SIRDALUD (tablets)
It is in a state of rest and this is where painful sensations appear that cannot be expressed in words, I think that someone is familiar with them, when “the veins are being pulled out of you.”
There are 30 capsules in a box of 6 mg each (there is also a dosage of 4 mg)
All information is written in Russian and English. The active substance in this drug is tizanidine, it is thanks to it that increased muscle tone is reduced and spasm is relieved. Spinal reflexes are suppressed and a muscle-relaxing effect occurs, that is, convulsions stop.
Surdalud MR was released in Turkey under license from a Swiss company.
The box contains the date of manufacture and expiration date of the drug.
Now the price. I can’t say that it’s too high, considering that this is exactly one month of use. But the question arises: why not just prescribe tizanidine for 100 rubles?
The indications for this drug are quite narrow, namely spasms and convulsions for various reasons.
Contraindications: age under 18 years, severe liver dysfunction, incompatibility with certain medications, all this is described in detail in the instructions.
Side effects: here, like most medications, there is a ready-made, but not published, horror book. BUT, like any drug, if you take it strictly according to the doctor’s recommendations (and I still advise you to read the instructions, since many doctors are too zealous in treatment), then the risk of side effects will be minimal.
The box contains three blisters of 10 capsules.
Sirdalud is taken once a day, preferably in the first half of the day (food intake has no effect), because the maximum effect begins after 8-9 hours. Abrupt discontinuation of the drug is not recommended; it is advisable to gradually reduce the dose until complete discontinuation. But according to the doctor, they do not refuse sirdalud completely, because with a good outcome of treatment, you can switch to taking it once every 2-3 days and even up to once every 5 days.
Which is exactly what happened. Mom took Sirdalud every day for almost 20 days, as she said: I’m already afraid to jinx it and say that the drug helps and the leg cramps have stopped. Then she started taking sirdalud every other day, now after more than a month, 1 capsule every 2-3 days is enough for my mother.
Modified release capsules - do you know what they are? What progress has come! This shell - a capsule - made using a special technology allows you to program and control the rate of release of the drug that is inside it! And here is the answer to the question - why didn’t the doctor prescribe cheap tizanidine!
White opaque capsules with the name of the drug and dosage written on them.
Of course, only a doctor can prescribe medications after studying each specific case of the disease and symptoms. If you are prescribed Sirdalud MR during treatment, then I recommend paying attention to it. In this particular case, this drug worked well.
Health and good mood to everyone!
Sirdalud mr caps with modif release 6mg N30
Indications for use of the drug SIRDALUD® MR are spasticity of skeletal muscles in neurological diseases (for example, multiple sclerosis, chronic myelopathy, degenerative diseases of the spinal cord, consequences of cerebrovascular accidents and cerebral palsy / patients over 18 years old).
pharmachologic effect
Centrally acting muscle relaxant. The main point of application of its action is in the spinal cord. By stimulating presynaptic α2 receptors, tizanidine inhibits the release of excitatory amino acids that stimulate N-methyl-D-aspartate-sensitive receptors (NMDA receptors). As a result, polysynaptic transmission of excitation is suppressed at the level of interneurons of the spinal cord. Since it is this mechanism that is responsible for excess muscle tone, when it is suppressed, muscle tone decreases. In addition to muscle relaxant properties, tizanidine also has a moderate central analgesic effect.
Sirdalud® MR 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
Suction
When taken orally, tizanidine is almost completely absorbed. The average Cmax value is reached within 8.5 hours and is approximately half the Cmax value when taking Sirdalud® tablets in a similar daily dose, divided into 3 doses, while the total exposure (AUC) remains unchanged.
Distribution
The sustained release of tizanidine from the modified-release capsule dosage form results in a “softened” pharmacokinetic profile, which ensures the maintenance of stable therapeutic plasma concentrations of tizanidine over 24 hours.
Plasma protein binding is 30%.
Metabolism
Tizanidine is rapidly and extensively metabolized in the liver. In vitro, tizanidine has been shown to be primarily metabolized by the CYP1A2 isoenzyme. Metabolites are inactive.
Removal
Tizanidine is excreted primarily by the kidneys (approximately 70% of the dose) in the form of metabolites; the share of unchanged substance accounts for only about 2.7%.
Pharmacokinetics in special clinical situations
Gender does not affect the pharmacokinetic parameters of tizanidine.
Dosage regimen
The drug is prescribed orally. The dosage regimen should be set individually.
The initial daily dose is 6 mg (1 capsule). If necessary, the daily dose can be gradually increased (“in steps”) by 6 mg (1 capsule) at intervals of 3-7 days. Clinical experience shows that for most patients the optimal dose is 12 mg/day. (2 caps.); in rare cases, it may be necessary to increase the daily dose to 24 mg.
Treatment of patients with renal failure (creatinine clearance < 25 ml/min)
It is recommended to start with taking the drug Sirdalud® at a dose of 2 mg 1 time / day.
The dose is increased in small “steps”, taking into account tolerability 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. Side effects
Adverse reactions are distributed according to the frequency of occurrence. To assess the frequency of adverse reactions, the following criteria were used: very often (≥10%); often (from ≥1% to <10%); sometimes (from ≥0.1% to <1%); rare (from ≥0.01% to <0.1%); very rare (<0.01%, including isolated reports). In one group, by frequency of occurrence, adverse reactions are ranked by degree of significance.
From the nervous system:
often - drowsiness, weakness, dizziness; rarely - hallucinations, insomnia, sleep disturbances.
