Sirdalud MR
Sirdalud MR: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Sirdalud MR
ATX code: M03BX02
Active ingredient: tizanidine (Tizanidine)
Manufacturer: Novartis Pharmaceuticals, S. A. (Novartis Farmaceutica, SA) (Spain); Novartis Saglik Gida ve Tarim Yuryunleri Sanayi ve Tikaret A. S. (Novartis Saglik Gida ve Tarim Urunlery San.ve Ticaret, AS) (Turkey)
Description and photo update: 2019-30-12
Prices in pharmacies: from 453 rubles.
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Sirdalud MR is a centrally acting muscle relaxant.
Release form and composition
The drug is available in the form of capsules with modified release: gelatinous, size 2, hard, opaque, white cap and body, gray inscription is applied: on the cap - Sirdalud, on the body - 6 mg; the contents of the capsules are round pellets of almost white or white color (10 capsules in blisters, in a cardboard box 1, 2 or 3 blisters and instructions for use of Sirdalud MR).
1 capsule contains:
- active substance: tizanidine hydrochloride - 6.864 mg, which in terms of tizanidine base is 6 mg;
- auxiliary components: gelatin, ethylcellulose, shellac, sugar spheres, titanium dioxide, talc;
- ink composition: shellac, titanium dioxide (E171), iron dye black oxide (E172).
Pharmacological properties
Pharmacodynamics
Sirdalud MR is a centrally acting muscle relaxant. The main point of application of its active substance, tizanidine, is the neurons of the spinal cord. The mechanism of action of the drug is due to the ability of tizanidine to stimulate presynaptic alpha2-adrenergic receptors, which leads to the suppression of the release of amino acids that excite and stimulate NMDA receptors (N-methyl-D-aspartate). As a result, there is a suppression of polysynaptic transmission of excitation at the level of intermediate neurons of the spinal cord and a decrease in muscle tone. Along with muscle relaxant properties, tizanidine has a moderately pronounced central analgesic effect.
With chronic spasticity of spinal and cerebral genesis, the therapeutic effect of Sirdalud MR provides a decrease in spasticity and clonic seizures, a decrease in resistance to passive movements, and an increase in the range of active movements.
The muscle relaxant effect of Sirdalud MR in the selection of an individual dose is measured using the "pendulum" test of Wartenberg and the Ashworth scale. The narrow therapeutic range of tizanidine and the high variability of its plasma concentrations affect the likelihood or frequency of side effects such as a decrease in heart rate (heart rate) and a decrease in blood pressure (blood pressure).
Pharmacokinetics
After taking Sirdalud MR inside, almost complete absorption of tizanidine occurs. The maximum concentration (C max) in blood plasma after a single dose of 12 mg is achieved within 8.5 hours and averages 6.6 ng / ml. This corresponds to approximately half of the C max after taking a similar dose of tizanidine in tablet form (4 mg 3 times a day). The total daily exposure AUC (area under the pharmacokinetic curve "concentration - time") remains unchanged.
Simultaneous food intake has no clinically significant effect on the pharmacokinetics of tizanidine.
Prolonged release of tizanidine from a modified release capsule results in a moderate pharmacokinetic profile and maintains a stable therapeutic plasma concentration of tizanidine for 24 hours.
Plasma protein binding - 30%.
Tizanidine is metabolized to a large extent (more than 95%) and rapidly in the liver with the participation of the CYP1A2 isoenzyme of the cytochrome P 450 system with the formation of inactive metabolites.
It is excreted mainly through the kidneys: unchanged - about 4.5%, in the form of metabolites - about 70%.
In the dose range from 1 mg to 20 mg, tizanidine is characterized by linear pharmacokinetics.
In case of impaired renal function with creatinine clearance (CC) less than 25 ml / min, the maximum average concentration of tizanidine in plasma increases by 2 times compared with healthy patients. An increase in the half-life to 14 hours causes an increase in the systemic bioavailability of tizanidine by about 6 times.
The results of specific studies of Sirdaluda MR in patients with impaired liver function are absent. But in connection with the intensive biotransformation of tizanidine in the liver, it should be assumed that functional liver pathologies may increase the systemic effect of tizanidine.
In men and women, the pharmacokinetic properties of Sirdalud MR are the same.
Data on the pharmacokinetics of the drug in patients over the age of 65 are limited.
Indications for use
The use of Sirdaluda MR is indicated in the treatment of neurological diseases accompanied by spasticity of skeletal muscles, including:
- degenerative pathologies of the spinal cord;
- multiple sclerosis;
- chronic myelopathy;
- the consequences of cerebrovascular accidents;
- the consequences of cerebral palsy in patients over the age of 18.
Contraindications
Absolute:
- severe liver dysfunction;
- deficiency of sucrose or isomaltose, glucose-galactose malabsorption syndrome, fructose intolerance;
- concomitant therapy with fluvoxamine, ciprofloxacin and other drugs that are potent inhibitors of the CYP1A2 isoenzyme;
- breast-feeding;
- age under 18;
- hypersensitivity to the components of the drug.
