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Medicinal reference book geotar. Detailed instructions for use and reviews of the muscle relaxant tizanidine

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Skeletal muscle spasms cause a lot of inconvenience, and can also cause the development pathological processes. Myelopathy of various etiologies requires the use of muscle relaxants to prevent spasm.

One such drug is Tizanidine.

We will discuss further how the drug Tizanidine works, its composition and contraindications.

Ask your question to a neurologist for free

Irina Martynova. Graduated from Voronezh State University medical university them. N.N. Burdenko. Clinical resident and neurologist of the BUZ VO \"Moscow Polyclinic\".

Manufacturer

The drug is produced by the trademark Teva in Israel. The average cost of a package is 160 rubles.

Composition and release form

The drug, which has a muscle relaxant effect, is produced in the form of white round tablets, separated by a stripe in the middle. The tablets are packaged in plastic blisters of 10 pcs. Each package contains 3 blisters and instructions for use.

One tablet contains the main active ingredient - tizanidine hydrochloride, which can be 2 or 4 mg, depending on the dosage of the drug.

There are also auxiliary components that ensure the effectiveness of the main component, as well as its maximum absorption in the body:

  • stearic acid;
  • silicon dioxide;
  • lactose and cellulose.

The main substance of the drug has direct impact on skeletal muscles, by reducing the synthesis of amino acids responsible for the increase in spasm. The tablets are almost completely absorbed into the blood, metabolized in the liver.

Decomposition products are excreted by the kidneys.

Application regimen and dosage


The maximum permissible daily dose of the drug should not exceed 36 g. The dosage and duration of treatment are selected individually, taking into account the personal characteristics of each patient.

Treatment begins with 2 g of the substance, gradually increasing to 10 g. Usually this therapeutic dose it is often enough to achieve a lasting antispasmodic and muscle relaxant effect.

The tablet is swallowed whole, without chewing, and washed down a small amount water.

Indications

Since the medicine affects skeletal muscles, its indications for use are as follows:

Included complex therapy the drug is used as an auxiliary medication in the treatment of spinal osteochondrosis.

Widely used in postoperative period, When we're talking about about surgery of the spine and its processes.

Contraindications


Absolute contraindication for use of this medicine are pathologies such as:

  • individual intolerance to the components of the drug;
  • chronic pathologies of the liver and kidneys late stages progression;
  • pregnancy and breastfeeding;
  • in combination with medications such as Fluvoxamine and Ciprofloxacin.

In what cases will the remedy not help?

Tizanidine Teva ineffective for relieving cramping pain internal organs, as well as in the treatment of cardiovascular diseases.

The drug has a targeted effect on polysynaptic reflexes, blocking them, thereby providing a relaxing effect.

Special instructions

In the presence of liver disease, the course of treatment begins with a minimum dosage of 2 mg. Gradually, the dose is increased to 20 mg per day, first increasing the daily dose, and then the frequency of doses. It is important to monitor the level of liver enzymes, as well as its performance, since it is this organ that experiences increased load when using Tizanidine.

Kidney pathologies require constant monitoring, since there have been cases of decrease glomerular filtration, which increases the nephrotoxicity of the drug itself several times. Urine and blood should be examined daily for the level of tizanidine hydrochloride in the body, which will help prevent the development of overdose and intoxication.

Since Tizanidine has a pronounced hypotensive effect and can cause drowsiness, it is not recommended to use it when it is necessary to perform work that requires increased concentration.

This includes driving a car, as well as mechanical monotonous work.

Nuances of use for special categories of patients

IN childhood this drug are not used because there is no reliable data on the ability to influence the formation of a growing organism.

Because Tizanidine almost completely absorbed into the blood, it is not used during pregnancy and lactation, since there is a high probability of developing pathologies in the child.

In old age, the drug is taken under the supervision of specialists, since there is a risk of developing renal and liver failure. Health status is monitored daily.

If necessary, the dose and frequency of doses are adjusted by the attending physician.

Overdose and adverse reactions


If the dosage of this drug is accidentally or intentionally increased, overdose symptoms may develop, which are manifested by clinical signs such as:

  • dizziness;
  • nausea;
  • tinnitus;
  • fainting;
  • pain in the epigastric abdomen;
  • bradycardia;
  • hypotension.

In particularly severe cases coma may develop, in which without timely provision medical care death occurs.

If an overdose is detected, symptomatic treatment is carried out aimed at restoring vital important functions body. The action plan includes a number of actions such as:

  • reduce the concentration of toxins in the body by washing the stomach and intestines, as well as introducing a sorbent;
  • normalize blood pressure and heart rate;
  • enter saline solutions, which are necessary to maintain the body.

Subject to availability hypersensitivity to the components of the drug, as well as non-compliance with recommendations regarding taking pills, may develop adverse reactions. The most common of them are:

  • dry mouth;
  • decreased quality of vision;
  • drowsiness;
  • decreased concentration;
  • chronic fatigue syndrome;
  • muscle spasms;
  • hallucinations;
  • a sharp decrease in heart rate and blood pressure to critical levels.

Somewhat less common are clinical manifestations caused by individual intolerance to the drug, such as:

  • ventricular tachycardia;
  • state of deep depression;
  • psycho-emotional disorder;
  • aching joints;
  • headache;
  • lack of appetite;
  • tremor;
  • decreased body temperature, chills;
  • limb spasms;
  • facial nerve paresis.

If adverse reactions are detected, it is necessary to stop the course of treatment, as well as carry out symptomatic treatment.

In most situations, the drug is replaced with a drug that is similar in effect, but different in composition and method of action.

When the drug is discontinued abruptly, the risks of developing arrhythmia, tachycardia and hypertension increase. In some cases, a disorder may develop cerebral circulation.

