Sirdalud
Sirdalud: 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. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Sirdalud
ATX code: М03ВХ02
Active ingredient: tizanidine (tizanidine)
Producer: NOVARTIS Saglik Gida ve Tarim Urunleri Sanayi ve Ticaret, AS (Turkey)
Description and photo update: 2019-13-08
Prices in pharmacies: from 188 rubles.
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Sirdalud is a central muscle relaxant drug.
Release form and composition
Sirdalud is available in the form of tablets: white or off-white, flat, round, with beveled edges, scored (2 mg tablets) or crossed lines (4 mg tablets) on one side and the OZ code (2 mg tablets) or RL (tablets 4 mg) on the other (10 pieces in blisters, in a cardboard box three blisters).
Composition of 1 tablet:
- active substance: tizanidine (in the form of tizanidine hydrochloride) - 2 mg or 4 mg;
- auxiliary components: lactose monohydrate, stearic acid, microcrystalline cellulose, anhydrous colloidal silicon dioxide.
Pharmacological properties
Pharmacodynamics
Tizanidine is a centrally acting muscle relaxant. It acts on certain areas of the spinal cord by stimulating presynaptic alpha 2 receptors, which leads to inhibition of excitatory amino acids that activate receptors for N-methyl-D-aspartate (NMDA receptors). This causes the inhibition of 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, a decrease in muscle tone is observed. In addition to muscle relaxant properties, tizanidine is also characterized by a moderate central analgesic effect.
The effectiveness of Sirdalud has been proven both for chronic spasms of cerebral and spinal genesis, and for muscle spasm, accompanied by acute pain. The drug reduces the risk of developing clonic seizures and reduces spasticity, which leads to a decrease in resistance to passive movements and an increase in the range of active movements. The muscle relaxant effect, measured by means of the "pendulum" test and the Ashworth scale, and side effects (lowering blood pressure and heart rate) are determined by the content of tizanidine in the blood plasma.
Pharmacokinetics
Tizanidine is absorbed almost completely and quickly enough. Its maximum plasma level is recorded approximately 1 hour after taking Sirdalud. The substance is largely metabolized during the "first pass" through the liver, due to which the bioavailability reaches an average of about 34%. The maximum concentration of tizanidine is 12.3 and 15.6 ng / ml after single and multiple doses of the drug at a dose of 4 mg, respectively.
After reaching equilibrium with intravenous administration, the average volume of distribution is 2.6 l / kg. Tizanidine binds to blood plasma proteins by about 30%.
Most of tizanidine (about 95%) is rapidly metabolized in the liver. In vitro metabolic processes in which this compound takes part are carried out using the isoenzyme CYP1A2 of the cytochrome P 450 system. Metabolites do not differ in pharmacological activity.
The half-life of the active component of Sirdalud from the systemic circulation on average ranges from 2 to 4 hours. Approximately 70% of the dose taken is excreted mainly in the urine in the form of metabolites. About 4.5% of tizanidine is excreted unchanged.
When taking 4 mg of Sirdalud in the form of tablets simultaneously with food intake, no changes in the pharmacokinetics of tizanidine are observed. Even taking into account the increase in the maximum concentration of the substance in the blood by a third when taken after meals, this effect has no clinical significance. In this case, the degree and rate of absorption [according to the data on the area under the pharmacokinetic curve "concentration-time" (AUC)] do not change.
For tizanidine, when taken in doses of 1–20 mg, linear pharmacokinetics are characteristic.
In patients with renal dysfunction (CC less than or equal to 25 ml / min), the maximum level of tizanidine in blood plasma is 2 times higher than that in healthy volunteers. The terminal half-life in such patients is about 14 hours, which approximately 6 times increases the systemic bioavailability of tizanidine, which is measured by AUC.
Pharmacokinetic studies of tizanidine in patients with liver dysfunctions have practically not been conducted. Since tizanidine is mainly metabolized in the liver with the participation of the isoenzyme CYP1A2 of the cytochrome system, liver dysfunctions can provoke an increase in the systemic exposure of the drug.
There is no reliable information on the pharmacokinetics of the drug in patients over 65 years of age. The pharmacokinetic characteristics of tizanidine are independent of gender, and the effect on them of race and ethnicity has not been studied.
Indications for use
According to the instructions, Sirdalud is used for painful muscle spasm caused by functional and static diseases of the spine (lumbar and cervical syndromes), or after surgery (for example, surgery for osteoarthritis of the hip joint or intervertebral hernia).
