Amigrenin - instructions for use, dose, side effects, contraindications

	Tab 50 mg	Tab 100 mg
Sumatriptan succinate	70 mg	140 mg
in terms of sumatriptan	50 mg	100 mg
Microcrystalline cellulose	16 mg	32 mg
Lactose (milk sugar)	61.8 mg	123.7 mg
Potato starch	5.8 mg	11.5 mg
Carboxymethyl starch sodium (primogel)	4.8 mg	9.6 mg
Magnesium stearate	1.6 mg	3.2 mg
Shell
Hypromellose (hydroxypropylmethylcellulose)	2.09 mg	4.18 mg
Povidone (polyvinylpyrrolidone)	1.4 mg	2.8 mg
Macrogol-4000 (polyethylene glycol 4000)	0.51 mg	1.02 mg
Talc	0.56 mg	1.12 mg
Titanium dioxide (E171)	0.44 mg	0.88 mg

Description:Round, biconvex tablets, covered with a film coat of white or white with a grayish cream color shade. On the cross-section, one or two layers are visible, the inner layer is white or white with a yellowish tinge.

Pharmacotherapeutic group:Anti-migraine means

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

Sumatriptan - Anti-migraine. Specific and selective agonist 5- HT₁-serotonin receptors, localized predominantly in the blood vessels of the brain, and does not affect other 5-HT-serotonin receptor subtypes (5-HT_2-7). Causes narrowing of the vessels of the carotid arterial bed, which supply extracranial and intracranial tissues (the expansion of the vessels of the meninges and / or their edema is the main mechanism of migraine development in humans) without significantly affecting cerebral blood flow.Suppresses the activity of the receptors of the endings of the afferent fibers of the trigeminal nerve in the dura mater (as a result, the secretion of sensory neuropeptides decreases). Eliminates the associated nausea and photophobia associated with migraine attacks. In 50-70% of cases, it quickly eliminates an attack with oral administration in a dose of 25-100 mg. Within 24 hours, a relapse may occur in 1/3 of the cases requiring re-application. The onset of action is 30 minutes after oral administration at a dose of 100 mg.

Pharmacokinetics:

Ingestion sumatriptan quickly absorbed. 70% of the maximum plasma concentration is reached after 45 minutes. After oral administration in a dose of 100 mg, the maximum concentration in blood plasma is an average of 54 ng / ml. Bioavailability is 14% due to presystemic metabolism and incomplete absorption. The connection with plasma proteins is 14-21%. Metabolized by oxidation with the participation of monoamine oxidase A (MAO) with the formation of metabolites, the main one being indoleacetic analogue of sumatriptan, not having pharmacological activity against 5HT1 and 5HT2-serotonin receptors. The elimination half-life is 2 hours.The main metabolite (indoleacetic analogue of sumatriptan) is excreted by the kidneys in the form of free acid and its glucuronide conjugate. Migraine attacks do not seem to have a significant effect on the pharmacokinetics of sumatriptan taken internally.

Indications:Coping migraine attacks with and without aura.

Contraindications:

-Increased sensitivity to the components of the drug;

- hemiplegic, basilar or ophthalmoplegic migraine forms;

ischemic heart disease (IHD), incl. angina pectoris (including Prinzmetal angina), myocardial infarction (including history), postinfarction cardiosclerosis, and the presence of symptoms suggesting the presence of IHD;

- Occlusive diseases of peripheral arteries;

- an insult or a transient ischemic attack (including in an anamnesis);

- uncontrolled arterial hypertension;

marked renal or hepatic insufficiency;

- Reception simultaneously with medicines containing ergotamine or its derivatives;

- intake simultaneously with MAO inhibitors and a period of up to 14 days after their cancellation;

-About 18 years old and over 65 years of age (safety and efficacy not established);

-lactation (within 24 hours after taking the drug), pregnancy.

Carefully:Controlled arterial hypertension; diseases in which absorption, metabolism or excretion of sumatriptan may change (eg, impaired renal or hepatic function); epilepsy (including any conditions with a decrease in the threshold of convulsive readiness); in patients with hypersensitivity to sulfonamides (allergic reactions are possible, up to anaphylaxis).

Pregnancy and lactation:

Sumatriptan is contraindicated during pregnancy.

Sumatriptan is excreted in breast milk, and therefore it is not recommended to breast-feed for 24 hours after taking the drug.

Dosing and Administration:

Inside. The tablet is swallowed whole with water.

The recommended dose of Amigrenin is one tablet of 50 mg. Some patients may require a higher dose of 100 mg. If migraine symptoms do not disappear and do not decrease after taking the first dose of the drug, then for cupping the same An attack should not be repeated. However, Amigrenin can be used for cupping subsequent migraine attacks.If the patient feels better after the first dose, and then the symptoms resume, you can take a second dose within the next 24 hours.

The maximum dose of Amigrenin should not exceed 300 mg during the 24-hour period.

Precautions for use

Sumatriptan should be prescribed only if the diagnosis of migraine is undoubted, and it should be used as soon as possible after the onset of a migraine attack, although it is equally effective when used at any stage of an attack. Do not use sumatriptan with a preventive purpose.

As with the use of other anti-migraine drugs, before the appointment of sumatriptan, patients with a newly diagnosed migraine or atypically migraine should exclude other potentially dangerous neurological diseases. It should be borne in mind that in patients suffering from migraine, the risk of developing a stroke or transient impairment of cerebral circulation is increased. Sumatriptan Do not prescribe to patients at risk of cardiovascular disease without a preliminary examination to exclude it.Such patients include postmenopausal women, men over the age of 40, persons with IHD risk factors. The performed examination does not always allow to reveal the SSS disease; transient intense pain and chest tightness, extending to the neck area, and arising after taking sumatriptan, may be symptoms of coronary heart disease. In very rare cases, patients may experience serious adverse reactions from the cardiovascular system, in whose anamnesis there was no cardiovascular pathology.

