IMIGRAN

Active material: Sumatriptan
When ATH: N02CC01
CCF: Serotoninovыh agonist 5-HT₁-receptors. Protivomigrenoznoy drug with activity
ICD-10 codes (testimony): G43
When CSF: 02.16.05.01
Manufacturer: GlaxoSmithKline s. p. a.. (Italy)

Pharmaceutical form, composition and packaging

Spray nazalynыy in the form of clear liquid from yellow to dark yellow color.

Excipients: potassium phosphate monosubstituted, sodium phosphate dibasic anhydrous, sulfuric acid, Sodium hydroxide, Purified water.

Disposable dispensers (1) – blisters (1) – packs cardboard.

Spray nazalynыy in the form of clear liquid from yellow to dark yellow color.

Excipients: potassium phosphate monosubstituted, sodium phosphate dibasic anhydrous, sulfuric acid, Sodium hydroxide, Purified water.

Disposable dispensers (1) – blisters (1) – packs cardboard.

Pharmacological action

Protivomigrenoznoy drug with activity. Agonist of serotonin 5HT_1D-receptors. Does not affect other subtypes of receptor 5NT (5HT₂– 5HT₇). 5HT_1D-receptors are located, mainly, in the blood vessels of the brain, and their stimulation leads to narrowing of these vessels. Vascular Carotid extracranial krovosnabzhaet pool and intrakranialnye fabrics (incl. meningeal sheath), and is considered to be, that expansion of these vessels and/or swelling of the wall is the main mechanism of migraines in humans. Reduces the sensitivity of the trigeminal nerve. Both of these effects can be the basis of the action protivomigrenoznogo sumatriptan.

Clinical effect noted usually through 30 minutes after intranasal application preparation.

Pharmacokinetics

Absorption and distribution

After intranasal rapidly absorbed, C_max Plasma is 12.9 ng / ml achieved after 1-1.5 no. Due to presistemnogo metabolism, the average absolute bioavailability in intra application product is 15.8% from the p/to the introduction.

Plasma protein binding – 14-21%, the average total V_d is 170 l.

Metabolism and excretion

T_1/2 – about 2 no. The average total plasma clearance averages 1160 ml / min, renal clearance – 260 ml / min, nepochechnyj clearance – about 80% of the total clearance.

The main mechanism for deducing of sumatriptan is oxidative metabolism, which is carried out under the action of the enzyme MAO type a. The main metabolite – indoluksusnyj analogue of sumatriptan – excreted mainly in the urine, where it is in the form of free acid and conjugate sulfatnogo glukuronidnyi. This metabolite has no activity relative to 5NT₁– or 5NT₂-Receptor. Secondary metabolites are identified.

Migraine attacks have no significant effect on the pharmacokinetics of sumatriptan, applied intranasally.

Pharmacokinetics in special clinical situations

In patients with impaired liver should expect increasing levels of sumatriptan in plasma as a result of lower presistemnogo ground clearance.

Testimony

-cupping the migraine with aura or without it.

Dosage regimen

The drug is prescribed for 20 mg (1 dose) in each nostril.

It should be remembered, that removals of sumatriptan and migraine attacks in strength and clinical manifestations may vary not only in different patients, but the same patient, It is therefore quite effective dose may be 10 mg. If after the first dose of a migraine attack are not docked, a second dose of the drug to short the same migraine attack should not appoint. However, you can apply for knocking over Imigran subsequent bouts of migraine.

If the patient felt improvement after the first dose of the drug, and then resumed symptoms, during the following 24 h, you can enter a second dose provided, that the interval between doses is not less than 2 no. During the 24-hour period, you can enter the intranasal no more 2-x doses Imigrana on 20 mg.

Instructions for use nasal spray

Nasal spray consists of the following parts.

1.Tip.

2.Finger clip.

3. Blue button. The button is triggered only once, Therefore, you should not click on it, until the tip is not entered in the bow, otherwise the entire dose disappears.

The patient should take comfortable position (You can sitting). Preliminary it is necessary to clean the nasal cavity. Remove the blister and pull the nasal spray. Do not press the blue button. What follows is hard pressed one nostril with your finger to the nasal septum, breathe calmly through the mouth. Insert the tip into the other nostril approx. 1 cm. Not zaprokidawati head, close mouth. Make a quiet breath through the nose and simultaneously to press the blue button with your thumb.

Button may seem a bit tight. The patient may hear a faint clicking. Open your mouth and breathe calmly through the mouth. Not zaprokidawati head. Make calm breaths through the nose, and exhale through your mouth during 10-20 sec. Do not breathe deeply. After using the drug, the patient can feel the appearance of moisture in the nasal cavity and a weak taste (These feelings are not dangerous and are spontaneously). After a single use of the dispenser should be thrown away.

Side effect

Unwanted reactions listed depending on the anatomic-physiological classification and incidence. Frequency is defined as follows:: Often (>1/10), often (>1/100 and <1/10), sometimes (>1/1000 and <1/100), rarely (>1/10 000 and <1/1000), rarely (<1/10 000), including individual cases. Data were evaluated clinical studies, It must be borne in mind, the incidence of adverse reactions against the backdrop of the admission of drugs did not take into account comparisons. Also take into account the postmarketing data.

Clinical studies

From the nervous system: often, dizziness, drowsiness, sensory disturbances, including paresthesias and decrease in sensitivity.

Cardio-vascular system: often – transient increase of HELL (shortly after taking the drug), tides.

The respiratory system: often – breathlessness, lung, transient stinging or irritation in the nasal cavity or throat, nose bleed.

From the digestive system: often – nausea, vomiting (a causal link is not proved); rarely – minor variations in liver samples.

