Composition, form of production and packaging
The tablets covered with a film shell of white color, oval, biconcave, with a risk on both sides and side, with engraving "SN" on one side and "50" on the other.
1 tab.
sumatriptan succinate 70 mg,
which corresponds to sumatriptan content of 50 mg
[PRING] lactose monohydrate - 70 mg, croscarmellose sodium - 6 mg, lactose anhydrous (Pharmatose DCL 21) - 105.7 mg, microcrystalline cellulose (Avicel PH 102) 45.3 mg, magnesium stearate 3 mg.
The composition of the film shell: lactose monohydrate - 4.32 mg, mannitol - 2.76 mg, titanium dioxide - 2.4 mg, talc - 1.8 mg, triacetin - 0.72 mg.
2 pcs. - blisters (1) - packs of cardboard.
3 pcs. - blisters (1) - packs of cardboard.
3 pcs. - blisters (2) - packs of cardboard.
3 pcs. - blisters (4) - packs of cardboard.
3 pcs. - blisters (6) - packs of cardboard.
3 pcs. - blisters (8) - packs of cardboard.
The tablets covered with a film shell of white color, oval, biconcave, with engraving "SN" on one side and "100" on the other.
1 tab.
sumatriptan succinate 140 mg,
which corresponds to sumatriptan content of 100 mg
[PRING] lactose monohydrate 140 mg, croscarmellose sodium 12 mg, anhydrous lactose (Pharmatose DCL 21) 211.4 mg, microcrystalline cellulose (Avicel PH 102) 90.6 mg, magnesium stearate 6 mg.
The composition of the shell: lactose monohydrate - 8.64 mg, mannitol - 5.52 mg, titanium dioxide - 4.8 mg, talc - 3.6 mg, triacetin - 1.44 mg.
2 pcs. - blisters (1) - packs of cardboard.
3 pcs. - blisters (1) - packs of cardboard.
3 pcs. - blisters (2) - packs of cardboard.
3 pcs. - blisters (4) - packs of cardboard.
3 pcs. - blisters (6) - packs of cardboard.
3 pcs. - blisters (8) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Anti-migraine drug. A specific selective agonist of serotonin 5-HT 1D (5-hydroxytryptamine subtype of 1D) receptors, localized predominantly in the blood vessels of the brain, does not affect other serotonin 5-HT receptor subtypes (5-HT 2 -5-HT 7 ). Causes narrowing of the vessels of the carotid arterial bed, which supply extracranial and intracranial tissues (the expansion of the vessels of the meninges and / or their edema is the main mechanism of migraine development in humans) without significantly affecting cerebral blood flow. Suppresses the activity of the receptors of the endings of the afferent fibers of the trigeminal nerve in the dura mater (as a result, the secretion of sensory neuropeptides decreases). Both of these effects can underlie the anti-migraine effect of sumatriptan.
Eliminates the associated nausea and photophobia associated with migraine attacks.
In 50-70% of cases, it quickly eliminates an attack with oral administration in a dose of 25-100 mg. Within 24 hours, a relapse may occur in 1/3 of the cases requiring re-application.
The clinical effect is usually seen 30 minutes after ingestion.
PHARMACOKINETICS
Suction
After oral administration, it is rapidly absorbed from the digestive tract. After 45 minutes, the concentration of sumatriptan in plasma reaches 70% of C max .Bioavailability is 14% (due to presystemic metabolism and incomplete absorption). After oral administration of sumatriptan in a dose of 100 mg C max in blood plasma is 54 ng / ml.
Distribution
Binding to plasma proteins is 14-21%. The total V d is 170 liters (2.4 l / kg).
Metabolism
Metabolized by oxidation with the participation of MAO (predominantly isoenzyme A) to form the main metabolite, the indoleacetic analogue of sumatriptan, which does not possess pharmacological activity against serotonin 5-HT 1 - and 5-HT 2 -receptors.
