What is Diclofenac

Pharmacological Mechanism

Diclofenac can competitively inhibit the cyclooxygenase activity in the arachidonic acid metabolic pathway, thereby reducing the synthesis of prostaglandins (PGE1 and PGE2) in inflammatory tissues. At the same time, it can also competitively inhibit the activity of 5-lipoxygenase in the arachidonic acid metabolism pathway and reduce the production of leukotriene B4 in inflammatory tissues. Therefore, diclofenac can effectively relieve the redness and swelling symptoms of inflammatory tissues and reduce ibone resorption and semilunar valve damage in inflammatory joints.

Figure 1. Diclofenac mechanism of action. (Gan TJ., et al.; 2010)

Its analgesic effect is mainly through inhibiting the synthesis and release of prostaglandins, reducing the sensitivity of the body's pain receptors to inflammatory stimuli and increasing the body's pain threshold.

Pharmacological Effects

Diclofenac is a nonsteroidal compound that exerts its pharmacological effects by inhibiting prostate synthesis. It has anti-rheumatic, anti-inflammatory, analgesic and antipyretic effects. It is characterized by significant relief of clinical signs and symptoms such as a variety of pain, joint swelling, trauma and postoperative inflammation. Topical application of topical latex allows its active ingredients to penetrate the skin, accumulate in subcutaneous tissue, and resist acute and chronic inflammatory reactions.

Take enteric-coated tablets for oral administration and are rapidly and completely absorbed. Taking 50mg, the average peak time is 2h, and the peak concentration is 1.5fμg/ml. There is a linear relationship between blood concentration and dose. The plasma protein binding rate of diclofenac is 99.7%, which is mainly bound to albumin. The plasma half-period is 1 to 2 hours. Diclofenac can enter the synovial fluid, and the highest concentration in the synovial fluid is measured approximately 2 to 4 hours after the peak plasma concentration. The apparent elimination half-period of the drug in synovial fluid is 3 to 6 hours. Only 4 to 6 hours after administration, the concentration of diclofenac in synovial fluid is already higher than its concentration in plasma, and can be maintained for 12 hours. Diclofenac is metabolized in the liver, and approximately 60% of the drug is excreted in the urine as glucuronides and hydroxylates. When latex is applied topically, its active ingredients are absorbed through the skin, with the absorption amount being approximately 6% of the applied dose. It then penetrates through the skin to the area of inflammation.

Ecological Hazard

Diclofenac, an anti-inflammatory drug commonly used in livestock farming, once caused a natural disaster in the ecosystem. Researchers found that diclofenac, an anti-inflammatory drug widely used in livestock, was responsible for killing three species of vultures in the Indian subcontinent. The study found that the vultures died of kidney failure and gout. Through specific research, it was found that the reason was because vultures pecked at the carcasses of livestock contaminated with diclofenac, and every time a vulture ate meat containing diclofenac, there was a 1% chance of death. The decline of vultures has led to an increase in the number of wild dogs, and the increasing number of wild dogs has also increased the risk of rabies in humans. Not only that, the growth of wild dog groups in villages, towns and the wild has caused leopards living in deep forests to turn to hunting wild dogs, increasing the chance of leopards injuring people. At the same time, because wild dogs are not as efficient at decomposing carcasses as vultures (their strong acidity inhibits the growth of bacteria), this further aggravates the deterioration of the natural environment.