Available analogues of sirdalud for muscle spasms. Which is better: Sirdalud or Tizanidin-Teva Sirdalud or tizalud which is better

Greetings to all who have looked at my review!

Osteochondrosis once became a problem for me. Wedged so that I could barely crawl. The sciatic nerve was clamped and then I limped to the neurologist. Sirdalud was prescribed to me in combination therapy with other drugs. The effect was, but the heaviness in the epigastric region worried me. Like a heavy lump in the guts. So unpleasant. And at another appointment, they replaced it with Midocalm. The treatment has gone much better!

However, not everything is so smooth. My ligaments are weak and I don't know where I could have torn a ligament in my thigh. My leg did not work well, I could not sleep and limped for half a year according to various doctors who gave me the craziest diagnoses. Looking at the pictures, I just laughed at the diagnoses, because in the past I was also related to the healthcare system and I already understand the pictures, nothing written in the conclusion did not correspond to reality.

On the recommendation of friends, after three "specialists" from the polyclinic, I went to see a neurologist with the highest category, for a fee. Previously, he told me to do an MRI of the spine. Everything turned out to be in order there. The influence of sports and the chiropractor was not in vain.

At the reception, he twisted and twisted my leg for a long time. I looked at all the pictures. Then he said that I had a tear in the ligaments. Moreover, next to the nerve, it becomes inflamed and hurts, from this there was pain, muscle clamping was also. He prescribed a whole footcloth of pills according to the scheme, lotions, as many as three physiotherapy procedures.

Tizalud.

Was discharged to me in the treatment regimen. I was afraid that there would be side effects, like Sirdalud's.

The drug is Ukrainian.

Prescribed for me was 20 tablets, to drink for two weeks at night, one at a time. So what is left.

The price of the issue is $ 7.

The tablets are small, white, in the center there is a notch for dividing in half. Not covered with a shell.

Instruction.

Indications for use
Painful muscle spasm associated with static and functional diseases of the spine (cervical and lumbar syndromes), as well as after surgical interventions (for a herniated disc, osteoarthritis of the hip joint), skeletal muscle spasticity in neurological diseases (multiple sclerosis, chronic degenerative myelopathy, spinal cord, cerebrovascular accident, cerebral palsy).
Contraindications
The drug is not prescribed for severe liver dysfunction, concomitant administration of fluvoxamine, increased individual sensitivity to drug components, pregnancy, breastfeeding, under the age of 18.
Pregnancy and lactation
Taking the drug during pregnancy is contraindicated. If treatment with tizanidine is necessary, breastfeeding should be discontinued.
Method of administration and dosage
Adults are taken orally, regardless of food intake, with a small amount of liquid. The dosage regimen is set individually, taking into account the indications, effectiveness and tolerability of therapy.
For painful muscle spasm, 2 mg or 4 mg are prescribed 3 times a day. In severe cases, 2 mg or 4 mg of tizanidine are additionally prescribed at night.
With spasticity of skeletal muscles due to neurological diseases, the initial daily dose should not exceed 6 mg (2 mg 3 times a day). The daily dose can be increased gradually, by 2-4 mg per day, at intervals of 3-4 to 7 days. Usually, the optimal therapeutic effect is achieved with a daily dose of 12 to 24 mg, distributed over 3 or 4 doses at regular intervals.
The highest daily dose of tizanidine for adults is 36 mg per day.
In patients with renal insufficiency (creatinine clearance less than 25 ml / min), the initial dose is 2 mg once a day. The dose increase should be carried out gradually, taking into account the effectiveness and tolerability of therapy. If a more pronounced effect is required, it is recommended to first increase the dose prescribed 1 time per day, after which the frequency of administration is increased.
The duration of the course of therapy is determined depending on the dynamics of muscle-tonic and pain manifestations. In case of acute pain of muscle genesis, the duration of taking the drug is from 1 to 2-3 weeks. With chronic pain syndromes, a longer course may be needed, which is determined individually and on average ranges from 3-6 weeks to 1 year.
If the recommended doses are exceeded, the following are possible: nausea, vomiting, arterial hypotension, dizziness, drowsiness, miosis, anxiety, respiratory failure, coma Treatment: cancel the drug, rinse the stomach, take activated charcoal, urgently consult a doctor. The forced diuresis is shown. There is no specific antidote.
Side effect
From the side of the central nervous system: drowsiness, weakness, dizziness, dry mouth; rarely - sleep disorders, hallucinations.
From the side of the musculoskeletal system: rarely - muscle weakness.
From the digestive system: rarely - nausea, gastrointestinal disorders, transient increase in the activity of hepatic transaminases; very rarely - acute hepatitis.
From the side of the cardiovascular system: often - a decrease in blood pressure, bradycardia.
Others: fatigue, rarely - allergic reactions (itching, rash, urticaria).
In case of any undesirable phenomena, you should consult your doctor!

I especially want to highlight the moment of pregnancy and lactation! Muscle relaxants relax muscles by acting on the central nervous system, that is, on the brain, so no matter how bad it is, you should not take them in pregnancy, and in lactation only if you stop feeding, because excreting with milk can negatively affect the health of the baby.

In action.

In the complex treatment it helped quite well. I limped every day less and less.

Finally released after physiotherapy.

