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

Components	Amount, mg
	10 mcg / dose	20 mg / dose
Active substance:
Sumatriptan	10,0	20,0
Excipients:
Potassium dihydrogen phosphate	1,4	1,4
Sodium hydrogen phosphate	0,11	0,11
Sulfuric acid¹	2,0*	4,0*
Sodium hydroxide	*	*
Purified water	Up to 0.1 ml	Up to 0.1 ml

1. The concentration of sulfuric acid is 20%.

* - to adjust the pH to a level of 5.0-6.0 (mean pH - 5.5).

Description:Transparent solution from light yellow to dark yellow.

Pharmacotherapeutic group:Anti-migraine means

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

The 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-NT₁D are located, mainly, in the cranial blood vessels, and their stimulation leads to narrowing of the vessels. 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. Sumatriptan reduces the sensitivity of the trigeminal nerve. Both these effects can underlie the anti-migraine effect of sumatriptan.

The clinical effect is noted 15 minutes after intranasal administration drug in a dose of 20 mg.

Pharmacokinetics:Migraine attacks do not significantly affect the pharmacokinetics sumatriptan, applied intranasally.

Suction

After intranasal administration sumatriptan quickly absorbed, the maximum concentration in the plasma is achieved after 1-1,5 hours. After taking the drug at a dose of 20 mg, the average value of the maximum plasma concentration is 12.9 ng / ml. Due to presystemic metabolism, the average absolute bioavailability for intranasal use of the drug is 15.8% of that for subcutaneous administration.

Distribution

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

Metabolism

The main metabolite, indoleacetic analogue sumatriptan, is excreted mainly by the kidneys in the form of free acid and glucuronide konyogata. This metabolite has no activity with respect to 5-HT₁or 5-HT₂receptors. Secondary metabolites of sumatriptan were not detected.

Excretion

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

The main mechanism for removing sumatriptan is the oxidative metabolism, carried out by means of the enzyme 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. Did not have There were significant differences in the pharmacokinetics of sumatriptan in the subcutaneous administration of y patients with moderate impairment of liver function compared with healthy patients from the control group.

Patients of adolescence from 12 years to 17 years

The mean maximum concentrations of sumatriptan in plasma were 13.9 mg / mL, and the mean half-life was approximately 2 hours after taking 20 mg of sumatriptan intranasally.In population pharmacokinetic modeling, it was found that the values of clearance and volume of distribution increased in accordance with the increase in body weight. Thus, in patients with low body weight, sumatriptan exposure is relatively higher.

Indications:

Coping migraine attacks with an aura or without an aura.

This dosage form is especially indicated in migraine attacks accompanied by nausea and vomiting, as well as to achieve immediate clinical effect.

Contraindications:

- Hypersensitivity to any of the components of the drug.

- Hemiplegic, basilar and ophthalmoplegic forms of migraine.

- Ischemic heart disease (IHD) (including myocardial infarction, postinfarction cardiosclerosis, Prinzmetal angina [vasospastic angina]), as well as symptoms suggesting the presence of IHD.

- Diseases of peripheral vessels.

- Stroke and transient ischemic attacks (including in the anamnesis).

- Uncontrolled hypertension.

- Severe liver dysfunction.

- Receiving concomitantly with ergotamine or its derivatives (including methyl ester) or other tryptanes / agonists of 5-HT1 receptors.

- Use on the background of monoamine oxidase (MAO) inhibitors or earlier than 2 pedules after the withdrawal of these drugs.

- Children under 12 years.

Carefully:Care should be taken when prescribing the preparation "Imigran®" to patients with epilepsy (including, in any condition with a decrease in the threshold of convulsive readiness); controlled hypertension; a violation of the liver and / or kidney function.

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. Available post-registration data for more than 1000 women who took the drug "Imigran®" during I trimester of pregnancy. 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 II and III trimester of pregnancy is limited.

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

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

Adults aged 18 years and over

The recommended dose of the drug "Imigran®" is 20 mg in one nasal passage. It should be remembered that the absorption of the drug and migraine attacks in terms of intensity and clinical manifestations may differ not only in different patients, but also in the same patient, so a dose of 10 mg may be quite effective. 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 "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, then a second dose can be given within the next 24 hours, provided that the interval between doses is at least 2 hours.

During the 24-hour period, it is possible to administer intranasally not more than 2 doses of the preparation "Imigran®" to 20 mg.

Adolescents aged 12 to 17 years (inclusive)

The recommended dose of the drug "Imigran®" is 10 mg in one nasal passage.

It should be remembered that the absorption of the drug and migraine attacks in terms of intensity and clinical manifestations may differ not only in different patients, but also in the same patient, so a dose of 20 mg may be required.

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 "Imigran®" can be used to stop subsequent migraine attacks.

During the 24-hour period, no more than 2 doses of "Nmigran®" preparation, 20 mg each, can be administered intranasally.

Children under 12 years of age

The effectiveness and safety of the use of the drug "Imigran®" in patients of this category has not yet been established.

Patients older than 65 years

There are no clinical data on the use of the drug in patients in this category.

INSTRUCTION FOR USING THE NEXT PANEL

Do not open the blister pack until you are ready to use the drug. Each spray is sealed in a blister pack to keep it clean and safe. If you are wearing a spray without a blister pack or an open blister, it may not work properly when you need it. Each spray contains only one dose of the preparation "Imigran®".

Do not press the button until the tip is inserted into the nasal passage, otherwise the entire dose will be lost.

The nasal spray consists of the following parts:

Tip

This part is inserted into nostril.

Finger clamp

For this part, you keep the spray when you use it.

