QuickView for Prednisolone (compound)

Summary
General Info

PubChem

PubChem Compound 11245343

Name:	Prednisolone
PubChem Compound ID:	11245343
Description:	A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.
Molecular formula:	C₂₁H₂₈O₅
Molecular weight:	360.444 g/mol

DrugBank

Identification

Name:	Prednisolone
Name (isomeric):	DB00860
Drug Type:	small molecule
Description:	A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.
Synonyms:	Predisolone Sodium Phosphate; Prednisolone Acetate; Prednisolonum [INN-Latin]; Methylprednisolone Acetate; Prednisolone Tebutate; Deltahydrocortisone; Prednisolona [INN-Spanish]; Prednisolone Sodium Phosphate; PRDL
Brand:	Klismacort, Ultracortene H, Decortin H, Prednis, Ulacort, Nor-Pred T.B.A., Fernisolone, Delta-Cortef, Hydroretrocortine, Ocu-Pred Forte, Inflamase Mild, Key-Pred, Metacortandralone, Ak-Pred, Paracotol, Hydroretrocortin, I-Pred, Cotogesic, Pred Mild, Codelcortone, Donisolone, Delcortol, Delta F, Inflamase Forte, Econopred Plus, Di-Adreson F, Predalone 50, Predair, Erbacort, Orapred, Supercortisol, Hostacortin H, Predcor-25, Medrol Acetate, Hydeltra, Predonine, Ultra Pred, Prednelan, Fernisolone P, Precortancyl, Ultracortene-Hydrogen, Predonin, Ak-Tate, Decaprednil, Medrol, Cotolone, Nisolone, Hydrodeltalone, Hydeltra-Tba, Deltacortril, Flamasone, Depo-Medrol, Delta-Stab, Precortisyl, Predcor-Tba, Dydeltrone, Alphadrol, Ultracorten H, Dicortol, Predni-Dome, Dexa-Cortidelt Hostacortin H, Cortalone, Deltasolone, Meticortelone, Lentosone, Steran, Deltacortril Enteric, Precortalon, Solone, Predate Tba, Derpo Pd, Paracortol, Hydeltrone, Predniliderm, Ultracortene-H, Prenolone, Lite Pred, Deltisilone, Ophtho-Tate, Panafcortelone, Sterane, Articulose-50, Meti-Derm, Prelone, Rolisone, Predne-Dome, Eazolin D, M-Predrol, Predalone T.B.A., Hydrodeltisone, Scherisolon, Sterolone, Cordrol, Precortilon, Prednicen, Erbasona, Metreton, Ocu-Pred, Predcor-50, Econopred, Hydeltrasol, Predniretard, Estilsona, Co-Hydeltra, Pediapred, Deltacortenol, Pred Forte, Fernisolone-P, Predair A, Predair Forte, Predate-50
Brand name mixture:	Ak Cide Oph Soln(Prednisolone Acetate + Sulfacetamide Sodium), Blephamide Oph Ont(Prednisolone Acetate + Sulfacetamide Sodium), Blephamide Opht Suspension(Prednisolone Acetate + Sulfacetamide Sodium), Surolan Drops(Miconazole Nitrate + Polymyxin B Sulfate + Prednisolone Acetate), Dioptimyd Ointment(Prednisolone Acetate + Sulfacetamide Sodium), O... show more » Ak Cide Oph Soln(Prednisolone Acetate + Sulfacetamide Sodium), Blephamide Oph Ont(Prednisolone Acetate + Sulfacetamide Sodium), Blephamide Opht Suspension(Prednisolone Acetate + Sulfacetamide Sodium), Surolan Drops(Miconazole Nitrate + Polymyxin B Sulfate + Prednisolone Acetate), Dioptimyd Ointment(Prednisolone Acetate + Sulfacetamide Sodium), Optisone(Neomycin + Prednisolone), Liquichlor(Chloramphenicol + Prednisolone + Squalane + Tetracaine), Metimyd Oph Sus(Prednisolone Acetate + Sulfacetamide Sodium), Chlorasone(Chloramphenicol + Prednisolone Acetate), Dioptimyd Suspension(Prednisolone Acetate + Sulfacetamide Sodium), Prednisize Solution(Camphor + Chlorophenol + Cresyl Acetate + Prednisolone), Canaural(Diethanolamine Fusidate + Framycetin Sulfate + Nystatin + Prednisolone), Pred C Tab(Aluminum Hydroxide + Prednisolone + Salicylamide + Vitamin C), Vanectyl-P Tablets(Prednisolone + Trimeprazine Tartrate), Vasocidin Ophthalmic Solution(Prednisolone Sodium Phosphate + Sulfacetamide Sodium), Quiex-Pred Sus(Aminophylline + Guaifenesin + Prednisolone), Delta-Albaplex Tablets(Novobiocin (Novobiocin Sodium) + Prednisolone + Tetracycline Hydrochloride) show less «
Category:	Antineoplastic Agents, Hormonal, Adrenergic Agents, Antineoplastic Agents, Glucocorticoids, Anti-inflammatory Agents
CAS number:	50-24-8

Pharmacology

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 mar... show more » 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. show less «
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 pot... show more » 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. show less «
Absorption:	Readily absorbed by gastrointestinal tract, peak plasma concentration is reached 1-2 hours after administration.
Protein binding:	Very high (>90%)
Biotransformation:	Excreted in the urine as either free or glucoconjugate.
Half Life:	2-3 hours
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.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take with food to reduce gastric irritation.

