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

Components	amount
	50 mg / tab.	100 mg / tab.
*Core tablet (mg / tablet)*
Active substance
Sumatriptan succinate	70,00	140,0
(equivalent to sumatriptan)	50,00	100,00
Excipients
Lactose Monohydrate	70,00	140,0
Lactose anhydrous	140,0	-
Microcrystalline cellulose	15,5	15,5
Sodium croscarmellose	3,0	3,0
Magnesium stearate	1,25-1,75	1,25-1,75
Mass of the core	299.75-300.25 mg	299.75-300.25 mg
The theoretical weight of the tablet (s	306.6 mg	306.6 mg
shell)
*Casing of the tablet*
Pick up pink YS-1-1441-G	6,6
Methylhydroxypropylcellulose	4,06
Titanium dioxide	1,93
Triacetin	0,6
Iron oxide red	0,01
Drop off white OY-S-7393		6,6
Titanium dioxide		1,0
Methylhydroxypropylcellulose		5,6

Description:

For a dosage of 50 mg: pink oval, biconvex tablets, covered with a shell, engraved with the inscription "50" on one side and a level surface on the other.

For a dosage of 100 mg: white or almost white, oval, biconvex tablets covered with a shell, engraved with the inscription "100" on one side and a level surface on the other.

Pharmacotherapeutic group:Anti-migraine means

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

Mechanism of action

Sumatriptan-selective agonist of vascular 5-hydroxytryptamine-1 receptors (5-HT₁D), does not affect other 5-HT receptor subtypes (5-HT₂-5-HT₇). Receptors _5-_HT₁_D are located mainly in the cranial blood vessels of the brain, and their stimulation leads to narrowing of these vessels.

In animals sumatriptan selectively acts on the vasoconstriction of the branches of the carotid artery, without affecting the blood flow in the vessels of the brain. The vascular carotid artery pool supplies extracranial and intracranial tissues (including meningeal membranes), and it is believed that the expansion of these vessels and / or edema of their walls is the main mechanism of migraine in man.

In addition, experimental data make it possible to judge that sumatriptan reduces the sensitivity of the trigeminal nerve. Both these effects can underlie the anti-migraine effect of sumatriptan.

The clinical effect is usually seen 30 minutes after oral intake of 100 mg of the drug.

Although the recommended dose for oral administration is 50 mg, migraine attacks vary in severity in both the patient and in different patients. Doses of 25 mg to 100 mg showed greater efficacy compared with placebo in clinical studies, but a 25 mg dose was statistically significantly less effective than 50 mg and 100 mg.

Sumatriptan has demonstrated efficacy in the treatment of migraine attacks, including menstrual-associated migraine.

Pharmacokinetics:

The migraine attacks do not have a significant effect on the pharmacokinetics of sumatriptan taken internally.

Suction

After oral administration sumatriptan quickly absorbed, 70% of the maximum plasma concentration is achieved after 45 minutes. After taking a dose of 100 mg, the average value of the maximum concentration in the blood plasma is 54 ng / ml. Average the absolute bioavailability is 14% partly due to presystemic metabolism, in part because of incomplete absorption.

Distribution

Sumatriptan binds to plasma proteins to an insignificant extent (14-21%), the average total volume of distribution is 170 liters.

Metabolism

The main metabolite, an indoleacetic analogue of sumatriptan, is excreted mainly in the urine, in the form of free acid and a glucuronide conjugate. This metabolite has no activity with respect to 5-HT₁ and 5-HT₂-serotonin receptors. Secondary metabolites of sumatriptan were not detected.

Excretion

The half-life is approximately 2 hours. The average total plasma clearance is approximately 1160 ml / min, the average renal clearance is approximately 260 ml / min, the extra-neural clearance is about 80% of the total clearance.

Sumatriptan is metabolized by the action of monoamine oxidase A.

Special patient groups

Patients with impaired hepatic function

Due to the decrease in the presystem clearance of sumatriptan in patients with impaired liver function, the content of sumatriptan in blood plasma increases.

