Instruction for use: Sumatriptan

The Latin name of the substance Sumatriptan

Sumatriptanum (genus. Sumatriptani)

Chemical name

3- [2- (Dimethylamino) ethyl] -N-methylindole-5-methanesulfonamide (and as a succinate)

Gross formula

C₁₄H₂₁N₃O₂S

Pharmacological group

Serotonergic agents

The nosological classification (ICD-10)

G43 Migraine: The pain of migraine; Migraine; hemiplegic migraine; Migraine headache; A migraine attack; Continuous headache; hemicranias

G43.0 Migraine without aura [simple migraine]: Migraine without aura

G43.1 Migraine with aura [classic migraine]: Basilar migraine; Migraine with aura

CAS Code

103628-46-2

Characteristics of substance Sumatriptan

Selective 5-HT1 receptor agonist. White or off-white powder, easily soluble in water and saline.

Pharmacology

Pharmacological action - antimigraine.

Is reacted with 5-HT1-receptors (not affect the subtypes of 5-HT2 - 5-HT7-receptors), especially in the blood vessels of the brain (stimulation of 5-HT1-receptors leads to vasoconstriction). Selectively excites serotonin 5-HT1D-receptor cerebral vessels (dura basilar artery), inhibits activation of the trigeminal system and reduces the accumulation of specific stimulating protein in the nuclei of the trigeminal nerve, activates antinociceptive serotonergic mechanisms brainstem. It causes a narrowing of the vessel dilated during an attack and thus stops the attack. It stops the development of a migraine attack without having a direct analgesic effect.

Quickly absorbed when taken orally and after intranasal use. Bioavailability is 15% due to presystemic metabolism and incomplete absorption. Cmax when administered 100 mg is 51 ng / ml and is achieved within 2-2.5 hours (with migraine attacks somewhat faster than in the inter-rush period). After intranasal administration, Cmax in plasma is 12.9 ng / ml and is reached after 1-1.5 hours. The level of binding to plasma proteins is low (14-21%). The average volume of distribution is 2.4 l / kg. Biotransformiroetsa involving MAO, preferably the MAO A, with the formation of metabolites, the main ones are indoleacetic analogue sumatriptan without having pharmacological activity towards the 5-HT1- and 5-HT2-receptor, and its glucuronide; Secondary metabolites are not identified. T1 / 2 is 2.5 hours, the total plasma clearance is 1160 ml / min on average, the kidney clearance is 260 ml / min, the extra-neural clearance is about 80% of the total clearance. It is excreted by the kidneys (renal excretion - about 60%, mainly in the form of inactive metabolites - 97%), the rest is excreted with feces.

The clinical effect is usually observed 30 minutes after oral administration of sumatriptan at a dose of 100 mg and 15 minutes after intranasal administration of 20 mg. In 50-70% of cases, quickly stops migraine attack with oral administration at a dose of 25 to 100 mg. Eliminates the associated with migraine attack nausea and photophobia. The greatest effect is observed when used at the height of an attack. About a third of cases within the next 24 hours, a relapse may occur, which necessitates repeated use.

Application of substance Sumatriptan

Curbing migraine attacks (with or without aura).

Contraindications

Hypersensitivity, hemiplegic, basilar or oftalmoplegicheskaya form of migraine, myocardial infarction (including history), uncontrolled hypertension, coronary heart disease (including suspected it), angina, including Prinzmetal angina, occlusive peripheral vascular disease, transient ischemic attack (including history), stroke (including history), expressed by the liver and / or kidney, simultaneous ergotamine or with sumatriptan its derivatives (Including metisergid), as well as simultaneous administration of MAO inhibitors and a period of up to 2 weeks after their withdrawal.

Restrictions on the use

Epilepsy (including any condition with a reduction in seizure threshold), hypertension (controlled), pregnancy, breast-feeding, age and 18 years of age (safety and efficacy not established), age over 65 years (application experience is limited).