Blue button

When the button is pressed, the full dose of the spray is injected into the nostril. The button only works once. Do not press the button until the tip is inserted into the nasal passage, otherwise the entire dose will be lost.

How to use the preparation "Imigran®"

1. Remove the blister pack and remove the nasal spray immediately before use.

2. Take a comfortable position. You can inject the drug while sitting.

3. Clean the nasal cavity.

4. Hold the nasal spray as shown in Figure A. Do not press the blue button.

Figure A

5. Firmly press one nostril with your finger to the nasal septum. It does not matter which nostril you choose.

6. Insert the tip of the spray into the other nostril, how comfortable - about 1 cm (Figure B). Make a quiet exhalation through the mouth. Keep your head straight, close your mouth.

7. Begin to breathe freely through the nose. Take a quiet breath through your nose and at the same time press hard on the blue button with your thumb. The button may seem a little tight. You can hear a faint click.Continue to breathe while using the nasal spray (Figure B).

8. You can remove the tip of the spray from the nose and remove the finger from the other nostril. Keep your head straight for 10-20 seconds, inhale calmly through your nose, and exhale through your mouth. This will help the drug stay in the nasal cavity. After using the spray, moisture in the nasal cavity and a slight taste can be felt - these sensations are normal and will soon pass.

After a single use, the vial is empty and should be discarded.

Side effects:

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

Frequency of occurrence of undesirable reactions

Disturbances from the nervous system

Very often: dysgeusia.

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: dyspnea, mild transitory irritation of the mucosa or burning sensation in the nasal cavity or throat, nosebleed.

Disorders from the gastrointestinal tract

Often: nausea, vomiting (cause-and-effect relationship not proven).

Disturbances from musculoskeletal and connective tissue

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

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 moderately severe, transient).

Laboratory and instrumental data

Very rare: minor deviations in liver function tests.

Post-Business Monitoring

Frequency of occurrence of undesirable phenomena

Immune system disorders

It is not known: hypersensitivity reactions, which vary from dermal

manifestations prior to anaphylaxis.

Disorders of the psyche

Unknown: alarm.

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 onset of seizures, in some patients risk factors were not detected), tremor, dystopia, 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, atrial flutter, arrhythmias, ECG signs of transient myocardial ischemia, coronary vasospasm, angina pectoris, myocardial infarction.

Vascular disorders

Unknown: arterial hypotension, Raynaud's syndrome.

Disorders from the gastrointestinal tract

Unknown: ischemic colitis, dysphagia, a feeling of discomfort in the abdomen, diarrhea.

Disturbances from the skin and subcutaneous tissues

Unknown: hyperhidrosis.

Disturbances from musculoskeletal and connective tissue

Unknown: stiff neck, arthralgia.

Overdose:

A single dose of "Imigran®" at a dose of 40 mg intranasally did not lead to any new side effects other than those listed above. In the course of clinical studies, healthy volunteers received 20 mg of sumatriptan 3 times a day for 4 days without the occurrence of any significant adverse reactions.

Treatment

Monitor patients for at least 10 hours and, if necessary, conduct symptomatic therapy. 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.

There are limited data on the interaction with drugs containing ergotamine or other 5-HT 5-HT agonists₁ 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 / agonist 5-HT₁ receptors, 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 5-HT | receptors, before applying sumatriptan. Conversely, it is recommended that you 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, vegetative lability and neuromuscular disorders) as a result of the concomitant 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 drug "Imigran®" should be prescribed only if the diagnosis of migraine is undoubted.

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

Before the beginning of treatment with the drug "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 the preparation "Imigran®".

After receiving the drug "Imigran ®", transient symptoms may occur, including pain and tightness in the chest, 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 at risk of cardiovascular disease without a preliminary examination to exclude it (such patients include malignant smokers or users of nicotine replacement therapy, postmenopausal women, men over the age of 40 and patients with risk factors for the development of IHD).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 drug "Imigran ®" should be used with caution in patients with controlled hypertension, as a small number of patients experienced a transient increase in blood 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 preparation "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 drug "Imigran ®" should be used with caution in patients who have a history of convulsions or have other risk factors for reducing the threshold of convulsive readiness.

In patients with an increased susceptibility to sulfanilamides, the preparation "Imigran®" can cause allergic reactions, which range from skin manifestations of hypersensitivity to anaphylaxis. Data on cross-sensitivity are limited, but vigilance should be observed before starting the use of the preparation "Imigran®" in such patients. Undesirable reactions can occur more often during simultaneous application of tryptanes 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,related to drug abuse). In this case, the possibility of drug cancellation should be considered. Do not exceed the recommended dose of the drug "Imigran ®".

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 use of the drug "Imigran®", so they should be especially careful when driving or moving machinery.

Form release / dosage:Spray nasal dosed.

Packaging:

A glass vial (type I, Ph. Eur.) Containing one dose of the drug in a plastic dispenser, sealed with a rubber stopper and closed with a cap. One dosing device per polyethylene / paper blister. For 1, 2, 4, 6, 12 and 18 blisters together with instructions for medical use in a cardboard box.

Storage conditions:In the dark place at a temperature of 2 to 30 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015723 / 01

Date of registration:15.05.2009 / 18.05.2012

Expiration Date:Unlimited

The owner of the registration certificate:GlaxoSmithKline Manufakchuring SpA GlaxoSmithKline Manufakchuring SpA Italy

Manufacturer: & nbsp

GlaxoSmithKline Manufacturing, S.p.A. Italy

Representation: & nbspGlaxoSmithKline Trading, ZAOGlaxoSmithKline Trading, ZAO