tablets: painful muscle spasms associated with static and functional spine disorders (cervical and lumbar syndromes) or following a surgical procedure, e.g. a hernia of the nucleus pulposus or hip arthritis.Tablets and MR capsules: increased muscle tone in neurological diseases, e.g. multiple sclerosis, chronic spinal cord diseases, spinal cord degenerative diseases, as a consequence of cerebral palsy and cerebral palsy (in adults who have previously been diagnosed with this disease).
Composition:
1 tabl (divisible) contains 4 mg of tizanidine in the form of hydrochloride. One modified-release (MR) capsule contains 6 mg of tizanidine in the form of a hydrochloride.
Action:
A drug with a central action to reduce skeletal muscle tone. The main site of action of tizanidine is the spinal cord, where by stimulation of presynaptic α receptors2 inhibits the release of amino acids that stimulate N-methyl-D-aspartate (NMDA) receptors. Inhibition of polysynaptic signals at the level of spinal insertion neurons leads to a reduction in increased muscle tone. Tizanidine also has a moderate central analgesic effect. It has a beneficial effect in acute painful muscle spasms as well as in chronic spasticity of spinal or cerebral origin. It reduces resistance to passive movements, reduces increased muscle tension and clonus, improves muscle strength dependent on will. Following oral administration, tizanidine is absorbed quickly and almost completely, reaching a maximum blood concentration approximately 1 hour after taking the drug. The average bioavailability is about 34% due to the significant first pass effect. About 30% is bound to plasma proteins. It is metabolized in the liver to inactive metabolites. T0,5 is 2-4 h. It is excreted mainly in the urine (approximately 70%) in the form of metabolites, approximately 2.7% of the drug is excreted unchanged. As a result of the slowed release of tizanidine from MR capsules, the maximum average blood concentrations achieved in approximately 8.5 hours are approximately half the concentrations obtained when using comparable daily doses of a tablet formulation given in 3 doses, while the total amount of changes. In patients with renal insufficiency (creatinine clearance <25 ml / min), maximum blood levels are twice as high and T0,5 it is extended to about 14 hours.
Contraindications:
Hypersensitivity to tizanidine or other components of the preparation. Significant abnormal liver function, permanent elevation of aminotransferase 3 times above the upper limit of normal. Concomitant use of strong CYP1A2 inhibitors (eg fluvoxamine or ciprofloxacin). The use is not recommended in children - the experience of using patients in this group is limited.
Precautions:
Use with medications that prolong the QT interval. Because of the risk of serious side effects, including severe hypotension, caution should be used in patients taking CYP1A2 inhibitors and / or antihypertensive medicinal products. Use with caution in the elderly and in patients with impaired renal or hepatic function. Treatment with the product should be discontinued if the serum ALT or AST is above the upper limit of three times the normal range. The tablets contain lactose and therefore should not be used in patients with rare hereditary galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
It is not recommended during pregnancy unless the benefits of therapy outweigh the risks resulting from the use of the preparation. It should not be used during breast-feeding.
Side effects:
Very common: drowsiness, dizziness, gastrointestinal disturbances, dry mouth, muscle weakness, fatigue. Common: sleep disorders (including insomnia), hypotension, nausea, low blood pressure, increased transaminases. Uncommon: bradycardia.Not known: hallucinations, confusion, balance disorders, blurred vision, fainting, hepatitis, liver failure, weakness, withdrawal syndrome. In addition, after the use of higher doses, the following may occur:torsade de pointes. After sudden discontinuation of tizanidine for prolonged and / or high doses and (or) concomitantly with blood pressure-lowering drugs, rebound hypertension and tachycardia were observed. In extreme cases, hypertension with rebound can lead to stroke.
Dosage:
Orally. Adults: Painful muscle spasms: 2-4 mg tablets 3 times a day; in severe cases you can take an extra dose of 2 mg or 4 mg at bedtime. Increased muscle tone in neurological diseases: tablets - initially no more than 6 mg per day in 3 divided doses, the daily dose may be gradually increased (at intervals of half a week or weeks) by 2-4 mg; Do not use a daily dose of more than 36 mg, the optimal response of the patient is obtained after administration of 12-24 mg per day in 3-4 doses; MR capsules - initially 6 mg once a day, the daily dose can be increased gradually (at weekly or weekly intervals) by 6 mg, usually 6-24 mg once a day, the optimal dose for most patients is 12 mg once a day ( 2 capsules of 6 mg each). In patients with renal impairment (creatinine clearance <25 ml / min) and moderate hepatic impairment, it is recommended to start treatment with 2 mg once a day (do not use the MR form due to the indivisibility of the capsule); the dose should be increased slowly, depending on the tolerance and the effectiveness of the drug (it is recommended to increase the one-time daily dose, and then increase the frequency of administration).
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