Drug/Small Molecule:
prednisolone

2D structure

Overview

Generic Names: Deltahydrocortisone; Methylprednisolone Acetate; PRDL; Predisolone Sodium Phosphate; Prednisolona [INN-Spanish]; Prednisolone Acetate; Prednisolone Sodium Phosphate; Prednisolone Tebutate; Prednisolonum [INN-Latin]
Trade Names: Ak-Pred; Ak-Tate; Alphadrol; Articulose-50; Co-Hydeltra; Codelcortone; Cordrol; Cortalone; Cotogesic; Cotolone; Decaprednil; Decortin H; Delcortol; Delta F; Delta-Cortef; Delta-Stab; Deltacortenol; Deltacortril; Deltacortril Enteric; Deltasolone; Deltisilone; Depo-Medrol; Derpo Pd; Dexa-Cortidelt Hostacortin H; Di-Adreson F; Dicortol; Donisolone; Dydeltrone; Eazolin D; Econopred; Econopred Plus; Erbacort; Erbasona; Estilsona; Fernisolone; Fernisolone P; Fernisolone-P; Flamasone; Hostacortin H; Hydeltra; Hydeltra-Tba; Hydeltrasol; Hydeltrone; Hydrodeltalone; Hydrodeltisone; Hydroretrocortin; Hydroretrocortine; I-Pred; Inflamase Forte; Inflamase Mild; Key-Pred; Klismacort; Lentosone; Lite Pred; M-Predrol; Medrol; Medrol Acetate; Metacortandralone; Meti-Derm; Meticortelone; Metreton; Nisolone; Nor-Pred T.B.A.; Ocu-Pred; Ocu-Pred Forte; Ophtho-Tate; Orapred; Panafcortelone; Paracortol; Paracotol; Pediapred; Precortalon; Precortancyl; Precortilon; Precortisyl; Pred Forte; Pred Mild; Predair; Predair A; Predair Forte; Predalone 50; Predalone T.B.A.; Predate Tba; Predate-50; Predcor-25; Predcor-50; Predcor-Tba; Predne-Dome; Prednelan; Predni-Dome; Prednicen; Predniliderm; Predniretard; Prednis; Predonin; Predonine; Prelone; Prenolone; Rolisone; Scherisolon; Solone; Steran; Sterane; Sterolone; Supercortisol; Ulacort; Ultra Pred; Ultracorten H; Ultracortene H; Ultracortene-H; Ultracortene-Hydrogen
Brand Mixtures: Ak Cide Oph Soln (Prednisolone Acetate + Sulfacetamide Sodium); Blephamide Oph Ont (Prednisolone Acetate + Sulfacetamide Sodium); Blephamide Opht Suspension (Prednisolone Acetate + Sulfacetamide Sodium); Canaural (Diethanolamine Fusidate + Framycetin Sulfate + Nystatin + Prednisolone); Chlorasone (Chloramphenicol + Prednisolone Acetate); Delta-Albaplex Tablets (Novobiocin (Novobiocin Sodium) + Prednisolone + Tetracycline Hydrochloride); Dioptimyd Ointment (Prednisolone Acetate + Sulfacetamide Sodium); Dioptimyd Suspension (Prednisolone Acetate + Sulfacetamide Sodium); Liquichlor (Chloramphenicol + Prednisolone + Squalane + Tetracaine); Metimyd Oph Sus (Prednisolone Acetate + Sulfacetamide Sodium); Optisone (Neomycin + Prednisolone); Pred C Tab (Aluminum Hydroxide + Prednisolone + Salicylamide + Vitamin C); Prednisize Solution (Camphor + Chlorophenol + Cresyl Acetate + Prednisolone); Quiex-Pred Sus (Aminophylline + Guaifenesin + Prednisolone); Surolan Drops (Miconazole Nitrate + Polymyxin B Sulfate + Prednisolone Acetate); Vanectyl-P Tablets (Prednisolone + Trimeprazine Tartrate); Vasocidin Ophthalmic Solution (Prednisolone Sodium Phosphate + Sulfacetamide Sodium)
PharmGKB Accession Id: PA451096

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. PubChem (source: Drug Bank)

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. (source: Drug Bank)

ATC Therapeutic Categories

  • A07EA:Corticosteroids acting locally
  • C05AA:Corticosteroids
  • D07AA:Corticosteroids, weak (group I)
  • D07AC:Corticosteroids, potent (group III)
  • D07XA:Corticosteroids, weak, other combinations
  • D10AA:Corticosteroids, combinations for treatment of acne
  • H02AB:Glucocorticoids
  • R01AD:Corticosteroids
  • S01BA:Corticosteroids, plain
  • S01CB:Corticosteroids/antiinfectives/mydriatics in combination
  • S02BA:Corticosteroids
  • S03BA:Corticosteroids

