Medicinal reference book geotar. Tizalud tablets: instructions for use Pharmacological effects and pharmacokinetics

Dosage form:   tablets Composition:

Active substance: Tizanidine hydrochloride - 2.288 mg and 4.576 mg in terms of tizanidine - 2.0 mg and 4.0 mg;

Excipients:

[Lactose anhydrous (lactopress)

117.012 mg and 234.024 mg, Microcrystalline cellulose 14.0 mg and 28.0 mg, Carboxymethyl starch sodium

(Primogel) 4.2 mg and 8.4 mg, Magnesium stearate 2.5 mg and 5.0 mg].

Tablet weight is 140.0 mg and 280.0 mg.

Description:

Tablets are white or white with a yellowish tint, round, biconvex with a score.

Pharmacotherapeutic group:Centrally acting muscle relaxant ATX:  

M.03.B.X Other centrally acting muscle relaxants

M.03.B.X.02 Tizanidine

Pharmacodynamics:

Centrally acting muscle relaxant. The main point of application is in the spinal cord. By stimulating presynaptic alpha2-adrenergic receptors, it suppresses the release of excitatory amino acids from interneurons of the spinal cord, which leads to inhibition of polysynaptic transmission of excitation in the spinal cord. As a result, muscle tone decreases. In addition to muscle relaxant properties, it also has a central, moderately pronounced analgesic effect.

Effective against acute painful muscle spasms and chronic spasms of spinal and cerebral origin. Reduces spasticity and clonic convulsions, as a result of which resistance to passive movements decreases and the range of active movements increases.

Pharmacokinetics:

Absorption - high; time to reach maximum plasma concentration (Cmax) - 1-2 hours. Bioavailability - 34%. Eating does not affect Coca Neti Ku Pharma. Volume of distribution - 2.6 l/kg. Communication with plasma proteins - 30%. In the dose range from 4 to 20 mg, pharmacokinetics are linear. Metabolized quickly and largely in the liver (95%) with the formation of inactive metabolites. The half-life (T1/2) is 2-4 hours. It is excreted mainly by the kidneys (70% of the dose in the form of metabolites, 2.7% unchanged). In patients with renal failure (creatinine clearance less than 25 ml/min), the maximum plasma concentration (Cmax) increases by 2 times, T1/2 - 14 hours, the area along the pharmacokinetic concentration-time curve (AUC) increases by 6 times.

Indications:

painful muscle spasm associated with static and

functional diseases of the spine (cervical and lumbar syndromes), as well as after surgical interventions (for example, for a herniated disc or osteoarthritis of the hip joint);

spasticity of skeletal muscles in neurological diseases (for example, multiple sclerosis, chronic myelopagia, degenerative diseases of the spinal cord, consequences of cerebrovascular accidents, as well as cerebral palsy / patients over 18 years old /).

Contraindications:

Severe liver dysfunction;

Hypersensitivity to tizanidine and other components of the drug;

Rare hereditary lactose intolerance, severe lactase deficiency, glucose-galactose malabsorption (for this dosage form containing lactose);

The use of tizanidine in children (under 18 years of age) is not recommended, because experience with the drug in this category of patients is limited.

Carefully:

renal failure, arterial hypotension,

bradycardia, simultaneous use of oral contraceptives, age over 65 years

Pregnancy and lactation:

Since there have been no controlled studies of tizanidine in pregnant women, it should not be used during pregnancy unless the expected benefit to the mother outweighs the possible risk to the fetus.

Tizanide is excreted in breast milk in small quantities. However, if it is necessary to use tizanidine during lactation, the issue of stopping breastfeeding should be considered.

Directions for use and dosage:

Relief of painful muscle spasms: orally, 2-4 mg 3 times a day, in severe cases - an additional 2-4 mg at night.

Treatment of spasticity caused by neurological diseases: initial dose - 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 is 12-24 mg in 3-4 doses; the maximum daily dose is 36 mg.

If you need to get a more pronounced effect, it is recommended to first increase the dose prescribed once a day, then increase the frequency of administration.

Side effects:

From the nervous system: drowsiness, dizziness, hallucinations, insomnia, sleep disorders.

From the cardiovascular system: bradycardia, decrease in blood pressure (in some cases pronounced, up to collapse and loss of consciousness).

From the digestive system: dry mouth, nausea, dyspepsia, increased activity of “liver” transaminases, hepatitis, liver failure.

From the musculoskeletal system: muscle weakness.

Other: increased fatigue, hypercreatininemia.

In case of abrupt withdrawal after prolonged treatment and/or taking high doses of the drug (as well as after simultaneous use with antihypertensive drugs): tachycardia, increased blood pressure, in some cases - acute cerebrovascular accident.

Overdose:

Symptoms: nausea, vomiting, marked decrease in blood pressure, dizziness,

drowsiness, miosis, anxiety, respiratory failure, coma.

Treatment: gastric lavage, administration of activated carbon, forced diuresis, symptomatic therapy.

Interaction:

Concomitant use of tizanidine with fluvoxamine or ciprofloxacin, inhibitors of cytochrome P450 isofermeite 1A2, leads to a 33-fold increase in tizanidine AUC. The result of combined use may be a clinically significant and prolonged decrease in blood pressure, leading to drowsiness, weakness, and inhibited psychomotor reactions (in some cases, even collapse and loss of consciousness).

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

Ethanol and sedatives can enhance the sedative effect of tizanidine, so simultaneous use with other sedatives and/or alcohol is not recommended.

