Sumatriptan

AMIGREN capsules 50 mg, capsules 100 mg

Instruction manual

For medical use of the drug

Amigren

(amigren)

Structure:

Active substance: sumatriptan;

1 capsule contains sumatriptan succinate in terms of sumatriptan 50 mg or 100 mg;

excipients: lactose, monohydrate; microcrystalline cellulose; croscarmellose sodium; magnesium stearate;

capsule shell composition: gelatin, titanium dioxide (E 171), ponso 4R (E 124).

Dosage form.

Capsules 50 mg No. 1, 50 mg No. 3, 100 mg No. 1, 100 mg No. 3.

Pharmacotherapeutic group.

Selective agonist of 5nt1 receptors of serotonin. drugs used to treat migraines. PBX code n02c c01.

Pharmacological properties.

sumatriptan is a selective 5nt1 receptor agonist that does not affect other 5nt1 receptors. these receptors are found mainly in cranial blood vessels. in experimental studies, it was found that sumatriptan has a selective vasoconstrictor effect on blood vessels in the system of carotid arteries, but does not affect cerebral circulation. the carotid artery system supplies blood to extra- and intracranial tissues, such as the meninges. due to the expansion of these vessels, migraine develops. Additionally, using experimental data, it was proved that sumatriptan inhibits trigeminal nerve activity. these are two possible mechanisms due to which the antimigraine activity of sumatriptan is manifested.

The clinical effect is observed 30 minutes after oral administration of 100 mg of the drug.

Pharmacokinetics After oral administration, sumatriptan is rapidly absorbed, reaching 70% of the maximum concentration after 45 minutes. After taking 100 mg, the average maximum plasma concentration is 45 ng / ml. The bioavailability after oral administration is 14%, partly due to the presystemic metabolism, partly as a result of incomplete absorption. Binding to blood plasma proteins is low (14-21%), the average volume of distribution is 17 l. The average total plasma clearance is approximately 1160 ml / min, and the average renal clearance is approximately 260 ml / min. Non-renal clearance is approximately 80% of the total clearance, this suggests that sumatriptan is excreted mainly in the form of metabolites. The main metabolite, the indolacetic analogue of sumatriptan, is excreted in the urine, where it is contained in the form of a free acid and conjugated compound with glucuronide. It does not have 5HT1 and 5HT2 activity. No other metabolites have been identified. The pharmacokinetics of oral sumatriptan does not significantly change during a migraine attack.

Pharmaceutical characteristics.

Basic physical and chemical properties: No. 1 hard gelatin capsules of cylindrical shape with hemispherical ends; the body is white, the cap is red.

The contents of the capsules are odorless white or almost white powder.

Clinical characteristics.

Indications.

To quickly alleviate the condition with migraine attacks, with or without an aura.

Contraindications

Hypersensitivity to any component of the drug.

A history of myocardial infarction, coronary heart disease, Prinzmetal angina, peripheral vascular disease, or symptoms characteristic of coronary heart disease.

A stroke or a passing history of cerebrovascular accident.

Moderate or severe arterial hypertension and mild uncontrolled arterial hypertension.

Severe liver failure.

Concomitant use of ergotamine or its derivatives (including methysergide) (see section "Interaction with other drugs and other types of interactions").

Concomitant use of a tryptan / 5-hydroxytryptamine receptor agonist (5-HT₁) (cm.section “Interaction with other drugs and other types of interactions”).

Competitive use of monoamine oxidase inhibitors (MAO) and Amigren. Amigren should not be used within 2 weeks after the withdrawal of MAO inhibitors.

Interaction with other drugs and other types of interactions.

There is no evidence of interaction with propranolol, flunarizine, pisotifen, or alcohol.

Data regarding co-administration with drugs containing ergotamine or other tryptan / 5-HT1 receptor agonists are limited. Prolonged vasospastic reactions are theoretically possible, therefore such combined use is contraindicated (see section "Contraindications").

