Sumatriptan 100mg 10 pills

1 film-coated tablet, 100 mg contains:

• active substance: sumatriptan succinate 140.00 mg, in terms of sumatriptan 100.00 mg;

• excipients: hyprolose (Klucel LF hydroxypropyl cellulose) 8.00 mg, calcium hydrogen phosphate dihydrate 88.00 mg, croscarmellose sodium 6.00 mg, magnesium stearate 4.00 mg, mannitol 97.92 mg, calcium stearate 2.08 mg, cellulose microcrystalline 54.00 mg;

• film coating composition: Selecoat AQ-02003 14.00 mg, including: [hypromellose (hydroxypropyl methylcellulose) 8.4 mg, macrogol (polyethylene glycol 6000) 2.8 mg, titanium dioxide 2.8 mg].

Pharmacodynamics

Sumatriptan is a selective agonist of vascular 5-hydroxytrypt-

min-1 receptors (5-HT1D), does not affect other subtypes of 5-HT receptors (5-HT2-5-HT7). 5-HT1D receptors are located mainly in the cranial blood vessels of the brain, and their stimulation leads to a narrowing of these vessels. 

In animals, sumatriptan selectively acts on vasoconstriction of the branches of the carotid artery, without affecting blood flow in the vessels of the brain. The vascular pool of the carotid artery supplies the extracranial and intracranial tissues (including meningeal membranes), it is believed that the expansion of the vessels of the meninges and / or their edema is the main mechanism for the development of migraine in humans.

In addition, experimental data suggest that sumatriptan reduces trigeminal sensitivity. Both of these effects may underlie the anti-migraine action of sumatriptan.

Sumatriptan has been shown to be effective in treating migraine attacks, including menstrual-associated migraines.

The onset of action is 30 minutes after ingestion at a dose of 100 mg. Although the recommended oral dose is 50 mg, migraine attacks vary in severity in both one patient and different patients. Doses of 25 mg to 100 mg have been shown to be more effective than placebo in clinical trials, but a dose of 25 mg is statistically significantly less effective than 50 mg and 100 mg.

Pharmacokinetics

Migraine attacks do not significantly affect the pharmacokinetics of sumatriptan taken orally. 

Suction

After oral administration, it is rapidly absorbed, after 45 minutes its plasma concentration reaches 70% of the maximum level. The average absolute bioavailability is 14%, partly due to the presystemic metabolism, partly due to incomplete absorption. The average maximum plasma concentration (TCmax) after ingestion of 100 mg is 54 ng / ml.

Distribution

Communication with plasma proteins - 14-21%, the average total distribution volume of 170 liters.

Metabolism

The main metabolite, the indole-acetic analogue of sumatriptan, is excreted mainly in the urine as a free acid and glucuronide conjugate. This metabolite is not active against 5-HT1 and 5-HT2 serotonin receptors.

No secondary metabolites of sumatriptan were detected.

Breeding

The half-life (T1 / 2) is approximately - 2 hours. The average total plasma clearance is 1160 ml / min; average renal clearance - 260 ml / min; extrarenal clearance - about 80% of the total clearance.

Sumatriptan is metabolized by monoamine oxidase A.

Pharmacokinetics in patients of special groups

In patients with impaired liver function, the bioavailability of the drug can significantly increase due to an increase in the concentration of sumatriptan in plasma as a result of a decrease in presystem clearance.

The effect of moderate hepatic impairment (class B on the Child-Pugh scale) on the pharmacokinetics of sumatriptan with subcutaneous administration was evaluated. No significant differences were found in the pharmacokinetics of sumatriptan when administered subcutaneously in patients with moderate hepatic impairment compared with healthy patients from the control group.

Relieving migraine attacks with or without aura, including menstrual-associated migraine attacks.

Pregnancy

The use of sumatriptan during pregnancy is possible only if the intended benefit to the mother outweighs the possible risk to the fetus. 

The data obtained with the use of sumatriptan in more than 1000 women in the first trimester of pregnancy do not contain sufficient information to draw final conclusions about the risk of developing congenital malformations in the fetus, and experience with the use of sumatriptan in the second and third trimesters of pregnancy is also limited.

The results of preclinical studies in animals did not show a direct teratogenic effect of sumatriptan on the fetus or a negative effect on the prenatal and postnatal development of the embryo or fetus in rats. However, there is evidence of the effect of sumatriptan on the viability of the embryo and fetus in rabbits.

Breastfeeding period

Sumatriptan has been shown to be excreted in breast milk after subcutaneous administration. Breastfeeding should be stopped during the use of sumatriptan, breastfeeding is possible no earlier than 12 hours after taking the drug.