Special instructions:

It is recommended to monitor liver function once a month for the first 4 months of treatment, in those patients prescribed a daily dose of 12 mg or higher, as well as in cases where clinical signs suggestive of impaired liver function are observed, such as unexplained nausea, anorexia , feeling tired. If the activity of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) persistently exceeds the upper limit of normal by 3 times or more, stop taking tizanidine.

Patients with congenital long QT interval syndrome should be prescribed with caution, because In preclinical studies of chronic toxicity in animals (dogs), a prolongation of the Q-T interval was noted when the drug was used at a dose equivalent to the maximum dose for humans. Due to the threat of withdrawal syndrome, the dose of tizanidine is reduced gradually.

Impact on the ability to drive vehicles. Wed and fur.:

During treatment, care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Centrally acting muscle relaxant. The mechanism of action is associated with stimulation of presynaptic α2 receptors, which leads to suppression of the release of excitatory amino acids (glutamic acid, aspartic acid), which stimulate receptors for N-methyl-D-aspartate. As a result, polysynaptic transmission of excitation is suppressed at the level of interneurons of the spinal cord. It also has a moderate central analgesic effect due to inhibition of the function of interneurons of the dorsal horns of the spinal cord. Reduces resistance to passive movements, reduces spasms and clonic convulsions, increases the strength of voluntary contractions. Does not affect neuromuscular transmission.
After use, tizanidine is quickly and almost completely absorbed from the gastrointestinal tract. Concomitant food intake does not affect the pharmacokinetics of tizanidine. In the dose range from 4 to 20 mg, the pharmacokinetics of the drug is linear. The drug is characterized by a low individual range of pharmacokinetic parameters. The maximum concentration in blood plasma is achieved 1-2 hours after administration. Due to the pronounced effect of the first passage through the liver, bioavailability is 34%, binding to plasma proteins is 30%. Tizanidine is quickly and in large quantities metabolized in the liver to form inactive metabolites. Penetrates through the blood-brain barrier and in small amounts into breast milk. The half-life of elimination from the systemic circulation is 2-4 hours. Excretion occurs mainly by the kidneys (60-70%) and intestines (20-25%), mainly in the form of metabolites, as well as unchanged (about 5%).
In patients with renal failure (creatinine clearance ≤25 ml/min), the maximum concentration in blood plasma is 2 times higher than that in healthy volunteers, the half-life is extended to 14 hours.
When taken orally, the effect of the drug appears within 30-45 minutes, the maximum effect occurs within 1-2 hours.

Indications for use of the drug Tizalud

painful muscle spasm associated with static and functional diseases of the spine (cervical and lumbar syndromes), as well as after surgical interventions (for a herniated disc, osteoarthritis of the hip joint); spasticity of skeletal muscles in neurological diseases (multiple sclerosis, chronic myelopathy, degenerative diseases of the spinal cord, cerebrovascular accidents, cerebral palsy).

Use of the drug Tizalud

Adults take orally, regardless of food, with a small amount of liquid. The dosage regimen is set individually, taking into account the indications, effectiveness and tolerability of therapy.
At painful muscle spasm prescribed 2 or 4 mg 3 times a day. In severe cases, an additional 2 or 4 mg of tizanidine is prescribed at night.
At spasticity of skeletal muscles caused by neurological diseases, the initial daily dose should not exceed 6 mg (2 mg 3 times a day). The daily dose can be increased gradually by 2-4 mg/day, at intervals of 3-4 to 7 days. Typically, the optimal therapeutic effect is achieved with a daily dose of 12-24 mg, distributed over 3 or 4 doses at equal intervals.
The highest dose of tizanidine for adults is 36 mg/day.
In patients with renal failure (creatinine clearance ≤25 ml/min), the initial dose is 2 mg 1 time per day. The dose should be increased gradually, taking into account the effectiveness and tolerability of therapy. If a more pronounced effect is required, it is recommended to first increase the dose used once a day, and then increase the frequency of use.
The duration of the course of therapy is determined depending on the dynamics of muscle-tonic and pain manifestations. For acute pain of muscular origin, the duration of taking the drug is from 1 to 2-3 weeks. For chronic pain syndromes, a longer course may be required, which is determined individually and averages from 3-6 weeks to 1 year.

Contraindications to the use of Tizalud

Severe liver dysfunction, simultaneous use of fluvoxamine, increased individual sensitivity to the components of the drug, during pregnancy and lactation, in children under 18 years of age.

Side effects of the drug Tizalud

From the side of the central nervous system: drowsiness, weakness, dizziness, dry mouth; rarely - sleep disorders, hallucinations.
From the musculoskeletal system: rarely - muscle weakness.
From the gastrointestinal tract: rarely - nausea, gastrointestinal disorders, transient increase in the activity of liver transaminases; very rarely - acute hepatitis.
From the cardiovascular system: often - decreased blood pressure, bradycardia.
Others: fatigue, rarely - allergic reactions (itching, rash, urticaria).

Special instructions for the use of Tizalud

Use with caution in elderly patients due to the likelihood of a significant decrease in renal clearance.
If side effects occur, possibly related to impaired liver function (unexplained nausea, anorexia, fatigue), as well as in patients using tizanidine at a daily dose of 12 mg, it is necessary to monitor liver function tests once a month in the first 4 months of treatment. If serum levels of hepatic transaminases persistently exceed the upper limit of normal by ≥3 times, use of the drug should be discontinued.
Since the tablets contain lactose, it is not recommended to use the drug in patients with hereditary galactose intolerance, severe lactase deficiency and glucose (galactose) malabsorption.
Use during pregnancy and lactation. Taking the drug during pregnancy is contraindicated. If treatment with tizanidine is necessary, breastfeeding should be discontinued.
Impact on the ability to drive vehicles and machinery. If side effects from the central nervous system (drowsiness, etc.) occur, patients should refrain from types of work that require high concentration and quick reaction, such as driving vehicles or working with machines and mechanisms.

