各论II 27、肾上腺皮质激素药物(1)
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Medulla:epinephrine norepinepherine
Adrenocorticoid
Glucocorticoids : hydrocortisone, cortisone Mineralocorticoids： aldosterone，desoxycortone Sex hormones
(2) Permissive action Potentiating the effects of catecholamines and glucagon
(3) Anti-inflammatory effects Acute: inhibiting microvascular leakage
leukocyte infiltration Chronic: inhibiting fibroblast proliferation
Drugs affecting endocrine system
Drugs related to adrenocortical hormones Thyroid hormones and antithyroid drugs Insulin and oral hypoglycemic drugs
Cortex:adrenocorticoid Glucocorticoids (Glucocorticosteroids) Mineralocorticoids Sex hormones
regulating related gene transcription biological effects (usually slow)
Action mode of glucocorticoid drugs
CBG: corticosteroid binding globulin
S: glucocorticoid steroids
(central obesity: moon face, buffalo hump)
d) Water and electrolytic: Na+ excretion ↓, K+ excretion ↑,
Ca2+ excretion↑and absorption↓
Glucocorticoid drugs
Fludrocortisone (氟氢可的松)
(地塞米松)
Triamcinolone (曲安西龙)
Non-gene modulation
Gene modulation (GCS, TH)
Mechanisms of glucocorticoid actions
binding to glucocorticoid receptor (GR) nuclear translocation binding to GRE or nGRE
deposition of collagen cicatrization (瘢痕形成)
Glucocorticoid drugs
a) Inhibiting inflammation related proteins or enzymes
Dexamethasone was used GR was labeled with green fluorescent protein
1. Pharmacological effects
Mechanisms of glucocorticoid actions (1) Effects on metabolisms (2) Permissive action (3) Anti-inflammatory effects (4) Effects on immune and allergy (5) Anti-shock (6) Other effects
Structure and Activity Relationship
(2) 9引入氟原子: fludrocortosone (氟氢可的松).
基本结构
(3)引入甲基: 6-methylprednisolone,dexamethasone (6甲泼尼龙, 地塞米松).
(4) 16引入羟基: triamcinolone(曲安西龙).
antipyretic effects effects on blood and blood-forming organs skeletal system CNS effects
Glucocorticoid drugs
(1) Effects on metabolisms a) Carbohydrate: blood glucose ↑: gluconeogenesis ↑, glycolysis↓, glucose utilization↓ b) Protein: synthesis ↓, degradation ↑ c) Lipid: long term use: plasma cholesterol ↑, fat redistribution
GR: glucocorticoid receptor
HSP: heat shock protein
IP: immunophilin
GRE: glucocorticoidresponse element
Nuclear translocation of glucocorticoid receptors (GR)
(1) 1位和2位碳之间改成不饱和的双键:
cortisone prednisone hydrocortisone prednisolone
基本结构
Co百度文库tisone (可的松)
Prednisone (泼尼松)
Hydrocortisone
(氢化可的松, Cortisol)
Prednisolone (泼尼松龙)
黄山药
穿地龙
薯蓣属植物（黄山药、穿地龙） 提取薯蓣皂苷元合成皮质激素
Basic structure of adrenocorticoid drugs
甾核结构
Cortisone (可的松)
Hydrocortisone (氢化可的松)
aldosterone (醛固酮)
Structure and Activity Relationship
Adrenocorticoid
Glucocorticoids : hydrocortisone, cortisone Mineralocorticoids： aldosterone，desoxycortone Sex hormones
(2) Permissive action Potentiating the effects of catecholamines and glucagon
(3) Anti-inflammatory effects Acute: inhibiting microvascular leakage
leukocyte infiltration Chronic: inhibiting fibroblast proliferation
Drugs affecting endocrine system
Drugs related to adrenocortical hormones Thyroid hormones and antithyroid drugs Insulin and oral hypoglycemic drugs
Cortex:adrenocorticoid Glucocorticoids (Glucocorticosteroids) Mineralocorticoids Sex hormones
regulating related gene transcription biological effects (usually slow)
Action mode of glucocorticoid drugs
CBG: corticosteroid binding globulin
S: glucocorticoid steroids
(central obesity: moon face, buffalo hump)
d) Water and electrolytic: Na+ excretion ↓, K+ excretion ↑,
Ca2+ excretion↑and absorption↓
Glucocorticoid drugs
Fludrocortisone (氟氢可的松)
(地塞米松)
Triamcinolone (曲安西龙)
Non-gene modulation
Gene modulation (GCS, TH)
Mechanisms of glucocorticoid actions
binding to glucocorticoid receptor (GR) nuclear translocation binding to GRE or nGRE
deposition of collagen cicatrization (瘢痕形成)
Glucocorticoid drugs
a) Inhibiting inflammation related proteins or enzymes
Dexamethasone was used GR was labeled with green fluorescent protein
1. Pharmacological effects
Mechanisms of glucocorticoid actions (1) Effects on metabolisms (2) Permissive action (3) Anti-inflammatory effects (4) Effects on immune and allergy (5) Anti-shock (6) Other effects
Structure and Activity Relationship
(2) 9引入氟原子: fludrocortosone (氟氢可的松).
基本结构
(3)引入甲基: 6-methylprednisolone,dexamethasone (6甲泼尼龙, 地塞米松).
(4) 16引入羟基: triamcinolone(曲安西龙).
antipyretic effects effects on blood and blood-forming organs skeletal system CNS effects
Glucocorticoid drugs
(1) Effects on metabolisms a) Carbohydrate: blood glucose ↑: gluconeogenesis ↑, glycolysis↓, glucose utilization↓ b) Protein: synthesis ↓, degradation ↑ c) Lipid: long term use: plasma cholesterol ↑, fat redistribution
GR: glucocorticoid receptor
HSP: heat shock protein
IP: immunophilin
GRE: glucocorticoidresponse element
Nuclear translocation of glucocorticoid receptors (GR)
(1) 1位和2位碳之间改成不饱和的双键:
cortisone prednisone hydrocortisone prednisolone
基本结构
Co百度文库tisone (可的松)
Prednisone (泼尼松)
Hydrocortisone
(氢化可的松, Cortisol)
Prednisolone (泼尼松龙)
黄山药
穿地龙
薯蓣属植物（黄山药、穿地龙） 提取薯蓣皂苷元合成皮质激素
Basic structure of adrenocorticoid drugs
甾核结构
Cortisone (可的松)
Hydrocortisone (氢化可的松)
aldosterone (醛固酮)
Structure and Activity Relationship