Description
Latin name
Amigrenin
release form
Amigrenin. Coated tablets.
Packing
2 pcs – blister packagings (1) – packs of cardboard.
Pharmacological action of
Antimigraine preparation. A specific selective agonist of serotonin 5HT1B-1D receptors (5-hydroxytryptamine-1-like) located primarily in the smooth muscles of the walls of the blood vessels of the brain. Stimulation of 5HT1 receptors leads to selective narrowing of blood vessels in the carotid artery system and a decrease in the processes of neurogenic inflammation, without having a significant effect on cerebral blood flow. In addition, it has been experimentally established that sumatriptan inhibits trigeminal nerve activity.
It is believed that these effects help to reduce the severity of pain in migraines.
Clinical effect is observed 30 minutes after oral administration of the drug.
Pharmacokinetics
Absorption
When ingested, sumatriptan is rapidly absorbed from the digestive tract, after 45 minutes its concentration in the plasma reaches 70% of max. Absolute bioavailability when administered through presystemic metabolism and incomplete absorption is an average of 14%.
Distribution of
Plasma protein binding is 14-21%.
Metabolism
Biotransformed with the formation of metabolites, the main of which is the indoluxus analogue of sumatriptan.
Excretion of
T1 / 2 is 2 hours. The main metabolite of sumatriptan is excreted mainly in the urine as a free acid or glucuronide conjugate
Indications
Relief of acute migraine attacks, with or without aura.
Contraindications
hemiplegic, basilar and ophthalmoplegic forms of migraine
ischemic heart disease (including angina pectoris)
occlusive peripheral arterial disease
uncontrolled arterial hypertension or congestive heart failure liver
simultaneous administration of preparations containing ergotamine or its derivatives
simultaneous administration of MAO inhibitors and the period up to 14 days after their withdrawal
pregnancy
lactation period (gr feeding-stand)
patients age 18 and older than 65 years
hypersensitivity to the drug.
Use during pregnancy and lactation
The drug is contraindicated in pregnancy and lactation (breastfeeding).
Composition of
1 tablet contains sumatriptan (as succinate) 100 mg
Excipients:
microcrystalline cellulose – 32 mg,
lactose (milk sugar) – 123.7 mg,
potato starch – 11.5 mg sodium potassium starch, 11.5 mg carmel starch 9.6 mg,
magnesium stearate – 3.2 mg.
Shell composition:
hypromellose (hydroxypropylmethyl cellulose) – 4.18 mg,
povidone (polyvinylpyrrolidone) – 2.8 mg,
macrogol 4000 (polyethylene glycol 4000) – 1.02 mg,
talcum – 1.12 mg, srdlkg1 titanium dioxide.
Dosage and Administration
Amigrenin is not intended for prophylactic use.
Adults are prescribed a single dose of 50 mg, in some cases 100 mg.
The maximum daily dose is 300 mg.
If the symptoms of migraine do not disappear and do not decrease after taking the first dose of Amigrenin, then the drug should not be prescribed again to stop the ongoing attack. If the symptoms have decreased or disappeared, and then resumed, you can take a second dose over the next 24 hours. The interval between doses of the drug should be at least 2 hours.
Side effects of
From the cardiovascular system: hyperemia of the skin and mucous membranes, hypotension, tachycardia, palpitations, attack of angina pectoris, transient increase in blood pressure, transient ECG changes of the ischemic type, bradycardia in isolated cases – manifestations of Raynaud’s syndrome.
From the side of the central nervous system: dizziness, weakness, drowsiness, 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.
Others: tingling, heat, heaviness, pressure or contraction in various parts of the body, myalgia are possible.
Overdose
Symptoms: increased side effects.
Treatment: In case of overdose, the patient should be monitored for 10 hours, carrying out symptomatic therapy as needed.
Storage conditions
The drug should be stored in a dry, dark place.
Keep out of the reach of children.
Expiration
2 years.
The active substance
Sumatriptan
dosage form
dosage form
tablets
