Expiration date: 02/2022
The composition and form of issue:
Tablets, film-coated. 1 tablet contains:
sumatriptan (sumatriptan succinate) 50 or 100 mg
excipients: lactose monohydrate lactose anhydrous microcrystalline croscarmellose sodium magnesium stearate coating on the aspirin: dosage 50 mg — Opadry pink YS-1-1441-G metilgidroksipropilzelluloza titanium dioxide triacetin iron oxide red for dosing 100 mg — Opadry white OY-S-7393 titanium dioxide metilgidroksipropilzelluloza
in blister 2 PCs. in a box 1 blister.
Spray for nasal use. 1 dose contains:
sumatriptan 10 or 20 mg
excipients: potassium phosphate odnosemjannyj sodium disodium phosphate anhydrous sulphuric acid sodium hydroxide purified water
in disposable vials with a metering device in box 1 or 2 bottles.
Description pharmaceutical form:
50 mg tablets: pink, oval biconvex coated tablet engraved with "IMIGRAN" on one side and "50" on the other (or smooth on one side and engraved "50" on the other). The dimensions of the tablets: 12×6,5 mm. At the break you can see two layers: the inner layer (core tablets) is a white or almost white outer layer (shell tablet) — pink.
Tablets 100 mg: white or almost white, oval biconvex coated tablet engraved with "GLAXO" on one side and "IMIGRAN" on the other (or smooth on one side and engraved "100" on the other). The dimensions of the tablets: 12×6,5 mm. At the break of the tablet white, or almost white.
Nasal spray: transparent liquid from light yellow to dark yellow.
Selective agonist of 5-HT1 receptors (5-HT1D).
Interacts with 5-HT1 receptors (no effect on 5-HT2 — 5-HT7 receptor subtypes), mainly in the blood vessels of the brain (their stimulation leads to narrowing of blood vessels).
Sumatriptan is rapidly absorbed after ingestion and after intranasal. The ingestion 70% of the Cmax in plasma is reached after 45 min, when taken in a dose of 100 mg Cmax in the plasma is, on average, 54 ng/ml After intranasal C Max in plasma achieved through 1-1. 5 h is 12.9 ng/ml.
Average absolute bioavailability when administered at 14% due to presystemic metabolism and incomplete absorption. Due to first-pass metabolism average absolute bioavailability in intra application is 15.8% of the one when s/to the introduction. In patients with hepatic impairment should expect higher levels of sumatriptan in plasma by reducing presystemic clearance.
The degree of binding with plasma proteins is small (14-21%), the total volume of distribution averages 170 l, T1/2 — approximately 2 hours Total plasma Cl averages 1160 ml/min, kidney Cl — 260 ml/min, vnepochechny klirens — about 80% of total clearance.
In adolescents (12-17 years) average Cmax in plasma is 13.9 ng/ml, the average T1/2 about 2 h in adolescents with overweight there is an increase in clearance and volume of distribution of a preparation, therefore at a lower body mass they have a higher exposure of sumatriptan.
The main mechanism of elimination of sumatriptan is oxidative metabolism, which is under the action of the enzyme MAO type A. the Main metabolite indelicacy analogue of sumatriptan is mainly excreted in the urine, where it is in the form of the free acid and glucuronide conjugate. This metabolite has no activity against 5-HT1 or 5-HT2-receptors. Secondary metabolites have not been identified. Migraine attacks, apparently, do not have a significant effect on the pharmacokinetics of sumatriptan taken orally or intranasally.
Description pharmacological action:
In animals sumatriptan selectively constricts blood vessels in the system of carotid arteries, but does not alter cerebral blood flow. It is believed that the expansion of the blood vessels and/or swelling of the wall is the main mechanism of migraines in humans. In addition, it is experimentally established that sumatriptan inhibits trigeminal nerve activity. Both of these effects can be the basis protivomigrenoznogo of sumatriptan.
The clinical effect observed 30 min after oral administration at a dose of 100 mg and 15 minutes after intranasal administration.
Relief of migraine attacks (with aura or without it).
Hypersensitivity hemiplegic, basilar, and oftalmologicheskiy forms of migraine myocardial infarction (including history) coronary artery disease or suspected of being present, Prinzmetal's angina peripheral vascular disease transient violation of cerebral circulation (including in history) stroke (including in history) uncontrolled hypertension severe violation of the liver and/or kidney simultaneous reception Imigran with ergotamine or its derivatives (including metisergid), as well as the simultaneous admission of MAO inhibitors and the period up to 2 weeks after their withdrawal.
With caution in: epilepsy (including any condition with reduced seizure threshold), hypertension (controlled), pregnancy, lactation, age to 18 years (safety and effectiveness are not installed), age older than 65 years.
Application of pregnancy and breast-feeding:
Pregnant women Imigran can be assigned only in the case when the expected benefit to the mother outweighs the potential risk to the fetus. You should avoid breastfeeding for 24 hours after sumatriptan.
Common symptoms: pain, tingling, sensation of heat, sensation of pressure or gravity (these symptoms are usually transient but may be intense and occur in any part of the body including chest and throat), flushing, dizziness, feeling of weakness and/or tiredness, drowsiness (usually slightly or moderately expressed and are transient in nature).