Excretion
T 1/2 sumatriptan - about 2 hours. Plasma clearance - 1160 ml / min, renal clearance - 260 ml / min; non-adrenal clearance - 80% of the total clearance.
It is excreted by the kidneys, mainly in the form of metabolites (97% after ingestion) - free acid or glucuronide conjugate.
INDICATIONS
- Migraine (relief of attacks, with or without aura).
DOSING MODE
The drug is taken orally. The tablet should be swallowed whole, washed down with water.
Treatment begins as soon as possible after the onset of a migraine attack (although the drug is effective at any stage of the attack).
For relief of acute migraine attacks, the recommended dose for adults is 50 mg 1 time / day. Some patients may require a higher dose of 100 mg. If the symptoms do not disappear and do not decrease after the first dose, then to stop the same attack, do not take the drug again. However, the drug can be used to stop subsequentmigraine attacks.
If the patient feels better after the first dose and then the symptoms resume, a second dose can be taken within the next 24 hours at intervals of at least 2 hours after the first dose. The maximum dose of sumatriptan is 300 mg for 24 hours.
SIDE EFFECT
Common reactions: pain, a feeling of heat or tingling, a feeling of constriction or severity. These symptoms are usually transient, but can be intense and occur in any part of the body, including the chest and throat. Tides, dizziness, a feeling of weakness, a feeling of fatigue, drowsiness is usually expressed weakly or moderately and is of a transient nature.
From the cardiovascular system: a decrease in blood pressure, a transient increase in blood pressure (observed soon after taking sumatriptan), bradycardia, tachycardia (including ventricular), arrhythmias, angina pectoris; heart rhythm disturbances, transient ECG changes in ischemic type, myocardial infarction, coronary artery spasm; in isolated cases - Raynaud's syndrome.
On the part of the digestive system: nausea, vomiting, ischemic colitis (the relationship of these side effects with sumatriptan is not established), dysphagia, a feeling of discomfort in the abdomen.
Movement disorders: a feeling of stiffness (these symptoms are usually transient, but can be intense and occur in any part of the body, including the chest and throat);tremor, stiffness of the neck muscles.
From the nervous system: sensory disorders, including paresthesia; convulsive attacks (in a number of cases they were observed in patients with seizures in the anamnesis or in conditions predisposing to the onset of seizures, in some patients predisposing factors were not found), dystonia.
On the part of the senses: diplopia, flashing of "flies" before the eyes, nystagmus, scotoma, reduced visual acuity. Very rarely develops a partial transient loss of vision. However, it should be borne in mind that visual impairment can be associated with migraine attacks.
Allergic reactions: skin rash (including hives and erythematous rashes), skin itching, anaphylactic reactions.
On the part of laboratory indicators: insignificant changes in the activity of hepatic transaminases.
From the respiratory system: shortness of breath, nosebleed.
CONTRAINDICATIONS
- hemiplegic, basilar or ophthalmoplegic form of migraine;
- IHD (including suspicion of it);
- angina (including angina of Prinzmetal);
- Myocardial infarction (including in history);
- postinfarction cardiosclerosis;
uncontrolled arterial hypertension;
- occlusive diseases of peripheral vessels;
- stroke or transient ischemic impairment of cerebral circulation (including anamnesis);
- taking concomitantly with ergotamine or its derivatives (including metisergide);
- use against the background of taking MAO inhibitors or earlier than 2 weeks after the withdrawal of these drugs;
- marked violation of liver and / or kidney function;
- children and adolescence under 18;
- Older age (over 65 years);
- Pregnancy;
- lactation period (within 24 hours after taking the drug);
- Hypersensitivity to the components of the drug.
Carefully:
- epilepsy (including any condition with a decrease in the threshold of convulsive alertness);
- controlled arterial hypertension;
- impaired liver and kidney function;
- in patients with hypersensitivity to sulfonamides (allergic reactions are possible with severity from skin manifestations to anaphylaxis).
PREGNANCY AND LACTATION
Contraindicated use of the drug during pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in marked violation of kidney function.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe violation of liver function.
