各论II 27、肾上腺皮质激素药物.pptxVIP

Drugs affecting endocrine system;Drugs related to adrenocortical hormones Thyroid hormones and antithyroid drugs Insulin and oral hypoglycemic drugs;;Adrenocorticoid;黄山药;;Structure and Activity Relationship;Structure and Activity Relationship;Non-gene modulation;;Action mode of glucocorticoid drugs CBG: corticosteroid binding globulin S: glucocorticoid steroids GR: glucocorticoid receptor HSP: heat shock protein IP: immunophilin GRE: glucocorticoid-response element;Nuclear translocation of glucocorticoid receptors (GR) 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 antipyretic effects effects on blood and blood-forming organs skeletal system CNS effects;(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 (central obesity: moon face, buffalo hump) d) Water and electrolytic: Na+ excretion ↓, K+ excretion ↑, Ca2+ excretion↑and absorption↓ ;(2) Permissive action Potentiating the effects of catecholamines and glucagon ? (3) Anti-inflammatory effects Acute: inhibiting microvascular leakage leukocyte infiltration Chronic: inhibiting fibroblast proliferation deposition of collagen cicatrization (瘢痕形成);a) Inhibiting inflammation related proteins or enzymes inducing lipocortin, inhibiting phospholipase A2 activity, decreasing mediators: PGs, LTs, PAF inhibiting the expression of PLA2, COX-2, inducible NOS, etc. inducing ACE, degrade bradykinin. ;; a) Inhibiting infla