Glucocorticoid drugs D 2. ADME and properties of commonly used rugs Binding to corticosteroid- binding globulin(cBG,皮质激 素运载蛋白) in the plasma o Cortisone and prednisone are reduced and transformed to hydrocortisone and prednisolone (active forms) in the liver D Metabolism will be increased by hepatic enzyme inductors (phenobarbital, phenytoin, rifampin, etc
2. ADME and properties of commonly used drugs Binding to corticosteroid-binding globulin (CBG, 皮质激 素运载蛋白) in the plasma Cortisone and prednisone are reduced and transformed to hydrocortisone and prednisolone (active forms) in the liver Metabolism will be increased by hepatic enzyme inductors (phenobarbital, phenytoin, rifampine, etc.) Glucocorticoid drugs
Glucocorticoid drugs Commonly used drugs a Short-acting: hydrocortisone( cortisol)氢化可的松 cortisone可的松 a Intermediate-acting: prednisone泼尼松强的松 prednisolone泼尼松龙强的松龙 o Long-acting: dexamethasone地塞米松 Topical: fluocinolone氟轻松
Commonly used drugs Short-acting: hydrocortisone (cortisol) 氢化可的松 cortisone 可的松 Intermediate-acting: prednisone 泼尼松, 强的松 prednisolone 泼尼松龙, 强的松龙 Long-acting: dexamethasone 地塞米松 Topical: fluocinolone 氟轻松 Glucocorticoid drugs
表35-1常用糖皮质激素类药物的比较 药理活性 药物 等效剂量半衰期作用持续 水盐代谢糖代谢抗炎作用 (mg) (min 间(h (比值) (比值) 比值) 短效 氢化可的松 1.0 1.0 20.00 可的松 0.8 0. 0.8 25.00 中效 泼尼松 0.8 4.0 3.5 5.00 60 泼尼松龙 0.8 4.0 4.0 5.00 200 12-36 甲泼尼龙 0.5 5.0 5.0 4.00 180 12-36 曲安西龙 5.0 5.0 4.00 >200 长效 地塞米松 0 20~30300.75100~300 倍他米松 20~30 25~35 0.60 100~300 36
Glucocorticoid drugs 0 3 Clinical uses o(iMmune diseases autoimmune disorders自身免疫性疾病: rheumatic fever, rheumatic carditis, rheumatic arthritis, osteoarthritis, systemic lupus erythematosus, polyarteritis nodosa, nephritic syndrome, etc b) rejection of organ transplantation器官移植排斥反应 c) allergic diseases过敏性疾病: urticaria, serum sickness, contact dermatitis, drug allergic reactions, chronic severe asthma, status asthmaticus, angioneurotic edema, etc
3. Clinical uses (1) Immune diseases a)autoimmune disorders 自身免疫性疾病: rheumatic fever, rheumatic carditis, rheumatic arthritis, osteoarthritis, systemic lupus erythematosus, polyarteritis nodosa, nephritic syndrome, etc. b) rejection of organ transplantation 器官移植排斥反应 c) allergic diseases 过敏性疾病: urticaria, serum sickness, contact dermatitis, drug allergic reactions, chronic severe asthma, status asthmaticus, angioneurotic edema, etc. Glucocorticoid drugs
Glucocorticoid drugs o(2)Severe infection and inflammation o a acute severe infections: merely suppressing inflammatory manifestations 0 Causion: combination with effective antimicrobial drugs o Usually not used in viral infections except for those with cerebral edema or severe systemic symptoms o b prevention of sequelae of some types of inflammation, such as in brain, heart, eye, joint, etc
(2) Severe infection and inflammation a) acute severe infections: merely suppressing inflammatory manifestations Causion: combination with effective antimicrobial drugs ! Usually not used in viral infections except for those with cerebral edema or severe systemic symptoms b) prevention of sequelae of some types of inflammation, such as in brain, heart, eye, joint, etc. Glucocorticoid drugs