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

Tablet core aids: lactose monohydrate 125 mg, or 250 mg, microcrystalline cellulose 100 mg or 200 mg, magnesium stearate 1.5 mg or 3.0 mg, croscarmellose sodium 2.0 mg or 4.0 mg, talc 1.5 mg or 3.0 mg.

Auxiliary substances of the film shell: hypromellose - 5.9 mg or 11.8 mg, macrogol 6000 (polyethylene glycol 6000) 2.3 mg or 4.6 mg, titanium dioxide 0.92 mg or 1.84 mg, polysorbate 80 0.88 mg or 1.76 mg.

Description:

Tablets are round, biconvex, covered with a film coat of white color.

Pharmacotherapeutic group:antimigraine agent

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

Sumatriptan is a selective agonist of vascular 5-hydroxytryptamine-1 receptors (5-HT₁_D), does not affect other 5-HT receptor subtypes (5-HT₂- 5-HT₇). Receptors 5-HT₁_D are located mainly in the cranial blood vessels of the brain, and their stimulation leads to narrowing of these vessels.

In animals 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.In addition, preclinical data allow us to judge that sumatriptan reduces the sensitivity of the trigeminal nerve. Both these effects can underlie the anti-migraine effect of sumatriptan.

Sumatriptan is effective in the treatment of menstrual migraine, i.e. migraine without an aura, which occurs 3 days before - 5 days after the menstrual cycle. The clinical effect is usually observed in 30 minutes after oral intake of 100 mg of the drug.

Despite the fact that the recommended oral dose is 50 mg, migraine attacks vary in severity in both the patient and the 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.

Pharmacokinetics:

The migraine attacks do not have a significant effect on the pharmacokinetics of sumatriptan taken internally.

Suction

After oral intake quickly absorbed, after 45 minutes its concentration in the plasma reaches 70% of the maximum. After taking 100 mg, the mean maximum plasma concentration is 54 ng / ml.The average absolute bioavailability is 14%, in part due to presystemic metabolism, partly due to incomplete absorption.

Distribution

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

Metabolism

The main metabolite, indoleacetic analogue of sumatriptan, is excreted mainly in urine, in the form of free acid and glucuronide. This metabolite has no activity with respect to 5-HT₁ and 5-HT₂-serotonin receptors. Secondary metabolites of sumatriptan were not detected.

Excretion

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

Sumatriptan is metabolized by the action of 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.

Patients of different age groups

Pharmacokinetics in patients older than 65 years is not significantly different from that in patients of a younger age.

There are no significant differences in sumatriptan pharmacokinetics in patients of different ethnic groups.

Indications:

Coping migraine attacks with or without an aura, including episodes of menstrual-associated migraine.

Assign only with a verified diagnosis of migraine.

Contraindications:

- Hypersensitivity to any of the components of the drug;

- gemiplegic, basilar or ophthalmoplegic form of migraine;

- and(including my suspicion of it), angina pectoris (including Prinzmetal angina), myocardial infarction (including history), postinfarction cardiosclerosis, as well as symptoms suggesting the presence of coronary heart disease;

- farmakologicheski uncontrolled arterial hypertension;

- aboutperipheral vascular cessation;

- andnsult or transient impairment of cerebral circulation (including in anamnesis);

- tsevere violations of the liver and / or kidney function;

- aboutsimultaneous administration with ergotamine or its derivatives (including metisergide) or other tryptamines / agonists of 5-HT₁-serotonin receptors;

- PTreatment with monoamine oxidase inhibitors no earlier than 2 weeks after the withdrawal of these drugs;

- atozrast to 18 years and over 65 years of age (efficacy and safety not established);

- at connection with the presence of lactose in the formulation, its administration is contraindicated in congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

- Arterial hypertension (controlled);

- epilepsy (including any condition with a reduced epileptic threshold);

- diseases in which the absorption, metabolism or excretion of this drug can change (eg, impaired renal or hepatic function);

- pregnancy;

- the period of breastfeeding;

- in patients with hypersensitivity to sulfanilamides (taking sumatriptan may 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.

Pregnancy and lactation:

Pregnancy

The use of sumatriptan during pregnancy is possible only in the case,if the intended benefit for the mother is greater than the potential risk to the fetus (adequate and strictly controlled safety studies have not been carried out).

Available post-registration data for more than 1000 women who took sumatripan during the first 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 sumatriptan in the II and III trimesters of pregnancy is limited.

