Sumatriptan, 100 mg 2 pcs

Sumatriptan is a specific selective agonist of 5NT1D-serotonin receptors (5-hydroxytryptamine-1-like receptors) located mainly 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).

In experimental studies it is shown that sumatriptan causes selective narrowing of carotid arteries, which supply blood to extracranial and intracranial tissues, including cerebral membranes (dura mater).including cerebral membranes (dilation of these vessels and/or their
edema is the main mechanism of migraine development in humans), without having a significant effect on the cerebral blood flow.

It is also found experimentally that sumatriptan suppresses the activity of receptors of trigeminal nerve afferent fiber endings. It eliminates nausea and photophobia associated with migraine attack.

Indications

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

Active ingredient

Sumatriptan

Composition

One tablet of 100 mg contains:

active ingredient:

sumatriptan (sumatriptan succinate) 100.00 mg (140.00 mg);

excipients:

lactose monohydrate 140.00 mg,

croscarmellose sodium 3.00 mg,

Microcrystalline cellulose 13.50 mg,

Colloidal silica 0.50 mg,

Magnesium stearate 3.00 mg;

Opadray II white coating 33G28707 (Hypromellose (E 464) 4.0000 mg,

titanium dioxide (E 171) 2.4000 mg,

How to take, the dosage

Oral (tablet is swallowed whole with water). Initial single dose is 50 mg, if necessary the dose may be increased to 100 mg.

If migraine symptoms do not disappear and do not decrease after the first dose, the second dose is not prescribed to stop an ongoing attack.

To stop subsequent attacks (when symptoms decrease or disappear and then resume) a second dose may be taken within the next 24 hours, provided that the interval between doses is at least 2 hours. The maximum daily dose if taken orally is 300 mg.

Interaction

Sumatriptan does not interact with propranololol, flunarizine, pizotifene and ethyl alcohol. Simultaneous use of sumatriptan with ergot alkaloids and their derivatives (including methysergide) or other triptans/agonists of 5NT1-serotonin receptors is accompanied by increased risk of long-term vasospasm and ischemia.

Sumatriptan can be used no earlier than 24 hours after taking ergot alkoloids and their derivatives or other triptans/serotonin 5NT1 receptor agonists, in turn, drugs containing ergot alkoloids can be taken no earlier than 6 hours after taking sumatriptan, other triptans/serotonin 5NT1 receptor agonists can be taken no earlier than 24 hours after taking sumatriptan.

An interaction between sumatriptan and MAO inhibitors is possible and concomitant use is contraindicated.
There are very rare reports, derived from post-marketing surveillance, of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) when sumatriptan is used concurrently with selective serotonin reuptake inhibitors (SSRIs).

The development of serotonin syndrome has also been reported with concomitant use of triptans with selective serotonin and noradrenaline reuptake inhibitors (SSRIs).

There have been isolated reports of more pronounced adverse reactions from sumatriptan when used concomitantly with herbal preparations containing St. John’s wort.

Special Instructions

Sumatriptan is not intended to prevent migraine.

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

Sumatriptan should be used as soon as possible after a migraine attack, but the drug is equally effective at any stage of an attack. If there is no effect from the first dose, the diagnosis needs to be clarified.

When using sumatriptan for headache control in patients with previously undiagnosed migraine or with migraine with atypical symptoms, other potentially dangerous neurological diseases should be excluded. It should be borne in mind that in patients with migraine there is a risk of cerebrovascular complications development (including stroke or transient cerebrovascular disorders).

Sumatriptan should be used with caution in epilepsy and any other condition accompanied by decreased seizure threshold. If used concomitantly with SSRIs/ SSRIs, the patient’s condition should be closely monitored.

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

The exam does not always reveal cardiovascular disease in some patients. In very rare cases, transient side effects such as pain and tightness in the chest may occur after taking sumatriptan. The pain may be intense and irradiate to the neck (pharynx) area. If there is reason to believe that these symptoms may be a manifestation of CHD, the drug should be stopped and a diagnostic examination should be performed.

