Composition, form of production and packaging
Spray nasal dosed in the form of a clear solution from light yellow to dark yellow.
1 dose
sumatriptan 10 mg
Excipients: potassium dihydrogen phosphate - 1.4 mg, sodium hydrogen phosphate - 0.11 mg, sulfuric acid * - 2 mg **, sodium hydroxide **, purified water - up to 0.1 ml.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (1) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (2) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (4) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (6) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (12) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (18) - cardboard packs.
Spray nasal dosed in the form of a clear solution from light yellow to dark yellow.
1 dose
sumatriptan 20 mg
Excipients: potassium dihydrogen phosphate - 1.4 mg, sodium hydrophosphate - 0.11 mg, sulfuric acid * - 4 mg **, sodium hydroxide **, purified water - up to 0.1 ml.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (1) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (2) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (4) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (6) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (12) - cardboard packs.
1 dose - glass bottles (1) - dispensers plastic disposable (1) - plastic / paper blisters (18) - cardboard packs.
* The concentration of sulfuric acid is 20%.
** to adjust the pH to 5.0-6.0 (mean pH 5.5).
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
PHARMACHOLOGIC EFFECT
The drug with antimigraine activity. Sumatriptan is a selective agonist of vascular 5-hydroxytryptamine-1 receptors (5-HT 1 D), does not affect other 5-HT receptor subtypes (5-HT 2 -5-HT 7 ). Receptors 5-HT 1 D are located mainly in the cranial blood vessels, and their stimulation leads to narrowing of the vessels. Sumatriptan selectively acts on vasoconstriction of carotid branches, without affecting the blood flow in the vessels of the brain. The vascular carotid pool provides blood supply to extracranial and intracranial tissues (including meningeal membranes), and it is believed that the expansion of these vessels and / or the swelling 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 of the drug at a dose of 20 mg.
PHARMACOKINETICS
Migraine attacks do not have a significant effect on the pharmacokinetics of sumatriptan, the intranasal used.
Suction
After intranasal administration, sumatriptan is rapidly absorbed, C max in plasma is reached after 1-1.5 hours. After taking the drug at a dose of 20 mg, the average Cmax value in plasma is 12.9 ng / ml. Due to pre-systemic metabolism, the average absolute bioavailability for intranasal use of the drug is 15.8% of that for p / to administration.
Distribution
Sumatriptan binds to blood plasma proteins to an insignificant degree (14-21%), the average total Vd is 170 liters.
Metabolism
The main metabolite, the indoleacetic analogue of sumatriptan, is excreted mainly by the kidneys in the form of free acid and glucuronic conjugate. This metabolite has no activity with respect to 5-HT 1 - or 5-HT 2 -receptors. Secondary metabolites of sumatriptan were not detected.
Excretion
T 1/2 is approximately 2 hours. The average total plasma clearance is 1160 ml / min on average, the kidney clearance is 260 ml / min, the extra-neural clearance is about 80% of the total clearance. The main mechanism for the removal of sumatriptan is the oxidative metabolism, carried out by means of the enzyme MAO 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 for p / to administration. There were no significant differences in the pharmacokinetics of sumatriptan in patients with pectoral administration in patients with moderate impairment of liver function compared to healthy controls in the control group.
Patients of adolescence from 12 years to 17 years
The mean Cum maxmatriptan values ​​in plasma were 13.9 ng / ml, and the mean T 1/2 was approximately 2 hours after administration in a dose of 20 mg of sumatriptan intranasally. In population pharmacokinetic modeling, it was revealed that the clearance values ​​and V d increased in accordance with the increase in body weight. Thus, in patients with low body weight, sumatriptan exposure is relatively higher.
INDICATIONS
- arresting migraine attacks with 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.
DOSING MODE
The preparation of Imigran В® should not be prescribed as a prophylaxis. Do not exceed the recommended dose of Imigran В® .
It is recommended to start taking Imigran В® immediately, at the first manifestations of a migraine attack, while the preparation of Imigran В® is equally effective at any stage of a migraine attack.
Adults aged 18 years and over
The recommended dose of Imigran В® 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 paracetamol, acetylsalicylic acid or NSAIDs can be used to stop an attack. However, Imigran В® 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 administered within the next 24 hours, provided that the interval between doses is at least 2 hours.
During the 24-hour period, no more than 2 doses of ImigranВ®, 20 mg, can be administered intranasally.
