Sirdalud

International name: Tizanidine.

Pharmacological action

Active ingredient of Sirdalud – тизанидин – the muscle relaxant of the central action influencing skeletal muscles. The main influence appears on presynaptic a2 – receptors of a spinal cord, stimulating them тизанидин causes inhibition of products of amino acids which stimulate NMDA-receptors. Therefore there is a suppression of spinal neurons at intermediate level, thus excitement transfer is suppressed with a polisinaptichesky way.

Also as well as its analogs Sirdalud has moderate analgesic effect and reduces spasms and clonic spasms.

Sirdalud's pharmacokinetics

At internal reception Sirdalud is soaked up with high speed and almost completely. The maximum value of concentration of Sirdalud in blood comes in 8 hours. Bioavailability because of the expressed metabolism and passing through a liver makes about 34%.

Sirdalud is released from the medicinal capsule for a long time that softens a pharmacokinetic profile and provides support of stability of therapeutic concentration of drug in blood within 24 hours.

On laboratory responses Sirdalud quickly and with high percent is metabolized in a liver.

It is removed preferential through kidneys, on average approximately in 3 hours. About 70% of the accepted dose, are removed in the form of metabolites, invariable are about 2,7% of substance.

The sex of the patient does not influence pharmacokinetics.

At a renal failure the maximum concentration in a blood plasma increases approximately twice, and the elimination half-life increases till 14 o'clock.

As well as at Sirdalud's analogs meal does not influence pharmacokinetics and does not change drug absorption.

Indications to use

Drug Sirdalud is used at the spasms of skeletal muscles caused by neurologic pathologies such as multiple sclerosis, a cerebral palsy, diseases of a spinal cord, disturbance of blood circulation of a brain, a chronic myelipathy, etc.

And also at painful muscular spasms of different etymology:

• functional or static diseases of a backbone;
• postoperative period.

Sirdalud route of administration

At spasms of the skeletal muscles caused by neurologic pathology, the doctor selects an individual dosage, being guided by a clinical picture. According to the instruction Sirdalud is appointed by doses no more than 6 mg a day which are divided into three receptions. After from 3 to 7 days, increase in a dosage on 2-4 mg is possible. An optimum therapeutic dose 12-24 mg a day in 3-4 receptions with an equal interval of time between them are considered. The drug dosage over 36 mg a day is undesirable.

At painful muscular spasms about 2-4 mg 3 times a day are applied. At obviously expressed spasm reception before going to bed in addition of 2-4 mg of drug is possible.

To patients of old age drug is appointed, based on the assumption that at this category of persons the slowed-down renal clearance. In this regard use by elderly people of Sirdalud according to indications of renal activity is undesirable.

To the patients having a renal failure, the initial dose is appointed 2 mg / 24 hour at one time, after a while it is possible to increase a dosage taking into account portability.

About acceptance by Sirdalud's children of responses it is not enough for appointment of it as therapeutic means.

Side effects of Sirdalud

Sirdalud's use in low doses, seldom reveals side effects, and even at manifestation they have not expressed character. Are usually shown in the form of weakness, drowsiness, slight hypotension, dizziness, dryness of a mouth. More rare in the form of gastrointestinal disturbances and nausea.

At higher doses of Sirdalud, responses indicate that side effects have brighter character, but are not indications to drug withdrawal. More often they are shown in the form of bradycardia and arterial hypotension, is more rare in the form of frustration of a dream, muscular weakness, sleeplessness, hallucinations. Extremely seldom the acute hepatitis can be shown.

Contraindications

• Abnormal liver function;
• Hypersensitivity to a tizanidin or other components of drug;
• Combination of a tizanidin to Fluvoksamin.

Pregnancy

Researches on animals did not find teratogenic impact on a fruit. However researches of use of Sirdalud by pregnant women and the feeding women were not conducted, in this regard appointment it is not recommended by the instruction to Sirdalud's pregnant women, except cases when the advantage for mother exceeds possible risk for a fruit. The experiments made on animals showed what тизанидин in insignificant quantities gets into breast milk, in this regard appointment in the period of a lactation is not recommended.

Interaction with other drugs

According to the instruction Sirdalud the patients accepting CYP1 A2 inhibitors and флувоксамин are forbidden to appoint. Care at a combination to other CYP1 A2 inhibitors is also necessary (Pefloksatsin, Amiodaronum, Meksiletin, Propafenon, Pefloksatsin, Tsimetidin, Tsiprofloksatsin, Enoksatsin, oral hormonal contraceptives, Norfloxacin, Tiklopidin and Rofekoksib). At similar combinations dizziness and decrease in a psychomotor system is possible.

Sirdalud's combination to antihypertensives and diuretics can cause arterial hypotension and bradycardia.

Acceptance of sedatives or alcohol strengthens sedative influence of Sirdalud.

Overdose by Sirdalud

There are messages on overdose by Sirdalud, including administration of drug in a dose of 400 mg. Lethal outcomes are not recorded. The overdose is expressed in nausea, vomiting, arterial hypotension, dizziness, concern, a miosis, the broken breath, drowsiness, a coma. It is treated by repeated purpose of enterosorbents and a symptomatic treatment. As well as at Sirdalud's analogs the overdose is well blocked by an artificial diuresis.

Form of release of Sirdalud

Mg tablets 2 or 4.

Storage conditions

Drug is stored at a temperature of +15-+25 degrees of Page. In the places protected from access for children.