Sumatriptan Teva - instructions for use ⋆ migraine tablets

Compound

Tablets Sumatriptan Teva 50 mg

Active ingredient : sumatriptan succinate (70 mg, equivalent to 50 mg sumatriptan).
Excipients : lactose monohydrate, croscarmellose sodium, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate.
Film shell: Opadry II 33G28707 white (hypromellose (E464), titanium dioxide (E171), lactose monohydrate, macrogol-3000, triacetin).

Tablets Sumatriptan Teva 100 mg

Active ingredient : sumatriptan succinate (140 mg, equivalent to 100 mg sumatriptan).
Excipients : lactose monohydrate, croscarmellose sodium, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate.
Film shell: Opadry II 33G23092 peach (hypromellose (E 464), titanium dioxide (E 171), lactose monohydrate, macrogol-3000, triacetin, red iron oxide dye (E 172), yellow iron oxide dye (E 172), iron dye black oxide (E 172)).

Sumatriptan-teva 100 mg 6 pcs. film-coated tablets

pharmachologic effect

Antimigraine

Composition and release form Sumatriptan-teva 100 mg 6 pcs. film-coated tablets

One 50 mg tablet contains:

active substance sumatriptan (sumatriptan succinate) 50.00 mg (70.00 mg);
excipients: lactose monohydrate 70.00 mg, croscarmellose sodium 1.50 mg, microcrystalline cellulose 6.75 mg, colloidal silicon dioxide 0.25 mg, magnesium stearate 1.50 mg; shell Opadry II 33G23092 peach (hypromellose (E 464) 2.0000 mg, titanium dioxide (E 171) 1.1725 mg, lactose monohydrate 1.1000 mg, macrogol-3000 0.4000 mg, triacetin 0.3000 mg, iron dye red oxide (E 172) 0.0180 mg, yellow iron oxide dye (E 172) 0.0090 mg, black iron oxide dye (E 172) 0.0005 mg).

One 100 mg tablet contains:

excipients: lactose monohydrate 140.00 mg, croscarmellose sodium 3.00 mg, microcrystalline cellulose 13.50 mg, colloidal silicon dioxide 0.50 mg, magnesium stearate 3.00 mg; shell Opadry II 33G28707 white (hypromellose (E 464) 4.0000 mg, titanium dioxide (E 171) 2.4000 mg, lactose monohydrate 2.2000 mg, macrogol-3000 0.8000 mg, triacetin 0.6000 mg).

Film-coated tablets 50 mg, 100 mg.

2, 6, 12, 30 tablets in a blister made of polyvinyl chloride and aluminum foil.

1 blister along with instructions for use in a cardboard box.

Description of the dosage form

Tablets 50 mg: film-coated tablets from pink with a yellowish tint to pink, oval in shape with a dividing line on both sides. On one side there is an engraving “5” and “0”. On a cross section, the core is white or almost white.

Tablets 100 mg: film-coated tablets of white or almost white color, oval shape. On one side there is an engraving “100”. On a cross section, the core is white or almost white.

Directions for use and doses

Orally (swallow the tablet whole with water). The initial single dose is 50 mg; if necessary, the dose can be increased to 100 mg. If migraine symptoms do not disappear or improve after the first dose, then a second dose is not prescribed to relieve an ongoing attack. To relieve subsequent attacks (if symptoms decrease or disappear and then recur), you can take a second dose over the next 24 hours, provided that the interval between doses is at least 2 hours. The maximum daily dose when taken orally is 300 mg.

Pharmacodynamics

Sumatriptan is a specific selective agonist of 5HT1D-serotonin receptors (5-hydroxytryptamine-1-like), located primarily in the blood vessels of the brain. Stimulation of 5HT1D serotonin receptors leads to vasoconstriction. The drug does not affect other subtypes of 5HT-serotonin receptors (5HT2-5HT7).

Experimental studies have shown that sumatriptan causes selective narrowing of the carotid arteries, which supply blood to extracranial and intracranial tissues, incl. meninges (dilation of these vessels and/or their swelling is the main mechanism for the development of migraine in humans), without having a significant effect on cerebral blood flow. It has also been experimentally established that sumatriptan suppresses the activity of receptors at the endings of the afferent fibers of the trigeminal nerve. Eliminates nausea and photophobia associated with migraine attacks.