But until now I am periodically worried about my leg, then the massage therapist overdoes it, then workouts, but I try to give my leg a rest, magnetotherapy also saves.

Application by her husband.

He held out with his back to hernias! It used to get so tight on my back that I could barely walk, and you couldn't lure me to the doctor. I had to stab him with Naklofen, give him the remains of Tizalud. The exacerbation was going well. I'm afraid to go to my doctor ...

Analogs.

The original Sirdalud can be found even cheaper than Tizalud!

But I did not feel any side effects from him. Sirdalud did not suit me, oddly enough.

Mydocalm is also a muscle relaxant with the same indications. I also took it in this scheme, but at a different time.

Bottom line.

In complex therapy, it gave a very good effect without any side effects.

I will give four stars for the price only. I believe that a Ukrainian generic drug should be cheaper, if not twice, then one and a half times.

Drugs in this group are prescribed only by doctors and are available with a prescription!

Until next time! All good!

Active substance

Tizanidine

Release form, composition and packaging

Tablets from white to off-white, round, flat, with beveled edges, on one side of the line and the code "OZ".

Excipients: colloidal silicon dioxide - 0.3 mg, stearic acid - 3 mg, microcrystalline cellulose - 74.412 mg, lactose - 80 mg.

Tablets from white to almost white, round, flat, with beveled edges, crossed risks on one side, on the other - the "RL" code.

Excipients: colloidal silicon dioxide - 0.4 mg, stearic acid - 4 mg, microcrystalline cellulose - 101.024 mg, lactose - 110 mg.

10 pieces. - blisters (3) - cardboard packs.

pharmachologic effect

Tizanidine is a centrally acting muscle relaxant. The main point of application of its action is in the spinal cord. By stimulating presynaptic α 2 receptors, tizanidine inhibits the release of excitatory amino acids that stimulate N-methyl-D-aspartate receptors (NMDA receptors). As a result, at the level of intermediate neurons of the spinal cord, the polysynaptic transmission of excitation is suppressed. Since it is this mechanism that is responsible for excess muscle tone, then when it is suppressed, muscle tone decreases. In addition to the muscle relaxant properties, tizanidine also has a moderate central analgesic effect.

Sirdalud is effective both for acute painful muscle spasm and 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.

The muscle relaxant effect (measured on the Ashworth scale and using the "pendulum" test) and side reactions (decrease in heart rate and blood pressure) of the drug Sirdalud depend on the concentration of the drug in the blood.

Pharmacokinetics

Suction

Tizanidine is absorbed quickly and almost completely. C max in plasma is reached approximately 1 hour after taking the drug. Due to the pronounced metabolism during the "first pass" through the liver, the average bioavailability is about 34%.

Cmax of tizanidine is 12.3 ng / ml and 15.6 ng / ml after single and multiple doses of tizanidine at a dose of 4 mg, respectively.

Simultaneous food intake does not affect the pharmacokinetics of tizanidine (when using 4 mg in the form of tablets or 12 mg in the form of modified-release capsules).

Simultaneous food intake does not affect the pharmacokinetics of tizanidine (when using the drug in the form of 4 mg tablets). Despite the fact that the C max value increases by 1/3 when taken after meals, this is not clinically significant. There is no significant effect on absorption (AUC). Tizanidine in the dose range from 1 mg to 20 mg is characterized by linear pharmacokinetics.

Distribution

The average V d in equilibrium with intravenous administration is 2.6 l / kg. Plasma protein binding is 30%.

Metabolism

Tizanidine is rapidly and largely (about 95%) metabolized in the liver. In vitro, tizanidine is mainly metabolized by the CYP1A2 isoenzyme. The metabolites are inactive.

Withdrawal

The average T 1/2 of tizanidine from the systemic circulation is 2-4 hours. It is excreted mainly by the kidneys (approximately 70% of the dose) in the form of metabolites; the unchanged substance accounts for about 4.5%.

Pharmacokinetics in special clinical situations

Have patients with impaired renal function(CC ≤ 25 ml / min) C max of tizanidine in blood plasma is 2 times higher than in healthy volunteers, the final T 1/2 reaches 14 hours, which leads to an increased (approximately 6 times) systemic bioavailability of tizanidine (measured by AUC ).

Specific studies in patients with impaired liver function was not carried out. Since tizanidine is predominantly metabolized in the liver by the CYP1A2 isoenzyme, impaired liver function may lead to an increase in systemic exposure to the drug.

Pharmacokinetic data for patients over 65 years old limited.

Floor does not affect the pharmacokinetic properties of tizanidine.

Influence ethnicity and race on the pharmacokinetics of tizanidine has not been studied.

Indications

Painful muscle spasm:

- associated with static and functional diseases of the spine (cervical and lumbar syndromes);

- after surgical interventions (for example, for a herniated disc or osteoarthritis of the hip joint).

Spasticity of skeletal muscles in neurological diseases, including:

- with multiple sclerosis, chronic myelopathy, degenerative diseases of the spinal cord;

- with the consequences of disorders of cerebral circulation;

- with the consequences of cerebral palsy (patients over 18 years old).

Contraindications

- hypersensitivity to tizanidine or to any other component of the drug;

- severe liver dysfunction;

- simultaneous use with strong inhibitors of the isoenzyme CYP1A2, such as fluvoxamine or;

- patients under 18 years of age (since the experience of using the drug in this category of patients is limited).

