Imigran

Imigran is a drug for the treatment of migraines and is a selective agonist of serotonin 5HT1 receptors.

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Indications Imigran

The medicine is indicated for rapid pain relief during migraines (with or without aura).

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Release form

It is produced in tablets, 6 pieces per blister (1 blister per package with the medicine) or 2 pieces per blister (while the package contains 3 blister plates).

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Pharmacodynamics

Sumatriptan is a selective 5HT receptor agonist (1D), without affecting other 5HT receptors. These endings are located mainly inside the cranial vessels.

During experimental tests, it was found that sumatriptan has a selective vasoconstrictor effect on the vessels located within the carotid artery system, without affecting blood circulation in the brain. Through the carotid arteries, blood reaches intra- and extracranial tissues (for example, the meninges), the dilation of the vessels of which leads to the appearance of migraine.

Experimental tests have further revealed the inhibitory properties of the active ingredient in relation to the function of the trigeminal nerve. It is through these two mechanisms that sumatriptan exerts its anti-migraine effect.

The medicinal effect begins half an hour after oral administration of the drug (in the amount of 100 mg).

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Pharmacokinetics

When taken orally, the component is rapidly absorbed, reaching 70% of the peak level after 45 minutes. On average, the maximum plasma level at a dose of 100 mg is 45 ng / ml. The bioavailability level when taken orally is 14% (partly due to the presystemic exchange process, and partly due to incomplete absorption).

With plasma protein, synthesis is weak (14-21%), and the average level of distribution volume is 17 liters. The average total clearance is about 1160 ml/minute, and in the kidneys the average value is about 260 ml/minute.

Extrarenal clearance is approximately 80% of the total value, which allows sumatriptan excretion to be determined mainly in the form of breakdown products. The main one is the indoleacetic analogue of the active ingredient. It is excreted in the urine (in which it is determined as a free acid, as well as conjugated with the glucuronide substance) and has no 5HT1 or 5HT2 activity. Other breakdown products have not been identified.

The pharmacokinetic properties of orally administered sumatriptan change little during a migraine attack.

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Dosing and administration

It is forbidden to take pills as a preventive measure against an attack. It is also forbidden to exceed the recommended dosage.

The best time to take the pill is immediately after the attack begins, but the medicine will be effective at any stage.

Usually the medicine is prescribed in a dose of 50 mg (the size of 1 tablet). Sometimes it is allowed to increase the dosage to 2 tablets (100 mg).

If there is no effect, do not take a new dose during the same migraine attack. The next tablet can be taken only after the onset of a new attack.

If there is a reaction to the first dose, but with subsequent resumption of migraine manifestations, the 2nd tablet is allowed to be used over the next 24 hours, while the minimum interval between doses should be 2 hours. In total, no more than 300 mg of the drug can be taken per day (over 24 hours).

The tablets should be taken whole with water.

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Use Imigran during pregnancy

Prescribing to pregnant women is permitted only taking into account the possible assistance to the mother in relation to the risk of developing negative symptoms in the fetus.

It is known that when the active substance is administered subcutaneously, it penetrates into the mother's milk. The effect on the child can be reduced if the child is not breastfed for 12 hours after taking the medicine.

Contraindications

Among the contraindications of the drug:

• intolerance to the components of the drug;
• a history of myocardial infarction, as well as spontaneous angina pectoris, coronary heart disease, pathologies in the peripheral vascular area, or signs that are characteristic of coronary heart disease;
• a history of temporary cerebral circulatory disorder or stroke;
• severe or moderate increase in blood pressure or mild uncontrolled increase in blood pressure;
• severe stage of liver failure;
• taking it simultaneously with MAO inhibitors – it is allowed to start using Imigran at least 2 weeks after stopping taking the inhibitors;
• childhood and adolescence, since there is no information yet on the safety and effectiveness of the use of drugs in the above-described category of patients.

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Side effects Imigran

According to clinical trials, the following adverse reactions were identified:

• organs of the nervous system: a feeling of drowsiness or dizziness often occurs, as well as sensory disturbances (including hypoesthesia, as well as paresthesia);
• cardiovascular system organs: often a transient increase in blood pressure develops (immediately after taking the pill), as well as a rush of blood;
• respiratory system: dyspnea often occurs;
• digestive system: vomiting and nausea often developed in some patients, although a connection with drug use has not yet been established;
• connective tissue, muscles and skeleton: these manifestations are generally temporary, although they can be intense and affect different parts of the body (including the throat and sternum) - muscle pain or a feeling of heaviness often appears;
• general disorders: often there are painful sensations, a feeling of tension, compression, and also cold or heat (the manifestations are usually temporary, although sometimes they are intense and can affect different parts of the body (including the throat and sternum)). Often there is severe fatigue or a feeling of weakness (these manifestations are also temporary and usually have a moderate or mild degree of severity);
• test results: occasional minor changes in liver function test results.

Results of post-marketing studies:

• immunity: increased sensitivity (from skin reactions to cases of anaphylaxis);
• organs of the nervous system: occurrence of seizures. In some cases, such signs occurred in people with a tendency to seizures or with a history of conditions that could lead to such attacks; in addition, the development of dystonia, tremor, nystagmus or scotoma;
• visual organs: development of diplopia or flickering, deterioration of visual acuity, and also loss of vision (usually temporary). But such disorders can also occur due to the migraine attack itself;
• cardiovascular system organs: development of tachycardia, angina or bradycardia, increased heart rate, rhythm disturbances, temporary ischemic changes in ECG parameters, coronary vessel spasms, decreased blood pressure, myocardial infarction, Raynaud's syndrome;
• digestive organs: development of diarrhea or ischemic form of colitis;
• connective tissues, skeleton and muscles: joint pain, cervical radiculitis;
• mental disorders: feeling of excitement;
• subcutaneous tissues and skin: development of hyperhidrosis.

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Overdose

When oral doses exceeding 400 mg were used, only symptoms of adverse reactions occurred. In case of overdose, it is necessary to observe the patient for at least 10 hours, while carrying out standard supportive procedures.

There is no information on the impact of peritoneal dialysis or hemodialysis procedures on the parameters of the active component of the drug.

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Interactions with other drugs

There is no information on the interaction of the drug with alcoholic beverages, as well as flunarizine, propranolol, and pizotifen.

There is limited information on the combined use with drugs containing ergotamine or other triptan/5-HT1 receptor agonists. In theory, a prolonged vasospastic effect may develop, which is why combining such drugs is prohibited. It is not known how long the interval between doses of these drugs should be - it depends on the type of drugs and their dosages. Since the properties of ergotamine and triptan/5-HT1 receptor agonists may be enhanced by Imigran, a 24-hour interval must be observed before taking the latter.

At the same time, medications containing ergotamine are prohibited for use within 6 hours after taking Imigran, and triptan/5-HT1 receptor agonists are prohibited for use within 24 hours after taking Imigran.

There are isolated post-marketing reports of patients developing serotonin intoxication (manifestations include neuromuscular disorders, mental changes, and visceral instability) when combining the drug with selective serotonin reuptake inhibitors. There are also reports of the above-mentioned pathology occurring when triptans are combined with norepinephrine and serotonin reuptake inhibitors.

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Storage conditions

The medicine is stored in a place closed to children, in standard conditions for medicines. Temperature – no more than 30°C.

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Shelf life

Imigran is permitted to be used for 3 years from the date of manufacture of the drug.