Adolescents aged 12 to 17 years (inclusive)
The recommended dose of Imigran В® 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 paracetamol, acetylsalicylic acid or NSAIDs can be used to stop an attack. However, Imigran В® 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 administered within the next 24 hours, provided that the interval between doses is at least 2 hours.
During the 24-hour period, no more than 2 doses of ImigranВ®, 20 mg, can be administered intranasally.
Children under 12 years of age
The effectiveness and safety of the use of the drug Imigran В® 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.
Instructions for use of nasal spray
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 Imigran В® .
Do not press the button until the tip is inserted into the nasal passage, otherwise the entire dose will be lost.
Nasal Spray consists of the following parts: tip, finger clip, blue button.
Tip: this part is inserted into the nostril.
Finger clamp: for this part you hold the spray when you use it.
Blue button: when you press the button, 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 Imigran В®
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.
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. 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.
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 EFFECT
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: very often (> 1/10), often (> 1/100 and <1/10), infrequently (> 1/1000 and <1/100), rarely (> 1/10 000 and < 1/1000), very rarely (<1/10 000), is unknown (the frequency can not be estimated from available data).
From the nervous system: very often - dysgeusia; often - dizziness, drowsiness, sensitivity disorders (including paresthesia and decreased sensitivity).
From the side of the vessels: often - a transient increase in blood pressure (soon after taking the drug), hot flashes.
From the respiratory system, chest and mediastinum: often - shortness of breath, mild transitory irritation of the mucous membrane or burning sensation in the nasal cavity or throat, nosebleeds.
From the side of the digestive system: often - nausea, vomiting (the cause-and-effect relationship is not proven).
From the musculoskeletal system: often - a feeling of heaviness (usually transient, can be intense and occur in any part of the body, including the thorax and throat), myalgia.
Common reactions: 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 rarely - slight deviations in hepatic samples
Post-Business Monitoring
From the immune system: it is not known - hypersensitivity reactions, which vary from skin manifestations to anaphylaxis.
Disorders of the psyche: unknown - anxiety.
From the side of the nervous system: unknown - 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, some patients did not have risk factors), tremor, dystonia, nystagmus, scotoma.
From the side of the organ of vision: unknown - flickering, diplopia, decreased visual acuity, loss of vision (usually transient). However, visual disturbances can be caused by the actual migraine attack.
From the heart: unknown - bradycardia, tachycardia, atrial flutter, arrhythmias, signs of transient myocardial ischemia on the ECG, coronary vasospasm, angina pectoris, myocardial infarction.
From the side of the vessels: unknown - arterial hypotension, Raynaud's syndrome.
From the digestive system: unknown - ischemic colitis, dysphagia, a feeling of discomfort in the abdomen, diarrhea.
From the skin and subcutaneous tissues: unknown - hyperhidrosis.
From the musculoskeletal system and connective tissue: unknown - rigidity of the occipital muscles, arthralgia.
CONTRAINDICATIONS
- hypersensitivity to any of the components of the drug;
- hemiplegic, basilar and ophthalmoplegic forms of migraine;
- IHD (including myocardial infarction, postinfarction cardiosclerosis, Prinzmetal angina / vasospastic angina), as well as the presence of symptoms suggesting the presence of IHD;
- peripheral vascular disease;
- stroke and transient ischemic attacks (including in the anamnesis);
uncontrolled arterial hypertension;
severe liver dysfunction;
- simultaneous administration with ergotamine or its derivatives (including metisergid) or other 5-HT 1 -receptor agonists / tryptamines / agonists;
- use against the background of taking MAO inhibitors or earlier than 2 weeks after the withdrawal of these drugs;
- Children under 12 years old.
Caution should be given to the preparation of Imigran В® in patients with epilepsy (including under any conditions with a decrease in the threshold of convulsive readiness); controlled by arterial 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.
The data of post-registration observation of more than 1000 women who took the preparation of Imigran В® in the first trimester of pregnancy are available. 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 the II and III trimesters of pregnancy is limited.
The evaluation of 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 sc administration, sumatriptan is excreted in breast milk. Effects on the newborn can be minimized if avoiding breastfeeding for 12 hours after taking the drug.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug is contraindicated for severe renal impairment.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug is contraindicated for severe violation of liver function.
APPLICATION FOR CHILDREN
Contraindication: the patient is under 18 years old.
APPLICATION IN ELDERLY PATIENTS
Contraindication: the patient is over 65 years old.
SPECIAL INSTRUCTIONS
Imigran В® should be prescribed only if the diagnosis of migraine is undoubted.