APPLICATION FOR CHILDREN
Contraindicated in children and adolescents under 18 years.
APPLICATION IN ELDERLY PATIENTS
Contraindicated in old age (over 65 years).
SPECIAL INSTRUCTIONS
Sumatriptan should be prescribed only if the diagnosis of migraine is undoubted, and it should be used as soon as possible after the onset of a migraine attack, although it is equally effective when used at any stage of an attack.
The drug is not intended to prevent migraine (introduction during the migraine aura before the onset of other symptoms may not prevent the development of a headache).
As with the use of other antimigraine drugs, when prescribing sumatriptan in patients with a previously unidentified migraine or in patients with atypical migraine, other potentially serious neurologic conditions should be excluded. It should be noted that in patients with migraine, the risk of developing cerebrovascular complications (stroke or transient cerebral circulation disorders) is increased.
In patients at risk of cardiovascular disease, therapy is not initiated without a preliminary examination (postmenopausal women, men over the age of 40, persons with risk factors for developing coronary artery disease). The examination does not always make it possible to identify heart disease in some patients. In very rare cases, patients may experience serious adverse reactions from the cardiovascular system, in whose anamnesis there was no cardiovascular pathology. After taking the drug, transient intense pains and chest tightness that extend to the neck area may occur. If there is reason to believe that these symptoms are a manifestation of CHD, it is necessary to conduct an appropriate diagnostic examination.
Patients with controlled arterial hypertension should be administered with caution. in some cases there was a transient increase in blood pressure and OPSS; patients suffering from such diseases, in which absorption, metabolism or elimination of sumatriptan (for example, renal or hepatic dysfunction) can vary significantly.
There are very few reports of the development of serotonin syndrome (including psychiatric disorders, vegetative lability and neuromuscular disorders) after taking selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. The development of serotonin syndrome has also been reported with the joint administration of tryptanes and serotonin and noradrenaline reuptake inhibitors (IOZSiN). In the case of joint intake of SSRIs / SSRIs and sumatriptan, careful monitoring of this group of patients should be carried out.
Sumatriptan should be used with caution in patients with epilepsy or organic brain lesions in history with a decrease in the threshold of convulsive readiness.
In patients with hypersensitivity to sulfanilamides, the administration of sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis. Data on cross-sensitivity are limited, but caution should be exercised when assigning sumatriptan to such patients.
Abuse of medicines intended to stop migraine attacks is associated with increased headaches in sensitive patients (headache associated with drug abuse). In this case, the possibility of drug cancellation should be considered.
If there is no effect on the administration of the first dose, the diagnosis should be clarified.
The experience with sumatriptan in patients older than 65 years is limited (there is no significant difference in pharmacokinetics compared with younger patients).
Do not exceed the recommended dose of sumatriptan.
Impact on the ability to drive and use machinery
During the treatment period, patients should be careful when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
OVERDOSE
Symptoms: when ingested at a dose of up to 400 mg, there are no other adverse reactions other than those previously listed.
Treatment: symptomatic therapy, monitoring the patient for at least 10 hours. There is no data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in plasma.
DRUG INTERACTION
No interaction of sumatriptan with propranolol, flunarisin, pisotifen and ethanol was noted.
With the simultaneous administration of ergotamine and ergotamine-containing drugs, a prolonged vasospasm is possible. Sumatriptan can be prescribed no earlier than 24 hours after taking medications containing ergotamine; and vice versa, preparations containing ergotamine can be prescribed no earlier than 6 hours after taking sumatriptan.
Possible interaction between sumatriptan and MAO inhibitors (decrease in the intensity of metabolism of sumatriptan, increasing its concentration).
Perhaps the development of serotonin syndrome in the joint administration of sumatriptan and drugs from the group SSRIs and SSRIs.
The likelihood of side effects with the simultaneous administration of sumatriptan with preparations of St. John's wort is increased.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, dry, protected from light at a temperature of no higher than 30 В° C. Shelf life - 3 years.
