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Prospects for anti-inflammatory therapy of osteoarthritis
Last reviewed: 23.04.2024
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A new direction in the symptomatic treatment of osteoarthritis and other diseases of the musculoskeletal system is the use of combined inhibitors of cyclooxygenase and lipoxygenase - COX and LOG. Data from experimental studies suggest that an alternative (lipoxygenase) pathway for the metabolism of arachidonic acid, which leads to the formation of leukotrienes (LT), causes a number of inflammatory effects in patients with joint diseases. So, ЛТВ 4 is one of the most powerful factors of leukocyte chemotaxis, it also induces the production of cytokines by T lymphocytes and immunoglobulins in B lymphocytes. In addition, the so-called cysteinyl RT (or peptidoleicotrienes) - LTS 4, LTO 4 and LTE 4 - cause a number of inflammatory effects, among them edema, contraction of smooth muscles, which in the mucosa of the upper gastrointestinal tract can cause ischemia followed by erosion and ulcers. Two other forms of LOG-12-OG and 15-LOG-catalyze the formation of lipoxins, which have an anti-inflammatory effect.
The inhibition of the cyclooxygenase pathway by nonselective or selective NSAIDs can cause a shift in the cascade of arachidonic acid towards the lipooxygenase pathway with an increase in the production of leukotrienes and lipoxins. Therefore, it would be advisable to block both ways of arachidonate metabolism-cyclooxygenase and lipooxygenase-to obtain an anti-inflammatory and analgesic effect. However, the important point is the preservation of the production of anti-inflammatory lipoxins.
Lycophelone is a new pharmacotherapeutic agent blocking COX and 5-LOH. In studies in vitro, lycophelone inhibited COX (1C 50 ~ 0.16-0.21 uM) and 5-LOG (1C 50 ~ 0.18-0.23 цМ).
The new technology, called "host - guest", informs "classical" nonselective NSAIDs optimal pharmacokinetic properties and improves their tolerability. RVS is a new pharmacotherapeutic agent in which a molecule of piroxicam (a guest molecule) is introduced into P-cyclodextrin (a host molecule). This combination provides:
- high solubility,
- rapid absorption,
- minimal contact with the mucosa of the digestive tract,
- almost 100% bioavailability,
- quick start of action,
- pronounced analgesic effect when taken 1 time per day.
In a pilot comparative controlled study of the use of PBC (20 mg / day) and etodolac (400 mg / day) in 30 patients with pain syndrome in the lower spine, the first had a more pronounced analgesic effect. In another small controlled study, the efficacy of RVC at a dose of 20 mg / day was compared in 60 patients with musculoskeletal disorders with intramuscular injections of diclofenac (75 mg) and ketoprofen (100 mg). All three drugs had a rapid and pronounced analgesic effect. Of course, it is impossible to judge the effectiveness and tolerability of RVS in these studies, the results obtained require confirmation in large multicenter studies.
[1], [2], [3], [4], [5], [6], [7], [8], [9], [10], [11], [12], [13]