Application in pregnancy and lactation

When pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus (adequate and strictly controlled safety studies have not been carried out). Avoid breastfeeding for 24 hours after applying sumatriptan (penetrates into breast milk).

Side effects of Sumatriptan

From the cardiovascular system and blood (hematopoiesis, hemostasis): a decrease in blood pressure, a temporary increase in blood pressure (observed soon after admission), bradycardia, tachycardia (including ventricular), palpitations; In some cases - cardiac rhythm disturbances (up to ventricular fibrillation), transient ECG changes of ischemic type, myocardial infarction, coronary artery spasm; Sometimes Raynaud's syndrome develops.

On the part of the intestine: nausea and vomiting (usually with ingestion), a slight increase in liver enzymes, dysphagia, a feeling of discomfort in the abdomen; Rarely is ischemic colitis.

From the nervous system and sensory organs: dizziness, weakness and / or fatigue (more often with ingestion), drowsiness (usually mild or moderately expressed and of a transient nature); In some cases - convulsive attacks (usually in the presence of seizures in the history or in conditions predisposing to the occurrence of seizures); Sometimes - diplopia, flies flies before the eyes, nystagmus, scotoma, reduced visual acuity; Very rarely - a partial transient loss of vision (visual impairment can be associated with the very seizure of the migraine).

Reactions of hypersensitivity: skin manifestations (rash, hives, itching, erythema); In rare cases - anaphylaxis.

Other: pain, tingling, fever, feeling of pressure or heaviness (usually transient, but can be intense and occur in any part of the body, including the thorax and throat), myalgia, flushing of the blood to the face.

Local symptoms (with intranasal application): slight transient irritation or burning sensation in the nasal cavity and / or pharynx, nosebleeds.

Interaction

With simultaneous administration with ergotamine and ergotamine-containing drugs, a prolonged vasospasm was noted (sumatriptan can be prescribed not earlier than 24 hours after taking medications containing ergotamine, and preparations containing ergotamine can be prescribed no earlier than 6 hours after taking sumatriptan). Possible interaction between sumatriptan and MAO inhibitors (their simultaneous use is contraindicated). Possible interaction between sumatriptan and drugs from the group of selective serotonin reuptake inhibitors (SSRIs). No interaction of sumatriptan with propranolol, flunarisin, pizotifen and ethyl alcohol has been observed.

Overdose

Treatment: monitoring the patient for at least 10 hours, if necessary, maintenance therapy. There is no data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in plasma.

Routes of administration

Inside, intranasal.

Precautions for the substance of Sumatriptan

Not intended to prevent migraine headaches. The administration of the drug is possible only if the diagnosis is not in doubt. When prescribing sumatriptan in patients with a previously undiagnosed migraine or in patients with atypical migraine, other potentially serious neurological conditions should be excluded (as with other antimigraine drugs). It should be borne in mind that in patients with migraine increased risk of cerebrovascular disorders (for example, stroke or transient ischemic stroke).

The presence of risk factors from the cardiovascular system (women in the postmenopausal period, men over the age of 40 and patients with risk factors for the development of coronary artery disease) dictates the need for a preliminary examination to exclude cardiovascular pathology.

We reported the development of weakness, hyperreflexia and coordination failure after taking sumatriptan and drugs from the SSRI group (in the case of their simultaneous appointment, the patient's condition should be closely monitored).

Before and during treatment, it is necessary to eat regularly, keep to a diet, exclude products containing tyramine (chocolate, cocoa, nuts, citrus, beans, tomatoes, celery, cheeses), as well as alcoholic beverages (including dry, especially red, Wine, champagne, beer), to lead a healthy lifestyle, go in for sports (swimming, skiing, walking), have some passion that creates a positive emotional state and thereby prevents the emergence of migraine attacks.

People with hypersensitivity to sulfanilamides have a history of increased risk of allergic reactions. With caution appoint drivers of vehicles and people engaged in potentially hazardous activities that require increased attention and speed of response.