WITH caution it is recommended to use the drug in patients over 65 years of age, patients with impaired renal function, patients with moderate liver dysfunction; concomitantly with drugs that prolong the QT interval (for example, cisapride, azithromycin).

Dosage

Sirdalud has a narrow therapeutic index and high variability in the concentration of tizanidine in the blood plasma of patients, therefore, a careful selection of the dose is required.

The dose and dosage regimen should be selected individually, depending on the needs of the patient. The use of the drug at an initial dose of 2 mg 3 times / day reduces the risk of side effects.

The drug is taken orally. The 2 mg and 4 mg tablets can be divided into two equal portions.

At painful muscle spasm Sirdalud is usually used at a dose of 2 mg or 4 mg 3 times / day. In severe cases, an additional 2 mg or 4 mg can be taken (preferably at bedtime due to possible increased drowsiness).

At skeletal muscle spasticity due to neurological disease 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. As a rule, the optimal therapeutic effect is achieved with a daily dose of 12 to 24 mg, divided into 3 or 4 doses at regular intervals. Do not exceed a dose of 36 mg / day.

Experience of using the drug Sirdalud in patients aged 65 and over

Treatment patients with renal insufficiency (CC less than 25 ml / min) it is recommended to start with a dose of 2 mg 1 time / day. Increasing the dose is carried out in small "steps", taking into account the tolerance and effectiveness. If it is necessary to achieve a more pronounced effect, it is recommended to first increase the dose applied 1 time / day, after which the frequency of application is increased.

patients with severe liver dysfunction contraindicated. Have patients with moderate liver dysfunction the drug should be used with caution; it is recommended to start therapy with a minimum dose, with a gradual increase until an optimal balance of tolerance and effectiveness of therapy is achieved. Recommendations for monitoring liver function indicators are indicated in the "Special instructions" section.

Interruption of treatment

When discontinuing therapy with Sirdalud in order to reduce the risk of developing rebound arterial hypertension and tachycardia, the dose should be slowly reduced until the drug is completely discontinued, especially in patients receiving high doses of the drug for a long time.

Side effects

When taking the drug in small doses recommended for the relief of painful muscle spasm, drowsiness, increased fatigue, dizziness, dry mouth, decreased blood pressure, nausea, gastrointestinal disorders, increased activity of hepatic transaminases were noted. Typically, the above adverse reactions are mild and transient.

When taken at the higher doses recommended for the treatment of spasticity, the above adverse reactions (ADRs) are more frequent and more pronounced, but they are rarely so severe that discontinuation of the drug is required. In addition, the following phenomena may occur: bradycardia, muscle weakness, insomnia, sleep disturbances, hallucinations, hepatitis.

HP are grouped according to the MedDRA organ and organ system classification, and within each group are listed in decreasing order of frequency. Definition of categories of frequency of HP: very often (≥1 / 10); often (≥1 / 100,<1/10); нечасто (≥1/1000, <1/100); редко (≥1/10 000, <1/1000); очень редко (<1/10 000), включая отдельные сообщения.

From the nervous system: very often - drowsiness, dizziness.

From the side of the psyche: often - insomnia, sleep disturbances.

On the part of the cardiovascular system: often - a decrease in blood pressure (in some cases, pronounced, up to collapse and loss of consciousness); infrequently - bradycardia.

From the digestive system: very often - gastrointestinal disorders, dry mouth; often nausea.

From the musculoskeletal system: very often - muscle weakness.

General disorders: very often - increased fatigue.

Laboratory indicators: often - an increase in the activity of hepatic transaminases.

With a sharp withdrawal of the drug Sirdalud after prolonged treatment and / or taking high doses of the drug (as well as after simultaneous use together with antihypertensive drugs), the development of tachycardia and an increase in blood pressure were noted, which in some cases could lead to an acute violation of cerebral circulation, therefore, the dose of the drug Sirdalud should be reduced gradually until complete withdrawal of the drug.

Selected reports of HP based on clinical application data

Since in the post-registration period reports of HP come voluntarily from a population of uncertain size, it is not possible to reliably estimate the frequency of their occurrence ( frequency is unknown).

From the immune system: hypersensitivity reactions, including anaphylactic reactions, angioedema and urticaria.

From the side of the psyche: hallucinations, confusion.

From the nervous system: dizziness.

On the part of the organ of vision: blurred vision.

From the liver and biliary tract: hepatitis, liver failure.

On the part of the skin and subcutaneous tissues: skin rash, erythema, pruritus, dermatitis.

General disorders: asthenia, withdrawal syndrome.

If any of the side effects indicated in the instructions are aggravated, or the patient has noticed any other side effects not specified in the instructions, he should inform the doctor about it.

Overdose

To date, there have been several reports of an overdose of the drug Sirdalud, including a case when the dose was 400 mg. In all cases, the recovery was uneventful.

Symptoms: nausea, vomiting, decreased blood pressure, prolongation of the QT interval, dizziness, drowsiness, miosis, anxiety, respiratory depression, coma.

Treatment: to remove tizanidine from the body, repeated intake of activated carbon is recommended. Forced diuresis may also speed up the elimination of Sirdalud. In the future, symptomatic treatment is carried out.

