Amigrenin tablets, 100 mg 6 pcs

Pharmacotherapeutic group: antimigraine agent. ( NO. 02CC01).

Pharmacological properties

Pharmacodynamics:

Interacts with 5-hydroxytryptamine type I receptors located in the smooth muscle of the walls of blood vessels of the brain, selectively narrows the vessels in the carotid artery system, inhibits trigeminal nerve activity. All this contributes to reducing the severity of pain syndrome in migraine. Clinical effect is noted within 30 minutes.

Pharmacokinetics:

Sumatriptan is rapidly absorbed when taken orally. 70% of maximum serum concentration is reached after 45 minutes. Average value of absolute bioavailability is 14 % due to presystemic metabolism and incomplete absorption. The degree of binding to plasma proteins is low (14-21%), the elimination half-life is 2 hours. The main metabolite (indole acetic analog of sumatriptan) is excreted mainly with urine as free acid and its glucuronide conjugate.

Indications

Relief of acute migraine attacks (with and without aura).

Pharmacological effect

Pharmacotherapeutic group: antimigraine drug. (No. 02CC01).

Pharmacological properties

Pharmacodynamics:

Interacts with type I 5-hydroxytryptamine receptors located in the smooth muscles of the walls of blood vessels in the brain, selectively constricts blood vessels in the carotid artery system, and inhibits the activity of the trigeminal nerve. All this helps reduce the severity of migraine pain. The clinical effect is observed after 30 minutes.

Pharmacokinetics:

When taken orally, sumatriptan is rapidly absorbed. 70% of maximum serum concentration is achieved after 45 minutes. The average absolute bioavailability is 14% due to first-pass metabolism and incomplete absorption. The degree of binding to plasma proteins is low (14-21%), half-life is 2 hours. The main metabolite (indoleacetic analogue of sumatriptan) is excreted primarily in the urine in the form of the free acid and its glucuronide conjugate.

Special instructions

Sumatriptan should be prescribed with extreme caution for epilepsy (including any condition with a decreased seizure threshold), as well as for patients with controlled arterial hypertension. When prescribing Amigrenin to patients with newly diagnosed migraine or migraine with atypical symptoms, other potentially dangerous neurological diseases should be excluded. It must be borne in mind that patients with migraine are at risk of developing cerebrovascular complications (including stroke or transient cerebrovascular accident).

The drug should not be prescribed to patients at risk of developing pathology from the cardiovascular system, without prior examination to exclude the disease. The first 2-3 doses of the drug should be carried out under the supervision of a doctor (as spasm of the coronary arteries is possible). In patients with hypersensitivity to sulfonamides, when taking sumatriptan, allergic reactions may develop, which range from skin manifestations to anaphylactic shock.

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

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

Impact on the ability to drive vehicles and operate machinery

During therapy with sumatriptan, drowsiness may develop. Therefore, during the period of use of the drug, patients should be especially careful when driving a car and engaging in other potentially hazardous activities that require a high speed of psychomotor reactions.

Active ingredient

Sumatriptan

Composition

1 tab. contains:

Active ingredients: sumatriptan succinate 140 mg, which corresponds to the content of sumatriptan 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 mcg.

Contraindications

– hemiplegic, basilar and ophthalmoplegic forms of migraine;

— IHD (including angina pectoris);

– occlusive diseases of peripheral arteries;

– uncontrolled arterial hypertension;

— stroke or transient cerebrovascular accident (including history);

– severe liver dysfunction;

– simultaneous use of drugs containing ergotamine or its derivatives;

– simultaneous use of MAO inhibitors and a period of up to 14 days after their discontinuation;

– pregnancy;

– lactation period (breastfeeding);

— age of patients under 18 years and over 65 years;

– hypersensitivity to the drug.

Side Effects

From the cardiovascular system: hyperemia of the skin and mucous membranes, arterial hypotension, tachycardia, palpitations, angina pectoris, transient increase in blood pressure, transient ischemic ECG changes, bradycardia; in isolated cases – manifestations of Raynaud’s syndrome.

From the side of the central nervous system: dizziness, weakness, drowsiness, feeling of fatigue; visual impairment (diplopia, scotoma, decreased visual acuity).

From the digestive system: discomfort in the abdomen, dysphagia, nausea, vomiting; rarely – ischemic colitis, increased activity of liver enzymes.

Allergic reactions: rash, itching, erythema, urticaria, anaphylaxis.

Other: possible sensations of tingling, warmth, heaviness, pressure or compression in various parts of the body, myalgia.

Interaction

When taken simultaneously with ergotamine, prolonged vasospasm was observed. Amigrenin can be prescribed no earlier than 24 hours after taking medications containing ergotamine. Interaction between sumatriptan and MAO inhibitors is possible; their simultaneous use is contraindicated.

There are isolated reports of the development of weakness, hyperreflexia and loss of coordination in patients after concomitant use of sumatriptan and selective serotonin reuptake inhibitors.

Amigrenin and drugs of this group should not be prescribed simultaneously. Amigrenin and lithium preparations should not be prescribed simultaneously.

Overdose

Treatment: in case of overdose, the patient should be observed for 10 hours, providing symptomatic therapy as necessary.

Storage conditions

List B. Store in a dry place, protected from light, out of reach of children.

Shelf life

2 years. Do not use after the expiration date stated on the package.

Manufacturer

Veropharm LLC, Russia