Drug interactions

  • Ciprofloxacin;
  • Fluvoxamine;
  • Fluoroquinolone;
  • Verapamil;
  • Famotidine;
  • Acyclovir;
  • Amiodarone;
  • Propaphenone.

In the case of this drug interaction, there is a sharp decrease in blood pressure to critical levels, which is life-threatening and can provoke the development of coma.

The level of tizanidine hydrochloride in the blood should be monitored, provided that the patient is taking other medications, the main one active ingredient which this particular substance is.

Interaction with alcohol

Active ingredient when interacting with ethanol provokes increased intoxication of the body, which increases the intensity of adverse reactions. Therefore, the risks of developing fatal outcome, which occurs as a result of a sharp decrease in blood pressure and a slow heartbeat.

Storage and release from pharmacies

The drug is stored for no more than 3 years from the date of manufacture, in a cool, dry place.

Dispensed strictly according to a doctor's prescription.

Analogs


The drug has a lot of analogues that have an identical muscle relaxant effect on the body. The most common of them are:

  • Sirdalud – 45 rubles;
  • – 120 rubles;
  • Is Tizanidine an analogue of Mydocalm?

    Yes, drugs can be called analogues, despite their different composition. They have a muscle relaxant effect on skeletal muscles, eliminating spasms. However, Mydocalm manifests itself complex impact, also providing an anti-inflammatory and analgesic effect. The choice of drug primarily depends on the type of disease itself, as well as on age and individual characteristics patient.

    Is Sirdalud an analogue and synonym of Tizanidine?

    Yes, it is. Sirdalud tablets have similar composition, therefore the therapeutic effect is the same. These two drugs are synonyms and analogues. The only difference is pharmacological name. Therefore, it cannot be said that Tizanidine or Sirdalud is better, since they are identical.

    How does the drug affect potency?

    There is no reliable data regarding the direct effect on potency and sexual desire, however, based on the relaxation effect exhibited, there is a high probability that sexual activity may decrease slightly. If a decrease in potency is detected, it is recommended to reduce the dosage of the drug or switch to its analogues.

    Why can't you take Digoxin and Tizanidine at the same time?

    Digoxin can affect the smooth muscle of the heart muscle, reducing the frequency of its contractions. When taken simultaneously with Tizanidine, which is also capable of causing hypotension and bradycardia, adverse reactions may occur in the form of pathological low pressure and slowing the heart rate.

    How to use the drug for ankylosing spondylitis?

    In the presence of ankylosing spondylitis, the drug is approved for use only under the supervision of specialists, since there is a high probability of developing adverse reactions that can increase the manifestation of a chronic systemic disease.

    Does the drug come in injection form?

    Tizanidine injection is not given, since this drug is already well absorbed from the gastrointestinal tract, almost completely binding to blood proteins.

    Accordingly, there is no need to use medications in the form of injections.

Tizanidine refers to drugs from the group of muscle relaxants that have the ability to quickly relieve muscle tension, reduce increased tone muscles.

The drug is a means central action, which is often used in the treatment of osteochondrosis.

It helps relieve pain from injuries and dislocations of joints, and restores the mobility of the vertebrae. Often, Tizanidine is used in the treatment of osteochondrosis of the cervical spine.

Additionally, the doctor must prescribe a special therapeutic exercises, massage and manual therapy, taking nonsteroidal drugs that relieve inflammation.

Tizanidine is widely used for severe degenerative changes in the structure of the spine. This is fraught with impaired vertebral mobility, muscle strain and cramps.

Such spasms are accompanied severe pain, spasms, pinched nerves and inability to fully move. In addition, with such a spasm (especially in cervical spine), the oxygen supply to the brain is disrupted, which leads to severe hypoxia. In this case, Tizanidine is used, but only in complex therapy and as prescribed by a doctor.

Instructions for use

Tizanidine should be used strictly as prescribed by a doctor, and before using it, you should carefully study the detailed instructions.

Therapeutic effectiveness

Tizanidine is centrally acting muscle relaxant, i.e., it reduces stiffness, eliminates spasms and tone of skeletal muscles, and accelerates spontaneous contractions.

The drug has a relaxing effect on muscles by inhibiting polysynaptic reactions in the spinal cord. This effect is due to the fact that the active substance of the drug stimulates special adrenergic receptors and reduces the production of amino acids in spinal interneurons.

When taken orally, the drug is completely metabolized in the liver, binds to proteins and is excreted from the body along with urine. The active substance is completely leaves the body after 30-40 hours.


Within 2-3 hours after use, the medicine sharply reduces transmission nerve impulses in muscle tissue, relieving pain, restoring mobility of the spine and joints, eliminates cramps.

Composition and release form

The active ingredient of the drug is tizanidine hydrochloride. Additionally, the composition includes cellulose, silicon dioxide, lactose, povidone and stearic acid.

Tizanidine is produced by both the Russian company Vertex and the Hungarian pharmaceutical company. It is produced only in the form of round, flat tablets, whitish-yellow in color. Each tablet contains 2 or 4 mg of the active substance, and they are packaged in 10, 15 or 20 pieces in a contour blister, as well as 30 and 60 pieces in a plastic bottle.

Indications for use

Basically, Tizanidine is prescribed for the treatment of neurological pathologies that are accompanied by muscle spasms and cramps.

These include:

  • myelopathy (chronic);
  • osteochondrosis of the cervical and lumbar spine;
  • muscle spasms after hernia surgery or surgical treatment hip osteoarthritis;
  • multiple sclerosis;
  • stroke;
  • degenerative changes in the spinal cord.


Often, the drug is used in complex treatment disc protrusion, on initial stage development of intervertebral hernia.

Dosage and method of administration

You need to start taking the drug with a minimum single dose (2 mg), gradually increasing it to 4 mg. The medicine begins to act already 2 hours after administration, and the interval between doses should not be less than 8 hours.

This means that the standard dosage of the drug is 3 tablets taken at regular intervals. Take the drug, preferably after meals, with clean water.