• Hypersensitivity to any of the components of the drug.

• Hemiplegic, basilar or ophthalmoplegic forms of migraine.

• Coronary heart disease (CHD), (including suspicion of it), angina pectoris (including Prinzmetal's angina pectoris), myocardial infarction (including history), post-infarction cardiosclerosis, as well as symptoms suggesting the presence of coronary heart disease.

• Arterial hypertension of moderate and severe degree, uncontrolled arterial hypertension of mild degree.

• Peripheral occlusion diseases.

• Stroke or transient ischemic attack (including a history).

• Severe impairment of liver and / or kidney function.

• Simultaneous administration with ergotamine or its derivatives (including methysergide) or other tryptamines / agonists of 5-HT1 receptors.

• Use against the background of taking monoamine oxidase inhibitors (MAOs) or earlier than 2 weeks after discontinuation of these drugs.

• Age 18 and over 65 years of age (efficacy and safety not established).

• Epilepsy (including any condition with a reduced epileptic threshold).

• Arterial hypertension (controlled).

• Diseases in which absorption, metabolism, or excretion of sumatriptan may change (e.g., impaired renal or hepatic function).

• Hypersensitivity to sulfonamides (administration of sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis). Data on cross sensitivity is limited, but caution should be exercised when prescribing sumatriptan to such patients.

The adverse reactions presented below are listed according to organ damage 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 / 10000 and <1/1000), very rarely (<1/10000), unknown (frequency cannot be estimated from the available data).

Clinical trial data

Disorders from the nervous system:

often - dizziness, drowsiness, sensitivity disorders, including paresthesia and decreased sensitivity.

Violations of the vessels:

often - transient increase in blood pressure (observed soon after taking the drug), hot flashes.

Disorders from the respiratory system, chest and mediastinal organs:

often shortness of breath.

Violations of the gastrointestinal tract:

often - nausea, vomiting (a causal relationship between the occurrence of adverse reactions and taking the drug has not been proven).

Violations of 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 chest and throat).

General disorders and disorders at the injection site:

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 moderate, transient).

Laboratory and instrumental data:

very rarely - slight deviations in liver function tests.

Post-registration Observation Data

Immune system disorders:

frequency unknown - hypersensitivity reactions, including skin manifestations, as well as anaphylaxis.

Disorders from the nervous system:

the frequency is unknown - convulsive seizures (in some cases observed in patients with a history of convulsive seizures or in concomitant conditions predisposing to the occurrence of seizures; in some patients, no risk factors were identified), tremor, dystonia, nystagmus, scotoma.

Mental disorders:

frequency unknown - alarm.

Violations of the organ of vision:

the frequency is unknown - flickering, diplopia, decreased visual acuity, blindness (usually transient). However, visual disturbances can be caused by a migraine attack itself.

Heart Disorders:

the frequency is unknown - bradycardia, tachycardia, palpitations, arrhythmias, signs of transient myocardial ischemia on an ECG, coronary vasospasm, angina pectoris, myocardial infarction.

Violations of the vessels:

frequency unknown - arterial hypotension, Raynaud's syndrome.

Violations of the gastrointestinal tract:

frequency unknown - ischemic colitis, diarrhea.

Violations of the musculoskeletal and connective tissue:

frequency unknown - stiff neck, arthralgia.

Violations of the skin and subcutaneous tissues:

frequency unknown - hyperhidrosis.

No interaction of sumatriptan with propranolol, flunarizine, pizotifen and ethyl alcohol was observed in healthy volunteers.

With concomitant use with ergotamine, a prolonged spasm of the vessels was noted.

There is limited evidence of the interaction of sumatriptan with drugs containing ergotamine or other triptans / 5-HT1 receptor agonists. It is theoretically possible to increase the risk of coronary vasospasm, and the combined use of these drugs is contraindicated (see section "Contraindications").

The period of time that elapses between the use of sumatriptan and ergotamine-containing drugs or another triptan / 5-HT1 receptor agonist is unknown. It will depend, inter alia, on the dose and type of prescribed drugs. The action may be additive in nature. 

It is recommended to withstand at least 24 hours after the use of preparations containing ergotamine or another triptan / 5-HT1 receptor agonist before using sumatriptan. Conversely, it is recommended to wait at least 6 hours after using sumatriptan before using drugs containing ergotamine, and at least 24 hours before using another tryptan / 5-HT1 receptor agonist.

Perhaps the interaction between sumatriptan and MAO inhibitors, their simultaneous use is contraindicated (see section "Contraindications").

There are rare reports of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) resulting from the simultaneous use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. 

