptors (5HT_1D), does not affect other 5HT-serotonin receptor subtypes (5HT₂-5HT₇). The 5HT_1D receptors are located mainly in the blood vessels of the brain, and their stimulation results in the narrowing of these vessels. Decreases the sensitivity of the trigeminal nerve. Both of these effects may underlie the antimigraine action of sumatriptan. Clinical effect is usually noted 30 min after oral administration.

Pharmacokinetics

Sumatriptan is rapidly absorbed after oral administration, 70% of the C_max is reached in 45 min. After administration of 100 mg, the C_max in plasma averages 54 ng/mL. Bioavailability is 14% due to intense presystemic metabolism and incomplete absorption.

The binding to plasma proteins is low (14-21%). Sumatriptan is metabolized by MAO A. The main metabolite, the indole acetic analog of sumatriptan, is excreted mainly in the urine, as free acid and glucuronide conjugate. This metabolite has no activity toward 5NT₁– and 5NT₂-serotonin receptors. Migraine attacks do not appear to have a significant effect on the pharmacokinetics of sumatriptan taken orally.

Indications

Cutting migraine attacks with or without aura.

Active ingredient

Composition

How to take, the dosage

The tablets are taken orally with water.

The recommended single dose is 50 mg (1 tablet), in some cases a higher dose of 100 mg may be needed. If migraine symptoms do not disappear or diminish after the first dose, the drug should not be prescribed again to stop an ongoing attack. The drug can be used to control subsequent migraine attacks.

If symptoms decrease or disappear and then return, a second dose may be taken within the next 24 hours. The maximum dose of the drug is 300 mg for 24 hours.

Interaction

No drug interactions of sumatriptan with propranololol, flunarizine, pizotifen and ethanol have been noted.

Long-term vasospasm has been noted when concomitantly administered with ergotamine. Sumatriptan may not be administered earlier than 24 h after taking ergotamine-containing drugs, and ergotamine-containing drugs may not be administered earlier than 6 h after taking sumatriptan.

The concomitant use of sumatriptan and an MAOI inhibitor is contraindicated because of the possible interaction between the two.

There have been very rare reports from postmarketing surveillance of the development of serotonin syndrome (including mental disorders, autonomic lability, and neuromuscular disorders) as a result of concomitant use of SSRIs and sumatriptan. The development of serotonin syndrome has also been reported with concomitant administration of triptans with SSRIs.

Special Instructions

Sumatriptan should be prescribed only if the diagnosis of migraine is beyond doubt, and should be used as soon as possible after the onset of a migraine attack, although it is equally effective when used at any stage of the attack.

The drug should not be used prophylactically.

Sumatriptan should be used with caution in controlled arterial hypertension; conditions in which absorption, metabolism, or excretion of the drug may be altered (e.g., impaired renal or hepatic function).

There have been very rare reports from postmarketing surveillance of the development of serotonin syndrome (including mental disorders, autonomic lability, and neuromuscular disorders) as a result of concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. The development of serotonin syndrome has also been reported with concomitant administration of triptans with selective serotonin and norepinephrine reuptake inhibitors (SSRIs). In case of concomitant prescription with drugs from the group of SSRIs/ SSRIs, the patient’s condition should be closely monitored.

Sumatriptan should be used with caution in epilepsy and any condition with decreased seizure threshold.

The concomitant use of other triptans/5-HT1 agonists with sumatriptan is not recommended.

In patients with hypersensitivity to sulfonamides, the use of sumatriptan may cause allergic reactions, the severity of which ranges from skin manifestations to anaphylaxis. Data on cross-sensitivity are limited, but caution should be exercised when administering sumatriptan to such patients.

As with other antimigraine agents, other potentially serious neurologic conditions should be excluded when prescribing sumatriptan in patients with previously undiagnosed migraine or in patients with atypical migraine. It should be noted that patients with migraine have an increased risk of certain cerebrovascular complications (stroke or transient cerebrovascular impairment).

Sumatriptan should not be administered to patients with suspected heart disease without prior evaluation to rule out cardiovascular disease. These patients include postmenopausal women, men over 40 years of age and patients with risk factors for CHD. Although the examination does not always reveal cardiac disease in some patients, in very rare cases they develop cardiovascular side effects. After taking sumatriptan, transient intense pain and tightness in the chest, extending to the neck area, may occur. If there is reason to believe that these symptoms are a manifestation of CHD, an appropriate diagnostic evaluation should be performed.

Misuse of medications intended to control migraine attacks has been associated with increased headache in sensitive patients (drug abuse-related headache). In this case, withdrawal of the drug should be considered.

The recommended dose of sumatriptan should not be exceeded.

Impact on driving and operating machinery

Migraine patients may experience somnolence associated both with the disease itself and with taking sumatriptan, so they should be particularly careful when driving and operating moving machinery.

Contraindications

Side effects

Pain, fever, tingling, tightness or heaviness (usually transient, but can be intense and occur in different parts of the body, including the chest or throat); tingling, dizziness, weakness, fatigue, drowsiness (usually weak or moderate, transient) are also possible.

Cardiovascular system

BP decrease, bradycardia, tachycardia, transient BP increase, rarely – arrhythmia, transient ECG changes of ischemic type, coronary artery spasm, myocardial infarction, in single cases – Raynaud’s syndrome.

Digestive system

Nausea, vomiting, ischemic colitis (the relationship of these phenomena to sumatriptan intake is not precisely defined); feeling of discomfort in the stomach, dysphagia, increased liver transaminases activity.

CNS disorders

Dizziness; rarely – seizures (in some cases observed in patients with a history of seizures or in conditions predisposing to the development of seizures); sometimes – diplopia, scotoma, nystagmus, decreased visual acuity; extremely rare – partial transient loss of vision (note that visual disturbances may be associated with a migraine attack).

Allergic reactions

Rash, pruritus, erythema, urticaria; in single cases – anaphylactic reactions.

Overdose

In case of overdose, the patient should be observed for 10 h, providing symptomatic therapy as required.

There are no data on the effect of hemodialysis or peritoneal dialysis on the plasma concentration of sumatriptan.

Pregnancy use

The use of sumatriptan is contraindicated in pregnancy. Breast-feeding should be stopped during the treatment. If the drug is taken, breastfeeding is possible not earlier than 24 hours later.

Pediatric use

Contraindication: patients under 18 years of age.

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