Medicine

Diclofenac analogues: rating of non-steroidal anti-inflammatory drugs

Diclofenac analogues: rating of non-steroidal anti-inflammatory drugs

What Diclofenac?

Diclofenac (Diclofenac) is an NSAID (non-steroidal anti-inflammatory drug), which belongs to the group of phenylacetic acid derivatives. The drug was developed in 1966 and is currently widely used in inflammatory diseases of the musculoskeletal system, such as arthritis, osteoarthritis, osteochondrosis, etc.
IMPORTANT! According to WHO statistics, various diseases of the musculoskeletal system (ODA) affect 80% of the world's population, mostly people of working age: from 30 to 50 years. It is believed that diseases of the musculoskeletal system occupy the third place in the structure of modern diseases, second only to cardiovascular and oncological diseases. According to official statistics, the general dynamics of diseases of the musculoskeletal system in Russia since the end of the 20th century has been increasing by approximately 30% every decade.

The principle of action of nonsteroidal drugs

One of the most common pathological conditions in diseases of the musculoskeletal and connective tissue is pain. It is accompanied by impaired mobility, inflammation and fever. In the focus of inflammation, the cells of the affected tissues produce the hormones prostaglandins. These physiologically active substances of a lipid nature are produced by the body during swelling and inflammation, irritating the tissues of the joints, causing redness and pain. Prostaglandins act on special mechanisms in the brain responsible for thermoregulation, resulting in an increase in body temperature.

Launching the release of prostaglandins in the body is carried out by cyclooxygenase enzymes (hereinafter referred to as COX). The action of NSAIDs, including Diclofenac, is aimed at stopping the production of COX. Non-steroidal anti-inflammatory drugs block the synthesis of cyclooxygenase, which means they stop the production of prostaglandins. Therefore, with the help of NSAIDs it is possible to influence the development of the inflammatory process.

IMPORTANT! “Non-steroidal anti-inflammatory drugs are among the most commonly used drugs in both prescription and over-the-counter drugs. This is due to a wide range of therapeutic effects. However, there is a downside: these are the drugs that most often cause unwanted drug reactions,” Viktor Anatolyevich Gankov, surgeon of the highest qualification category, MD, professor at the Department of General Surgery of the ASMU.

Non-steroidal anti-inflammatory drugs, in addition to relieving inflammation, lowering temperature and eliminating pain, have a number of positive side effects. For example, doctors use this group of drugs with increased blood viscosity to improve its rheological properties, thin it, reduce clotting and prevent thrombosis. PVPS increase the percentage of plasma (liquid part) in the total blood volume, reduce lipid content and reduce its viscosity. Therefore, with anemia and disorders of the coagulation system (hemocoagulation), this type of drug is contraindicated.

Classification of non-steroidal anti-inflammatory drugs

So, the action of NSAIDs is selective or non-selective inhibition of cyclooxygenases and prostaglandin synthesis.
In a healthy body, there is a balance between all types of COX. But it is violated with the development of the disease, and its adjustment is required. NSAIDs act on cyclooxygenase isoforms in different ways, so it is important to choose the right drug in order to obtain the desired therapeutic effect and prevent unwanted reactions.

According to their effect on COX, NSAIDs are divided into the following groups: -marked”>

  • selective COX-1 inhibitors (low doses of acetylsalicylic acid);
  • non-selective COX inhibitors (most “standard” NSAIDs);
  • predominantly selective COX-2 inhibitors (nimesulide, meloxicam);
  • specific (highly selective) COX-2 inhibitors (coxibs).
  • In the early 1970s, the British pharmacologist John Robert Vane proved that the anti-inflammatory effect of NSAIDs is associated with their ability to inhibit COX-2, and common side effects: damage to the gastrointestinal tract, kidneys, impaired platelet aggregation – with suppression of COX-1 activity.
    Diclofenac (Voltaren, Naklofen, Ortofen, Diklak, Diclonac P, Vurdon, Olfen, Dolex, Dicloberl, Clodifen) is actively used in the treatment of diseases accompanied by pain of any origin, has a combined anti-inflammatory and analgesic effect on both COX isoforms. To a greater extent, the effect is pronounced on COX-2.

    The inhibition of COX-1 in Diclofenac is weaker than that of Ibuprofen and Naproxen, therefore Diclofenac rarely causes adverse reactions from the gastrointestinal tract.

    Despite the slight effect on COX-1, diclofenac shows greater efficacy than selective COX-2 inhibitors (meloxicam, celecoxib) in cases of treatment, such as arthritis, when COX-1 is involved in the pathogenesis of the disease.

    Indications for the use of NSAIDs:

    • gout in any form;
    • arthritis, arthrosis;
    • pain syndrome in oncology;
    • postoperative pain;
    • feverish conditions;
    • renal colic;
    • soft tissue inflammation;
    • osteochondrosis;
    • cephalgia;
    • migraine

    Contraindications:
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  • individual intolerance to the components of the drug;
  • ulcerative lesions of the digestive tract;
  • leukopenia and thrombopenia;
  • severe dysfunction kidneys and liver;
  • pregnancy.
  • The choice of a drug is always made on the basis of indications, taking into account contraindications. In addition, in the process of taking medications, it is necessary to monitor unwanted reactions of the body. These measures are necessary to prevent the development of complications or exacerbations of chronic diseases.

    Adverse drug reactions are any unintended and harmful reaction to the human body that occurs in response to the use of drugs in recommended doses for the purpose of prevention, treatment and diagnosis, or to change physiological functions. (International drug monitoring the role of the hospital. Geneva WHO, 2008)Diclofenac analogues are also inhibitors of COX-1 and COX-2, their mechanisms of action are similar. Such drugs differ in the main active ingredient in the composition, as well as indications and contraindications. Therefore, before buying and taking the drug, we recommend that you consult with your doctor.

    Diclofenac analogues:

    • Dolgit (Dolorgiet, Germany). The drug, the active substance is ibuprofen. Release form – gel for external use. Contraindications – local allergic reaction.
    • Nurofen Express Forte (Reckitt Benckiser, Netherlands). Pain reliever based on ibuprofen. Release form – capsules for internal use.
    • Voltaren Emulgel (Novartis Pharma, Switzerland). The active substance is diclofenac sodium. Release form – patches, gels, suppositories.
    • Note! Artrofoon is an innovative drug of domestic development. Note that it does not belong to the group of NSAIDs, but it can be used in joint therapy with them. It contributes not only to the relief of pain, but also to the elimination of the cause of pain in a natural, physiological way, unlike fast-acting remedies with a short-term effect. In addition to pain, the drug relieves swelling and stiffness in the joints and reduces the frequency of exacerbations. It has a lasting effect, promotes a longer remission and has practically no side effects, therefore it does not have a negative effect on the gastrointestinal tract.

    Diclofenac can be replaced

    Diclofenac analogs are drugs that which have a similar mechanism of action. In addition to a direct effect on the inflammatory process, they can have a concomitant effect on the body, differ in contraindications, negative reactions and side effects. or health problems precluding the use of NSAIDs, in such cases monotherapy with Artrofoon is possible.
    IMPORTANT! Before taking any medicine, you should consult your doctor. Be healthy!

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