Test 4 notes 4 - T reatment With Corticosteroids Physiologic Actions of the Glucocorticoid Hormones The endogenous glucocorticoid hormones

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Treatment With Corticosteroids Physiologic Actions of the Glucocorticoid Hormones The endogenous glucocorticoid hormones, primarily cortisol, enter through the plasma membranes of their target cells and combine with their receptors in the cytosol of the cell. This hormone-receptor complex then enters the nucleus of the target cells and combines with a specific DNA binding domain on certain chromosomes called the Glucocorticoid- Response Element. This binding (interaction) then results in the activation of certain genetic sequences that result in the synthesis of enzymes and other proteins that ultimately result in the physiologic actions of cortisol and the glucocorticoid hormones and drugs. These actions are: - Suppresses inflammation - Suppresses immune responses - Increases gluconeogenesis - Promotes glycogenolysis - Increases insulin resistance - Increases action of proteolytic enzymes and breaks down protein - Inhibits protein synthesis - Increases actions of lipolytic enzymes and breaks down fat - Produces sodium and water retention (partial agonist on aldosterone receptors) - Promotes the excretion of potassium (also an aldosterone receptor effect) List of the Short-Acting Glucocorticoid Drugs cortisone (Cortone) hydrocortisone (Cortisol) (Cortef) (Solu-Cortef) (Hydrocortone) Also many over-the-counter cream and ointment preparations: (Cortaid) (Lanacort) (Orabase) (Cortifoam) etc. Topical preparations will be discussed in the section on Drugs Affecting the Dermatological System. Pharmacodynamics of the Short-Acting Glucocorticoid Drugs Being glucocorticoid "steroid" hormones, these drugs act in a manner identical to the actions of the endogenous glucocorticoid hormones; that is, they interact with glucocorticoid hormone receptors. In addition, these agents also have fairly strong affinity and intrinsic activity on aldosterone receptors. Pharmacokinetics of the Short-Acting Glucocorticoid Drugs The short-acting agents are well absorbed by the oral, I.M. and transcutaneous routes, depending on the brand. Hydrocortisone is also administered I.V. They are metabolized by the liver and excreted in the urine. 1
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Treatment With Corticosteroids Advantages of the Short-Acting Glucocorticoid Drugs - Rapid (for glucocorticoids) onset of action; within hours. - Long duration of action; 1-2 days - Effective in once-a-day dosing - Some topicals (in low doses) available over-the-counter - Good for rapid replacement use in glucocorticoid-deficient individual (like Addison's disease) - Have some anti-inflammatory uses - Can support a failing circulation by provoking retention of sodium and water to improve
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This note was uploaded on 05/19/2011 for the course NURSING 517/617 taught by Professor Lipstate during the Spring '11 term at University of Louisiana at Lafayette.

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Test 4 notes 4 - T reatment With Corticosteroids Physiologic Actions of the Glucocorticoid Hormones The endogenous glucocorticoid hormones

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