Imigran - Instructions For Use, Price, Reviews, Spray, Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Imigran

Imigran: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. , Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Imigran

ATX code: N02CC01

Active ingredient: sumatriptan (sumatriptan)

Producer: GlaxoSmithKline Pharmaceuticals (Poland), GlaxoSmithKline Manufakchuring S.p. A. (GlaxoSmithKline Manufacturing SpA) (Italy)

Description and photo update: 2019-26-08

Imigran is a drug with anti-migraine action, an agonist of serotonin 5-HT ₁ receptors.

Release form and composition

Dosage forms:

• Coated tablets: oval biconvex shape with a flat surface on one side, the inscription is engraved on the other: pink tablets - "GX ES3", almost white or white - "GX ET2" (2 pcs. In blisters, in a cardboard pack 1 blister);
• Nasal spray: clear liquid from dark yellow to light yellow (in disposable dispensers, 1 dispenser in a blister, 1 blister in a cardboard box).

Each pack also contains instructions for using Imigran.

The active ingredient of Imigran is sumatriptan:

• 1 tablet: 50 mg or 100 mg (as sumatriptan succinate 70 mg and 140 mg, respectively);
• 1 dispenser: 10 mg, 20 mg.

Auxiliary components:

• Tablets: croscarmellose sodium, anhydrous lactose, lactose monohydrate, microcrystalline cellulose, magnesium stearate;
• Spray: sodium phosphate disubstituted anhydrous, sodium hydroxide, sulfuric acid, potassium phosphate monobasic, purified water.

Additionally, as part of a tablet shell with engraving:

• GX ES3 (50 mg): pink opadry YS-1-1441-G, iron oxide red, titanium dioxide, triacetin, methylhydroxypropyl cellulose;
• "GX ET2" (100 mg): white opad OY-S-7393, titanium dioxide, methyl hydroxypropyl cellulose.

Pharmacological properties

Pharmacodynamics

Imigran is one of the drugs with anti-migraine activity. The active ingredient - sumatriptan, is a selective agonist of vascular 5-hydroxytryptamine-1-receptors (5-HT ₁ D), it has no effect on other subtypes of 5-HT receptors (5-HT ₂ –5-HT ₇). 5-HT ₁ D receptors are located predominantly in cranial blood vessels, and due to their stimulation, vasoconstriction occurs.

The substance selectively affects the vasoconstriction of the branches of the carotid artery, without affecting the blood flow in the vessels of the brain. The blood supply to intracranial and extracranial tissues (including the meningeal membranes) is provided by the vascular basin of the carotid artery. It is believed that the main mechanism of migraine in humans is the expansion of these vessels and / or edema of their walls. Sumatriptan helps to reduce the sensitivity of the trigeminal nerve. Both of these properties can underlie the mechanism of the anti-migraine action of the substance.

The development of the clinical effect of Imigran is noted: after intranasal administration at a dose of 20 mg - after 15 minutes; after oral administration in a dose of 100 mg - after 30 minutes.

Although the recommended dose for oral administration is 50 mg, it should be borne in mind that migraine attacks differ in severity both in one patient and in different patients. Compared to placebo, doses in the 25–100 mg range were more effective, but statistically 25 mg was significantly less effective than 50 and 100 mg.

Sumatriptan is effective in the treatment of migraine attacks, including menstrual-associated migraine.

Pharmacokinetics

Migraine attacks do not significantly affect the pharmacokinetic processes of sumatriptan administered intranasally or orally.

Sumatriptan is rapidly absorbed after oral administration, 70% of the plasma C _max (maximum concentration) is reached in 45 minutes. The average C _max in blood plasma after taking 100 mg is 54 ng / ml. The average value of the absolute bioavailability is 14% (partly this is due to first-pass metabolism, partly - with incomplete absorption).

Sumatriptan is rapidly absorbed after intranasal administration, the time to reach C _max in plasma is 1–1.5 hours. Its average value after taking 20 mg of Imigran is 12.9 ng / ml. The average value of the absolute bioavailability is 15.8% of that after subcutaneous administration (associated with first-pass metabolism).

