Sumatriptan
Sumatriptan: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Sumatriptan
ATX code: N02CC01
Active ingredient: Sumatriptan (Sumatriptan)
Producer: KANONFARMA PRODUCTION, CJSC (Russia) Kievmedpreparat, OJSC (Ukraine)
Description and photo update: 2018-22-10
Prices in pharmacies: from 76 rubles.
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Sumatriptan is a drug with anti-migraine activity.
Release form and composition
Dosage forms of Sumatriptan release:
- film-coated tablets: biconvex, round, white (2, 6 or 10 pcs. in blisters, in a cardboard box 1–3 blisters);
- tablets: oblong, biconvex, almost white or white, engraved "C" on one side, on the other (depending on the dose) - "33" (50 mg) or "34" (100 mg) (1-7 or 10 pcs in blisters, in a carton box 1-6, 8 or 10 blisters; 2, 10, 50 or 100 pcs. in cans, in a carton box 1 can).
Composition of 1 film-coated tablet:
- active substance: sumatriptan - 50 or 100 mg (sumatriptan succinate - 70 or 140 mg);
- auxiliary components (50/100 mg): croscarmellose sodium - 2/4 mg; talc - 1.5 / 3 mg; magnesium stearate - 1.5 / 3 mg; lactose monohydrate - 125/250 mg; microcrystalline cellulose - 100/200 mg;
- shell (50/100 mg): polysorbate-80 - 0.88 / 1.76 mg; titanium dioxide - 0.92 / 1.84 mg; hypromellose - 5.9 / 11.8 mg; macrogol 6000 - 2.3 / 4.6 mg.
Composition of 1 tablet:
- active substance: sumatriptan - 50 or 100 mg (in the form of sumatriptan succinate - 69.98 or 139.96 mg);
- auxiliary components (50/100 mg): magnesium stearate - 2.38 / 4.76 mg; sodium bicarbonate - 10/20 mg; calcium hydrogen phosphate - 53.44 / 106.88 mg; croscarmellose sodium - 11/22 mg; microcrystalline cellulose - 22.5 / 45 mg; polysorbate-80 - 0.7 / 1.4 mg.
Pharmacological properties
Pharmacodynamics
Sumatriptan is a selective agonist of vascular 5-hydroxytryptamine-1-receptors (5-HT 1D), it has no effect on other subtypes of 5-HT receptors (5-HT 2 - 5-HT 7). The 5-HT 1D receptors are located predominantly in the cranial blood vessels of the brain; as a result of their stimulation, these vessels narrow.
Sumatriptan in animals selectively affects the vasoconstriction of the branches of the carotid artery, without affecting the blood flow in the vessels of the brain. Thanks to the vascular basin of the carotid artery, the intracranial and extracranial tissues (including the meningeal membranes) are supplied with blood. It is believed that the edema of the walls of these vessels and / or their expansion is the main mechanism of the appearance of migraine in humans. Also, according to preclinical data, sumatriptan reduces the sensitivity of the trigeminal nerve. Both of these effects can underlie the anti-migraine effect of the drug.
Sumatriptan is effective in the treatment of menstrual migraine, i.e. migraine without an aura that develops 3 days before the menstrual cycle or 5 days after it. The clinical effect appears, as a rule, 30 minutes after taking 100 mg of the drug.
Migraine attacks vary in severity both in different patients and in the same patient. The dose range of 25–100 mg is the most effective compared to placebo, but the dose of 25 mg has significantly less effect than 50 and 100 mg.
Pharmacokinetics
Migraine attacks do not significantly affect the pharmacokinetics of sumatriptan.
Absorption: after oral administration, the substance is rapidly absorbed, its plasma concentration after 45 minutes reaches 70% of the maximum. The maximum concentration in blood plasma after taking 100 mg averages 54 ng / ml. The average absolute bioavailability is 14%, partly due to first pass metabolism, partly due to incomplete absorption.
Distribution: binding of sumatriptan to plasma proteins occurs to an insignificant extent (from 14 to 21%), the average total volume of distribution is 170 liters.
Metabolism: excretion of the main metabolite, the indoleacetic analogue of sumatriptan, occurs mainly in the urine, in the form of glucuronide and free acid. This metabolite has no activity towards 5-HT 1 and 5-HT 2 -serotonin receptors. No minor metabolites were found.
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 - approximately 80% of the total clearance.
Sumatriptan is metabolized by monoamine oxidase A.
In patients with impaired hepatic function, the plasma content of sumatriptan in the blood increases.
Indications for use
Sumatriptan is prescribed for the relief of migraine attacks with / without aura, including attacks of menstrual-associated migraine.
The drug should be prescribed only in cases of a verified diagnosis.