The development of serotonin syndrome was also reported with the simultaneous use of triptans with selective serotonin and noradrenaline reuptake inhibitors (SSRIs).

The drug Sumatriptan Canon should not be prescribed as a prophylaxis. Do not exceed the recommended dose of the drug.

It is recommended to start taking the drug Sumatriptan Canon immediately, at the first manifestations of a migraine attack, while the drug Sumatriptan Canon is equally effective when used at any stage of a migraine attack. 

The drug is used orally, swallowing the whole tablet and drinking it with water.

Adults

The recommended dose is 50 mg (1 tablet). Some patients may require a dose of 100 mg.

If, after taking the first dose, the migraine attack does not stop, the second dose of the drug for stopping the same migraine attack should not be prescribed. In such cases, paracetamol, acetylsalicylic acid, or non-steroidal anti-inflammatory drugs can be used to stop the attack. 

However, Sumatriptan Canon can be used to stop subsequent migraine attacks.

If the patient felt improvement after the first dose of the drug, and then the symptoms recur, you can take a second dose, provided that the interval between doses is at least 2 hours and not more than 300 mg is taken over a 24-hour period. 

Sumatriptan can be used no earlier than 24 hours after taking drugs 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 old)

Efficiency and safety in this group of patients has not been demonstrated.

Elderly patients (over 65 years old)

Experience with sumatriptan in patients over 65 years of age is limited. The pharmacokinetics in patients of this population are not significantly different from those in patients of a younger age, but until additional clinical data are obtained, the use of sumatriptan in patients over 65 years of age is not recommended.

Symptoms

When ingesting up to 400 mg, no other adverse reactions are observed, other than those listed above in the section "Side effects".

Treatment

In case of an overdose of sumatriptan, the condition of the patients should be monitored for at least 10 hours and, if necessary, symptomatic therapy should be carried out. There is no data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in blood plasma.

The drug should be prescribed only if the diagnosis of migraine is not in doubt.

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

Before starting treatment, it is necessary to exclude types of potentially dangerous neurological pathology (for example, stroke, transient ischemic attacks) in the case when the patient has atypical symptoms or when the patient is not diagnosed with a condition requiring the use of the drug.

Transient symptoms may occur after taking the drug, including chest pain and tightness, which can be intense and spread to the neck. If there is reason to believe that these symptoms are a manifestation of coronary heart disease, it is necessary to conduct an appropriate diagnostic examination.

The drug should not be used in patients with risk factors for the development of coronary heart disease, including malicious smokers or users of nicotine replacement therapy, without a preliminary examination of the cardiovascular system. 

Particular attention should be paid to women in the postmenopausal period and men over the age of 40 with these risk factors. However, the examination does not always reveal the heart disease in each patient. 

In very rare cases, serious adverse reactions from the cardiovascular system may occur in patients with no history of cardiovascular disease.

The drug should be used with caution in patients with controlled arterial hypertension, since a small number of patients showed a transient increase in blood pressure and peripheral vascular resistance.

There are rare reports from post-registration observation of the development of serotonin syndrome (including mental status disorders, autonomic lability and neuromuscular disorders) resulting from the simultaneous use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. 

It was also reported on the development of serotonin syndrome due to the simultaneous use of triptans and selective noradrenaline reuptake inhibitors (SSRIs). In the case of simultaneous use of drugs from the SSRI and / or SSRI group, the patient's condition should be carefully monitored.

The simultaneous use of any triptan (5-HT1 agonist) with sumatriptan is not recommended.

Sumatriptan should be used with caution in patients in whom absorption, metabolism or excretion of sumatriptan can be significantly altered, for example, in patients with hepatic insufficiency or impaired renal function (class A or B on the Child-Pugh scale). 

Sumatriptan should be used with caution in patients with a history of seizures or other risk factors for lowering the threshold of seizure readiness, since cases of seizures have been reported when taking sumatriptan.

In patients with hypersensitivity to sulfonamides with the introduction of sumatriptan, there is an increased risk of allergic reactions (from skin manifestations to anaphylactic shock). Cross-sensitivity data are limited, so caution should be exercised before using sumatriptan in these patients.

Adverse reactions may occur more often during the simultaneous use of triptans and herbal preparations containing St. John's wort (Hypericum perforatum).

The abuse of drugs designed to relieve acute headache is associated with increased headaches in sensitive patients (headache associated with drug abuse). In this case, consider discontinuing the drug.

Impact on the ability to drive vehicles and mechanisms

Patients with migraine may experience drowsiness associated with both the disease itself and the use of the drug. During the treatment period, care must be taken when driving vehicles and when working with moving mechanisms.

tablets coated with a film membrane of white or almost white, round, biconvex.