Prednisolone¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ 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.
Pharmacology
Prednisolone¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
Protein Binding
Prednisolone¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Very high (>90%)
Half-life
Prednisolone¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2-3 hours
Absorption
Prednisolone¿¡ ´ëÇÑ Absorption Á¤º¸ Readily absorbed by gastrointestinal tract, peak plasma concentration is reached 1-2 hours after administration.
Prednisolone¿¡ ´ëÇÑ Biotransformation Á¤º¸ Excreted in the urine as either free or glucoconjugate.
Toxicity
Prednisolone¿¡ ´ëÇÑ Toxicity Á¤º¸ 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.
Drug Interactions
Prednisolone¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Ambenonium The corticosteroid decreases the effect of anticholinesterasesEdrophonium The corticosteroid decreases the effect of anticholinesterasesNeostigmine The corticosteroid decreases the effect of anticholinesterasesPyridostigmine The corticosteroid decreases the effect of anticholinesterasesWarfarin The corticosteroid alters the anticoagulant effectAcenocoumarol The corticosteroid alters the anticoagulant effectDicumarol The corticosteroid alters the anticoagulant effectAnisindione The corticosteroid alters the anticoagulant effectMidodrine Increased arterial pressureAspirin The corticosteroid decreases the effect of salicylatesBismuth Subsalicylate The corticosteroid decreases the effect of salicylatesSalicylate-magnesium The corticosteroid decreases the effect of salicylatesSalicylate-sodium The corticosteroid decreases the effect of salicylatesSalsalate The corticosteroid decreases the effect of salicylatesTrisalicylate-choline The corticosteroid decreases the effect of salicylatesTalbutal The barbiturate decreases the effect of the corticosteroidSecobarbital The barbiturate decreases the effect of the corticosteroidQuinidine barbiturate The barbiturate decreases the effect of the corticosteroidPrimidone The barbiturate decreases the effect of the corticosteroidPhenobarbital The barbiturate decreases the effect of the corticosteroidPentobarbital The barbiturate decreases the effect of the corticosteroidMethylphenobarbital The barbiturate decreases the effect of the corticosteroidMethohexital The barbiturate decreases the effect of the corticosteroidHexobarbital The barbiturate decreases the effect of the corticosteroidHeptabarbital The barbiturate decreases the effect of the corticosteroidDihydroquinidine barbiturate The barbiturate decreases the effect of the corticosteroidButethal The barbiturate decreases the effect of the corticosteroidButalbital The barbiturate decreases the effect of the corticosteroidButabarbital The barbiturate decreases the effect of the corticosteroidAprobarbital The barbiturate decreases the effect of the corticosteroidAmobarbital The barbiturate decreases the effect of the corticosteroidChlorotrianisene The estrogenic agent increases the effect of the corticosteroidClomifene The estrogenic agent increases the effect of the corticosteroidDiethylstilbestrol The estrogenic agent increases the effect of the corticosteroidEstradiol The estrogenic agent increases the effect of the corticosteroidEstriol The estrogenic agent increases the effect of the corticosteroidConjugated Estrogens The estrogenic agent increases the effect of the corticosteroidEstrone The estrogenic agent increases the effect of the corticosteroidEstropipate The estrogenic agent increases the effect of the corticosteroidEthinyl Estradiol The estrogenic agent increases the effect of the corticosteroidMestranol The estrogenic agent increases the effect of the corticosteroidQuinestrol The estrogenic agent increases the effect of the corticosteroidEthotoin The enzyme inducer decreases the effect of the corticosteroidFosphenytoin The enzyme inducer decreases the effect of the corticosteroidMephenytoin The enzyme inducer decreases the effect of the corticosteroidPhenytoin The enzyme inducer decreases the effect of the corticosteroidRifampin The enzyme inducer decreases the effect of the corticosteroidItraconazole The imidazole increases the effect and toxicity of the corticosteroidKetoconazole The imidazole increases the effect and toxicity of the corticosteroid
Prednisolone¿¡ ´ëÇÑ Description Á¤º¸ 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]