Contraindications
Absolute:
- migraine in hemiplegic, basilar or ophthalmoplegic forms;
- Ischemic heart disease (coronary artery disease), including the presence of suspicion of it, angina pectoris (including Prinzmetal's angina pectoris), myocardial infarction (including a burdened history), postinfarction cardiosclerosis, as well as symptoms that suggest the presence of ischemic heart disease;
- liver / kidney dysfunction in severe course;
- pharmacologically uncontrolled arterial hypertension;
- stroke or transient disorders of cerebral circulation (including a burdened history);
- peripheral vascular occlusive disease;
- congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
- combined use with ergotamine or its derivatives (including methysergide) or other tryptamines / agonists of 5-HT 1 -serotonin receptors;
- combined use with monoamine oxidase inhibitors (use is possible no earlier than 14 days after their cancellation);
- age under 18 and over 65;
- pregnancy and lactation;
- individual intolerance to the components of the drug.
Relative (diseases / conditions in the presence of which the appointment of Sumatriptan requires caution):
- epilepsy, including any condition with a lowered epileptic threshold;
- controlled arterial hypertension;
- diseases in which a change in the absorption, metabolism or excretion of sumatriptan is possible (for example, functional disorders of the kidneys / liver);
- hypersensitivity to sulfonamides (taking the drug can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis);
- the presence of cross-sensitivity.
Instructions for the use of Sumatriptan: method and dosage
Sumatriptan is taken orally with water. The tablet must be swallowed whole.
The drug should be used for the intermittent treatment of migraine attacks. With a preventive purpose, it cannot be taken.
After a migraine attack occurs, treatment should be started as early as possible (although sumatriptan is equally effective at any stage of the attack).
In acute attacks, 50 mg is prescribed, in some cases it is possible to take an increased dose (100 mg).
In order to stop subsequent attacks (with a decrease / disappearance of symptoms, and then their resumption), the administration can be repeated within the next 24 hours (with an interval of 2 hours).
The maximum daily dose is 300 mg.
If Sumatriptan is ineffective for relieving migraine symptoms, a repeated dose is not prescribed. In such cases, paracetamol, acetylsalicylic acid or non-steroidal anti-inflammatory drugs are indicated. Sumatriptan may be taken to control subsequent seizures.
The drug should not be used in combination with ergotamine or its derivatives (including methysergide).
The recommended dose for patients with hepatic impairment is 50 mg.
Side effects
Some of the symptoms described below as side effects may be symptoms associated with migraines.
Possible adverse reactions (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare; with an unrefined frequency - if it is impossible to estimate the frequency occurrence of violations):
- nervous system: often - drowsiness, dizziness, sensitivity disorders, including decreased sensitivity and paresthesia;
- respiratory system / chest organs: often - shortness of breath;
- vessels: often - hot flashes, a transient increase in blood pressure (soon after taking Sumatriptan);
- musculoskeletal / connective tissue: often - a feeling of heaviness (usually transient, can be intense and appear in any part of the body, including the throat and chest), myalgia;
- digestive system: often - vomiting, nausea (a causal relationship with the intake of Sumatriptan has not been proven);
- instrumental / laboratory data: very rarely - slight deviations in liver function tests;
- general disorders: often - pain, feeling of heat or cold, constriction or pressure (usually transient, can be intense and appear in any part of the body, including the throat and chest), fatigue and weakness (usually transient, weak or moderate pronounced character).
Violations recorded during post-registration observations:
- immune system: with an unknown frequency - hypersensitivity reactions (from skin manifestations of hypersensitivity to anaphylaxis);
- musculoskeletal / connective tissue: with unknown frequency - arthralgia, neck stiffness;
- digestive system: with an unknown frequency - diarrhea, ischemic colitis;
- skin / subcutaneous tissue: with unknown frequency - hyperhidrosis;
- psyche: with an unknown frequency - anxiety;
- nervous system: with an unknown frequency - seizures (sometimes observed in patients with a history of seizures or in the presence of concomitant conditions that predispose to seizures; in some patients, risk factors were not identified), scotoma, tremor, nystagmus, dystonia;
- cardiovascular system: with an unknown frequency - bradycardia, tachycardia, palpitations, angina pectoris, arrhythmias, signs of transient myocardial ischemia on the ECG, coronary vasospasm, myocardial infarction, Raynaud's syndrome, lowering blood pressure;
- organ of vision: with an unknown frequency - diplopia, flickering, decreased visual acuity / loss of vision (usually transient; it must be taken into account that visual impairments may be associated with a migraine attack).
Overdose
The development of any other adverse reactions, except for the above, when taking a dose of 400 mg is not observed.
