Diclofenac sodium

Diclofenac sodium is a drug from the NSAID group, which is an α-toluic acid derivative.

[1], [2], [3], [4], [5]

Indications of the diclofenac sodium

It is used in such cases:

• with rheumatoid arthritis, rheumatism, Bechterew's disease, and also with inflammation in the area of the joints with soft tissues, against which there are painful sensations (this includes traumas of the ODA);
• with arthrosis with neuritis, spondyloarthrosis and radiculitis, and also with exacerbation of gout, lumbago and neuralgia;
• with a primary degree of dysmenorrhea.

A short-term course of medicine is prescribed to eliminate bursitis or tendonitis, as well as pain that develops after surgical interventions.

[6]

Release form

The release is carried out in the form of an injection solution, in ampoules with a volume of 3 ml. Inside the box contains 5 or 10 ampoules with a solution.

[7], [8], [9], [10]

Pharmacodynamics

The drug has strong anti-inflammatory and analgesic properties, as well as moderate antipyretic effects. During therapy with rheumatic diseases, it reduces pain in the joints (both in motion and at rest), weakens their swelling and stiffness, which occurs in the morning, and at the same time helps to increase the amount of movement inside the affected joints. A stable effect develops after 1-2 weeks of therapy.

The drug in the form of injections is usually prescribed at the initial stages of treatment of rheumatological pathologies, as well as with pain sensations of a different origin.

[11], [12], [13],

Pharmacokinetics

Absorption.

With a 75 mg IM injection, it immediately begins to absorb - reaching peak plasma values is observed after approximately 20 minutes (the average is about 2.5 μg / ml (or 8 μmol / L)). Immediately after reaching this mark, there is a rapid decrease in the plasma parameters of the substance. The amount of active ingredient absorbed is linearly proportional to the dose size of the drug. Values of AUC for IM solution administration exceed the rectal or oral dosage form by about half, because in the latter cases, approximately half of all diclofenac undergoes the first hepatic pass.

With repeated use of drugs, its pharmacokinetics remain the same.

If the patient follows the intervals required between the injections, the cumulation of the substance does not occur.

Distribution.

Protein synthesis inside the blood serum (mostly with albumin) is 99.7%. At the same time, the average index distributive volume reaches 0.12-0.17 l / kg.

Diclofenac is able to pass into synovia, in which its peak values are observed later than in the blood plasma (approximately 2-4 hours). The average half-life of synovia is 3-6 hours. At the end of 2 hours after the peak plasma values are reached, the diclofenac level in synovia will be higher than inside the plasma, and these values will remain higher for a period of up to 12 hours.

Metabolic processes.

Part of the process of diclofenac metabolism occurs with the help of glucuronization of an unmodified molecule, but mainly by disposable and reusable methoxylation, as a result of which several phenolic decay products (3-hydroxy-, as well as 4'-hydroxy- and 5'-hydroxy-, and in addition 4 ', 5-dihydroxy with 3'-hydroxy-4'-methoxydiclofenac), most of which are converted to glucuronide-type conjugates.

Two of these degradation products are bioactive, although much less than the active substance of drugs.

Excretion.

The total level of plasma clearance of the active ingredient is 263 ± 56 ml / minute. The final half-life is equal to 1-2 hours. The half-life of 4 decay products, including 2 pharmacoactive products, is also quite short and is equal to 1-3 hours. Metabolite 3'-hydroxy-4'-methoxy-diclofenac has a longer half-life, but it generally does not have drug activity.

Approximately 60% of the administered dose of the solution is excreted in the urine under the guise of glucuronated conjugates of the unaltered active ingredient, and in addition in the form of decay products, most of which are glucuronic conjugates. Only 1% of the dose is excreted unchanged. The remainder of the injected drug is excreted under the guise of metabolites, along with feces and bile.

[14], [15], [16],

Dosing and administration

Adults injected in / m method in the amount of 75 mg, 1-2 times per day - in acute stage of the disease or in case of exacerbation of chronic pathology.

For children older than 6 years of age, the size of the dosage is chosen by the doctor (with the calculation of 2 mg / kg, it is required to inject a daily portion of the solution 2 or 3 times).

Often, the treatment course lasts for 4-5 days.

[24], [25], [26]

Use of the diclofenac sodium during pregnancy

It is forbidden to use the solution during pregnancy or lactation.

Contraindications

The main contraindications:

• an ulcer developing in the gastrointestinal tract;
• available in the history of bleeding within the gastrointestinal tract;
• hepatic / renal pathologies;
• intolerance of the medicinal product;
• acute form of the common cold, urticaria, as well as bronchial asthma and other signs of allergy caused by the use of NSAIDs;
• children's age is less than 6 years.

[17], [18], [19], [20]

Side effects of the diclofenac sodium

Among the side effects possible development of dyspepsia, bleeding and lesions of erosive and ulcerative character inside the gastrointestinal tract, and in addition symptoms of allergy, dizziness and a feeling of irritability or drowsiness. On the site of the / m introduction of the medicine, abscesses, burning sensation and necrosis of fat layers can occur.

If a patient develops any unusual symptoms, immediately consult a doctor regarding the continued use of Diclofenac sodium.

[21], [22], [23]

Interactions with other drugs

If the patient is using any other medications, you need to inform your doctor about it.

The combination of diclofenac sodium with methotrexate potentiates the toxic properties of the latter. When combined with lithium salts or digoxin, they increase their plasma values.

The drug weakens the effect of antihypertensive agents and furosemide.

Combination with other NSAIDs (eg, GCS or aspirin) increases the likelihood of bleeding in the gastrointestinal tract.

[27], [28], [29]

Storage conditions

Diclofenac sodium should be kept in a dark place inaccessible to children. Temperature mark - no more than 25ºС.

[30], [31], [32]

Special instructions

Reviews

Diclofenac sodium in the form of injections has a rapid onset of exposure - this is noted by many of the patients in their reviews. Reduction of pain symptoms is felt after 20-30 minutes, while in case of oral intake the effect of the effect develops only after 1.5-2 hours.

In the case of the / m injection, the absorption of the drug from the muscle is gradual, which allows you to limit the 1-time administration. A more detailed treatment plan is determined by the doctor.

Among the shortcomings, there is a fairly frequent development of side effects, which affect a variety of body systems - NA, GIT, skin reactions. The latter sometimes arise due to injections - at the injection site.

[33], [34],

Shelf life

Diclofenac sodium is allowed to be used for 2 years from the date of release of the drug.

[35],