Sirdalud: instructions for use, price and reviews. Analogues of the drug

Pharmacodynamics and pharmacokinetics

Tizanidine is a skeletal muscle relaxant whose main site of action is the spinal cord. This drug reduces the increased tone of the skeletal muscles, relieves spasms, and increases the strength of voluntary contractions. Sirdalud is effective for chronic spasticity of cerebral and spinal origin and for acute muscle spasm . In addition, it also has a mild analgesic effect.

Tizanidine is absorbed quite quickly and virtually completely. The highest level of drug concentration in plasma can be observed approximately an hour after its administration. The substance is excreted by the kidneys.

Medicine Sirdalud: instructions

For the treatment of spasticity of skeletal muscles caused by neurological pathology, 6 mg of the drug per day is prescribed. The dose is divided into three doses in equal quantities. Thus, the minimum single dose starts from 2 mg. If it is necessary to increase the therapeutic effect, the daily dose is increased gradually, adding 2 mg per day every week. Severe diseases of muscle tone are relieved with a dose of 12 to 24 mg per day. The number of receptions can be increased up to 4 times.

At the same time, you should not exceed the maximum allowable amount of 36 mg per day.

For older patients over 65 years of age, it is recommended to begin treatment with a minimum amount of Tizanidine. If 2 mg does not give the expected effect, a gradual increase in daily intake is allowed while monitoring the patient's condition. It is recommended to follow the same regimen when treating patients with impaired renal function. Eating may increase the period during which the maximum amount of Tizanidine is concentrated in the patient's blood. Therefore, take the medicine an hour after eating.

Indications for use of Sirdalud

What are Sirdalud tablets for? Indications for use are as follows:

muscle spasm , which is associated with diseases of the spine (these include lumbar and cervical syndromes), or which appeared after the intervention of a surgeon;
spasticity of skeletal muscles in the manifestation of neurological diseases ( multiple sclerosis , chronic myelopathy , cerebral palsy , degenerative diseases of the spinal cord).

Sirdalud: what is the drug prescribed for?

The reason for prescribing Sirdalud is various muscle spasms caused by diseases of the spine, including localization in the cervical lumbar region. In addition, pain after surgical reduction of intervertebral hernias is also relieved by taking Sirdalud.

If the cause of pain in the muscles is multiple sclerosis, or a congenital pathology in the form of diagnosed cerebral palsy, which causes spasticity of the muscular skeleton, Sirdalud is prescribed.

Side effects

Side effects of Sirdalud include:

dizziness , drowsiness , sleep disturbances , insomnia ;
bradycardia , decreased blood pressure;
stomach upsets , nausea , dry mouth ;
increased fatigue, muscle weakness ;
increased activity of liver transaminases.

As a result of abrupt cessation of taking Sirdalud after a long period of treatment, tachycardia and increased blood pressure may develop, which can lead to impaired blood circulation in the brain, so the dose of the drug should be reduced gradually, until it is completely discontinued.

As a result of clinical studies, the following adverse events were identified, the frequency of which was not identified:

confusion , hallucinations , vertigo ;
blurred vision;
liver failure , hepatitis ;
withdrawal syndrome , asthenia .

Sirdalud in the treatment of chronic headache

About the article

8933

Regular issues of "RMZh" No. 22 dated November 19, 2004 p. 1250

Category: Neurology

Author: Kalashnikova L.A.

For quotation:

Kalashnikova L.A. Sirdalud in the treatment of chronic headache. RMJ. 2004;22:1250.

