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

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

The composition of the drug and the form of release

1 capsule of the product contains:

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

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

Pharmacological influence and pharmacokinetics

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

Also, the drug reduces resistance during passive movements, softens spasmodic reflexes and clonic seizures.

The intensity of voluntary reflexes also increases. Moreover, interaction with neuromuscular transmission missing.

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

In this case, bioavailability matters - 34%.

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

Who is the drug assigned to?

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

Indications for use of Tizaluda:

Important! During the time that manifested itself due to diseases of a neurological nature, the dose of the drug 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 active ingredients medication;
• acute abnormalities in the liver;
• joint use of Ciprofloxacin with Fluvoxamine.

More detailed information on contraindications to Tizalud is in the official instructions supplied with the drug.

Tactics and strategy of therapy

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

The mode of use and dosage is prescribed by the doctor, taking into account the individual characteristics of the patient and such moments as allergic reactions and age. The maximum 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 rate will already be 2 mg once a day.

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

Overdose cases

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

• drowsiness;
• nausea;
• anxiety;
• vomiting attacks;
• arterial hypotension;
• distress;
• bradycardia;
• miosis;
• lengthening of the QT gap;
• dizziness;
• coma.

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

Possible admission troubles

When taking the drug, the following side effects were noticed:

• serum transaminase;
• 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 spasm.

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

There are such side effects: arterial hypotension, bradycardia, muscle weakness, bad dream, bouts of hallucinations and even hepatitis.

special instructions

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

For example, managing 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 need to contact your doctor for advice.

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

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

For those with kidney dysfunction, no more than 2 mg of the drug per day can be prescribed. Further, there is a very accurate increase in the dose, at this time the patient is under the constant supervision of a doctor. Initially, the amount of the drug taken per day rises, only then the number of doses.

Interaction with other drugs

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

It is also necessary with extreme caution to take the drug with such drugs, due to which the QT interval increases. And the combined use of tizanidine with alcohol will increase its effect on the body.

Reception during pregnancy and lactation

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

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

It is known that the active ingredient tizanidine in small quantities enters the mother's milk. That is why, for women who feed a baby with their milk, medicine is also not prescribed.

There is still no information about the effect of the drug on children and adolescents. Therefore, the medicine is not prescribed to them.

From the practice of patients

Tizalud tablets have found their admirers among patients, which is confirmed by numerous reviews on the network.

The drug began to be taken after cramps in the feet began to disturb. There were no prerequisites for this, no injuries or anything like that, probably just age.

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

Oksana Dmitrievna 62 years old, Irkutsk

It was, as a result, the artery was interrupted and the blood supply in the brain was disrupted, there were a lot of negative symptoms, a sheer nightmare.

The district hospital prescribed a number of medications for healing and restoration of function circulatory system and the brain, but after long-term use, I did not see any positive sensations, except for side effects. Now I'm trying this drug. I will definitely write about the results.

Ivan 44 years old, Tver

My husband and I got into a car accident as a result of a head injury. For six months I just felt sick every day, I could neither work nor sleep normally.

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

Alisa 19 years old, Syktyvkar

Storage conditions and periods

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

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

What is the drug "Tizalud"? Instructions for use, reviews and features of this medication will be discussed below. You will also find out if the tool in question has side effects and prohibitions to use.

Form, packaging of medication, composition

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

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

Tablets "Tizalud", reviews of which are presented below, are packed in contour cells that are placed in cardboard boxes.

Oral pharmacology

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

What changes occur in the human body after taking the medication in question? The impact of it active ingredient on alpha2-adrenergic receptors (presynaptic) contributes to the inhibition of the process of release of excitatory amino acids from intermediate spinal neurons, which ultimately leads to a delayed polysynaptic propagation of an impulse in spinal cord... Thanks to this mechanism of action, the tone of the patient's muscle tissue is significantly reduced.

Features of the drug

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 seizures, as a result of which the resistance to passive movements decreases, and the likelihood of active actions increases.