Drug interactions Tizalud

Concomitant use of tizanidine with the CYP1A2 inhibitor fluvoxamine is contraindicated.
Caution should be exercised when using tizanidine in combination with other CYP1A2 inhibitors, namely: antiarrhythmic drugs (amiodarone, mexiletine, propafenone), cimetidine, fluoroquinolones (enoxacin, pefloxacin, ciprofloxacin, norfloxacin), rofecoxib, oral contraceptives and ticlopidine.
With the simultaneous use of tizanidine and antihypertensive drugs, including diuretics, the development of arterial hypotension and bradycardia is possible.
When used in combination, sedatives and alcohol may enhance the sedative effect of tizanidine.

Tizalud overdose, symptoms and treatment

If recommended doses are exceeded, nausea, vomiting, arterial hypotension, dizziness, drowsiness, miosis, anxiety, respiratory failure, coma are possible. .
Treatment:
drug withdrawal, gastric and intestinal lavage, repeated intake of activated carbon, symptomatic therapy. Forced diuresis is indicated. There is no specific antidote.

Storage conditions for the drug Tizalud

At a temperature not higher than 25 °C.

List of pharmacies where you can buy Tizalud:

  • Saint Petersburg

What is the drug "Tizalud"? Instructions for use, reviews and features of this medicine will be discussed below. You will also find out whether the product in question has side effects and prohibitions on use.

Form, packaging of medicine, composition

In what form is the drug "Tizalud" produced? Patient reviews report that this medication is sold in tablet form, which may include 4 or 2 mg of the active ingredient tizanidine.

In addition to the mentioned substance, the composition of the drug in question includes such additional elements as anhydrous lactose, sodium carboxymethyl starch, magnesium stearate and microcrystalline cellulose.

Tizalud tablets, reviews of which are presented below, are packaged in contour cells, which are placed in cardboard boxes.

Pharmacology of the oral agent

What is remarkable about a drug like Tizalud? Instructions and expert reviews indicate that this drug is a muscle relaxant that exhibits a central effect.

What changes occur in the human body after taking the medicine in question? The effect of its active component on alpha2-adrenergic receptors (presynaptic) contributes to inhibition of the process of release of excitatory amino acids from intermediate spinal neurons, which ultimately leads to slow polysynaptic propagation of the impulse in the spinal cord. Thanks to this mechanism of action, the tone of the patient’s muscle tissue is significantly reduced.

Features of the medicine

What other properties are characteristic of the drug "Tizalud"? Reviews claim that, in addition to the muscle relaxant effect, tizanidine has a moderate analgesic effect.

According to the instructions, such tablets are very effective for chronic spasms of spinal and cerebral origin, as well as painful and acute spasms of muscle tissue.

Taking this medication significantly reduces muscle spasticity and clonic convulsions, as a result of which resistance to passive movements is reduced and the likelihood of active actions is increased.

Indications for taking the medication

Under what patient conditions does a remedy such as Tizalud work most effectively? Reviews of the drug indicate that this medication quite well and quickly eliminates muscle spasms that are observed in pathologies of the spinal column and are accompanied by pain. Thus, the remedy in question is often prescribed for:

  • spondylosis;
  • hemiplegia;
  • osteochondrosis;
  • syringomyelia;
  • lumbar and cervical syndromes.

Are there other indications for the drug Tizalud? Reviews from experts say that this remedy is actively used in the postoperative period after intervention for intervertebral hernias and osteoarthritis of the femoral joint. Also, the tablets in question are good for pain and muscle spasticity caused by neurological diseases, including chronic myelopathy, cerebral palsy, degenerative changes in the spinal cord, convulsions of central origin, cerebrovascular accidents, multiple sclerosis, stroke, cranial and brain injuries.

Prohibitions on the use of oral medications

What contraindications should patients be aware of before taking Tizalud tablets? The instructions and reviews report that there are not very many prohibitions on the use of this medicine. These include only the following conditions:

  • patient hypersensitivity to tizanidine, as well as other components of the drug;
  • parallel use of drugs such as Ciprofloxacin and Fluvoxamine, as well as other potent inhibitors of the CYP1A2 isoenzyme.
  • liver pathologies (severe);
  • gestation period;
  • minor age;
  • breastfeeding period.

Prescribing medication with caution

The medication in question should be prescribed with caution in the following cases:

  • with renal failure;
  • aged over 65-68 years;
  • with bradycardia;
  • with arterial hypotension;
  • when used together with oral contraceptives.

The drug "Tizalud" (tablets): instructions for use

Reviews from doctors report that this medication should be taken only after an individual consultation with a specialist.

Tizalud tablets are taken orally with plain water, regardless of the meal.

The dosage of this medicine depends on the type and course of the disease. According to the instructions, for neurological pathologies that cause painful (spastic) contraction of muscle tissue, treatment is recommended to begin with a daily dose of 6 mg, which is divided into three doses. Depending on the nature of the spasm and pain, this amount of the drug can be increased by 2-4 mg over the next 3-7 days.