From the side of cardiovascular system: arterial hypotension, bradycardia, tachycardia (including ventricular), palpitations, temporary increase in blood pressure (observed soon after administration of sumatriptan) there are rare reports of cardiac arrhythmias (up to fibrillation), transient ECG changes, ischemic-type, myocardial infarction, spasm of the coronary arteries sometimes develop Raynaud's syndrome.
The gastro-intestinal tract: some patients have nausea and vomiting (these side effects with the intake of sumatriptan has not been established) a slight increase in liver enzymes, dysphagia, discomfort in the abdomen rarely — ischemic colitis.
CNS and organ: there are some rare reports of convulsive seizures after taking sumatriptan. In some cases they were observed in patients with a history of seizures or with conditions predisposing to the occurrence of seizures in some patients predisposing factors have been identified. Sometimes after taking Imigran noted diplopia, flashing in the eyes, nystagmus, scotoma, reduced visual acuity. Rarely developed transient partial loss of vision. However, it should be borne in mind that visual disturbances can be associated with the very attack of migraine.
Hypersensitivity reactions: cutaneous manifestations (rash, urticaria, pruritus, erythema) to rare cases, anaphylaxis.
Local symptoms (when applying spray): slight transient irritation or burning sensation in the nose or throat, nasal bleeding.
Not observed interaction of sumatriptan with propranolol, flunarizine, pizotifen and ethyl alcohol. While concurrent use with ergotamine was noted prolonged spasm of the blood vessels (sumatriptan may be administered no earlier than 24 h after administration of drugs, containing ergotamine, products containing ergotamine, you can assign no earlier than 6 h after administration of sumatriptan). Perhaps the interaction between sumatriptanom and MAO inhibitors, counter their simultaneous use.
There are separate reports on the development of weakness, hyperreflexia and poor coordination of a patient after simultaneous administration of sumatriptan and drugs from the group of selective inhibitors of serotonin reuptake (SSRIs). In the case of co-administration of sumatriptan and SSRIs should carefully monitor the patient's condition.
Method of application and dose:
Inside, intranasal. Imigran is recommended to apply as early as possible after the start of a migraine attack, but it is equally effective when used at any stage of the attack.
Inside (tablet swallow whole with water), adults: the recommended dose is 1 tablet, 50 mg (some patients may require higher dose of 100 mg).
Intranasal, adults (18 years and older) 20 mg (1 dose) Imigran spray one half of the nose. It should be remembered that absorption of sumatriptan and migraine attacks and clinical manifestations may vary not only among different patients but also in one and the same patient, therefore, may be effective dose of 10 mg.
If the migraine symptoms do not disappear or shrink after the first dose Imigran (regardless of method of application), the acceptance of a second dose for the relief of this attack should not be assigned. However, Imigran is possible to apply for subsequent relief of migraine attacks. If the patient felt improvement after the first dose, then the symptoms resumed, you can take a second dose within the next 24 hours the Maximum dose Imigran should not exceed 300 mg for any 24-hour period (ingestion), or two doses Imigran at 20 mg (with intranasal use).
Imigran reception inside in a dose of 400 mg or a single p/to the introduction in the dose of 16 mg or introduction Imigran a single dose of 40 g intranasally did not cause any side effects other than those listed above.
Treatment: monitoring of patients not less than 10 hours, if necessary, standard supportive treatment. No data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in plasma.
Imigran should not be used in prophylactic purposes. The drug should be prescribed only if diagnosis is not in doubt. As the use of other protivomigrenozhnykh of funds, the appointment Imigran in patients with previously diagnosed migraine or in patients with atypical migraine to exclude other potentially serious neurological conditions. Note that patients with migraine increased risk of certain cerebrovascular disorders (e.g. stroke or transient ischemic stroke).
Sumatriptan should not be prescribed to patients with presumed heart disease without prior examination to exclude cardiovascular disease. Such patients include women in post-menopausal stages, men over the age of 40 years and patients with risk factors for coronary heart disease. Although the survey is not always possible to detect heart disease in some patients, in very rare cases they develop side effects from the cardiovascular system. After taking the sumatriptan may arise simply intense pain and tightness in the chest, extending to the neck. If there is reason to believe that these symptoms are a manifestation of CHD, it is necessary to conduct appropriate diagnostic tests.
Patients with controlled hypertension, sumatriptan should be administered with caution, because in some cases there was observed a transient increase in blood pressure and peripheral vascular resistance.
In case of simultaneous appointment with drugs from the group of SSRIs should carefully monitor the patient's condition.
You should be wary of sumatriptan in patients suffering from such diseases, which can significantly change the absorption, metabolism or excretion of the drug (e.g. impairment of renal function or liver). Care must be taken in patients with the history of epilepsy or structural brain damage that reduce the seizure threshold.
In patients with hypersensitivity to sulfonamides introduction of sumatriptan can cause allergic reactions that range from cutaneous manifestations to anaphylaxis. Data on cross-sensitivity is limited but caution should be exercised in the appointment of sumatriptan to these patients.
Clinical experiences Imigran in patients of elderly age (over 65 years) is limited. There are no significant differences in pharmacokinetic indices of sumatriptan in elderly and younger patients, but until more clinical research data is not recommended Imigran patients older than 65 years.
Patients with migraine may experience drowsiness, associated both with the disease and receiving Imigran, so they must be especially careful when driving and working with moving machinery.
Do not exceed the recommended dose Imigran.