Sirdalud (active substance - tizanidine) is a central muscle relaxant with a point of application of the action in the alpha receptors of the spinal cord.
As a result of the effect on the receptors, there is a decrease in the production of amino acids stimulating the transfer of a nerve impulse, it is due to this that the final action of the drug occurs - blocking at the level of intermediate neurons of the exciting momentum. There is an easy analgesic effect.
The active substance is absorbed quickly and almost completely when taken orally. The maximum concentration of tizanidine in plasma is noted one hour after taking the drug.
Clinical and pharmacological group
Miorelaxant of central action.
Terms of sale from pharmacies
It is possible to buy under the prescription of the doctor.
Price
How much is Sirdalud in pharmacies? The average price is at the level of250 rubles.
.Composition and form of release
Medicinal form of Sirdaluda - tablets: from almost white to white, round, flat, with bevelled edges of the form, 2 mg - on one side the code "OZ" and squashed risk; for 4 mg - on one side the code "RL on the other crossing risks (in blisters for 10 pcs., 3 blisters per carton pack).
Composition of 1 tablet:
- active substance: tizanidine - 2 or 4 mg (in the form of tizanidine hydrochloride, 88 or, 76 mg);
- additional components: anhydrous colloidal silicon dioxide /, mg, microcrystalline cellulose - 7, 12/10, 24 mg, stearic acid - 3/4 mg, lactose monohydrate - 80/110 mg.
pharmachologic effect
Sirdalud refers to muscle relaxants of central action. It affects certain parts of the spinal cord by stimulating presynaptic alpha2 receptors, which leads to inhibition of excitatory amino acids that activate receptors for N-methyl-D-aspartate (NMDA receptors). This causes oppression of the polysynaptic transmission of excitation at the level of intermediate neurons localized in the spinal cord. Since excessive muscle tone is provoked precisely by this mechanism, when it is suppressed, there is a decrease in muscle tone. In addition to muscle relaxant properties, tizanidine is also characterized by a central analgesic effect of moderate severity.
Sirdalud has been shown to be effective in both chronic spasms of cerebral and spinal genesis, and in muscle spasm accompanied by acute pain sensations. The drug reduces the risk of developing clonic seizures and reduces spasticity, which causes a decrease in resistance to passive movements and an increase in the volume of active movements. The miorelaxing effect, measured by the "pendulum" test and the Ashworth scale, and side effects (decrease in blood pressure and heart rate) are determined by the content of tizanidine in plasma blood.
Indications for use
The instructions for the use of the medicinal product indicate the following indications for its use:
- cervical and lumbar syndromes;
- Muscle painful spasms caused by diseases of the spine;
- pain after surgical interventions, neurological pathologies, herniated intervertebral disc, osteoarthritis, treatment of osteochondrosis;
- spasticity of skeletal muscles in neuralgia, multiple sclerosis, chronic myelopathy, childhood Cerebral palsy, degenerative diseases of the spinal cord, the consequences of brain damage blood circulation.
Contraindications
Absolute:
- age under 18 years (safety and efficacy for this group of patients not studied);
- lactation period (safety and efficacy for this group of patients not studied);
- individual intolerance to the components of the drug;
- severe violations of the liver;
- combined use with potent inhibitors of cytochrome P450 1A2 (CYP1A2), such as ciprofloxacin or fluvoxamine;
- rare hereditary intolerance of galactose, severe lactase deficiency or malabsorption of galactose / glucose (lactose is included in the formulation).
Caution is required in the appointment of Sirdalud in the presence of the following diseases / conditions (relative contraindications):
- age from 65 years;
- pregnancy (safety and efficacy for this group of patients has not been studied, the use of Sirdalud is possible if the expected effect is higher than possible harm);
- functional kidney disorders;
- moderate violations of the liver.
Intended use for pregnancy and lactation
Studies were conducted on animals that did not demonstrate the presence of a teratogenic effect of the drug on the fetus. However, in pregnant women, controlled studies of the drug were not performed. Therefore, it is still recommended not to prescribe Sirdalud during pregnancy.