Sirdalud (Tizanidine hydrochloride) – an agonist? 2- (presynaptic) adrenergic receptors, blocking the release of excitatory neurotransmitters, primarily norepinephrine and aspartate in the spinal cord and brain (at the level of the blue spot - locus ceruleus). Thanks to this, Sirdalud has a muscle relaxant effect and, in addition, has an antinociceptive effect that is not associated with the effect on the central opioid system [2,4]. The drug is available in tablets of 2 and 4 mg and is used mainly to eliminate painful muscle spasms and reduce muscle spasticity observed in various neurological diseases. The central mechanism of action of the drug is associated with the effect on the structures of the brain stem (locus ceruleus), the presence of antinociceptive and muscle relaxant effects is a theoretical justification for the use of Sirdalud in the treatment of certain types of primary headaches, in the genesis of which central dysregulation of the tone of the cranial and cerebral arteries is important, tone of the pericranial muscles, as well as a decrease in the threshold of pain perception. According to the international classification of headaches (1988) and its revised version (2004), a distinction is made between primary headaches, which are independent nosologies, and secondary headaches, which are manifestations of various neurological and systemic diseases [7,8]. The two most common types of primary headaches are migraine and tension headache. The characteristic features of migraine are a moderate or severe headache, lasting from 4 to 72 hours, usually one-sided and pulsating, aggravated by movement, accompanied by nausea and/or vomiting, phono- and photophobia. Unlike migraines, tension headaches are of mild or moderate intensity, pressing or squeezing in nature, usually bilateral in localization, are not aggravated by physical activity, and are not accompanied by vomiting or severe nausea, although they may be combined with mild nausea or photo- or phonophobia. There are two subtypes of tension headache: those associated with tension in the pericranial muscles, which is recorded by palpation or electromyography; without tension of the pericranial muscles [7]. Both migraines and tension headaches can be episodic or chronic. At the same time, the chronic variant of migraine was first identified as its independent subtype only in the revised version of the international classification of headaches (2004) [8]. The most relevant is drug correction of the chronic version of migraine and tension headache. Pain is considered chronic if it bothers the patient more than 15 days a month for at least 3 months. Both types of primary chronic headache can be complicated by headache caused by excessive use of analgesics and other drugs [3]. The latter represent an independent type of cephalalgia. The relevance of the treatment of primary headaches is determined by their prevalence, the most frequent development in young and middle age, which is associated with considerable economic losses due to temporary disability. According to epidemiological studies conducted in the USA, the frequency of migraine in the population is 13% [9]. The prevalence of episodic tension-type headache reaches 38%, and chronic headache – 2% (and the latter significantly reduces the ability of patients to work) [14]. The relevance of the treatment of primary headaches is also due to the difficulties of drug correction that often arise, especially in chronic cases. In this regard, the search and use of non-traditional but pathogenetically based drugs is of great importance, one of which is Sirdalud, which affects the central brainstem regulatory mechanisms and the antinociceptive system, which are involved in the genesis of primary headaches. Special studies assessing the effectiveness of Sirdalud in the treatment of primary headaches are few. E.G. Filatova et al (1997) used Sirdalud in 32 patients with chronic tension-type headache at a daily dose of 4 and 6 mg [1]. The course of treatment was 14 days. In 75% of cases, a decrease in headache was noted, and in all cases its presence was combined with tension in the pericranial muscles. Along with this, the patients also experienced a decrease in anxiety and depression, which indicated the psychotropic effect of the drug. In addition, there was a normalization of night sleep and a decrease in autonomic disorders. When studying the nociceptive flexor reflex, the authors found an increase in its threshold, as well as in the pain threshold, which indicated an increase in the activity of the antinociceptive system. In the absence of tension in the pericranial muscles or with a high level of anxiety, there was no effect from the use of Sirlalud. Side effects included drowsiness and mild dizziness. The authors concluded that, along with antidepressants, Sirdalud plays an important role in the treatment of chronic tension-type headaches associated with pericranial muscle tension. Clinical trials conducted abroad have also shown the effectiveness of Sirdalud in the treatment of chronic headaches [5,6,11,12,13,15,16]. A double-blind placebo-controlled study conducted by R. Fogelhom et al., K. Murros (1992) [5] showed that treatment with Sirdalud at a dose of 6-18 mg per day for 6 weeks significantly reduced the intensity of chronic tension-type headache. Smaller doses of Sirdalud (3 mg per day, divided into 3 doses), according to Japanese researchers, also provide a good effect: a significant reduction in the intensity, frequency and duration of chronic tension headaches during a 4-week course of treatment was noted in 2/3 of patients [ 15,16]. It should be noted that the use of small doses of the drug is especially important in patients prone to hypotension, because Sirdalud may slightly reduce blood pressure. The reduction in chronic tension headaches noted by M. Sakuta and K. Takeda (1991) [11] in 90% of patients was accompanied by positive changes in electromyographic parameters recorded in the pericranial muscles. A preliminary study of 39 patients with chronic headaches (mainly migraine type) demonstrated the feasibility of using Sirdalud [12]. Thus, a decrease in the intensity, frequency and daily duration of headaches in the first 4 weeks of treatment was noted in 49% of patients, in 5–8 and 9–12 weeks – in 64% and 65% of patients, respectively. Moreover, at 9–12 weeks of treatment, the condition of 67% of patients improved by half compared to the baseline. The dose of the drug was increased gradually over 4 weeks and varied from 4 to 20 mg per day, averaging 13.5 mg/day. (divided into 3 doses). Side effects noted in more than 10% of patients were mild or moderate and included drowsiness, weakness, dry mouth, and rarely constipation and hyperkinesis. An increase in liver enzymes while taking Sirdalud was observed in only 1 out of 39 patients, and after cessation of treatment the indicators completely returned to normal. Preliminary data on the effectiveness, good tolerability and safety of Sirdalud were confirmed in a blinded, placebo-controlled trial that included 292 patients with primary headaches (migraine - 77%, chronic migraine headache or chronic tension-type headache - 23%) [13]. It was shown that a decrease in the frequency, duration and intensity of headaches in the first 4 weeks of treatment with Sirdalud (three times a day with a gradual increase in dose to an average daily dose of 18 mg) was observed in more than half of the cases, which was statistically significantly different from the placebo effect. Moreover, the drug was equally effective in treating all three types of primary headaches. Adverse effects were reported in more than 10% of patients and included drowsiness (47%), dizziness (24%), dry mouth (23%), asthenia (19%). The high effectiveness of the drug for various types of headaches, according to the authors, indicates the participation of? 2 adrenergic receptors in their pathophysiology, that is, consistent with the role of central mechanisms in their genesis. The possibility of using Sirdalud in combination with non-steroidal anti-inflammatory drugs in the treatment of headaches arising from excessive use of analgesics and other drugs to relieve migraine attacks (drug-dependent headache) deserves attention. As a rule, when analgesics are discontinued in these cases, the headache intensifies (rebound phenomenon). According to TR Smith (2002) [17], in these cases, the administration of Sirdalud in combination with non-steroidal anti-inflammatory drugs is effective. After 6 weeks of treatment, the effect was noted in 65% of patients, after 12 – in 69%. In contrast to the positive assessment of Sirdalud in the treatment of headaches, K. Murros et al. (2000) obtained different data [10]. Considering the effectiveness of Sirdalud in the treatment of chronic tension headaches, in a randomized, double-blind, placebo-controlled study, the authors unexpectedly obtained a pronounced placebo effect. Thus, the effectiveness of 6 mg or 12 mg of Sirdalud, taken once in the evening by 165 patients for 6 weeks, did not differ from that in patients taking placebo. The data obtained, according to the authors, confirm the significant role of psychophysiological mechanisms in the development of chronic tension-type headache. Thus, the summation of the few studies shows the effectiveness of Sirdalud in most cases of chronic headaches, primarily tension headaches involving the pericranial muscles, as well as chronic migraine. The inconsistency of the data obtained by K. Murros et al. with the rest available in the literature is apparently associated with the peculiarities of the dosage of the drug, and therefore further research is advisable.

