Tizanidine

Brand Novartis

In stock 1445 Items

Available since: 2019-09-19

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Clinical Pharmacology

Sirdalud is a centrally acting muscle relaxant. The main point of application of its action is in the spinal cord. By stimulating presynaptic alpha2 receptors, it suppresses the release of excitatory amino acids that stimulate receptors for N-methyl-D-aspartate (NMDA receptors). As a result, at the level of intermediate neurons in the spinal cord, polysynaptic excitation transfer is suppressed. Since this mechanism is responsible for excessive muscle tone, when it is suppressed, muscle tone decreases. In addition to muscle relaxant properties, tizanidine also has a central moderate analgesic effect.

Sirdalud is effective both in acute painful muscle spasm and in chronic spasticity of spinal and cerebral genesis. Reduces spasticity and clonic convulsions, resulting in reduced resistance to passive movements and increases the amount of active movements.

Pharmacokinetics

Suction.
Tizanidine is absorbed quickly and almost completely. The maximum plasma concentration (Cmax) is reached approximately 1 hour after taking the drug. Due to the pronounced metabolism during the "first pass" through the liver, the average bioavailability value is about 34%.

Distribution.
The average value of the volume of distribution during the period of equilibrium with intravenous administration of the drug is 2.6 l / kg. Plasma protein binding is 30%. In the dose range from 4 to 20 mg tizanidine pharmacokinetics is linear. Given the low interindividual variability of pharmacokinetic parameters (in particular, such as Cmax and the area under the concentration-time curve / AUC /), when taking tizanidine inside, one can reliably predict the values of its concentration in plasma. Gender does not affect the pharmacokinetic parameters of tizanidine.

Metabolism.
It has been shown that tizanidine is rapidly and extensively metabolized in the liver. In vitro, it has been shown that tizanidine is mainly metabolized by the 1A2 isoenzyme of the cytochrome P450 system. Metabolites are inactive.

Derivation.
The average half-life of tizanidine from the systemic blood flow is 2-4 hours. The drug is excreted mainly by the kidneys (approximately 70% of the dose) in the form of metabolites; unchanged substance accounts for about 2.7%.

Features of pharmacokinetics in certain groups of patients
It was found that in patients with renal insufficiency (creatinine clearance less than 25 ml / min), the mean C max was 2 times higher than in healthy volunteers, and the final half-life lengthened to about 14 hours, resulting in an average AUC of 6 time.

Food effect
Simultaneous food intake does not affect the pharmacokinetics of tizanidine. Although the Cmax value increases by 1/3, it is believed that this is not clinically significant. No significant effect on absorption (AUC) is noted.

Indications

Painful muscle spasms in diseases of the spine (including osteochondrosis, spondylosis, syringomyelia, hemiplegia, cervical and lumbar syndromes);
After surgery for herniated disc or osteoarthritis of the hip,
Spastic condition of skeletal muscles caused by neurological diseases: multiple sclerosis, chronic myelopathy, degenerative diseases of the spinal cord, disorders of cerebral circulation, stroke, head injuries, cerebral palsy, convulsions of central origin.

Composition

1 tablet contains:
active ingredient: tizanidine (in the form of hydrochloride) 4 mg;
excipients: colloidal anhydrous silicon dioxide; stearic acid; MCC; lactose monohydrate

Tizanidine is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Sirdalud	Novartis	Switzerland	pills
Tizanidin-Teva	Teva	Israel	pills
Tizanil	Simppex Pharma	India	pills
Tizalud	Veropharm	Russia	pills
Sirdalud	Novartis	Switzerland	capsules

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Dosage and Administration

Inside Dosing regimen should be selected individually.

With painful muscle spasm prescribe the drug Sirdalud in a dose of 2 or 4 mg 3 times a day. In severe cases, before bedtime, you can additionally take 2 or 4 mg.

With skeletal muscle spasticity caused by neurological diseases, the dose should be selected individually. The initial daily dose should not exceed 6 mg, divided into 3 doses. The dose can be increased gradually, by 2–4 mg, at intervals of 3–4 to 7 days. Usually, the optimal therapeutic effect is achieved with a daily dose of 12 to 24 mg, divided into 3 - 4 doses at regular intervals. Do not exceed the dose of 36 mg per day.