It is recommended to prescribe Sirdalud MR with caution in case of impaired renal function, moderate liver dysfunction, congenital lengthening of the QT interval syndrome, concomitant use of oral contraceptives or tizanidine, the patient is over 65 years of age.
During pregnancy, taking capsules is allowed only in special cases, when, according to the doctor, the expected clinical effect for the mother outweighs the potential risk to the fetus.
Sirdalud MR, instructions for use: method and dosage
Sirdalud MR capsules are taken orally.
The doctor selects the dosage regimen individually, taking into account the narrow therapeutic range inherent in tizanidine and the significant variability of its concentrations in blood plasma.
Recommended dosage: initial dose - 6 mg (1 pc.) 1 time per day. Then, as needed, the dose is gradually increased by 6 mg every 3-7 days. Based on clinical practice, it has been established that in most cases the optimal maintenance dose is 12 mg once a day. The daily dose range is from 6 mg to 24 mg, therefore, if necessary, it is possible to use Sirdalud MP at a dose of 24 mg once a day.
In patients over the age of 65 years or with moderate hepatic impairment, the usual dosing regimen is used, only caution is required when increasing the dose so as not to cross the border of the ratio of optimal tolerance and effectiveness of therapy.
The use of Sirdalud MR in case of impaired renal function (CC less than 25 ml / min) is indicated only in patients with a previously titrated optimal dose of tizanidine when treated with other dosage forms. The initial dose should be increased at long intervals, taking into account the tolerance and effectiveness of therapy.
If it is necessary to achieve a more pronounced effect, it is first recommended to increase the daily dose, and then the frequency of administration.
The treatment should be discontinued by slowly decreasing the dose of Sirdaluda MR. Particular care must be taken in patients who have taken high doses of tizanidine during a long course of therapy. Rapid withdrawal is associated with a high risk of developing tachycardia and increased blood pressure, up to acute cerebrovascular accident.
Side effects
- from the immune system: hypersensitivity reactions, including urticaria, angioedema, anaphylactic reactions;
- from the nervous system: very often - drowsiness, dizziness; frequency not established - vertigo;
- mental disorders: often - insomnia, sleep disorder; frequency not established - confusion, hallucinations;
- from the side of the heart: infrequently - bradycardia;
- from the side of the vessels: often - lowering blood pressure (including a pronounced decrease in blood pressure, up to loss of consciousness and collapse);
- from the digestive system: very often - dry mouth, gastrointestinal disorders; often - nausea;
- from the liver and biliary tract: the frequency has not been established - liver failure, hepatitis;
- from the musculoskeletal system: very often - muscle weakness;
- on the part of the organ of vision: frequency not established - blurred vision;
- general disorders: very often - increased fatigue; frequency not established - withdrawal syndrome, asthenia;
- laboratory parameters: often - an increase in the activity of hepatic transaminases;
- others: against the background of taking low doses in order to relieve painful muscle spasm, it is possible that moderate and transient reactions such as dry mouth, nausea, drowsiness, dizziness, increased fatigue, lowering blood pressure, gastrointestinal disorders, increased activity of hepatic transaminases may occur; while taking higher doses of Sirdaluda MR, used to treat spasticity, sleep disturbances, insomnia, bradycardia, muscle weakness, hallucinations are possible, as well as side reactions similar to those that occur while taking low doses, only their frequency and severity are more expressed, in rare cases they may require interruption of treatment.
Overdose
Symptoms: drowsiness, nausea, vomiting, lowering blood pressure, respiratory failure, prolongation of the QTc interval, dizziness, anxiety, miosis, coma.
Treatment: multiple intake of activated carbon and forced diuresis are shown in order to quickly remove the active substance from the body. Careful monitoring of the patient's condition and symptomatic therapy, if necessary.
special instructions
If side effects appear, you should consult a doctor.
It should be borne in mind, since Sirdalud MR has a sedative effect, hallucinations may occur against the background of its use.
Treatment should be accompanied by a regular check of the liver function in patients taking tizanidine in a daily dose of 12 mg or more, or if, during therapy, the patient has clinical signs of a functional liver disorder such as fatigue, nausea, anorexia. During the first 4 months in this category of patients, it is recommended to carry out functional liver tests once a month. If there is a persistent excess of the upper limit of the normal level of ALT (alanine aminotransferase) and AST (aspartate aminotransferase) in the blood serum by 3 times or more, then a decision should be made to stop taking Sirdalud MR.
Influence on the ability to drive vehicles and complex mechanisms
During the period of treatment with Sirdalud MR capsules, patients should be careful when driving vehicles or complex mechanisms, and in case of drowsiness, it is necessary to refrain from these and other activities that require significant concentration of attention and high speed of psychomotor reactions.
Application during pregnancy and lactation
The use of Sirdaluda MP capsules during breastfeeding is contraindicated.