An assessment was made of the effect of moderate hepatic impairment (class B on the Child-Pugh scale) on the pharmacokinetics of sumatriptan when administered subcutaneously. There were no significant differences in the pharmacokinetics of sumatriptan for subcutaneous administration in patients with moderate impairment of liver function compared to healthy controls in the control group.

Indications:Coping migraine attacks with or without an aura, including episodes of menstrual-associated migraine.

Contraindications:

- Hypersensitivity to any of the components that make up the drug;

- hemiplegic, basilar and ophthalmoplegic forms of migraine;

- ischemic heart disease (IHD) (including myocardial infarction, postinfarction cardiosclerosis, Prinzmetal angina), as well as symptoms suggesting the presence of IHD;

- Occlusal diseases of peripheral vessels;

- stroke or transient ischemic attack (including in anamnesis);

uncontrolled arterial hypertension;

- administration simultaneously with ergotamine or its derivatives (including metisergid) or other tryptans / agonists of 5-HT1 receptors;

- use on the background of monoamine oxidase (MAO) inhibitors or earlier than 2 weeks after the withdrawal of these drugs;

- severe degree of impaired liver and / or kidney function;

- age to 18 years and over 65 years (safety and efficacy of the drug Imigran is not established).

Carefully:

- Controlled arterial hypertension;

- diseases in which the absorption, metabolism or excretion of this drug can 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 sulfanilamides (taking sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations of hypersensitivity to anaphylaxis). Data on cross-sensitivity are limited, but caution should be exercised when using sumatriptan in such patients;

- in patients with lactase deficiency, galactose intolerance and glucose-galactose malabsorption (the preparation contains lactose).

Pregnancy and lactation:

Pregnancy

The use of sumatriptan in pregnancy is possible only if the intended benefit to the mother exceeds the possible risk to the fetus.

The data of post-registration observation of more than 1000 women who received Imigran during the first trimester of pregnancy are available. Due to insufficient information, it is premature to make final conclusions about increasing the risk of congenital malformations. The experience of using the drug in women in the II and III trimesters of pregnancy is limited.

The evaluation of experimental animal studies did not show a direct teratogenic or adverse effect on prenatal and postnatal development. However, rabbits had an effect on the viability of the embryo and fetus.

Breastfeeding period

It has been shown that after subcutaneous administration sumatriptan excreted in breast milk. Effects on the newborn can be minimized if avoiding breastfeeding for 12 hours after taking the drug.

Dosing and Administration:

The preparation of Imigran should not be prescribed as a prophylaxis. Do not exceed the recommended dose of Imigran.

It is recommended to start taking Imigran immediately, with the first signs of a migraine attack, while the preparation of Imigran is equally effective when applied at any stage of the migraine attack.

The drug is used inside, swallowing the tablet whole and washing down with water.

Adults

The recommended dose is 50 mg (1 tablet). Some patients may require a dose of 100 mg.

If, after taking the first dose, a migraine attack is not stopped, the second dose of the drug to stop the same migraine attack should not be prescribed. In such cases, to stop the attack, you can apply paracetamol, acetylsalicylic acid or NSAIDs. However, the preparation of Imigran can be used to stop subsequent migraine attacks.

If the patient feels better after the first dose of the drug and then the symptoms resume, a second dose can be taken, provided that the interval between doses is at least 2 hours, and no more than 300 mg is taken within a 24-hour period.

Sumatriptan can be used no earlier than 24 hours after taking medications containing ergotamine; and vice versa, preparations containing ergotamine can be used no earlier than 6 hours after taking sumatriptan.

Special patient groups

Children and teenagers (under the age of 18)

The effectiveness of Imigran in this group of patients has not been demonstrated.

Patients of advanced age (over 65 years)

The experience of using the drug Imigran in patients older than 65 years is limited. The pharmacokinetics in patients in this population do not significantly differ from those in younger patients, but until additional clinical data are obtained, the use of sumatriptan in patients older than 65 years is not recommended.