Sumatriptan binds to blood plasma proteins insignificantly (from 14 to 21%), the average total _Vd (volume of distribution) is 170 liters.

The main metabolite is the indoleacetic analogue of sumatriptan; excretion is carried out mainly by the kidneys in the form of a glucuronic conjugate and free acid. This metabolite has no activity against 5-HT ₁ - or 5-HT ₂ -receptors. No minor metabolites of the substance were found.

T _1/2 (half-life) - approximately 2 hours. The average total plasma clearance is about 1160 ml / min, renal clearance is 260 ml / min, and extrarenal clearance is approximately 80% of the total. Sumatriptan is metabolized by MAO (monoamine oxidase) -A.

When hepatic function is impaired, the presystemic clearance of the substance decreases and its plasma concentration increases. In moderate liver dysfunctions, significant changes in pharmacokinetic parameters are not observed.

Due to the intranasal use of Imigran in patients 12–18 years old, the mean plasma C _{max of} sumatriptan is 13.9 ng / ml, the mean T _1/2 is about 2 hours after the 20 mg dose. Clearance and V _d increases according to the increase of body weight, ie. E. Exposure of sumatriptan at relatively low body weight above.

Indications for use

Film-coated tablets

Elimination of pain syndrome of acute migraine attacks with or without aura.

Nasal spray

Relief of migraine attacks with or without aura.

Imigran in this dosage form is especially indicated for migraine attacks, which are accompanied by nausea and vomiting, as well as when it is necessary to achieve an immediate clinical effect.

Contraindications

Absolute:

• Ischemic heart disease (IHD), including Prinzmetal's angina pectoris, myocardial infarction, postinfarction cardiosclerosis (including with symptoms or suspicions of IHD);
• Ophthalmoplegic, basilar and hemiplegic forms of migraine;
• Occlusive pathology of peripheral vessels;
• Uncontrolled arterial hypertension;
• Stroke or transient violation of cerebral circulation (including a burdened history);
• Severe liver dysfunction;
• Severe renal impairment (tablets);
• Concomitant therapy with monoamine oxidase (MAO) inhibitors and up to two weeks after their withdrawal;
• Concomitant use with drugs containing ergotamine or its derivatives, including methysergide, or with other triptans / agonists of 5-HT ₁ receptors;
• Age up to 12 years old (for spray), up to 18 years old (for tablets) and over 65 years old;
• Hypersensitivity to drug components.

Relative (therapy with Imigran should be carried out under medical supervision in the presence of the following diseases / conditions):

• Controlled arterial hypertension;
• Epilepsy (including any conditions in which there is a decrease in the seizure threshold);
• Diseases that may affect the absorption, metabolism or excretion of Imigran (for example, impaired renal / liver function);
• Lactase deficiency, galactose intolerance and glucose-galactose malabsorption (tablets, since they contain lactose);
• Hypersensitivity to sulfonamides (the use of sumatriptan can lead to the development of allergic reactions, their severity varies from skin manifestations to anaphylaxis);
• Pregnancy and lactation.

Imigran, instructions for use: method and dosage

Film-coated tablets

Imigran tablets are taken orally, swallowed whole and washed down with a sufficient amount of water.

The effect of the drug at any stage of the attack is the same, but it is advisable to use it when the first symptoms of migraine occur.

The recommended dosage for the relief of an acute migraine attack is 50-100 mg once. In the absence of a clinical effect, a repeated dose should not be taken to relieve the pain syndrome of an ongoing attack.

If symptoms recur after the first attack has subsided, the second dose can be taken within the next 24 hours, observing the interval between doses of at least 2 hours.

The maximum dose of Imigran should not exceed 300 mg in 24 hours.

Nasal spray

Spray Imigran is used intranasally, injecting the prescribed dose into one nostril.

Carefully, without pressing the blue button, remove the dispenser from the blister. Firmly pressing one nostril against the nasal septum with your finger, you should breathe calmly through your mouth. Insert the pipette tip into the open nasal passage (pre-cleaned) to a depth of about 1 cm. Do not tilt your head back, close your mouth. While inhaling calmly through the nose, press the blue button firmly with your thumb. Then, for 10-20 seconds, you should calmly inhale through the nose and exhale through the mouth.

