Tizanidine-Teva - instructions for use, dose, side effects, contraindications

Active substance: tizanidine hydrochloride (tizanidine) 2.29 mg (2.0 mg) / 4.58 mg (4.0 mg); auxiliary substances: lactose (lactose anhydrous) 57.91 mg / 115.82 mg; SMCC 501 solid (microcrystalline cellulose 98%, silicon dioxide colloid 2%) 22.575 mg / 45.15 mg; SMCC 901 solid (microcrystalline cellulose 98%, colloidal silicon dioxide 2%) 22.575 mg / 45.15 mg; stearic acid 2,150 mg / 4,30 mg.

Description:

Tablets 2 mg. Round biconvex tablets white or almost white with a risk on one side and engraved "T2" on the other.

Tablets 4 mg. Round biconvex tablets white or almost white with

crosswise risk on one side and engraving "T4" - on the other.

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 an agonist of alpha2-adrenergic receptors located in the central nervous system at the supraspinal and spinal levels. Stimulating presynaptic alpha 2-adrenergic receptors, tizanidine suppresses the release of excitatory amino acids that stimulate receptors sensitive to N-methyl-D-acapartate (NMDA receptors). As a result, the polysynaptic transmission of excitation is suppressed at the level of the intermediate neurons of the spinal cord. Tizanidine does not directly affect skeletal muscles, neuromuscular synapses, or monosynaptic reflexes.

Tizanidine reduces spasticity and clonic convulsions, as a result of which the resistance of muscles to passive movements in the joints decreases and the volume of active movements increases.

Pharmacokinetics:

Suction

Absorption of tizanidine is high, the time to reach the maximum concentration in the plasma (Tmax) is 1-2 hours. Bioavailability is 34%. Eating does not affect the pharmacokinetics. Distribution and Metabolism

The volume of distribution is 2.6 l / kg. Connection with plasma proteins - 30%.

In the dosage range of 4 to 20 mg, the pharmacokinetics are linear. Tizanidine is metabolized to a large extent in the liver (95%) with the formation of inactive metabolites.

Excretion

The half-life period (T1 / 2) is 3-5 hours. It is mainly excreted by the kidneys (70% in unchanged form, 2.7% in the form of metabolites) and excreted with faeces (20%).

In patients with renal insufficiency (creatinine clearance less than 25 ml / min), the maximum plasma concentration (Cmax) increases 2-fold, Tt-14 hours, the area under the concentration-time curve (AUC) increases 6-fold.

Indications:Spasticity of skeletal muscles in multiple sclerosis, spinal cord injuries.

Contraindications:

Hypersensitivity to tizanidine or other components of the drug; pregnancy; the period of breastfeeding; age under 18 years (effectiveness and safety not established); severe liver dysfunction; simultaneous application with potent inhibitors of the isoenzyme CYP1A2 (fluvoxamine, ciprofloxacin), alpha2-adrenomimetics, lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Carefully:

Patients over 65 years of age; renal failure (CC less than 25 ml / min); simultaneous use with oral contraceptives, antiarrhythmics, cimetidine, norfloxacin, rofecoxib, ticlopidine, detoxin,

beta-adrenoblockers, sedatives, ethanol, diuretics, hypotensive drugs.

Pregnancy and lactation:

Application during pregnancy and during breastfeeding is contraindicated. Impact on the ability to manage transport and work with machinery.

Care should be taken during the use of the drug Tizanidine-Teva due to the possible development of adverse reactions that may adversely affect the ability to drive vehicles and perform potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Dosing and Administration:

Inside. The initial dose is 2 mg, followed by a 2 mg dose increase with intervals of at least 3-4 days.

The maximum daily dose is 36 mg.

Dosing regimen should be set individually, the daily dose divided into several receptions (up to 3-4), depending on the needs of the patient. Usually, no more than 24 mg / day is needed.

Treatment of patients with renal insufficiency (CC less than 25 ml / min) is recommended to start at a dose of 2 mg once a day. The dose should be increased gradually, taking into account the tolerance and effectiveness: first increase the dose, and then increase the frequency of application.

In patients older than 65 years, the drug Tizanidine-Teva should be used under close monitoring of kidney function due to the possible reduction in the glomerular filtration rate.