Pharmacology, Interactions, and Contraindications

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. (source: Drug Bank)

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. (source: Drug Bank)

Food Interactions

Avoid alcohol. Avoid caffeine.
Take with food to reduce gastric irritation. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Excreted in the urine as either free or glucoconjugate. (source: Drug Bank)

Protein Binding

Very high (>90%) (source: Drug Bank)

Absorption

Readily absorbed by gastrointestinal tract, peak plasma concentration is reached 1-2 hours after administration. (source: Drug Bank)

Toxicity

LD<sub>50</sub>=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. (source: Drug Bank)

Isomeric SMILES Code:

C[C@]12C[C@@H]([C@H]3[C@H]([C@@H]1CC[C@@]2(C(=O)CO)O)CCC4=CC(=O)C=C[C@]34C)O (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
CCL2
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  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
CEBPD
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  • PD
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No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A1
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  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
DUSP1
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
FKBP5
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
HLA-DRB1
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
HLA-DRB4
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  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
INSR
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
IRS2
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  • PD
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Publications
Phenotype data available No genotype data Literature annotations available Not annotated
ISG20
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
KLF9
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
LIMK2
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
MAP2K1
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  • PD
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Phenotype data available No genotype data Literature annotations available Not annotated
MCL1
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  • PD
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
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  • PK
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  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SDC2
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
SIK1
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  • PD
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Phenotype data available No genotype data Literature annotations available Not annotated
STAT1
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  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
TXNIP
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  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
ZBTB16
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  • PD
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No phenotype data No genotype data Literature annotations available Not annotated
ZFP36L2
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  • PD
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
SERPINA6 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
acenocoumarol Uncurated Annotation The corticosteroid alters the anticoagulant effect (source: Drug Bank)
amobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
aspirin Uncurated Annotation The corticosteroid decreases the effect of salicylates (source: Drug Bank)
butalbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
clomifene Uncurated Annotation The estrogenic agent increases the effect of the corticosteroid (source: Drug Bank)
dicumarol Uncurated Annotation The corticosteroid alters the anticoagulant effect (source: Drug Bank)
diethylstilbestrol Uncurated Annotation The estrogenic agent increases the effect of the corticosteroid (source: Drug Bank)
edrophonium Uncurated Annotation The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
estradiol Uncurated Annotation The estrogenic agent increases the effect of the corticosteroid (source: Drug Bank)
estrone Uncurated Annotation The estrogenic agent increases the effect of the corticosteroid (source: Drug Bank)
ethinyl estradiol Uncurated Annotation The estrogenic agent increases the effect of the corticosteroid (source: Drug Bank)
hexobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
itraconazole Uncurated Annotation The imidazole increases the effect and toxicity of the corticosteroid (source: Drug Bank)
ketoconazole Uncurated Annotation The imidazole increases the effect and toxicity of the corticosteroid (source: Drug Bank)
mephenytoin Uncurated Annotation The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank)
mestranol Uncurated Annotation The estrogenic agent increases the effect of the corticosteroid (source: Drug Bank)
methylphenobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
neostigmine Uncurated Annotation The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
pentobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
phenobarbital Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
phenytoin Uncurated Annotation The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank)
primidone Uncurated Annotation The barbiturate decreases the effect of the corticosteroid (source: Drug Bank)
pyridostigmine Uncurated Annotation The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
rifampin Uncurated Annotation The enzyme inducer decreases the effect of the corticosteroid (source: Drug Bank)
salicylate-magnesium Uncurated Annotation The corticosteroid decreases the effect of salicylates (source: Drug Bank)
salicylate-sodium Uncurated Annotation The corticosteroid decreases the effect of salicylates (source: Drug Bank)
warfarin Uncurated Annotation The corticosteroid alters the anticoagulant effect (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Glaucoma
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  • PD
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
HIV Infections
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
Inflammation
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  • PD
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Precursor Cell Lymphoblastic Leukemia-Lymphoma
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  • PD
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Publications
No phenotype data No genotype data Literature annotations available Not annotated
Purpura, Thrombotic Thrombocytopenic
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  • PD
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Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. A subtype of childhood acute lymphoblastic leukaemia with poor treatment outcome: a genome-wide classification study
  2. Physicochemical determinants of human renal clearance
  3. SMARCB1 and PARP1 expression in CEPH cell lines
  4. SWI/SNF chromatin-remodeling complex and glucocorticoid resistance in acute lymphoblastic leukemia
  5. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00860
KEGG Compound ID:
C07369
KEGG Drug ID:
D00472
PubChem Compound ID:
5755
PubChem Substance ID:
148534

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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