The drug enters the breast milk, so for lactating women, the drug is also not recommended for prescription.
Dosage and route of administration
As indicated in the instructions for use, Sirdalud has a narrow therapeutic index and a high variability in the concentration of tizanidine in the blood plasma of patients, so a careful selection is necessary dose.
Dose and dosage regimen should be selected individually, depending on the needs of the patient. The use of the drug in an initial dose of 2 mg 3 times / day reduces the risk of side effects.
The drug is taken orally. Tablets of 2 mg and 4 mg can be divided into two equal parts.
- In a painful muscle spasm, Sirdalud, as a rule, is used in a dose of 2 mg or 4 mg 3 times / day. In severe cases, you can additionally take 2 mg or 4 mg (preferably at bedtime due to possible increased sleepiness).
- With spasticity of skeletal muscles due to neurological diseases, the initial daily dose should not exceed 6 mg divided into 3 doses. The dose should be increased gradually, by 2-4 mg, at intervals of 3-4 to 7 days. Typically, the optimal therapeutic effect is achieved at a daily dose of 12 to 24 mg, divided into 3 or 4 doses at regular intervals. Do not exceed the dose of 36 mg / day.
- The experience of using the drug Sirdalud in patients aged 65 years and older is limited. It is recommended to start therapy with a minimal dose with a gradual increase to achieve the optimal ratio of tolerability and efficacy of therapy.
- Treatment of patients with renal insufficiency (CC less than 25 ml / min) is recommended to begin with a dose of 2 mg 1 time / day. Increase the dose by small "steps taking into account portability and effectiveness. If it is necessary to achieve a more pronounced effect, it is recommended first to increase the dose applied 1 time / day, then increase the frequency of application.
The use of the drug Sirdalud in patients with impaired hepatic function is contraindicated. In patients with impaired liver function of medium degree, the drug should be used with caution; it is recommended to start therapy with a minimal dose, with a gradual increase to achieve an optimal ratio of tolerability and efficacy therapy. Recommendations for monitoring liver function indicators are listed in the section "Special instructions".
Interruption of treatment
When treatment with Sirdalud is discontinued in order to reduce the risk of developing ricochet arterial hypertension and tachycardia, slowly reduce the dose to complete withdrawal of the drug, especially in patients receiving high doses of the drug for a long time time.
Side effect
When using Sirdalud in small doses (with painful muscle spasms), the following side effects are moderately expressed and pass on their own. Admission of higher doses of the drug, recommended for spasticity, leads to an increase in the incidence of and increase in the severity of adverse reactions, however, really serious cases requiring the discontinuation of the drug occur rarely.
- Musculoskeletal system: very often - myasthenia gravis;
- Laboratory indicators: often - increased activity of liver enzymes;
- Digestive system: very often - gastrointestinal disorders, a feeling of dryness in the oral cavity; often - nausea;
- Nervous system and psyche: very often - dizziness, drowsiness; often - sleep disorders, insomnia;
- Cardiovascular system: often - lowering of blood pressure (in some cases expressed, up to loss of consciousness and collapse); infrequently bradycardia;
- Other reactions: very often - increased fatigue.
In clinical practice, undesirable side effects from the following systems and organs were noted (their incidence was not established):
- Liver and biliary tract: liver failure, hepatitis;
- Nervous system, psyche and sense organs: vertigo, confusion, blurring of vision, hallucinations;
- Other reactions: withdrawal syndrome, asthenia.
Overdose
All known cases of an overdose resulted in recovery. If the dose is exceeded, the patient may feel nausea, drowsiness, anxiety, dizziness. Warnings of sorbents, in particular activated charcoal, will prevent severe consequences.
Recommended symptomatic treatment and increased diuresis.
special instructions
Patients who have drowsiness as a result of the use of the drug should be advised to refrain from activities, requiring high concentration of attention and quick reaction, for example, driving vehicles or working with machines and mechanisms.