Patients with controlled arterial hypertension should be administered with caution, as in some cases there has been an increase in arterial pressure and peripheral vascular resistance; in patients suffering from such diseases, in which the absorption, metabolism or excretion of this drug can significantly change (for example, kidney or liver damage).

In very rare cases, serotonin syndrome (including psychiatric disorder, autonomic lability, and neuromuscular disorders) can develop as a result of the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan.Also, the development of serotonin syndrome was reported against the background of the simultaneous administration of triptans with selective serotonin and noradrenaline reuptake inhibitors (SSRIs). In the case of simultaneous administration with drugs from the SSRI / SSRIH group, the patient's condition should be closely monitored. Sumatriptan should be used with caution in patients with epilepsy or organic brain damage in history with a reduction in the threshold of convulsive activity.

The concomitant use of other tryptans / 5-HT1 agonists with sumatriptan is not recommended. In patients with hypersensitivity to sulfanilamides, taking sumatriptan can cause allergic reactions that range from skin manifestations to anaphylaxis. Data on cross-sensitivity are limited, however, caution should be exercised when assigning sumatriptan to such patients. Abuse of medicines intended to stop migraine attacks is associated with increased headaches in sensitive patients (headache associated with drug abuse). In this case, the possibility of drug cancellation should be considered.

Do not exceed the recommended dose of sumatriptan.

Side effects:

Research and analysis of clinical and postmarketing data sumatriptan allowed to identify the following undesirable reactions depending on the anatomical and physiological classification and frequency of occurrence. The frequency is defined as follows: very often (> 1/10); often (> 1/100 and <1/10); sometimes (> 1/1000 and <1/100); rarely (> 1/10 000 and <1/1000); very rarely <1/10 000), including individual cases.

Analysis of clinical trials:

From the nervous system: often - dizziness, drowsiness, sensitivity disorders, including paresthesia and decreased sensitivity.

From the side of the cardiovascular system, often - a transient increase in blood pressure (soon after taking the drug), hot flashes.

From the respiratory and thoracic organs: often - shortness of breath; light, transient irritation of the mucosa or burning sensation in the nasal cavity or throat, nosebleeds.

From the gastrointestinal tract: often - nausea, vomiting (cause-and-effect relationship is not proven).

From the side of the musculoskeletal system and connective tissue: often - a feeling of heaviness (usually transient, can be intense and occur in any part of the body, including the chest and throat).

General and local reactions: often - pain, a feeling of cold or heat, a feeling of pressure or constriction (usually transient, can be intense and occur in any part of the body, including the chest and throat). Often - weakness, fatigue (usually mild or moderately expressed, transient).

Laboratory indicators: very rarely - slight deviations in liver function tests.

Analysis of postmarketing observations:

From the immune system: very rarely - hypersensitivity reactions, including skin manifestations, as well as anaphylaxis.

From the nervous system: very rarely convulsive seizures (in a number of cases observed in patients with convulsive episodes in the anamnesis or with concomitant conditions predisposing to the onset of seizures, some patients did not have risk factors), tremor, dystonia, nystagmus, scotoma.

From the side of the organs of sight: very rarely - flashing, diplopia, reduced visual acuity. Blindness (usually transient).However, visual disturbances can be caused by the actual migraine attack.

From the side of the cardiovascular system: very rarely - bradycardia, tachycardia, flutter, arrhythmias, transient changes in the ECG, coronary vasospasm, angina pectoris, myocardial infarction. Very rarely - hypotension, Raynaud's syndrome.

From the gastrointestinal tract: very rarely - ischemic colitis, dysphagia, a feeling of discomfort in the abdomen.

Overdose:

Symptoms: when taking sumatriptan inside at a dose of up to 400 mg, there are no other adverse reactions other than those listed above.

Treatment: gastric lavage; follow the patient's condition for 10 hours and, if necessary, carry out symptomatic therapy. There is no evidence of the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in blood plasma.

Interaction:

No interaction of sumatriptan with propranolol, flunarizine, pisotifen and ethyl alcohol has been observed.

With simultaneous administration with ergotamine, a prolonged vasospasm was noted. Sumatriptan can be prescribed not earlier than 24 hours after preparations containing ergotamine; and vice versa, preparations containing ergotamine can be prescribed no earlier than 6 hours after taking sumatriptan.

Interaction between sumatriptan and MAO inhibitors, as well as sumatriptan and drugs from the group of selective serotonin reuptake inhibitors (SSRIs), is possible. There are separate reports on the development of weakness, hyperreflexia and movement coordination disorders in patients after SSRIs, as a result of the possible development of serotonin syndrome. Also, the development of serotonin syndrome was reported against the background of the simultaneous administration of triptans with selective serotonin and noradrenaline reuptake inhibitors (SSRIs). In case of their simultaneous application, the patient's condition should be carefully monitored.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 50 mg and 100 mg.

Packaging:

For 2 or 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 2 or 10 tablets in a jar of polymer materials with a screw neck and cap screwed from polypropylene and low-pressure polyethylene.

Each jar or 1 circuit cell package for 2 or 10 tablets, or 3 contour packs of 2 tablets together with the instruction for use, is placed in a pack of cardboard.

Storage conditions:At a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:4 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001758 / 01

Date of registration:14.08.2008 / 17.09.2015

Expiration Date:Unlimited

The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia

Manufacturer: & nbsp

VEROPHARM SA Russia

Information update date: & nbsp03.08.2017

Illustrated instructions

Instructions

Amigrenin® (Amigrenin®)