Tisanil, pills 2mg, 30pcs

Composition

1 film-coated tablet contains:

active ingredients:

tizanidine 2 mg;

excipients:

MCC,

lactose monohydrate,

stearic acid,

colloidal anhydrous silicon dioxide

Pharmacological action

Tisanil has a muscle relaxant, analgesic effect. By stimulating presynaptic_a2receptors, 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 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. Interindividual 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-life was extended to 14 hours. Concomitant food intake does not have a clinically significant effect on the pharmacokinetics of tizanidine.

Indications

• painful muscle spasms;
• spasticity in multiple sclerosis;
• spasticity in spinal cord injuries;
• spasticity caused by traumatic brain injury.

Use during pregnancy and lactation

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

• Hypersensitivity to any component of Tisanil;
• severe liver dysfunction;
• concomitant use with fluvoxamine;
• pregnancy;
• lactation;
• children under 18 years of age (due to insufficient data).

With caution:

• renal insufficiency;
• elderly age;
• concomitant use with inhibitors of the CYP1A2 isoenzyme (antiarrhythmic drugs-amiodarone, mexiletine, propafenone; cimetidine, fluoroquinolones, rofecoxib, oral contraceptives, ticlopidine).

Side effects

Nervous system disorders: drowsiness, dizziness, hallucinations, insomnia, sleep disorders.

From the cardiovascular system: bradycardia, decreased blood pressure (in some cases pronounced, up to collapse and loss of consciousness).

From the digestive system: dry mouth, nausea, dyspepsia, increased activity of hepatic transaminases, hepatitis, liver failure.

Musculoskeletal system disorders: muscle weakness.

Other: increased fatigue, hypercreatininemia.

If the drug is abruptly discontinued after prolonged treatment and / or taking high doses of the drug (as well as after simultaneous use with antihypertensive drugs): tachycardia, increased blood pressure, acute cerebrovascular accident.

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

Tisanil is taken orally. Relief of painful muscle spasm: 2-4 mg 3 times a day, in severe cases-an additional 2-4 mg at night.

Treatment of skeletal muscle spasticity in neurological diseases: the initial dose is 2 mg 3 times a day, then the dose is gradually increased by 2-4 mg at intervals of 3-7 days. The optimal daily dose is 12-24 mg in 3-4 divided doses, the maximum daily dose is 36 mg.

In patients with renal insufficiency (with creatinine clearance If necessary, the dose is increased gradually, taking into account tolerability. If you need to get a more pronounced effect, it is recommended to first increase the dose prescribed once a day, then — multiplicity of the assignment.

Overdose

Symptoms: nausea, vomiting, decreased blood pressure, dizziness, drowsiness, agitation, prolongation of the QT interval, miosis, anxiety, respiratory disorders, coma.

Treatment: gastric lavage, use of activated charcoal, forced diuresis, symptomatic therapy.

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

Osteochondrosis, Sciatica, Lumbago, Muscle Spasm, Sciatica