Side effects:

The undesirable reactions presented below are listed in accordance with the damage to organ systems and frequency of occurrence. The frequency is defined as follows: Often (> 1/10); often (> 1/100 and <1/10); infrequently (> 1/1000 and <1/100); rarely (> 1/10 000 and <1/1000); rarely (< 1/10 000); unknown (the frequency can not be estimated from available data).

Clinical Trials Data

Frequency of occurrence of undesirable reactions

Disturbances from the nervous system

Often: dizziness, drowsiness, sensitivity disorders (including paresthesia and decreased sensitivity).

Vascular disorders

Often: a transient increase in blood pressure (soon after taking the drug), hot flashes.

Disturbances from the respiratory system, chest and mediastinal organs

Often: shortness of breath.

Disorders from the gastrointestinal tract

Often: nausea, vomiting (cause and effect of the occurrence of unwanted reactions with taking the drug is not proven).

Disturbances from musculoskeletal and connective tissue

Often: a sense of heaviness (usually transient, can be intense and occur in any part of the body, including the thorax and throat).

General disorders and disorders at the site of administration

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), weakness, fatigue (usually mild or moderate, transitory).

Laboratory and instrumental data

Very rare: minor deviations in liver function tests.

Post-registration data

Frequency of occurrence of undesirable reactions

Immune system disorders

It is not known: hypersensitivity reactions that vary from skin manifestations of hypersensitivity to anaphylaxis.

Disturbances from the nervous system

It is not known: convulsive seizures (in a number of cases, observed in patients with convulsive attacks in the anamnesis or with concomitant conditions predisposing to the occurrence of seizures, some patients did not have risk factors), tremor, dystonia, nystagmus, scotoma.

Disturbances on the part of the organ of sight

Unknown: flickering, diplopia, decreased visual acuity. Loss of vision (usually transient). However, visual disturbances can be caused by the actual migraine attack.

Heart Disease

Unknown: bradycardia, tachycardia, palpitations, arrhythmias, ECG signs of transient myocardial ischemia, coronary vasospasm, angina pectoris, myocardial infarction.

Vascular disorders

Unknown: lowering blood pressure, Raynaud's syndrome.

Disorders from the gastrointestinal tract

Unknown: ischemic colitis, diarrhea.

Disturbances from musculoskeletal and connective tissue

Unknown: stiff neck, arthralgia.

Disorders of the psyche

Unknown: alarm.

Disturbances from the skin and subcutaneous tissues

Unknown: hyperhidrosis.

Overdose:Symptoms

Administration of the drug Imigran orally in a dose of more than 400 mg did not cause any undesirable reactions, in addition to those listed above.

Treatment

In case of an overdose, patients should be monitored for at least 10 hours and, if necessary, symptomatic therapy should be performed. There is no data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in 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.

There are limited data on the interaction with preparations containing ergotamine or other tryptans / agonists of 5-HT1 receptors. Theoretically, an increased risk of coronary vasospasm, and the joint use of these drugs is contraindicated.

The time period that must elapse between the use of sumatriptan and ergotamine-containing drugs or another tryptane / 5-HT1 receptor agonist is unknown.It will depend, inter alia, on the dose and type of prescription drugs. The action can be additive. It is recommended to wait at least 24 hours after using drugs containing ergotamine or another tryptan / agonist of 5-HT1 receptors before applying sumatriptan. Conversely, it is recommended to wait at least 6 hours after applying sumatriptan before using ergotamine-containing drugs and at least 24 hours before using another tryptane / 5-HT1 agonist receptor.

Possible interaction between sumatriptan and MAO inhibitors, their simultaneous use is contraindicated.

There are rare reports obtained as a result of post-registration observation of the development of serotonin syndrome (including psychiatric disorders, autonomic lability and neuromuscular disorders) as a result of the simultaneous use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Also, the development of serotonin syndrome was reported with the simultaneous use of tryptanes with selective serotonin and noradrenaline reuptake inhibitors (SSRIs).