Imigran В® is contraindicated for hemiplegic, basilar and ophthalmoplegic migraine forms.
Before starting treatment with Imigran В®, it is necessary to exclude the types of potentially dangerous neurological pathologies (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 Imigran В® .
After taking Imigran В® , transient symptoms may occur, including pain and chest tightness, 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 В® in patients at risk of cardiovascular disease without a preliminary examination to exclude them (such patients include malignant smokers or users of nicotine replacement therapy, postmenopausal women, men over the age of 40 and patients with risk factors 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 В® should be used with caution in patients with controlled hypertension, t. in a small number of patients, a transient increase in blood pressure and peripheral vascular resistance was observed.
There are rare reports resulting from post-marketing surveillance, the development of serotonin syndrome (including mental disorders, vegetative lability and neuromuscular disorders) as a result of concurrent use of SSRIs and sumatriptan. It was also reported on the development of serotonin syndrome on the background of the simultaneous use of triptans with SNRIs.
In the case of simultaneous application of drugs of SSRI and / or SNRI should be carefully monitored patient condition.
Simultaneous use of any of triptane (5-HT 1 agonist) with sumatriptan is not recommended.
Preparation Imigran В®should be used with caution in patients who can change significantly the absorption, metabolism or excretion of sumatriptan, for example in patients with impaired renal or hepatic function (class A or B on the Child-Pugh).
The drug Imigran В® should be used with caution in patients who have a history of convulsions, or who have other risk factors reduce the seizure threshold.
Patients diagnosed with hypersensitivity to sulfonamides reception Imigran preparation В® can cause allergic reactions which range from the cutaneous manifestations of hypersensitivity to anaphylaxis. About cross-sensitivity data are limited, but you should be very careful before applying medication ImigranВ® in these patients.
Undesired reactions may occur more frequently during the simultaneous use of triptans and herbal preparations containing St. John's wort (Hypericum perforatum).
Abuse of drugs designed for the acute relief of headache associated with increased headaches in susceptible patients (headache associated with the abuse of drugs). In this case, you should consider discontinuation of the drug.
Do not exceed the recommended dose of the drug Imigran В® .
Impact on the ability to drive vehicles and manage machinery
In patients with migraine may occur drowsiness, associated with both the disease itself and the reception of the drug Imigran В® , so they need to be especially careful while driving or moving machinery.
OVERDOSE
Symptoms: single dose of the drug Imigran В® 40mg intranasally does not cause any new side effects than those mentioned above. In clinical studies, the healthy volunteers received 20 mg of sumatriptan 3 times / day for 4 days, without causing any significant side reactions.
Treatment: monitoring of the patient for at least 10 hours and, if necessary symptomatic therapy. No data on the effect of hemodialysis or peritoneal dialysis on plasma concentrations of sumatriptan.
DRUG INTERACTION
There was no interaction of sumatriptan with propranolol, flunarizine, pizotifenom and ethanol.
There is limited information about the interaction with preparations containing ergotamine or other triptans / agonists 5-HT 1 receptors. It is theoretically possible increased risk of coronary vasospasm, and the combined use of these drugs is contraindicated.
The period that should elapse between the application of sumatriptan and ergotamine-containing preparations or other triptane / agonist 5-HT 1 receptor is unknown. It will depend, including, on the dose and type of prescribed drugs. The action may be additive in nature. It is recommended to wait at least 24 hours after administration of preparations containing ergotamine or triptan other / agonist 5-HT 1receptor, prior to use of sumatriptan. Conversely, it is recommended to wait at least 6 hours after administration of sumatriptan before applying the preparations containing ergotamine, and at least 24 hours before applying another triptane / agonist 5-HT 1 receptors.
Possible interaction between sumatriptan and MAO inhibitors, their simultaneous use is contraindicated.
There are very rare reports resulting from post-marketing surveillance, the development of serotonin syndrome (including mental disorders, vegetative lability and neuromuscular disorders) resulting from concomitant use of selective serotonin reuptake inhibitors (SSRI) and sumatriptan. It was also reported on the development of serotonin syndrome on the background of co-administration of triptans with selective serotonin reuptake inhibitors and norepinephrine (SNRI).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
RU / STP / 0001/16, the date of creation of the material 12/16/2016
TERMS AND CONDITIONS OF STORAGE
The drug should be kept out of the reach of children, protected from light at a temperature of from 2 В° to 30 В° C. Shelf life - 3 years.