Drug interactions

With the simultaneous use of the drug Sirdalud with inhibitors of cytochrome CYP1A2, it is possible to increase the concentration of tizanidine in the blood plasma. In turn, an increase in the concentration of tizanidine in plasma can lead to symptoms of drug overdose, incl. lengthening of the QT interval c.

The simultaneous use of the drug Sirdalud with inducers of CYP1A2 can lead to a decrease in the concentration of tizanidine in plasma. Reduced plasma levels of tizanidine can lead to a decrease in the therapeutic effect of Sirdalud.

Contraindicated combinations of the drug Sirdalud

Concomitant use of tizanidine with fluvoxamine or ciprofloxacin, which are inhibitors of cytochrome CYP1A2, is contraindicated.

When using the drug Sirdalud with fluvoxamine or ciprofloxacin, there is a 33-fold and 10-fold increase in the AUC of tizanidine, respectively. The result of the combined use may be a clinically significant and prolonged decrease in blood pressure, accompanied by drowsiness, dizziness, a decrease in the speed of psychomotor reactions (in some cases, up to collapse and loss of consciousness).

It is not recommended to prescribe tizanidine together with other inhibitors of the CYP1A2 isoenzyme - antiarrhythmic drugs (, mexiletine, propafenone), cimetidine, some fluoroquinolones (enoxacin, pefloxacin, norfloxacin), rofecoxib, oral contraceptives, ticlopidine.

Combinations of the drug Sirdalud requiring caution

Care must be taken when using Sirdalud together with drugs that prolong the QT interval (for example, cisapride, amitriptyline, azithromycin).

Antihypertensive drugs

The simultaneous appointment of the drug Sirdalud with antihypertensive drugs, including diuretics, can sometimes cause a pronounced decrease in blood pressure (in some cases up to collapse and loss of consciousness) and bradycardia.

With a sharp withdrawal of the drug Sirdalud after using it together with antihypertensive drugs, the development of tachycardia and an increase in blood pressure were noted, which in some cases can lead to acute cerebrovascular accident.

Rifampicin

The simultaneous administration of the drug Sirdalud and rifampicin leads to a 50% decrease in the concentration of tizanidine in the blood plasma. As a result, the therapeutic effect of the drug Sirdalud may decrease, which may be of clinical significance for some patients. Long-term combined use of rifampicin and tizanidine should be avoided; if it is impossible, careful selection of the dose of tizanidine (increase) is recommended.

Other medicines

Sedatives, sleeping pills (benzodiazepine, baclofen), and other drugs such as antihistamines can also increase the sedative effect of tizanidine.

You should avoid taking the drug Sirdalud with other agonists of α 2 -adrenergic receptors (for example, clonidine) due to the potential increase in the hypotensive effect.

Smoking

The systemic bioavailability of Sirdalud in male smokers (more than 10 cigarettes per day) is reduced by about 30%. Long-term therapy with the drug Sirdalud of smoking men may require higher doses than the average therapeutic.

Alcohol

During therapy with Sirdalud, alcohol should be avoided, because it can increase the likelihood of developing adverse events (for example, a decrease in blood pressure and lethargy). Sirdalud can enhance the inhibitory effect of ethanol on the central nervous system.

special instructions

Arterial hypotension can occur against the background of the use of the drug Sirdalud, as well as as a result of drug interactions with CYP1A2 inhibitors and / or. A pronounced decrease in blood pressure can lead to loss of consciousness and collapse.

Cases of liver dysfunction associated with tizanidine have been reported, but these cases have been rare with a daily dose of 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 in a daily dose of 12 mg or more, as well as in cases where clinical signs are observed that suggest liver dysfunction. - such as unexplained nausea, anorexia, feeling tired. In the case when the activity of ALT and AST in the serum persistently exceeds the VGN by 3 times or more, the use of the drug Sirdalud should be discontinued.

Influence on the ability to drive vehicles and mechanisms

Patients who experience drowsiness while using the drug should be advised to refrain from activities that require a high concentration of attention and quick reactions, such as driving vehicles or working with machines and mechanisms.

Pregnancy and lactation

Since no controlled studies have been conducted on the use of tizanidine in pregnant women, it should not be used during pregnancy unless the potential benefit outweighs the potential risk.

In animal studies, no teratogenicity phenomena have been identified. When used in doses of 10 and 30 mg / kg / day in animals, an increase in gestational age was noted, cases of prenatal and postnatal fetal loss, as well as fetal growth retardation were recorded. When using the above doses, females showed pronounced signs of muscle relaxation and sedation. Based on body surface area, the indicated doses exceeded the maximum recommended dose for humans (0.72 mg / kg / day) by 2.2 and 6.7 times.

In animal studies, tizanidine was excreted in small amounts in milk from lactating females. Sirdalud should not be used during lactation (breastfeeding), because there is no data on the penetration of tizanidine into human breast milk.

Contraception. Patients with preserved reproductive potential should be informed about the adverse effects of the drug on the developing fetus, identified in animal studies. During the use of the drug, as well as within 1 day after discontinuation of the drug, patients with preserved reproductive potential should use reliable methods of contraception (with correct and prolonged use of which the frequency of pregnancy is<1%).

Pregnancy test. Before starting the use of the drug Sirdalud in patients with preserved reproductive potential, it is recommended to obtain a pregnancy test result.

