Use in drug addicts
Diclofenac belongs to the group of non-narcotic analgesics (unlike morphine, codeine, fentanyl and tramadol).
Even in large doses, it is not a psychoactive drug and has no addictive potential, that is, with short- or long-term use it does not cause either physiological or psychological dependence. However, you should be aware that diclofenac can delay the active breakdown products of morphine in the blood. This is important to remember for those taking morphine - a side effect such as respiratory depression may occur.
Side effects
Diclofenac (and most other nonsteroidal anti-inflammatory drugs) blocks the production of prostaglandins. These same substances are included in the layer that protects the gastric mucosa from damage and chemical irritants. That is, long-term use of the analgesic diclofenac can lead to the development of gastritis and ulcers of the stomach and duodenum. Other rare side effects:
- nausea, discomfort in the upper abdomen, abdominal pain
- excess gas, constipation or diarrhea
- headaches and dizziness
- insomnia, tinnitus, irritability, malaise and fatigue
Some side effects are specific: they depend on the form of use of diclofenac. So, if you use external agents (gel, ointment), redness or rash on the skin is possible, and when administering rectal suppositories, inflammation of the rectum is possible (very rare); with intramuscular administration, a small inflammatory focus may form at the injection site.
Diclofenac is the optimal choice of non-steroidal anti-inflammatory drug for a family doctor
Professor R.M. Balabanova
Institute of Rheumatology RAMS, Moscow
Family medicine began its revival in Russia at the end of the 20th century. In the diagnosis and treatment of rheumatic diseases, the role of the family doctor is especially significant, since these diseases can occur in family members of different ages - from children to the elderly. Rheumatic diseases are quite widespread in the population, especially such as pain in the lower back, osteoarthritis, osteoporosis, reactive arthritis, rheumatoid arthritis, psoriatic arthritis. The proportion of gout has increased. It is well known that first-degree relatives have an increased risk of developing rheumatism, rheumatoid arthritis, and ankylosing spondylitis, which may be due to both the carriage of a certain genetic marker and intrafamilial contamination of a bacterial and/or viral infection [5].
In the treatment of rheumatic diseases, the role of a correct lifestyle is important, therefore the family doctor must teach the patient and family members proper nutrition, the basics of physical and mental rehabilitation, because all diseases belonging to ICD class XIII are accompanied by almost constant pain in various parts of the musculoskeletal system, which leads to a decrease in the quality of life of patients, the development of depression, and their exclusion from the social environment and professional activities [2].
The main task of the doctor is primarily to reduce pain, improve or restore the patient's functional ability. To achieve this goal, non-steroidal anti-inflammatory drugs (NSAIDs) are optimal, accounting for 4.5% of all prescriptions. Among NSAIDs, diclofenac is the gold standard for assessing analgesic and anti-inflammatory effects.
Diclofenac is a derivative of arylacetic acid, available in the form of sodium and potassium salts. There are more than 50 drugs on the pharmaceutical market under different brand names, which may differ in therapeutic effect, number and severity of side effects.
Diclofenac (D) compares favorably with other NSAIDs in that it is available in various dosage forms: regular and prolonged tablets, injections, as well as for local therapy in the form of ointments, creams, and gels.
For oral administration, D is available in the form of tablets 25100 mg, incl. coated (film, enteric), regular and delayed (retarded) release, the latter provides a longer effect of the drug. There are also 50 mg D tablets and 75 mg capsules. It should be especially noted that there is a form D for children, film-coated tablets of 15 mg.
For parenteral administration, use a 2.5% solution in a 3 ml ampoule (75 mg of active substance). The doctor has D for rectal administration of suppositories of 50 and 100 mg, and for children 25 mg.
Systemic intake of D can be limited using forms for local use: 1.5% gel, 1.2% ointment, 1% emulgel. This method of treatment D can be used not only to relieve joint pain, but also for traumatic injuries of the musculoskeletal system, myositis, phlebitis.
Recommended daily doses are 75150 mg in 23 doses. Treatment should begin with the minimum effective dose. Daily fluctuations in the symptoms of the disease require clarification of the timing of admission. Synchronizing the administration of D allows you to increase the effectiveness and reduce the number of side effects, especially when taking short-lived NSAIDs, which include D. It should be remembered that the analgesic and anti-inflammatory activity of the drug does not always correspond to the same dose. As a rule, the analgesic effect is achieved with a lower concentration of the drug.
D is an organic acid with a relatively low pH, due to which it actively binds to plasma proteins and accumulates at the site of inflammation. It penetrates well into the joint cavity, reaching a maximum concentration 24 hours later than in plasma (240 and 60 minutes, respectively). The half-life of D from plasma is 130, from synovial fluid 200 minutes, and the maximum concentration is 0.6 and 0.2 μg/ml, respectively. Parenteral administration of D allows one to reach maximum concentration after 10-30 minutes, and rectal administration after 60 minutes. Taking 100 mg of retardated form D slows down the achievement of maximum plasma concentrations by up to 5 hours.
Food intake slows down the rate of absorption of D. D should be prescribed with caution to patients with insufficient renal and liver function, because At the same time, the metabolism and excretion of the drug changes. In these cases, the daily dose of the drug should be reduced.
The family doctor should keep in mind that D can be used not only for rheumatic diseases, but also for diseases of the ENT organs, headaches, algomenorrhea, and fever due to ARVI. As a short-lived drug, D can be prescribed to lactating women (but not pregnant women!).