If after 3-4 days of therapy (at a dosage of 2 mg), positive effect is not observed, then use tablets with a dosage of 4 mg. It is important that daily amount active substance did not exceed 36 mg.

Otherwise, severe complications may develop. In some cases, the doctor may prescribe treatment for individual scheme, with mandatory physiotherapy and massage.

Drug compatibility

Under no circumstances should Tizanidine be taken together with Ciprofloxacin and Fluvoxamine. This is fraught with impaired psychomotor reactions, sharp decline pressure.

No less dangerous simultaneous administration medications together with other drugs related to inhibitors of the CYP1A2 isoenzyme (Fluoroquinolone, Acyclovir, Verapamil, Amiodarone, Ticlopidine, etc.).

The combination of Tizanidine with oral contraceptives, causing hypotension and bradycardia, will be hazardous to health. You should not drink alcohol while taking medication, which increases the content of the active substance in the blood.

Video: "What is disc protrusion: the main difference from a hernia"

Adverse reactions

Tizanidine can often cause negative reactions, such as slowing down heart rate, weakness and drowsiness, hypotension and hypotension, fatigue, dizziness and hallucinations.

Much less frequently, the following conditions have been observed:

If such signs appear, you must stop taking the drug and consult a doctor to prescribe another drug.

Overdose

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Next fact

Experts have conducted numerous studies of cases of both slight overdose and severe overdose. In both cases, patients experienced severe drowsiness and lethargy, cardiac dysfunction, slow heartbeat, loss of consciousness, hallucinations and coma. This condition requires immediate gastric lavage and contacting a doctor for symptomatic treatment.

Contraindications

Tizanidine is not prescribed for individual intolerance active component, lactose allergies, severe liver damage.

Pregnancy, lactation

The drug is never prescribed for the treatment of pregnant and lactating women.

Special instructions

Use extreme caution when using Tizanidine if the patient has arterial hypotension, severe renal (liver) failure, congenital prolongation of the QT interval, cardiac pathologies. Such diseases require constant monitoring and control of the state of the cardiovascular and urinary systems.

Impact on the ability to drive vehicles

The drug may cause psychomotor disorders, drowsiness, reduces reaction speed. Therefore, during treatment with Tizanidine (especially at the beginning of therapy), it is necessary to refrain from driving a car and potentially engaging in activities dangerous species activities.

For children

Treatment with Tizanidine is strictly contraindicated in children under 18 years of age.

Kidney damage

For patients suffering from severe kidney pathologies and renal failure, the drug is prescribed with extreme caution.

Liver pathologies

For any form of liver failure or hepatitis, Tizanidine is prescribed extremely rarely. Such therapy requires regular monitoring of ALT and AST levels, and the standard dosage should be halved.


Release form and composition

Dosage form of Tizanidine - tablets: biconvex, round, almost white with a yellowish tint or white (10 pcs. in blister packs, in a cardboard pack of 3 or 6 packs; 15 pcs in blister packs, in a cardboard pack of 2 or 4 packaging; 20 pcs. in blister packs, 3 packs in a cardboard pack; 30 pcs. in blister packs, 1 or 2 packs in a cardboard pack; ).

Composition of 1 tablet:

  • active ingredient: tizanidine – 2 or 4 mg (tizanidine hydrochloride – 2.288 or 4.576 mg);
  • auxiliary components (2/4 mg): magnesium stearate – 1.1/2.2 mg; microcrystalline cellulose – 50.512/101.024 mg; colloidal silicon dioxide – 1.1/2.2 mg; anhydrous lactose – 55/110 mg.

Pharmacological properties


Pharmacodynamics

Tizanidine is a centrally acting muscle relaxant.

Main effects of the active substance:

  • stimulation of presynaptic alpha-2 adrenergic receptors of the spinal cord;
  • suppression of the release of transmitter amino acids that stimulate N-methyl-D-aspartate receptors (NMDA receptors), which causes inhibition of polysynaptic transmission of excitation in the spinal cord. Since this mechanism is responsible for excess muscle tone; when it is suppressed, the tone decreases;
  • reduction of muscle rigidity during passive movements, due to which the resistance to passive movements decreases and the volume of active movements increases;
  • increasing the strength of voluntary contractions of skeletal muscles;
  • reduction of clonic convulsions and spasms.

Pharmacokinetics

Absorption: the substance is absorbed almost completely and quickly. The maximum concentration in plasma is 12.3 and 15.6 ng/ml after a single and multiple doses of the drug in a dose of 4 mg, respectively, achieved after approximately 1 hour. The average bioavailability is approximately 34% (associated with pronounced metabolism).

Distribution: binding to plasma proteins – 30%; the average volume of distribution is 2.6 l/kg. Pharmacokinetics in the dose range from 4 to 20 mg is linear. When tizanidine is taken orally, plasma concentrations in the blood can be reliably predicted.

Metabolism: occurs quickly, about 95% in the liver, with the subsequent formation of inactive metabolites. Tizanidine is mainly metabolized by isoenzyme 1A2 of the cytochrome P450 system.

Excretion: the half-life of the substance from the bloodstream varies from 2 to 4 hours. It is excreted in the form of metabolites mainly by the kidneys (approximately 70% of the dose); unchanged substance – approximately 4.5%.

The average maximum concentration of the drug in plasma in renal failure (creatinine clearance ≤ 25 ml/min) increases by 2 times compared to values ​​in healthy volunteers, the final half-life is 14 hours, which entails a significant increase in the systemic bioavailability of the substance.

Impaired hepatic function may result in increased systemic exposure to tizanidine.

Indications for use

  • painful muscle spasms;
  • spasticity of skeletal muscles associated with diseases and damage to the spinal cord, multiple sclerosis.