Indications for taking medication

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

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

Are there other indications for the medicine "Tizalud"? Experts say that this remedy is actively used in the postoperative time after intervention for intervertebral hernias and osteoarthritis of the hip joint. Also, the tablets in question help well with pain syndrome and muscle spasticity triggered by neurological diseases, including chronic myelopathy, cerebral paralysis, degenerative changes in the spinal cord, seizures of central origin, cerebrovascular accident, multiple sclerosis, stroke, trauma to the skull and brain.

Prohibitions on the use of oral medication

What contraindications should patients know about before taking Tizalud tablets? Instructions, reviews report that there are not very many prohibitions on the use of this medication. These include only the following conditions:

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

Cautious prescribing of the drug

With caution, the medication in question should be prescribed in the following cases:

• with renal failure;
• over the age of 65-68;
• with bradycardia;
• with arterial hypotension;
• at joint application with oral contraceptives.

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

The doctors' comments indicate that this medication should be taken only after individual consultation with a specialist.

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

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

As medical practice shows, the maximum therapeutic effect noted when taking a daily dose of 12-24 mg. At the same time, 36 mg is the maximum allowable daily dosage.

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

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

Side 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. Among the most common side effects the following can be distinguished:

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

It should also be noted that the abrupt withdrawal of the drug "Tizalud", especially after its combination with antihypertensive drugs and prolonged 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 with Tizalud tablets

With a rather gross and regular violation of the dosage regimen, as well as when taking high doses of the drug in question, the patient experiences the following conditions: drowsiness, nausea, turning into vomiting, dizziness, hypotension, anxiety, miosis, coma, respiratory failure.

With such symptoms, the patient requires immediate gastric lavage, as well as cleansing the intestines with an enema. In addition, the victim is shown the intake of sorbents, diuresis (forced) and further symptomatic therapy.

Interaction with other medicines

Tizalud, according to the instructions, can cause a "withdrawal" syndrome, therefore, at the end of treatment, the dose must be reduced gradually.

Release form and composition

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

The medicines Sirdalud, Tizanidin-Teva, Tizanil and Sirdalud MR are analogs of Tizalud in terms of the active substance.

If necessary, due to hypersensitivity or the presence of contraindications, the doctor may recommend the use of one of the analogs of Tizaluda with a similar mechanism of action: Baklosan, Tolperisone-OBL, Midocalm, Tolperisone and Midocalm-Richter.

Indications for use of Tizaluda

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 surgery, including surgery for the hip joint or intervertebral disc;
• Arising from the 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 transferred, traumatic brain injury, cerebral palsy.

Contraindications

According to the instructions, Tizalud is contraindicated to take:

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

Tizalud tablets should be taken with extreme caution:

• Concurrently with oral contraceptives;
• With arterial hypotension;
• Against the background of hepatic or renal failure;
• With congenital lengthening of the Q-T interval;
• Against the background of bradycardia;
• Seniors over 65.

Method of administration and dosage

To reduce the severity of painful muscle spasm, 1-2 tablets of Tizaluda (2 mg each) are usually prescribed three times a day. When severe course diseases, you can additionally take a single dosage 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. A gradual increase (at intervals of 3-7 days) of a single dosage by 2-4 mg is possible. The maximum daily dosage is 36 mg, divided by 3-4 times.

When prescribing Tizaluda in a daily dosage of more than 12 mg, it is necessary to assess liver function at least once a month for four months. If the activity indicators of AST and ALT during this period exceed the upper limit of the norm by more than 3 times, Tizaluda is discontinued.

Side effects of Tizaluda

According to reviews, the medication Tizalud most often causes drowsiness, a decrease blood pressure, dryness of the oral mucosa, fatigue, bradycardia, 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 Tizaluda after prolonged therapy, as well as after taking it in high doses or simultaneously with antihypertensive drugs, can cause an increase in blood pressure, in some cases - cerebrovascular accident, proceeding in an acute form.

Also, Tizalud, according to reviews, 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 carbon is indicated. Also in this case, forced diuresis is performed.