From the cardiovascular system:
often - bradycardia, decreased blood pressure; in some cases - a pronounced decrease in blood pressure up to collapse and loss of consciousness.
From the digestive system:
often - dry mouth; rarely - nausea, gastrointestinal disorders, increased activity of liver transaminases; very rarely - hepatitis, liver failure.
From the musculoskeletal system:
rarely - muscle weakness.
Other:
often - increased fatigue.
When taken in small doses recommended for relieving painful muscle spasms, drowsiness, increased fatigue, dizziness, dry mouth, decreased blood pressure, nausea, gastrointestinal disorders, and increased activity of liver transaminases were observed. Usually the above reactions are moderate and transient.
When taken at higher doses recommended for the treatment of spasticity, the above adverse reactions occur more often and are more severe, but they are rarely so severe that treatment has to be interrupted. In addition, the following phenomena may occur: decreased blood pressure, bradycardia, muscle weakness, insomnia, sleep disturbance, hallucinations, hepatitis.
Contraindications to the use of the drug SIRDALUD® MR
- severe liver dysfunction;
- simultaneous use with strong inhibitors of CYP1A2 isoenzymes (including fluvoxamine or ciprofloxacin);
- hypersensitivity to tizanidine or any other component of the drug.
The use of Sirdalud MR in children is not recommended, because Experience with the drug in children is limited.
Use of the drug SIRDALUD® MR during pregnancy and breastfeeding
Since there are no controlled studies of tizanidine in pregnant women, it should not be used during pregnancy unless the potential benefit outweighs the potential risk.
Tizanidine is excreted in breast milk in small quantities. However, women who are breastfeeding children should not use the drug.
Use for liver dysfunction
Contraindicated in cases of severe liver dysfunction.
Use for renal impairment
Carefully _
Sirdalud® MR should be used in patients with renal failure.
Cautions:
Cases of liver dysfunction associated with tizanidine have been reported, but these cases have been rare with daily doses up to 12 mg. In this regard, it is recommended to monitor 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 or higher, as well as in cases where clinical signs suggestive of impaired liver function are observed. such as unexplained nausea, anorexia, feeling tired. In cases where serum levels of ALT and AST persistently exceed ULN by 3 times or more, the use of Sirdalud MR should be discontinued.
Sirdalud® MR should not be abruptly discontinued; the dose of the drug should be reduced gradually.
When Sirdalud MR was abruptly discontinued after prolonged treatment and/or taking high doses of the drug (as well as after simultaneous use with antihypertensive drugs), the development of tachycardia and an increase in blood pressure was observed, which in some cases can lead to acute cerebrovascular accident.
Caution should be exercised when using Sirdalud MR in patients with renal failure. When using Sirdalud MR in patients with renal failure (creatinine clearance less than 25 ml/min), adjustment of the dosage regimen is necessary.
Caution should be exercised when using Sirdalud MR in elderly patients. Experience with the use of Sirdalud MR in elderly patients is limited. Based on pharmacokinetic data, it can be assumed that in some cases renal clearance in these patients may be significantly reduced.
Use in pediatrics
Experience with the drug in children is limited. Therefore, the use of Sirdalud MR in this category of patients is not recommended.
Impact on the ability to drive vehicles and operate machinery
If drowsiness, dizziness, or a decrease in blood pressure develop during therapy with Sirdalud MR, you should refrain from types of work that require a high concentration of attention and quick reaction, for example, driving a vehicle or operating machinery.
Overdose
To date, there have been several reports of overdose of Sirdalud MR, including a case where the dose taken was 400 mg.
Symptoms:
nausea, vomiting, decreased blood pressure, prolongation of the QTc interval, dizziness, drowsiness, miosis, anxiety, respiratory failure, coma.
Treatment:
To remove the drug from the body, repeated gastric lavage and the administration of activated charcoal are recommended.
Forced diuresis may also speed up the elimination of tizanidine. Subsequently, symptomatic therapy is carried out. Drug interactions
When Sirdalud MR is used together with inhibitors of the CYP1A2 isoenzyme, an increase in the concentration of tizanidine in the blood plasma is possible.
Concomitant use of tizanidine with fluvoxamine or ciprofloxacin, inhibitors of cytochrome P450 isoenzyme 1A2, results in a 33-fold or 10-fold increase in the AUC of tizanidine, respectively. The result of combined use may be a clinically significant and prolonged decrease in blood pressure, leading to drowsiness, weakness, and inhibited psychomotor reactions (in some cases, even collapse and loss of consciousness). Concomitant use of tizanidine with fluvoxamine or ciprofloxacin is contraindicated.
The simultaneous administration of tizanidine with other inhibitors of the CYP1A2 isoenzyme - antiarrhythmic drugs (amiodarone, mexiletine, propafenone), cimetidine, fluoroquinolones (enoxacin, pefloxacin, ciprofloxacin, norfloxacin), rofecoxib, oral contraceptives, ticlopidine.
With an increase in the concentration of tizanidine in the blood plasma, a prolongation of the QTc interval is possible, which is characteristic of an overdose of the drug.
The simultaneous administration of Sirdalud MR with antihypertensive drugs, including diuretics, can sometimes cause a decrease in blood pressure (in some cases, even collapse and loss of consciousness) and bradycardia.
Ethanol or sedatives may enhance the sedative effect of Sirdalud MR, therefore simultaneous use with other sedatives and/or alcohol is not recommended.
Conditions for dispensing from pharmacies
The drug is available with a prescription.
Storage conditions and periods
List B. The drug should be stored out of the reach of children at a temperature not exceeding 30°C. Shelf life: 3 years.