Contraindications

Absolute:

  • severe liver dysfunction;
  • combined use with alpha-2 adrenergic agonists, fluvoxamine, ciprofloxacin and other potent inhibitors of the CYP1A2 isoenzyme;
  • galactose intolerance, lactase deficiency, glucose-galactose malabsorption;
  • pregnancy and lactation;
  • children under 18 years of age;
  • individual intolerance to the components included in the drug.

Relative (diseases/conditions in the presence of which Tizanidine is prescribed with caution, in some cases under the control of laboratory parameters functional state heart and ECG monitoring):

  • arterial hypotension;
  • moderately severe hepatic dysfunction;
  • congenital long QT syndrome;
  • bradycardia;
  • renal failure;
  • combined use with norfloxacin, ticlopidine, beta-blockers, diuretics, ethanol, per oral contraceptives, antihypertensive, antiarrhythmic and sedatives, digoxin, cimetidine, rofecoxib;
  • age from 65 years.

Instructions for use of Tizanidine: method and dosage

Tizanidine is taken orally.

The doctor selects the dose individually, since the drug has a narrow therapeutic index and high variability in plasma concentrations in the blood.

The minimum risk of adverse reactions is observed when taking the drug 3 times a day, 2 mg. For painful muscle spasms, the single dose can be increased to 4 mg. In severe cases, your doctor may prescribe an additional 2 or 4 mg at bedtime.

For spasticity of skeletal muscles associated with neurological diseases, the dosage 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 is usually achieved with a daily dose of 12–24 mg in 3–4 doses at equal intervals. The maximum prescribed is 36 mg per day.

For patients over 65 years of age, it is recommended to start taking Tizanidine with minimum doses. Subsequently, the dosage regimen is established taking into account the optimal ratio of effectiveness and tolerability.

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

Tizanidine should be discontinued gradually, which will reduce the likelihood of a rebound increase in blood pressure and tachycardia. This especially applies to cases long-term use drug or therapy in high doses Oh.

Side effects

Possible adverse reactions (> 10% - very common; > 1% and< 10% – часто; >0.1% and< 1% – нечасто; >0.01% and< 0,1% – редко; < 0,01% – очень редко, с учетом сообщений об in some cases):

  • digestive system: very often – gastrointestinal disorders, xerostomia; often – nausea;
  • cardiovascular system: often - a decrease in blood pressure (in some cases it is pronounced, up to loss of consciousness and collapse); uncommon – bradycardia;
  • nervous system: very often – dizziness, drowsiness;
  • musculoskeletal system: very often – muscle weakness;
  • subcutaneous tissue/skin: allergic reactions(in particular rash);
  • psyche: often – hallucinations, insomnia, sleep disturbances;
  • laboratory parameters: often - increased activity of microsomal liver enzymes;
  • general disorders: very often – increased fatigue, withdrawal syndrome.

With the abrupt withdrawal of Tizanidine after its prolonged use or administration in high doses, as well as after combined use with drugs with antihypertensive effects, the development of tachycardia and increased blood pressure was observed. In some cases, this led to acute cerebrovascular accidents. In connection with the above, discontinuation of therapy should be carried out gradually.

There are reports of such violations (a cause-and-effect relationship has not been established, the frequency of occurrence of these side effects cannot be determined):

  • nervous system: vertigo;
  • psyche: anxiety disorders, hallucinations, confusion;
  • biliary tract, liver: liver failure, acute hepatitis;
  • organ of vision: blurred vision;
  • general disorders: asthenia, withdrawal syndrome.

Overdose

Main symptoms: vomiting, nausea, marked decrease in blood pressure, prolongation of the QTc interval, drowsiness, dizziness, anxiety, miosis, coma, respiratory failure.

Therapy: to remove tizanidine from the body, gastric lavage and administration of large quantity liquids, multiple uses activated carbon. Forced diuresis also accelerates the elimination of the substance. Subsequently, symptomatic therapy is carried out.

Recovery in all cases of overdose, including taking 400 mg of Tizanidine, was uneventful.

Special instructions

Hypotension may occur while taking Tizanidine. With a pronounced decrease in blood pressure, collapse and loss of consciousness are possible.

You must abstain from drinking alcohol during treatment.

There is information about cases of development of liver function disorders, however, when taking the drug in a daily dose of 12 mg, this rarely occurs. In connection with the above, patients using Tizanidine at a dose of 12 mg per day are recommended to monitor liver function tests once a month in the first 4 months of therapy. Also control liver function follows when clinical signs, suggesting liver dysfunction, including unexplained nausea, anorexia, fatigue. If the serum levels of alanine aminotransferase and aspartate aminotransferase are persistently exceeded by 3 times compared to the upper limit of normal, the drug is discontinued.

Impact on the ability to drive vehicles and complex mechanisms

Taking into account the profile of adverse reactions, it is recommended to refrain from driving vehicles during therapy.

Use during pregnancy and lactation

According to the instructions, Tizanidine is contraindicated for use during pregnancy and lactation (there are no clinical data confirming the safety/efficacy of the drug in this group of patients).

Use in childhood

Tizanidine is not prescribed to children under 18 years of age due to the lack of data confirming its effectiveness/safety.

For impaired renal function

In renal failure with creatinine clearance ≤ 25 ml/min, therapy should be administered with caution.

For liver dysfunction

For severe liver disorders, Tizanidine is not prescribed; for moderate ones, the drug should be used with caution.

Use in old age

For patients over 65 years of age, Tizanidine is prescribed with caution; minimal doses are indicated at the beginning of therapy. Subsequently, the dosage regimen is established taking into account the optimal ratio of effectiveness and tolerability.