Drug interactions

Tizalud, according to the instructions, is not recommended to be taken simultaneously with antihypertensive drugs because of the risk of a pronounced decrease in blood pressure and the development of bradycardia. It is also considered undesirable to use the medication together with other alpha2-adrenostimulants.

Sedatives and ethanol can increase the side effects associated with central depression. nervous system.

Concomitant use with oral contraceptive medications can lead to a decrease in the effectiveness of Tizalud.

Storage conditions

Tizalud is one of the muscle relaxants central action dispensed from pharmacies as prescribed by a doctor. The shelf life of the tablets is 24 months, subject to the manufacturer's recommended storage conditions.

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

It is made on the basis of the active ingredient - tizanidine. It is used as an antispasmodic for painful muscle spasms. Tizanidine helps to increase the strength of voluntary muscle contractions, relaxation of 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;
• circulatory disorders of the brain;
• multiple sclerosis;
• for the treatment of various lesions of the spine;
• with craniocerebral trauma;
• v postoperative periods with osteoarthritis of the hip and herniated intervertebral discs.

Contraindications

Do not take Tizaluda tablets if you have:

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

Side effects

When taking Tezaluda, drowsiness, fatigue, nausea, decreased blood pressure, insomnia, dry mouth, muscle weakness, liver failure, skin rash, itching are observed. With a sharp withdrawal of the drug, tachycardia, cerebrovascular accident may develop.

Analogs

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

• Tizanidine-Ratiopharm;
• Mioflex;
• Miaxil;
• Baclofen

What is the drug "Tizalud"? Instructions for use, reviews and features of this medication will be discussed below. You will also learn about whether the agent in question has side effects and prohibitions to use.

Form, packaging of medication, composition

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

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

Tablets "Tizalud", reviews of which are presented below, are packed in contour cells that are placed in cardboard boxes.

Oral pharmacology

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

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

Features of the drug

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 seizures, as a result of which the resistance to passive movements decreases, and the likelihood of active actions increases.

Indications for taking medication

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

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

Are there other indications for the medicine "Tizalud"? Experts say that this remedy is actively used in the postoperative time after intervention for intervertebral hernias and osteoarthritis of the femoral joint. Also, the considered tablets help well with pain and muscle spasticity provoked by neurological diseases, including chronic myelopathy, cerebral palsy, degenerative changes in the spinal cord, seizures of central origin, cerebrovascular accidents, multiple sclerosis, stroke, trauma to the skull and brain.

Prohibitions on the use of oral medication

What contraindications should patients know about before taking Tizalud tablets? Instructions, reviews report that there are not very many prohibitions on the use of this medication. These include only the following conditions:

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

Cautious prescribing of the drug

With caution, the medication in question should be prescribed in the following cases:

• with renal failure;
• over the age of 65-68;
• with bradycardia;
• with arterial hypotension;
• when used together with oral contraceptives.

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

The doctors' comments indicate that this medication should be taken only after individual consultation with a specialist.

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

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

As medical practice shows, the maximum therapeutic effect is observed when taking a daily dose of 12-24 mg. At the same time, 36 mg is the maximum allowable daily dosage.

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

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

Side 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. Among the most common side effects are the following:

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

It should also be noted that the abrupt withdrawal of the drug "Tizalud", especially after its combination with antihypertensive drugs and prolonged 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 with Tizalud tablets

With a rather gross and regular violation of the dosage regimen, as well as when taking high doses of the drug in question, the patient experiences the following conditions: drowsiness, nausea, turning into vomiting, dizziness, hypotension, anxiety, miosis, coma, respiratory failure.

With such symptoms, the patient requires immediate gastric lavage, as well as cleansing the intestines with an enema. In addition, the victim is shown the intake of sorbents, diuresis (forced) and further symptomatic therapy.

Interaction with other medicines

With which medicines is it forbidden to take the drug "Tizalud"? Parallel use of this medication with "Fluvoxamine", "Ciprofloxacin" and other potent inhibitors of the isoenzyme CYP1A2 (including "Amiodarone", "Mexiletin", "Propafenone", "Cimetidine", "Norfloxacin", "Enoxacin", "Pefloxacin "," Rofecoxib "and oral contraceptives) not allowed.

