Amigrenin, 100 mg 2 pcs

Interacts with 5-hydroxytryptamine type 1 receptors located in the smooth muscle of the walls of blood vessels of the brain.

Stimulation of 5HT₁ receptors leads to selective vasoconstriction in the carotid artery system and reduction of neurogenic inflammation processes, while not having a significant effect on cerebral blood flow. In addition, it is experimentally established that sumatriptan inhibits trigeminal nerve activity.

Preferentially narrows the vessels in the carotid artery system, inhibits the activity of the trigeminal nerve. Contributes to reduction of the severity of pain syndrome in migraine. The clinical effect is observed within 30 minutes.

Pharmacokinetics

Absorption

. When administered orally, sumatriptan is rapidly absorbed from the gastrointestinal tract, reaching a plasma concentration of 70% of C_max after 45 min. Absolute bioavailability when administered orally due to presystemic metabolism and incomplete absorption is on average 14%.

Distribution

The binding to plasma proteins is 14-21%.

Metabolism

It is biotransformed with the formation of metabolites, the main one being the indoleukasic analogue sumatriptan.

Elevation

T_1/2 is 2 h. The main metabolite of sumatriptan is excreted mainly in the urine as free acid or glucuronide conjugate

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Indications

Cure acute attacks of migraine, with or without aura.

Active ingredient

Composition

1 tablet contains sumatriptan (in the form of succinate) 100 mg;

Excipients:

Microcrystalline cellulose – 32 mg,

lactose (milk sugar) – 123.7 mg,

potato starch – 11.5 mg,

sodium carboxymethyl starch (primogel) – 9.6 mg,

magnesium stearate – 3.2 mg.

Shell composition:

hypromellose (hydroxypropyl methylcellulose) – 4.18 mg,

povidone (polyvinylpyrrolidone) – 2.8 mg,

macrogol 4000 (polyethylene glycol 4000) – 1.02 mg,

talc – 1.12 mg,

titanium dioxide (E171) – 880 µg.

How to take, the dosage

Amigrenin is not intended for prophylactic use.

Adults are prescribed in a single dose of 50 mg, in some cases 100 mg. The maximum daily dose is 300 mg.

If migraine symptoms do not disappear or diminish after the first dose of Amigrenin, the drug should not be repeatedly prescribed to stop an ongoing attack. If symptoms decrease or subside and then resume, a second dose may be taken within the next 24 hours. The interval between doses should be at least 2 h.

Interaction

The concomitant use of ergot alkaloids, lithium preparations, serotonin reuptake inhibitors, MAO inhibitors is unacceptable.

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

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Special Instructions

When prescribing Amigrenin to patients with newly diagnosed 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 (including stroke or transient cerebrovascular disorders).

The drug should not be administered to patients at risk of cardiovascular pathology without prior examination to rule out the disease. The first 2-3 doses of the drug should be taken under the supervision of a physician (because coronary artery spasm is possible).

Patients with hypersensitivity to sulfonamides when taking Amigrenin may develop allergic reactions that range from skin manifestations to anaphylactic shock.

If there is no effect on administration of the first dose, the diagnosis should be clarified.

Clinical experience with the drug in patients over 65 years of age is limited (no significant difference in pharmacokinetics compared to younger patients).

Influence on driving and operating machinery

Drowsiness may develop during Amigrenin therapy. Therefore, during the period of the drug use patients should be especially careful to drive vehicles and engage in other potentially hazardous activities requiring high speed of psychomotor reactions.

Contraindications

Individual intolerance to the drug, CHD including. angina pectoris, hemiplegic, basilar or ophthalmoplegic forms of migraine, peripheral arterial occlusive disease, uncontrolled arterial hypertension, history of stroke or transient cerebral circulation disorder, liver failure, pregnancy, breastfeeding, childhood, old age (over 65 years), concomitant use with ergotamine and its derivatives.

With caution – epilepsy (including any condition with reduced epileptic threshold), arterial hypertension (controlled), concomitant use of MAO inhibitors and the period up to 14 days after their withdrawal.

Side effects

A sensation of tingling, warmth, heaviness, pressure in different parts of the body, hyperemia of skin and mucous membranes; dizziness, fatigue, weakness, sleepiness; angina pectoris attack, hypotension, tachycardia, palpitations, transient BP increase, transient ECG changes of ischemic type, bradycardia, in single cases – Raynaud’s syndrome; abdominal discomfort, dysphagia, nausea, vomiting, ischemic colitis; visual disturbances (diplopia, scotoma, decreased visual acuity); allergic reactions (rash, urticaria, pruritus, erythema, anaphylaxis); change of liver function tests; myalgia.

Overdose

Symptoms: intensification of side effects.

Treatment: In case of overdose, the patient should be observed for 10 hours, giving symptomatic therapy as needed.

Pregnancy use

The drug is contraindicated in pregnancy and during lactation (breast-feeding).

Pediatric use

The drug is contraindicated in children and adolescents under 18 years of age.

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