Pharmacodynamics and pharmacokinetics
Tolperisone-OBL is a muscle relaxant drug. Shows inhibitory selective activity in relation to the caudal part of the reticular formation of the brain, has anticholinergic effects of central action.
Does not affect the peripheral nervous system , has a mild vasodilating and antispasmodic effect.
When taken orally, absorption of the drug, thanks to the tablet shell, occurs in the small intestine. The drug has 17-20% bioavailability.
TCmax in the blood is detected after 30-60 minutes. Metabolism takes place in the kidneys and liver. T1/2 about 150 minutes. In the form of metabolites, almost all of the drug is excreted in the urine (99%).
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.
Indications for use
Cerebral and spinal palsy (limb contracture, muscle spasm, hypertonicity, spinal automatism).
Painful conditions that are accompanied by dystonia , spasm or rigidity , as well as obliterating lesions of the arteries : diabetic angiopathy , vascular obliterating atherosclerosis of the extremities, Raynaud's syndrome , thromboangiitis .
Extrapyramidal disorders (atherosclerotic and postencephalitic parkinsonism ).
Consequences of diseases associated with disorders of vascular innervation: angioedema ( intermittent), acrocyanosis .
Postthrombotic changes in venous blood and lymph circulation, hypertonicity in combination with impaired muscle tone of another type, encephalopathy of vascular origin, spastic paralysis in children, trophic ulcer of the leg, epilepsy .
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.
Instructions for use Tolperisone-OBL
Instructions for use of Tolperisone-OBL involve taking the drug tablets orally.
As a rule, the initial dosage of the drug prescribed to adult patients is 50 mg. This dose is taken 2-3 times in 24 hours.
Subsequently, a gradual increase in dosage to 150 mg with the same frequency of dosing per day is indicated.
The daily dosage for children is divided into 3 doses and is:
- 1-6 years - 5 mg per kilogram of weight;
- 7-14 years - from 2 to 4 mg per kilogram of weight.
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.
Analogues of Tolperizon-OBL
Level 4 ATC code matches:
Tizanil
Tizanidine
Tizalud
Mydocalm-Richter
Mydocalm
Baklosan
Sirdalud
Baclofen
Analogues of the drug are represented by the following drugs:
- Mydocalm;
- Baklosan;
- Sirdalud;
- Lioresal;
- Tizanil;
- Tizalud;
- Tizanidine;
- Tolperisone.
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.
Tolperizon-OBL price, where to buy
average price of Tolperisone in tablets, with the active ingredient tolperisone hydrochloride 150 mg No. 30 – 190 rubles.
The price of ampoules of the closest analogue of Tolperizon-OBL - Mydocalm Richter , 1 ml No. 5, is about 450 rubles.
- Online pharmacies in RussiaRussia
ZdravCity
- Tolperisone-OBL tablets p.p.o.
150 mg 30 pcs. JSC Obolenskoe farm. enterprise 284 rub. order
Tolperisone tablets p/o 150 mg No. 10x3
Name
Tolperisone tablets 150 mg in container pack No. 10x3
Description
The tablets are white, round, biconvex, film-coated, with a slight characteristic odor.
Main active ingredient
Tolperisone
Release form
Pills
Dosage
150mg
Pharmacological properties
Tolperisone is a drug that acts on the central nervous system. It is used in the treatment of increased muscle tone.
Indications for use
immediate or long-term treatment of pathologically increased skeletal muscle tone in organic neurological diseases (damage to the pyramidal tracts, multiple sclerosis, cerebrovascular disorders, myelopathy, encephalomyelitis, etc.); treatment of muscle hypertonicity and muscle spasms accompanying diseases of the musculoskeletal system (eg spondylosis, spondyloarthritis, cervical and lumbar syndromes, arthrosis of large joints); rehabilitation treatment after surgical interventions in orthopedics and traumatology; treatment of obliterating vascular diseases, as well as syndromes resulting from impaired vascular innervation (for example, acrocyanosis, intermittent angioedema); Specific indications in pediatric practice are Little's disease and other encephalopathies accompanied by muscular dystonia.