Impact on fertility. In animal studies, there was no adverse effect on fertility in males and females when using tizanidine at a dose of 10 mg / kg / day. There was a decrease in fertility in males receiving tizanidine at a dose exceeding 30 mg / kg / day, and in females at a dose exceeding 10 mg / kg / day. Based on body surface area, the indicated doses exceeded the maximum recommended dose for humans (0.72 mg / kg / day) by 2.2 and 6.7 times. Maternal behavioral effects and clinical signs, including marked sedation, weight loss, and ataxia, were observed with these doses.

Childhood use

Experience with the drug in patients under 18 years of age is limited. The use of the drug Sirdalud in this category of patients is not recommended.

With impaired renal function

Treatment patients with renal insufficiency (CC less than 25 ml / min) it is recommended to start with a dose of 2 mg 1 time / day. Increasing the dose is carried out in small "steps", taking into account the tolerance and effectiveness. If it is necessary to obtain a more pronounced effect, it is recommended to first increase the dose prescribed 1 time / day, after which the frequency of administration is increased.

For violations of liver function

The use of the drug Sirdalud in patients with severely impaired liver function contraindicated. Have patients with moderately severe liver dysfunction the drug should be used with caution; it is recommended to start therapy with a minimum dose, with a gradual increase until an optimal balance of tolerance and effectiveness of therapy is achieved.

Use in the elderly

Experience of using Sirdalud at patients aged 65 years and older limited. It is recommended to start therapy with a minimum dose with a gradual increase until the optimal balance of tolerance and effectiveness of therapy is achieved.

Conditions of dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

The drug should be stored out of the reach of children at a temperature not exceeding 25 ° C. The shelf life is 5 years.

They are considered extremely popular, and people, both old and young, are susceptible to them. One of the most common and effective medications for therapy is Sirdalud. The medicine helps to eliminate muscle spasm, get rid of pain, restore blood flow in soft tissues. Reception Sirdalud must be coordinated with a specialist. The drug has a strong effect on internal organs and can cause significant harm if used improperly.

The medicine is available for purchase at any pharmacy. It is produced mainly in tablet form. They are gray or white, often round in shape. The preparation contains an active ingredient - tizanidine hydrochloride. Taking into account the type of agent, tizanidine is added in an amount of 2 or 4 mg.

Tablets 2 and 4 mg are almost identical, with a difference in the code (OZ and RL). The composition of the drug also includes additional components necessary for more effective assimilation of tizanidine. In addition, it is possible to find Sirdalud in capsules in pharmacies.

Pharmacological effects

Sirdalud is classified as a muscle relaxant of central action, with the main active ingredient tizanidine. Thanks to its effect, the excitation between neurons in the spinal cord, which is a provoking factor of muscle hypertonicity, is reduced.

The muscle relaxant Sirdalud helps to relax the striated muscles in the patient's musculoskeletal system, and has a moderate anesthetic effect.

Sirdalud reduces the number of chronic seizures, eliminates spasms. A muscle relaxant is actively used in the treatment of neurological pathological processes of a spastic nature; it is also suitable for the acute and chronic phases of diseases. After entering the body, the muscle relaxant is rapidly and fully absorbed, reaching maximum concentration values ​​at the cellular plasma level after 60 minutes.

Indications for use

Reception of Sirdalud is justified when it is necessary to reduce tension in the smooth muscles of the skeleton and eliminate cramps. The key feature of the drug will be that the drug provides effective relaxation of the spinal cord, does not adversely affect the functioning of the central nervous system. Since the main purpose of the drug will be a muscle relaxant effect on the spinal cord, the main testimony to its application will be:

• Spinal hernia with pinched nerve.
• Spasm in the muscles, which is caused by diseases of the spine (spondylosis, osteochondrosis, hemiplegia).
• Neurological disorders that provoke spasm of cross-striated and smooth muscles (sclerosis, cerebral palsy, cerebral hemorrhage, convulsions, failure in the blood flow of the brain).
• Osteoarthritis of the hip.

Sirdalud is prescribed for sclerotic prostatitis. It is one of the most difficult types of the disease, which is associated with a pronounced staging. The drug makes it possible to get rid of unpleasant symptoms, normalize urination, and improve erectile function. In addition, the course use helps to slow down the formation of the pathological process during complex treatment.

Application rules, dosage

When a specialist prescribes a minimum dose of a drug of 2 mg three times a day, there is no likelihood of side effects with negative reactions.

Sirdalud therapy is carried out under the direct control of the functioning of the cardiovascular system: measurements of blood pressure, ECG, laboratory blood and urine tests.

The appointment and dosage of a muscle relaxant is selected by the doctor on an individual basis, taking into account the course of the underlying disease, age indicators that accompany the pathological process:

• When discomfort during muscle spasm is pronounced - up to 4 mg 3 times a day.
• In case of neurological disorders with spasticity of the skeletal muscles - 3 doses of Sirdalud, the total concentration of the drug at the initial stage of therapy does not exceed a daily dose of 6 mg. The dosage is increased by 2-4 mg gradually, at intervals.
• To achieve an optimal therapeutic effect, the daily dose is prescribed in the range of 12-26 mg. An increase in the concentration of muscle relaxant more than 36 mg is prohibited.
• Patients in old age are advised to start therapy with Sirdalud with the lowest dosage, which increases over time until the proper therapeutic effect is achieved.

