International name: Tizanidine (Tizanidine).
The active substance sirdalud - tizanidine - the central muscle relaxant action affects skeletal muskulaturu.Osnovnoe effect in the presynaptic a2 - receptors of the spinal cord, encouraging them tizanidine inhibits the production of amino acids that stimulate the NMDA receptors. As a result, a suppression of spinal neurons in the intermediate level, so the transfer is suppressed by the excitation polysynaptic.
As well as its analogs Sirdalud has a moderate analgesic effect and reduce spasms and clonic convulsions.
When an internal reception Sirdalud absorbed at high speed and almost completely. Sirdalud maximum concentration in the blood occurs within 8 hours. Bioavailability is expressed because metabolism and passage through the liver is about 34%.
Sirdalud released from the dosage capsule for a long time, which mitigates the pharmacokinetic profile, and supports the stability of therapeutic drug concentrations in the blood for 24 hours.
In laboratory reviews Sirdalud quickly and with a high percentage is metabolized in the liver.
Excreted mainly via the kidneys, with an average of about 3 hours. About 70% of the dose, is excreted as metabolites remains unchanged about 2, 7% of the substance.
Gender does not affect the patient's pharmacokinetics.
In renal insufficiency, the maximum plasma concentration is increased about two times, and the elimination half-life increases to 14 hours.
Like analogs sirdalud meal no effect on the pharmacokinetics and absorption of the drug does not change.
Sirdalud indications for use
Preparation Sirdalud is used in skeletal muscle spasms caused by neurological disorders such as multiple sclerosis, cerebral palsy, spinal cord diseases, poor circulation brain, chronic myelopathy, and others.
And also for painful muscle spasms different etymology:
- functional or static disease of the spine;
- postoperative period.
When skeletal muscle spasms caused by neurological disorders, the doctor selects the individual dosage, focusing on the clinical picture. According to the instructions assigned Sirdalud doses up to 6 mg per day, which is divided into three portions. After 3 to 7 days, possibly increasing dosages of 2-4 mg. Considered optimal therapeutic dose of 12-24 mg per day in 3-4 divided doses with regular intervals between them. Junk is the dosage in excess of 36 mg per day.
With painful muscle spasms applied 2-4 mg 3 times a day. At the express spasm can receive bedtime further 2-4 mg.
Elderly patients drug is given based on the assumption that this category of persons slow renal clearance. In this regard, the use of undesirable elderly sirdalud on indications of renal activity.
Patients suffering from renal impairment, the initial dose is assigned to 2 mg / 24 hours at a time, over time you can increase the dosage based on tolerability.
Adoption of children sirdalud reviews is not enough to designate it as a therapeutic agent.
Side effects sirdalud
Application sirdalud in low doses, rarely brings side effects, even when they are not the manifestation pronounced. Usually manifested as weakness, drowsiness, mild hypotension, dizziness, dry mouth. Less often in the form of gastrointestinal disorders and nausea.
At higher doses sirdalud, reviews suggest that the side effects are more vibrant character, but not an indication to remove the drug. Most often they appear as bradycardia and hypotension, sometimes in the form of sleep disturbances, muscle weakness, insomnia, hallucinations. Very rarely can occur acute hepatitis.
- Abnormal liver function;
- Hypersensitivity to tizanidine or any other components of the drug;
- The combination of tizanidine with fluvoxamine.
Animal studies have found no teratogenic effects on the fetus. However, research use sirdalud pregnant and lactating women have not been conducted in this regard the appointment of pregnant sirdalud instruction is not recommended unless the benefit to the mother outweighs the potential risk to the fetus. The conducted experiments on animals have shown that small amounts of tizanidine into breast milk, concerning the appointment during lactation is not recommended.
Interaction with other drugs
According to the instructions Sirdalud is prohibited to assign patients taking inhibitors CYP1 A2 and fluvoxamine. Also, caution is needed in combination with other inhibitors CYP1 A2 (pefloxacin, Amiodarone, Mexiletine, Propafenone, pefloxacin, cimetidine, ciprofloxacin, enoxacin, oral hormonal contraceptives, norfloxacin, ticlopidine, and rofecoxib). In such combinations, dizziness and decreased psychomotor.
Combining sirdalud with antihypertensive drugs and diuretics can cause hypotension and bradycardia.
Adoption of sedatives or alcohol increases the sedative effect of Sirdalud.
There are reports of overdose sirdalud, including taking the drug at a dose of 400 mg. Deaths have been recorded. Overdose expressed in nausea, vomiting, hypotension, dizziness, anxiety, cramps, breathing problems, drowsiness, coma. Treated Multiple assignment enterosorbents and symptomatic treatment. As with analogue sirdalud overdose well blocked by forced diuresis.
Form release sirdalud
Tablets 2 or 4 mg.
The drug is stored at a temperature of +15 - +25 degrees C. In places protected from access by children.