Common reactions: often – pain, feeling cold or heat, a feeling of pressure or tension (usually transient, can be intense and occur in any part of the body, including the chest and throat), weakness, fatiguability (usually slightly or moderately expressed, transient).

Other: often – feeling of weight (usually transient, can be intense and occur in any part of the body, including the chest and throat).

Postmarketingovoe monitoring

From the nervous system: rarely – seizures (in some cases observed in patients with convulsive seizures in history or when accompanying conditions, predisposing to seizures; some patients risk factors have been identified), tremor, dystonia, nistagmo.

On the part of the organ of vision: rarely – twinkle, diplopia, reduced visual acuity, scotoma, blindness (usually passing). Disorder can be caused by actual attack of migraine.

Cardio-vascular system: rarely – bradycardia, tachycardia, flutter, Arrhythmia, Transient changes in the ECG, Coronary Vasospasm is, angina, myocardial infarction, hypotension, Raynaud's syndrome.

From the digestive system: rarely – ishemicheskiy colitis, dysphagia, abdominal discomfort.

Allergic reactions: rarely – hypersensitivity reactions, including skin manifestations, as well as anaphylaxis.

Contraindications

- Hemiplegic, basilar migraine and oftalmoplegicheskaya form;

- CHD (incl. myocardial infarction, postinfarktnыy kardioskleroza, Prinzmetal angina), as well as the presence of symptoms, to suggest the presence of ISCHEMIC HEART DISEASE;

- Occlusive peripheral vascular disease;

— stroke and transient ischemic attack (incl. history);

- Uncontrolled hypertension;

— expressed by the liver and/or kidney disease;

-simultaneous reception with ergotaminom or its derivatives (including methysergide);

— the simultaneous admission of MAO inhibitors or earlier, than 2 a week after the cancellation of these drugs;

- Pregnancy;

age of the patient to 18 and older 65 years;

— idiosyncrasy to any component of the drug.

FROM caution should designate product in epilepsy (incl. under any conditions with declining threshold sudorojna preparedness), hypertension (controlled), lactation (breast-feeding did not previously, than 24 h after dosing).

Pregnancy and lactation

The drug is contraindicated in pregnancy.

FROM caution should be used during lactation (breast-feeding did not previously, than 24 h after dosing).

Cautions

Imigran should appoint only, If the diagnosis of migraine is not in doubt.

You cannot use the drug as a preventive measure.

In patients not previously diagnosed with migraine or in patients with atypical migraine to exclude other neurological pathology. It should be noted, that patients with migraine increased risk of cerebrovascular violations identified (eg, stroke or transient ischemic attack).

After taking Sumatriptan may experience temporary pain and tightness in the chest, extending to the neck area. If there is reason to believe, that these symptoms are a manifestation of ISCHEMIC HEART DISEASE, There is a need to conduct appropriate diagnostic examination.

Should not be prescribed to patients at risk of cardiovascular pathology without preliminary survey with a view to its exclusion (in postmenopausal women, men over the age of 40 years and patients with risk factors for coronary heart disease). The survey does not always provide heart disease in some patients. In very rare cases, patients may cause serious adverse reactions on the part of the cardiovascular system, in history which has not been observed cardiovascular pathology.

The drug should be administered with caution to patients with controlled hypertension, tk. in some cases, there has been a tranzithornoe ad and ROUND; in patients with diseases, where can significantly vary the absorption, metabolism or excretion of Imigran (eg, renal failure or liver).

There are very rare posts, obtained through post-marketing surveillance, on the development of serotonin syndrome (including mental illness, Autonomic lability and neuromuscular violation) as a result of
concomitant use of selective serotonin reuptake inhibitors and sumatriptan. It was also reported on the development of serotonin syndrome amid simultaneous appointment triptanov with selective inhibitors of reverse takeover serotonin and norepinephrine. In the case of a simultaneous appointment with drugs from the Group should carefully the condition of the patient. Imigran should use caution in patients with epilepsy or organic brain disorder with declining threshold sudorojna preparedness.

Concomitant use of other triptanov/5-NT₁-agonists with sumatriptanom is not recommended.

In patients with hypersensitivity to sulfanilamidam admission Imigrana can cause allergic reactions, which vary from skin manifestations to anaphylaxis. Data on cross-sensitivity are limited, However, caution must be exercised in the appointment Imigrana such patients.

Abuse of drugs, intended for cupping the migraines, associated with increased headaches in sensitive patients (headache, associated with the abuse of drugs). You should consider the preparation.

Do not exceed the recommended dose Imigrana.

Overdose

Introduction in one dose Imigrana 40 g route did not cause any side effects, In addition to the above.

Treatment: monitor the status of patients at least 10 h and, if necessary, symptomatic therapy. No data on the effect of hemodialysis or peritoneal dialysis on plasma concentrations of sumatriptan.

Drug Interactions

There has been interaction with sumatriptan propranololom, flunarizinom, pizotifenom and ethanol.

When concomitantly with ergotamine long vasospasm observed. Sumatriptan may be nominated not earlier, than 24 hours after ingestion, containing ergotamine; and vice versa, preparations, containing ergotamine, It can be administered no earlier than, than 6 hours after administration of sumatriptan.

Interoperability between sumatriptan and MAOIs, their concurrent use is contraindicated.

There are very rare posts, obtained through post-marketing surveillance, on the development of serotonin syndrome (including mental illness, Autonomic lability and neuromuscular violation) as a result of
concomitant use of selective serotonin reuptake inhibitors and sumatriptan. It was also reported on the development of serotonin syndrome amid simultaneous appointment triptanov with selective serotonin reuptake inhibitors.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children, the dark place at a temperature from 2° to 30° c. Shelf life – 3 year.