Tisanil, pills 4mg, 30pcs

Composition

Each tablet contains as an Active ingredient 2,4 or 6 mg of tizanidine and auxiliary substances-microcrystalline cellulose 74.71,101.02 or 127.64 mg, lactose monohydrate 79.00,109.43 or 118.14 mg, stearic acid 0.30,0.40 or 0.50 mg, colloidal anhydrous silicon dioxide 2.88,4.576 or 6.864 mg

Pharmacological action

By stimulating presynaptic a2 receptors, it suppresses the release of excitatory amino acids that stimulate N-methyl-D-aspartate receptors (NMDA receptors). As a result, polysynapic transmission of arousal is suppressed at the level of intermediate neurons in the spinal cord. Since imekno this mechanism is responsible for excessive muscle tone, when it is suppressed, muscle tone decreases. It also has a central moderate analgesic effect.

Pharmacokinetics:

It is absorbed quickly and almost completely. The maximum concentration in the blood plasma is reached approximately 1 hour after use. Due to the pronounced metabolism during the “first pass” through the liver, the average bioavailability value is about 34%. Binding to plasma proteins is 30%.

In the dose range from 4 to 20 mg, the pharmacokinetics of tizanidine are linear. Inter-individual variability of pharmacokinetic parameters is low. Gender does not affect the pharmacokinetics of tizanidine. It is metabolized in the liver, mainly by isoenzyme 1 A 2 of the cytochrome P 450 system.

Metabolites are inactive. The elimination half-life is 2-4 hours. It is mainly excreted by the kidneys in the form of metabolites, a small part-in unchanged form. In patients with renal insufficiency (creatinine clearance less than 25 ml/min), the average value of the maximum plasma concentration was 2 times higher than in healthy volunteers, and the half-elimination period was extended to 14 hours.

Concomitant food intake does not have a clinically significant effect on the pharmacokinetics of tizanidine.

Indications

• Painful muscle spasm associated with static and functional diseases of the spine, as well as after surgical interventions;
• spasticity of skeletal muscles in neurological diseases (multiple sclerosis, chronic myelopathy, degenerative diseases of the spinal cord, cerebral circulation disorders, cerebral palsy (in patients older than 18 years).

Use during pregnancy and lactation

Contraindicated in children under 18 years of age (due to insufficient data).

Since no controlled studies have been conducted on the use of tizanidine in pregnant women, it should not be used during pregnancy, unless the expected benefit to the mother exceeds the possible risk to the fetus.

Tizanidine slightly penetrates into breast milk, so during breastfeeding, the drug should be discontinued.

Contraindications

• Severe hepatic impairment,
• hypersensitivity to any of the components of the drug,
• concomitant use with fluvoxamine,
• age up to 18 years (due to insufficient data),
• pregnancy and lactation.

With caution: renal insufficiency, elderly, concomitant use with CYP1A2 inhibitors (antiarrhythmic drugs (amiodarone, mexiletine, propafenone), cimetidine, fluoroquinolones, rofecoxib, oral contraceptives, ticlopedin).

Side effects

Drowsiness, weakness, dizziness, slight decrease in blood pressure, dry mouth, nausea, gastrointestinal disorders, transient increase in the activity of hepatic transaminases.

When taking the drug in higher doses additionally, you may experience: low blood pressure, bradycardia, muscle weakness, insomnia, sleep disorders, hallucinations, acute hepatitis (very rare), anxiety.

Interaction

Concomitant use of tizanidine with fluvoxamine or ciprofloxacin (inhibitors of the CYP1A2 isoenzyme) leads to a 33-fold increase in the AUC of tizanidine. As a result, a clinically significant and prolonged decrease in blood pressure may occur, leading to drowsiness, weakness, and slowing of psychomotor reactions (in some cases, loss of consciousness); prolongation of the QT interval (see “Overdose”).

Concomitant use of tizanidine with other inhibitors of the CYP1A2 isoenzyme — antiarrhythmic drugs (amiodarone, mexiletine, propafenone), cimetidine, fluoroquinolones (enoxacin, pefloxacin, norfloxacin), rofecoxib, oral contraceptives, ticlopidine-is not recommended.

Antihypertensive drugs increase the risk of a marked decrease in blood pressure and bradycardia.

Ethanol, CNS depressants, may increase the sedative effect of tizanidine, so concomitant use of tizanidine with CNS depressants and / or alcohol is not recommended.

How to take, course of use and dosage

Inside.

In case of painful muscle spasm: 2-4 mg three times a day. In severe cases, an additional 2-4 mg is taken before bedtime.

In case of skeletal muscle spasticity: 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 3-7 days. The optimal therapeutic effect is achieved with a daily dose of 12-24 mg divided into 3-4 doses at regular intervals.

The maximum daily dose is 36 mg.

In patients with renal insufficiency, it is recommended to start treatment with a dose of 2 mg once a day. Increasing the dose should be carried out gradually, focusing on tolerability and effectiveness. If it is necessary to increase the dose, first increase the dosage prescribed 1 time a day, and then increase the frequency of use.

Overdose

Symptoms: nausea, vomiting, low blood pressure, dizziness, drowsiness, miosis, anxiety, respiratory disorders, coma.

Treatment: Repeated use of activated charcoal is recommended to remove the drug from the body. Forced diuresis may also accelerate the elimination of tizanidine. In the future, symptomatic therapy is carried out.

Special instructions

Hepatic impairment associated with tizanidine has been reported, but these cases were rarely reported with a daily dose of up to 12 mg. In this regard, it is recommended to monitor liver function tests 1 time per month in the first 4 months of treatment in those patients who are prescribed tizanidine at a daily dose of 12 mg or higher, as well as in cases where there are clinical signs that suggest impaired liver function, such as unexplained nausea, anorexia, fatigue. If the activity of AST and ALT in serum persistently exceeds the ULN by 3 times or more, the use of Tisanil should be discontinued.

Patients with congenital QT prolongation syndrome should be prescribed tizanidine with caution, because in preclinical studies of chronic toxicity in animals (dogs), prolongation of the QT interval was noted when using the drug at a dose equivalent to the maximum dose for humans.

In patients with coronary heart disease and / or heart failure, the ECG should be monitored regularly.

In patients with myasthenia gravis, it should be used with extreme caution only in cases where the expected benefit significantly exceeds the possible risk.

Influence on the ability to drive a car or perform work that requires an increased rate of physical and mental reactions.

If you develop drowsiness, dizziness, or a decrease in blood pressure during Tisanil therapy, you should refrain from types of work that require high concentration of attention and rapid reaction, for example, driving vehicles or working with mechanisms.

Form of production

Film-coated tablets.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 30 °C

Shelf life

3 years

Active ingredient

Tizanidine

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

For adults as directed by your doctor

Indications

Lumbago, Sciatica, Muscle Spasm, Sciatica, Osteochondrosis