The dose of Imigran depends on the clinical manifestation of the attack and can be 10 mg or 20 mg of sumatriptan.

If the migraine attack cannot be controlled with the first dose, the second dose should not be used.

The recommended dose of Imigran spray for children 12-18 years old is 10 mg in one nasal passage. Since the absorption of sumatriptan and migraine attacks have significant variability in clinical manifestations and intensity, a dose of 20 mg may be required. If the migraine attack does not stop after the first dose, the second dose of Imigran should not be administered to stop the same attack. In such cases, the use of paracetamol, acetylsalicylic acid or non-steroidal anti-inflammatory drugs is indicated.

If, after a temporary improvement due to the use of the first dose, the symptoms of the disease have resumed, then the second dose can be administered within the next 24 hours, while maintaining an interval between doses of at least 2 hours.

Intranasally, you can enter no more than 2 doses of 20 mg per 24 hours.

Side effects

Film-coated tablets

• Nervous system: dizziness, hot flashes, weakness (transient, usually mild or moderate); rarely - feeling tired, sleepy; in some cases - seizures (more often in patients with a history of epilepsy or structural brain lesions that can cause the development of epilepsy); sometimes - diplopia, nystagmus, scotoma, flickering before the eyes, decreased visual acuity; very rarely - transient partial loss of vision (it should be borne in mind that the migraine attack itself can cause visual impairment);
• Cardiovascular system: bradycardia, arterial hypotension, palpitations, transient increase in blood pressure (immediately after taking the pill), tachycardia (including ventricular); in some cases - cardiac arrhythmias, transient changes in ischemic electrocardiography (ECG), coronary artery spasm, myocardial infarction, Raynaud's syndrome;
• Digestive system: possibly - nausea, vomiting (the connection with the use of Imigran has not been established); rarely - ischemic colitis; in some cases - a slight increase in the activity of liver enzymes, a feeling of discomfort in the abdomen, dysphagia;
• Allergic reactions: in some cases - erythema, skin rash, itching on the skin, anaphylaxis;
• Others: possibly - pain, a feeling of heat and / or tingling, a transient feeling of heaviness, compression, pressure in any part of the body, including the throat and chest.

Nasal spray

• Nervous system: often - drowsiness, dizziness, sensitivity disorders (including decreased sensitivity, paresthesia);
• Cardiovascular system: often - hot flashes, transient increase in blood pressure (soon after instillation);
• Respiratory system: often - a slight burning sensation and transient irritation of the mucous membrane of the nose and / or throat, shortness of breath, nosebleeds;
• Digestive system: often - nausea, vomiting; very rarely - minor violations of liver function tests;
• General reactions: often - fatigue, weakness, sensations of pain, heaviness, cold, heat, pressure or constriction (varying degrees of intensity, are transient, can occur in any part of the body).

Side effects from the use of Imigran spray obtained in post-marketing studies:

• Nervous system: very rarely - seizures (observed both in patients with seizures and conditions in history, and in patients without risk factors), dystonia, tremor, nystagmus;
• Organ of vision: very rarely - diplopia, decreased visual acuity, flickering, scotoma, blindness (usually transient);
• Cardiovascular system: very rarely - tachycardia, bradycardia, flutter, transient ECG changes, arrhythmias, angina pectoris, coronary vasospasm, myocardial infarction, Raynaud's syndrome, hypotension;
• Digestive system: very rarely - dysphagia, ischemic colitis, abdominal discomfort;
• Allergic reactions: very rarely - hypersensitivity reactions.

Overdose

A single intranasal administration of 40 mg of Imigran or oral administration in a dose of more than 400 mg did not lead to the development of any other adverse reactions, except for those described in the side effects.

Therapy: observation of the patient's condition is shown for at least 10 hours, if necessary, symptomatic treatment is prescribed. There is no evidence to support or refute the effect of hemodialysis / peritoneal dialysis on the plasma concentration of sumatriptan.

special instructions

Imigran can only be used with an accurate diagnosis of a migraine attack.

