Sumatriptan - instructions for use, dose, side effects, contraindications

A selective agonist of serotonin 5-HT1 receptors located mainly in the blood vessels of the brain. Does not affect other serotonin receptor subtypes (5-HT2-7).

Pharmacokinetics:

Absorption at ingestion, intranasal and n / k introduction is rapid. F 15% for ingestion, 17% for intranasal use, 97% for p / to administration, quickly distributed in the body tissues, passage through the BBB is limited. The connection with plasma proteins is ~ 14-21%. Biotransformation in the liver. The half-life is 2-2.5 hours. Elimination by the kidneys (97% in the form of metabolites).

Indications:

Coping of migraine attacks and Horton's syndrome (histamine cephalalgia).

ICD-10

VI.G40-G47.G43 Migraine

VI.G40-G47.G44.0 "Syndrome" of "histamine" "headache"

Contraindications:

Hypersensitivity; hemiplegic, basilar or ophthalmoplegic forms of migraine; IHD (including suspected), angina pectoris (including Prinzmetal angina), myocardial infarction (including in anamnesis), uncontrolled AH, occlusive diseases of peripheral arteries, stroke or transient ischemic stroke (including in anamnesis), hepatic and / or kidney failure.

Carefully:

Epilepsy (including any condition with reduced convulsive threshold), controlled by AH, pregnancy, breast-feeding, children and adolescence (under 18 years of age),elderly age (over 65 years), simultaneous use of drugs containing ergotamine and its derivatives, as well as MAO inhibitors and the first 2 weeks after their cancellation.

Pregnancy and lactation:

The clinical experience of using sumatriptan in pregnancy is limited, and therefore it is contraindicated for use.

With caution should be used during lactation. It is not recommended to breast-feed a baby for 24 hours after taking sumatriptan.

FDA recommendation category C.

Dosing and Administration:

To stop a migraine attack for ingestion, the dose is 100 mg once; sometimes an effective dose may be less than 100 mg; in case of resumption of an attack, repeated administration is possible, with the daily dose not exceeding 300 mg. S / o injected at a dose of 6 mg; if necessary, repeated injection at the same dose can be performed no earlier than 1 hour after the first administration; the maximum daily dose of sc - 12 mg.

With Horton's syndrome injected sc in a dose of 6 mg once during an attack; the maximum daily dose is 12 mg; the interval between injections is at least 1 hour.

Side effects:

From the side of the central nervous system: dizziness, weakness, drowsiness.

From the side of the cardiovascular system: arterial hypotension or a short-term increase in blood pressure, bradycardia or tachycardia.

From the digestive system: nausea, vomiting.

Dermatological reactions: skin rashes, erythema, itching.

Local reactions: with p / to the introduction - a short-term pain at the injection site.

Other: sensation of heat, tingling, pain, pressure, or constriction in different parts of the body.

Overdose:

Severe severity of adverse reactions. The average dose that can cause an overdose: 400 mg when taken orally, 16 mg with p / to the introduction, 40 mg with a nasal spray.

Treatment is symptomatic. It is necessary to monitor the patient within 10 hours. There is no information on the effectiveness of hemodialysis.

Interaction:

MAO inhibitors - a decrease in the intensity of metabolism of sumatriptan, an increase in its concentration in plasma; hypertensive crisis, severe hyperthermia, convulsive paroxysms. The interval between taking drugs should be at least 14 days.

Selective inhibitors of serotonin reuptake - weakness, hyperreflexia, movement coordination disorders.

Ergotamine and ergotamine-containing drugs - a prolonged vasospasm.Reception should be disconnected in time not less than 1 day.

Special instructions:

Common for all the triptans.

Not intended to prevent migraine: the introduction during the migraine aura before the onset of other symptoms does not prevent the development of a headache.

In 50-70% of cases, a sudden attack of migraine when administered in a dose of 25-100 mg. Within 24 hours, a relapse may occur in 1/3 of the cases requiring re-use of the drug.

Tablets are swallowed whole (without breaking, not chewing), squeezed with enough water.

Patients at risk (who have cardiovascular disease) should be examined before starting the treatment. The risk group also includes postmenopausal women, men over the age of 40, persons with IHD risk factors.

When appointing during breastfeeding, it is not recommended to breast-feed the baby for 24 hours after taking the medication.

In the absence of the effect of taking the first dose, the diagnosis should be clarified.

The experience with sumatriptan in patients older than 65 years is limited, but there is no significant difference in pharmacokinetics compared with younger patients.

Before prescribing sumatriptan, patients with newly diagnosed or atypically migraine should exclude other potentially dangerous neurological diseases.

It should be borne in mind that in patients suffering from migraine, there is a risk of developing a stroke or transient disorders of the cerebral circulation.

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Almotriptan in a dose of 12.5 mg can serve as an alternative drug for patients who have sumatriptan in a dose of 50 mg does not produce the desired effect.

Instructions

Sumatriptan (Sumatriptanum)

Coping of migraine attacks and Horton's syndrome (histamine cephalalgia).