Efficacy and safety of using phenylbutazone for intramuscular administration in osteoarthritis of the knee joint


Introduction

Osteoarthritis (OA) is one of the most common diseases of the musculoskeletal system, which is a leading cause of disability in older people.
At the same time, in recent decades there has been an increase in morbidity among the adult working population. Against the background of long-term pain syndrome, the quality of life of patients decreases, depression and other comorbid conditions may develop [1–3]. As large epidemiological studies show, in the Russian Federation the prevalence of OA is 11–13% among the adult population [4, 5]. The incidence of symptomatic knee OA reaches 25% in a cohort of people over 65 years of age [6]. The symptoms of OA at the onset are limited to pain, sometimes swelling and stiffness of the affected joints; in the later stages, a persistent dysfunction is formed, which leads to loss of performance. Radiologically, OA is manifested by a decrease in the thickness of the articular cartilage, the formation of subchondral sclerosis and osteophytes along the edges of the articular surfaces; an objective examination reveals signs of synovitis, and against the background of a long-term inflammatory process, hypertrophy of the synovial membrane and deformation develop [7].

The modern concept of treating OA is based on the use of drug therapy, the goal of which is to suppress local inflammation and slow down the degeneration of articular cartilage. Also in complex treatment, non-drug methods are used: physiotherapy, physical therapy, reduction of excess body weight, and attempts are made to correct biomechanical disorders [8].

In outpatient practice, non-steroidal anti-inflammatory drugs (NSAIDs) are most often prescribed, which can reduce the intensity of pain and improve the patient’s quality of life in a short period of time. However, to achieve maximum analgesic effect, the use of NSAIDs in maximum therapeutic dosages is required. With long-term use of NSAIDs, the risk of adverse reactions from the gastrointestinal tract (erosion, ulcers, bleeding), cardiovascular system (including vascular accidents), hemostasis system, etc. increases [9].

Currently, there is a trend towards more frequent use of parenteral forms of NSAIDs due to their higher bioavailability, which provides an accelerated onset of analgesic effect compared to oral forms [10]. At the same time, the issue of the safety of using NSAIDs in different dosage forms remains relevant [9].

Purpose of the study:

to evaluate the effectiveness and safety of intramuscular injections of the drug AMBENIUM® parenteral (TRIVIUM-XXI LLC) for OA of the knee joint.

Material and methods

The prospective study included 30 patients with knee OA, of which 21 (70%) were women. The median age of patients was 48 [35; 62] years, median disease duration - 5 [2; 10 years. 9 (30%) patients had comorbid pathology: arterial hypertension (55.5%), history of myocardial infarction (11.1%), autoimmune thyroiditis (11.1%), diabetes mellitus (11.1%), ulcerative medical history (11.1%). Before the study, 43.3% of patients were taking NSAIDs with insufficient analgesic effect.

Criteria for inclusion in the study:

age from 25 to 75 years;

X-ray diagnosis of knee OA;

inflammatory phenotype of knee OA, confirmed by the presence of effusion and/or thickening of the synovium on ultrasound;

severe joint pain (≥40 mm on visual analogue scale, VAS) and/or the need for regular use of NSAIDs;

signed informed consent to participate in the study.

Criteria for non-inclusion in the study:

surgery on the joint being examined;

intra-articular injection of glucocorticosteroids or hyaluronic acid for 6 weeks. before the start of the study;

infectious arthritis or pain in the knee joint caused by other causes (intra-articular tumor, villonodular synovitis);

severe diseases of the liver, kidneys, blood, cardiovascular system, malignant neoplasms, including in history (less than 5 years old), gastric or duodenal ulcers in the acute stage;

participation in another clinical trial;

poor general condition or other reasons that would make it difficult for the patient to make regular visits to the study center;

pregnancy or lactation;

hypersensitivity to the components of the drug.

For local intramuscular administration, the drug AMBENIUM® parenteral was used (solution for intramuscular administration containing sodium phenylbutazone 400 mg, in terms of phenylbutazone - 373.4 mg; lidocaine hydrochloride monohydrate 4 mg, in terms of lidocaine hydrochloride - 3.75 mg; excipients : propylene glycol, sodium hydroxide, water for injection). The drug was administered intramuscularly three times with an interval of 7±2 days.

The results of treatment were assessed during 5 consecutive visits: before the start of the course, after the 2nd and 3rd administration (7±2 and 14±2 days), 28±2 and 56±2 days after the start of the study. The effectiveness criteria were a decrease in pain intensity according to VAS, positive dynamics of functional activity according to the HAQ-DI (Health Assessment Questionnaire Disability Index) and KOOS (Knee injury and Osteoarthritis Outcome Score) questionnaires, verbal assessment of the effect of the therapy by the patient (bad, weak, satisfactory, good, excellent), daily requirement for taking other NSAIDs. On the day of the procedure, the patient was prohibited from taking NSAIDs.