As medical practice shows, the maximum therapeutic effect is observed when taking a daily dose of 12-24 mg. In this case, 36 mg is the maximum permissible daily dosage.

To relieve painful spasms of skeletal muscles, Tizalud tablets, reviews of which are controversial, are prescribed 2-4 mg three times a day. In especially severe cases, doctors recommend additional medication at night in the same amount (that is, 2-4 mg).

The duration of use of the drug "Tizalud" depends on the dynamics of muscle-tonic and pain manifestations. As a rule, acute muscle pain requires careful treatment for 8-20 days. For chronic pain syndrome, depending on the severity and origin, the patient may need longer therapy, which is determined on an individual basis (can last for one year).

Adverse reactions

Unfortunately, taking the medication in question can cause many negative reactions from the central nervous system, digestive tract, cardiovascular and respiratory systems, and others. Some of the most common side effects include the following:

  • nausea, hepatitis, dizziness, dyspepsia;
  • drowsiness, bradycardia, hallucinations;
  • liver failure, sleep disturbances, dry mouth;
  • insomnia, increased activity of liver transaminases, muscle weakness, decreased blood pressure;
  • increased fatigue, hypercreatininemia.

It should also be noted that abrupt withdrawal of the drug "Tizalud", especially after its combination with antihypertensive drugs and long-term treatment or taking large dosages, can quite easily lead to the development of tachycardia, increased blood pressure, and in some cases to acute cerebrovascular accident .

Overdose of Tizalud tablets

With a fairly severe and regular violation of the dosage regimen, as well as when taking increased doses of the drug in question, the patient experiences the following conditions: drowsiness, nausea leading to vomiting, dizziness, development of hypotension, anxiety, miosis, coma, respiratory failure.

With such symptoms, the patient requires immediate gastric lavage, as well as bowel cleansing with an enema. In addition, the victim is advised to take sorbents, diuresis (forced) and further symptomatic therapy.

Interaction with other medications

What medications are prohibited from taking Tizalud? Parallel use of this medication with Fluvoxamine, Ciprofloxacin and other potent inhibitors of the CYP1A2 isoenzyme (including Amiodarone, Mexiletine, Propafenone, Cimetidine, Norfloxacin, Enoxacin, Pefloxacin, Ticlopidine ", "Rofecoxib" and oral contraceptives) are not allowed.

Antihypertensive medications significantly increase the risk of lowering the patient’s blood pressure and the development of bradycardia.

Ethanol and sedatives may enhance the hypnotic effects of tizanidine.

Special information

When conducting long-term therapy with Tizalud, doctors need to monitor the patient’s liver condition at least once a month (preferably during the first four months of treatment).

Due to the risk of “withdrawal syndrome” if treatment is stopped, the dose of tizanidine should be reduced gradually.

It is better to avoid taking Tizalud tablets if the patient’s professional activity involves driving vehicles and carrying out dangerous or precise work.

Cost, analogues

The cost of the drug in question in Russian pharmacies is about 130-175 rubles (for 30 tablets, 2 mg and 4 mg). If required, this medication can be replaced with such drugs as “Tolperil”, “Lioresal”, “Mydocalm”, “Baklosan”, “Tolperisone” and others.

"Tizalud" is a drug whose main purpose is to eliminate cramps and reduce the number of spasms in skeletal muscles. The required effect is achieved thanks to tisinidine, the main active substance of the medical drug.

Composition of the drug

One tablet contains 2 or 4 mg of tizanidine. Excipients: sodium carboxymethyl starch, anhydrous lactose, magnesium, microcrystalline cellulose.

Medicinal properties

"Tizalud" is a centrally acting muscle relaxant drug. It effectively helps eliminate acute muscle spasms, as well as spasms of spinal etiology. This drug also relieves inflammation and swelling of the affected joints.

Tizalud is excreted in bile and urine.

Indications for use

The use of "Tizaluda" is effective for the following diseases and conditions:

  • Skeletal muscle spasm that was caused by damage to the vertebrae
  • Spasm in the cervical and lumbar regions
  • Pathologies of the spine that are accompanied by acute pain
  • Multiple sclerosis, which causes spasticity in skeletal muscles
  • Degenerative diseases of the spinal cord
  • Herniated disc
  • Osteoarthritis of the hip
  • Painful sensations after operations
  • Hemiplegia
  • Myelopathy
  • Cerebral paralysis
  • Stroke
  • Circulatory disorders
  • Cramps.

Release form

The average price is from 120 to 150 rubles.

This drug is available in the form of tablets in dosages of 2 and 4 mg. One package of “Tizalud” tablets contains 30 pieces. Odorless tablets.

Mode of application

Tizalud is intended to be used internally.

To relieve muscle spasms, you need to take 2 mg three times a day. In particularly severe cases, the dose can be increased to 4 mg per day.

The total duration of therapy is determined by the attending physician depending on the susceptibility of the body, symptoms and severity of the disease.

During pregnancy and breastfeeding

Tizalud tablets should not be used during pregnancy, unless the benefits to the expectant mother are greater than the possible risks to the fetus.

However, if there is a need for treatment with Tizalud during lactation, as a result of which the baby may suffer, then the question of stopping breastfeeding should be raised.

Since the drug is prohibited for use by pregnant women, you need to know other, safer ways to treat seizures, which you can read about in the article:.

Contraindications

The drug has the following contraindications:

  • Age up to 18 years
  • Pregnancy
  • Lactation period
  • Severe liver diseases
  • Individual intolerance to the components of the drug
  • Period after stroke
  • Simultaneous therapy with the drug Ciprofloxacin.