Directions for use and doses
Adults The average daily dose, depending on the individual need and tolerance of the drug by the patient, is 150-450 mg, divided into 3 doses. Children The drug is prescribed to children weighing more than 30 kg (over 10 years old) at a daily dose of 2-4 mg/kg body, in 3 divided doses. Considering the low daily doses, when treating children it is recommended to use Tolperisone, film-coated tablets 50 mg. Because The tablets are not intended to be divided into parts; the drug should be prescribed to children weighing 30 kg or more. Use in children Data on the safety and effectiveness of tolperisone in children are limited. Patients with impaired renal function Data on use in patients with impaired renal function are limited. A higher incidence of adverse reactions was observed in this group of patients. Patients with moderate renal impairment require dose titration and careful monitoring. The use of tolperisone is not recommended in patients with severe renal impairment. Patients with impaired liver function Data for use in patients with impaired liver function are limited. A higher incidence of adverse reactions was observed in this group of patients. Patients with moderate hepatic impairment require dose titration and careful monitoring. The use of tolperisone is not recommended in patients with severe liver dysfunction. Directions for use: Use after meals with a glass of water. It is not recommended to take on an empty stomach, as insufficient food may reduce the bioavailability of tolperisone.
Use during pregnancy and lactation
If you are pregnant or breastfeeding, think you are pregnant or are planning a pregnancy, consult your doctor or pharmacist before taking this medicine. Although Tolperisone has not been proven to be toxic to a baby, after a careful risk/benefit assessment, your doctor should decide whether you should use the drug, especially in the first three months of pregnancy. Tolperisone should not be used during pregnancy (especially in the first trimester) unless the expected benefit clearly justifies the potential risk to the fetus. Since there is no data on the excretion of tolperisone in breast milk, the use of this drug is contraindicated during breastfeeding.
Precautionary measures
Hypersensitivity reactions When using drugs containing tolperisone, the development of hypersensitivity reactions was most often reported. Allergic reactions ranged from mild skin reactions to severe systemic reactions, including anaphylactic shock. Symptoms of an allergic reaction: skin redness, rash, urticaria, itching, angioedema (Quincke's edema), tachycardia, hypotension and shortness of breath. Female patients with hypersensitivity reactions to other drugs or a history of allergic reactions are at higher risk. In cases of known hypersensitivity to lidocaine, increased caution should be exercised during the use of tolperisone due to possible cross-reactions. Be alert for any symptoms of hypersensitivity. If symptoms develop, you should immediately stop taking tolperisone and consult a doctor immediately. Patients who have had an episode of hypersensitivity should not re-administer tolperisone. This medicine contains lactose monohydrate. Patients with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Interaction with other drugs
If you are taking other medications at the same time, you should consult your doctor. The simultaneous use of tolperisone and the following drugs: thioridazine, tolterodine, venlafaxine, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine, may increase the blood levels of these drugs. The bioavailability of tolperisone decreases if taken on an empty stomach. Although tolperisone is a centrally acting drug, its sedative effect is very low. In case of simultaneous administration with other centrally acting muscle relaxants, the dose of tolperisone should be reduced. Tolperisone enhances the effect of niflumic acid, therefore, with simultaneous use, a reduction in the dose of niflumic acid or other non-steroidal anti-inflammatory drugs should be considered.
Contraindications
Hypersensitivity to tolperisone or other similar chemicals (epiresone), as well as to excipients. Myasthenia. Breastfeeding period.
Compound
Each tablet contains: active ingredient: tolperisone hydrochloride - 50 mg or 150 mg; excipients: hydroxypropylcellulose, crospovidone, citric acid monohydrate, stearic acid, colloidal silicon dioxide anhydrous, magnesium stearate, lactose monohydrate, Opadry II (including polyvinyl alcohol, partially hydrolyzed, talc, macrogol 3350 (polyethylene glycol), titanium dioxide E 171).
Overdose
The most common symptoms of overdose are drowsiness, gastrointestinal disorders (nausea, vomiting, epigastric pain), tachycardia, hypertension, bradykinesia and dizziness. Cases of seizures and coma have been reported. There is no specific antidote. Symptomatic treatment is recommended. In case of overdose, consult a doctor immediately!
Side effect
In the post-registration period, the number of messages received about the development of hypersensitivity reactions associated with the use of tolperisone was about 50-60% of all messages received. In most cases these were non-serious adverse reactions. Life-threatening allergic adverse reactions have been reported very rarely. Adverse reactions are listed according to the classification of undesirable side effects in accordance with the damage to organs and organ systems and the frequency of development: very often (? 1/10), often (? 1/100, but
Storage conditions
In a place protected from light and moisture, at a temperature from 15 'C to 25 °C.
Introduction
Osteoarthritis (OA) is a heterogeneous group of diseases of various etiologies with similar biological, morphological, clinical manifestations, which are based on damage to all components of the joint, primarily cartilage, as well as subchondral bone, synovial membrane, ligaments, capsule, periarticular muscles [1] . The disease is an important medical, social and economic problem due to its widespread prevalence (6.43% in the population, correlates with age and reaches maximum values of 13.6% in people over 45 years old), a significant deterioration in the quality of life of patients due to constant pain syndrome, as well as high disability [2].
