Sumatriptan Canon pills 100mg, 10pcs

Composition

1 film-coated tablet,100 mg contains:

• Active ingredient: sumatriptan succinate 140.00 mg, based on sumatriptan 100.00 mg;

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

• composition of the film shell:  Selecoate AQ-02003 14.00 mg, including: [hypromellose (hydroxypropylmethylcellulose) 8.4 mg, macrogol (polyethylene glycol 6000) 2.8 mg, titanium dioxide 2.8 mg].

Pharmacological action

Pharmacodynamics

Sumatriptan is a selective agonist of vascular 5-

hydroxytryptamine-1 receptors (5-HT1D), does not act on other subtypes of 5-HT receptors (5-HT 2-5-HT 7).5-HT1D receptors are located mainly in the cranial blood vessels of the brain, and their stimulation leads to narrowing of these vessels.

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

In addition, experimental data suggest that sumatriptan reduces the sensitivity of the trigeminal nerve. Both of these effects may underlie the antimigrenous effect 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 oral use at a dose of 100 mg. Although the recommended oral dose is 50 mg, migraine attacks vary in severity both in one patient and in different patients. Doses from 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.

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

Suction

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

Distribution

Plasma protein binding is 14-21%, with an average total volume of distribution of 170 liters.

Metabolism

The main metabolite, the indoleacetic analog of sumatriptan, is mainly excreted in the urine as a free acid and a glucuronide conjugate. This metabolite has no activity against 5-HT1-and 5-HT2-serotonin receptors.

No minor metabolites of sumatriptan were detected.

Deduction

The half-life (T 1/2) is approximately 2 hours. The average total plasma clearance is 1160 ml / min; the average renal clearance is 260 ml / min; the extrarenal clearance is 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 may significantly increase due to an increase in the concentration of sumatriptan in plasma as a result of a decrease in presystemic clearance.

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

Indications

Management of migraine attacks with or without aura, including menstrual-associated migraines.

Use during pregnancy and lactation

Pregnancy

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

The data obtained from the use of sumatriptan in more than 1,000 women in the first trimester of pregnancy do not contain sufficient information to draw definitive conclusions about the risk of developing congenital malformations in the fetus, and the experience of using 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 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.

Breast-feeding period

It has been shown that after subcutaneous use, sumatriptan is excreted in breast milk. Breast-feeding should be discontinued during the use of sumatriptan, breast-feeding is possible no earlier than 12 hours after taking the drug.

Contraindications

• Hypersensitivity to any of the components of the drug.

• Hemiplegic, basilar, or ophthalmoplegic forms of migraines.

• Coronary heart disease (CHD), (including suspected cases), angina pectoris (including Prinzmetal angina pectoris), myocardial infarction (including a history), post-infarction cardiosclerosis, as well as symptoms that suggest the presence of coronary heart disease.

• Moderate and severe arterial hypertension, uncontrolled mild arterial hypertension.

• Occlusive diseases of peripheral arteries.

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

• Severe liver and/or kidney function disorders.

• Concomitant use with ergotamine or its derivatives (including metisergide) or other tryptamines / 5-HT1 receptor agonists.

• Use while taking monoamine oxidase (MAO) inhibitors or earlier than 2 weeks after discontinuation of these drugs.

• Age up to 18 and over 65 years (efficacy and safety have not been established).

With caution:

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

• Arterial hypertension (controlled).

• Diseases that may alter the absorption, metabolism, or elimination of sumatriptan (for example, impaired renal or hepatic function).

• Hypersensitivity to sulfonamides (use of 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 prescribing sumatriptan to such patients.

Side effects

The adverse reactions listed below are listed according to organ damage and frequency of occurrence. The frequency is defined as follows:

very common (≥1/10), common (≥1/100 and <1/10), infrequent (≥1/1000 and <1/100), rare (≥1/10000 and <1/1000), very rare (

Data from clinical trials

Nervous system disorders:

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

Vascular disorders:

often – a transient increase in blood pressure (observed shortly after taking the drug), hot flashes.

Respiratory, thoracic and mediastinal disorders:

often-shortness of breath.

