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The most popular analgesics
Pain syndrome in osteoarthritis (OA), rheumatoid arthritis (RA) and other inflammatory diseases of the joints is the main reason for visiting a doctor, significantly limits the ability of patients, including the ability to work. The main group of pain relief drugs prescribed for OA and RA are non-steroidal anti-inflammatory drugs (NSAIDs). However, the group of NSAIDs is represented by drugs of different chemical nature, which causes heterogeneity of clinical efficacy and safety. [1]. NSAIDs are the most popular analgesics, but some of them carry gastrointestinal (GI) and cardiovascular (CV) risks.
Selectivity for “bad” cyclooxygenase
Cyclooxygenase (COX) is the main target molecule of NSAIDs, this enzyme has two of the most studied isoforms that stimulate the production of various products from the same substrate – arachidonic acid (AA) [2]. COX 1 stimulates the formation of substances that function to a greater extent under normal conditions, while COX 2 is an isoform whose expression is increased during inflammation. COX 2 stimulates the synthesis of pro-inflammatory AA products. When taking non-selective for COX 2 drugs, the risk of adverse reactions (AR) from the gastrointestinal tract increases, so selectivity for COX 2 is a safety factor for NSAIDs. The most selective NSAID for COX 2 is etoricoxib. [3].
Made in Russia
Etoricoxib under the trade name Etorelex has been registered in Russia since 2019. The emergence of a highly selective NSAID in a wide range of oral dosages has increased the availability of medical care for patients with OA and RA. The Russian-made drug has a relatively low cost, which is important for patients who need frequent pain relief.
Efficacy in pain relief
Etoricoxib, celicoxib, diclofenac, indomethacin, ibuprofen, and paracetamol are used to treat OA and RA. Various clinical studies have shown that etoricoxib (Etorelex) is as good or superior to other NSAIDs in pain relief. [3]. In addition, the advantage of etoricoxib is the rapid onset of the effect (after 28 minutes), the long-term effect with a single dose (up to 24 hours).
Safety of the gastrointestinal tract and cardiovascular system
Coxibs are four times more GI safe than other NSAIDs [4]. The safety of celecoxib and etoricoxib (Etorelex) was found to be comparable. A comparison of GI risks of AE between etoricoxib and traditional NSAIDs (naproxen and diclofenac) in the treatment of OA and RA was presented by Feng et al. in a meta-analysis. [2]. A meta-analysis showed that with etoricoxib, the risks of GI AE were lower than with naproxen (0,59 (95% CI, 0,48–0,72) and diclofenac (0,67 (95% CI, 0,59 –0,76).
The risk of damage to the cardiovascular system, obviously, does not depend on the selectivity to COX 2 and generally characterizes the entire group of NSAIDs, including coxibs. [5]However, pain in OA and RA has also been shown to be a significant risk factor for cardiovascular disease. To date, more and more evidence suggests that against the background of the use of NSAIDs, the risk of cardiovascular disease due to chronic pain syndrome is reduced. [3].
Thus, etoricoxib (Etorelex) is not inferior or superior to other NSAIDs in terms of effectiveness, and also has advantages in terms of speed and duration of the onset of effect. Etoricoxib has a more favorable safety profile in relation to the gastrointestinal tract and cardiovascular system than most members of this group, which allows the drug to be used for urgent and chronic pain.