In order to avoid the formation of rebound hypertension with a rapid heartbeat from the withdrawal of the drug, the dose is gradually reduced at the end of therapy. In particular, this is carried out in patients who have been taking the agent in question for a long time. When, during therapy, the patient observes drowsiness, low blood pressure, he needs to refrain from performing work duties that require concentration.

Contraindications for use

There are certain contraindications to the use of this medication:

• significant violations of the liver;
• simultaneous use with fluvoxamine;
• hypersensitivity to tizanidine or to other components of the drug.

Since no studies have been conducted on the use of tizanidine during pregnancy, it is best not to use it at this stage. As an exception, there may be situations where the likely effect will increase the potential risk. Tizanidine is excreted in mother's milk in a small amount. However, it is not recommended to use the drug while breastfeeding.

At the moment, it is not known how Sirdalud affects the child's body. Therefore, persons under the age of 18 should not be treated with such a remedy. It is optimal to use analogs of such a medicine, which are more safe for the baby's body. Analogs of this drug are selected directly by a specialist.

In addition, the drug should be used with extreme caution in the elderly and people with liver problems or kidney failure. Sirdalud is absorbed by the liver, and excreted through the kidneys. Therefore, patients with such pathological processes should consult a specialist before using a medication.

Side effects

During the use of a drug in an insignificant content for a medicinal effect in pathological processes that are associated with muscle cramps, side effects are not formed.

Occasionally, nausea, disruptions in the functioning of the gastrointestinal tract, and an increase in liver activity develop. Drowsiness, dryness in the oral cavity, weakness, low blood pressure, and dizziness are often formed.

When the agent is prescribed in a higher concentration to eliminate spasticity, the negative effect is more pronounced and is formed much more often.

However, this effect does not mean giving up the use of pills. Often, patients develop arterial hypotension, heart rhythm disturbances. Rare manifestations also include hallucinations, sleep disturbances, insomnia, and muscle weakness. Acute hepatitis is extremely rare.

Interaction

Persons who have begun to use the medicine need to remember that taking Sirdalud and alcoholic beverages is prohibited. Alcohol can not only reduce the effectiveness of the effect of the drug, but also significantly increase side effects.

In addition, in the process of undergoing therapy, it is optimal to abandon transport control and work with complex mechanisms. This is due to the fact that the active components of the drug are capable of provoking weakness and apathy. It also lowers blood pressure and causes muscle weakness.

Sirdalud can be used with other medications. Vinpocetine and Sirdalud can be taken together if prescribed by a specialist. Medicines have various effects on the body and contribute to the fastest recovery.

Sirdalud and Movalis are referred to as muscle relaxants. Movalis is considered Sirdalud's deputy, but the second agent is more harmless to the patient. Medicines are prescribed in combination, but you need to carefully calculate the dose.

Price for Sirdalud

The drug Sirdalud in tablet form is sold in pharmacies directly on the prescription of the attending physician. Cost is the best value for money. Therefore, the agent in question is quite popular, and is often recommended for therapeutic purposes. Price preparation of 2 mg of active substance is approximately 250 r., 4 mg -350 r.

Sirdalud: analogues are cheaper

Given that the medication is quite expensive, patients can use cheaper analogs drugs that help to save the family budget and eliminate their own diseases. They have approximately the same muscle relaxant effect:

• Baclofen
• Midocalm.
• Miorix.

To determine the optimal remedy in terms of effectiveness and in order to avoid side effects, contraindications, and other factors, it is required to carry out a comparative analysis of each remedy, having become familiar with its features and properties.

Baclofen or Sirdalud - which is more effective?

Baclofen will be the active ingredient in this remedy. The use of a drug in large quantities can cause depression of the central nervous system. Like Sirdalud, Baclofen is quickly absorbed into the stomach, reaching a significant therapeutic effect in a short period of time.

The medication is prohibited from taking in the presence of a peptic ulcer during an exacerbation, with personal susceptibility to the active component. Baclofen is considered a highly addictive narcotic drug. Exceeding the dosage leads to dangerous complications, and in some situations - to respiratory arrest and death, therefore it can be used only on the recommendation of a doctor, strictly following the recommended dosage.

Sirdalud orMidocalm - what's the difference?

Mydocalm includes the active ingredient - tolperisone chloride, and the active ingredient of Sirdalud - tizanidine. The main advantage of Mydocalm will be the absence of a sedative effect when taking the medicine. The pluses of Sirdalud include higher availability. Contraindications to use are under 3 years of age, myasthenia gravis, personal susceptibility to the drug.

Miorix orSirdalud - which is better?

The tool helps to relieve muscle spasm, accompanied by intense pain in the musculoskeletal system. It is prescribed as an auxiliary drug for limited physical activity and physical education. Miorix increases muscle tone, helps to get rid of conditions that provoke spasm (discomfort, stiffness in movement, hypersensitivity). Based on this, we can conclude that Miorix has the same therapeutic effect, and what is better - the doctor will advise in each case.

Tizalud andSirdalud - what to choose for osteochondrosis?