Drug interactions

Features of the combined use of Tizanidine with inducers/inhibitors of the CYP1A2 isoenzyme:

  • inhibitors: increased plasma concentrations of tizanidine in the blood, which may cause overdose symptoms, including prolongation of the QTc interval; use with fluvoxamine and ciprofloxacin is contraindicated, as this can lead to a prolonged decrease in blood pressure, accompanied by dizziness, drowsiness, and a decrease in the speed of psychomotor reactions (in some cases, even loss of consciousness and collapse); combination with other inhibitors of the CYP1A2 isoenzyme, including antiarrhythmic drugs, cimetidine, some fluoroquinolones, rofecoxib, oral contraceptives and ticlopidine, is not recommended;
  • inducers: decreased plasma levels of tizanidine, which may cause a decrease in the effectiveness of the drug.

Combinations that require caution when prescribing:

  • drugs that prolong the QT interval, including amitriptyline, cisapride, azithromycin;
  • rifampicin: possible significant decrease plasma concentration of tizanidine in the blood. If necessary combined use It is recommended to increase the dose of Tizanidine;
  • other alpha-2 adrenergic agonists (including clonidine): this combination may potentially enhance the hypotensive effect (the combination is recommended to be avoided);
  • drugs with antihypertensive effects, including diuretics: a pronounced decrease in blood pressure (in some cases, up to loss of consciousness and collapse) and bradycardia are possible. If tizanidine is abruptly discontinued after combination therapy tachycardia and increased blood pressure were noted, which in some cases can lead to acute disorder cerebral circulation;
  • drugs with sedative and hypnotic effect(benzodiazepine, baclofen) and some other drugs such as antihistamines: may increase sedative effect tizanidine;
  • ethanol: increased likelihood of adverse reactions;
  • smoking: the systemic bioavailability of tizanidine in men who smoke is significantly reduced; during long-term therapy, higher doses of the drug may be required.

Analogues of Tizanidine are Sirdalud, Tizalud, Tizanil.

Terms and conditions of storage

Store in a place protected from light and moisture, at temperatures up to 25 °C. Keep away from children.

Shelf life – 3 years.

Conditions for dispensing from pharmacies

Dispensed by prescription.

Reviews of Tizanidine

According to reviews, Tizanidine is effective drug, however it is noted frequent development significant side effects. These include drowsiness, weakness, severe dizziness and urge to vomit, which may cause drug withdrawal.

Price for Tizanidine in pharmacies

The approximate price for Tizanidine (30 tablets per package) is 110–160 rubles.

Tizanidine contains the active substance tizanidine, as well as auxiliary components:

  • anhydrous lactose;
  • microcrystalline cellulose;
  • colloidal silicon dioxide;
  • stearic acid.

Release form

Tablets 2 and 4 mg, round. Color white.

On one side of the tablet there is a dividing strip, on the second there is a T2 or T4 marking.

Pharmacological action

Tizanidine is a centrally acting muscle relaxant. Once the active substance of the drug enters the body, it helps to reduce the tone of skeletal muscles, reduces their resistance during passive movements, reduces spasmodic reaction, enhances voluntary contractions.

In general, the drug has muscle-relaxing effect due to inhibition of spinal polysynaptic reflexes. This action caused by the release amino acids from the presynaptic terminals of spinal interneurons.

Pharmacodynamics and Pharmacokinetics

Absorption and distribution

After oral administration Tizanidine is essentially completely absorbed. Absolute bioavailability is approximately 40% (CV = 24%), due to extensive first pass through the liver.

The active substance of the drug is distributed with an average steady-state volume of distribution of 2.4 l/kg (CV = 21%). Protein binding is 30%.

Metabolism and excretion

The half-life of Tizanidine is approximately 2.5 hours (CV = 33%). Approximately 95% of the administered dose is metabolized. Basic cytochrome P450 isoenzyme participates in CYP1A2 metabolism with the formation of active metabolites. Their half-life ranges from 20 to 40 hours.

Excreted mainly through the kidneys (60%) and gastrointestinal tract (20%).

Indications for use of Tizanidine

Tizanidine is prescribed for the treatment of skeletal muscle spasticity, which accompanies the development of neurological diseases, such as:

The drug is also indicated for painful spasms of skeletal muscles that develop as a result of damage to the spine.

Contraindications

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

Side effects

A study of the effects of Tizanidine on patients revealed side effects, such as drowsiness, dry mouth, hypotension, lowering blood pressure, bradycardia, dizziness, weakness or asthenia, muscle spasms, hallucinations, fatigue, liver dysfunction and hepatotoxicity.

Less commonly, the following side effects may occur during treatment with this drug:

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

Instructions for use of Tizanidine

In accordance with the instructions for use of Tizanidine, the recommended starting dose is 2 mg.

Because the effect of the tablets peaks approximately 1 to 2 hours after dosing and dissipates between 3 and 6 hours after dosing, treatment may be given at 6 to 8 hour intervals. You can take no more than three tablets during the day.

The dosage may be gradually increased to 4 mg per dose if there is no benefit after four days of starting treatment. The total daily dose should not exceed 36 mg. Single doses more than 16 mg have not been studied.

Dosing in patients with renal impairment

Tizanidine tablets should be used with caution in patients with renal impairment (creatinine clearance

Dosing in patients with hepatic impairment

Also, this drug should be prescribed with caution to patients with any form of liver failure. In such patients, individual doses should be reduced during titration.

When treating patients with liver failure, it is necessary to regularly monitor levels aminotransferases. First monitoring is recommended one month after treatment.

Overdose

During a study of the effects of this drug on the body, specialists identified cases of intentional and accidental overdose of Tizanidine. Clinical manifestations overdoses have different pharmacology.

In most cases, there is a decrease in the sensorium, including lethargy, drowsiness, confusion And coma. Overdose also manifests itself in cardiac muscle dysfunction, including bradycardia and hypotension.

Interaction with other drugs

Interaction with Fluvoxamine and Ciprofloxacin

Simultaneous use Fluvoxamine or Ciprofloxacin and Tizanidine is contraindicated. Changes in the pharmacokinetics of Tizanidine with joint reception With Fluvoxamine or Ciprofloxacin can lead to a significant decrease in blood pressure, drowsiness and impaired psychomotor functions.

