Rapiped - instructions for use, doses, side effects, contraindications

active substance: sumatriptan succinate 70 mg corresponding to 50 mg sumatriptan. Excipients: lactose monohydrate 70 mg, croscarmellose sodium 6 mg, lactose anhydrous (Pharmatose DCL 21) 105.7 mg, microcrystalline cellulose (Avicel PH 102) 45.3 mg, magnesium stearate 3 mg. shell: lactose monohydrate 4.32 mg, mannitol 2.76 mg, titanium dioxide 24 mg, talc 1.8 mg, triacetin 0.72 mg.

1 tablet, film-coated, 100 mg contains:

active substance: sumatriptan succinate 140 mg corresponding to 100 mg sumatriptan. ^;

Excipients: lactose monohydrate 140 mg, croscarmellose sodium 12 mg, lactose anhydrous (Pharmatose DCL 21) 211.4 mg, microcrystalline cellulose (Avicel PH 102) 90.6 mg, magnesium stearate 6 mg. shell: lactose monohydrate 8.64 mg, mannitol 5.52 mg, titanium dioxide 4.8 mg, talc 3.6 mg, triacetine 1.44 mg.

Description:

Tablets 50 mg: oval biconvex tablets coated with a film sheath, white with a risk on both sides and side, with an engraving "SN" on one side and "50" on the other side;

Tablets 100 mg: oval biconvex tablets covered with a film shell, white with an engraving "SN" on one side and "100" on the other side.

Pharmacotherapeutic group:Anti-migraine means.

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

Anti-migraine means. A specific selective agonist (5-hydroxytryptamine-1-serotonin receptor) (5HT_ID), localized predominantly in the blood vessels of the brain, does not affect other subtypes of 5-HT-serotonin receptors (5HT₂-5NT₇). Causes narrowing of the vessels of the carotid arterial bed, which supply extracranial and intracranial tissues (the expansion of the vessels of the meninges and / or their edema is the main mechanism of migraine development in humans) without significantly affecting cerebral blood flow. Suppresses the activity of the receptors of the endings of the afferent fibers of the trigeminal nerve in the dura mater (as a result, the secretion of sensory neuropeptides decreases). Both of these effects can underlie the anti-migraine effect of sumatriptan. Eliminates the associated nausea and photophobia associated with migraine attacks. In 50-70% of cases, it quickly eliminates an attack with oral administration in a dose of 25-100 mg. Within 24 hours, a relapse may occur in 1/3 of the cases requiring re-application. The clinical effect is usually seen 30 minutes after ingestion.

Pharmacokinetics:After oral intake quickly absorbed, after 45 minutes its concentration in the plasma reaches 70% of the maximum level. Bioavailability - 14% (due to presystemic metabolism and incomplete absorption). After ingestion 100 mg sumatriptan the maximum concentration in the blood plasma (Cmax) is 54 ng / ml. The connection with plasma proteins is 14-21%, the total volume of distribution is 170 l (2.4 l / kg). Metabolized by oxidation with the participation of monoamine oxidase (MAO) (preferably isoenzyme A) to form the main metabolite - an indoleacetic analog of sumatriptan, which does not have pharmacological activity against 5HT₁-5NT₂-serotonin receptors, the main metabolite is excreted mainly in the urine, in the form of free acid and its glucuronide conjugate. The half-life of sumatriptan (T_1/2) - about 2 hours. Plasma clearance - 1160 ml / min, renal clearance - 260 ml / min; non-adrenal clearance - 80% of the total clearance.

It is excreted by the kidneys, mainly in the form of metabolites (97% after ingestion) - free acid or glucuronide conjugate.

Indications:Migraine (relief of seizures, with or without an aura).

Contraindications:Hypersensitivity to any component of the drug; hemiplegic, basilar or ophthalmoplegic forms of migraine; ischemic heart disease (IHD) (including suspicion of it), angina pectoris (including angina of Prinzmetal), myocardial infarction (including in the anamnesis), postinfarction cardiosclerosis, uncontrolled arterial hypertension, occlusive diseases of peripheral blood vessels, stroke, or transient ischemic attack (including history), taking concomitantly with ergotamine or its derivatives (including metisergid), use against the background of taking MAO inhibitors or earlier than 2 weeks after the withdrawal of these drugs, a pronounced impairment of function liver and / or and kidney, childhood and adolescence (under 18 years), elderly (over 65 years), pregnancy, lactation (within 24 hours after taking the drug).

Carefully:

- epilepsy (including any conditions with a decrease in the threshold of convulsive readiness);

- controlled arterial hypertension;

- impaired liver and kidney function;

- in patients with hypersensitivity to sulfonamides (allergic reactions are possible with severity from skin manifestations to anaphylaxis)

Dosing and Administration:

Inside, swallowing the tablet whole and squeezed water.

Begin treatment as soon as possible after the onset of a migraine attack (although the drug is effective at any stage of the attack).

For relief of acute attacks of migraine, the recommended dose for adults is 50 mg once a day. Some patients may require a higher dose of 100 mg. If the symptoms do not disappear and do not decrease after the first dose, then for cupping the same An attack should not be repeated. However, the drug can be used for cupping subsequent migraine attacks.

If the patient feels better after the first dose and then the symptoms resume, you can take a second dose within the next 24 hours at intervals of at least two hours after taking the first dose. The maximum dose of sumatriptan should not exceed 300 mg during the 24-hour period.

Side effects:

Are common: Pain, a feeling of heat or tingling, a feeling of constriction or heaviness. These symptoms are usually transient, but can be intense and occur about any part of the body, including the chest and throat.