The main mechanism of action of D, like other NSAIDs, is the suppression of the activity of the enzyme cyclooxygenase (COX), responsible for the conversion of arachidonic acid into prostaglandins (PG), prostacyclin, and thromboxane. COX has 2 isoforms that differ in a number of parameters, in particular, localization in tissues and functional ability. COX1 (constitutive) is present in varying amounts in almost all tissues and regulates the formation of physiological PGs. COX2 is practically not detected normally, but its level increases tens and hundreds of times during inflammation. At the same time, in some tissues it plays the role of a physiological enzyme (brain, kidneys, bone tissue, reproductive system). Other mechanisms of action of NSAIDs are also discussed, in particular, the suppression of uncontrolled proliferation of tumor cells as a result of PG inhibition of cell apoptosis. This fact is confirmed by data on the protective effect of NSAIDs on epithelial tumors and Alzheimer's disease [4].
D refers to drugs that equally inhibit COX1 and COX2, which explains its greater safety, especially with regard to the development of complications from the gastrointestinal tract (GIT). D occupies an intermediate position among acid NSAIDs in terms of the risk of gastrointestinal ulceration. For comparison, the toxicity index of indomethacin is 6.3, and D is 3.9. The relative risk of bleeding in persons over 60 years of age when taking D is 4.2, indomethacin is 11.3, and piroxicam is 13.7.
When prescribing NSAIDs, the doctor must inform his patient about the possibility of developing negative phenomena, among which, first of all, one should be wary of ulceration of the gastrointestinal mucosa. Risk factors for gastrointestinal tract damage include: female gender, age over 65 years, a history of ulcers, taking high doses of the drug, combined use of glucocorticosteroids and anticoagulants, smoking, alcohol consumption, H. pylori infection. If complaints from the gastrointestinal tract appear, it is necessary to perform an endoscopy, and if you are taking D systematically, this procedure should be prescribed every 46 months, because NSAID gastropathy is often asymptomatic (silent).
The hepatotoxic effect of D occurs less frequently than during treatment with indomethacin, mainly in elderly people suffering from osteoarthritis and rheumatoid arthritis. Elderly patients are more likely to have a negative effect on kidney function and the circulatory system, especially if there are signs of this pathology. The risk of circulatory decompensation in elderly patients with latent congestive heart failure while taking NSAIDs is close to that with gastrointestinal complications [4]. The family doctor is well aware of the presence of concomitant diseases of his patients, so it is easier for him to avoid possible complications when using D in combination with other drugs. It is known that D increases the plasma concentration of digoxin, lithium, cyclosporine A, incl. increases its nephrotoxicity; increases the toxicity of methotrexate. Against the background of potassium-sparing diuretics, D increases the risk of hyperkalemia, and against the background of anticoagulants, the risk of bleeding. D reduces the effect of diuretics, antihypertensives and hypnotics. Concomitant use of antidiabetic agents can lead to both hypo and hyperkalemia.
In recent years, much attention has been paid to selective COX2 inhibitors. A comparative study of diclofenac sodium at a daily dose of 150 mg and celecoxib at a dose of 200 mg showed that clinical efficacy and improvement in the functional state of joints in patients with osteoarthritis were the same for these drugs, which confirms the importance of diclofenac as the gold standard NSAID in the new, 21st century [ 3]. Diclofenac sodium should be used to treat chronic diseases. For acute pain, pain in the lower back, it is preferable to take potassium salt D (Rapten Rapid). As shown in works [1,6], Rapten Rapid has a persistent analgesic effect 2 days faster than diclofenac sodium, ibuprofen, and indomethacin. With a minimum of side effects (8%, 10%, 5%, 15%, respectively), which did not require discontinuation of the drug.
Rapten Rapid is prescribed to adults at a dose of 50-150 mg/day in 23 doses; in pediatrics only to children over 14 years of age.
Rapten Rapid has a short half-life. After 2 hours, the maximum plasma concentration is reached, and after 7 hours it is completely eliminated. The drug is characterized by the absence of accumulation and enterohepatic circulation.
Rapten Rapid can be recommended not only for the relief of acute pain, but also as an analgesic for induction therapy for 10-14 days with a further transition to diclofenac sodium.
Thus, diclofenac can be the drug of choice in the treatment of acute and chronic pain, inflammation, and the variety of dosage forms allows you to choose the most effective and safe one.
Literature:
1. Zborovsky A.B., Zborovsky B.V., Derevyanko L.I. Experience with the use of raptenarapide in the treatment of articular syndrome in RA. Scientific and practical rheumatology, 2001, 2, 3742.
2. Nasonova V.A. International decade dedicated to osteoarticular disorders. RMJ, vol. 8, no. 9, 2000, 36971.
3. Nasonova V.A. Rational use of NSAIDs in rheumatology. RMJ, 2002, vol. 10, no. 6, 302306.
4. Nasonov E.L. Nonsteroidal anti-inflammatory drugs for rheumatic diseases: standard of treatment. RMJ, 2001, vol. 9, no. 78, 265270.
5. Nasonova V.A., Denisov L.N. Rheumatic diseases in the practice of a family doctor. RMJ, 2001, vol. 9, no. 23, 103841.
6. Shostak N.A., Denisov L.N., Shemetov D.A. Efficacy and tolerability of rapten rapid in patients with low back pain syndrome. Scientific and practical rheumatology, 2001, No. 5, 8486.
Published with permission from the administration of the Russian Medical Journal.