Antihypertensive drugs significantly increase the risk of lowering the patient's blood pressure and the development of bradycardia.

Ethanol and sedatives can enhance the hypnotic effects of tizanidine.

Specific information

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

Because of the threat of withdrawal from treatment, the dose of tizanidine should be reduced gradually if treatment is abandoned.

It is better to refuse Tizalud tablets if professional activity the patient is associated with driving vehicles and carrying out hazardous 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 by such means as "Tolperil", "Liorezal", "Midocalm", "Baklosan", "Tolperison" and others.

Composition and release form of the drug

Tablets color, white or white with a yellowish tinge, round, biconvex, with a line.

Excipients: anhydrous lactose (lactopress), microcrystalline cellulose, sodium carboxymethyl starch (primogel), magnesium stearate.

10 pieces. - contour cell packaging (3) - cardboard packs.

pharmachologic effect

Central action. Reduces the increased tone of skeletal muscles, relieves their spasm; reduces muscle resistance during passive movements, increases the strength of voluntary contractions. The muscle relaxant effect of tizanidine is probably due to inhibition of spinal polysynaptic reflexes, which is associated with a decrease in the release of excitatory amino acids from the presynaptic terminals of spinal interneurons, as well as stimulation of α 2 -adrenoreceptors. Tizanidine does not affect the transmission of excitation in neuromuscular synapses.

Indications

Spastic condition of skeletal muscles caused by neurological diseases (chronic myelopathy, stroke, degenerative diseases of the spinal cord). Painful spasm of skeletal muscles caused by damage to the spine (cervical and lumbar syndromes) or arising after surgery (for intervertebral disc or hip osteoarthritis).

Contraindications

Hypersensitivity to tizanidine.

Dosage

To stop painful skeletal muscle spasm, use 2-4 mg 3 times / day; in severe cases, it is additionally recommended to take 2-4 mg at night. For spastic muscle conditions caused by neurological diseases, the initial dose is 6 mg / day in 3 divided doses. The dose is gradually increased by 2-4 mg / day every 3-7 days. The optimal therapeutic effect is usually achieved at a dose of 12-24 mg / day, divided into 3-4 doses. Do not exceed a dose of 36 mg / day.

Side effects

When using tizanidine in relatively small doses on rare occasions drowsiness, a feeling of fatigue, dry mouth, nausea, a slight decrease in blood pressure are observed; in higher doses- these effects occur more often and are more pronounced, in addition, muscle weakness, bradycardia, an increase in serum transaminase activity are possible.

Drug interactions

With simultaneous use with antihypertensive drugs (including with diuretics), severe arterial hypotension and bradycardia may develop.

Description

Tablets round shape with a flat surface with beveled edges and a line, white or almost white.

Compound

1 tablet contains tizanidine 2 mg or 4 mg;

Excipients: microcrystalline cellulose, anhydrous lactose, anhydrous colloidal silicon dioxide, stearic acid.

Release form

Tablets.

Pharmacotherapeutic group

Muscle relaxants of central action.

Pharmacological properties

Pharmacodynamics. Tizanidine is a centrally acting skeletal muscle relaxant. Its main site of action is the spinal cord. By stimulating presynaptic α2-adrenergic receptors, it inhibits the release of amino acids that stimulate N-methyl-D-aspartate receptors (NMDA receptors). As a result, polysynaptic signal transmission at the level of interneuronal connections in the spinal cord, which is responsible for excessive muscle tone, is inhibited, and muscle tone decreases. Tizalud is effective both for acute painful muscle spasms and for chronic spasticity of spinal and cerebral origin. It reduces resistance to passive movements, inhibits spasm and clonic convulsions, and improves the strength of active muscle contractions.

Pharmacokinetics.

