第十一章肾上腺皮质激素类药物 PPT课件.pptVIP

Adrenocorticosteroids Pharmacological effects Anti-inflammatory effect Immunosupporessive effects Antitoxic action Antishock effect other effects Adrenocorticosteroids Antishock effect the supra-large dose steroids is extensive used in clinical treatment of all kinds of severe shock, especially toxic shock. The mechanism of the action has the relation with the following factors: Adrenocorticosteroids Increase the contraction of the heart muscle and dilate the blood vessels of spasmodic contraction. Decrease the sensitivity of blood vessels to some vasocontrictive substances and relieve blood vessels spasm, result in the improvement of microcirculation and reduction of symptoms of toxic shock. Adrenocorticosteroids Stabilization of lysosomal membranes, reduces the formation of myocardial-depressant factor (MDF) that decrease myocardial contraction force and prevents the release of proteolytic enzymes. Anti-inflammation effects Immunosupporessive effects Antitoxic action Adrenocorticosteroids Other effects blood and hematopoietic system CNS the development of the fetus. appear to antagonize the effect of vitamin D and calcium absorption. stimulate excessive production of acid and pepsin in the stomach and may cause peptic ulcer. Adrenocorticosteroids Pharmacokinetics Glucocorticoids may be given by a variety of routes. Most are active when given orally. All can be given systemically, either intramuscularly (im) or intravenously (iv). They may also be given topically. In plasma, cortisol is bound to plasma proteins. Corticosteroid-binding globulin （CBG） Albumin. Both CBG-bound and albumin-bound steroids are biologically inactive. Adrenocorticosteroids Hydrocortisone t1/2 =90 minutes, Tpeak=1-2h. metabolism in the liver, finally excreted in the urine. If there is a double bond between C1-C2 or a fluorin atom at C9, metabolism is slowed. Cortisone and prednisone are inactive until converted in the liver to hydrocortisone and prednisolone, r