Precautionary measures

Caution should be taken when taking the drug under the following circumstances:

  • Old age (over 60 years)
  • Arterial hypotension;
  • Acute renal failure
  • Deterioration of liver function.

Interaction with other drugs

This drug cannot be combined with inhibitors of the CYP1A2 isoenzyme - antiarrhythmic drugs:

  • Cimetidine
  • Pefloxacin
  • Ticlopidine
  • Norfloxacin
  • Fluvoxamine
  • Amiodarone.

Also, the substance tizanidine cannot be combined with ethanol and antihypertensive drugs, since this increases the risk of bradycardia and increased blood pressure.

Tizanidine should not be taken with alcoholic beverages, as this may cause side effects to the patient.

Side effects

This drug may cause the following side effects:

  • In the nervous system:
    • Drowsiness or, conversely, loss of sleep
    • Dizziness and headaches
    • Hallucinations
    • Cramps.
  • In the digestive system:
    • Diarrhea, nausea
    • Hepatitis
    • Constipation
    • Heartburn and dry mouth
    • Increased liver enzymes.
  • In the cardiovascular system:
    • A sharp decrease in blood pressure
    • Collapse
    • Loss of consciousness
    • Arrhythmia or tachycardia
    • Bradycardia.
  • Other side effects:
    • Loss of strength, weakness and fatigue
    • Muscle pain
    • Cerebrovascular accident.

Overdose

In case of overdose, the patient may experience the following symptoms:

  • Nausea
  • Increased blood pressure
  • Convulsions
  • Heavy breathing
  • Nervousness and anxiety
  • Dizziness
  • Hypotension
  • Drowsiness.

Conditions and shelf life

The drug must be stored in a dry and dark place at a temperature of no more than 25 degrees.

Shelf life: 2 years from the production date indicated on the package.

Analogs

Tizalud has the following medicinal analogues:

Novartis Pharma, Switzerland
Price from 200 to 230 rub.

Main action: centrally acting muscle relaxant. Reduces spasticity in the patient, as well as convulsions. Prescribed for chronic myelopathy, multiple sclerosis, paralysis and many other diseases. Release form: round white tablets packed in a foil blister.

pros

  • Effectively relieves muscle spasms
  • Helps relieve pain after surgery

Minuses

  • Contraindicated in renal failure
  • Not recommended for use in old age.

Polpharma, Poland
Price from 240 to 270 rub.

Main action: centrally acting muscle relaxant. Prescribed for neurological diseases. Ingredients: baclofen - 25 mg.

pros

  • Increases movement in affected joints
  • Absorbed quickly.

Minuses

  • Contraindicated during pregnancy
  • It is not recommended to take for atherosclerosis.

« «

Teva Private, Hungary.
Price from 150 to 200 rub.

Main action: centrally acting muscle relaxant. Reduces the tone of skeletal muscles and relieves spasm. It also reduces muscle resistance during movements and increases their contractions. Composition: tizanidine – 4 mg. Available in the form of white tablets. which on one side have a characteristic engraving “T2”.

pros

  • Relieves pain from injuries of the spine and joints
  • Improves blood circulation

Minuses

  • Does not combine well with other drugs
  • Contraindicated for use in patients with renal failure.

Tizalud has an analgesic effect, is able to reduce the intensity of spasms, clonic convulsions and increase the intensity of voluntary contractions. The drug belongs to the group. Medicine is prescribed for.

The principle of operation affects presynaptic receptors, which reduces the degree of excitability of amino acids that affect M-methyl-B-aspartate receptors. As a result, at the level of spinal cord neurons, polysynaptic reactions are extinguished.

Composition of the drug and release form

1 capsule of the product contains:

  • 2 mg tizanidine (in the form of hydrochloride) - the main active ingredient;
  • stearic acid;
  • cellulose;
  • lactose anhydrous.

A blister contains 10 tablets, one box contains 3 blisters.

Pharmacological effects and pharmacokinetics

The drug is capable of causing a weak analgesic effect caused by inhibition of the functioning of neurons in the posterior parts of the spinal cord.

The medicine also reduces resistance during passive movements, softens spasmodic reflexes and clonic convulsions.

The intensity of voluntary reflexes also increases. In this case, there is no interaction with neuromuscular transmission.

Tizanidine is the main active ingredient of Tizalud and is very quickly absorbed by the body. Within an hour, its concentrate in the blood plasma reaches its maximum value.

In this case, bioavailability matters - 34%.

The substance is 30% bound to plasma protein. The deviation of pharmaceutical parameters is very low: (Cmax and AUC), because of this it is possible to reliably estimate the drug concentrate in blood plasma orally.

Who is the drug prescribed for?

The drug is prescribed to adult patients suffering from diseases of the neuromuscular system, prescribed: 2 - 4 mg three times a day. If the patient is experiencing a particularly severe form of the disease, 2 or 4 mg can be taken as a supplement before bedtime.

Indications for use of Tizalud:

Important! During times of neurological diseases, the dosage of the medication must be selected separately in each individual case.

Contraindications for use

In the following cases, the use of the drug is not recommended:

  • hypersensitivity to one of the active ingredients of the drug;
  • acute disturbances in liver function;
  • combined use of Ciprofloxacin with Fluvoxamine.

More detailed information about contraindications to Tizalud is in the official instructions that come with the drug.

