Estilsona
Estilsona - 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 Estilsona
Estilsona is a synthetic glucocorticoid used as antiinflammatory or immunosuppressive agent. Estilsona 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.
Estilsona 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.
Estilsona Interactions
Estilsona Contraindications
Systemic fungal infections.
Additional information about Estilsona
Estilsona 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 Estilsona 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. Estilsona 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. Estilsona 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
Edrophonium The corticosteroid decreases the effect of anticholinesterases
Neostigmine The corticosteroid decreases the effect of anticholinesterases
Pyridostigmine The corticosteroid decreases the effect of anticholinesterases
Warfarin The corticosteroid alters the anticoagulant effect
Acenocoumarol The corticosteroid alters the anticoagulant effect
Dicumarol The corticosteroid alters the anticoagulant effect
Anisindione The corticosteroid alters the anticoagulant effect
Midodrine Increased arterial pressure
Aspirin The corticosteroid decreases the effect of salicylates
Bismuth Subsalicylate The corticosteroid decreases the effect of salicylates
Salicylate-magnesium The corticosteroid decreases the effect of salicylates
Salicylate-sodium The corticosteroid decreases the effect of salicylates
Salsalate The corticosteroid decreases the effect of salicylates
Trisalicylate-choline The corticosteroid decreases the effect of salicylates
Talbutal The barbiturate decreases the effect of the corticosteroid
Secobarbital The barbiturate decreases the effect of the corticosteroid
Quinidine barbiturate The barbiturate decreases the effect of the corticosteroid
Primidone The barbiturate decreases the effect of the corticosteroid
Phenobarbital The barbiturate decreases the effect of the corticosteroid
Pentobarbital The barbiturate decreases the effect of the corticosteroid
Methylphenobarbital The barbiturate decreases the effect of the corticosteroid
Methohexital The barbiturate decreases the effect of the corticosteroid
Hexobarbital The barbiturate decreases the effect of the corticosteroid
Heptabarbital The barbiturate decreases the effect of the corticosteroid
Dihydroquinidine barbiturate The barbiturate decreases the effect of the corticosteroid
Butethal The barbiturate decreases the effect of the corticosteroid
Butalbital The barbiturate decreases the effect of the corticosteroid
Butabarbital The barbiturate decreases the effect of the corticosteroid
Aprobarbital The barbiturate decreases the effect of the corticosteroid
Amobarbital The barbiturate decreases the effect of the corticosteroid
Chlorotrianisene The estrogenic agent increases the effect of the corticosteroid
Clomifene The estrogenic agent increases the effect of the corticosteroid
Diethylstilbestrol The estrogenic agent increases the effect of the corticosteroid
Estradiol The estrogenic agent increases the effect of the corticosteroid
Estriol The estrogenic agent increases the effect of the corticosteroid
Conjugated Estrogens The estrogenic agent increases the effect of the corticosteroid
Estrone The estrogenic agent increases the effect of the corticosteroid
Estropipate The estrogenic agent increases the effect of the corticosteroid
Ethinyl Estradiol The estrogenic agent increases the effect of the corticosteroid
Mestranol The estrogenic agent increases the effect of the corticosteroid
Quinestrol The estrogenic agent increases the effect of the corticosteroid
Ethotoin The enzyme inducer decreases the effect of the corticosteroid
Fosphenytoin The enzyme inducer decreases the effect of the corticosteroid
Mephenytoin The enzyme inducer decreases the effect of the corticosteroid
Phenytoin The enzyme inducer decreases the effect of the corticosteroid
Rifampin The enzyme inducer decreases the effect of the corticosteroid
Itraconazole The imidazole increases the effect and toxicity of the corticosteroid
Ketoconazole The imidazole increases the effect and toxicity of the corticosteroid
Food Interactions: Not Available
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 Estilsona: Liquid Oral
Solution / drops Ophthalmic
Tablet Oral
Suspension Ophthalmic
Solution 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
