Sumatriptan-Alium, 50 mg 2 pcs

Pharmacological group: Antimigraine agent.

TAC code: N02CC01.

Pharmacological properties

Pharmacodynamics
Sumatriptan is a specific selective agonist of vascular 5-hydroxytryptamine-1 -receptors (5NT1D), does not affect other 5NT-serotonin receptor subtypes (5NT2 to 5NT7).

The 5NT1D receptors are located mainly in the blood vessels of the brain, and their stimulation leads to narrowing of these vessels. It reduces the sensitivity of the trigeminal nerve. Both of these effects may underlie the antimigraine action of sumatriptan. Clinical effects are usually noted 30 minutes after oral administration of the drug.

Pharmacokinetics
After oral administration, sumatriptan is rapidly absorbed, with 70% of maximum plasma concentration reached after 45 minutes. After administration of 100 mg, maximum plasma concentration averages 54 mg/ml. Bioavailability is 14 % due to intensive presystemic metabolism and incomplete absorption. Binding to plasma proteins is low (14-21%).

Sumatriptan is metabolized by monoamine oxidase 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 towards 5HT1 – and 5HT2 – serotonin receptors.

Indications

Relief of migraine attacks (with or without aura).

Pharmacological effect

Pharmacological group: Antimigraine drug.

ATX code: N02CC01.

PHARMACOLOGICAL PROPERTIES

Pharmacodynamics
Sumatriptan is a specific selective agonist of vascular 5-hydroxytryptamine-1 receptors (5HT1D), does not affect other subtypes of 5HT-serotonin receptors (5HT2 – 5HT7).

5HT1D receptors are located primarily in the blood vessels of the brain, and their stimulation causes these vessels to constrict. Reduces the sensitivity of the trigeminal nerve. Both of these effects may underlie the antimigraine action of sumatriptan. The clinical effect is usually observed 30 minutes after oral administration of the drug.

Pharmacokinetics
After oral administration, sumatriptan is rapidly absorbed, 70% of the maximum plasma concentration is achieved after 45 minutes. After taking 100 mg, the maximum plasma concentration averages 54 mg/ml. Bioavailability is 14% due to intensive first-pass metabolism and incomplete absorption. Communication with plasma proteins is low (14-21%).

Sumatriptan is metabolized by monoamine oxidase A. The main metabolite, the indoleacetic analogue of sumatriptan, is excreted primarily in the urine, in the form of a free acid and a glucuronide conjugate. This metabolite has no activity towards 5HT1 and 5HT2 serotonin receptors.

Special instructions

Sumatriptan is not intended for the prevention of migraine.

Sumatriptan should only be taken if the diagnosis of migraine is certain.

Sumatriptan should be used as soon as possible after the onset of a migraine attack, but the drug is equally effective at any stage of the attack. If there is no effect from the first dose, the diagnosis should be clarified.

Patients at risk for the cardiovascular system should not begin therapy without prior examination (postmenopausal women, men over 40 years of age, persons with risk factors for coronary artery disease).

Before prescribing sumatriptan to patients with newly diagnosed or atypical migraine, other potentially dangerous neurological diseases should be excluded.

Chest pain and tightness may occur after taking sumatriptan. The pain can be intense and radiate 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 examination.

Impact on the ability to drive vehicles and control equipment

With migraine, as well as during therapy with sumatriptan, drowsiness may develop. Therefore, during the period of use of sumatriptan, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Sumatriptan

Composition

Each film-coated tablet contains sumatriptan succinate 70 mg or 140 mg (in terms of sumatriptan 50 mg and 100 mg).
Excipients: lactose (milk sugar), calcium hydrogen phosphate (dibasic calcium phosphate), magnesium stearate, povidone.
Excipients for the coating: hypromellose (hydroxypropyl methylcellulose), copovidone (copolyvidone), polyethylene glycol 6000 (macrogol), talc, titanium dioxide, crimson dye [Ponceau 4R].