Tactics and strategy of therapy

Persons who have reached the age of majority take the drug orally, regardless of when food is taken, and wash down the medicine with water.

The regimen of use and dosage is prescribed by the doctor, taking into account the individual characteristics of the patient and such factors as allergic reactions and age. The maximum general daily intake of the drug for adults is 36 mg per day.

For people who suffer from acute renal failure, the dose must be reduced; for them the daily norm will be 2 mg once a day.

Increase the dose slowly, taking into account how effectively the medicine works and how the body reacts to it. To obtain a more pronounced effect, initially increase the dosage of the drug, and only then the frequency of administration per day.

Cases of overdose

An overdose of the drug has not yet been thoroughly studied, so it is impossible to say exactly about the consequences. In isolated cases, the following symptoms were noticed:

  • drowsiness;
  • nausea;
  • anxiety;
  • vomiting attacks;
  • arterial hypotension;
  • distress;
  • bradycardia;
  • miosis;
  • QT prolongation;
  • dizziness;
  • coma.

In cases of overdose, first of all, the stomach is washed many times with solutions of activated carbon. Forced diuresis is carried out, it helps in the rapid removal of drug residues from the body. Further treatment is carried out according to the symptoms.

Possible troubles during admission

The following side effects were observed when taking the drug:

  • serum transaminases;
  • predisposition to sleep;
  • dysfunction in the digestive system;
  • excessive fatigue;
  • low pressure;
  • seizures;
  • dry mouth.

Symptoms are most often mild and only visible in patients using Tizalud to combat muscle spasms.

In those people who take a large dosage for treatment, the symptoms of side effects appear much more clearly and more often, but usually they never cause concern, are considered a normal, concomitant phenomenon, and treatment is not stopped.

There are also such side effects: arterial hypotension, bradycardia, muscle weakness, poor sleep, attacks of hallucinations and even hepatitis.

special instructions

The drug may affect the ability to normally drive a vehicle or operate machinery. When the central nervous system begins to experience side effects as a result of the drug (the person wants to sleep, etc.), the patient should refuse such work that requires increased attention or reaction.

For example, driving various vehicles or other mechanisms. If, when taking the drug, the symptoms of side effects do not go away for a long time or, even worse, intensify, you should consult your doctor for advice.

When side effects occur, it may be due to liver weakness (sudden nausea, fatigue, etc.) and in people who take more than 12 mg of tizanidine per day. In such cases, it is necessary to monitor the liver through special tests (tests) monthly, during the first half of treatment.

If the amount of liver transaminases exceeds the prescribed level three times, the drug should be stopped immediately.

For those who have kidney dysfunction, no more than 2 mg of the drug per day can be prescribed. Next, a very careful increase in the dose occurs, at which time the patient is under the constant supervision of a doctor. Initially, the amount of the drug taken per day increases, and only then the number of doses.

Interaction with other drugs

If, in addition to Tizalud, any other medicine is prescribed, before taking them together, be sure to consult your doctor about this possibility. It is strictly forbidden to take tizanidine and the inhibitor fluvoxamine at the same time.

It is also necessary to take the drug with extreme caution with drugs that increase the QT interval. And the combined use of tizanidine with alcohol will enhance its effect on the body.

Use during pregnancy and lactation

There is very little information that explains the effect of the drug on pregnant women, so it is not prescribed during pregnancy.

There are exceptions when the drug is still prescribed, in cases where its benefit is more important for the life of the mother than the potential risk for the unborn child.

It is known that the active substance tizanidine passes into mother's milk in small quantities. That is why the medicine is also not prescribed to women who feed their baby with their own milk.

There is no information yet regarding the effect of the drug on children and adolescents. Therefore, they are not prescribed medicine.

From patient experience

Tizalud tablets have found their admirers among patients, as confirmed by numerous reviews online.

I started taking the drug after I started to experience cramps in my feet. There were no prerequisites for this, no injuries or anything like that, probably just age.

As a result, after consulting with a doctor, I received a prescription for Tizalud. The treatment complex lasted two months, although after the first two weeks the symptoms disappeared. After a while I plan to take the drug again for prevention purposes.

Oksana Dmitrievna 62 years old, Irkutsk

There was, as a result, an artery was interrupted and the blood supply to the brain was disrupted, there were a lot of negative symptoms, a real nightmare.

The district hospital prescribed a number of drugs to heal and restore the function of the circulatory system and brain, but after long-term use, I did not see any positive sensations other than side effects. Now I'm trying this drug. I will definitely write about the results.

Ivan 44 years old, Tver

My husband and I were in a car accident, resulting in a head injury. I just felt sick every day for six months; I couldn’t work or sleep normally.

Tizalud helped almost immediately, after a month of taking it everything fell into place.

Alisa 19 years old, Syktyvkar

Storage conditions and periods

The medicine should be stored in the original box at a temperature of 15 - 25 ° C. Keep out of reach of sunlight and children. The shelf life of the drug is three years.

There are analogues of Tizalud on the market with similar characteristics:

What is the drug "Tizalud"? Instructions for use, reviews and features of this medicine will be discussed below. You will also find out whether the product in question has side effects and prohibitions on use.

Form, packaging of medicine, composition

In what form is the drug "Tizalud" produced? Patient reviews report that this medication is sold in tablet form, which may include 4 or 2 mg of the active ingredient tizanidine.

In addition to the mentioned substance, the composition of the drug in question includes such additional elements as anhydrous lactose, sodium carboxymethyl starch, magnesium stearate and microcrystalline cellulose.

