Sumatriptan-Alium, 100 mg 2 pcs

Sumatriptan is an antimigraine agent.

Pharmacodynamics

Sumatriptan is a specific selective agonist of 5NT1D-serotonin receptors (5-hydroxytryptamine-1-like) located mainly in the blood vessels of the brain. Stimulation of 5HT1D-serotonin receptors leads to vasoconstriction. The drug does not affect other subtypes of 5HT-serotonin receptors (5HT2-5HT7).

In experimental studies it is shown that sumatriptan causes selective narrowing of carotid arteries, which supply blood to extracranial and intracranial tissues, including cerebral membranes (dilation of these vessels and/or their edema is the main mechanism of migraine development in humans), while not having a significant effect on cerebral blood flow. It is also experimentally established that sumatriptan inhibits the activity of receptors of trigeminal nerve afferent fibers endings. It eliminates nausea and photophobia associated with migraine attack.

Pharmacokinetics

Absorption. After oral administration, sumatriptan is rapidly absorbed, after 45 min its plasma concentration reaches 70% of the maximum value. After oral intake of sumatriptan in a dose of 100 mg maximum plasma concentration is reached in 2-2.5 hours and averages 54 ng/ml. Absolute bioavailability when administered orally is on average 14% due to presystemic metabolism and incomplete absorption.

Distribution. Binding to plasma proteins is 14-21%, total volume of distribution averages 170 L (2.4 L/kg).
Metabolism. Sumatriptan is metabolized by oxidation with the participation of monoamine oxidase (MAO) (mainly isoenzyme A) to form metabolites, the main of which is the indole acetic analog of sumatriptan, which has no pharmacological activity against 5HT1- and 5NT2-serotonin receptors, and its glucuronide.

Elimination. The elimination half-life is 2-2.5 hours. On average, plasma clearance is 1160 ml/minute, renal clearance is 260 ml/minute. Extra renal clearance is 40% after oral administration. It is excreted by the kidneys, mainly as metabolites (97% after oral administration) of free acid or glucuronide, the rest is excreted by the intestine.

Indications

Migraine (to control attacks, with or without aura).

Active ingredient

Composition

1 film-coated tablet contains:

The active ingredient

Sumatriptan (sumatriptan succinate) 100.00 mg (140.00 mg).

Ancillary substances:

Lactose,

Calcium hydrophosphate,

Magnesium stearate,

Povidone.

How to take, the dosage

Orally (the tablet is swallowed 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

In concomitant administration with ergotamine and ergotamine-containing drugs prolonged vasospasm is possible.

Possible interaction between sumatriptan and MAO inhibitors (decreased intensity of sumatriptan metabolism, increased concentration).

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

No interaction of sumatriptan with propranololol, flunirizine, pizotifen and ethanol has 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 should be clarified. When using sumatriptan for headache control in patients with previously undiagnosed migraine or with migraine with atypical symptoms, other potentially dangerous neurological diseases should be excluded. It should be borne in mind that in patients with migraine there is a risk of cerebrovascular complications development (including stroke or transient cerebrovascular disorders).

Sumatriptan should be used with caution in epilepsy and any other condition accompanied by decreased seizure threshold. If used concomitantly with SSRIs/ SSRIs, the patient’s condition should be closely monitored.

Before using sumatriptan in patients, the presence of cardiovascular disease should be excluded, especially in patients at risk. These patients include postmenopausal women, men over 40 years of age, and patients with risk factors for CHD.

The exam does not always reveal cardiovascular disease in some patients. In very rare cases, transient side effects such as pain and tightness in the chest may occur after taking sumatriptan. The pain may be intense and irradiate to the neck (pharynx) area. If there is reason to believe that these symptoms may be a manifestation of CHD, the drug should be stopped and a diagnostic examination should be performed.

Sumatriptan treatment should be used with caution in patients with controlled arterial hypertension because increased BP and peripheral vascular resistance may be observed in individual cases. Sumatriptan should be used with caution in patients with conditions in which absorption, metabolism, or excretion of sumatriptan may be significantly altered, such as renal or hepatic impairment.

In patients with hypersensitivity to sulfonamides when using sumatriptan, allergic reactions are possible, which range from skin manifestations to anaphylactic shock. There are limited data on cross-sensitivity, but caution is necessary when using sumatriptan in such patients.

Misuse of medications intended to relieve migraine attacks is associated with an increase in headaches in sensitive patients (drug abuse-related headache).
In this case, withdrawal of the drug should be considered.

Influence on the ability to drive and operate machinery

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

Contraindications

Side effects

Cardiovascular system disorders: very rare – bradycardia, tachycardia, arrhythmia, transient increase in blood pressure (BP) (immediately after treatment start), transient signs of myocardial ischemia on electrocardiogram, coronary spasm, myocardial infarction, Raynaud’s syndrome, BP reduction, “flushes” 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 – convulsions (usually in the presence of seizures in the history); 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, a feeling of heat, a feeling of weakness and/or fatigue, nasal bleeding, 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. When administered subcutaneously at a dose 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, symptomatic therapy if necessary. There are no data on the effect of hemodialysis and peritoneal dialysis on the concentration of sumatriptan in plasma.

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