Sirdalud tablets 4mg, No. 30

Painful muscle spasm:

- associated with static and functional diseases of the spine (cervical and lumbar syndromes);

- 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 myelopathy, degenerative diseases of the spinal cord, the consequences of cerebrovascular accidents and cerebral palsy (patients over 18 years of age).

Inside. The dosage regimen should be selected individually.

SirdaludЃ has a narrow therapeutic index and high variability in the concentration of tizanidine in the blood plasma of patients, therefore, a careful selection of the dose is required.

An initial dose of 2 mg 3 times a day can minimize the risk of adverse reactions. The dose should be carefully selected taking into account the individual needs of the patient.

For painful muscle spasm, SirdaludЃ is usually prescribed at a dose of 2 or 4 mg 3 times a day. In severe cases, an additional 2 or 4 mg can be taken (preferably at bedtime due to possible increased drowsiness).

2 and 4 mg tablets can be divided into 2 equal portions.

For skeletal muscle spasticity due to neurological diseases, the initial daily dose should not exceed 6 mg, divided into 3 doses. The dose can be increased gradually, by 2-4 mg, at intervals of 3-4 to 7 days. Usually, the optimal therapeutic effect is achieved with a daily dose of 12 to 24 mg, divided into 3 or 4 doses at regular intervals. Do not exceed a dose of 36 mg / day.

Interruption of treatment. When discontinuing therapy with SirdaludЃ in order to reduce the risk of developing rebound hypertension and tachycardia, the dose should be slowly reduced until the drug is completely discontinued, especially in patients receiving high doses of the drug for a long time.

Special patient groups

Patients over 65 years of age. The experience of using the drug SirdaludЃ in patients aged 65 years and older is limited. It is recommended to start therapy with a minimum dose with a gradual increase until the optimal balance of tolerance and effectiveness of therapy is achieved.

Renal dysfunction. Treatment of patients with renal insufficiency (Cl creatinine? 25 ml / min) is recommended to start with a dose of 2 mg 1 time per day. The dose is increased in small steps, taking into account the tolerance and effectiveness. If it is necessary to obtain a more pronounced effect, it is recommended to first increase the dose prescribed once a day, after which the frequency of administration is increased.

Liver dysfunction. The use of the drug SirdaludЃ in patients with severely impaired liver function is contraindicated. In patients with moderately severe liver dysfunction, the drug should be used with caution; it is recommended to start therapy with a minimum dose, with a gradual increase until the optimal balance of tolerance and effectiveness of therapy is achieved.

Tablets from white to almost white, round, flat, with beveled edges, on one side intersecting marks, on the other - the code 'RL'.

1 tab. tizanidine hydrochloride 4.576 mg,

which corresponds to the content of tizanidine base 4 mg

Excipients: colloidal silicon dioxide - 0.4 mg, stearic acid - 4 mg, microcrystalline cellulose - 101.024 mg, lactose - 110 mg.

- Hypersensitivity to tizanidine or any other component of the drug;

-severe liver dysfunction;

- simultaneous use with strong inhibitors of cytochrome P450 1A2 (CYP1A2), such as fluvoxamine or ciprofloxacin.

Experience with the drug in patients under 18 years of age is limited. The use of SirdaludЃ in this population is not recommended.

With caution: age over 65 years, renal dysfunction, moderate liver dysfunction.

pharmachologic effect

Muscle relaxant of central action. The main point of application of its action is in the spinal cord. By stimulating presynaptic ?2-adrenergic receptors, it inhibits the release of excitatory amino acids that stimulate N-methyl-D-aspartate receptors (NMDA receptors). As a result, polysynaptic transmission of excitation is suppressed at the level of intermediate neurons of the spinal cord. Since it is this mechanism that is responsible for excess muscle tone, then when it is suppressed, muscle tone decreases. In addition to muscle relaxant properties, tizanidine also has a central, moderate analgesic effect.

Tizanidine is effective for chronic spasticity 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

After oral administration, tizanidine is rapidly and almost completely absorbed from the gastrointestinal tract. Bioavailability is about 34%. Plasma protein binding - 30%.

Tizanidine is rapidly and largely (about 95%) metabolized in the liver. In vitro, tizanidine is metabolized mainly by the CYP1A2 isoenzyme of the cytochrome P450 system. The metabolites are inactive.

T1 / 2 averages 2-4 hours. It is excreted by the kidneys (approximately 70% of the dose) in the form of metabolites, unchanged - about 4.5%.

Side effect

From the nervous system: very often - drowsiness, dizziness.

