Acetate Prednisolone Prednisolone-21-acetate

Details:

Prednisolone Acetate

Prednisolone is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions. It is the active metabolite of the drugprednisone is used especially in patients with hepatic failure, as these individuals are unable to metabolise prednisone into prednisolone.

Uses

Prednisolone is a corticosteroid drug with predominant glucocorticoid low mineralocorticoidactivity, making it useful fthe treatment of a wide range of inflammatory auto-immuneconditions such as asthma,uveitis, pyoderma gangrenosum, rheumatoid arthritis, ulcerative colitis, pericarditis, temporal arteritis and Crohn's disease, Bell's palsy, multiple sclerosis,cluster headaches, vasculitis, acute lymphoblastic leukemia and autoimmune hepatitis,systemic lupus erythematosus, Kawasaki diseaseand dermatomyositis. It is also used ftreatment of sarcoidosis, though the mechanism is unknown.

Prednisolone acetate ophthalmic suspension (eye drops) is an adrenocortical steroid product, prepared as a sterile ophthalmic suspension used to reduce swelling, redness, itching, allergic reactions affecting the eye.

Prednisolone can also be used as an immunosuppressive drug for organ transplants in cases of adrenal insufficiency (Addison's disease).

Corticosteroids inhibit the inflammatory response to a variety of inciting agents, it is presumed, delay slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, scar formation with inflammation.

Mechanism of action

Prednisolone irreversibly binds with glucocorticoid receptors (GR) alpha beta fwhich they have a high affinity. AlphaGR BetaGR are found in virtually all tissues with variable numbers between 3000 10000 per cell, depending on the tissue involved. Prednisolone can activate influence biochemical behaviour of most cells. The steroid/receptcomplexes dimerise interact with cellular DNA in the nucleus, binding to steroid-response elements modifying gene transcription. They induce synthesis of some proteins, inhibit synthesis of others.

Not all metabolic actions on genes are known. Most mediatproteins are enzymes, e.g., cAMP-dependent kinase

Anti-inflammatory immunosuppressive actions:

• Inhibition of gene transcription for COX-2, cytokines, cell adhesion molecules, inducible NO synthase
• Blockage of Vit D3-mediated induction of osteocalcin gene in osteoblasts
• Modification of collegenase gene transcription
• Increase synthesis annexin-1, important in negative feedback on hypothalamus and anteripituitary gland

Regulation of gene suppression leads to systemic suppression of inflammation immune response. This is of clinical usefulness but ultimately leads to gluconeogenesis, proteolysis lipolysis. Gene transcription returns to normal after cessation, but sudden stoppage can cause Addison's disease. Osteoporosis is permanent.