Absorption and distribution. Tizanidine is rapidly absorbed. Maximum plasma concentrations are reached approximately 1 hour after application. The average absolute bioavailability is 34%. Mean volume of distribution at steady state (Vss) after intravenous use is 2.6 l / kg. Plasma protein binding is 30%. The relatively low deviation of pharmacokinetic parameters (Cmax and AUC) among patients facilitates a reliable preliminary assessment of blood plasma levels after oral administration.

Metabolism / excretion. The drug undergoes rapid and extensive metabolism in the liver. Tizanidine is metabolized primarily by CYP1A2. The metabolites are inactive. They are excreted mainly by the kidneys (70%). The elimination of the total radioactivity (i.e., the substance in unchanged form and metabolites) is biphasic, with a fast initial phase (half-life T1 / 2 = 2.5 hours) and a slower elimination phase (T1 / 2 = 22 hours). Only a small amount of the substance in unchanged form (about 2.7%) is excreted by the kidneys. The average elimination half-life of the substance in unchanged form is 2–4 hours.

Pharmacokineticsin certain groups of patients. In patients with renal failure(creatinine clearance less than 25 ml / min) the mean maximum plasma concentration is 2 times higher than that in healthy volunteers, and the final half-life is extended to approximately 14 hours, as a result of which the area under the concentration-time curve (AUC) increases in 6 times on average.

No studies have been performed in patients with impaired liver function.

Tizanidine is metabolized by the CYP1A2 isoenzyme in the liver. In patients with impaired liver function, higher plasma concentrations of the substance may appear. Tizalud is contraindicated in patients with severely impaired liver function.

Pharmacokinetic data on elderly patients are limited.

Gender does not affect the pharmacokinetic properties of tizanidine.

The effect of ethnicity and race on the pharmacinetics of tizanidine has not been studied.

The influence of food. Concomitant food intake does not affect the pharmacokinetic profile of Tizalud tablets. Although the maximum concentration value increases by one third, this is not clinically significant. There was no significant effect on absorption.

Indicationsto use

Painful muscle spasm. Spasticity due to multiple sclerosis. Spasticity due to spinal cord injury. Spasticity due to brain damage.

Contraindications

Hypersensitivity to tizanidine or to any excipients of the drug. Severe liver dysfunction. Concomitant use of tizanidine with potent inhibitors of CYP1A2, such as fluvoxamine or ciprofloxacin.

Drug interactions

Concomitant use of known CYP1A2 inhibitors can increase plasma levels of tizanidine. An increase in the level of tizanidine in blood plasma can lead to the appearance of overdose symptoms such as prolongation of the QT interval.

The simultaneous use of known inducers of CYP1A2 can reduce the level of tizanidine in the blood plasma. A decrease in the level of tizanidine in blood plasma may lead to a decrease in the therapeutic effect of Tizalud.

Concomitant use of potent CYP1A2 inhibitors such as fluvoxamine or ciprofloxacin with tizanidine is contraindicated. The simultaneous use of tizanidine with fluvoxamine increases the AUC of tizanidine by 33 times, while the simultaneous use of tizanidine with ciprofloxacin increases the AUC of tizanidine by 10 times. This can lead to a clinically significant and long-term decrease in blood pressure, accompanied by drowsiness, dizziness, and decreased psychomotor productivity.

Simultaneous use of tizanidine with other inhibitors of CYP1A2, such as antiarrhythmic drugs (amiodarone, mexiletine, propafenone). cimetidine, some fluoroquinolones (enoxacin, pefloxacin, norfloxacin), rofecoxib, oral contraceptives, and ticlopyridine are not recommended.

The simultaneous use of the drug Tizalud with antihypertensive drugs, including diuretics, can sometimes cause arterial hypotension and bradycardia. Some patients receiving concomitant treatment with antihypertensive drugs experienced rebound arterial hypertension and rebound tachycardia with sudden withdrawal of tizanidine. In some cases, rebound arterial hypertension can cause a stroke.

