Composition, form of production and packaging
The tablets covered with a covering of pink color, oval, biconcave, with an engraved inscription "50" on one side and an equal surface on another.
sumatriptan succinate 70 mg,
which corresponds to sumatriptan content of 50 mg
Excipients: lactose monohydrate - 70 mg, anhydrous lactose - 140 mg, microcrystalline cellulose - 15.5 mg, croscarmellose sodium - 3 mg, magnesium stearate - 1.25-1.75 mg.
Composition of the shell: opadrai pink YS-1-1441-G - 6.6 mg (methyl hydroxypropyl cellulose - 4.06 mg, titanium dioxide - 1.93 mg, triacetin - 0.6 mg, iron oxide red - 0.01 mg).
2 pcs. - blisters (1) - packs of cardboard.
Tablets covered with a coat of white or almost white, oval, biconcave, engraved with the inscription "100" on one side and a level surface on the other.
sumatriptan succinate 140 mg,
which corresponds to sumatriptan content of 100 mg
Excipients: lactose monohydrate - 104 mg, microcrystalline cellulose - 15.5 mg, croscarmellose sodium - 3 mg, magnesium stearate - 1.25-1.75 mg.
Sheath composition: opedrai white OY-S-7393 - 6.6 mg (titanium dioxide - 1 mg, methylhydroxypropylcellulose - 5.6 mg).
2 pcs. - blisters (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2017.
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 these vessels.
In animals sumatriptan selectively acts on the 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.
In addition, experimental data suggest that sumatriptan reduces the sensitivity of the trigeminal nerve. Both these effects can underlie the anti-migraine effect of sumatriptan.
The clinical effect is usually observed 30 minutes after oral administration of the drug at a dose of 100 mg.
Although the recommended dose for oral administration is 50 mg, migraine attacks vary in severity in both the patient and in different patients. Doses of 25 mg to 100 mg showed greater efficacy compared with placebo in clinical studies, but a 25 mg dose was statistically significantly less effective than 50 mg and 100 mg.
Sumatriptan has shown effectiveness in the treatment of migraine attacks, including menstrual-associated migraine.
Migraine attacks do not have a significant effect on the pharmacokinetics of sumatriptan, the intranasal used.
After oral administration, sumatriptan is rapidly absorbed, 70% of the plasma C max is reached after 45 minutes. After taking a dose of 100 mg, the average value of Cmax in blood plasma is 54 ng / ml. The average absolute bioavailability is 14%, partly due to presystemic metabolism, partly due to incomplete absorption.
Sumatriptan binds to blood plasma proteins to an insignificant degree (14-21%), the average total Vd is 170 liters.
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.
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. Sumatriptan is metabolized by 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.
- arresting migraine attacks with or without an aura, including episodes of menstrual-associated migraine.
The preparation of Imigran В® is not intended for use 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.
The drug is used inside, swallowing the tablet whole and washing down with water.
The recommended dose is 50 mg (1 tablet). Some patients may require a dose of 100 mg.
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, the preparation Imigran В® can be used to supervise subsequent migraine attacks.
If the patient feels better after the first dose of the drug and then the symptoms resume, you can take a second dose, provided that the interval between doses is at least 2 hours, and no more than 300 mg is taken within a 24-hour period.
Sumatriptan can be used no earlier than 24 hours after taking medications containing ergotamine; and vice versa, preparations containing ergotamine can be used no earlier than 6 hours after taking sumatriptan.
Special patient groups
Children and adolescents (under 18 years of age): the efficacy of Imigran В® in this group of patients has not been demonstrated.
Patients of advanced age (over 65 years): The experience of using Imigran В® in patients older than 65 years is limited. The pharmacokinetics in patients in this population do not significantly differ from those in younger patients, but until additional clinical data are obtained, the use of sumatriptan in patients older than 65 years is not recommended.
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).
Clinical Trials Data
From the nervous system: 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.
On the part of the digestive system: often - nausea, vomiting (cause and effect of the occurrence of unwanted reactions with the drug 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 chest and throat).