The drug is also used for spasticity of skeletal muscles in diseases of a neurological nature, for example, in chronic myelopathy, multiple sclerosis, degenerative diseases of the spinal cord, cerebral palsy (in patients over 18 years of age) and the consequences of cerebrovascular accidents.
Contraindications
Absolute:
- severe hepatic dysfunction;
- children and adolescents up to 18 years old (due to the limited experience of use in this age category);
- concomitant use with ciprofloxacin or fluvoxamine;
- hypersensitivity to the main or auxiliary components of the drug.
Relative (Sirdalud is used with caution):
- moderate liver dysfunction;
- impaired renal function;
- advanced age over 65 years.
Instructions for use of Sirdalud: method and dosage
Sirdalud tablets are taken orally. The dosage regimen is selected individually, taking into account the characteristics of a particular patient.
The initial dose is 2 mg three times a day, at this dose the risk of unwanted side reactions is minimized.
Tablets of different dosages (2 mg and 4 mg) can be divided into two equal parts.
Recommended doses of Sirdalud:
- painful muscle spasm: 2 mg or 4 mg three times a day. If necessary, an additional intake of one tablet (2 mg or 4 mg) is possible, preferably at bedtime, as the drug may cause drowsiness;
- spasticity of skeletal muscles due to neurological diseases: the initial dose is no more than 6 mg per day in three divided doses, then the dose is gradually increased by 2–4 mg every 3–7 days. The optimal therapeutic effect was observed at a daily dose of 12-24 mg in 3-4 doses at regular intervals. The maximum dose is 36 mg per day.
Patients over 65 years of age and persons with moderate impairment of liver function are prescribed Sirdalud with caution, starting treatment with a minimum dose, which is gradually increased until the dose that is optimal in terms of effectiveness and tolerance is reached.
In renal failure (creatinine clearance less than 25 ml / min) at the beginning of therapy, the dose of the drug is 2 mg once a day. Then it is gradually increased, taking into account the tolerance and effectiveness of Sirdalud. If it is necessary to obtain a more pronounced effect, first, the dose taken once is increased, and then the frequency of application is increased.
The withdrawal of the drug is carried out gradually, especially in patients who have received Sirdalud in high doses for a long time. Otherwise, there is a likelihood of developing a rebound increase in blood pressure and tachycardia.
Side effects
- digestive system: very often - gastrointestinal disorders, a feeling of dryness in the mouth; often - nausea;
- cardiovascular system: often - a decrease in blood pressure (in some cases, pronounced, up to loss of consciousness and collapse); infrequently - bradycardia;
- nervous system and psyche: very often - dizziness, drowsiness; often - sleep disturbances, insomnia;
- musculoskeletal system: very often - myasthenia gravis;
- laboratory indicators: often - increased activity of liver enzymes;
- other reactions: very often - increased fatigue.
When using Sirdalud in small doses (with painful muscle spasm), the listed side effects are moderately expressed and go away on their own. Taking higher doses of the drug recommended for spasticity leads to an increase in the occurrence and severity of adverse reactions, however, truly severe cases requiring discontinuation of the drug are rare.
In clinical practice, undesirable side effects from the following systems and organs were noted (the frequency of their occurrence has not been established):
- liver and biliary tract: liver failure, hepatitis;
- nervous system, psyche and sensory organs: vertigo, confusion, blurred vision, hallucinations;
- other reactions: withdrawal syndrome, asthenia.
Overdose
Currently, several cases of drug overdose are known, including a case when the taken dose of Sirdalud was 400 mg. In all the situations described above, complete recovery was observed, the process of which proceeded without any peculiarities. Overdose symptoms include drowsiness, dizziness, anxiety, lengthening of the QT interval, decreased blood pressure, nausea, vomiting, depression of the respiratory center, coma.
For the complete elimination of Sirdalud from the body, repeated intake of activated carbon is recommended. Presumably, forced diuresis also promotes accelerated elimination of tizanidine. In the future, symptomatic therapy may be required.
special instructions
Liver dysfunction was more often observed in patients who received Sirdalud at a dose of more than 12 mg per day. In such patients, as well as in patients with clinical signs of impaired hepatic function (nausea, fatigue, anorexia), it is recommended to monitor liver function and conduct appropriate tests once a month during the first 4 months of therapy. If the levels of alanine aminotransferase and aspartate aminotransferase consistently exceed the upper limit of the norm by 3 or more times, the drug should be discontinued.
