Sumamigran (Sumatriptan), 100 mg, 2 pcs.

Pharmacological action - serotonergic, anti-migraine.

Sumatriptan is a specific selective agonist of vascular 5-hydroxytryptamine-1 receptors (5HT _1D ), does not affect other subtypes of 5HT-serotonin receptors (5HT ₂ –5HT ₇ ).

5HT _1D receptors are located mainly in the blood vessels of the brain, and their stimulation leads to a narrowing of these vessels. Reduces the sensitivity of the trigeminal nerve. Both of these effects may underlie the anti-migraine action of sumatriptan. The clinical effect is usually observed 30 minutes after ingestion of the drug.

Pharmacokinetics

After oral administration, sumatriptan is rapidly absorbed, 70% of C _{max is} reached after 45 minutes. After taking 100 mg C _max in plasma is an average of 54 ng / ml. Bioavailability is 14% due to intensive presystemic metabolism and incomplete absorption. Plasma protein binding is small (14–21%).

Sumatriptan is metabolized under the influence of MAO A. The main metabolite, the indole-acetic analog of sumatriptan, is excreted mainly in urine, in the form of a free acid and glucuronide conjugate. This metabolite is not active against 5HT ₁ and 5HT ₂ serotonin receptors. Migraine attacks do not seem to have a significant effect on the pharmacokinetics of sumatriptan taken orally.

Relieving migraine attacks with or without aura.

The use of sumatriptan is contraindicated in pregnancy. At the time of treatment should stop breastfeeding. In the case of taking the drug, breastfeeding is possible no earlier than 24 hours later.

Use in children

Contraindication: age of patients is up to 18 years.

• individual hypersensitivity to any component of Sumumigraine;
• hemiplegic, basilar and ophthalmoplegic form of migraine;
• IHD (including myocardial infarction, post-infarction cardiosclerosis, Prinzmetal angina), as well as the presence of symptoms suggesting the presence of IHD;
• peripheral vascular occlusion diseases;
• stroke or transient ischemic attack (including history);
• uncontrolled arterial hypertension;
• concomitant use with ergotamine or its derivatives (including metisegrid);
• use against the background of taking MAO inhibitors or earlier than 2 weeks after their cancellation;
• severe impaired liver and / or kidney function;
• age up to 18 years and older than 65 years (safety and efficacy not established);
• pregnancy and lactation.

From the body as a whole

Pain, sensations of heat, tingling, feeling of constriction or heaviness (usually transient, but can be intense and occur in various parts of the body, including in the chest or throat); hot flashes are also possible, Dizziness, a feeling of weakness, a feeling of tiredness, drowsiness (usually mild or moderate, are transient).
    
From the cardiovascular system

Decrease in blood pressure, bradycardia, tachycardia, transient increase in blood pressure; rarely - rhythm disturbances, transient ECG changes of the ischemic type, spasm of the coronary arteries, myocardial infarction; in isolated cases - Raynaud's syndrome.
    
From the digestive system

Nausea, vomiting, ischemic colitis (the relationship of these phenomena with the administration of sumatriptan is not precisely established); discomfort in the abdomen, Dysphagia, increased activity of hepatic transaminases.
    
Central nervous system

dizziness; rarely, bouts of seizures (in some cases, have been 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 rarely - partial transient loss of vision (it should be borne in mind that visual impairment can be associated with a migraine attack).
    
Allergic reactions

Rash, itching, erythema, urticaria; in isolated cases - anaphylactic reactions.

No drug interaction of sumatriptan with propranolol, flunarizine, pisotifen and ethanol was noted.

There was a prolonged spasm of blood vessels while taking ergotamine. Sumatriptan can be prescribed no earlier than 24 hours after taking drugs containing ergotamine, and drugs containing ergotamine can be prescribed no earlier than 6 hours after taking sumatriptan.

The simultaneous use of sumatriptan and an MAO inhibitor is contraindicated, because interaction between them is possible.

There are very rare reports, obtained as a result of post-marketing observation, about the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) as a result of the concomitant use of SSRIs and sumatriptan. It was also reported on the development of serotonin syndrome against the background of the simultaneous administration of triptans with SSRIs.

The tablets are taken orally as a whole, washed down with water.

The recommended single dose is 50 mg (1 tab.), In some cases, it may be necessary to use the drug in a higher dose of 100 mg. If the symptoms of migraine do not disappear and do not decrease after taking the first dose, then the drug should not be prescribed again to stop the ongoing attack. The drug can be used to stop subsequent migraine attacks.

If the symptoms have decreased or disappeared, and then resumed, you can take a second dose over the next 24 hours. The maximum dose of the drug is 300 mg for 24 hours.

In case of overdose, the patient should be observed for 10 hours, conducting symptomatic therapy as necessary.

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

Sumatriptan should be prescribed only if the diagnosis of migraine is not in doubt, and it 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 can not be used for preventive purposes.

Sumatriptan should be taken with caution in case of controlled hypertension; diseases in which absorption, metabolism, or excretion of the drug may change (for example, impaired renal or hepatic function).

There are very rare reports from post-marketing observation about the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) resulting from the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. It was also reported on the development of serotonin syndrome against the background of the simultaneous administration of triptans with selective serotonin and noradrenaline reuptake inhibitors (SSRIs). In the case of simultaneous administration with drugs from the SSRI / SSRI group, the patient's condition should be carefully monitored.

Sumatriptan should be taken with caution in epilepsy and any condition with a lower threshold for convulsive readiness.

Concomitant use of other tryptans / 5-HT1 agonists with sumatriptan is not recommended.

In patients with hypersensitivity to sulfonamides, the use of sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis. Data on cross sensitivity is limited, but caution should be exercised when prescribing sumatriptan to such patients.

As with other anti-migraine agents, when prescribing sumatriptan in patients with previously undiagnosed migraine or in patients with atypical migraine, it is necessary to exclude other potentially serious neurological conditions. It should be noted that patients with migraine have an increased risk of developing certain cerebrovascular complications (stroke or transient cerebrovascular accident).

Sumatriptan should not be prescribed to patients with suspected heart disease without a preliminary examination in order to exclude cardiovascular pathology. These patients include postmenopausal women, men over the age of 40, and patients with risk factors for developing CHD. Although the examination does not always allow the detection of heart disease in some patients, in very rare cases they develop side effects from the cardiovascular system. After taking sumatriptan, transient intense pain and chest tightness may occur, extending to the neck. If there is reason to believe that these symptoms are a manifestation of coronary artery disease, it is necessary to conduct an appropriate diagnostic examination.

The abuse of drugs intended to relieve migraine attacks is associated with increased headaches in sensitive patients (headache associated with drug abuse). In this case, consider discontinuing the drug.

Do not exceed the recommended dose of sumatriptan.

Influence on the ability to drive vehicles and control mechanisms

Patients with migraine may experience drowsiness associated with both the disease itself and the administration of sumatriptan, so they should be especially careful when driving and working with moving machinery.

Sumamigraine. Film-coated tablets.