Despite the high negative significance of this pathology, modern regulatory documents on the provision of specialized care for OA have not been developed. The existing standard of care for patients with coxarthrosis from 2005 is recommended for use in federal specialized medical institutions [3], and the relatively modern standard from 2012 regulates exclusively primary health care provided on an outpatient basis [4]. Both orders include only symptomatic drugs, while etiopathogenetic therapy is not indicated. Therefore, practicing doctors use clinical recommendations and treatment protocols for patients with OA in their work [5]. According to these documents, a generally accepted treatment regimen involves 3 successive stages [6, 7]:
1) non-pharmacological methods: lifestyle changes, excess weight loss, physical exercise, use of orthopedic products, physiotherapeutic and spa treatment;
2) drug therapy: NSAIDs, non-selective COX-2 inhibitors (paracetamol, diclofenac, ibuprofen, ketoprofen, naproxen), moderately selective COX-2 inhibitors (meloxicam, nimesulide, aceclofenac), selective COX-2 inhibitors (celecoxib, etoricoxib), opioid analgesics (tramadol) if NSAIDs are ineffective, intra-articular administration of corticosteroids (methylprednisolone or triamcinolone), chondroprotectors (chondroitin sulfate, glucosamine sulfate, hyaluronic acid derivatives), interleukin 1 inhibitor - diacerein, unsaponifiable compounds of avocado and soy (NSAC) - piaskledin;
3) surgical treatment - endoprosthetics.
The first nonspecific symptoms of OA (pain, limited range of motion) appear even in the absence of radiological changes in the joint and are most likely caused by muscle spasm. However, in most domestic clinical recommendations there is no such class of drugs as centrally acting muscle relaxants, while the Kazakhstan Protocol for the Treatment of OA (2013) contains such drugs [8]. The inclusion of centrally acting muscle relaxants in the complex conservative treatment regimen for OA of large joints, especially in the initial stages of the pathology, seems to be pathogenetically justified and an appropriate addition to the generally accepted treatment regimen.
The purpose of the study was to compare the effectiveness of the generally accepted regimen of conservative drug therapy for hip OA (NSAIDs + chondroprotectors) and a modified regimen (NSAIDs + chondroprotectors + centrally acting muscle relaxant - tolperisone).
Results and discussion
Upon admission, patients in both groups had the following levels of the studied criteria (Tables 2, 3).
Table 2. Clinical indicators of the studied criteria at admission
Table 3. Paraclinical and laboratory indicators of the studied criteria upon admission
As can be seen from table. 2 and 3, no significant, statistically significant differences in the studied criteria were found in the groups of patients.
The dynamics of therapy effectiveness criteria in the comparison group are presented in Fig. 1.
Rice. 1. Dynamics of the studied criteria for the effectiveness of treatment in the comparison group.
In the majority of patients in the comparison group ( n
=34) the increase in the amplitude of flexion, extension and rotation of the hip had a statistically significant increase (11±30;
p
<0.05).
The VAS pain index value decreased by more than 20 mm ( p
<0.01). At the same time, the severity of synovitis and laboratory criteria also had positive dynamics, but did not always have statistical confirmation (Table 4).
Table 4. Dynamics of clinical and laboratory criteria for the effectiveness of therapy in the comparison group
Thus, by the end of observation in this group of patients, all studied criteria had positive dynamics compared to the initial values: the amplitude of hip movements and the severity of pain showed statistically significant changes, and changes in the severity synovitis and laboratory parameters were unreliable.
The changes in the studied data in the main observation group looked somewhat different (Fig. 2).
Rice. 2. Dynamics of the studied criteria for the effectiveness of treatment in the main observation group.
In the main group, the same trends were observed as in the comparison group: most significant and reliable ( p
<0.01) the intensity of the pain syndrome on the VAS scale decreased - minus 33 mm, in addition,
the amplitude of all hip movements increased p The severity of synovitis and laboratory criteria also had positive, statistically insignificant dynamics (Table 5).
Table 5. Dynamics of clinical and laboratory criteria for the effectiveness of therapy in the main group
Thus, the differences between the groups consisted primarily in more reliable and pronounced clinical (the amplitude of hip movements increased: 11±30 at p<0.05 in the comparison group and 14± 20 at p
<0.01 in the main group) and subjectively stated paraclinical (pain intensity on the VAS scale decreased by 21 mm in the first group and by 33 mm in the second,
p
<0.01) effects of therapy (Fig. 3, 4).
Rice. 3. Dynamics of the amplitude of hip movements in the control and main groups upon admission and on the 12th day of therapy.
Rice. 4. Dynamics of VAS in the control and main groups upon admission and on the 12th day of therapy.