Tizanil - instructions for use, doses, side effects, contraindications

Active substance: Tizanidine hydrochloride (equivalent to tizanidine) for tablets 2 mg - 2.288 (2) mg, for tablets 4 mg - 4.576 (4) mg, for tablets 6 mg - 6.864 (6) mg. Excipients: microcrystalline cellulose for tablets 2 mg - 74.71 mg, for tablets 4 mg - 101.02 mg, for tablets 6 mg - 127.64 mg, lactose monohydrate for tablets 2 mg - 79.00 mg, for tablets 4 mg - 109.43 mg, for tablets 6 mg - 118.14 mg, stearic acid for tablets 2 mg - 0.30 mg, for tablets 4 mg - 0.40 mg, for tablets 6 mg - 0.50 mg, silicon dioxide colloidal anhydrous for tablets 2 mg - 2.88 mg, for tablets 4 mg - 4.576 mg, for tablets 6 mg - 6.864 mg.

Description:

Tablets are white or almost white in color, flat-cylindrical with a bevel on both sides.

For tablets of 2 mg: with a risk on one side and with a number 2 on the other side.

For tablets of 4 mg: with a cross-shaped risk on one side and number 4 on the other side.

For tablets of 6 mg: with a cross-shaped risk on one side and number 6 on the other side.

Pharmacotherapeutic group:Miorelaxant of central action

ATX: & nbsp

M.03.B.X Other muscle relaxants of central action

M.03.B.X.02 Tizanidine

Pharmacodynamics:

Tizanidine is a central muscle relaxant. The main point of application of its action is in the spinal cord. By stimulating presynaptic ag-adrenergic receptors, tizanidine suppresses excretion of excitatory amino acids that stimulate receptors for N-Memrf-D-acmpxaTy (NMDA receptors). As a consequence, at the level of the intermediate neurons of the spinal cord, the polysubstance transmission of excitation is suppressed. Since this mechanism is responsible for the excess muscle tone, when it is suppressed, the muscle tone decreases.

Pharmacokinetics:

Absorption is high; time to reach the maximum plasma concentration (TCmax) - 1 hour Bioavailability - about 34%. Eating does not affect the pharmacokinetics.

The volume of distribution in the equilibrium state is 160 liters. The connection with plasma proteins is 30%. In the dose range of 4 to 20 mg, the pharmacokinetics are linear.

Metabolised rapidly and largely in the liver (95%) by the isoenzyme CYP1A2 with the formation of inactive metabolites. It is excreted mainly by the kidneys

(70% of the dose in the form of metabolites, 2.7% in unmodified form). It is biphasic:

period of tincture (T1 / 2) in the first phase - 2.5 h; the final T1 / 2 - 22 hours. The average half-period of unchanged substance is 2-4 hours.

In patients with renal insufficiency (creatinine clearance <25 ml / min), the maximum concentration in blood plasma (Cmax) increases 2 times, T 1/2 - 14 hours, the area under the pharmacokinetic curve "concentration-time" (AUC) increases in 6 time.

Indications:

Painful muscle spasms.

Spasticity in multiple sclerosis.

Plasticity in case of spinal cord injuries.

Spasticity, caused by a traumatic brain injury.

Contraindications:

Hypersensitivity to tizanidine and other components of the drug.

Severe impairment of liver function.

Simultaneous application with powerful inhibitors of CYP1A2 isoenzymes (including fluvoxamine, androfloxacin),

Hereditary lactose intolerance, lactase deficiency, glucose-galactose malabeorbtion.

Children under 18 years.

Carefully:

Renal failure, arterial hypotension, bradycardia, simultaneous intake of oral contraceptives, age over 65 years.

Do not abruptly cancel Tizanil, the dose of the drug is reduced gradually.

Pregnancy and lactation:

Since controlled trials of tizanidip use in pregnant women have not been performed, it should not be used in pregnancy, except when the expected benefit to the mother exceeds the possible risk to the fetus.

Tizannind infiltrates insignificantly into breast milk, so during breastfeeding the drug should be withdrawn.

Dosing and Administration:

designate inside.

Curbing a painful muscle spasm: but 2 4 mg 3 times a day, in heavy

cases - additionally at night 2-4 mg.

Treatment of spasticity of skeletal musculature 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 of 12-24 mg in 3-4 doses, the maximum daily dose of 36 mg

Patients with renal insufficiency (with a creatinine clearance <25 ml / min) receive the drug with 2 mg I once a day. If necessary, increase the dose gradually, taking into account the tolerance. If it is necessary to obtain a more pronounced effect, it is recommended first to increase the dose prescribed once a day, then - the frequency of the appointment.

