Tizanidine

width = Tizanidine is a central muscle relaxant that is used to reduce muscle spasms caused by various neurological diseases.

Active components of the drug have a direct effect on the nervous system, which as a result contributes to to alleviate the condition of patients with stroke, multiple sclerosis, cerebral palsy and various degenerative diseases the spine.

The active substance is rapidly absorbed into the digestive tract, the maximum concentration is observed 2-3 hours after administration. The use of food does not affect the pharmacodynamics. Tizanidine is excreted mainly through the urinary system.

Clinical and pharmacological group

Miorelaxant of central action.

Terms of sale from pharmacies

Can buyby prescription.

Price

How much does tizanidine cost in pharmacies? The average price is at the level of170 rubles.

Composition and form of release

Tizanidine tablets are white, round and biconvex. The main active substance of the drug is tizanidine in the form of hydrochloride, its content in one tablet is 2 or 4 mg. It also includes additional components, which include:

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Anhydrous lactose.
Microcrystalline cellulose.
Stearic acid.
Anhydrous colloidal silicon dioxide.

Tablets are packaged in a blister for 10 pieces. Cardboard pack contains 3 blisters with tablets (30 pieces), as well as instructions for using the medication.

pharmachologic effect

Tizanidine is an agonist of alpha2-adrenergic receptors located in the central nervous system at the supraspinal and spinal levels. By stimulating presynaptic alpha2-adrenergic receptors, tizanidine inhibits the release of excitatory amino acids that stimulate receptors sensitive to N-methyl-D-aspartate (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 muscle, 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.

Indications for use

Tablets Tizanidine must be used to eliminate the spastic and convulsive state of skeletal muscles that occur against the background of the following neurological diseases:

pathology of the spinal cord of a degenerative nature;
spasticity;
opistonus;
hernia;
stroke;
multiple sclerosis;
myelopathy with chronic course;
convulsions;
myoclonia.

Contraindications

The drug is contraindicated in patients taking potent CYP1A2 inhibitors, such as fluvoxamine or ciprofloxacin.

Intended use for pregnancy and lactation

Due to the fact that the components of the drug can have a negative impact on the child, during pregnancy, women are not recommended to use tizanidine for treatment.

When taking medication during breastfeeding, the constituent components of the medicine fall into the composition of breast milk. Doctors recommend in cases of acute necessity for the use of the medicine to cancel breastfeeding.

Dosage and route of administration

As indicated in the instructions for use, tizanidine is taken orally. The doctor selects a dose individually, because the drug has a narrow therapeutic index and high variability in plasma concentration in the blood.

The minimal risk of adverse reactions is observed when taking the drug 3 times a day for 2 mg. With painful muscle spasms, a single dose can be increased to 4 mg. In severe cases, the doctor may be prescribed an additional 2 or 4 mg before bedtime.

With spasticity of skeletal muscles associated with neurological diseases, the dosing regimen is set individually.

The maximum daily dose at the beginning of therapy is 6 mg in 3 divided doses. In the future, with an interval of 3-7 days, it is possible to increase it by 2-4 mg.
The optimal therapeutic effect, as a rule, is achieved at a daily dose of 12-24 mg in 3-4 doses at equal intervals of time. Maximum prescribed 36 mg per day.

For patients older than 65 years, Tizanidine should be taken with a minimum of doses. In the future, the dosing regimen is set taking into account the optimal ratio of efficacy and tolerability.

The recommended initial dose for creatinine clearance is ≤ 25 ml / min - once a day, 2 mg. The dose should be increased slowly, gradually, taking into account the effectiveness and tolerability. If a more pronounced effect is required, an increase in a single dose, then a multiplicity of application, is recommended first.

Abolition of Tizanidine should be carried out gradually, which will reduce the likelihood of a ricochet increase in blood pressure and tachycardia. In particular, this applies to cases of prolonged use of the drug or therapy in high doses.

Side effects

In the study of the action of Tizanidine on patients, side effects such as drowsiness, dry mouth, hypotension, decrease arterial pressure, bradycardia, dizziness, weakness or asthenia, muscle spasms, hallucinations, fatigue, impaired liver function and hepatotoxicity.

Less frequently, treatment with this medication may result in the following undesirable effects:

hepatitis;
convulsions;
depression;
joint pain;
paresthesia;
Stevens-Johnson syndrome;
anaphylactic shock;
exfoliative dermatitis;
ventricular tachycardia;
rash;
tremor.

Overdose

The main symptoms: vomiting, nausea, pronounced lowering of blood pressure, lengthening of the interval QTc, drowsiness, dizziness, anxiety, miosis, coma, respiratory failure.

Therapy: for the removal from the body of tizanidine recommended to carry out gastric lavage, the reception of a large amount of fluid, the repeated use of activated carbon. Also accelerated excretion of the substance contributes to forced diuresis. In the future, symptomatic therapy is performed.

Recovery in all cases of overdose, including the administration of 400 mg of tizanidine, was without any particularities.

special instructions

Before you start using the drug, read the special instructions:

It is necessary to use the preparation with extreme caution in patients with impaired renal and hepatic activity.
During the simultaneous use of ethanol and muscle relaxants with a sedative effect, the sedation increases.
When using the medication together with antihypertensive drugs, namely diuretics, arterial hypotension and bradycardia can occur.
In the initial period of medical therapy, there may be increased drowsiness, so avoid activities that require increased concentration.

Interaction with other drugs

Simultaneous application with potent inhibitors of the isoenzyme CYP1A2 (fluvoxamine, ciprofloxacin) significantly increases the concentration of tizanidine in blood plasma and increases the likelihood of side effects reactions. Hypotensive drugs, including diuretics, with simultaneous use with tizanidine increase the risk of a pronounced decrease in blood pressure and bradycardia.

With simultaneous use with oral contraceptive drugs, antiarrhythmic drugs, cimetidine, norfloxacin, rofecoxib, ticlopidine significantly reduced clearance tizanidine. With the simultaneous use of sedative drugs and ethanol with tizanidine, the risk of central nervous system depression increases. Paracetamol increases TCmax for 16 min (does not have clinical significance).

Reviews

We offer you to read reviews of people who used the drug Tizanidine:

Victor. After the operation on the spine for a long time did not take strong drugs, but one day the pain returned. Rushed to the hospital, where the doctor prescribed tyzanidine. I took it for the night, and in the morning a miracle happened - everything was over! Nothing hurts and no unpleasant symptoms. Like this.
Valentina. At mum against a background of a stroke spasm of skeletal muscles began to arise, which simply did not give her rest. I did not pull and immediately took her to the doctor. After the examination, the doctor recommended taking Tizanidine to relieve spasms. She took 3 tablets a day. In general, after using this remedy, it became much better, all the unpleasant sensations passed. And I did not notice any side effects. True, at first she had drowsiness and increased weakness, but all this quickly passed.
Katerina. I probably do not fit the drug. Almost immediately after the reception, the head became very dizzy, and nausea appeared. I thought that the body would get used to it and everything would go away, but further problems with the stomach started. I had to ask the doctor to replace the medicine.