Interaction with CYP1A2 inhibitors

Due to potential drug interactions, simultaneous use of Tizanidine with other CYP1A2 inhibitors such as Zileyton, Fluoroquinolone should be avoided.

Taking the drug together with strong CYP1A2 inhibitors (Amiodarone, Mexiletine, Propafenone, Verapamil, Cimetidine, Famotidine, oral contraceptives, Acyclovir, And Ticlopidine) is strictly contraindicated.

Interaction with contraceptives

Concomitant use of Tizanidine with oral contraceptives not recommended. But if current state health requires treatment using this drug, the dosage should be minimal.

Incorrect dosing can lead to side effects: arterial hypotension, bradycardia, excessive drowsiness.

Interaction with alcohol

Alcohol increases the concentration of the active substance of the drug in the blood, which can lead to unwanted reactions.

Storage conditions

Best before date

The shelf life of the drug is 3 years.

Terms of sale

Dispensed from pharmacies with a doctor's prescription with the appropriate stamp.

Tizanidine analogs Level 4 ATX code matches:

On pharmaceutical market There are analogues of Tizanidine, which include:

  • Sirdalud;
  • Sirdalud MR;
  • Tizalud;
  • Tizanidin-Teva;
  • Tizanil-Teva.

Reviews of Tizanidine

Tizanidine is a drug that is tolerated differently by patients. Reviews about this drug allow us to conclude that taking it does not always have the expected effect.

Side effects occur in one out of three cases. For example, Elena from Barnaul writes:

“... Tizanidine was prescribed because I began to suffer from severe muscle pain and spasms. After taking the second pill, I felt severe dizziness, weakness and the urge to vomit. I thought it was just my body being so weak that it was reacting this way. I decided that continuing to take the pills would be fine. But no, everything continued and got worse - problems with the stomach, blood pressure, palpitations. After contacting a doctor, the tablets were replaced.”

Oleg from Novosibirsk also wrote about the manifestation of an adverse reaction:

“... I started taking Tizanidine and after the first pill I almost fell asleep right at work. I understood the mechanism of action - muscle spasm goes away during sleep.”

It is worth noting that there are only a few such reviews on the Internet; reviews are mostly positive, which indicates the effectiveness of this drug.

Tizanidine price

The cost of Tizanidine is optimal in terms of price/quality ratio, which is why many specialists prescribe these tablets for the treatment of their patients.

The price of Tizanidine tablets varies from 110 to 160 rubles and depends on the quantitative content of the active substance in one tablet.

  • Online pharmacies in RussiaRussia

WER.RU

    Tizanidine-Teva tablets 2 mg 30 pcs. Teva

    Tizanidine-Teva tablets 4 mg 30 pcs.Teva

    Tizanidine tablets 4 mg 30 pcs. Berezovsky Pharmaceutical Plant

ZdravZone

    Tizanidine-Teva 4 mg No. 30 tabletsTeva Pharmaceutical

    Tizanidine-Teva 2 mg No. 30 tabletsTeva Pharmaceutical

Pharmacy IFC

    Tizanidin-Teva Pharmaceutical plant Teva Private Co., Hungary

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PLEASE NOTE! Information about medications on the site is for reference and general information, collected from publicly available sources and cannot serve as a basis for making a decision on the use of medications in the course of treatment. Before using the drug Tizanidine, be sure to consult with your doctor.

Tizanidine is a medicine from the group of muscle relaxants. Prescribed to patients suffering from muscle pain, as well as a number of diseases.

At first it was used only for neurological diseases, but due to its analgesic properties, it began to be used by patients with headaches, neuropathic pain and a variety of musculoskeletal pain.

Most often it is prescribed to patients with complaints of osteochondrosis or hernia.

Pharmacological action

Tizanidine affects increased muscle tone, making it smaller, and at the same time relieves spasms. In addition, it does not affect skeletal muscles.

It has an analgesic effect and reduces the manifestations of both chronic and acute pain.

Pharmacokinetics of the drug

The tablets are absorbed very quickly, which is confirmed by tests - within just an hour the drug appears in the blood. The medicine is excreted from the body along with urine.

Indications for use

This drug is prescribed:

  • for painful muscle spasms associated with functional damage spine;
  • with multiple sclerosis;
  • after surgery for osteoarthritis or herniated disc;
  • for chronic myelopathy;
  • after a stroke;
  • for degenerative diseases of the spinal cord and seizures of central origin.

The Hidden Danger of Medicine

There are reasons why taking Tizanidine may not be safe.

They are called:

  • severe liver and kidney disease;
  • individual intolerance to the drug;
  • age (the drug is not prescribed for children);
  • pregnancy and lactation;
  • taking the tablets together with fluvomexamine.

Mechanism of action

Tizanidine stimulates alpha2-adrenergic receptors and thereby inhibits the release of amino acids that stimulate NMDA receptors.

Because of this, at the level of spinal cord neurons, polysynaptic transmission of excitation is suppressed. In addition, the drug does not affect monosynaptic reflexes and skeletal muscles.

Instructions for use

Dosages and methods of use of the drug depending on concomitant illness and neglect of the disease.

The initial dose of the drug is 2 mg. In this case, the effect of the medicine appears a few hours after administration, and ends after approximately 6 hours.

Therefore, the interval between doses should be 6–7 hours. Gradually the dosage can be increased to 4 mg. IN in rare cases the daily dose of the drug can be 36 mg.

Sick, suffering various diseases kidney or liver problems, should take this medicine very carefully. In addition, you should definitely consult with your doctor.

The first time after taking the drug, you should pay attention to how you feel. If it worsens, then you need to reduce the dose of the medicine.