Literature 1. Filatova E.G., Solovyova A.D., Danilov A.B Treatment of tension headaches with sirdalud. Journal of Neurology and Psychiatry named after. S.S. Korsakova 1997; No. 7; 36–38. 2. Chen D–F, Bianchetti V., Weissendanger M. Involvement of noradrenergic systems in the modulation of cutaneous reflexes. Motor disturbances I. Ed. R Benecke ea London 1987:187–195. 3. Colas R., Munoz P., Temprano R., ea Chronic daily headache with analgesic overuse: epidemiology and impact on quality of life. Neurology 2004; 62:1338–42. 4. Davis J., Johanston S.E. InhibitionbyDS103–282 of D– (3–H)–aspartate release from spinal cord slices. Br J Pharmacol 1983;78:28–30. 5. Fogelholm R., Murros K. Tizanidine in chronic tension-type headache: a placebo controlled double-blind crosses-over study. Headache 1992; 32:509–513. 6. Freitag FG Preventative treatment for migraine and tension–type headaches: do drugs having effects on muscle spasm and tone have a role? CNS Drugs. 2003; 17(6): 373–81. 7. Headache Classification Committee of the International Headache Society. Classification and Diagnostic criteria for headache disorders, cranial neuralgias and facial pain. Cephalalgia 1988; 8 (suppl 7): 1–96. 8. Headache Classification Committee of the International Headache Society. The international classification of headache disorders. Cephalalgia 2004; 24:1–160. 9. Lipton RB, Stewart WF, Diamond S. et al. Prevalence and burden of migraine in the United States: results from the American Migraine Study II. Headache 2001; 41: 646–657. 10. Murros K, Kataja M, Hedman C, Havanka H, et al. Modified–release formulation of tizanidine in chronic tension–type headache. Headache. 2000; 40(8): 633–7. 11. Sakuta M., Takeda K. Beneficial effect of tizanidine on the ischemic muscle contraction in chronic muscle contraction headache. Cephalalgia 1991; 11(suppl.11):339–340. 12. Saper JR, Lake AE 3rd, Cantrell DT, Winner PK, White JR. Chronic daily headache prophylaxis with tizanidine: a double-blind, placebo-controlled, multicenter outcome study. Headache. 2002; 42(6): 470–82. 13. Saper JR, Winner PK, Lake AE 3rd. An open–label dose–titration study of the efficacy and tolerability of tizanidine hydrochloride tablets in the prophylaxis of chronic daily headache. Headache. 2001; 41(4): 357–68. 14. Schwartz BS, Stewart WF, Simon D., Lipton RB Epidemiology of tension-type headache. JAMA 1998; 279:381–383. 15. Shimomura T., Awaki E., Takahashi K. Treatment of tension-type headache with tizanidine hydrochloride: relationship between plasma MHPG concentration and clinical effects. Cephalalgia 1991; 11 (suppl 11): 333–334. 16. Shimomura T., Awaki E., Kowa H., Takahashi K. Treatment of tension–type headache with tizanidine hydrochloride: its efficacy and relationship to the plasma MHPG concentration. Headache 1991; 31:601–604. 17. Smith TR Low–dose tizanidine with nonsteroidal anti–inflammatory drugs for detoxification from analgesic rebound headache. Headache. 2002 Mar;42(3):175–7.