Pharmacokinetics

Suction. After oral administration, sumatriptan is rapidly absorbed; after 45 minutes its concentration in the blood plasma reaches 70% of the maximum value. After oral administration of sumatriptan at a dose of 100 mg, the maximum concentration in the blood plasma is reached after 2-2.5 hours and averages 54 ng/ml. Absolute bioavailability after oral administration averages 14% due to first-pass metabolism and incomplete absorption.

Distribution. Plasma protein binding is 14-21%, the total volume of distribution averages 170 l (2.4 l/kg).

Metabolism. Sumatriptan is metabolized by oxidation with the participation of monoamine oxidase (MAO) (mainly isoenzyme A) with the formation of metabolites, the main of which is the indoleacetic analogue of sumatriptan, which does not have pharmacological activity against 5HT1- and 5HT2-serotonin receptors, and its glucuronide.

Excretion. The half-life is 2-2.5 hours. On average, plasma clearance is 1160 ml/min, renal clearance is 260 ml/min. Extrarenal clearance is 40% after oral administration. It is excreted by the kidneys, mainly in the form of metabolites (97% after oral administration) of free acid or glucuronide, the rest is excreted by the intestines.

Indications for use Sumatriptan-teva 100 mg 6 pcs. film-coated tablets

Migraine (to relieve attacks, with or without aura).

Contraindications

Hypersensitivity to sumatriptan or other components of the drug; hemiplegic, basilar and ophthalmoplegic forms of migraine; coronary heart disease (CHD) (including myocardial infarction, post-infarction cardiosclerosis, Prinzmetal's angina); patients with risk factors for developing coronary artery disease; stroke or transient cerebrovascular accident (including history); occlusive diseases of peripheral vessels; uncontrolled arterial hypertension; severe liver and/or kidney failure; simultaneous use with ergot alkaloids and their derivatives (including methysergide) or other triptans/5HT1-serotonin receptor agonists (see section “Interaction with other drugs”); simultaneous use of MAO inhibitors and a period of up to 14 days after their discontinuation (see section “Interaction with other drugs”); age under 18 years, patients over 65 years old; lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully

Epilepsy (including any conditions accompanied by a history of decreased seizure threshold), organic brain damage, controlled arterial hypertension, renal dysfunction and/or mild to moderate liver dysfunction, pregnancy.

Application Sumatriptan-teva 100 mg 6 pcs. film-coated tablets during pregnancy and breastfeeding

Despite the fact that safety data obtained from the use of sumatriptan in 1000 women in the first trimester of pregnancy do not contain sufficient information, there is no basis to draw definitive conclusions about the risk of congenital malformations in the fetus. Experience with the use of sumatriptan in the second and third trimester of pregnancy is limited. The use of sumatriptan during pregnancy is possible only if the expected benefit to the mother outweighs the potential risk to the fetus. Breastfeeding should be discontinued while using sumatriptan and for 24 hours after stopping its use.

special instructions

Sumatriptan is not intended for the prevention of migraine.

Sumatriptan should only be taken if the diagnosis of migraine is certain.

Sumatriptan should be used as soon as possible after the onset of a migraine attack, but the drug is equally effective at any stage of the attack. If there is no effect from the first dose, the diagnosis should be clarified. When using sumatriptan to relieve headaches in patients with previously undiagnosed migraine or migraine with atypical symptoms, other potentially dangerous neurological diseases should be excluded. It must be borne in mind that patients with migraine are at risk of developing cerebrovascular complications (including stroke or transient cerebrovascular accident).

Sumatriptan should be taken with caution in case of epilepsy and any other conditions accompanied by a decrease in the seizure threshold. In case of simultaneous use with SSRIs/SNRIs, the patient's condition should be carefully monitored.

Before using sumatriptan, patients should exclude the presence of cardiovascular disease, especially in patients at risk. These patients include postmenopausal women, men over 40 years of age, and patients with risk factors for coronary artery disease.

