Central muscle relaxants in rheumatology practice

The article describes the general principles of the treatment of musculoskeletal pain, discusses modern approaches to the treatment of osteoarthritis (OA) and nonspecific back pain (NBS). The issues discussed are: the efficacy and tolerability of the combined use of non-steroidal anti-inflammatory drugs (NSAIDs) of predominantly selective action (aceclofenac) and a centrally acting muscle relaxant (tolperisone) in the treatment of OA and NBS. Two clinical observations are presented that confirm the benefits of combined administration of NSAIDs and muscle relaxants in the treatment of OA and NBS. The efficacy and favorable safety profile of aceclofenac has been demonstrated in patients with comorbid diseases. Tolperisone has shown its efficacy both as a mean of controlling pain associated with muscle tension, and as an element of combination therapy not only for NBS, but also for OA.

Scientific and practical approaches to optimizing the pharmaceutical supply of pediatric palliative patients with paralytic syndromes

Today, palliative care (PC) as a system has a complex structure with stable orderliness, interrelated elements and subsystems. The problem of providing PD with an appropriate level and quality to the children population is particularly acute; it is due to differences in the duration of provision, the necessity to provide educational services, and the socialization of palliative children. At the same time, an important aspect in achieving an appropriate quality of life for children and their families related to health is the assessment of not only medical and social, but also pharmaceutical provision. The aim of the work is to substantiate the approaches to optimization of pharmaceutical support of pediatric palliative patients with paralytic syndromes. The study objects were data from medical records, theactual consumption of medicines by pediatric patients of the Kharkiv healthcare institution where palliative care was provided, as well as data on the state registration of medicines in Ukraine. During the study, clinical and anamnestic, sociological, and marketing methods were used. Based on the results of the analysis of clinical and anamnestic data and the overall assessment of symptoms in a sample group of palliative children with paralytic syndromes, which was 115 people, pathological conditions that led to frequent or permanent distress were identified. Among them, the spastic syndrome prevailed in 100% of cases, the pain syndrome in 66% of cases, the convulsive syndrome in 59%, respectively, and digestive disorders were observed in 82.6% of patients in the sample. It was found that a large proportions of drugs for pharmacological correction of symptoms in the sample of patients were formed by antiepileptic drugs, laxatives and centrally acting muscle relaxants. The results of the marketing analysis of a definite segment of the pharmaceutical market showed a rather limited range of drugs for pediatric dosage forms and concentrations, and it on average ranged from 3.1% to 25% in the pharmacotherapeutic groups studied. Thus, the results obtained prove the need to develop mechanisms for optimizing the pharmaceutical supply of pediatric palliative patients, in particular, expanding the range of medicines approved for use in pediatric practice.

RESUME-1: a Phase III study of tolperisone in the treatment of painful, acute muscle spasms of the back

Tolperisone is a nonopioid, centrally acting muscle relaxant in clinical development in the USA for the treatment of symptoms associated with acute, painful muscles spasms of the back. CLN-301, RESUME-1, is a 14-day double-blind, randomized, placebo-controlled, parallel-group Phase III study of the efficacy and safety of tolperisone administered orally three-times daily in 1000 male and female subjects at approximately 70 clinical sites in the USA experiencing back pain due to or associated with muscle spasm of acute onset. Tolperisone is a promising therapeutic for managing acute, painful muscle spasms of the back as it appears to lack the off-target CNS effects often seen with conventional skeletal muscle relaxants. Clinical Trials Registration: NCT04671082

Tolperisone in the combination treatment of muscular tonic syndrome in individuals with a high level of physical activity

Introduction. Dorsalgia is one of the most common diseases in individuals practising regular physical training and sports Rationale. Because of the growth of the number of physically active individuals expected to rise by 2024, the improvement of drug and physical rehabilitation methods comes into sharp focus.The objective of the study is to evaluate the clinical efficacy of the use of a centrally acting muscle tolperisone-containing relaxant in the combined treatment of dorsalgia accompanied by a muscular tonic syndrome.Materials and methods. In the study, two groups of patients (30 people each) with muscular tonic syndrome received therapy that included NSAIDs and a neurotropic vitamin complex (in the comparison group), and additionally a centrally acting muscle relaxant (in the treatment group).The treatment outcome was assessed by changes in complaints and the objective neurological status of patients, the degree of muscle soreness upon palpation, and the evaluation of pain syndrome using a visual analogue scale.The shear wave elastography (SWE) of defunct muscles was used as an objective assessment method.Earlier in clinical practice, muscle tension in patients was usually assessed using manual palpation, i.e., only qualitatively and subjectively. SWE is an operator-independent, relatively reproducible, and quantitative method for assessing tendons and muscles. SWE was used in this study to obtain more objective assessment and comparison of the elasticity of “affected” and “healthy” symmetrical back muscles before and after the use of drugs.Results. The study showed a high clinical efficacy of tolperisone in the combination therapy of the lower back pain accompanied by muscular tonic syndrome, which was confirmed by a more significant decreased muscle-tonic syndrome based on the evaluation of complaints and the degree of muscle soreness upon palpation, a more pronounced regression of pain syndrome according to VAS in the treatment group of patients vs the comparison group. According to the elastography findings before and after treatment, the group receiving tolperisone showed a more significant decrease in muscular tonic syndrome.Сonclusion. The study confirmed the clinical efficacy of tolperisone manufactured by Sotex pharmaceutical company. On these grounds we recommend that the drug is used in combination therapy for dorsalgias (dorsopathies) accompanied by a muscular tonic (myofascial) syndrome both in patients without a proper level of physical activity, and in those practising regular physical training and sports.

Medication usage and falls in people with multiple sclerosis

There is a need to identify modifiable risk factors for falls in people with multiple sclerosis (MS) to enable the design of successful falls prevention interventions. There is conflicting evidence regarding the association between medication use and occurrence of falls in MS. A total of 101 people with MS had medications classified using the Anatomical Therapeutic Classification system and number of falls prospectively monitored for 3 months. No association was noted between number of medications and falls. The use of genitourinary and sex hormones (odds ratio (OR) = 5.154, 95% confidence interval (CI) = 1.427–18.609, p = 0.012) and centrally acting muscle relaxant (OR = 5.181, 95% CI = 1.546–17.364, p = 0.008) medications were associated with an increased odds of being a faller.

FORMULATION AND EVALUATION OF SUSTAIN RELEASE CYCLOBENZAPRINE HYDROCHLORIDE PELLETS

Cyclobenzaprine Hydrochloride is a centrally acting muscle relaxant which is mostly available in the form of tablets and capsules. The present aim of the study was to develop a sustained release formulation of cyclobenzaprine Hydrochloride pellets using powder layering technique. Nine different formulations of pellets were prepared by using different concentrations of Ethyl Cellulose-50, Hypromellose (HPMC), and PEG 6000 of all formulations, F8 formulation was the optimized formulation. The kinetic studies of F8 formulation was best fitted in the First order model as it had the highest value (R2 = 0.981) and it follows non- fickian diffusion. Among all the formulations F8 gave better drug release 85.7% when compared to innovator, F8 was selected as optimized formulation. The optimized formulation was kept for stability studies for 3 months at 40°C /75% RH and 25°C /60% RH and the results indicated that there was no much variation in their physiochemical characteristics and the formulation was found to be stable.