Tizalud tablets, reviews of which are presented below, are packaged in contour cells, which are placed in cardboard boxes.

Pharmacology of the oral agent

What is remarkable about a drug like Tizalud? Instructions and expert reviews indicate that this drug is a muscle relaxant that exhibits a central effect.

What changes occur in the human body after taking the medicine in question? The effect of its active component on alpha2-adrenergic receptors (presynaptic) contributes to inhibition of the process of release of excitatory amino acids from intermediate spinal neurons, which ultimately leads to slow polysynaptic propagation of the impulse in the spinal cord. Thanks to this mechanism of action, the tone of the patient’s muscle tissue is significantly reduced.

Features of the medicine

What other properties are characteristic of the drug "Tizalud"? Reviews claim that, in addition to the muscle relaxant effect, tizanidine has a moderate analgesic effect.

According to the instructions, such tablets are very effective for chronic spasms of spinal and cerebral origin, as well as painful and acute spasms of muscle tissue.

Taking this medication significantly reduces muscle spasticity and clonic convulsions, as a result of which resistance to passive movements is reduced and the likelihood of active actions is increased.

Indications for taking the medication

Under what patient conditions does a remedy such as Tizalud work most effectively? Reviews of the drug indicate that this medication quite well and quickly eliminates muscle spasms that are observed in pathologies of the spinal column and are accompanied by pain. Thus, the remedy in question is often prescribed for:

  • spondylosis;
  • hemiplegia;
  • osteochondrosis;
  • syringomyelia;
  • lumbar and cervical syndromes.


Are there other indications for the drug Tizalud? Reviews from experts say that this remedy is actively used in the postoperative period after intervention for intervertebral hernias and osteoarthritis of the femoral joint. Also, the tablets in question are good for pain and muscle spasticity caused by neurological diseases, including chronic myelopathy, cerebral palsy, degenerative changes in the spinal cord, convulsions of central origin, cerebrovascular accidents, multiple sclerosis, stroke, cranial and brain injuries.

Prohibitions on the use of oral medications

What contraindications should patients be aware of before taking Tizalud tablets? The instructions and reviews report that there are not very many prohibitions on the use of this medicine. These include only the following conditions:

  • patient hypersensitivity to tizanidine, as well as other components of the drug;
  • parallel use of drugs such as Ciprofloxacin and Fluvoxamine, as well as other potent inhibitors of the CYP1A2 isoenzyme.
  • liver pathologies (severe);
  • gestation period;
  • minor age;
  • breastfeeding period.

Prescribing medication with caution

The medication in question should be prescribed with caution in the following cases:

  • with renal failure;
  • aged over 65-68 years;
  • with bradycardia;
  • with arterial hypotension;
  • when used together with oral contraceptives.

The drug "Tizalud" (tablets): instructions for use

Reviews from doctors report that this medication should be taken only after an individual consultation with a specialist.

Tizalud tablets are taken orally with plain water, regardless of the meal.

The dosage of this medicine depends on the type and course of the disease. According to the instructions, for neurological pathologies that cause painful (spastic) contraction of muscle tissue, treatment is recommended to begin with a daily dose of 6 mg, which is divided into three doses. Depending on the nature of the spasm and pain, this amount of the drug can be increased by 2-4 mg over the next 3-7 days.

As medical practice shows, the maximum therapeutic effect is observed when taking a daily dose of 12-24 mg. In this case, 36 mg is the maximum permissible daily dosage.

To relieve painful spasms of skeletal muscles, Tizalud tablets, reviews of which are controversial, are prescribed 2-4 mg three times a day. In especially severe cases, doctors recommend additional medication at night in the same amount (that is, 2-4 mg).

The duration of use of the drug "Tizalud" depends on the dynamics of muscle-tonic and pain manifestations. As a rule, acute muscle pain requires careful treatment for 8-20 days. For chronic pain syndrome, depending on the severity and origin, the patient may need longer therapy, which is determined on an individual basis (can last for one year).

Adverse reactions

Unfortunately, taking the medication in question can cause many negative reactions from the central nervous system, digestive tract, cardiovascular and respiratory systems, and others. Some of the most common side effects include the following:

  • nausea, hepatitis, dizziness, dyspepsia;
  • drowsiness, bradycardia, hallucinations;
  • liver failure, sleep disturbances, dry mouth;
  • insomnia, increased activity of liver transaminases, muscle weakness, decreased blood pressure;
  • increased fatigue, hypercreatininemia.

It should also be noted that abrupt withdrawal of the drug "Tizalud", especially after its combination with antihypertensive drugs and long-term treatment or taking large dosages, can quite easily lead to the development of tachycardia, increased blood pressure, and in some cases to acute cerebrovascular accident .

Overdose of Tizalud tablets

With a fairly severe and regular violation of the dosage regimen, as well as when taking increased doses of the drug in question, the patient experiences the following conditions: drowsiness, nausea leading to vomiting, dizziness, development of hypotension, anxiety, miosis, coma, respiratory failure.

With such symptoms, the patient requires immediate gastric lavage, as well as bowel cleansing with an enema. In addition, the victim is advised to take sorbents, diuresis (forced) and further symptomatic therapy.

Interaction with other medications

According to the instructions, Tizalud can cause withdrawal syndrome, therefore, upon completion of treatment, the dose must be reduced gradually.

Release form and composition

The drug Tizalud is produced in the form of tablets containing the active substance (tizanidine) in quantities of 2 mg and 4 mg.