Side effects:

From the nervous system: snotty, dizziness, hallucinations, insomnia, sleep disturbance.

From the cardiovascular system: bradycardia, lowering of arterial pressure (in some cases expressed, up to collapse and loss of consciousness).

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

From the musculoskeletal system: muscle weakness.

Other: increased fatigue, hypercreatininaemia.

With a sharp withdrawal of the drug after prolonged treatment and / or reception of high doses of the drug (and also after simultaneous application together with hypotensive drugs): tachycardia, increased blood pressure, acute impairment of cerebral circulation.

Overdose:

Overdose

Symptoms: nausea, vomiting, lowering of arterial pressure, dizziness, drowsiness, agitation, prolongation of the QT interval, miosis, anxiety, respiratory failure, coma. Treatment: gastric lavage, taking activated charcoal, conducting forced diuresis, symptomatic therapy.

Interaction:

The simultaneous use of tizanidine with fluvoxamine or ciprofloxacin (inhibitors of the isoenzyme CYP1A2) leads to a 33-fold increase in the area under the concentration-time (AUC) curve of tizanidine. As a result, a clinically significant and prolonged decrease in arterial pressure may result, leading to drowsiness, weakness and retardation of psychomotor reactions (in some cases to the postural consciousness); prolongation of QT interval (see section "Overdose").

It is not recommended simultaneous use of tizanidine with other inhibitors of the isoenzyme CYP1A2 - antiarrhythmic drugs (amiodarone, mscyletine, propafenone), cimetidine, fluoroquilones (enoxacin, pefloxacin, norfloxacin), rofecoxib, oral contraceptives, ticlopidite.

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

Ethanol, CNS depressant agents may increase the sedative effect of tizanidine, therefore, simultaneous use of tizanidine with CNS depressant and (or) alcohol,

Special instructions:

Reported cases of violations of liver function associated with tizanidine, but when the drug in a daily dose of up to 12 mg, these cases were rare. In this regard, it is recommended to monitor functional liver function tests once a month in the first 4 months of treatment in those patients who are assigned tizanidine in a daily dose of 12 mg and above, as well as in those cases when there are clinical signs suggesting a violation of liver function such as: unexplained nausea, anorexia, a feeling of fatigue. In the case when the activity of aspartate aminotransferase and alanikinotransferase in the serum persistently exceed 1 upper limit of the norm by 3 times or more, Tizanil application should be discontinued. Patients with the syndrome of congenital extension of the Q-T interval tizanidine should be administered with caution, as in pre-clinical studies of chronic toxicity in animals (dogs), the Q-T interval is prolonged when the drug is administered at a dose equivalent to the maximum dose for a human.

Patients with ischemic heart disease and / or heart failure should be monitored regularly by the ECG.

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

Effect on the ability to drive transp. cf. and fur:

With the development of drowsiness, dizziness, or lowering blood pressure on the background of therapy, Tizanil should refrain from types of work that require high concentration of attention and quick reaction, for example, driving or working with machinery.

Form release / dosage:

Tablets 2 mg, 4 mg, 1 mg. For 10 tablets in a blister of PVC / 113/1 SHDH / alum,

For a dosage of 2 mg: 3 blisters per pack of cardboard along with instructions for use.

For a dosage of 4 mg: 1 or 3 blisters per pack of cardboard along with instructions for use.

For the dosage of b mg: 3 blisters per pack of cardboard along with the instructions for use.

Packaging:

For 10 tablets in a blister of PVC / 113/1 SHDH / alum,

For a dosage of 2 mg: 3 blisters per pack of cardboard along with instructions for use.

For a dosage of 4 mg: 1 or 3 blisters per pack of cardboard along with instructions for use.

For the dosage of b mg: 3 blisters per pack of cardboard along with the instructions for use.

Storage conditions:

In dry, protected from the light at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use the product after the date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000831

Date of registration:11.09.2012

The owner of the registration certificate: Simpex Pharma Pvt Ltd. Simpex Pharma Pvt Ltd. India

Manufacturer: & nbsp

SIMPEX PHARMA, Pvt. Ltd. India

Representation: & nbspKORAL-MED, CJSCKORAL-MED, CJSC

Information update date: & nbsp29.08.2015

Illustrated instructions

Instructions

Tizanil® (Tizanil)