In case of an overdose for at least 10 hours, the patient's condition should be monitored, if necessary, supportive treatment is carried out. There is no information on the effect of peritoneal dialysis / hemodialysis on the plasma concentration of sumatriptan.
special instructions
Before starting therapy for a headache attack in patients who have not previously been diagnosed with migraine, or with an atypical form of migraine, other potentially serious types of neurological pathology should be excluded. Patients with migraine are at increased risk of developing certain cerebrovascular disorders (eg, transient ischemic attacks or stroke).
After taking Sumatriptan, pain and pressure in the chest may develop. Symptoms can be intense and extend to the neck. If there is reason to believe that these disorders are a manifestation of coronary heart disease, the drug is not used in the future, and an appropriate diagnostic examination should be carried out.
In cases of risk factors for the onset of coronary heart disease, including heavy smokers or patients using nicotine replacement therapy, it is not recommended to prescribe Sumatriptan without preliminary examination of the cardiovascular system. Postmenopausal women and men over 40 years of age who have the listed risk factors need special attention. However, it should be borne in mind that examination to reveal heart disease does not always allow, and in very rare cases, serious cardiac complications were observed in patients without concomitant cardiovascular diseases.
During the period of therapy, a small number of patients with mild controlled arterial hypertension experienced a transient increase in peripheral vascular resistance and blood pressure, and therefore Sumatriptan was prescribed with caution.
There are rare reports, received during post-registration observation, about the development of serotonin syndrome (includes mental status disorders, neuromuscular disorders and autonomic lability) with the combined use of Sumatriptan with selective serotonin reuptake inhibitors (SSRIs). There is also evidence of the occurrence of serotonin syndrome against the background of combined use with triptans and selective norepinephrine reuptake inhibitors (SNRIs). If it is necessary to carry out a combination therapy, the patient's condition should be monitored.
Caution when using Sumatriptan must be observed in cases of the likelihood of a significant change in the absorption, metabolism or excretion of the active substance of the drug, in particular, in hepatic insufficiency or impaired renal function. The initial dose in patients with hepatic impairment should not exceed 50 mg.
Long-term use of any type of pain reliever for headaches can worsen the pain. In cases of such a situation or suspicion of it, Sumatriptan should be canceled and an additional examination should be carried out. Overuse headache may be suspected in patients with daily / recurrent headaches despite the regular use of headache medication.
Influence on the ability to drive vehicles and complex mechanisms
Due to the fact that against the background of migraine, the development of drowsiness associated with illness / therapy is possible, caution must be exercised when driving vehicles.
Application during pregnancy and lactation
The drug is contraindicated for use during pregnancy and lactation.
During lactation, the resumption of breastfeeding is possible 24 hours after taking Sumatriptan.
Pediatric use
According to the instructions, Sumatriptan is not prescribed to children under 18 years of age (due to insufficient clinical data confirming the effectiveness / safety of the drug).
With impaired renal function
- severe renal dysfunction: therapy is contraindicated;
- renal impairment: Sumatriptan must be used with caution.
For violations of liver function
- severe violations of hepatic function: therapy is contraindicated;
- hepatic impairment: Sumatriptan should be used with caution.
Use in the elderly
Patients over 65 years of age are not prescribed Sumatriptan, which is due to the lack of clinical data confirming its effectiveness / safety.
Drug interactions
With the combined use of Sumatriptan with certain drugs / substances, the following effects may develop:
- ergotamine or other triptans / 5-HT 1 -serotonin receptor agonists: there is a theoretical possibility of an increased risk of coronary vasospasm; the combination is contraindicated (a break after taking these drugs should be at least 24 hours, after taking Sumatriptan - at least 6 hours);
- monoamine oxidase inhibitors: development of interaction; the combination is contraindicated;
- drugs containing St. John's wort: more frequent development of side reactions of Sumatriptan;
- SSRI, SSRI: development of serotonin syndrome.
Analogs
The analogues of Sumatriptan are: Sumamigren, Trimigren, Sumitran, Amigrenin, Sumarin, Rapimed, Imigran.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Sumatriptan
According to reviews, Sumatriptan is an effective drug, more affordable in comparison with a number of analogues. It is noted that the drug in many cases relieves migraine attacks that last for several days and are not relieved by other anesthetic drugs.
Among the shortcomings, they usually indicate prolonged weakness after administration. In these cases, after taking the pill, it is recommended to remain calm (best of all - sleep in a dark and quiet place). They also note the development of side effects and the fact that the drug is quite expensive if attacks occur frequently.
Price for Sumatriptan in pharmacies
The approximate price for Sumatriptan is:
- coated tablets: 50 mg each (2 pcs. in a package) - 70-120 rubles; 100 mg each (2 or 10 pcs. in a package) - 120-185 or 600-675 rubles;
- tablets of 100 mg (2 pcs. in a package) - 130-175 rubles.
Sumatriptan: prices in online pharmacies
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