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Instructions for use of Sirdalud (Method and dosage)

The medicine is taken orally, the dose is determined based on the individual characteristics of the human body. To minimize the risk of side effects, you should start with a dose of 1 tablet (2 mg) or half a tablet (4 mg) 3 times a day.

For severe muscle spasms, tablets of 2 mg or 4 mg are prescribed 3 times a day. In particularly severe cases, you can take an additional dose of 2 mg or 4 mg before bedtime.

If skeletal muscle spasticity occurs, which can be caused by neurological diseases, the initial dose is 6 mg per day, taken in 3 divided doses. The dose must be increased gradually, by 2-4 mg, over an interval of 3 to 7 days. The optimal effect is achieved when taking 12-24 mg per day 3-4 times a day. You should not take a dose higher than 36 mg per day.

Persons over 65 years of age are recommended to start taking the drug with a minimum dose, gradually increasing it to the optimal size, which will allow achieving effective therapy with minimal side effects.

Patients with impaired renal function should begin treatment with a dose of 2 mg per day at a time. The dose is increased gradually, in small steps, taking into account the effectiveness and tolerability of the drug.

Instructions for use of the drug Sirdalud MR

The drug is a capsule containing 6 mg of tizanidine. The initial dose of Sirdalud is 1 capsule per day. The dose can be gradually increased by 6 mg at intervals of 3 to 7 days. For most patients, the optimal dose is 12 mg per day. In rare cases, the dose can be increased to 24 mg (4 capsules) per day.

Injections of this drug can only be prescribed by a doctor.

Sirdalud tablets - composition and principle of action

The main substance of the product, sold under the name Sirdalud, is tizanidine in a volume of 2 mg or 4 mg. Auxiliary components are:

stearic acid;
MCC;
lactose monohydrate;
anhydrous colloidal silicon dioxide.

The drug is sold in 30 pieces per package. Each package contains 3 blisters, each containing 10 doses. One tablet can contain 2 mg or 4 mg of the active substance, which allows the doctor to prescribe an effective and safe therapeutic dose with an accuracy of 1 mg.