Side effects:

The frequency of side effects is classified according to the recommendations of the World Health Organization: very often - not less than 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0,1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - 0.01%, including single messages.

From the nervous system: often - drowsiness, dizziness; rarely - insomnia, hallucinations, sleep disorder.

From the cardiovascular system: often - lowering blood pressure, bradycardia.

On the part of the digestive system, often - dryness of the oral mucosa, rarely - nausea, a violation of the function of the gastrointestinal tract.

From the liver and bile ducts: very rarely - the transient increase in the activity of "liver" transaminases, hepatitis, liver failure.

From the musculoskeletal system: rarely - muscle weakness.

Other: very often - increased fatigue; often - withdrawal syndrome *.

* With a sharp cancellation after prolonged treatment and / orreception of high doses of the drug (and also after application together with antihypertensive drugs) increases the risk of developing tachycardia, increasing blood pressure, in some cases - acute violation of cerebral circulation.

Overdose:

Symptoms, nausea, vomiting, marked decrease in blood pressure, prolongation of the interval QT (c), dizziness, drowsiness, miosis, anxiety, respiratory depression, coma.

Treatment-, gastric lavage, repeated use of activated charcoal, carrying out forced diuresis, symptomatic therapy, taking a lot of fluids.

Interaction:

Simultaneous application with potent inhibitors of the isoenzyme CYP1A2 (fluvoxamine, ciprofloxacin) significantly increases the concentration of tizanidine in the blood plasma and increases the likelihood of adverse reactions.

Hypotensive drugs, including diuretics, with simultaneous use with tizanidine increase the risk of a pronounced decrease in blood pressure and bradycardia.

When used simultaneously with oral contraceptives, antiarrhythmic drugs, cimetidine, norflokeacin, rofecoxib, ticlopidone, the clearance of tizanidine is significantly reduced.

With the simultaneous use of sedative drugs and ethanol with tizanidine, the risk of central nervous system depression increases.

Paracetamol increases TCmax by 16 min (does not have clinical significance).

Special instructions:

Care should be taken when using Tizanidine-Teva in patients with renal insufficiency. When using Tizanidine-Teva in patients with renal insufficiency (CC less than 25 ml / min), a dose reduction may be required. It is recommended to monitor liver function indices 1 once a month during the first 4 months of treatment in those patients who are taking a drug T izanidin-T eva in a daily dose of 12 mg and above, as well as in cases where there are clinical signs suggestive of liver dysfunction , such as unexplained nausea, anorexia, a feeling of fatigue. In the case when the activity of "hepatic" transaminases is 3 times or more above the upper limit of the norm, Tizanidine-Teva should be stopped.

With the simultaneous application of the drug-Teva tizanidine with inhibitors of CYP1A2 isoenzyme may increase tizanidine concentration in blood plasma, which in turn may be the cause of the symptoms of an overdose, in particular lengthening QT (c) interval.The simultaneous use of Tizanidine-Teva with inhibitors of the isoenzyme CYP1A2 and other drugs that can lead to an elongation of the QT (c) interval is not recommended.

Care should be taken when treating tizanidine with cardiovascular disease, ischemic heart disease. It is necessary to regularly monitor laboratory parameters of the functional state of the heart and monitor the ECG.

The withdrawal of Tizanidine-Teva should be gradual because of the risk of withdrawal syndrome (see "Side effect" section).

It has been reported that there are rare cases of muscle weakness when using tizanidine (see section "Side effect"). In clinical trials, it was shown that tizanidine does not adversely affect the strength of muscle contraction.

Form release / dosage:

Tablets 2 mg, 4 mg.

10 tablets in a blister made of polyvinyl chloride and aluminum foil.

By 2, 3, 5 or 10 blisters together with instructions for use in a cardboard pack.

Packaging:

Tablets 2 mg, 4 mg.

10 tablets in a blister made of polyvinyl chloride and aluminum foil.

By 2, 3, 5 or 10 blisters together with instructions for use in a cardboard pack.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

Shelf life 3 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-001812

Date of registration:27.08.2012

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

TEVA Pharmaceutical Works Private, Ltd. Co. Hungary

Information update date: & nbsp29.08.2015

Illustrated instructions

Instructions

Tizanidine-Teva (Tizanidin-Teva)