The time interval between admission of sumatriptan and drugs containing ergotamine or other triptan / 5-HT1 receptor agonists is unknown. It depends on the dose and type of medication used. Since these effects can be enhanced by taking Amigren, it is necessary to adhere to a 24-hour interval between taking medications containing ergotamine and other triptan / 5-HT1 receptor agonists and taking Amigren. Accordingly, preparations containing ergotamine and other tryptan / 5-HT1 receptor agonists cannot be used within 6 hours after taking Amigren.

The interaction may occur between sumatriptan and MAO inhibitors, therefore, their simultaneous use is contraindicated (see section "Contraindications").

There are few reports of patients developing serotonin syndrome (including altered mental state, visceral instability, neuromuscular disorders) after taking selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. There are reports of the development of serotonin syndrome with the simultaneous use of triptans and serotonin and norepinephrine reuptake inhibitors (SNRIs) (see section "Peculiarities of use").

Features of the application.

Amigren capsules are used only with a clearly established diagnosis of migraine.

Amigren is not used to treat hemiplegic, basilar and ophthalmoplegic migraines.

As with the use of other drugs, for the relief of migraine attacks in patients with a previously unknown diagnosis of migraine and in patients with an established diagnosis, but in the presence of atypical symptoms, it is necessary to exclude the presence of another serious neurological pathology before taking sumatriptan. It should be noted that patients with migraine have an increased risk of cerebrovascular disorders (stroke, transient cerebrovascular accident).

The use of sumatriptan in some patients causes transient symptoms such as pain, a feeling of constriction in the chest, which could be intense and spread to the larynx (see section “Adverse reactions”). If such symptoms indicate coronary heart disease, an appropriate cardiac examination should be performed.

Sumatriptan should not be prescribed to patients with suspected heart disease without a preliminary examination to identify cardiovascular pathology. This group includes women in the postmenopausal period, men from 40 years old and patients with risk factors for developing coronary heart disease. However, such an examination cannot always detect the presence of heart disease, therefore, in rare cases, patients with undiagnosed heart disease have severe cardiological complications. With caution, Amigren should be prescribed to patients under observation for arterial hypertension, since a small number of patients may experience a transient increase in blood pressure and peripheral vascular resistance.

Isolated cases of the occurrence of serotonin syndrome in patients (including altered mental state, visceral instability, neuromuscular disorders) that occur after taking selective serotonin reuptake inhibitors (SSRI) and sumatriptan are described. There are reports of the development of serotonin syndrome with the simultaneous administration of triptans and serotonin and noradrenaline reuptake inhibitors (SNRIs). If the simultaneous use of Amygren and SSRI / SNRI are clinically justified, it is advisable that a preliminary examination of patients be performed (see the section "Interaction with other drugs and other types of interactions").

It is not recommended to use sumatriptan with any triptan / 5HT1 agonist at the same time.

Amigren should be prescribed with caution to patients with a significant violation of the absorption, metabolism or elimination of the drug, for example, with renal and liver failure.

Amigren should be prescribed with caution to patients with a history of seizures or with risk factors for lowering the seizure threshold.

In patients with hypersensitivity to sulfonamides, allergic reactions may occur after the use of Amigren. Reactions can be detected ranging from skin hypersensitivity to anaphylaxis. The presence of cross-sensitivity is limited, however, care must be taken when prescribing the drug to such patients.

The recommended doses of Amigren should not be exceeded.

Intensive treatment of acute migraine attacks is associated with an exacerbation of headache (headache due to intensive treatment) in sensitive patients. It may be necessary to discontinue treatment.

Adverse reactions can occur more often during the combined use of triptans and preparations from herbs containing St. Johns wort (Hypericum perforatum).

Prolonged use of any type of pain medication can aggravate a headache. In the event of such a situation or its threat, you need to consult a doctor and stop treatment. In patients who often or daily have a headache due to the regular use of medicines for headaches, a diagnosis of headache due to the abuse of painkillers can be made.

The drug contains lactose, so patients with the rare hereditary forms of galactose intolerance, lactose deficiency or glucose-galactose malabsorption syndrome should not use the drug.