Sumatriptan treatment should be used with caution in patients with controlled arterial hypertension because increased BP and peripheral vascular resistance may be seen in individual cases.

Sumatriptan should be used with caution in patients with conditions in which absorption, metabolism, or excretion of sumatriptan may be significantly altered, such as renal or hepatic dysfunction. Patients with hypersensitivity to sulfonamides when using sumatriptan may have allergic reactions that range from skin manifestations to anaphylactic shock.

The data on cross-sensitivities are limited, but caution is necessary when using sumatriptan in such patients.

Misuse of medications intended to relieve migraine attacks is associated with an increase in headaches in sensitive patients (headache associated with medication abuse).

In this case, withdrawal of the drug should be considered.

Influence on the ability to drive and operate machinery

In migraine, as well as during sumatriptan therapy, drowsiness may develop. Therefore, during sumatriptan use, caution should be exercised while driving motor transport and engaging in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

• High sensitivity to sumatriptan or other drug components;

• .Hemiplegic, basilar and ophthalmoplegic forms of migraine;

• ischemic heart disease (IHD) (incl.ч. myocardial infarction, postinfarction cardiosclerosis, Prinzmetal’s angina);

• patients with risk factors for CHDPatients with risk factors for CHD;

• stroke or transient cerebral circulation disorder (includingч. history);

• peripheral vascular occlusive disease;

• uncontrolled arterial hypertension;
• • severe hepatic and/or renal insufficiency;
  • Simultaneous use with ergot alkaloids and their derivatives (including.ч.
  • concurrent use with ergot alkaloids and their derivatives (including methysergide) or other triptans/serotonin 5NT1 receptor agonists;
  • current use of MAO inhibitors and up to 14 days after their withdrawal;
  • under 18 years of age, patients over 65 years of age;
  • lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

  With caution

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

Side effects

The frequency 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 – at least 0.1%, but less than 1%;

rarely – at least 0.01%, but less than 0.1%;

very rarely – less than 0.01% (including isolated cases).

Cardiovascular system:

very rare – bradycardia, tachycardia, arrhythmia, transient increase in blood pressure (BP) (immediately after treatment initiation), transient signs of myocardial ischemia on electrocardiogram, coronary spasm, myocardial infarction, Raynaud’s syndrome, BP decrease, “tides” of blood to the face.

Respiratory system:

often – shortness of breath, transient mucous membrane irritation or burning sensation in the nasal cavity or throat.

Digestive system disorders:

often – nausea, vomiting; slight increase in the activity of “liver” enzymes;

very rarely – ischemic colitis, diarrhea, feeling of discomfort in the abdomen.

On the nervous system:

often – dizziness, somnolence, impaired sensitivity, including paresthesias, hypoesthesia;

very rarely – seizures (usually with a history of seizures);

unknown frequency – tremor, dystonia, anxiety.

Visually impaired:

infrequent – diplopia, flickering “flies” before the eyes, nystagmus, scotoma, decreased visual acuity;

very rare – partial transient vision loss (it should be noted that visual disturbances may be associated with the migraine attack itself).

Musculoskeletal system:

often – myalgia;

unknown frequency – neck stiffness, arthralgia.

Allergic reactions:

very rare – skin rash, urticaria, skin itching, erythema, anaphylaxis.

Other:

frequent – pain, tingling, sensation of heat, sensation of weakness and/or fatigue, nasal bleeding, 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.

Overdose

Sumatriptan did not cause any side effects when administered in a single subcutaneous dose of 12 mg. When administered subcutaneously in 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, administration of activated charcoal, patient monitoring for at least 10 h, symptomatic therapy if necessary. There are no data on the effect of hemodialysis and peritoneal dialysis on the plasma concentration of sumatriptan.

Similarities

Amigrenin, Sumamigren, Sumatriptan, Sumatriptan-OBL, Sumatriptan-Teva