indication

For the treatment of primary or secondary adrenocortical insufficiency, such as congenital adrenal hyperplasia, thyroiditis. Also used to treat psoriatic arthritis, rheumatoid arthritis, ankylosing spondylitis, bursitis, acute gouty arthritis and epicondylitis. Also indicated for treatment of systemic lupus erythematosus, pemphigus and acute rhematic carditis. Can be used in the treatment of leukemias, lymphomas, thrombocytopenia purpura and autoimmune hemolytic anemia. Can be used to treat celiac disease, insulin resistance, ulcerative colitis and liver disorders.

pharmacology

Prednisolone is a synthetic glucocorticoid used as antiinflammatory or immunosuppressive agent. Prednisolone is indicated in the treatment of various conditions, including congenital adrenal hyperplasia, psoriatic arthritis, systemic lupus erythematosus, bullous dermatitis herpetiformis, seasonal or perennial allergic rhinitis, allergic corneal marginal ulcers, symptomatic sarcoidosis, idiopathic thrombocytopenic purpura in adults, leukemias and lymphomas in adults, and ulcerative colitis. Glucocorticoids are adrenocortical steroids and cause profound and varied metabolic effects. In addition, they modify the body's immune responses to diverse stimuli.

mechanism of action

Glucocorticoids such as Prednisolone can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of glucocorticoids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. Prednisolone reduces inflammatory reaction by limiting the capillary dilatation and permeability of the vascular structures. These compounds restrict the accumulation of polymorphonuclear leukocytes and macrophages and reduce the release of vasoactive kinins. Recent research suggests that corticosteroids may inhibit the release of arachidonic acid from phospholipids, thereby reducing the formation of prostaglandins. Prednisolone is a glucocorticoid receptor agonist. On binding, the corticoreceptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing an increase or decrease in expression of specific target genes, including suppression of IL2 (interleukin 2) expression.

toxicity

LD₅₀=500 mg/kg (oral, rat), short-term side effects include high blood glucose levels and fluid retention. Long term side effects include Cushing's syndrome, weight gain, osteoporosis, glaucoma, type II diabetes and adrenal suppression.

biotransformation

Excreted in the urine as either free or glucoconjugate.

absorption

Readily absorbed by gastrointestinal tract, peak plasma concentration is reached 1-2 hours after administration.

half life

2-3 hours

drug interactions

Acenocoumarol: The corticosteroid, prednisolone, alters the anticoagulant effect, acenocoumarol.

Acetylsalicylic acid: The corticosteroid, prednisolone, may decrease the effect of the salicylate, acetylsalicylic acid.

Ambenonium: The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, ambenonium.

Amobarbital: The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisolone.

Anisindione: The corticosteroid, prednisolone, alters the anticoagulant effect of anisindione.

Aprobarbital: The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, prednisolone.

Bismuth Subsalicylate: The corticosteroid, prednisolone, may decrease the effect of the salicylate, bismuth subsalicylate.

Butabarbital: The barbiturate, butabarbital, may decrease the effect of the corticosteroid, prednisolone.

Butalbital: The barbiturate, butalbital, may decrease the effect of the corticosteroid, prednisolone.

Butethal: The barbiturate, butethal, may decrease the effect of the corticosteroid, prednisolone.

Chlorotrianisene: The estrogenic agent, chlorotrianisene, may increase the effect of the corticosteroid, prednisolone.

Clomifene: The estrogenic agent, clomifene, may increase the effect of the corticosteroid, prednisolone.

Conjugated Estrogens: The estrogenic agent may increase the effect of the corticosteroid, prednisolone.

Dicumarol: The corticosteroid, prednisolone, alters the anticoagulant effect of dicumarol.

Diethylstilbestrol: The estrogenic agent, diethylstilbestrol, may increase the effect of the corticosteroid, prednisolone.

Dihydroquinidine barbiturate: The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, prednisolone.

Edrophonium: The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, edrophonium.

Estradiol: The estrogenic agent, estradiol, may increase the effect of the corticosteroid, prednisolone.

Estriol: The estrogenic agent, estriol, may increase the effect of the corticosteroid, prednisolone.

Estrone: The estrogenic agent, estrone, may increase the effect of the corticosteroid, prednisolone.

Estropipate: The estrogenic agent, estropipate, may increase the effect of the corticosteroid, prednisolone.

Ethinyl Estradiol: The estrogenic agent, ethinyl estradiol, may increase the effect of the corticosteroid, prednisolone.

Ethotoin: The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, prednisolone.

Fosphenytoin: The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, prednisolone.

Heptabarbital: The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, prednisolone.

Hexobarbital: The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, prednisolone.

Itraconazole: The imidazole, itraconazole, may increase the effect and toxicity of the corticosteroid, prednisolone.

Ketoconazole: The imidazole, ketoconazole, may increase the effect and toxicity of the corticosteroid, prednisolone.

Magnesium salicylate: The corticosteroid, prednisolone, may decrease the effect of magnesium salicylate.

Mephenytoin: The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, prednisolone.

Mestranol: The estrogenic agent, mestranol, may increase the effect of the corticosteroid, prednisolone.

Methohexital: The barbiturate, methohexital, may decrease the effect of the corticosteroid, prednisolone.

Methylphenobarbital: The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, prednisolone.

Midodrine: Increased arterial pressure

Neostigmine: The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, neostigmine.

Pentobarbital: The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisolone.

Phenobarbital: The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, prednisolone.

Phenytoin: The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, prednisolone.

Primidone: The barbiturate, primidone, may decrease the effect of the corticosteroid, prednisolone.

Pyridostigmine: The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, pyridostigmine.

Quinestrol: The estrogenic agent, quinestrol, may increase the effect of the corticosteroid, prednisolone.

Quinidine barbiturate: The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, prednisolone.

Rifampin: The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, prednisolone.

Salicylate-sodium: The corticosteroid, prednisolone, may decrease the effect of the salicylate, salicylate-sodium.

Salsalate: The corticosteroid, prednisolone, may decrease the effect of the salicylate, salsalate.

Secobarbital: The barbiturate, secobarbital, may decrease the effect of the corticosteroid, prednisolone.

Tacrine: Tacrine and Prednisolone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.

Talbutal: The barbiturate, talbutal, may decrease the effect of the corticosteroid, prednisolone.

Trastuzumab: Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.

Trisalicylate-choline: The corticosteroid, prednisolone, may decrease the effect of the salicylate, trisalicylate-choline.

Vecuronium: Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Prednisolone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.

Warfarin: The corticosteroid, prednisolone, alters the anticoagulant effect of warfarin.