During pregnancy, tizanidine should be prescribed with caution, taking capsules is allowed in special cases if the expected clinical effect for the mother outweighs the potential risk for the fetus.
Pediatric use
The use of Sirdaluda MR is contraindicated for the treatment of children and adolescents under the age of 18 years.
With impaired renal function
It is recommended to use Sirdalud MR with caution in case of impaired renal function.
For patients with CC less than 25 ml / min, the administration of the drug is indicated only if the optimal dose is titrated during treatment with other dosage forms of tizanidine. The initial dose should be increased at longer intervals, given the tolerability and efficacy of therapy.
For violations of liver function
The use of Sirdalud MR is contraindicated for the treatment of patients with severely impaired liver function.
The drug should be prescribed with caution if the liver function is moderately impaired.
Use in the elderly
It is recommended with caution to prescribe Sirdalud MR to patients over the age of 65 years, using the general dosage regimen for treatment. When choosing the optimal maintenance dose, it is necessary to carefully monitor the tolerance and effectiveness of therapy in patients.
Drug interactions
With the simultaneous use of Sirdalud MR:
- fluvoxamine, ciprofloxacin and other inhibitors of the isoenzyme CYP1A2: a combination with drugs that inhibit the isoenzyme CYP1A2 can lead to an increase in the level of tizanidine in blood plasma and be accompanied by symptoms of overdose, including prolongation of the QTc interval. AUC of tizanidine when combined with fluvoxamine increases 33 times, and with ciprofloxacin - 10 times. This can cause a prolonged, clinically significant decrease in blood pressure, dizziness, drowsiness, a decrease in the speed of psychomotor reactions, and in some cases, loss of consciousness and collapse. Therefore, concomitant therapy with fluvoxamine or ciprofloxacin is contraindicated;
- antiarrhythmics (propafenone, amiodarone, mexiletine), rofecoxib, cimetidine, oral contraceptives, ticlopidine and fluoroquinolones such as enoxacin, norfloxacin or pefloxacin: it is not recommended to combine the administration of these drugs with Sirdalud MR;
- inducers of the CYP1A2 isoenzyme: a combination with drugs that induce the CYP1A2 isoenzyme can cause a decrease in the concentration of tizanidine in plasma and lead to a decrease in the therapeutic effect of the drug;
- amitriptyline, cisapride, azithromycin: take the listed and other drugs that prolong the QT interval with caution;
- antihypertensive drugs: against the background of concomitant therapy with diuretics and other antihypertensive drugs, a decrease in blood pressure (including loss of consciousness, up to collapse) and bradycardia may occur. After using Sirdaluda MR together with antihypertensive drugs, in case of abrupt withdrawal of tizanidine, there is a risk of tachycardia, increased blood pressure, acute cerebrovascular accident;
- rifampicin: it should be borne in mind that long-term combined use of rifampicin and tizanidine leads to a decrease in the level of tizanidine in blood plasma by 50% and a decrease in its therapeutic effect. In cases where this combination is clinically justified, it is recommended to increase it when selecting the dose of tizanidine;
- benzodiazepines, baclofen and other hypnotics, sedatives, blockers of histamine H1 receptors: the combination with these drugs can increase the sedative effect of Sirdalud MR;
- alpha2-adrenergic agonists: clonidine and other alpha2-adrenergic agonists enhance the hypotensive effect of Sirdalud MR;
- nicotine: when smoking, it should be borne in mind that smoking more than 10 cigarettes a day reduces the bioavailability of the drug by about 30%, therefore, it may be necessary to take higher doses (compared to average therapeutic doses) with a long course of treatment in smoking patients;
- ethanol: the use of alcohol or ethanol-containing medicines is recommended to be avoided. This is due to an increase in the depressing effect of alcohol on the central nervous system and an increased risk of developing adverse events (including lowering blood pressure, lethargy).
Analogs
Analogs of Sirdalud MR are Baklosan, Kalmirex, Midocalm, Sirdalud, Tizalud, Tizanidin, Tizanidin-SZ, Tizanidin-Teva, Tizanil, Tolperison-OBL, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Sirdalud MR
Patients in reviews of Sirdaluda MR indicate the effectiveness of the drug, its gradual mild and long-term effect. The absence of adverse reactions, such as drowsiness, weakness, or decreased blood pressure, is noted. Particular attention is paid to the need to select the optimal individual dosage regimen.
In some cases, patients complain that mistakenly selected high doses of tizanidine with prolonged action have a negative effect on their general condition and performance, causing weakness in the limbs, dizziness, and drowsiness.
Price for Sirdalud MR in pharmacies
The price of Sirdalud MP 6 mg, modified release capsules, for a package containing 30 pieces, can range from 533 rubles.
Sirdalud MR: prices in online pharmacies
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Drug name Price Pharmacy |
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Sirdalud mr caps. with mod. release 6mg n30 453 r Buy |
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Sirdalud MP 6 mg modified release capsules 30 pcs. 453 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
