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

Lactose monohydrate is 32.5 mg, anhydrous lactose is 21.5 mg,cellulose microcrystalline - 17.75 mg, croscarmellose sodium - 3 mg, silicon dioxide colloid - 1.5 mg, magnesium stearate - 2.25 mg, talc - 1.5 mg, purified water * - q.s.

- - evaporates in the production process.

- Tablets 100 mg

Each tablet contains

Active substance:

Sumatriptan succinate 140 mg,

equivalent to sumatriptan 100 mg.

Excipients:

Lactose monohydrate - 65 mg, anhydrous lactose - 43 mg, microcrystalline cellulose - 35.5 mg, croscarmellose sodium - 6 mg, silicon dioxide colloid - 3 mg, magnesium stearate 4.5 mg, talc - 3 mg, purified water * q.s.

- - evaporates in the production process

Description:

Tablets 50 mg:

Tablets from white to almost white, oval, biconcave, with a separation risk on both sides and with engraving "S" and "50" on each side of the risks from one side of the tablet.

Tablets 100 mg:

Tablets from white to almost white, oval, biconvex, with a separation risk on both sides and with engraved "S" and "100" on each side of the risks from one side of the tablet.

Pharmacotherapeutic group:Anti-migraine means.

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:Anti-migraine means.Specific and selective agonist of 5-HT1-serotonin receptors, localized predominantly in the blood vessels of the brain, and does not affect other subtypes of 5-HT-serotonin receptors (5-HT2-7). 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). 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 onset of action is 30 minutes after oral administration of the drug.

Pharmacokinetics:After oral administration sumatriptan quickly absorbed, 70% of the maximum plasma concentration is achieved after 45 minutes.After taking 100 mg, the maximum concentration in the blood plasma is an average of 54 ng / ml. Bioavailability is 14% due to intensive pre-systemic metabolism and incomplete absorption. The connection with plasma proteins is low (14-21%). The total volume of distribution is 170 l (2.4 l / kg). Sumatriptan metabolized under the action of monoamine oxidase (MAO) (preferably isoenzyme A). The main metabolite, indoleacetic analogue of sumatriptan, is excreted, mainly in urine, in the form of free acid and glucuronide. This metabolite has no activity with respect to 5HT, - and 5HT2-serotonin receptors. The half-life period (T1 / 2) is 2-2.5 hours. The plasma clearance is 1160 ml / min, the renal clearance is 260 ml / min, the extra-neural clearance is 80% of the total clearance.

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

The migraine attacks do not have a significant effect on the pharmacokinetics of sumatriptan taken internally.

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

Contraindications:

- Hypersensitivity to the components of the drug;

- hemiplegic, basilar or ophthalmoplegic forms of migraine;

- ischemic heart disease (IHD) (including suspected of it), angina (incl.stenocardia Prinzmetal), myocardial infarction (including in the anamnesis);

- stroke or transient impairment of cerebral circulation (including in anamnesis);

- Occlusal diseases of peripheral vessels;

- arterial hypertension (uncontrolled);

- simultaneous administration of medications containing ergotamine and its derivatives (including methylsigid);

- simultaneous application with ergot alkaloids and their derivatives is contraindicated within 24 hours, as well as other 5-HT1-serotonin receptor agonists;

- use against the background of taking MAO inhibitors and up to 14 days after their withdrawal;

- deficiency of lactase, lactose intolerance, glucose-galactose malabsorption;

- severe hepatic and / or renal insufficiency;

- age is 18 years and over 65;

- pregnancy and latency.

Carefully:

- controlled arterial hypertension;

- diseases in which absorption, metabolism or excretion of sumatriptan may change (eg, impaired renal and hepatic function);

- epilepsy (including any condition with a reduced threshold of convulsive readiness);

- in patients with hypersensitivity to sulfanilamides, taking sumatriptan may cause allergic reactions of varying severity (from skin manifestations to anaphylaxis).Data on cross-sensitivity are limited, however, sumatriptan should be administered to such patients with caution.

Pregnancy and lactation:Do not prescribe Sumarin to pregnant women and women during breastfeeding.

Dosing and Administration:Inside. Treatment begins as soon as possible after the onset of a migraine attack (although the drug is equally effective at any stage of the attack). The recommended dose is one tablet of 50 mg (the tablet should be swallowed whole, washed down with water). Some patients may need a higher dose of 100 mg. If migraine symptoms do not disappear and do not decrease after taking the first dose, then the drug is not prescribed again to stop the ongoing attack. To stop subsequent attacks (with a decrease or disappearance of symptoms and then resume), you can take a second dose within the next 24 hours, provided that the interval between admission is at least 2 hours. During any 24-hour period, the maximum dose of the drug should not exceed 300 mg / day.

Side effects:

Undesirable adverse reactions are listed below, depending on the anatomical and physiological classification and frequency of occurrence.The frequency is defined as follows: very often (> 1/10); often (> 1/100 and <1/10); infrequently (> 1/1000 and <1/100); rarely (> 1/10000 and <1/1000); very rarely (<1/10000), including individual cases.

