Expiration date: 05/2025

The composition and form of issue:

Tablets, film-coated. 1 tablet contains tizanidine 2, 4 or 6 mg

excipients: MKC — 101,02 or 127,64 of 74.71 mg of lactose monohydrate — 79 109,43 or 118,14 mg stearic acid is 0.3 to 0.4 or 0.5 mg silicon dioxide, colloidal anhydrous — or 6,864 4,576 of 2.88 mg 

in a contour acheikova packing 10 PCs. in cardboard pack 1,3 or 5 packs.

Description pharmaceutical form:

Tablets white or almost white, ploskotsylindriceskie, with chamfer on both sides.

Tablets 2 mg: scored one side and engraved "2" on the other.

Tablets 4 mg: with cross scored on one side and engraved "4" on the other.

Tablets 6 mg: with cross scored on one side and engraved "6" on the other.

Feature:

Relaxant skeletal muscles of the Central action.

Pharmacokinetics:

If ingestion is absorbed rapidly and almost completely. Cmax in plasma is reached after about 1 h after ingestion. Because of pronounced metabolism at the first passage through the liver average bioavailability is about 34%. The plasma protein binding is 30%. In the dose range of 4 to 20 mg pharmacokinetics of tizanidine has linear character. Interindividual variability of pharmacokinetic parameters is low. Gender does not affect the pharmacokinetics of tizanidine. Metabolized in the liver, mainly by the isoenzyme 1A2 of cytochrome P450. The active metabolites. T1/2 is 2-4 h. write mainly kidneys in the form of metabolites, a small part — in not changed kind.

In patients with renal insufficiency (Cl creatinine less than 25 ml/min) the average value of Cmax in the plasma in 2 times exceeded this indicator in healthy volunteers, T1/2 was extended to 14 h.

Simultaneous eating does not affect the pharmacokinetics of tizanidine.

Description pharmacological action:

Stimulating presynaptic ALPHA2-adrenergic receptors, Titanyl inhibits the release of excitatory amino acids that stimulate the receptors to N-methyl-D-aspartate (NMDA receptors). Consequently, at the level of intermediate neurons of the spinal cord are suppressed polysynaptic excitation transfer. Since this mechanism is responsible for excessive muscle tone, when you the suppression of muscle tone decreases. In addition to the muscle relaxant effect of tizanidine also has a moderate Central analgesic effect.

Indications:

• painful muscle spasm associated with static load and functional disorders of the spine and after surgery
  
• the skeletal muscle spasm in neurologic diseases (disseminated sclerosis, chronic myelopathy, degenerative diseases spinal cord, cerebral circulatory disorders, cerebral palsy) in patients older than 18 years.
  

Contraindications:

• hypersensitivity to any component of the drug
  
• marked disorders of liver function
  
• concomitant use of fluvoxamine
  
• pregnancy
  
• lactation
  
• children up to age 18 years (insufficient data).
  

With caution:

• renal failure
  
• old age
  
• the simultaneous use with inhibitors of isoenzyme CYP1A2 (antiarrhythmic drugs — amiodarone, meksiletin, propafenone cimetidine, fluoroquinolones, rofecoxib, oral contraceptives, tiklopidin).
  

Application of pregnancy and breast-feeding:

Contraindicated in pregnancy. At the time of treatment should stop breastfeeding.

Side effects:

Drowsiness, weakness, dizziness, minor decrease in blood pressure, dry mouth, nausea, gastrointestinal disorders, transient increase in liver transaminases.

While taking the drug in higher doses the following possible effects: hypotension, bradycardia, muscle weakness, insomnia, sleep disorders, hallucinations, acute hepatitis (very rare), anxiety.

Drug interactions:

Concurrent use with fluvoxamine leads to a 33-fold increase in the area under the curve "concentration-time" tizanidine, resulting in developing long-lasting decrease in blood pressure, drowsiness, weakness and lethargy.

While the application was Titania with antihypertensive drugs (including diuretics) may develop hypotension and bradycardia.

Sedatives and alcohol may enhance the sedative effect was Titania.

Concomitant use of oral contraceptives leads to a significant reduction in the clearance of tizanidine.

Method of application and dose:

Inside.

For painful muscle spasm 2-4 mg 3 times a day. In severe cases, at bedtime additional 2-4 mg.

When spasticity of skeletal muscles, the initial dose should not exceed 6 mg (3 admission). Gradually increase by 2-4 mg every 3-7 days. Optimal therapeutic effect is achieved at a daily dose of 12-24 mg (in 3-4 divided doses, at equal intervals of time). The maximum daily dose should not exceed 36 mg/day.

In patients with renal insufficiency is recommended to start treatment with doses of 2 mg 1 time per day. The increase in dose should be gradual, focusing on tolerability and efficacy.

If necessary, increase dose, increase the dosage first appointed 1 time a day, then the multiplicity of the drug.

Overdose:

Symptoms: nausea, vomiting, hypotension, dizziness, somnolence, miosis, restlessness, respiratory failure, coma.

Treatment: to remove the drug from the body it is recommended that multiple-purpose sorbent, such as activated carbon. Perhaps the removal was Titania will also accelerate forced diuresis. Further symptomatic therapy.

Special instructions:

Reported cases of liver dysfunction associated with tizanidine, however, when applied to a daily dose of 12 mg it's unlikely. In this regard, it is recommended to monitor liver function tests 1 per month in the first 4 months of treatment, and if the levels of ALT and AST in serum consistently exceed the upper limit of normal 3 times or more, the application has Titania should be discontinued.

Patients who have marked drowsiness should refrain from activities that require high concentration and speed of psychomotor reactions, such as driving or working with machines and mechanisms.