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

Cutting migraine attacks (with or without aura).

Active ingredient

Composition

How to take, the dosage

Overly (swallow the tablet whole with water).

The initial single dose is 50 mg; if necessary, the dose can be increased to 100 mg.

If migraine symptoms do not disappear or decrease after the first dose, a second dose to stop an ongoing attack is not indicated.

To control subsequent attacks (when symptoms decrease or disappear and then resume), a second dose may be taken within the next 24 hours, provided that there is at least a 2-hour interval between doses.

The maximum daily dose when taken orally is 300 mg.

Interaction

Possible prolonged vasospasm when concomitantly administered with ergotamine and ergotamine-containing drugs.

Possible decrease in the intensity of sumatriptan metabolism, increase in its concentration, with interaction between sumatriptan and MAO inhibitors.

In concomitant use of sumatriptan and drugs from the group of selective serotonin reuptake inhibitors, weakness, hyperreflexia, and impaired coordination of movements may occur.

The interaction of sumatriptan with propranololol, flunirizine, pizotifen and ethanol has not been noted.

Special Instructions

Sumatriptan is not intended to prevent migraine.

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

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

In patients of cardiovascular risk group the therapy should not be started without prior investigation (women after menopause, men after 40 years of age, patients with CHD risk factors).

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

Pain and tightness in the chest may occur after taking sumatriptan. The pain may be intense and irradiate into the neck. If these symptoms are suspected to be a manifestation of CHD, an appropriate evaluation should also be performed.

Impact on driving ability and operating machinery

In migraine, as well as during sumatriptan therapy, drowsiness may develop. Therefore, during sumatriptan use, caution should be exercised when driving motor transport and engaging in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

With caution:

Side effects

The incidence of side effects is classified according to the recommendations of the World Health Organization: very frequently – at least 10%; frequently – at least 1%, but less than 10%; infrequently – at least 0.1%, but less than 1%; rarely – at least 0.01%, but less than 0.1%; very rarely – less than 0.01% (including single cases).

Cardiovascular system disorders: very rare – bradycardia, tachycardia, arrhythmia, transient increase of blood pressure (BP) (immediately after treatment start), transient signs of myocardial ischemia on electrocardiogram, coronary spasm, myocardial infarction, Raynaud’s syndrome, decrease of BP, “tides” of blood to the face.

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

The digestive system: frequently – nausea, vomiting; slight increase in the activity of “liver” enzymes; very rarely – ischemic colitis, diarrhea, a feeling of discomfort in the abdominal area.

Nervous system disorders: frequently – dizziness, somnolence, sensitivity disorders, including paraesthesia, hypoesthesia; very rarely – seizures (usually with seizures in the anamnesis); unknown frequency – tremor, dystonia, anxiety.

Visually: infrequent – diplopia, flickering of “flickers” before eyes, nystagmus, scotoma, decreased visual acuity; very rare – partial transient loss of vision (it should be noted that visual disturbances may be associated with the attack of migraine).

Musculoskeletal system: often – myalgia; unknown frequency – neck stiffness, arthralgia.

Allergic reactions: very rare – skin rash, urticaria, pruritus, erythema, anaphylaxis.

Others: often – pain, tingling, sensation of heat, feeling of weakness and/or fatigue, nosebleed, 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.

Overdose

Sumatriptan did not cause any side effects when administered in a single subcutaneous dose of 12 mg.

In subcutaneous doses greater than 16 mg or when administered orally greater than 400 mg, sumatriptan did not cause any unanticipated side effects other than those listed above.

Treatment: gastric lavage, administration of activated charcoal, patient monitoring for at least 10 hours, and symptomatic therapy if necessary.

Similarities