From the nervous system

Often: dizziness, drowsiness, sensitivity disorders, including paresthesia and decreased sensitivity.

Rarely: convulsive seizures (in a number of cases observed in patients with convulsive attacks in the anamnesis or with concomitant conditions predisposing to the onset of seizures), tremor, dystonia, nystagmus, scotoma.

From the side of the cardiovascular system

Often: transient increase in blood pressure (soon after taking the drug), "hot flashes".

Rarely: bradycardia, tachycardia, cardiac arrhythmias, arrhythmias, ECG transient changes, coronary vasospasm, angina pectoris, myocardial infarction, lowering of arterial pressure, Raynaud's syndrome.

From the respiratory and thoracic

Often: dyspnea, mild transitory irritation of the mucosa or burning sensation in the nasal cavity or throat, nosebleeds.

From the gastrointestinal tract:

Often: nausea, vomiting (cause-and-effect relationship not proven).

Rarely: ischemic colitis, dysphagia, a feeling of discomfort in the abdomen.

From the side of the musculoskeletal system and connective tissue:

Often: feeling of heaviness (usually transient, can be intense and arise in

any part of the body, including the thorax and throat).

From the immune system

OcheMr.rarely: hypersensitivity reactions, including skin manifestations, as well as anaphylaxis.

From the side of the organ of vision

Rarely: flickering before the eyes, diplopia, decreased visual acuity, blindness (usually transient). However, visual disturbances can be caused by the actual migraine attack.

General and local reactions

Often: pain, a feeling of cold or heat, a feeling of pressure or constriction (usually transient, can be intense and occur in any part of the body, including the chest and throat), weakness, fatigue. Overdose:

When administered by Sumarin in a dose of up to 400 mg, there are no side effects other than those listed above.

In the case of an overdose of Sumarin, patients should be monitored for at least 10 hours.If necessary, symptomatic therapy is performed. Data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in plasma are absent.

Interaction:

With simultaneous use with ergotamine and ergotamine-containing medicines, a prolonged vasospasm is possible (Sumarin can be taken no earlier than 24 hours after taking medications containing ergotamine, and vice versa, drugs containing ergotamine can be used not earlier than 24 hours after admission Sumarin).

Possible interaction between sumatriptan and monoamine oxidase (MAO) inhibitors. Simultaneous application of Sumarin and MAO inhibitors is contraindicated. In rare cases, as a result of the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan, the development of serotonin syndrome (including psychiatric disorders, autonomic lability and neuromuscular disorders) is possible. It is also possible the development of serotonin syndrome with the simultaneous administration of tryptanes with selective serotonin and noradrenaline reuptake inhibitors (SSRIs).

Special instructions:

Sumarin 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 to prevent migraine (introduction during the migraine aura before the onset of other symptoms may not prevent the development of a headache).

When appointing Sumarin, patients with a previously diagnosed migraine or patients with an atypical migraine should exclude other potentially serious neurological conditions. It should be borne in mind that in patients with migraine there is a risk of developing a stroke or transient disorders of the cerebral circulation. Patients at risk of cardiovascular disease do not begin therapy without a preliminary examination (women in the postmenopausal period, men over the age of 40, persons with risk factors for coronary heart disease (CHD)). The performed examination does not always allow revealing 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.If there is no effect on the administration of the first dose, the diagnosis should be clarified. After taking the sumarin, there may be pain and a feeling of tightness in the chest. The pain can be intense and radiate into the neck. If there is reason to believe that these symptoms are manifestations of coronary heart disease (CHD), an appropriate examination is necessary.

Patients with controlled arterial hypertension should be administered with caution, as in some cases transient increases in blood pressure and periphyrical vascular resistance were 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).

It is necessary to monitor the patient's condition in case of simultaneous use of SSRI / SSRIs and sumatriptan.

Sumarin should be used with caution in patients with epilepsy and organic brain lesions in the anamnesis with a decrease in the threshold of convulsive readiness.

In patients with hypersensitivity to sulfanilamides, 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.

It is not recommended concomitant use of other tryptans / agonists of 5-HT1-serotonin receptors with Sumarin.

In sensitive patients, headaches may be aggravated by the abuse of drugs designed to stop migraine attacks. In this case, the possibility of drug cancellation should be considered.

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 Sumarin.

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 requiring increased concentration of attention and speed of psychomotor reactions, due to the possibility of occurrence of drowsiness associated with both the disease itself and with the use of Sumarin.

Form release / dosage:

Tablets of 50 mg and 100 mg.

Packaging:3 tablets in a blister of aluminum foil and PVC / PVDC; 1 or 2 blisters with instructions for use in a cardboard box.

Storage conditions:In a dry place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001068

Date of registration:27.10.2011

The owner of the registration certificate:Ranbaxy Laboratories LimitedRanbaxy Laboratories Limited India

Manufacturer: & nbsp

RANBAXY LABORATORIES, Ltd. India

Representation: & nbspRABBAYS LABORATORY LIMITEDRABBAYS LABORATORY LIMITED

Information update date: & nbsp04.09.2015

Illustrated instructions

Instructions

Sumarin® (Sumarin®)