From the side of the psyche: often - insomnia, sleep disturbances; frequency unknown - hallucinations, confusion ..

On the part of the cardiovascular system: often - a decrease in blood pressure (in some cases, pronounced, up to vascular collapse and loss of consciousness); infrequently - bradycardia.

From the digestive system: very often - dyspeptic symptoms, dry mouth; often nausea.

From the liver and biliary tract: the frequency is unknown - hepatitis, liver failure.

From the musculoskeletal system: very often - muscle weakness.

On the part of laboratory parameters: often - an increase in the activity of hepatic transaminases.

From the immune system: hypersensitivity reactions (including anaphylactic reactions, angioedema, urticaria).

On the part of the skin and subcutaneous tissues: the frequency is unknown - skin rash, erythema, pruritus, dermatitis.

Others: very often - increased fatigue; frequency unknown - asthenia, withdrawal syndrome, blurred vision.

Application during pregnancy and lactation

During pregnancy, it should be used only after consulting a doctor, in cases where the intended benefit to the mother outweighs the potential risk to the fetus or infant.

Contraindicated for use during lactation (breastfeeding).

Application for violations of liver function

Use in patients with severe liver dysfunction is contraindicated. Use with caution in patients with moderate liver dysfunction. It is recommended to start therapy with a minimum dose, with a gradual increase until the optimal balance of tolerance and effectiveness of therapy is achieved.

Application for impaired renal function

Use with caution in patients with impaired renal function. It is recommended to start therapy with a minimum dose, with a gradual increase until the optimal balance of tolerance and effectiveness of therapy is achieved.

Application in children

Contraindicated for use in children and adolescents under the age of 18 years.

Use in elderly patients

Use with caution in patients over 65 years of age. It is recommended to start therapy with a minimum dose, with a gradual increase until the optimal balance of tolerance and effectiveness of therapy is achieved.

special instructions

When discontinuing therapy with tizanidine, in order to reduce the risk of developing rebound arterial hypertension and tachycardia, its dose should be slowly reduced until it is completely canceled in patients receiving high doses of tizanidine for a long time.

With a sharp withdrawal of tizanidine after prolonged treatment and / or taking in high doses, as well as after simultaneous use with antihypertensive drugs, the development of tachycardia and an increase in blood pressure was noted, which in some cases can lead to acute cerebrovascular accident, therefore, the dose of tizanidine should be gradually reduced to complete cancellation.

When using tizanidine, it is recommended to monitor liver function tests 1 time / month in the first 4 months of treatment in patients receiving tizanidine in a daily dose of 12 mg or more, as well as in cases where there are clinical signs suggesting liver dysfunction (such as unexplained nausea, anorexia, feeling tired). In cases where the activity of ALT and ACT in serum persistently exceeds VGN by 3 times or more, the use of tizanidine should be discontinued.

During the use of tizanidine and within 1 day after the termination of its administration, patients with preserved reproductive potential should use reliable methods of contraception.

Influence on the ability to drive vehicles and mechanisms

During the period of tizanidine use, patients should be careful when driving vehicles and mechanisms, as well as when engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

With the simultaneous use of tizanidine with inhibitors of the isoenzyme CYP1A2, an increase in the concentration of tizanidine in the blood plasma is possible, which, in turn, can lead to symptoms of an overdose, incl. to prolongation of the QT interval (c).

With the simultaneous use of tizanidine with inducers of the isoenzyme CYP1A2, it is possible to reduce the concentration of tizanidine in the blood plasma, which may lead to a decrease in its therapeutic effect.

When tizanidine is used concomitantly with fluvoxamine or ciprofloxacin, a 33-fold and 10-fold increase in the AUC of tizanidine is observed, respectively. The result of simultaneous use may be clinically significant and prolonged arterial hypotension, accompanied by drowsiness, dizziness, a decrease in the speed of psychomotor reactions (in some cases, up to collapse and loss of consciousness).

With the simultaneous use of tizanidine with antihypertensive drugs, including diuretics, a decrease in blood pressure (in some cases up to vascular collapse and loss of consciousness) and bradycardia are possible.

When used simultaneously with tizanidine, sedatives, hypnotics (benzodiazepine, baclofen), blockers of histamine H1 receptors can enhance the sedative effect of tizanidine.

The simultaneous use of tizanidine and rifampicin leads to a 50% decrease in the concentration of tizanidine in the blood plasma.

With the simultaneous use of ethanol, drugs with a sedative effect, the sedative effect of tizanidine is enhanced.

The systemic bioavailability of tizanidine in smoking patients (more than 10 cigarettes per day) is reduced by about 30%.