Muscle relaxants are medications that relax the human striated muscles. Muscle relaxants are drugs that reduce the tone of skeletal muscles, thereby reducing a person’s motor activity, up to complete immobilization. Until a certain time, they were widely used exclusively in anesthesiological practice to relieve muscle tone during operations. Today, the scope of use of muscle relaxants in medicine and aesthetic cosmetology has expanded significantly.
Composition and dosage forms
The drug is available in the form of tablets for oral administration: white or cream-colored, biconvex, with a characteristic medicinal odor. Dosage of the active component: 50 and 150 mg.
The active ingredient of the drug is tolperisone hydrochloride, which has a relaxing effect on the fibers of muscle tissue. Each tablet, in addition to the active component, contains auxiliary and formative components:
- lactose;
- lemon acid;
- stearic acid;
- crospovidone.
The drug shell contains: talc, titanium dioxide, polyvinyl chloride and other components.
Effective but expensive medicines
Muscle relaxants are actively used in medical practice today. They are prescribed to patients with pain of varying intensity caused by diseases of the spinal column and musculoskeletal system. The dosage is always selected individually, and an impeccable therapeutic effect occurs within a few minutes after use. Such drugs have a relatively small list of contraindications and restrictions on use. Their only drawback is their high price, because the cost of some medications reaches up to 7,000 rubles.
Mechanism of action of the drug Tolperisone
The drug selectively inhibits the activity of parts of the brain responsible for regulating the motor functions of muscles. It has a central anticholinergic effect, has a slight antispasmodic effect, expands the lumen and reduces vascular tone. Tolperisone does not affect the activity of the peripheral nervous system.
The drug tablets dissolve and are absorbed into the blood in the gastrointestinal tract. Their active component has a bioavailability of about 20%. The effect of the medicine begins 20–30 minutes after administration, reaching a maximum within 1–1.5 hours. The effect lasts 4–5 hours. The medication does not accumulate in the body. All its substances are transformed in the liver. Metabolites are excreted through the kidneys in the urine within 6–8 hours.
Types of muscle relaxants
Based on the mechanism of action, there are two main types of muscle relaxants:
Central muscle relaxants are drugs that inhibit the central structures of muscle tone. These chemicals have a direct effect on the parts of the central nervous system, brain and spinal cord that are involved in the regulation of muscle tone. Peripheral muscle relaxants are agents that penetrate into direct neuromuscular transmission. These medications relax voluntary muscles by blocking the signal from the motor nerve to the muscle.
For what diseases is Tolperisone indicated?
It is recommended to use the drug in the following conditions:
- increased tone, muscle spasms;
- spastic contractures of the limbs;
- cerebral palsy;
- dysfunction of the spinal cord;
- rigidity, muscle dystonia;
- obliterating sclerosis of the extremities;
- Raynaud's syndrome;
- diabetic angiopathy, thromboangiitis and other manifestations of arterial damage;
- Parkinson's disease;
- acrocyanosis, dysbasia, other painful conditions caused by disorders of vascular innervation;
- disturbances of venous circulation and lymph movement in conditions after thrombosis;
- vascular encephalopathy;
- infantile spastic paralysis;
- trophic ulcers of the lower extremities;
- epilepsy.
The medication is approved for use from the age of 1 year.
Medical certificate
The course of some diseases (for example, osteochondrosis, neuralgia, coxarthrosis, herniated disc) is often accompanied by an increase in muscle tone. Their unnatural activity leads to pinched nerve endings, which causes severe pain. It becomes difficult for a person to move and lead a normal lifestyle. Treatment of this condition is usually complex and necessarily involves the use of muscle relaxants. In combination with non-steroidal anti-inflammatory drugs and other medications, they help relieve pain and relieve muscle spasms. The specific medications, their dosage and duration of use are selected by the doctor.
When is Tolperisone contraindicated?
It is necessary to refuse treatment with the drug during pregnancy and lactation. There is not enough information about the effect of the active substance on fetal formation. The systemic effect that it causes can affect the condition of both mother and child and cause irreversible disorders.
Other contraindications for use:
- myasthenia gravis;
- individual hypersensitivity to the components of the drug;
Signs of a possible allergic reaction to Tolperisone: bronchospasm, skin itching, urticaria, the appearance of red spots - erythema, anaphylactic shock, Quincke's edema.
Side effects of the drug
During treatment with Tolperisone tablets, the following may appear:
- muscle weakness;
- dyspnea;
- increased fatigue;
- dizziness;
- drowsiness during the daytime;
- decreased blood pressure;
- pain in the stomach and abdominal cavity;
- nausea, vomiting.
In the absence of a serious threat to the physical condition, such symptoms do not require discontinuation of the drug.
Discussion
Based on the results of RCTs, some national guidelines [39–47] recommend the use of muscle relaxants for the treatment of acute LBP, usually in combination with analgesics or NSAIDs. In general, the data from the studies reviewed indicate a higher effectiveness of treatment with muscle relaxants compared to placebo, both as monotherapy and as adjunctive therapy. There are no uniformly accepted standards for assessing clinical outcomes yet. In early studies [23, 26], the main focus was on pain relief and investigators used only VAS to assess pain intensity as an endpoint. More recent studies have also begun to focus on improving the mobility of patients, as evidenced by the results of assessments of activities of daily living and scores on functional scales.