Use during pregnancy or lactation.

Amigren is not recommended for pregnant women. if necessary, the ratio of the expected benefit to the mother and the possible risk to the fetus should be weighed.

Use with caution during lactation. It is not recommended to breast-feed a baby for 24 hours after taking the drug.

Children.

It is not recommended to use, since until this time the effectiveness and safety of the use of sumatriptan for the treatment of children have not been established.

The ability to influence the reaction rate when driving or working with other mechanisms.

Drowsiness can be a consequence of both migraine and its treatment with migraine, so you should avoid driving or working with other mechanisms while taking the drug or a migraine attack.

Dosage and administration.

Amigren capsules can not be used to prevent an attack.

Amigren is recommended to be used as soon as possible after the onset of a migraine attack, although it is equally effective at every stage of the attack.

The recommended dose of Amigren for adults is 50 mg (1 tablet). In some cases, the dose can be increased to 100 mg (2 capsules).

Amigren can be used for new migraine attacks, but if the first dose of the drug is ineffective, the drug should not be reused during the same attack.

If the patient has responded to the first dose, but the symptoms are restored, the second dose can be applied over the next 24 hours, while the total daily dose should not exceed 300 mg.

Capsules should be swallowed whole, washed down with water.

Children

Until this time, the effectiveness and safety of the use of sumatriptan for the treatment of children has not been established, therefore, children are not used.

Elderly patients (age from 65 years)

Experience with sumatriptan for treating patients over 65 years of age is not enough. Although the pharmacokinetics of the drug does not differ from that of younger people, until additional clinical data are obtained, the appointment of Amigren to elderly patients is not recommended.

Adverse Reactions

On the part of the immune system: hypersensitivity reactions - from skin hypersensitivity to cases of anaphylaxis.

From the nervous system: dizziness; drowsiness; violation of sensitivity, including paresthesia and hypoesthesia; cramps. Although some of these cases were noted in patients with seizures or with conditions that may lead to them, there is a history of seizures in patients without any tendency to them; tremor, dystonia, nystagmus, scotoma.

From the psyche: arousal.

From the cardiovascular system: a transient increase in blood pressure immediately after taking the drug, a rush of blood, bradycardia, tachycardia, increased heart rate, rhythm disturbance, transient ischemic changes on the ECG, coronary artery spasm, angina pectoris, myocardial infarction, hypotension, Raynauds disease .

From the respiratory system: shortness of breath.

From the digestive tract: nausea and vomiting that occur in some patients, but their relationship with the use of sumatriptan is not fully understood; ischemic colitis, diarrhea.

From the musculoskeletal system: a feeling of heaviness, myalgia. Induced symptoms are usually transient, can be intense in nature and affect any part of the body, including the chest and throat; stiff neck muscles, arthralgia.

From the side of the organs of vision: flicker, diplopia, decreased visual acuity, loss of vision (usually transient). However, visual impairment may be a consequence of a migraine attack itself.

On the part of the skin: hyperhidrosis.

General disorders: pain, a feeling of warmth or cold, constriction or tension (the above symptoms are usually transient, can be intense and affect any part of the body, including the chest and throat); a feeling of weakness, fatigue (the above symptoms are mainly mild or moderate in nature and are transient).

Laboratory indicators: slight changes in functional liver tests were observed.

Overdose.

Doses in excess of 400 mg (orally) did not cause any other side effects except those indicated above.

Treatment: conducting maintenance therapy and monitoring the patient for at least 10 hours.

The effect of hemodialysis or peritoneal dialysis on the level of Amigren in blood plasma has not been established.

Shelf life.

2 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °С.

Keep out of the reach of children.

Packaging.

1 capsule in a blister; 1 or 3 blisters in a box.

Vacation category.

On prescription.

Manufacturer.

LLC Astrapharm.

The location of the manufacturer and the address of the place of business.

Ukraine, 08132, Kiev-Svyatoshinsky borough, city of Cherry, st. Kiev, 6.