Actions of Fleximat in details
Fleximat is a glucocorticosteroid (GCS). This medication inhibits the function of leukocytes and tissue macrophages. Prednisolone restricts the migration of leukocytes in the area of inflammation. This drug violates the ability of macrophages to phagocytosis and the formation of interleukin-1. Fleximat contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in inflammation. This medicine decreases capillary permeability caused by histamine release. Prednisolone inhibits the activity of fibroblasts and collagen formation.
Fleximat inhibits the activity of phospholipase A2 which leads to suppression of the synthesis of prostaglandins and leukotrienes. This medication inhibits the release of COX (especially COX-2), which also helps reduce the production of prostaglandins.
Fleximat reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils as a result of their displacement from the bloodstream into lymphoid tissue; suppresses the formation of antibodies.
Prednisolone inhibits the release of pituitary ACTH and beta-lipotropina but it does not reduces the level of circulating beta-endorphin. This drug also inhibits the secretion of TSH and FSH.
Fleximat has a vasoconstrictor effect with direct application to the vessels.
Prednisolone has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. It stimulates gluconeogenesis, amino acid contributes to the capture of the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver, prednisolone enhances the deposition of glycogen by stimulating the activity of glikogensintetazy and synthesis of glucose from the products of protein metabolism. This medicine increases blood glucose activates the secretion of insulin.
Prednisolone inhibits glucose uptake by fat cells that leads to the activation of lipolysis. However, due to an increase in insulin secretion is stimulated lipogenesis which contributes to the accumulation of fat.
Fleximat also has catabolic effects in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone prednisolone affects the processes of water and electrolyte metabolism: promotes the excretion of potassium and calcium, delay in the body of sodium and water. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting the long-term therapy with corticosteroids. As a result of the catabolic actions it may suppress growth in children.
In high doses prednisone can increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. This medication stimulates the excessive production of hydrochloric acid and pepsin in the stomach which leads to the development of peptic ulcers.
When systemic use the therapeutic activity of prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.
For external and local application the therapeutic activity of prednisolone is due to anti-inflammatory, antiallergic and antiexudative (due to vasoconstrictor effect) effect.
As compared with hydrocortisone the anti-inflammatory activity of prednisolone is 4 times greater, the mineralocorticoid activity is 0.6 times smaller.
Fleximat pharmacology
Fleximat is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1 and COX-2, enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs, acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme's active site, studies have found that acetaminophen indirectly blocks COX, and that this blockade is ineffective in the presence of peroxides. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. This enzyme is now referred to as COX-3. Its exact mechanism of action is still poorly understood, but future research may provide further insight into how it works.
References
- EPA DSStox. "Etofenamate: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