The results of animal studies did not show a direct teratogenic effect of sumatriptan on the fetus or a negative effect on the peri- and postnatal development of an embryo or fetus in rats. However, there is evidence of the effect of sumatriptan on the viability of the embryo and fetus in rabbits when taking large doses of sumatriptan.

Breastfeeding period

Sumatriptan penetrates into breast milk. To avoid negative effects on the baby, breastfeeding should be stopped during sumatriptan application and within 24 hours after the end of its use.

Dosing and Administration:

Inside.The tablet should be swallowed whole, washed down with water.

Sumatriptan is used for intermittent therapy of migraine attacks. The drug should not be used for preventive purposes.

Begin treatment as early as possible after the onset of migraine attacks (although the drug is equally effective at any stage of the attack).

For relief of acute migraine attacks adults - 50 mg, in some cases, the dose can be increased to 100 mg.

To stop subsequent attacks (with a decrease or disappearance of symptoms, and then resume), you can take a second dose within the next 24 hours, provided that the interval between admission is at least 2 hours.

During any 24 hours of the period, the maximum dose is 300 mg / day.

If migraine symptoms do not disappear and do not decrease after taking the first dose, then a second dose is not prescribed again to stop the ongoing attack. In this case, paracetamol, acetylsalicylic acid or non-steroidal anti-inflammatory drugs. Sumatriptan can be taken to stop subsequent seizures.

Sumatriptan is recommended for use as a monotherapy for migraine, should not be used sumatriptan simultaneously with ergotamine or its derivatives (including metisergide).

Patients with impaired hepatic function: the recommended dose is 50 mg.

Children

Effectiveness and safety of sumatriptan in children less than 10 years old not studied. There are no clinical data available for this age group.

Effectiveness and safety of sumatriptan in children from 10 to 17 years were not demonstrated in clinical studies conducted in this age group. Therefore, the use of sumatriptan in children from 10 to 17 years is not recommended.

Elderly patients (over 65 years of age)

The experience of using sumatriptan in patients over the age of 65 is limited.

Pharmacokinetics does not differ significantly from young ones, but until appropriate clinical data are available, the use of sumatriptan in patients over the age of 65 is not recommended.

Side effects:

Undesirable reactions are listed below, depending on the anatomophysiological classification and frequency of occurrence.

The frequency 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), the frequency is unknown (the frequency can not be estimated from available data). Some of the symptoms that have been described as undesirable symptoms may be symptoms associated with migraine. 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 and thoracic: often - shortness of breath.

From the gastrointestinal tract: often - nausea, vomiting (cause and effect of the occurrence of unwanted reactions with the drug is not proven).

From the musculoskeletal and connective tissue: often - a feeling of heaviness (usually transient, can be intense and occur in any part of the body, including the thorax and throat), myalgia.

General disorders and disorders at the site of administration: often - pain, cold or hot feeling, 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 moderate, transient).

Laboratory and instrumental data: very rarely minor deviations in liver function tests.

Post-registration data

From the immune system: frequency unknown - hypersensitivity reactions, which range from skin manifestations of hypersensitivity to anaphylaxis.

From the nervous system: frequency unknown - convulsive seizures (in a number of cases observed in patients with convulsive episodes in the anamnesis or with concomitant conditions predisposing to the onset of seizures, in some patients, risk factors were not detected), tremor, dystonia, nystagmus, scotoma.

From the side of the organ of vision: Frequency 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: frequency unknown - bradycardia, tachycardia, palpitations, arrhythmias, ECG signs of transient myocardial ischemia, coronary vasospasm, angina pectoris, myocardial infarction.

From the side of the vessels: frequency unknown - lowering blood pressure, Raynaud's syndrome.

From the gastrointestinal tract: frequency unknown - ischemic colitis, diarrhea.

From the musculoskeletal and connective tissue: frequency unknown - neck stiffness, arthralgia.

From the side of the psyche: frequency unknown - alarm.

From the skin and subcutaneous tissues: frequency is unknown - hyperhidrosis.

Overdose:

Symptoms: when ingested to 400 mg, no other adverse reactions are noted other than those listed above.

Treatment: monitoring the patient's condition for at least 10 hours, if necessary - maintenance therapy. There is no data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in plasma.

Interaction:

There was no interaction of sumatriptan with propranolol, flunarisin, pisotifen and ethyl alcohol in healthy volunteers.

Contraindicated concomitant use of sumatriptan and ergotamine or other triptans / agonists 5-HT₁-serotonin receptors. Theoretically, an increased risk of coronary vasospasm, and the joint use of these drugs is contraindicated (see section "Contraindications").