Arterial hypotension can occur with the use of the drug Sirdalud, as well as as a result of drug interaction with inhibitors of CYP1A2 and / or antihypertensive drugs. A pronounced decrease in blood pressure can lead to loss of consciousness and collapse.
Reported cases of violations of liver function associated with tizanidine, but with a daily dose of up to 12 mg, these cases were rare. In this regard, it is recommended to monitor functional liver function tests once a month in the first 4 months of treatment in those patients who are prescribed tizanidine at a daily dose of 12 mg and above, as well as in those cases when there are clinical signs suggesting a violation of liver function - such as unexplained nausea, anorexia, a feeling of fatigue. In the case when the activity of ALT and AST in the serum stably exceeds the VGN 3 times or more, the use of the drug Sirdalud should be discontinued.
Interaction with other drugs
When using the drug, it is necessary to take into account the interaction with other drugs:
- With caution, it is necessary to take Sirdalud with those drugs that extend the QT interval (amitriptyline, cisapride, azithromycin, etc.).
- It is not recommended to take medicine with antiarrhythmic drugs (such as Propafenone, mexiletine, amiodarone), some fluoroquinolones (norfloxacin, enoxacin, perfloxacin), cimetidine, ticlopidine, oral contraceptives, rofecoxib.
- Contraindicated in the use of Sirdaluda along with fluvoxamine, ciprofloxacin. The result of simultaneous application can be a significant reduction in blood pressure, which is accompanied by dizziness and drowsiness, in some cases - loss of consciousness.
- The use of Sirdalurda together with rifampicin reduces the content of tizanidine in plasma and, accordingly, reduces the therapeutic effect of the drug.
- Simultaneous consumption of the drug with inhibitors of cytochrome CYP1A2 leads to an increase in the level of tizanidine in the plasma, which in turn leads to the appearance of symptoms of an overdose. Simultaneous consumption of Sirdalud with inducers CYP1A2 leads to a decrease in the level of tizanidine, which causes a decrease in the medicinal properties of the drug.
- Treatment with the drug of smoking men may require an increase in the dose. Alcohol should be avoided, since the drug can increase the negative effect of alcohol on the central nervous system. The sedative effect of Sirdalud can enhance sleeping pills, sedatives and antihistamines.
Reviews
We offer to familiarize with reviews of people who used the drug Sirdalud:
- Ira. The doctor has written out, an inflammation of a back nerve. In the kit are also other drugs, this one said to drink only at night 2mg once a day. There were pobochki in the beginning for both droppers and nyxes all together, at once also not to understand from what. This drug is clearly only for the night, sleep well in the morning, there is a dull pain in the back, like an improvement. Voobshchem my advice or council only for the night and not on three tablets in day.
- Olga. I was prescribed a doctor for pain when there was a strong stretching of the chest muscles. But my back and legs are already aching for a long time. After taking movalis with sirdaloud, the pain in his back was gone, but the muscles of his chest were not particularly affected. Of the pobochek nothing was, except as a retardation and immediately in a dream tends, probably so the doctor appointed them to drink an hour before bedtime.
- Alina. We prescribed sirdalud for the treatment of osteochondrosis of the spine. There was a strong spasm of muscles, at first the doctor pricked diprospan, and then he prescribed these pills. As soon as the effect of the injection of improvements was passed, I did not feel any further, although I took these pills as prescribed for a minimum of two weeks. Well, at least there were no side effects, but they are horrible here.
Analogues
From similar means for the treatment of spastic conditions can be used:
- Baclofen.
- Midsummer.
- Mioryx.
- Tizalud.
- Tolperil.
- Tizanil.
- Tizanidine-TEVA tablets.
Before buying an analogue, consult your doctor.
Shelf life and storage conditions
Tablets should be stored in a place inaccessible to children in a dark cool place for not more than 3 years from the date of manufacture, which is indicated on the box.
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