2010/09/20

Amigrenin

Composition, structure and packing

Tablets, coated white or white with grayish-cream shade of color, with a double-convex surface.

1 tab. sumatriptan (in the form of succinate) 50 mg - 100 mg.

Excipients: microcrystalline cellulose, lactose, potato starch, sodium karboksimetilkrahmal, magnesium stearate, or oksipropiltsellyuloza oksipropilmetiltsellyuloza, polyvinylpyrrolidone, polyethylene glycol 4000, talc, titanium dioxide.

Clinico-pharmacological group: agonist 5-HT1-receptor.

The drug with protivomigrenoznoy activity.

Pharmacological action

Protivomigrenozny drug. Specific selective serotonin agonist 5HT1B-1D-receptors (5-hydroxytryptamine-1-like), located mainly in the smooth muscle walls of blood vessels of the brain. Stimulation of 5HT1-receptors leads to selective vasoconstriction in the carotid arteries and reduction processes of neurogenic inflammation, without causing any significant effect on cerebral blood flow. In addition, the experimentally found that sumatriptan inhibits trigeminal nerve. It is believed that these effects contribute to the reduction of pain syndrome during migraine.

The clinical effect observed 30 min after oral administration.

Pharmacokinetics

Absorption

When receiving the drug inside sumatriptan is rapidly absorbed from the gastrointestinal tract, through 45 minutes of its plasma concentration reaches 70% of C max. Absolute oral bioavailability due presistemnogo metabolism and incomplete absorption averages 14%.

Distribution

Plasma protein binding is 14-21%.

Metabolism

Biotransformiruetsya with the formation of metabolites, the main of which is the analogue of indoluksusny sumatriptan.

Withdrawal

T1 / 2 is 2 hours

The main metabolite of sumatriptan, is derived mainly from the urine in the form of free acid or glyukuronidnogo conjugate.

Statement
relief of acute migraine with aura or without her.

Dosage regimen

Amigrenin not intended to apply to prevention. Adults appoint 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 or decrease after the first dose Amigrenina, the drug should not be reappointed for relieving the ongoing attack. If the symptoms are diminished or gone, and then resumed, you can take a second dose during the next 24 hours interval between doses of the drug should not be less than 2 hours

Side effect
Since the cardiovascular system: hyperemia of the skin and mucous membranes, hypotension, tachycardia, sensation of palpitations, heart attack, transient increase in blood pressure, transient ECG changes of ischemic type, bradycardia, and in rare cases - manifestations of Raynaud's syndrome.
From the side of the central nervous system: dizziness, weakness, drowsiness, fatigue, visual disturbances (diplopia, scotoma, reduced visual acuity).
On the part of the digestive system: a feeling of abdominal discomfort, dysphagia, nausea, vomiting, rarely - ischemic colitis, increased activity of liver enzymes.

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

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

Contraindications
hemiplegic, basilar and oftalmoplegicheskaya forms of migraine;
CHD (including angina);
occlusive peripheral arterial disease;
uncontrolled arterial hypertension;
stroke or transient cerebral blood flow (including history);
marked disturbances of liver function;
simultaneous reception of preparations containing ergotamine or its derivatives;
simultaneous reception of MAO inhibitors and the period to 14 days after their removal;
Pregnancy
Lactation (breastfeeding);
patients age 18 years and over 65 years;
Hypersensitivity to the drug.

Pregnancy and lactation

The drug is contraindicated during pregnancy and lactation (breastfeeding).

Application for violations of liver function

Contraindications disturbancies liver function.

Cautions

With great care should be administered sumatriptan in epilepsy (including under any conditions with a reduction in the threshold of convulsive readiness), as well as patients with controlled hypertension. In appointing Amigrenina patients with newly diagnosed migraine or migraine, which flows with atypical symptoms, should exclude other potentially serious neurological diseases.

It must be borne in mind that patients with migraine are at risk of cerebrovascular complications (including stroke or transient cerebral circulatory disorders). The drug should not be given to patients at risk of development of pathology of the cardiovascular system, without the prior survey in order to eliminate the disease.

The first 2-3 taking the drug should be under the supervision of a physician (as is possible spasm of the coronary arteries). In patients with hypersensitivity to sulfanilamide when taking sumatriptan, may develop allergic reactions ranging from skin manifestations to anaphylactic shock. In the absence of effect on the introduction of the first dose should clarify the diagnosis.

Clinical experience with the drug in patients aged over 65 years is limited (no significant difference in pharmacokinetics compared with younger patients is not observed).

Effects on ability to drive vehicles and management mechanisms

The therapy sumatriptanom may develop drowsiness. Therefore, the period of the drug patients should take special care driving and doing other potentially hazardous activities that require high speed of psychomotor reactions.

Overdose

Treatment: In case of overdose should observe the patient for 10 hours, spending symptomatically as needed.

Drug Interactions

At the same time.The celebrated with ergotamine long vasospasm. Amigrenin can be assigned no earlier than 24 hours after receiving preparations containing ergotamine. Perhaps the interaction between sumatriptanom and MAO inhibitors, their simultaneous use is contraindicated.

There are some reports on the development of weakness, hyperreflexia and poor coordination in patients after simultaneous reception of sumatriptan and selective serotonin reuptake inhibitors.

It should not be simultaneously appointed Amigrenin and drugs in this group.

It should not be simultaneously appointed Amigrenin and lithium preparations.

Terms and Conditions of storage

List B. The drug should be stored in a dry, dark place.

Shelf life - 2 years.