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
From the immune system: it is not known - hypersensitivity reactions, which vary from skin manifestations to anaphylaxis.
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.
Disorders of the psyche: unknown - anxiety.
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, palpitations, 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 side of the digestive system: unknown - ischemic colitis, diarrhea.
From the musculoskeletal system and connective tissue: unknown - rigidity of the occipital muscles, arthralgia.
From the skin and subcutaneous tissues: unknown - hyperhidrosis.
- Hypersensitivity to any of the components that make up the drug;
- hemiplegic, basilar and ophthalmoplegic forms of migraine;
- IHD (including myocardial infarction, postinfarction cardiosclerosis, Prinzmetal angina) or the presence of symptoms suggesting the presence of IHD;
- occlusive diseases of peripheral vessels;
- Stroke or transient ischemic attack (including in the anamnesis);
uncontrolled arterial hypertension;
- severe degree of impaired hepatic function / or kidney function;
- 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;
- age of patients under 18 years old and over 65 years of age (safety and efficacy of Imigran В® is not established).
- controlled arterial hypertension;
- diseases in which the absorption, metabolism or excretion of this drug can change (eg, impaired renal or hepatic function);
- epilepsy (including any condition with a decrease in the threshold of convulsive alertness);
- in patients with increased sensitivity to sulfanilamides (taking sumatriptan may cause allergic reactions, the severity of which varies from skin manifestations of hypersensitivity to anaphylaxis). Data on cross-sensitivity are limited, but caution should be exercised when using sumatriptan in such patients;
- in patients with lactase deficiency, galactose intolerance and glucose-galactose malabsorption (the preparation contains lactose).
PREGNANCY AND LACTATION
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.
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
Contraindicated in severe impairment of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violations of liver function.
APPLICATION FOR CHILDREN
The drug is contraindicated in children and adolescents under 18 years of age.
APPLICATION IN ELDERLY PATIENTS
The drug is contraindicated in patients older than 65 years.
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 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-HT 1 -agonist) with sumatriptan is not recommended.
The preparation of Imigran В® should be used with caution in patients who may significantly change absorption, metabolism or excretion of sumatriptan, for example, patients with impaired renal or hepatic function (class A or B on the Child-Pugh scale).
The preparation of Imigran В® should be used with caution in patients who have a history of seizures or who have other risk factors for reducing the threshold of convulsive readiness.
In patients with an increased susceptibility to sulfanilamides, taking Imigran В® can cause allergic reactions, which range from skin manifestations of hypersensitivity to anaphylaxis. Data on cross-sensitivity are limited, but caution should be exercised before starting the use of Imigran В® in these patients.
Undesirable reactions may occur more often during the simultaneous use of triptans 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 associated with drug abuse). In this case, the possibility of drug cancellation should be considered.
Impact on ability to drive vehicles and manage mechanisms
In patients with migraine, there may be drowsiness associated with both the disease itself and with the use of Imigran В® , so they should be especially careful when driving or moving machinery.
Symptoms: taking Imigran В® orally at a dose of more than 400 mg did not cause any undesirable reactions other than those listed above.
Treatment: monitoring of patients for at least 10 hours and, if necessary, symptomatic therapy. There is no evidence of the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in plasma.
No interaction of sumatriptan with propranolol, flunarisin, pisothiphene and ethanol was observed.
With simultaneous administration with ergotamine, a prolonged vasospasm was noted.
There are limited data on interactions with preparations containing ergotamine or other 5-HT 1 -receptor triptans / agonists. Theoretically, an increased risk of coronary vasospasm, and the joint use of these drugs is contraindicated.
The period that must elapse between the use of sumatriptan and ergotamine-containing drugs or another tryptane / agonist of 5-HT 1 -receptors is unknown. It will depend, in part, 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 1 -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 5-HT 1 -receptor tryptane / agonist.
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 stored in reach of children at a temperature below 30 В° C. Shelf life - 3 years.