The muscle relaxant is made from tizanidine hydrochloride in tablet form. Tizalud has a central effect, is characterized by a high therapeutic effect, and is well accepted by patients. Its use is recommended for muscle spasm with severe discomfort in pathologies of a neurological nature: degenerative changes, circulatory disorders of the brain, sclerosis, myelopathy. Tizalud is recommended for the treatment of diseases of the musculoskeletal system, in the postoperative period.

Tizalud can be prescribed together with Sirdalud, but only after prior consultation with a doctor. An analogue is more often prescribed in the acute period of osteochondrosis, since it is slightly stronger than Sirdalud.

Preparations containing Tizanidine (Tizanidine, ATC code M03BX02):

Frequent release forms (more than 100 proposals in Moscow pharmacies)
Name	Release form	Packing, pcs	Manufacturer country	Price in Moscow, r	Offers in Moscow
	2mg tablets	30	Germany and Turkey, Novartis	190- (average 224) -258	753↗
Sirdalud - original	4mg tablets	30	Germany and Turkey, Novartis	162- (average 328) -381	783↗
Sirdalud MR - original	sustained release capsules 6mg	30	Spain, Novartis	442- (average 547) -633 / td>	430↗
Tisalud	2mg tablets	30	Russia, Veropharm	96- (average 128) -149	132↗
Tisalud	4mg tablets	30	Russia, Veropharm	143- (average 179) -223	123↗
Rarely found forms of release (less than 100 proposals in Moscow pharmacies)
Tisanil	2mg tablets	30	India, Simpex	140- (average 165) -198	75↘
Tisanil	4mg tablets	30	India, Simpex	170- (average 245) -298	45↘
Tisanil	6mg tablets	30	India, Simpex	327	1↘

Sirdalud MR (original Tizanidine with modified release) - official instructions for use. Prescription drug, information is intended only for healthcare professionals!

Clinical and pharmacological group:

Muscle relaxant of central action

pharmachologic effect

Muscle relaxant of central action. The main point of application of its action is in the spinal cord. By stimulating presynaptic β 2 receptors, tizanidine inhibits the release of excitatory amino acids that stimulate receptors that are sensitive to N-methyl-D-aspartate (NMDA receptors). As a result, at the level of intermediate neurons of the spinal cord, the polysynaptic transmission of excitation is suppressed. Since it is this mechanism that is responsible for excess muscle tone, then when it is suppressed, muscle tone decreases. In addition to the muscle relaxant properties, tizanidine also has a moderately pronounced 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 of the Cmax value when taking Sirdalud® tablets in the same daily dose, divided into 3 doses, while the total exposure (AUC) remains unchanged.

Distribution

Prolonged release of tizanidine from the modified release capsule dosage form causes a "softened" pharmacokinetic profile, which ensures the maintenance of a stable therapeutic plasma concentration of tizanidine for 24 hours.

Plasma protein binding is 30%.

Metabolism

Tizanidine is rapidly and largely metabolized in the liver. In vitro it has been shown that tizanidine is mainly metabolized by the isoenzyme CYP1A2. The metabolites are inactive.

Withdrawal

Tizanidine is excreted mainly by the kidneys (approximately 70% of the dose) as metabolites; the unchanged substance accounts for only about 2.7%.

Pharmacokinetics in special clinical situations

Gender does not affect the pharmacokinetic parameters of tizanidine.

Indications for use of the drug SIRDALUD® MR

• spasticity of skeletal muscles in neurological diseases (for example, in multiple sclerosis, chronic myelopathy, degenerative diseases of the spinal cord, the consequences of cerebrovascular accidents and cerebral palsy / patients over 18 years of age /).

Dosage regimen

The drug is administered 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 ("in steps") increased by 6 mg (1 capsule) at intervals of 3-7 days. Clinical experience shows that for most patients, the optimal dose is 12 mg per day (2 capsules); in rare cases, it may be necessary to increase the daily dose to 24 mg.

Treatment of patients with renal impairment (CC< 25 мл/мин) рекомендуется начинать с приема препарата Сирдалуд® в дозе 2 мг 1 раз в сутки. Повышение дозы проводят малыми "шагами", с учетом переносимости и эффективности. Если необходимо получить более выраженный эффект, рекомендуется сначала увеличить дозу, назначаемую 1 раз в сутки, после чего увеличивают кратность назначения.

Side effect

Adverse reactions are distributed according to the frequency of occurrence. To assess the incidence of adverse reactions, the following criteria were used: very often (> 10%); often (from> 1% to<10%); иногда (от >0.1% to<1%); редко (от >0.01% before<0.1%); очень редко (<0.01%, включая отдельные сообщения). В одной группе по частоте возникновения нежелательные реакции ранжированы по степени значимости.

From the side of the nervous system: often - drowsiness, weakness, dizziness; rarely - hallucinations, insomnia, sleep disturbances.

From the side of the cardiovascular system: often - bradycardia, lowering 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 hepatic transaminases; very rarely - hepatitis, liver failure.

From the musculoskeletal system: rarely - muscle weakness.

Others: often - increased fatigue.

When taken in small doses, recommended for the relief of painful muscle spasm, drowsiness, increased fatigue, dizziness, dry mouth, decreased blood pressure, nausea, gastrointestinal disorders, increased activity of hepatic transaminases were noted. Usually, the above reactions are mild and transient.