For mathematical data processing, the Statistica 15.0 program (StatSoft Inc., USA) was used. Quantitative indicators are presented as the median, 25th and 75th percentiles (Me [25p; 75p]), qualitative parameters - as absolute and relative (%) indicators. To compare indicators, nonparametric Mann-Whitney and Pearson χ2 tests were used. Differences were considered statistically significant at p<0.05.

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Research results

During therapy with AMBENIUM® parenteral, pain intensity in the group as a whole significantly decreased from 40 [30; 60] to 20 [0; 30] points (p<0.0001), by the end of the study there was an increase in functional indicators according to KOOS (Table 1).

All patients showed a decrease in pain intensity by the end of observation. Complete pain relief occurred in 33.3% (Fig. 1) - this category of patients is represented by people under 45 years of age, and their OA was classified as secondary (associated with a previous injury). A slight positive change in pain intensity (no more than 10% of the initial level) was observed in 4 patients with primary OA; these patients were over 65 years of age (65, 71, 75 and 81 years).

In the examined group of patients, functional impairments in everyday life, on average, can be assessed as moderate. At the same time, 18% had a HAQ-DI index of more than 1.1 points, and 12 patients had minimal impairment (less than 1.1 points). During the study, there was a trend towards restoration of functions that ensure daily living activities. In 13 (43.33%) patients, complete recovery of basic vital functions was noted according to the HAQ-DI questionnaire.

According to dynamic ultrasound data of the knee joint, intramuscular administration of the study drug had an effect on all signs of inflammation (Table 2).

At inclusion in the study, all patients had thickening of the synovium up to 3 mm or more and/or the presence of fluid in the suprapatellar bursa. As a result of the treatment, excess fluid remained in only 30% of patients. The thickness of the synovial membrane, as well as the amount of fluid in the bursa, significantly decreased.

All patients showed a response to the therapy. In total, 26 (86.6%) patients were satisfied with the results of treatment. A verbal assessment of “excellent”, which corresponded to complete restoration of function and relief of pain in the target joint, was given by 7 (23.3%) patients; the effect was rated as good and satisfactory by 10 (33.3%) and 9 (30%) patients, respectively. And only in 4 (13.3%) patients the effect of treatment was weak.

AMBENIUM® parenteral was well tolerated. There were no cases of serious adverse events (AEs) that required discontinuation of further administrations of the drug. Depending on the degree of increase in alanine aminotransferase (ALT) and alkaline phosphatase (ALP) levels, drug-induced liver injury was classified as hepatocellular (cytolytic), cholestatic, or mixed. During therapy, in 3 (10%) patients, an increase in ALT levels was observed to be no more than 2 times the upper limit of normal, and in 2 (6.7%) patients, an increase in the level of alkaline phosphatase was observed. In all cases, drug-induced liver damage was assessed as mild and did not require exclusion of patients from the study.

There were no cases of hypersensitivity, and no redness or hardening of the soft tissue at the injection sites was observed. As the pain intensity decreased, patients did not require additional intake of another NSAID.

Discussion

Our data indicate the effectiveness of intramuscular injections of the drug AMBENIUM® parenteral for pain in the knee joint associated with OA. By the end of the observation, the severity of pain according to VAS decreased by almost 2 times. Moreover, a significant improvement was noted after 2 weeks. after the start of therapy, and then the severity of the effect increased. This result seems especially important, since all patients had previously received conservative treatment with NSAIDs, which did not allow significant improvement in their condition.

Our data confirm the results of a series of studies on the effectiveness of the use of parenteral forms of NSAIDs conducted in our country and abroad. V.B. Vasilyuk et al. [10] compared the effectiveness of intramuscular administration of phenylbutazone and diclofenac in patients with acute low back pain. The mean change in VAS pain intensity in the phenylbutazone group was statistically significant (p<0.001). In the same group, a smaller (29%) number of AEs was noted. In PM Brooks et al. [11] analyzed the effectiveness of different doses of phenylbutazone (300 and 50 mg). Before the start of the study, the articular index (AI) was 11.8±1.5 in the first group and 17.5±2.8 in the second (p=0.05). After 2 weeks observation in both groups there was a significant decrease in AI to 2.3±0.1 and 3.8±0.6, respectively, p=0.01).

In 2021, M. Worboys et al. [12] indicated excessive concerns regarding AEs with the use of phenylbutazone. The high frequency of AEs, including severe ones, depended less on the drug itself and more on the dose and duration of its use. In the case of adequate selection of dosage and frequency of administration, phenylbutazone as an analgesic that provides a short-term effect appears to be a completely safe drug, including in the presence of comorbid pathology. Its use does not carry excessive risks and can give good results.

In the study, there were no serious AEs that could cause gastrointestinal bleeding, liver or kidney dysfunction.

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