The time period that must elapse between the use of sumatriptan and ergotamine-containing drugs or another tryptane / agonist 5-HT₁-receptor, is unknown. It will depend, inter alia, on the dose and type of prescription drugs.The action can be additive.

It is recommended to withstand at least 24 hours after the use of preparations containing ergotamine or another tryptan / agonist 5-HT₁ receptors before application of 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 (see. The section "Contraindications").

There are rare reports of the development of serotonin syndrome (including mental disorders, vegetative lability and neuromuscular disorders) as a result of simultaneous 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).

Adverse reactions are noted more often with the simultaneous use of triptans with drugs,containing St. John's Wort.

Special instructions:

Sumatriptan should be used only in patients with a diagnosed migraine. The use of sumatriptan for hemiplegic, basilar and ophthalmoplegic migraine is not indicated.

Do not exceed the recommended dose of sumatriptan.

As with the use of other drugs for the treatment of acute migraine attacks, before treatment of a headache in patients who have not previously been diagnosed with migraine or in patients with atypical migraine, other potentially serious types of neurological pathology should be excluded. It should be noted that in patients with migraine, the risk of developing certain cerebrovascular disorders (for example, stroke or transient ischemic attacks (TIA)) is increased.

After taking Sumatrantan, such transitory symptoms as pain and pressure in the chest can occur. Symptoms can be intense and spread to the neck area. If there is reason to believe that these symptoms are a manifestation of coronary heart disease (CHD),further use of sumatriptan should be discontinued and an appropriate diagnostic examination performed.

Patients with risk factors for coronary heart disease, incl. avid smokers or patients using nicotine replacement therapy, without a preliminary examination of the cardiovascular system, should not be prescribed sumatriptan. Particular attention should be paid to postmenopausal women and men over the age of 40 who have these risk factors. However, the examination does not always reveal heart disease, and in very rare cases serious cardiac complications have occurred in patients without concomitant cardiovascular diseases.

A drug Sumatriptan should be used with caution in patients with controlled mild hypertension, since 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, the development of serotonin syndrome (including mental status disorders,vegetative lability and neuromuscular disorders) as a result of simultaneous application of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. Also, the development of serotonin syndrome was reported against the background of simultaneous use of sumatriptan with tryptanes and selective noradrenaline reuptake inhibitors (SSRIs).

If the patient is clinically justified by the simultaneous use of SSRIs and / or SSRIs, the patient's condition should be carefully monitored.

A drug Sumatriptan Caution should be used with caution in patients who may significantly change absorption, metabolism, or excretion of sumatriptan, for example, in patients with hepatic insufficiency or renal dysfunction. In patients with hepatic insufficiency, the initial dose should be 50 mg.

A drug Sumatriptan should be used with caution in patients with a history of seizures or other risk factors for reducing the threshold of convulsive readiness, since cases of seizures have been reported with sumatriptan.

In patients with established hypersensitivity to sulfonamides, taking the drug Sumatriptan can cause allergic reactions, which range from skin reactions of hypersensitivity to anaphylaxis. Data on cross-sensitivity are limited, so caution should be exercised before using the drug Sumatriptan these patients.

Adverse reactions can occur more often with the simultaneous use of triptans and drugs containing St. John's wort.

Long-term use of any type of painkiller for headaches can lead to their intensification. If this situation arises or is suspected, it is necessary to stop therapy and conduct an additional examination. Headache caused by excessive use of drugs may be suspected in patients suffering from recurrent or daily headaches, despite the regular use of medications for headaches.

Patients with rare hereditary lactose intolerance, lactase deficiency and glucose-galactose malabsorption should not take the drug Sumatran- tan, since lactose is included in its composition.

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 drug Sumatriptan. Patients should be especially cautious when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 50 mg and 100 mg.

Packaging:

For 2 or 6 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 2 or 6 tablets in a glass jar for storing medicines such as BPS with a triangular aureole, ukuporennuyu cover lid with a sealing element.

1 contour mesh package or jar with instructions for use is placed in a pack of cardboard for consumer packaging or cardboard chromium-ersatz recycled paper.

Storage conditions:

In the dark place at a temperature of no higher than 25 FROM.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003957

Date of registration:10.11.2016

Expiration Date:10.11.2021

The owner of the registration certificate:BIOCHEMIST, OJSC BIOCHEMIST, OJSC Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Representation: & nbspBIOCHEMICAL JSC BIOCHEMICAL JSC Russia

Information update date: & nbsp11.12.2016

Illustrated instructions

Instructions

Sumatriptan (Sumatriptan)