Sirdalud is not recommended for patients with severe lactase deficiency, hereditary galactose intolerance or glucose / galactose malabsorption syndrome, since the tablets contain lactose.
With the development of drowsiness during treatment with the drug, patients should refrain from performing work associated with a high concentration of attention and a quick psychomotor reaction.
Application during pregnancy and lactation
Controlled studies of the use of Sirdalud in pregnant patients have not been conducted, therefore it should not be assigned to such a category of patients (except in cases where the potential benefits outweigh the possible risks). Experiments on animals did not reveal clear signs of teratogenicity of the drug. When it was administered to animals at daily doses of 10 and 30 mg / kg, an increase in the gestational period was observed. Cases of prenatal and postnatal fetal death, as well as delayed fetal development have been reported. When the above doses were taken by the females, they showed pronounced symptoms of sedation and muscle relaxation. Taking into account the body surface area, the above doses exceeded the maximum permissible dose for humans (0.72 mg / kg per day) by approximately 2.2 and 6.7 times.
Animal studies show that small concentrations of tizanidine are excreted in the milk of lactating females. It is not recommended to use Sirdalud during lactation, since there is no information about the penetration of this compound into breast milk in humans.
Before starting treatment with Sirdalud, patients of reproductive age should receive information about the result of a pregnancy test.
When Sirdalud was administered in daily doses of 10 and 30 mg / kg to males and females, males and females, respectively, there was no adverse effect on fertility. In males who received the drug in doses exceeding 30 mg / kg per day, and females in doses exceeding 10 mg / kg per day, a decrease in fertility was observed. Considering the body surface area, these doses exceeded the maximum permissible dose for humans (equal to 0.72 mg / kg per day) by 2.2 and 6.7 times. When taking such doses, pregnant females observed special clinical symptoms, expressed in ataxia, weight loss, and pronounced signs of sedation.
Drug interactions
Sirdalud is not recommended to be used concomitantly with cimetidine, rofecoxib, ticlopidine, antiarrhythmic drugs (propafenone, mexiletine, amiodarone), oral contraceptives and some fluoroquinolones (pefloxacin, enoxacin, norfloxacin), since such combinations can lead to an increase in plasmidine, lengthening of the QT interval c.
Sirdalud is prescribed with caution simultaneously with drugs that prolong the QT interval (azithromycin, amitriptyline, cisapride).
When used together with antihypertensive drugs, a pronounced decrease in blood pressure and bradycardia is possible; with rifampicin - a decrease in the concentration of tizanidine in plasma by 50%, which leads to a decrease in the therapeutic effect of Sirdalud.
In patients who smoke (smoking more than 10 cigarettes per day), the systemic bioavailability of tizanidine is reduced by almost 30%, therefore, with prolonged treatment, an increase in the dose of the drug may be required.
Ethanol may increase the risk of side effects of the drug. Sirdalud, in turn, is able to enhance the suppressive effect of alcohol on the central nervous system.
Antihistamines, sleeping pills, and sedatives can increase the sedative effect of tizanidine. Other α 2 -adrenergic receptor agonists, when used simultaneously with Sirdalud, potentially enhance the hypotensive effect.
Analogs
Tizalud and Midokalm are analogues of Sirdalud.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C out of reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Sirdalud
According to reviews, Sirdalud is used in patients of various age categories. On average, they assess the results of their treatment at 3.9 points out of 5. Many patients note the appearance of unpleasant side effects, among which fatigue and drowsiness prevail. Also reported a significant effect of the drug on the liver.
Doctors prescribe Sirdalud as a means of symptomatic therapy to reduce skeletal muscle spasms. In case of severe manifestations of side effects or the absence of a significant result after 3 days of treatment, you should consult a specialist who will adjust the therapy regimen.
Price for Sirdalud in pharmacies
The approximate price for Sirdalud with a dosage of 2 mg is 216-237 rubles, and with a dosage of 4 mg - 318-350 rubles (for a package containing 30 tablets).
Sirdalud: prices in online pharmacies
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Drug name Price Pharmacy |
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Sirdalud 2 mg tablets 30 pcs. 188 r Buy |
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Sirdalud tablets 2mg 30 pcs. 198 RUB Buy |
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Sirdalud 4mg tablets 30 pcs. 271 r Buy |
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Sirdalud 4 mg tablets 30 pcs. 271 r Buy |
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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!