Avoid alcohol. Avoid caffeine.

Drug interaction:

Dihydroquinidine barbiturate	The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, prednisolone.
Estradiol	The estrogenic agent, estradiol, may increase the effect of the corticosteroid, prednisolone.
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.
Hexobarbital	The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, prednisolone.
Salsalate	The corticosteroid, prednisolone, may decrease the effect of the salicylate, salsalate.

Dihydroquinidine barbiturate	The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, prednisolone.
Estradiol	The estrogenic agent, estradiol, may increase the effect of the corticosteroid, prednisolone.
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.
Hexobarbital	The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, prednisolone.
Salsalate	The corticosteroid, prednisolone, may decrease the effect of the salicylate, salsalate.
Bismuth Subsalicylate	The corticosteroid, prednisolone, may decrease the effect of the salicylate, bismuth subsalicylate.
Butalbital	The barbiturate, butalbital, may decrease the effect of the corticosteroid, prednisolone.
Heptabarbital	The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, prednisolone.
Ketoconazole	The imidazole, ketoconazole, may increase the effect and toxicity of the corticosteroid, prednisolone.
Quinidine barbiturate	The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, prednisolone.
Aprobarbital	The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, prednisolone.
Acenocoumarol	The corticosteroid, prednisolone, alters the anticoagulant effect, acenocoumarol.
Itraconazole	The imidazole, itraconazole, may increase the effect and toxicity of the corticosteroid, prednisolone.
Rifampin	The enzyme inducer, rifampin, 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.
Secobarbital	The barbiturate, secobarbital, may decrease the effect of the corticosteroid, prednisolone.
Acetylsalicylic acid	The corticosteroid, prednisolone, may decrease the effect of the salicylate, acetylsalicylic acid.
Diethylstilbestrol	The estrogenic agent, diethylstilbestrol, may increase the effect of the corticosteroid, prednisolone.
Amobarbital	The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisolone.
Magnesium salicylate	The corticosteroid, prednisolone, may decrease the effect of magnesium salicylate.
Midodrine	Increased arterial pressure
Ambenonium	The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, ambenonium.
Estriol	The estrogenic agent, estriol, may increase the effect of the corticosteroid, prednisolone.
Mestranol	The estrogenic agent, mestranol, may increase the effect of the corticosteroid, prednisolone.
Dicumarol	The corticosteroid, prednisolone, alters the anticoagulant effect of dicumarol.
Estropipate	The estrogenic agent, estropipate, may increase the effect of the corticosteroid, prednisolone.
Estrone	The estrogenic agent, estrone, may increase the effect of the corticosteroid, prednisolone.
Butabarbital	The barbiturate, butabarbital, may decrease the effect of the corticosteroid, prednisolone.
Clomifene	The estrogenic agent, clomifene, may increase the effect of the corticosteroid, prednisolone.
Warfarin	The corticosteroid, prednisolone, alters the anticoagulant effect of warfarin.
Methohexital	The barbiturate, methohexital, may decrease the effect of the corticosteroid, prednisolone.
Anisindione	The corticosteroid, prednisolone, alters the anticoagulant effect of anisindione.
Chlorotrianisene	The estrogenic agent, chlorotrianisene, may increase the effect of the corticosteroid, prednisolone.
Phenobarbital	The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, prednisolone.
Fosphenytoin	The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, prednisolone.
Conjugated Estrogens	The estrogenic agent may increase 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.
Mephenytoin	The enzyme inducer, mephenytoin, 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.
Methylphenobarbital	The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, prednisolone.
Quinestrol	The estrogenic agent, quinestrol, may increase the effect of the corticosteroid, prednisolone.
Butethal	The barbiturate, butethal, may decrease the effect of the corticosteroid, prednisolone.
Ethinyl Estradiol	The estrogenic agent, ethinyl estradiol, may increase the effect of the corticosteroid, prednisolone.
Talbutal	The barbiturate, talbutal, may decrease the effect of the corticosteroid, prednisolone.
Edrophonium	The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, edrophonium.
Phenytoin	The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, prednisolone.
Neostigmine	The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, neostigmine.
Ethotoin	The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, prednisolone.
Pentobarbital	The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, prednisolone.
Salicylate-sodium	The corticosteroid, prednisolone, may decrease the effect of the salicylate, salicylate-sodium.

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Targets

Glucocorticoid receptor

Enzymes

Cytochrome P450 3A4

Cytochrome P450 2A6

Transporters

Solute carrier organic anion transporter family member 1A2

Multidrug resistance protein 1

Carriers

Corticosteroid-binding globulin