Results of the post-registration clinical study "PARUS" on efficiency and safety assessment of Mydocalm-Richter for local injection therapy of a myofascial trigger zone.

AIM: The "PARUS" program included investigation of the analgesic, muscle relaxant and sedative effects of Mydocalm-Richter which acts as central muscle relaxant in patients with myofascial pain syndrome, taking into account its registered indication for use - the hypertonus and cross-striated muscle spasm. MATERIALS AND METHODS: Fifty patients with myofascial trigger points, the mean age of 41.67±11.86 years, have been enrolled in the study. All patients had undergone clinical examination that allowed the diagnosis of myofascial pain syndrome. The intensity of pain syndrome was evaluated using the pain visual analogue scales and McGill pain questionnaire. Visualization of area in spasm and evaluation of blood circulation was carried out using the ultrasound scan of target muscle. In order to objectively evaluate any conceivable hypotensive and sedative effects of Mydocalm-Richter we used the orthostatic test, Schulte's test for attention span and perfor-mance distribution and Munsterberg's test for attention discrimination and concentration. RESULTS: The analgesic and muscle relaxant effects of Mydocalm-Richter become apparent by day 3 post-injection, and the muscle relaxation effect is reaching its maximum on day 10 post-injection. Cardiovascular function following administration of Mydocalm-Richter was evaluated using the orthostatic test which revealed good orthostatic tolerance. Single injection of tolperisone hydrochloride possessing a central muscle relaxant activity has no sedative effect and does not influence patient response time. The ultrasound examination data demonstrated the improvement and in some cases restoration of blood circulation in the myofascial trigger points. CONCLUSION: Clinical study "PARUS" conducted in patients with myofascial pain has demonstrated a positive muscle relaxant and analgesic effect of Mydocalm-Richter that resulted in restoration of peripheral circulation in the myofascial trigger pointsconfirmed by ultrasound examination. An important benefit of this drug product is the absence of sedative effect and arterial hypotension.

[The experience of the using Tolperisone in a complex conservative therapy of an osteoarthrosis of a hip joint]. / Opyt primeneniia tolperizona v kompleksnoi konservativnoi terapii osteoartroza tazobedrennogo sustava.

AIM: The comparison of the efficiency of the standard scheme of a conservative medicinal therapy of an OA of a hip joint and the modified scheme (with the muscle relaxant of the central action - Tolperisone) was the research objective. MATERIAL AND METHODS: The prospective research of the complex conservative therapy of two pools of patients with initial stages of a coxarthrosis from 2014 for 2017 with the subject assessment articulary treatment components is conducted. RESULTS: As a result of the studying of the clinical performance of the modified scheme in comparison with the standard scheme of the therapy at patients with the prevalence of an arthritic component of a disease established the best results of the therapy.

[A clinical efficacy of electrode pharmaphoresis in treatment of railway workers with low-back pain].

OBJECTIVE: To evaluate clinical efficacy and tolerability of electrode pharmaphoresis using preparations xefocam and mydocalm-richter in railway workers with low-back pain. MATERIAL AND METHODS: Authors carried out an open prospective noncomparative study of 16 patients, aged 21-82 years, with spinal osteochondrosis with root syndrome and radiculopathia of the lumbar/sacral spine with pain syndrome regardless of its duration. Treatment efficacy was assessed by the dynamics of pain syndrome severity based on the scores of a self-rated scale completed by the patient and the McGill Pain Questionnaire. Quality-of-life was assessed with the Oswestry Disability Index before and in the end of treatment. Clinical outcome was evaluated with the modified Nurick scale. Electrode pharmaphoresis (the "Farma T.E.B. Trans Epidermal Barrier Physio" apparatus) was administered to all patients using xefocam (solution for injections 8 mg, 2 ml per procedure) and mydocalm-richter (solution for injections 100 mg, 2 ml per injection) in the lumbar/sacral spine. RESULTS AND CONCLUSION: The high clinical efficacy of electrode pharmaphoresis using xefocam and mydocalm-richter was shown. The complex restoration study resulted in the reduction of pain syndrome in all patients. Pain severity was reduced to mild grade in 68.8% to the middle of treatment and in 93.8% patients in the end of treatment. As a consequence of pain reduction, the functional activity (quality of self-service, daily activities) increased significantly in 68.8% of patients. Positive treatment effect was noted in 100% of patients, good tolerability of this medication in 87.5%.

Considerable interindividual variation in the pharmacokinetics of tolperisone HCl.

OBJECTIVE: The aim of this study was to determine the pharmacokinetic profiles of oral tolperisone hydrochloride in healthy volunteers. METHODS: After the oral administration of tolperisone hydrochloride, the plasma concentrations of tolperisone were measured in 15 healthy male Korean volunteers. The tolperisone concentration was determined using high-performance liquid chromatography with a C18 reverse-phase column. RESULTS: Very large interindividual differences in the AUC and Cmax were detected after oral tolperisone HCl. The AUC0-infinity, varied from 125.9-1,241.3 ng/ml x h, and the Cmax varied from 64.2 and 784.9 ng/ml. The tmax of tolperisone was 0.90 +/- 0.31 h and the mean half-life was 1.00 +/- 0.28 h. CONCLUSION: These results suggest that the pharmacological effect of oral tolperisone HCl varies between individuals, and the oral tolperisone HCl dose might need to be individualized.

[Use of local injections of tolperisone (midocalm) in combination with tractional therapy in the treatment of vertebral static syndrome].