Tides, dizziness, a feeling of weakness, a feeling of fatigue, drowsiness is usually expressed weakly or moderately and is of a transient nature.

From the cardiovascular system: decrease in blood pressure (BP), transient increase in blood pressure (observed soon after taking sumatriptan), bradycardia, tachycardia (including ventricular), arrhythmias, angina pectoris; heart rhythm disturbances, transient ECG changes in ischemic type, myocardial infarction, coronary artery spasm; in isolated cases - Raynaud's syndrome.

From the gastrointestinal tract: nausea, vomiting, ischemic colitis (the association of these side effects with sumatriptan is not established); dysphagia, a feeling of discomfort in the abdomen.

Movement disorders: a feeling of stiffness (these symptoms are usually transient, but can be intense and occur in any part of the body, including the chest and throat); tremor, stiff neck muscles.

From the central nervous system: sensory disorders, including paresthesia; convulsive attacks (in a number of cases they were observed in patients with a history of seizures or in conditions predisposing to the onset of seizures, in some patients predisposing factors were not found), dystopia.

From the sense organs: diplopia, flashing of "flies" before the eyes, nystagmus, scotoma, visual acuity reduction. Very rarely develops a partial transient loss of vision. However, it should be borne in mind that visual impairment can be associated with migraine attacks.

Allergic reactions: skin rash (including hives and erythematous rashes), skin itching, anaphylactic reactions.

From the laboratory indicators: minor changes in activity

"hepatic" transaminases.

Other: shortness of breath, nosebleed.

Overdose:

Symptoms: when ingestion up to 400 mg, there are no other adverse reactions other than those listed above.

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

Interaction:

No interaction of sumatriptan with propranolol, flunarizine, pizotifen and ethyl alcohol has been observed.

With simultaneous administration with ergotamine and ergotamine-containing drugs, a prolonged vasospasm is possible. Sumatriptan can be prescribed no earlier than 24 hours after taking medications,containing ergotamine; and vice versa, preparations containing ergotamine can be prescribed no earlier than 6 hours after taking sumatriptan.

Possible interaction between sumatriptan and MAO inhibitors (decrease in the intensity of metabolism of sumatriptan, increasing its concentration). It is possible to develop a serotonin syndrome with the simultaneous administration of sumatriptan and drugs from the group of selective serotonin reuptake inhibitors (SSRIs) and serotonin and norepinephrine reuptake inhibitors (SSRIs).

The probability of manifestation of side effects increases with the simultaneous administration of sumatriptan with preparations of St. John's wort perfumed.

Special instructions:

Sumatriptan should be prescribed only if the diagnosis of migraine is undoubted, and it should be used as soon as possible after the onset of a migraine attack, although it is equally effective when used at any stage of an attack. It is not intended for the prevention of migraine (introduction during migrnosnon aura to the occurrence of other symptoms may not prevent the development of a headache). As with other antimigraine drugs,when prescribing sumatriptan in patients with a previously unidentified migraine or in patients with atypical migraine, other potentially serious neurologic conditions should be excluded. It should be noted that in patients with migraine, the risk of developing cerebrovascular complications (stroke or transient cerebral circulation disorders) is increased.

Patients at risk of cardiovascular disease do not start therapy without a preliminary examination (women in the postmenopausal period, men over the age of 40, persons with risk factors for the development of IHD). The examination does not always make it possible to identify heart disease in some patients. In very rare cases, patients may experience serious adverse reactions from the cardiovascular system, in whose anamnesis there was no cardiovascular pathology. After taking the drug, transient intense pains and chest tightness that extend to the neck area may occur. If there are reasons to assume that these symptoms are a manifestation of coronary heart disease, it is necessary to conduct an appropriate diagnostic examination.Patients with controlled hypertension should be administered with caution, as in some cases transient increases in blood pressure and peripheral vascular resistance have been observed; in patients with such diseases, which can significantly change the absorption, metabolism or excretion of this drug (for example, a violation of kidney or liver function).

There were very few reports of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) after taking SSRIs and sumatriptan. The development of serotonin syndrome was also reported with the simultaneous administration of triptans and ISOSN. In the case of joint intake of SSRIs / SSRIs and sumatriptan, careful monitoring of this group of patients should be carried out.

Sumatriptan should be used with caution in patients with epilepsy or organic brain lesions in history with a decrease in the threshold of convulsive readiness.

In patients with hypersensitivity to sulfonamides, the administration of sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis.Data on cross-sensitivity are limited, but caution should be exercised when assigning sumatriptan to such patients. Abuse of medicines intended to stop migraine attacks is associated with increased headaches in sensitive patients (headache associated with drug abuse). In this case, the possibility of drug cancellation should be considered. If there is no effect on the administration of the first dose, the diagnosis should be clarified. The experience with sumatriptan in patients older than 65 years is limited (there is no significant difference in pharmacokinetics compared with younger patients).

Do not exceed the recommended dose of sumatriptan.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated 50 mg, 100 mg.

Packaging:For 2 or 3 tablets, film-coated, in a blister of PVC / Al and PVC / PVDC / Al.For 1 blister 2 tablets or 1,2, 4, 6, 8 blisters for 3 tablets together with instructions for use in a pack of cardboard.

Storage conditions:

List B.

In dry, dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children!

Shelf life:

3 years.

Do not use after the expiry date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001389/10

Date of registration:26.02.2010

The owner of the registration certificate:AKTAVIS, LTD. AKTAVIS, LTD. Russia

Manufacturer: & nbsp

AKTAVIS, LTD. Russia

Information update date: & nbsp06.09.2015

Illustrated instructions

Instructions

Rapimede (Rapimed)