Analogues of Tizalud in terms of the active substance are the medications Sirdalud, Tizanidin-Teva, Tizanil and Sirdalud MR.

If necessary, due to hypersensitivity or the presence of contraindications, the doctor may recommend the use of one of Tizalud’s analogues with a similar mechanism of action: Baklosan, Tolperisone-OBL, Mydocalm, Tolperisone and Mydocalm-Richter.

Indications for use of Tizalud

The medication Tizalud is prescribed according to the instructions for the treatment of painful muscle spasms:

  • Associated with functional and organic disorders of the spine, including osteochondrosis, cervical and lumbar syndromes, syringomyelia, spondylosis and hemiplegia;
  • Arising after surgical operations, including operations regarding the hip joint or intervertebral disc;
  • Arising due to spasticity of skeletal muscles against the background of various neurological diseases, including multiple sclerosis, chronic myelopathy, degenerative diseases of the spinal cord, residual effects of the past, traumatic brain injuries, cerebral palsy.

Contraindications

According to the instructions for Tizalud, it is contraindicated to take:

  • Against the background of hypersensitivity to the active (tizanidine) or auxiliary components included in the tablets;
  • During lactation;
  • Simultaneously with potent inhibitors of the CYP1A2 isoenzyme;
  • Against the background of severe liver failure;
  • During pregnancy;
  • In pediatrics.

You should take Tizalud tablets with extreme caution:

  • Simultaneously with oral contraceptives;
  • With arterial hypotension;
  • Against the background of liver or kidney failure;
  • With congenital long Q-T interval syndrome;
  • Against the background of bradycardia;
  • Elderly people over 65 years of age.

Directions for use and dosage

To reduce the severity of painful muscle spasms, 1-2 tablets of Tizaluda (2 mg) are usually prescribed three times a day. In case of severe illness, you can additionally take a single dose at night.

In the treatment of spasticity, which is caused by neurological diseases, Tizalud is prescribed in an initial dosage of 2 mg, which is taken 3 times a day. It is possible to gradually increase (at intervals of 3-7 days) a single dosage by 2-4 mg. The maximum daily dosage is 36 mg, divided into 3-4 times.

When prescribing Tizalud in a daily dosage of more than 12 mg, it is necessary to evaluate liver function at least once a month for four months. If the activity levels of AST and ALT during this period exceed the upper limit of normal by more than 3 times, stop taking Tizalud.

Side effects of Tizalud

According to reviews, the medication Tizalud most often causes drowsiness, decreased blood pressure, dry oral mucosa, fatigue, bradycardia, and hypercreatininemia.

In addition, according to reviews, Tizalud can lead to the development of:

  • Insomnia, hallucinations and sleep disorders (nervous system);
  • , nausea, hepatitis and liver failure (digestive system);
  • Muscle weakness (musculoskeletal system).

Abrupt withdrawal of Tizalud after long-term therapy, as well as after taking it in high doses or simultaneously with antihypertensive drugs, can cause an increase in blood pressure, and in some cases, cerebrovascular accident, which occurs in an acute form.

Also, according to reviews, Tizalud, when taken in high doses, can lead to an overdose, manifested in the form of nausea, respiratory failure, a pronounced decrease in blood pressure, dizziness, drowsiness, miosis, anxiety, coma. For treatment, in addition to gastric lavage, repeated intake of activated charcoal is indicated. Also in this case, forced diuresis is performed.

Drug interactions

According to the instructions, Tizalud is not recommended to be taken simultaneously with antihypertensive drugs due to the risk of a pronounced decrease in blood pressure and the development of bradycardia. The combined use of the drug with other alpha2-agonists is also considered undesirable.

Sedative medications and ethanol may increase side effects associated with depression of the central nervous system.

Concomitant use with oral contraceptive medications may reduce the effectiveness of Tizalud.

Storage conditions

Tizalud is one of the centrally acting muscle relaxants dispensed from pharmacies as prescribed by a doctor. The shelf life of the tablets is 24 months if the manufacturer's recommended storage conditions are observed.

Tizalud is intended to reduce spasms of skeletal muscles, reduce their resistance during movement and eliminate clonic seizures.

It is made on the basis of the active substance – tizanidine. It is used as an antispasmodic for painful muscle spasms. Tizanidine helps to increase the strength of voluntary muscle contractions and relax skeletal muscles in spastic conditions of cerebral and spinal origin.

Indications for use

Tizalud tablets are prescribed for the following neurological diseases:

  • stroke;
  • chronic myelopathy;
  • osteochondrosis;
  • cerebral paralysis;
  • cerebral circulatory disorders;
  • multiple sclerosis;
  • for the treatment of various spinal lesions;
  • for traumatic brain injuries;
  • in the postoperative periods for osteoarthritis of the hip and herniated intervertebral discs.

Contraindications

You should not take Tizaluda tablets if you have:

  • hypersensitivity to tizanidine;
  • severe liver and kidney pathologies;
  • should be taken with caution when using oral contraceptives or with arterial hypotension.

Side effects

When taking Tesalud, drowsiness, fatigue, nausea, decreased blood pressure, insomnia, dry mouth, muscle weakness, liver failure, skin rash, itching are observed. If the drug is abruptly discontinued, tachycardia and cerebrovascular accident may develop.

Analogs

Analogues by ATC code, release form and composition of active ingredients include the following drugs:

  • Tizanidine-Ratiopharm;
  • Myoflex;
  • Miaxil;
  • Baclofen.