A randomized double-blind study of the efficacy of midocalm combined with tractional therapy has been carried out in 24 patients (indexed group) comparing to the tractional therapy without midocalm (the drug has been substituted with placebo) in 25 patients (comparison group). The effective number of injections was 3-6 in the indexed group and 7 in the comparison group. A quantitative assessment revealed that in the indexed group treatment efficacy was 1,56 times higher and the effect achieved sooner than in the comparison group.

[Post-operative pain therapy of a chronic pain patient]. / Pharmakotherapie--Postoperative Schmerztherapie eines chronischen Schmerzpatienten.

Post-operative pain therapy of chronic pain patients poses a challenge. Here we report the perioperative management of a 39-year-old male under chronic therapy with oxycodon, gabapentin and tolperison. Particular the pharmacointeractions regarding premedication and postoperative dose finding of opioids with intravenous PCIA are discussed.

[A randomized, double blind, placebo-controlled study of the efficacy and safety of tolperisone in spasticity following cerebral stroke].

To study the efficacy and safety of tolperisone--a centrally acting muscle relaxant with membrane stabilizing activity--in the treatment of stroke-related spasticity. This was a randomized, double-blind, placebo-controlled, multicenter study with parallel groups. Treatment lasted 12 weeks and was started with a titration period of variable length (dose range 300-900 mg tolperisone daily). The degree of spasticity determined on the Ashworth Scale in the most severely affected joint area was denned as primary target parameter. Hundred and twenty patients (43 females, 77 males) in a mean age of 63,3 +/- 10,6 years were recruited and received treatment. In the majority of patients both limbs of each side were affected by the spasticity which on average had been present for 3,3 +/- 4,4 years. A 62% of the patients were treated with a daily dose >600 mg tolperisone. Tolperisone reduced the mean Ashworth Score by a mean of 1,03 +/- 0,71 compared with a mean reduction of 0,47 +/- 0,54 in the placebo group (p<0,0001). A 78,3% of the patients on tolperisone versus 45% of the placebo patients experienced a reduction by at least 1 point on the Ashworth Scale (p<0,0001). Functional and overall assessments of efficacy confirmed superior efficacy of tolperisone. Adverse events occurred less often on active treatment (n=19) than on placebo (n=26) and were mostly of mild-to-moderate intensity. No withdrawals caused by adverse events were reported in the tolperisone group. The findings of the present study demonstrate the efficacy and excellent tolerance of tolperisone in the treatment of spastic hypertonia following cerebral stroke. Study data further suggest that an individual dose titration which may exceed the recommended maximum dose of 450 mg daily results in optimized therapeutic benefit.

[Mydocalm causing anaphylaxis]. / Mydokalm przyczyna wstrzas anafilaktycznego.

The case of anaphylactic shock due to Mydocalm administration is presented. 49-year-old woman suffered from spinal osteoarthritis and she was treated with NSAIDs and Mydocalm for many years. 6 weeks before admission to hospital the first anaphylactic shock was developed with loss of consciousness after oral administration of Mydocalm. Then she was admitted to the hospital in order to diagnose and verify the suspicion whether Mydocalm caused this reaction. Percutaneous test with Mydocalm was performed and it caused anaphylactic shock. Only thirteen cases like this one have been documented in the world literature. It is the first case reported in Poland.

Evaluation of sedative effects of single and repeated doses of 50 mg and 150 mg tolperisone hydrochloride. Results of a prospective, randomized, double-blind, placebo-controlled trial.

Sedative effects of single and repeated doses of 50 mg and 150 mg tolperisone hydrochloride (Mydocalm), a centrally active muscle-relaxing agent, were evaluated in a placebo-controlled double-blind clinical trial. A total of 72 healthy young adults balanced by sex were randomized to receive 50 mg or 150 mg tolperisone hydrochloride or placebo t.i.d. for a period of 8 days. Control examinations were performed in the mornings of days 1 and 8 before intake of the morning dose and at 1.5, 4 and 6 hours postdose. The psychomotoric test battery used in this trial revealed no sedative effects of tolperisone hydrochloride in the given doses at any control examination. Subjective mood ratings quantified by the Welzel Colored Scales were not impaired either. The lack of differences in sedative potentials of tolperisone hydrochloride and placebo was confirmed by tests on differences and by tests on equivalence using 95% CI. The present study substantiates clinical experience and previous clinical trials demonstrating that tolperisone hydrochloride, though being a centrally active muscle relaxant, does not cause any sedation and does not impair reaction times.

Effects of a new centrally acting muscle relaxant, NK433 (lanperisone hydrochloride) on spinal reflexes.

(-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'-trifluoromethylpropiophenone++ + monohydrochloride, lanperisone hydrochloride (NK433) administered intravenously or orally depressed the mono- and polysynaptic reflex potential, dorsal root reflex potential, flexor reflex mediated by group II afferent fibers, patellar and flexor reflexes. These effects were reduced by spinal transection. NK433 inhibited the facilitation of the flexor reflex mediated by group II afferent fibers that was induced by intrathecal administration of noradrenaline-HCl. (+)-(1R,2R)-2-methyl-3-(1-pyrrolidinyl)-1-(4-trifluoromethylphenyl)-1-pr opanol (LPS-9)-HCl, a metabolite of NK433, also inhibited the spinal reflexes. Given orally, NK433 had effects more than three times stronger and tending to be longer-lasting than those of eperisone-HCl. These results suggest that NK433 exerts a non-selective inhibition on spinal reflexes and that inhibition of the descending noradrenergic tonic facilitation within the spinal cord is involved in the mechanism of spinal reflex depression by NK433. LPS-9 could contribute to the potent activity of NK433 after oral administration.