Use in patients with renal failure. Treatment of patients with renal insufficiency (Cl creatinine

Adverse reactions

Since the cardiovascular system: often - bradycardia, lowering blood pressure.

From the gastrointestinal tract: often - dry mouth; rarely - nausea, gastrointestinal disorders.

Liver: rarely - increased activity of hepatic transaminases, very rarely - hepatitis.

From the musculoskeletal system: rarely, muscle weakness.

Other: often - fatigue.

When taking small doses recommended for relief of painful muscle spasm, drowsiness, fatigue, dizziness, dry mouth, lowering blood pressure (BP), nausea, gastrointestinal disorders, increased liver transaminase activity were noted. Usually, the above-described adverse reactions are moderate and transient.

When receiving higher doses recommended for the treatment of spasticity, the above-mentioned adverse reactions occur more frequently and are more pronounced, but they are rarely so severe that treatment had to be interrupted. In addition, the following phenomena may occur: decreased blood pressure, bradycardia, muscle weakness, insomnia, sleep disturbances, hallucinations, hepatitis.

Contraindications

Carefully
Simultaneous use of Sirdalud with CYP1A2 inhibitors is not recommended.

Drug interactions

The simultaneous use of tizanidine with fluvoxamine or ciprofloxacin, which are inhibitors of cytochrome P450 1A2, is contraindicated. The simultaneous use of tizanidine with fluvoxamine or ciprofloxacin leads to a 33-fold or 10-fold increase in AUC of tizanidine, respectively. The result of the combined use may be a clinically significant and prolonged decrease in blood pressure, leading to drowsiness, dizziness, inhibited psychomotor reactions. Do not recommend the simultaneous appointment of tizanidine with other inhibitors of CYP1A2 - antiarrhythmic drugs (amiodarone, mexiletin, propafenone), cimetidine, fluoroquinolones (enoxacin, pefloxacin, norfloxacin), rofecoksibom, oral contraceptives, ticlopidine.

The simultaneous appointment of Sirdalud with antihypertensive drugs, including diuretics, can sometimes cause a decrease in blood pressure and bradycardia. Alcohol or sedatives can enhance the sedative effect of the Sirdalud.

Pregnancy and Lactation

Since controlled studies on the use of tizanidine in pregnant women have not been conducted, it should not be used during pregnancy, unless the potential benefit outweighs the potential risk. Tizanidine is excreted in breast milk in small quantities, however, women who are breastfeeding children should not use the drug.

Special instructions

It was reported cases of dysfunction of the liver associated with tizanidine, however, when using a daily dose of up to 12 mg, these cases were rarely observed. In this regard, it is recommended to monitor functional liver function tests 1 time per month in the first 4 months of treatment in those patients who are prescribed tizanidine in a daily dose of 12 mg and above, as well as in cases where there are clinical signs suggesting impaired liver function, - such as unexplained nausea, anorexia, fatigue. In the case when serum ALT and ACT levels consistently exceed the upper limit of the norm by 3 times or more, the use of Sirdalud should be discontinued.

Since lactose is part of Sirdalud pills, it is not recommended to use the drug in patients with rare hereditary intolerance to galactose, with severe lactase deficiency or malabsorption of glucose / galactose.

Impact on the ability to drive a car and work with mechanisms. Patients who have drowsiness or dizziness, should refrain from types of work that require high concentration of attention and quick reaction, for example, driving vehicles or working with machines and mechanisms.

Overdosage

To date, several reports have been received of the overdose of Sirdalud, including the case when the accepted dose was 400 mg. In all cases, recovery was unremarkable.

Symptoms: nausea, vomiting, decrease in blood pressure, dizziness, drowsiness, miosis, anxiety, respiratory failure, coma.

Treatment. For removal of the drug from the body, multiple administration of activated charcoal is recommended. Forced diuresis may also accelerate the elimination of Sirdalud. Further symptomatic treatment is carried out.