Special instructions:

The preparation of Imigran should be prescribed only if the diagnosis of migraine is not in doubt.

The preparation of Imigran is contraindicated for use in hemiplegic, basilar and ophthalmoplegic forms of migraine.

Before starting treatment with Imigran it is necessary to exclude the types of potentially dangerous neurological pathology (for example, stroke, transient ischemic attacks) in case the patient has atypical symptoms or when the patient does not have a condition requiring the use of Imigran.

After taking Imigran, transient symptoms can occur, including pain and chest tightness, which can be intense and spread to the neck area. If there is reason to believe that these symptoms are a manifestation of CHD, it is necessary to conduct an appropriate diagnostic examination.

Do not use Imigran in patients with risk factors for developing coronary artery disease, including those with malignant smokers or users of nicotine replacement therapy, without a preliminary examination of the cardiovascular system.Particular attention should be given to women in the postmenopausal period and men over the age of 40 with these risk factors. However, the examination does not always make it possible to identify heart disease in each patient. In very rare cases, serious adverse cardiovascular reactions may occur in patients who have not had a history of cardiovascular disease.

The preparation of Imigran should be used with caution in patients with controlled hypertension, as in a small number of patients there was a transient increase in arterial pressure and peripheral vascular resistance.

There are rare reports obtained as a result of post-registration observation of the development of serotonin syndrome (including psychiatric disorders, autonomic lability and neuromuscular disorders) as a result of simultaneous use of SSRIs and sumatriptan. Also, the development of serotonin syndrome was reported against the background of the simultaneous use of triptans with SSRIs.

In the case of simultaneous use with drugs from the SSRIs and / or SSRIs, the patient's condition should be carefully monitored.

The simultaneous use of any tryptane (5-HT1 agonist) with sumatriptan is not recommended.

The drug Imigran should be used with caution in patients who may significantly change absorption, metabolism or excretion of sumatriptan, for example, in patients with impaired renal or hepatic function (class A or B on the Child-Pugh scale).

The preparation of Imigran should be used with caution in patients who have a history of seizures or who have other risk factors for reducing the threshold of convulsive readiness.

In patients with an increased susceptibility to sulfanilamides, taking Imigran can cause allergic reactions, which range from skin manifestations of hypersensitivity to anaphylaxis. Data on cross-sensitivity are limited, but one should be vigilant before using Imigran in such patients.

Undesirable reactions may occur more often during the simultaneous use of triptans and herbal preparations containing Hypericum perforatum (Hypericum perforatum).

Abuse of medicines intended for relief of acute headache,is associated with increased headaches in sensitive patients (headache associated with drug abuse). In this case, the possibility of drug cancellation should be considered.

Effect on the ability to drive transp. cf. and fur:In patients with migraine, there may be drowsiness associated with both the disease itself and with the drug Imigran. Patients should be especially careful when driving and working with moving machinery.

Form release / dosage:

Tablets coated with a coating, 50 mg and 100 mg.

Packaging:

2 tablets in an A1 / A1 blister or 2 tablets in a cold-formed foil blister (PVC / Al / PA) and a cover foil (paper / Al). 1 blister with instructions for use in a cardboard package.

Storage conditions:Store below 30 ° C. Keep out of the reach of children.

Shelf life:3 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011752 / 01

Date of registration:18.05.2010 / 26.07.2016

Expiration Date:Unlimited

The owner of the registration certificate:GlaxoSmithKline Trading, ZAO GlaxoSmithKline Trading, ZAO Russia

Manufacturer: & nbsp

GlaxoSmithKline Pharmaceuticals, S.A. Poland

Representation: & nbspGlaxoSmithKline Trading, ZAOGlaxoSmithKline Trading, ZAO

Information update date: & nbsp08.11.2017

Illustrated instructions

Instructions

Imigran® (Imigran®)