Diclonat P solution for intramuscular injection is a nonsteroidal anti-inflammatory agent with a pronounced anti-inflammatory, analgesic and antipyretic effect, inhibits platelet aggregation.
Diclofenac has anti-inflammatory, analgesic and antipyretic effects. Indirectly inhibiting cyclooxygenase 1 and 2, violates the metabolism of arachidonic acid, reduces the amount of prostaglandins in the focus of inflammation. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the joint. With injuries in the postoperative period, diclofenac reduces pain and inflammatory edema.
The time to reach Cmax with intramuscular use at a dose of 75 mg is 15-30 minutes, the value of Cmax is 1.9-4.8 (on average 2.7) mcg / ml. After 3 hours after administration, plasma concentrations averaged 10% of the maximum. Communication with plasma proteins - more than 99% (most associated with albumin). Metabolism occurs as a result of repeated or single hydroxylation and conjugation with glucuronic acid. CYP2C9 is involved in the metabolism of the drug. Pharmacological activity of metabolites is lower than diclofenac. Systemic clearance is 350 ml / min, Vd - 550 ml / kg. T1 / 2 from plasma -2hours. 65% of the administered dose is excreted in the form of metabolites by the kidneys, less than 1% is excreted unchanged, the rest of the dose is excreted in the form of metabolites with bile. In patients with severe renal insufficiency (creatinine clearance less than 10 ml / min), excretion of bile metabolites is increased, and there is no increase in their concentration in the blood. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac do not change. Diclofenac penetrates into breast milk.
Inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondyloarthritis, acute gouty arthritis), inflammatory processes in the pelvis, adnexitis, primary algomenorrhea,renal or biliary colic, proctitis, degenerative diseases of the musculoskeletal system (deforming osteoarthrosis, osteochondrosis), pain syndrome (lumbago, sciatica, neuralgia, myalgia, tendovaginitis, bursitis, rheumatic soft tissue damage, toothache and headache, migraine and pain, maternal mortality of another genesis), post-traumatic pain syndrome, accompanied by inflammation, postoperative pain, as part of complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome ( aringitis, tonsillitis, otitis media), febrile syndrome.
Dosage and administration
Introduced deeply intramuscularly. Single dose for adults - 75 mg (1 ampoule). If necessary, re-introduction is possible, but not earlier than after 12 hours. Duration of use is not more than 2 days, if necessary, further transferred to oral or rectal use of diclofenac.