The examination does not always reveal cardiovascular disease in some patients. In very rare cases, transient side effects such as chest pain and tightness may occur after taking sumatriptan. The pain can be intense and radiate to the neck (pharynx). If there is reason to believe that these symptoms may be a manifestation of coronary artery disease, it is necessary to stop taking the drug and perform a diagnostic examination. Treatment with sumatriptan should be carried out with caution in patients with controlled arterial hypertension, since in some cases an increase in blood pressure and peripheral vascular resistance may be observed. Sumatriptan should be used with caution in patients with diseases that may significantly alter the absorption, metabolism or excretion of sumatriptan, such as impaired renal or hepatic function. In patients with hypersensitivity to sulfonamides, when using sumatriptan, allergic reactions may develop, which range from skin manifestations to anaphylactic shock. Cross-sensitivity data are limited, but caution is warranted when administering sumatriptan to these patients.

Overuse of medications intended to treat migraine attacks is associated with increased headaches in sensitive patients (drug overuse headache).

In this case, the possibility of discontinuing the drug should be considered.

Overdose

When administered subcutaneously at a dose of 12 mg, sumatriptan did not cause any side effects. When administered subcutaneously at a dose greater than 16 mg or when administered orally greater than 400 mg, sumatriptan did not cause any unexpected side effects other than those listed above.

Treatment: gastric lavage, taking activated charcoal, monitoring the patient’s condition for at least 10 hours, and, if necessary, symptomatic therapy. There are no data on the effect of hemodialysis and peritoneal dialysis on plasma concentrations of sumatriptan.

Side effects Sumatriptan-teva 100 mg 6 pcs. film-coated tablets

The incidence of side effects is classified according to the recommendations of the World Health Organization: very often - at least 10%; often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01% (including isolated cases). From the cardiovascular system: very rarely - bradycardia, tachycardia, arrhythmia, transient increase in blood pressure (BP) (immediately after the start of treatment), transient signs of myocardial ischemia on the electrocardiogram, coronary vasospasm, myocardial infarction, Raynaud's phenomenon, decrease in blood pressure, "flushes" of blood to the face.

From the respiratory system: often - shortness of breath, transient irritation of the mucous membrane or a burning sensation in the nasal cavity or throat.

From the digestive system: often - nausea, vomiting; a slight increase in the activity of “liver” enzymes; very rarely - ischemic colitis, diarrhea, discomfort in the abdominal area.

From the nervous system: often - dizziness, drowsiness, sensory disturbances, including paresthesia, hypoesthesia; very rarely - seizures (usually with a history of seizures); unknown frequency - tremor, dystonia, anxiety.

On the part of the organ of vision: infrequently - diplopia, flashing “spots” before the eyes, nystagmus, scotoma, decreased visual acuity; very rarely - partial transient loss of vision (it should be borne in mind that visual impairment may be associated with the migraine attack itself).

From the musculoskeletal system: often - myalgia; unknown frequency - stiff neck, arthralgia.

Allergic reactions: very rarely - skin rash, urticaria, itching, erythema, anaphylaxis.

Other: often - pain, tingling, feeling of heat, feeling of weakness and/or fatigue, nosebleeds, feeling of tightness or heaviness (these symptoms are usually transient, but can be intense and occur in any part of the body, including the chest and neck); unknown frequency - increased sweating.

Drug interactions

Sumatriptan does not interact with propranolol, flunarizine, pizotifen and ethyl alcohol. Concomitant use of sumatriptan with ergot alkaloids and their derivatives (including methysergide) or other triptans/5HT1-serotonin receptor agonists is accompanied by an increased risk of developing prolonged vasospasm and ischemia. Sumatriptan can be used no earlier than 24 hours after taking ergot alkaloids and their derivatives or other triptans/5HT1-serotonin receptor agonists, in turn, drugs containing ergot alkaloids can be taken no earlier than 6 hours after taking sumatriptan, other triptans/5HT1-serotonin receptor agonists can be taken no earlier than 24 hours after taking sumatriptan.

Interaction between sumatriptan and MAO inhibitors is possible; their simultaneous use is contraindicated.

There are very rare reports from post-marketing surveillance of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) with simultaneous use of sumatriptan with selective serotonin reuptake inhibitors (SSRIs). The development of serotonin syndrome has also been reported during concomitant use of triptans with selective serotonin norepinephrine reuptake inhibitors (SNRIs).

Isolated reports have been received of more pronounced adverse reactions from sumatriptan when used simultaneously with herbal preparations containing St. John's wort.

Action

A drug with antimigraine activity. Selective 5-HT1 serotonin receptor agonist. Selective stimulation of these receptors leads to a narrowing of the dilated blood vessels of the brain and stops the migraine attack. Sumatriptan activates the sensitivity of trigeminal nerve receptors, preventing the release of pain mediators. Eliminates migraine-related nausea and photophobia.

