DIKVOL

Diclofenac

Solution for injections 75mg/3ml in ampoules.

Chemical name: 2-[(2,6-Dichlorophenyl-amino] benzol acetic acid, in the form of sodium salt).

Pharmacological group: Nonnarcotic analgetics, including non-steroid and other anti-inflammatory agents.

Pharmacology: Pharmacological action- anti-inflammatory, pain relieving, antipyretic, antirheumatic, antiaggregatory. It inhibits cyclooxygenase, as a result, the reactions of arachidonic cascade are blocked and the synthesis of prostaglandin E2, prostaglandin F2alpha, thromboxane, prostacyclin, leukotrienes and the emission of lysosomal enzymes; suppresses thrombocyte aggregation; in long-term application it gives desensitizing effect; in vitro causes retardation of proteoglycan in cartilages in concentrations similar to those observed in a man.

In intramuscular injection Cmax in plasma is reached in 10–20 minutes, protein binding- more than 99%. It penetrates well into the tissues and synovial fluid, where its concentration grows lower, in 4 hours it reaches higher values than in plasma. Approximately 35% is eliminated in the form of metabolites with feces; about 65% is metabolized in liver and is eliminated through kidneys in the form of non-active derivatives (in the unchanged form less than 1% is eliminated). Plasma T1/2- about 2 hours, synovial fluid — 3–6 hours; in adhering of recommended interval it does not cumulate. It relieves the pain in rest state and in motion, morning stiffness, arthrocele, improves functional ability of joints.

In inflammatory processes, arising after operations and traumas, quickly relieves both spontaneous pain and pain on movement, lowers inflammatory edema in wound site. In patients with polyarthritis, receiving course treatment, the concentration of synovial fluid in tissues is higher than in blood serum. In anti inflammatory action it excels acetylsalicylic acid, butadiene and ibuprofen; the data is available that the clinical effect is more pronounced and it is tolerated better compared to indometacin; in rheumatism and Marie-Striinipell disease it is equivalent to prednisolone and indometacin.

Indications: Inflammatory diseases of joints (rheumatoid arthritis, rheumatism, ankylosing spondylitis, chronic urarthritis), degenerative diseases (osteoarthrosis deformans, osteochondrosis), lumbago, ischias, neuralgia, myalgia, extra-articular tissue diseases (tendovaginitis, bursitis, rheumatic soft tissue involvement), posttraumatic pain syndromes, accompanied by inflammation, postoperative pains, bad attack of gout, primary algodismenorrhea, adnexitis, migraine episodes, renal and biliary colic, infections of ENT-organs, pneumonia residual effects.

Contraindications: Hypersensitivity (including nonsteroidal anti-inflammatory drugs), dyshematopoiesis of the uncertain etiology, «aspirin» bronchial asthma, childhood (under 6 years of age), last pregnancy trimester.

Application limitations: Liver and kidney malfunction, heart insufficiency, porphyria, work requiring increased attention, pregnancy, lactation (breast-feeding should be stopped).

Side effects: the increase of transaminase level in blood serum, headache, dizziness, agitation, insomnia, irritation, fatiguability, local allergic reactions, photosensibilization, purpura, increase of arterial pressure. In intramuscular injection- burning, rarely- formation of infiltrate.

Interaction: Increases the concentration of lithium, digoxin, indirect anticoagulants, oral antidiabetic preparations in blood. Intensifies the toxicity of methotrexat, cyclosporine, the possibility of glucocorticoid side effects development, lowers the effect of diuretics. The concentration in plasma decreases in application of acetylsalicylic acid.

Method of application and doses: As primary therapy (for e.g. in post surgical period) intramuscularly or intravenously- 1–2 ampoules daily during not more than 2 days.

Precaution measures: In long-term treatment regular observance of blood picture and liver function is necessary. During first 6 months of pregnancy the preparation should be administered according to strict indications and in the smallest dosage. Due to the possible decrease of reaction rate, it is not recommended to drive or work with equipment.

Form of issue: ready-made solution for injections in ampoules, 75/3ml, 5 ampoules in a package.