Overdose and additional instructions

To relieve muscle spasms, you need to take Tizanidine in the form of tablets of 2 or 4 mg 3 times a day.

When a patient has a spastic state of the muscles, the doctor should set the dose individually. In no case should you exceed the daily dosage of the drug – 36 mg.

As for the capsules, then at the beginning of treatment, the daily dose of the drug should not exceed 6 mg, that is, the patient can take only one capsule. The maximum by which the dosage rate can be increased is another 6 mg.

When taking medication, you may experience side symptoms. Most often, patients feel nausea, dizziness, drowsiness and weakness. Low blood pressure and stomach upset are also observed.

When used together with antihypertensive drugs, bradycardia and hypotension may occur. You should consult a doctor if, after taking the drug, the patient feels:

  • pain in the right side;
  • loss of appetite;
  • severe fatigue;
  • increased muscle spasms.

Medicines should not be taken during pregnancy or lactation. And if you can’t do without taking medication, then breast-feeding needs to stop.

Also, you should not take the medicine with alcohol, as it increases drowsiness. Patients over 65 years of age should use the drug with caution.

Children practically do not take the drug and doctors do not recommend it, at least until they are 18 years old.

Patients who suffer from renal failure, you should definitely reduce the dose. Patients with heart disease also need to take the pills with extreme caution.

If, while taking the medication, there is feeling unwell, then use should be stopped immediately.

If an overdose of the drug occurs, the first symptoms will be: vomiting, drowsiness and, in as a last resort, coma. At home, doctors recommend using activated carbon.

If the symptoms of poisoning do not go away and intensify, you should seek medical help.

Tizanidine is a drug from the group of centrally acting muscle relaxants. The composition contains the active ingredient of the same name – tizanidine. The drug reduces clonic convulsions, due to which muscle resistance to passive movements decreases, and the number of active movements increases. Additionally, Tizanidine exhibits an analgesic effect.

Tizanidine inhibits the release of excitatory amino acids that stimulate N-methyl-D-aspartate receptors (NMDA receptors). As a result, at the level interneurons spinal cord, polysynaptic transmission of excitation is suppressed. It is important that Tizanidine does not have a direct effect on skeletal muscle, neuromuscular junctions or monosynaptic reflexes.

Tizanidine 2mg and 4mg photo tablets

The active substance is quickly absorbed into the gastrointestinal tract, the maximum concentration is observed 2-3 hours after administration. Eating food has no effect on pharmacodynamics. Tizanidine is excreted mainly through the urinary system.

Indications for use: Tizanidine

Tizanidine is used for the following diseases and conditions in the patient:

  • Muscle spasm, accompanied by pain due to pathologies of the spine (osteochondrosis, spondylosis, hemiplegia, etc.);
  • Postoperative condition for vertebral hernia;
  • Osteoarthritis of the hip;
  • Spastic condition of skeletal muscles caused by neurological diseases(multiple sclerosis, chronic myelopathy, stroke, degenerative diseases of the spinal cord).

Instructions for use of Tizanidine, dosage

To stop painful spasms of skeletal muscles, use 2-4 mg 3 times a day; in severe cases, it is additionally recommended to take 2-4 mg at night (2 tablets of Tizanidine 2 mg).

For spastic muscle conditions caused by neurological diseases, the starting dosage is 6 mg/day in 3 divided doses. The dose is gradually increased by 2-4 mg/day every 3-7 days.

Optimal healing effect usually achieved at a dose of 12-24 mg/day, divided into 3-4 doses.

The maximum daily dose of 36 mg of tizanidine should not be exceeded.

Capsules

The initial daily dose is 6 mg (1 Tizanidine capsule).

If necessary, the daily dose can be gradually increased until the required therapeutic action– per 1 capsule at intervals of 3–7 days.

Clinical experience shows that for most patients the optimal dose is 12 mg per day (2 capsules). And only in rare cases may it be necessary to increase the daily dose to 24 mg.

If you take tizanidine regularly, if you miss a dose, take the drug as soon as you remember. If it is close to your next pill, skip the dose and take the medicine as usual. You should not take a double dose of the drug.

Features of long-term use:

Discontinuation of the drug Tizanidine should be done gradually due to the risk of developing “withdrawal” syndrome - it can manifest itself in the form of anxiety, hand tremors, increased blood pressure, increased heart rate and increased muscle tension. If these symptoms appear, you should consult a doctor immediately.

To stop taking the drug, you need to gradually reduce the dose.

Overdose:

There are currently several reports of overdose with Tizanidine, including a case where the dose taken was 400 mg. Recovery in all cases was uneventful.

In case of an overdose, nausea, vomiting, a pronounced decrease in blood pressure, dizziness, drowsiness, miosis, anxiety, respiratory failure, and coma are possible. Treatment is symptomatic.

According to doctors, Tizanidine is well tolerated by patients, many side effects and cases of overdose are caused by improper use of the drug, in violation of the schedule or dosage. There are known cases of interaction with other medications, the taking of which was not warned to the attending physician. Be careful.

Contraindications Tizanidine

  • hypersensitivity to tizanidine or other components of the drug;
  • pregnancy;
  • breastfeeding period;
  • age under 18 years (efficacy and safety have not been established);
  • severe liver dysfunction;

Tizanidine should not be used during pregnancy. If it is necessary to prescribe to nursing mothers, breastfeeding should be discontinued.

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

Alcohol increases the concentration of the active substance of the drug in the blood, which can lead to unwanted reactions.

Tizanidine analogues, list of drugs

Analogues of Tizanidine in terms of effect on the body - anticonvulsants:

  • Baclofen
  • Mydocalm
  • Sirdalud
  • Tizalud
  • Tizanil

It is important to understand that the instructions for use of Tizanidine, price and reviews do not apply to analogues. Should not be used this information as a guide for prescribing analogues or for replacing Tizanidine with analogues in the treatment regimen. Any actions must be agreed with the attending physician.