Sumatriptan - description of the substance

The therapeutic effect usually occurs 30 minutes after oral administration. The greatest effect is observed when used at the height of an attack.

Application and dosage

Orally (swallow the tablet whole with water).

The initial single dose is 50 mg; if necessary, the dose can be increased to 100 mg. The maximum daily dose when taken orally is 300 mg.

Sumatriptan should be used once per migraine attack and as soon as possible after the onset of the attack, but the drug is effective at any stage of the attack. If there is no effect from the first dose, the diagnosis should be clarified.

To control subsequent attacks, after symptoms have subsided and returned, a second dose may be taken over the next 24 hours, at least 2 hours apart.

Sumatriptan-Teva tablet p/o 50 mg N2 (Teva)

Sumatriptan should only be prescribed if the diagnosis of migraine is beyond doubt.

Sumatriptan should not be used for prophylactic purposes.

Sumatriptan is contraindicated for use in hemiplegic, basilar and ophthalmoplegic forms of migraine. As with other drugs used to treat acute migraine attacks, other types of neurological pathology must be excluded before treating a headache attack in patients with previously undiagnosed migraine or in patients with atypical migraine. It should be noted that patients with migraine have an increased risk of developing certain cerebrovascular events (eg, stroke or transient ischemic attack).

Taking sumatriptan may be associated with transient symptoms such as pain and tightness in the chest, spreading to the neck area; symptoms may be intense. If there is reason to believe that these symptoms are a manifestation of coronary artery disease, it is necessary to conduct an appropriate diagnostic examination.

Sumatriptan should not be used in patients at risk of cardiovascular pathology without prior examination to exclude it (such patients include postmenopausal women, men over the age of 40 years and patients with risk factors for the development of coronary artery disease). However, the examination does not always reveal heart disease in every patient. In very rare cases, serious cardiovascular adverse reactions may occur in patients without a history of cardiovascular disease.

Sumatriptan should be used with caution in patients with controlled hypertension, as transient increases in blood pressure and peripheral vascular resistance have been observed in a small number of patients.

There are rare reports from post-marketing surveillance of the development of serogonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) as a result of the simultaneous use of SSRIs and sumatriptan. The development of serotonin syndrome has also been reported during concomitant use of triptans with SSRIs.

If the patient is indicated for simultaneous use of drugs from the SSRI and/or SNRI group. The patient's condition should be carefully monitored.

Concomitant use of any triptan (5-HHT1 agonist) with sumatriptan is not recommended.

Sumatriptan should be used with caution in patients in whom the absorption, metabolism, or elimination of sumatriptan may be significantly altered (for example, patients with impaired renal or hepatic function).

Sumatriptan should be used with caution in patients with a history of seizures or other risk factors for lowering the seizure threshold.

In patients with known hypersensitivity to sulfonamides, taking sumatriptan may cause allergic reactions that range from skin manifestations of hypersensitivity to anaphylaxis. Cross-sensitivity data are limited, but caution should be exercised when using sumatriptan in such patients.

Overuse of medications intended to treat migraine attacks is associated with increased headaches in sensitive patients (drug overuse headache). In this case, the possibility of discontinuing the drug should be considered.

Do not exceed the recommended dose of sumatriptan.

Contraindications and restrictions

Hypersensitivity to any of the components of the drug.
Hemiplegic, basilar or ophthalmoplegic forms of migraine.
Coronary heart disease, angina pectoris, myocardial infarction, arterial hypertension, occlusive diseases of peripheral vessels, risk factors for diseases of the cardiovascular system.
Stroke or transient cerebrovascular accident (including history).
Severe liver and/or kidney failure.
Taking other serotonergic drugs (triptans, ergotamine), lithium salts, serotonin reuptake inhibitors and MAO inhibitors.
Lactose intolerance, glucose/galactose malabsorption syndrome, congenital lactase deficiency.
Ages under 18 and over 65 years of age (efficacy and safety have not been established).

with caution for epilepsy and any decrease in the threshold of convulsive readiness; controlled arterial hypertension; dysfunction of the liver and/or kidneys; hypersensitivity to sulfonamides; pregnancy and lactation (avoid breastfeeding for 12 hours after taking the drug).