The addition of muscle relaxants to NSAID therapy was subsequently established as the gold standard treatment for LBP. Thus, the use of combination therapy is advisable. In one early study in which baclofen was added to ibuprofen [26], there was little or no improvement, but later studies using tizanidine as well as thiocolchicoside [24, 25] showed greater treatment effectiveness when using muscle relaxants on based on improving functional parameters.
In addition to pain, decreased range of motion in the lumbar spine has a negative impact on daily activity and ability to work. Rapid rehabilitation is of great social importance, and the use of parenteral forms of drugs can increase the effectiveness of therapy. The results of a study conducted in 7 Russian clinical centers [19] showed a higher effectiveness of tolperisone in reducing pain intensity and increasing mobility when added to diclofenac. A more pronounced improvement was found in the early phase of treatment, when tolperisone injections were used, but later, when the drug was continued orally, the improvement persisted. The studies reviewed lasted for the most part 7-14 days and were aimed at assessing the effectiveness of therapy in the acute period of the disease. Tolperisone was used up to 21 days and showed more pronounced effectiveness from 10 days until the end of treatment [17].
Systematic reviews found no significant difference in effectiveness between different muscle relaxants. However, data from head-to-head comparisons have been limited. Thiocolchicoside and tizanidine were compared in two studies [27, 34], both of which found thiocolchicoside to be superior in pain relief as well as more beneficial for mobility, although the differences were not statistically significant. One study [18] compared the effects of tolperisone and thiocolchicoside and found a more pronounced effect of tolperisone when assessing all parameters, including pain rating scales and functional test results.
Most studies included patients with at least moderate LBP. The use of baclofen has been studied in more severe patient conditions, and treatment results have shown its higher effectiveness [32]. It is reasonable to assume that patients with moderate to severe symptoms will achieve greater benefit from combination therapy that includes analgesics and muscle relaxants.
The studies primarily included patients aged 17 to 75 years, without conducting separate analyzes by age subgroups. Only one study [17] emphasized that patients aged 40 to 60 years achieved the best results with tolperisone.
Adverse events with the use of muscle relaxants are usually mild in severity and do not differ between drugs. When muscle relaxants are used in addition to NSAIDs, the incidence and severity of adverse events do not increase. Some muscle relaxants are characterized by a sedative effect [35, 36]. The potential for sedation has been studied with tizanidine, thiocolchicoside and tolperisone. A comparative study [27] showed a less pronounced sedative effect of thiocolchicoside compared to tizanidine. It was also found that tolperisone has no effect on psychomotor activity (indicators do not differ from placebo) [37]. The use of any drugs that may adversely affect wakefulness should be carefully considered in light of immediate and long-term consequences (impact on ability to drive, work, sleep, etc.) [48].
Restrictions
Not all muscle relaxants existing in the world with indications for use in acute LBP were included in the review. To make this review more informative and relevant for practical purposes in the area under study, attention was focused on drugs available in Russia, Belarus and Kazakhstan. Because most studies were conducted at least 10 years ago, they used different designs. LBP was assessed using various scales; functional activity was used as the main symptom and indicator.
Use of Tolperisone: instructions
The treatment regimen depends on the characteristics of the painful manifestations. General recommendations:
- 1 tablet with a dosage of 50 mg. 2–3 times a day for adults in the first days of therapy;
- 150 mg each. up to three times a day - if the drug is well tolerated in the subsequent period.
For children under 15 years of age, the dosage is selected taking into account body weight:
- 2–4 mg per 1 kg of weight: children from 1 to 6 years old;
- 5 mg per 1 kg. weight: from 7 to 14 years.
The time of eating does not affect the absorption of the drug.
An overdose of the drug is fraught with respiratory problems, cardiac depression, and vascular collapse. It is important to use it strictly as prescribed by the doctor, after carefully studying the instructions. After taking each dose, monitor changes in physical condition.
special instructions
The therapeutic effect of the drug is enhanced and prolonged when combined with peripheral muscle relaxants, Clonidine, psychoactive and anesthetic agents. Tolperisone reduces the speed of motor skills and mental reactions, affects concentration. During the treatment period, it is necessary to refrain from driving and working with complex mechanisms.
The combination of the drug with alcohol is unacceptable, as it leads to serious intoxication, a sharp decrease in vascular tone, and damage to the central nervous system.
What are muscle relaxants?
Osteochondrosis is almost always accompanied by acute pain, which hampers movement and prevents normal movement and simple physical actions. Therefore, the patient is prescribed drugs that can reduce muscle tone, reduce pain, and increase the effectiveness of physiotherapeutic procedures. They are recommended for use against the background of manual therapy and exercise therapy; the dosage is selected individually, after undergoing a full examination.
There are two types of muscle relaxants:
- Antispasmodics. Aimed at reducing muscle tone. Helps relax and bring muscles back to normal. They are used in case of severe spasms or moderate intensity.
- Blockers. They help to quickly relax muscles and relieve nervous tension. Moreover, with their help, the “zero mark” is achieved. Used exclusively in surgery.
Muscle relaxants are manufactured by pharmaceutical companies and are based on glycerin or benzimidazole. But there are also mixed varieties, such as, for example, “Belofen”, “Mydocalm”.
Muscle relaxants for osteochondrosis are used only when mobility is lost or reduced; they are not suitable for relaxing muscles and eliminating pain. These medications are not used independently, but are often included in a complex and perfectly complement anti-inflammatory medications, painkillers and antibiotics.