Contraindications

Hypersensitivity to any component of the drug.
Hemiplegic, basilar and ophthalmoplegic forms of migraine.
Coronary heart disease (CHD) (including myocardial infarction, post-infarction cardiosclerosis, Prinzmetal’s angina), as well as the presence of symptoms suggesting the presence of CHD.
Occlusive diseases of peripheral vessels.
Stroke or transient ischemic attack (including history).
Uncontrolled arterial hypertension.
Taken simultaneously with ergotamine or its derivatives (including methysergide).
Use of monoamine oxidase inhibitors (MAOIs) or earlier than 2 weeks after discontinuation of these drugs.
Severe dysfunction of the liver and/or kidneys.
Ages under 18 years and over 65 years (the safety and effectiveness of sumatriptan have not been established).
Pregnancy and lactation period.

With caution:

controlled arterial hypertension;
diseases that may alter the absorption, metabolism, or elimination of this drug (for example, impaired renal or hepatic function);
epilepsy (including any conditions with a decrease in the seizure threshold);
in patients with hypersensitivity to sulfonamides (administration of sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis. Data on cross-sensitivity are limited, but caution should be exercised when prescribing sumatriptan to such patients).

Side Effects

The incidence of side effects is classified according to the recommendations of the World Health Organization: very often – at least 10%; often – at least 1%, but less than 10%; infrequently – not less than 0.1%, but less than 1%; rarely – not less than 0.01%, but less than 0.1%; very rarely – less than 0.01% (including isolated cases).

From the cardiovascular system: very rarely – bradycardia, tachycardia, arrhythmia, transient increase in blood pressure (BP) (immediately after the start of treatment), transient signs of myocardial ischemia on the electrocardiogram, spasm of the coronary vessels, myocardial infarction, Raynaud’s syndrome, decrease in blood pressure, “flushes” of blood to the face.

From the respiratory system: often – shortness of breath, transient irritation of the mucous membrane or a burning sensation in the nasal cavity or throat.

From the digestive system: often – nausea, vomiting; a slight increase in the activity of liver enzymes; very rarely – ischemic colitis, diarrhea, discomfort in the abdominal area.

From the nervous system: often – dizziness, drowsiness, sensory disturbances, including paresthesia, hypoesthesia; very rarely – convulsions (usually with a history of convulsions); unknown frequency – tremor, dystonia, anxiety.

On the part of the organ of vision: infrequently – diplopia, flashing “spots” before the eyes, nystagmus, scotoma, decreased visual acuity; very rarely – partial transient loss of vision (it should be borne in mind that visual impairment may be associated with the migraine attack itself).

From the musculoskeletal system: often – myalgia; unknown frequency – stiff neck, arthralgia.

Allergic reactions: very rarely – skin rash, urticaria, itching, erythema, anaphylaxis.

Other: often – pain, tingling, feeling of heat, feeling of weakness and/or fatigue, nosebleeds, feeling of tightness or heaviness (these symptoms are usually transient, but can be intense and occur in any part of the body, including the chest and neck); unknown frequency – increased sweating.

Interaction

Prolonged vascular spasm is possible when administered simultaneously with ergotamine and ergotamine-containing drugs.

It is possible that the rate of metabolism of sumatriptan may decrease and its concentration may increase due to the interaction between sumatriptan and MAO inhibitors.

With the simultaneous use of sumatriptan and drugs from the group of selective serotonin reuptake inhibitors, the development of weakness, hyperreflexia and impaired coordination of movements is possible.

There were no interactions between sumatriptan and propranolol, flunirizine, pizotifen and ethanol.

Overdose

When administered subcutaneously at a dose of 12 mg, sumatriptan did not cause any side effects.

When administered subcutaneously at a dose greater than 16 mg or when administered orally greater than 400 mg, sumatriptan did not cause any unexpected side effects other than those listed above.

Treatment: gastric lavage, taking activated charcoal, monitoring the patient’s condition for at least 10 hours, and, if necessary, symptomatic therapy.

Storage conditions

At a temperature not exceeding 25° C, in a dry place, protected from light and out of reach of children.

Shelf life

2 years.

Manufacturer

Alium JSC, Russia