Let's look at how to take Tizanidine and what properties this drug has. Muscle tissue human tends to contract. Sometimes, according to various reasons, the muscles of the body remain in a contracted state for a long time. Muscle spasm occurs. This is a very unpleasant and painful condition that worsens a person’s quality of life.

The release form of the medicine is round and convex tablets on both sides. Color white. Tizanidine 2 mg - one tablet contains 2 mg of the main substance. Auxiliary components include lactose, silicon, magnesium. One blister contains 10 tablets. The package may consist of 1–3 blisters. The drug is also available in polymer jars of 100 tablets.

What properties does Tizanidine have?

There are drugs that relax muscles and relieve them from spasm. Such drugs are common name- muscle relaxants. They influence motor neurons, as well as at the junctions of nerve endings and muscles.

Instructions for use of Tizanidine contain detailed description properties of the drug, indications and contraindications for use.

This medicine is marketed under various trade names.

Pharmacological action - antispastic. This means that the medicine relieves spasms smooth muscle and relieves increased muscle tone.

Tizanidine tablets have similar pharmacological properties with Mydocalm and Baclofen, but their mechanism of action is different.

The absorption of the substance is quite good, the medicine almost completely penetrates the blood. The highest concentration is observed after 1–2 hours. It is excreted from the body by the urinary system 3 hours after administration.

In the international drug classification system, the drug is listed as M03BX02. It is included in the list of vital and important medicines, which approved by the Ministry Healthcare.

Who is Tizanidine indicated for?

Let's consider the indications for use of this drug.
One of the indications is spasmodic pain in skeletal muscles caused by diseases of the spine:

  • osteochondrosis;
  • spondylosis;
  • hemiplegia;
  • herniated intervertebral discs;
  • osteoarthritis of the hip.

Indications for neurological diseases:

  • multiple sclerosis;
  • stroke;
  • spinal cord diseases;
  • cerebrovascular accident;
  • cerebral palsy;
  • skull injuries.

Contraindications to the use of the drug

There are contraindications to the use of the medication. The medicine is not used if there is sensitivity to this substance. There is no data on the effect of the drug on children's body. During pregnancy and while breastfeeding this remedy not used.

In general, the medicine is well tolerated, but side effects are possible:

  • the appearance of drowsiness;
  • feelings of overwork;
  • dizziness;
  • rashes in the mouth;
  • feeling of nausea.

Overdose and interactions with medications

If the dose of the drug is increased, muscle weakness will appear, sleep will be disturbed, blood pressure will drop, and the pulse will slow down.

For liver and kidney diseases, the dose of the drug is reduced. Because the medicine causes drowsiness and muscle weakness, then people whose work involves concentration and quick reactions should be very careful.

Drug interactions with other drugs manifest themselves in different ways.

In combination with drugs that lower blood pressure, diuretics, blood pressure can drop sharply, and the pulse can slow down.

In combination with alcohol, the relaxing effect of the drug is enhanced.

If an overdose of the drug occurs, before the ambulance arrives, you need to induce vomiting, take a sorbent and a diuretic. Symptoms similar condition are: respiratory failure, convulsions, fainting, loss of consciousness.

Reception features

To relieve muscle pain, the medicine is taken orally several times a day. It makes no difference when the drug is taken - before or after meals.

For neurological spasms, an individual course of therapy is selected based on the patient’s condition. The dosage of the drug and the duration of the course of treatment are prescribed by the doctor.

The medication is often used for exacerbation of osteochondrosis and the appearance of painful sensation in the spine. The pain appears due to muscle spasm, which the medication copes well with. As a result, the spasm decreases or disappears altogether.

Prices for the drug and its analogues

The drug, compared to , has quite cheap price. The cost of one package of 30 tablets starts from 150 rubles.

During an exacerbation of diseases of the musculoskeletal system, the medicine is often prescribed with Diclofenac or other non-steroidal drugs.

is the most popular substitute for Tizanidine. This similar drug, but with another trade name. Available in the form of tablets of 2–4 mg. Most main feature Sirdaluda is the ability to reduce muscle tone while maintaining strength in the muscles. After administration, the medicine is quickly absorbed, and within an hour its therapeutic effect is felt.

Let's consider in what areas of medicine this drug is used.

Neurology, rheumatology, traumatology, surgery, orthopedics, as well as sports medicine.
The drug has the same contraindications and side effects as Tizanidine.

Doctors often prescribe Tizanil to patients. The active substance of this medication irritates the corresponding receptors of the spinal cord and blocks excitation impulses sent along nerve fibers to the muscular frame of the back. This leads to restoration of mobility spinal column by reducing tension in the back muscles. The course of treatment with Tizanil is approximately 30–45 days. Treatment usually begins with a small dose. Then the dosage is gradually increased.

This drug, like the previous ones, consists of tizanidine, therefore it acts on the body in the same way as the above drugs.

So, Tizanidine are:

  • Sirdalud;
  • Sirdalud MR;

They are produced in different countries, so drug prices may vary.

TO Russian analogue refers to Tizanil and Tizalud. The price for 30 tablets of 2 mg is 135 rubles, and for tablets of 4 mg - 190 rubles. Tizanil is produced by the Berezovsky Pharmaceutical Plant, and Tizalud is produced by the Veropharm company.

TO foreign analogues include:

  1. (Germany, Switzerland, India) - the cost of the drug depends on the weight and varies from 200 to 500 rubles. Produced by Novartis Pharma Production and Dr. Reddy's laboratories."
  2. Sirdalud MR (Switzerland, India) - the price of 30 tablets weighing 6 mg is 573 rubles.
  3. Tizanidin-Teva (Hungary, Israel) - price, depending on the weight of the tablets, ranges from 120 to 170 rubles. Produced by the pharmaceutical company Teva.