The use of Imigran for prophylaxis is contraindicated!

Violation of the dosage regimen is prohibited.

If there is no clinical effect from the first dose, it is necessary to clarify the diagnosis.

When prescribing Imigran to relieve headaches in patients with undiagnosed migraine or atypical migraine symptoms, prior exclusion of other potentially dangerous neurological pathologies is required. It should be borne in mind that with migraine there is a risk of stroke, transient disorders of cerebral circulation and other cerebrovascular complications.

Without preliminary examination in order to exclude cardiovascular diseases in patients at risk (postmenopausal period in women, men over the age of 40, predisposition to coronary heart disease) Imigran should not be prescribed.

The occurrence of a side effect in the form of intense pain radiating to the neck and a feeling of tightness in the chest can be a symptom of the manifestation of coronary artery disease, therefore, a diagnostic examination is necessary.

Imigran should be used with caution in functional disorders of the kidneys or liver (due to a possible significant violation of absorption, metabolism, excretion of sumatriptan), controlled arterial hypertension (since there is a risk of a transient increase in blood pressure and peripheral vascular resistance).

Careful monitoring of the patient's condition is required while taking serotonin reuptake inhibitors.

With hypersensitivity to sumatriptan, it is possible to develop skin allergic manifestations up to anaphylactic shock.

Influence on the ability to drive vehicles and complex mechanisms

During the period of a migraine attack and the use of Imigran, the patient should be very careful to drive vehicles and mechanisms.

Application during pregnancy and lactation

• Pregnancy: Imigran can be used only in cases where the expected benefit from therapy outweighs the possible risk;
• Lactation period: the effect of sumatriptan on a newborn can be minimized if breastfeeding is avoided for 12 hours after using the drug (the substance is excreted in breast milk).

Pediatric use

Contraindication:

• Spray: up to 12 years old (the method of using Imigran in children aged 12-18 years old differs from adults, which is associated with the peculiarities of pharmacokinetic processes);
• Tablets: up to 18 years old.

With impaired renal function

• Severe renal dysfunction (tablets): Imigran therapy is contraindicated;
• Renal dysfunction: the drug should be used under medical supervision.

For violations of liver function

• Severe violations of hepatic function: therapy with Imigran is contraindicated;
• Hepatic dysfunction: the drug should be used under medical supervision.

Use in the elderly

Imigran therapy in elderly patients is contraindicated, since the safety profile has not been studied.

Drug interactions

Concomitant therapy with ergotamine causes prolonged vasospasm, therefore, sumatriptan should be used 24 hours after taking products containing ergotamine, and drugs containing ergotamine can be used only 6 hours after sumatriptan.

Due to possible interactions, concomitant use with MAO inhibitors is contraindicated.

When combining Imigran and other triptan drugs with selective serotonin reuptake inhibitors, there is a risk of developing serotonin syndrome with a possible mental disorder, autonomic lability and neuromuscular disorders.

Interaction with ethanol, flunarizine, propranolol, pizotifen was not recorded.

Analogs

Imigran analogues are: Algomax, Migranol, Stopmigren, Sumatriptan, Sumatriptan-Teva, Amigrenin, Zomig, Rapimog, Rizamigren, Relpax, Frovamigran, Sumamigren.

Terms and conditions of storage

Keep out of the reach of children.

Store at temperature: tablets - up to 30 ° C, spray - 2-30 ° C, protected from light.

Shelf life: 50 mg tablets - 3 years, 100 mg tablets - 4 years; spray - 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Imigran

Reviews about Imigran characterize it as an effective drug. Some users note that it is more practical to use the spray, its effect develops almost immediately after application. There are almost no reports of side effects.

The cost of the drug in most cases is estimated as justifiably high, since cheaper analogues do not have such a quick and pronounced therapeutic effect.

Price for Imigran in pharmacies

The approximate price for Imigran is:

• Tablets (2 pcs. In a package): dosage 50 mg - 225 rubles; dosage of 100 mg - 397 rubles;
• Spray 20 mg / dose (single-use vials): 1 pc. - 349 rubles; 2 pcs. - 423 rubles.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!