The simultaneous use of the drug Tizalud with rifampicin can lead to a 50% decrease in the concentration of tizanidine. Thus, the therapeutic effect can be reduced with the use of rifampicin during therapy with the drug Tizalud, which may be clinically beneficial for some patients. Long-term simultaneous use should be avoided, and if necessary, the dosage should be adjusted very carefully.

The use of the drug Tizalud leads to a 30% decrease in the systemic effect of tizanidine in smoking men (more than 10 cigarettes per day). Long-term use the drug for men who smoke a lot requires the appointment of higher doses of the drug.

The simultaneous use of the drug Tizalud and other drugs of central action (for example, sedatives and hypnotics(benzodiazepine or baclofen), some antihistamines and analgesics, psychotropic drugs, narcotic drugs) can enhance the effects of each drug and enhance the hypnotic effect of Tizaluda. This applies, in particular, to the simultaneous use of alcohol, which can unpredictably change or enhance the effect of Tizaloud and increase the risk of adverse reactions, therefore, you should refrain from drinking alcohol.

The administration of the drug Tizalud together with a2-adrenergic agonists (for example, with clonidine) should be avoided due to their potential additive hypotensive effect.

If you are taking any other medicines, consult your doctor about the possibility of using the medicine.

Precautionary measures

The concomitant use of CYP1A2 inhibitors with tizanidine is not recommended.

After sudden drug withdrawal or rapid decline dose in patients, arterial hypertension and tachycardia may occur. In some cases, such rebound arterial hypertension can cause a stroke. Treatment with tizanidine should not be discontinued abruptly, but only by gradually reducing the dose.

For patients with renal impairment (creatinine clearance

Liver failure associated with the use of tizanidine has been reported, but this has rarely been observed in patients receiving daily doses up to 12 mg. In this regard, it is recommended to monitor liver function once a month during the first 4 months of therapy in those patients who are using tizanidine at a dose of 12 mg or more and in patients with clinical symptoms indicating liver failure (eg, nausea, loss of appetite, or increased fatigue of unknown etiology). The use of the drug Tizalud should be discontinued if the levels of ALT or ACT in serum exceed the upper limit of the norm by 3 times or more for a long period.

Arterial hypotension can occur during the use of tizanidine, as well as as a result drug interactions with CYP1A2 inhibitors and / or antihypertensive drugs. Severe forms of arterial hypotension such as loss of consciousness and circulatory collapse have been reported.

Caution should be exercised when using this drug with drugs that prolong the QT interval (eg, cisapride, amitriptyline, azithromycin).

Caution is needed for patients with ischemic disease heart and / or heart failure. ECG monitoring should be carried out at regular intervals at the beginning of the use of the drug Tizalud in such patients.

Patients with myasthenia gravis need to carefully assess the risk-benefit ratio before using this drug.

The experience of using children and adolescents is limited, therefore, the use of the drug Tizalud is not recommended for this category of patients.

Caution should be exercised when using this drug in elderly patients.

Tizalud tablets contain lactose. Tizalud tablets are not recommended for patients with rare hereditary diseases - galactose intolerance, severe lactase deficiency or glucose-galactose malabsorption syndrome.

Application in the periodbeing pregnant or breastfeeding

Pregnancy.

Data on the use of the drug Tizalud in pregnant women are limited, so it should not be prescribed during pregnancy, unless the potential benefit to the mother outweighs possible risk for the fetus.

Lactation.

It was found that tizanidine penetrates in small amounts into breast milk... Therefore, women who are breastfeeding should not be prescribed the drug.

Fertility

The available data indicate that tizanidine, which was used at a dose of 10 mg / kg per day in male rats and at a dose of 3 mg / kg per day in female rats, did not cause impairment of fertility. A decrease in fertility was observed in male rats that received tizanidine at a dose of 30 mg / kg per day and in female rats that received tizanidine at a dose of 10 mg / kg per day. Sedation, weight loss, and ataxia have also been observed with these doses.

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Tizanidine can cause drowsiness, dizziness and / or arterial hypotension, thus impairing the patient's ability to drive or operate machinery. The risks are increased with the simultaneous use of alcohol.