When taken at the higher doses recommended for the treatment of spasticity, the above adverse reactions are more frequent and more severe, but they are rarely so severe that treatment has to be interrupted. In addition, the following phenomena may occur: lowering blood pressure, bradycardia, muscle weakness, insomnia, sleep disturbances, hallucinations, hepatitis.

Contraindications to the use of SIRDALUD® MR

• severe liver dysfunction;
• simultaneous use with strong inhibitors of CYP1A2 isoenzymes (including fluvoxamine or ciprofloxacin);
• hypersensitivity to tizanidine or to any other component of the drug.

Use of the drug SIRDALUD® MR during pregnancy and breastfeeding

Since no controlled studies have been conducted on the use 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 amounts. However, women who are breastfeeding children should not use the drug.

Application for violations of liver function

Contraindicated in severe liver dysfunction.

Application for impaired renal function

Sirdalud® MR should be used with caution in patients with renal insufficiency.

Use in elderly patients

Use in children under 12 years of age

special instructions

Cases of liver dysfunction associated with tizanidine have been reported, but these cases have been rare with a daily dose of 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 in a daily dose of 12 mg or more, as well as in cases where clinical signs are observed that suggest liver dysfunction. such as unexplained nausea, anorexia, feeling tired. When serum ALT and AST levels are persistent

Cases of liver dysfunction associated with tizanidine have been reported, but these cases have been rare with a daily dose of 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 in a daily dose of 12 mg or more, as well as in cases where clinical signs are observed that suggest liver dysfunction. such as unexplained nausea, anorexia, feeling tired. In the case when the levels of ALT and AST in serum persistently exceed VGN by 3 times or more, the use of Sirdalud MR should be discontinued.

Sirdalud® MR should not be abruptly canceled, the dose of the drug should be reduced gradually.

With a sharp cancellation of Sirdalud MR 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 were noted, in some cases, which could lead to acute cerebrovascular accident.

Caution should be exercised when using Sirdalud MR in patients with renal insufficiency. When using Sirdalud MR in patients with renal insufficiency (CC less than 25 ml / min), correction of the dosage regimen is necessary.

Caution should be exercised when using Sirdalud MR in elderly patients. The experience of using 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

The experience of using the drug in children is limited. Therefore, the use of Sirdaluda MR in this category of patients is not recommended.

Influence on the ability to drive vehicles and use mechanisms

With the development of drowsiness, dizziness or a decrease in blood pressure during therapy with Sirdalud MR, one should refrain from types of work that require a high concentration of attention and a quick reaction, for example, driving vehicles or working with mechanisms.

Overdose

To date, there have been several reports of an overdose of Sirdalud MR, including a case when the dose 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, multiple gastric lavage and the appointment of activated carbon are recommended. Forced diuresis may also speed up the elimination of tizanidine. In the future, symptomatic therapy is carried out.

Drug interactions

When using Sirdalud MR together with inhibitors of the isoenzyme CYP1A2, an increase in the concentration of tizanidine in the blood plasma is possible.

The simultaneous use of tizanidine with fluvoxamine or ciprofloxacin, inhibitors of the isoenzyme 1A2 of cytochrome P450, leads, respectively, to a 33-fold or 10-fold increase in the AUC of tizanidine. The result of the combined use may be a clinically significant and prolonged decrease in blood pressure, leading to drowsiness, weakness, inhibited psychomotor reactions (in some cases, up to collapse and loss of consciousness). Concomitant use of tizanidine with fluvoxamine or ciprofloxacin is contraindicated.

The simultaneous appointment of tizanidine with other inhibitors of the CYP1A2 isoenzyme - antiarrhythmic drugs (amiodarone, mexiletine, propafenone), cimetidine, fluoroquinolones (enoxacin, pefloxacin, ciprofloxacin, norfloxacin), rofecoxibracepidom, peroral, oral contraceptives is not recommended.

With an increase in the concentration of tizanidine in the blood plasma, it is possible to lengthen the QTc interval, which is characteristic of drug overdose.

The simultaneous appointment of Sirdalud MR with antihypertensive drugs, including diuretics, can sometimes cause a decrease in blood pressure (in some cases up to collapse and loss of consciousness) and bradycardia.

Ethanol or sedatives can enhance the sedative effect of Sirdalud MR, therefore, simultaneous use with other sedatives and / or alcohol is not recommended.

Conditions of 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 is 3 years.

Indications for use of the drug Sirdalud in a dosage of 2 and 4 mg:

Spastic state of skeletal muscles caused by neurological diseases (multiple sclerosis, chronic myelopathy, stroke, degenerative diseases of the spinal cord). Painful spasm of skeletal muscles caused by damage to the spine (cervical and lumbar syndromes) or arising after surgery (for a herniated disc or osteoarthritis of the hip).

Dosage regimen for Sirdalud 2 and 4mg tablets

To stop painful spasm of skeletal muscles, use 2-4 mg 3 times a day; in severe cases, it is additionally recommended to take 2-4 mg at night. For spastic muscle conditions caused by neurological diseases, the initial dose is 6 mg per day in 3 divided doses. The dose is gradually increased by 2-4 mg per day every 3-7 days. The optimal therapeutic effect is usually achieved at a dose of 12-24 mg per day, divided into 3-4 doses. Do not exceed a dose of 36 mg per