Disorders of the gastrointestinal tract:

often – nausea, vomiting (the causal relationship of the occurrence of adverse reactions with taking the drug is not proven).

Musculoskeletal and connective tissue disorders:

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 tightness (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 samples.

Data from post-registration observations

Immune system disorders:

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

Nervous system disorders:

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

Mental disorders:

frequency unknown-alarm.

Visual disturbances:

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

Cardiac disorders:

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

Vascular disorders:

frequency unknown-hypotension, Raynaud’s syndrome.

Disorders of the gastrointestinal tract:

frequency unknown-ischemic colitis, diarrhea.

Musculoskeletal and connective tissue disorders:

frequency unknown – occipital muscle rigidity, arthralgia.

Skin and subcutaneous tissue disorders:

frequency unknown-hyperhidrosis.

Interaction

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

Long-term vasospasm was observed when taken concomitantly with ergotamine.

There are limited data on the interaction of sumatriptan with drugs containing ergotamine or other 5-HT1 receptor triptans/agonists. Theoretically, there may be an increased risk of coronary vasospasm, and the combined use of these drugs is contraindicated (see the section “Contraindications”).

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

It is recommended to wait at least 24 hours after the use of drugs 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 triptan/5-HT1 receptor agonist.

There may be an interaction between sumatriptan and MAO inhibitors, and their simultaneous use is contraindicated (see the section “Contraindications”).

Serotonin syndrome (including psychiatric disorders, autonomic lability, and neuromuscular disorders) has been reported infrequently as a result of concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan.

Serotonin syndrome has also been reported when triptans are co-administered with selective serotonin and norepinephrine reuptake inhibitors (SSRIs).

How to take, course of use and dosage

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

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

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

Adults

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

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

However, the drug Sumatriptan Canon 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, 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 over a 24-hour period.

Sumatriptan can be used no earlier than 24 hours after taking drugs containing ergotamine; conversely, drugs containing ergotamine can be used no earlier than 6 hours after taking sumatriptan.

Special patient groups

Children and adolescents (under 18 years of age)

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

Elderly patients (over 65 years of age)

Experience with sumatriptan in patients over 65 years of age is limited. The pharmacokinetics of 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 over 65 years of age is not recommended.

Overdose

Symptoms

When taken orally up to 400 mg, no other side effects are observed, except for those listed above in the “Side effect” section.

Treatment

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

Special instructions

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 the 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 has not been diagnosed with a condition that requires the use of the drug.

After taking the drug, transient symptoms may occur, including chest pain and 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 the drug in patients with risk factors for CHD, including heavy smokers or users of nicotine replacement therapy, without a preliminary examination of the cardiovascular system.

Special attention should be paid to post-menopausal women and men over the age of 40 with these risk factors. However, the examination does not always reveal heart disease in every patient.

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

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

There are rare reports from post-marketing surveillance of the development of serotonin syndrome (including mental status disorders, autonomic lability, and neuromuscular disorders) as a result of concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan.

Serotonin syndrome has also been reported with the concomitant use of triptans and selective norepinephrine reuptake inhibitors (SSRIs). In the case of concomitant use of drugs from the SSRI and/or SSRI group, the patient’s condition should be carefully monitored.

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

Sumatriptan should be used with caution in patients who may have significant changes in the absorption, metabolism or excretion of sumatriptan, for example, in patients with hepatic insufficiency or impaired renal function (Child-Pugh class A or B).

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

Patients with hypersensitivity to sulfonamides with the introduction of sumatriptan have an increased risk of allergic reactions (from skin manifestations to anaphylactic shock). Data on cross-sensitivity are limited, so caution should be exercised before using sumatriptan in these patients.

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

The abuse of medications intended for the relief of acute headache is associated with increased headaches in sensitive patients (headache associated with drug abuse). However, discontinuation of the drug should be considered.

Influence on the ability to drive vehicles and mechanisms

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

Form of production

film-coated tablets of white or almost white color, round, biconvex shape.

Storage conditions

At a temperature not exceeding 25 °C in the manufacturer’s packaging. Keep out of reach of children.

Shelf

life is 4 years.

Active ingredient

Sumatriptan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets