Nisolone: Full Drug Profile

Nisolone - General Information

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]

Pharmacology of Nisolone

Nisolone is a synthetic glucocorticoid used as antiinflammatory or immunosuppressive agent. Nisolone 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.

Nisolone for patients

Patients who are on immunosuppressant doses of corticosteroids should be warned to avoid exposure to chickenpox or measles. Patients should also be advised that if they are exposed, medical advice should be sought without delay.

Nisolone Interactions

Nisolone Contraindications

Systemic fungal infections.

Additional information about Nisolone

Nisolone 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.

Mechanism Of Action

Glucocorticoids such as Nisolone 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. Nisolone 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. Nisolone 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.

Drug Interactions

Ambenonium The corticosteroid decreases the effect of anticholinesterases

Generic Name

Prednisolone

Synonyms

PRDL; Deltahydrocortisone; Methylprednisolone Acetate; Predisolone Sodium Phosphate; Prednisolona [Inn-Spanish]; Prednisolone Acetate; Prednisolone Sodium Phosphate; Prednisolone Tebutate; Prednisolonum [Inn-Latin]

Drug Category

Antineoplastic Agents; Glucocorticoids; Anti-inflammatory Agents; Adrenergic Agents

Drug Type

Small Molecule; Approved

Other Brand Names containing Prednisolone

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;

Absorption

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

Toxicity (Overdose)

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.

Protein Binding

Very high (>90%)

Biotransformation

Excreted in the urine as either free or glucoconjugate.

Half Life

2-3 hours

Dosage Forms of Nisolone

Liquid Oral

Chemical IUPAC Name

(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one

Chemical Formula

C21H28O5

Prednisolone on Wikipedia

https://en.wikipedia.org/wiki/Prednisolone

Organisms Affected

Humans and other mammals