Diclofenac is the optimal choice of non-steroidal anti-inflammatory drug for a family doctor

The range of non-steroidal anti-inflammatory drugs for local external action is quite wide. In this regard, the choice between these drugs is relevant, namely, which is better: Diclofenac or Diclak. These drugs are actively prescribed for various diseases of the musculoskeletal system. Both drugs have a common active drug substance - diclofenac sodium. Therefore, their action is the same.

Comparison of the effectiveness of Diclofenac and Diclac

Diclofenac is more effective than Diclak - this means that the ability of the drug substance to provide the maximum possible effect is different.
For example, if the therapeutic effect of Diclofenac is more pronounced, then with Diclak it is impossible to achieve this effect even in large doses.

Also, the speed of therapy is an indicator of the speed of therapeutic action; Diclofenac and Diclac are also different, as is bioavailability - the amount of a drug substance reaching the place of its action in the body. The higher the bioavailability, the less it will be lost during absorption and use by the body.

Comparison of the safety of Diclofenac and Diclac

The safety of a drug includes many factors.

At the same time, in Diclofenac it is quite similar to Diklak. It is important where the drug is metabolized: drugs are excreted from the body either unchanged or in the form of products of their biochemical transformations. Metabolism occurs spontaneously, but most often involves major organs such as the liver, kidneys, lungs, skin, brain and others. When assessing the metabolism of Diclofenac, as well as Diklak, we look at which organ is the metabolizing organ and how critical the effect on it is.

The risk-benefit ratio is when the prescription of a drug is undesirable, but justified under certain conditions and circumstances, with the obligatory observance of caution in use. At the same time, Diclofenac does not have any risks when used, just like Diclak.

Also, when calculating safety, it is taken into account whether only allergic reactions occur or possible dysfunction of the main organs. In other matters, as well as the reversibility of the consequences of using Diclofenac and Diclac.

How do they work and in what cases are the drugs prescribed?

Gels Diclak and Diclofenac, being non-steroidal anti-inflammatory drugs for external use, have an analgesic and anti-inflammatory effect. Taking any of these drugs reduces pain, eliminates joint stiffness that appears after waking up in the morning, and their swelling. Treatment with Diclak or Diclofenac gels helps restore limb movement and helps reduce tissue swelling.

Diklak is also available in the form of ointment, tablets and injection solution. Diclofenac has the same dosage forms.

Diclofenac sodium suppresses the production of prostaglandins, which are conductors of inflammatory processes, and as a result, the cause of pain in the affected areas.

Indications for the purpose and use of these external agents are as follows:

• joint pathologies such as osteoarthritis and osteochondrosis
• rheumatism
• muscle and tendon sprain
• rheumatoid arthritis
• injuries and bruises
• myalgia and arthralgia resulting from excessive physical activity

The instructions for the drugs Diclofenac and Diclak recommend using them as follows: 2-4 g. The product is applied to the problem area in a thin layer, using light rubbing movements. This manipulation is repeated 2-3 times a day. Do not apply the gel to damaged skin and mucous membranes. The duration of treatment should not be more than 2 weeks, except in cases determined by the attending physician.

Comparison of addiction between Diclofenac and Diclac

Like safety, addiction also involves many factors that must be considered when evaluating a drug.

So, the totality of the values ​​of such parameters as “syndrome o” in Diclofenac is quite similar to the similar values ​​in Diklak. Withdrawal syndrome is a pathological condition that occurs after the cessation of intake of addictive or dependent substances into the body. And resistance is understood as initial immunity to a drug; in this it differs from addiction, when immunity to a drug develops over a certain period of time. The presence of resistance can only be stated if an attempt has been made to increase the dose of the drug to the maximum possible. At the same time, Diclofenac has quite a small amount of “syndrome”, just like Diclak.

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.

Comparison of side effects of Diclofenac and Diclac

Side effects or adverse events are any adverse medical event that occurs in a subject after administration of a drug.