Therefore, one should refrain from activities requiring high concentration attention and quick reaction, for example from driving vehicles or working with machines and mechanisms.

Children.

The experience of using the drug in pediatrics is limited. It is not recommended to prescribe Tizalud to children.

Method of administration and dosage

Tizalud has a narrow therapeutic range and high variability in plasma tizanidine concentration in different patients. Therefore, it is important to use optimal doses according to the patient's needs. Treatment should be started with a low dose of 2 mg, which minimizes the risk of adverse effects from taking the drug. If necessary, the dose of the drug should be gradually increased with all necessary precautions.

Adults

Relief of Painful Muscle Spasms

Apply 2-4 mg 3 times a day. In severe cases, an additional dose of 2 or 4 mg may be taken before bedtime.

Spasticitywith neurological disorders

The dose must be selected individually for each patient.

The initial daily dose should not exceed 6 mg, divided into 3 doses. It can be increased to 2-4 mg 2 times gradually at intervals of 3-7 days. As a rule, the optimal therapeutic effect is achieved with a daily dose of 12-24 mg, divided into 3 or 4 doses. Do not exceed the total daily dose 36 mg.

Special patient groups

Application for children and adolescents

The experience of using the drug Tizalud for children and adolescents is limited, therefore the drug is not recommended for use in children and adolescents.

Elderly patients

The experience of using the drug in elderly patients is limited, therefore, caution should be exercised when using the drug Tizalud in this category of patients. It is recommended to start treatment with the lowest dose and gradually increase it with caution in "small steps" until the optimal balance of individual tolerance and therapeutic efficacy of the drug is achieved.

Use in patients with impaired renal function

For patients with impaired renal function (CC

Use in patients with impaired liver function

Treatment of patients with severe liver dysfunction is contraindicated. Tizalud is extensively metabolized in the liver. The drug should be used with caution in the treatment of patients with moderately severe liver dysfunction. Treatment should be started with the lowest dosage; if necessary, increasing the dose should be carried out with caution and taking into account the patient's individual tolerance of the drug Tizalud.

Interrupt treatment

If necessary, interruption of drug treatment, the dose should be reduced slowly and gradually. This is especially true for patients who have received an increased dose of the drug for a long time. Thus, the risk of developing a rebound increase in blood pressure and tachycardia is reduced. elevated levels serum transaminases), as a rule, are mild and transient in patients using the low doses recommended for the relief of painful muscle spasm.

At doses higher than those recommended for the treatment of spasticity, the aforementioned adverse reactions are more frequent and more severe, but they are rarely severe enough to warrant discontinuation of treatment. Also, such side reactions may occur: arterial hypotension, bradycardia, muscle weakness, sleep disturbances, hallucinations and hepatitis.

The appearance of such symptoms has been reported after the sudden withdrawal of tizanidine, in particular after long-term treatment and / or high daily doses and / or concomitant therapy with antihypertensive drugs. Under these circumstances, patients may experience hypertension and tachycardia. In some cases, such rebound arterial hypertension can cause a stroke.

Therefore, treatment with tizanidine should not be stopped abruptly, but only by gradually reducing the dose.

From the side of the psyche: insomnia, sleep disturbance; hallucinations.

From the side of the central nervous system: drowsiness, dizziness; confusion of consciousness, vertigo.

From the sidecardiovascularsystems: arterial hypotension; bradycardia; syncope.

From the gastrointestinal tract: dry mouth, pain in gastrointestinal tract, gastrointestinal disorders; nausea.

From the sidehepatobiliarysystems: elevated serum transaminase levels; acute hepatitis, liver failure.

From the musculoskeletal system: muscle weakness.

General violations: increased fatigue; asthenia, withdrawal syndrome, hypersensitivity reactions.

On the part of the organs of vision: blurred vision.

Research: lowering blood pressure, increasing the level of transaminases.

Package

10 tablets in a blister; 3 blisters in a pack.

Manufacturer information

PJSC "Kiev Vitamin Factory".

04073, Ukraine, Kiev, st. Kopylovskaya, 38.