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

Headache, MigraineCutting acute migraine attacks (with and without aura).

Active ingredient

Sumatriptan

Composition

1 tablet 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 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 decrease after the first dose of Amigrenin, the drug should not be repeated to stop an ongoing attack.

If symptoms decrease or subside and then return, a second dose may be taken within the next 24 hours. The interval between doses should be at least 2 hours.

Interaction

In concomitant administration with ergotamine, prolonged vasospasm was noted. Amigrenin may be administered not earlier than 24 h after taking ergotamine-containing drugs. There may be interaction between sumatriptan and MAO inhibitors, their simultaneous use is contraindicated.

There have been isolated reports of weakness, hyperreflexia, and impaired 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 concomitantly.

Special Instructions

Sumatriptan should be administered with special caution in epilepsy (including any condition with decreased seizure threshold), as well as in patients with controlled arterial hypertension. 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 sumatriptan may develop allergic reactions, which range from skin manifestations to anaphylactic shock.

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

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

Influence on driving and operating ability

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

Contraindications

– hemiplegic, basilar and ophthalmoplegic forms of migraine;

– CHD (including angina pectoris);

– peripheral artery occlusive disease;

– uncontrolled arterial hypertension;

– stroke or transient cerebral circulation disorder (including history);

– significant impairment of liver function;

– concomitant use of drugs containing ergotamine or its derivatives;

– concomitant use of MAO inhibitors and up to 14 days after their withdrawal;

– pregnancy;

– lactation (breastfeeding) period;

– patients under 18 and over 65 years of age;

– hypersensitivity to the drug.

Side effects

Cardiovascular system disorders:hyperemia of skin and mucous membranes, arterial hypotension, tachycardia, palpitations, angina pectoris attack, transient BP increase, transient ECG changes of ischemic type, bradycardia; in single cases – manifestations of Raynaud’s syndrome.

CNS side:dizziness, weakness, drowsiness, fatigue; visual disorders (diplopia, scotoma, decreased visual acuity).

Digestive system disorders:A feeling of discomfort in the stomach, dysphagia, nausea, vomiting; rarely – ischemic colitis, increased liver enzyme activity.

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

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

Overdose

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

Similarities

Amigrenin, Sumamigren, Sumatriptan, Sumatriptan-OBL, Sumatriptan-Teva