Diclofenac's side effects are almost the same as Diclak's. They both have few side effects. This implies that the frequency of their occurrence is low, that is, the indicator of how many cases of an undesirable effect of treatment are possible and registered is low. The undesirable effect on the body, the strength of influence and the toxic effect of Diclofenac are similar to Diklak: how quickly the body recovers after taking it and whether it recovers at all.

Characteristics of non-steroidal anti-inflammatory drugs

Diclofenac is a phenylacetic acid derivative used in pharmacological preparations in the form of sodium salt. The mechanism of action of the non-steroidal anti-inflammatory drug is based on its ability to block the enzyme cyclooxygenase (COX), which stimulates the production of mediators of pain and inflammation - prostaglandins and bradykinins from arachidonic acid, as well as the bioactive compounds prostacyclin and thromboxane. The use of Diclofenac in tablets, ointments, parenteral solutions has a diverse effect on the human body:

• reducing the severity of pain;
• relief of inflammation and swelling;
• elimination of fever.

In medical practice, analogues of Diclofenac are distinguished based on their composition and therapeutic effect. This classification is necessary to quickly select a replacement NSAID if it is intolerable or exhibits an excessive number of side effects. Structural analogues of Diclofenac include Diclogen, Ortofen, Dikloberl, Voltaren, Diclak, Naklofen. They are of interest, first of all, to patients, since the cost of drugs can vary significantly. For example, the price of Ortofen ointment is 30-40 rubles, and for a package of Voltaren gel you will have to pay at least 200 rubles.

If a doctor prescribes an expensive structural analogue of Diclofenac, then you should not suspect him of any self-interest. The high price is often due to the high quality of the additional and active ingredients included in the ointment or tablets. Such a drug will be better absorbed and cause fewer side effects.

Rheumatologists, traumatologists, and neurologists rarely replace Naklofen with Diclogen or Dicloberl. In case of intolerance to Diclofenac or its low effectiveness in the treatment of any diseases, they include in therapeutic regimens other non-steroidal anti-inflammatory drugs that are similar in pharmacological action:

• Meloxicam;
• Nimesulide;
• Ketoprofen;
• Ketorolac;
• Metamizole;
• Perekoksib;
• Phenylbutazone;
• Indomethacin;
• Ibuprofen;
• Acetylsalicylic acid;
• Piroxicam.

These analogues of Diclofenac have few differences in instructions for use, price, and consumer reviews. But there is also a difference in action, which is caused by the biochemical properties of the active ingredients. In vitro studies have found that all NSAIDs inhibit prostaglandin production to varying degrees. The relationship between their anti-inflammatory and analgesic properties and the degree of mediator suppression has not yet been proven.

Diclofenac and its analogues are characterized by the presence of similar chemical and pharmacological activity. Most of them are weak organic acids that are quickly absorbed in the digestive tract. All NSAIDs in the systemic circulation bind to albumin and are evenly distributed in tissues. Non-steroidal anti-inflammatory drugs are classified into the following groups:

• short-lived (less than 6 hours);
• long-lived (more than 6 hours).

To replace Diclofenac, the doctor may prescribe both a short-lived and a long-lived analogue. This is due to the fact that there is no clear relationship between the duration of the drug’s presence in the human body and the severity of the therapeutic effect. Almost all NSAIDs quickly accumulate in the synovial fluid of the joints and are then metabolized in hepatocytes (liver cells) through the process of glucuronidation, forming biologically active and inactive conjugates. They are evacuated by the kidneys by approximately 65-80%.

Comparison of ease of use of Diclofenac and Diclac

This includes dose selection taking into account various conditions and frequency of doses. At the same time, it is important not to forget about the release form of the drug; it is also important to take it into account when making an assessment.

The ease of use of Diclofenac is approximately the same as Diclak. However, they are not convenient enough to use.

The drug ratings were compiled by experienced pharmacists who studied international research. The report is generated automatically.

Last update date: 2020-12-13 10:32:40