Tizanidine is a skeletal muscle relaxant. It mainly acts on the spinal cord, reducing the high tone of the muscular skeleton and releasing the clamped areas from spasm. An additional effect of the drug is an analgesic effect.

Tizanidine is actively absorbed in the gastrointestinal tract. After an hour, its maximum concentration in the blood is reached. The kidneys are involved in removing the substance from the body.

Sirdalud belongs to the centrally acting drugs of the muscle relaxant group.

Overdose

An overdose of Sirdalud can be expressed as follows:

decreased blood pressure;
vomiting , nausea ;
drowsiness , dizziness , anxiety, miosis ;
coma , respiratory failure.

Treatment: repeated intake of activated charcoal and forced diuresis will speed up the removal of the drug from the body. After removal, symptomatic treatment is carried out.

Overdose of Sirdalud

If the patient was unjustifiably prescribed the maximum dose of the drug, or he independently increased the number of doses, the following adverse reactions caused by an overdose may be observed:

vomit;
drowsiness;
loss of coordination;
dizziness;
decrease in systolic pressure;
miosis;
respiratory rhythm disturbances.

Significantly exceeding the maximum permissible daily dosage can put the patient into a coma.

Interaction

Concomitant use of the drug with inhibitors of cytochrome CYP1A2 leads to an increase in plasma levels of tizanidine, which in turn leads to overdose symptoms. Simultaneous consumption of Sirdalud with CYP1A2 inducers leads to a decrease in tizanidine levels, which causes a decrease in the medicinal properties of the drug.

The use of Sirdalud together with fluvoxamine and Ciprofloxacin . The result of simultaneous use can be a significant decrease in blood pressure, which is accompanied by dizziness and drowsiness, and in some cases, loss of consciousness.

It is not recommended to take the medicine with antiarrhythmic drugs (such as Propafenone , Mexiletine , Amiodarone ), some fluoroquinolones ( Norfloxacin , Enoxacin , Perfloxacin ), Cimetidine , Ticlopidine , oral contraceptives, Rofecoxib .

Sirdalud should be taken with caution with drugs that prolong the QT interval ( Amitriptyline , cisapride , Azithromycin , etc.).

The use of Sirdalud together with Rifampicin reduces the content of tizanidine in plasma and, accordingly, reduces the therapeutic effect of the drug.

Treatment of men who smoke with the drug may require an increase in dose. Alcohol should be avoided, as the medicine may enhance the negative effects of alcohol on the central nervous system. The sedative effect of Sirdalud can be enhanced by sleeping pills, sedatives and antihistamines.

special instructions

The drug is not recommended for patients with galactose intolerance , as well as those suffering from severe deficiency or glucose/galactose malabsorption , due to the presence of lactose in the composition.

Since one of the side effects of the drug is drowsiness, it is highly recommended to refrain from driving a car or performing work related to machinery or machinery.

Analogues of Sirdalud

Level 4 ATC code matches:
Tizanil

Tizanidine

Tolperisone-OBL

Tizalud

Mydocalm-Richter

Mydocalm

Baklosan

Baclofen

An analogue of Sirdalud in release form and composition is Tizalud .

Also, an analogue in composition is Mydocalm , which is available both in film-coated tablets and in the form of an injection solution.

Mydocalm or Sirdalud - which is better?

Sirdalud is more of a modern drug, having a dosage form that allows it to be taken once a day, while Mydocalm has been more studied by doctors and has broader indications for use. The side effects of both drugs are similar.

Reviews for Sirdalud

Reviews of Sirdalud tablets are left by patients of different ages. The average rating on the forums for this medicine is 3.9 points out of 5. Many patients note the occurrence of side effects such as drowsiness and fatigue. There are also reports of the drug's effect on the liver.

Reviews from doctors about Sirdalud: the drug is used for symptomatic treatment, it helps reduce spasms of the skeletal muscles. If side effects are severe or there is no result after 3 days of taking the medication, you must contact your doctor to adjust the treatment regimen.

Price for Sirdalud

The cost of Sirdalud 2 mg tablets is about 200 rubles, 4 mg packages are about 300 rubles.

The price of tablets in Ukraine for 2 mg is about 250 UAH, for 4 mg is about 350 UAH.

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