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Adrenocorticoids

Adrenocorticoids. Steroidal hormones synthesized by the adrenal glands. An inner medulla , which is a source of the catecholamines epinephrine and norepinephrine. An outer cortex , which secretes several classes of steroid hormones (glucocorticoids and mineralocorticoids, plus a few others). .

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Adrenocorticoids

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  1. Adrenocorticoids Steroidal hormones synthesized by the adrenal glands An inner medulla, which is a source of the catecholamines epinephrine and norepinephrine. An outer cortex, which secretes several classes of steroid hormones (glucocorticoids and mineralocorticoids, plus a few others). MEDC 603 Steroids

  2. Adrenocorticoids Aldosterone (11b,21-dihydroxy- pregn-4-ene-3,18,20-trione) Hydrocortisone (11b,17a,21-trihydroxy- pregn-4-ene-3,20-dione) MEDC 603 Steroids

  3. Overall Equilibrium in Aldosterone Opened form hemi-acetal form Aldosterone MEDC 603 Steroids

  4. Adrenocorticoids  Biological Activities 1. Glucocorticoid Activity 1.1 Effects on Metabolism 1.1.1 Stimulation of gluconeogenesis, particularly in the liver 1.1.2 Mobilization of amino acids from extrahepatic tissues 1.1.3 Inhibition of glucose uptake in muscle and adipose tissue 1.1.4 Stimulation of fat breakdown in adipose tissue 1.2 Effects on Inflammation and Immune Function 1.2.1 Anti-inflammatory properties 1.2.2 Immunosuppressive properties 1.3 Other Effects of Glucocorticoids 1.3.1 Multiple effects on fetal development (promote maturation of the lung) 1.3.2 Miscellaneous effects (Excessive glucocorticoid levels affect many systems, e.g., inhibition of bone formation, suppression of calcium absorption and delayed wound healing.) 2. Mineralocorticoid Activity 2.1 Effect on Electrolytes 2.1.1 Increased re-absorption of sodium 2.1.2 Increased renal excretion of potassium 2.2 Effect on Water 2.2.1 Increased re-absorption of water MEDC 603 Steroids

  5. Adrenocorticoids  Disease States  Addison's disease: Affects about 1 in 100,000 people; caused by adrenal in-sufficiency (90%); typical by auto-immune disorders; both cortisol and aldostertone hormones are lacking.  Cushing's disease: Affects about 10 to 15 million people / yr; caused by adrenal hyper-activity (cortisol); typical because of tumor growth exposure to prednisone for asthma, rheumatoid arthritis, lupus or other inflammatory diseases  Conn's syndrome: May affect 15% of patients with high blood pressure; caused by hyper production of aldosterone; inability of adrenal cortex to carry out 17a-hydroxylation; hypertension, loss of potassium in the urine, muscle weakness and passing of large volumes of urine (polyuria) MEDC 603 Steroids

  6. Glucocorticoids  Selected Indications • Allergic Rhinitis Rheumatoid Arthritis • Asthma Multiple Sclerosis • Carpal Tunnel Syndrome Dermatitis • COPD Osteoarthritis • Cystic Fibrosis Temporal Arteritis • Gout Psoriasis • Herniated Disc Shingles • Inflammatory Bowel Disease Tennis Elbow • Sinusitis Lupus Erythematosus MEDC 603 Steroids

  7. Phospholipase A2 Prostaglandins leucotrienes Cell membrane phospholipids Biochemical Mechanism of Action Cortisol Aldosterone Anti-inflammatory Action Mineralocorticoid Action Receptor Receptor Lipocortin Aldosterone- induced protein Regulates Na+-K+-ATPase Pump Na+ Influx MEDC 603 Steroids

  8. Biosynthesis of Adrenocorticoids Corticosterone MEDC 603 Steroids

  9. Metabolism of Adrenocorticoids MEDC 603 Steroids

  10. Structure-Activity Relationships Anti- Salt- Plasma inflammatory retaining half activity activity life Hydrocortisone 1 1 120 m Cortisone 0.8 0.8 30 m MEDC 603 Steroids

  11. Structure-Activity Relationships Anti- Salt- Plasma inflammatory retaining half activity activity life Prednisone 4 1 60 m Prednisolone 4 0.6 115-212 m MEDC 603 Steroids

  12. Structure-Activity Relationships Anti- Salt- Plasma inflammatory retaining half activity activity life 6a-methyl 4 0 78-188 m prednisolone Triamcinolone 5 0 200+ m MEDC 603 Steroids

  13. Structure-Activity Relationships Anti- Salt- Plasma inflammatory retaining half activity activity life Dexamethasone 30 0 110-210 m Betamethasone 35 0 300+ m MEDC 603 Steroids

  14. Structure-Activity Relationships Anti- Salt- Plasma inflammatory retaining half activity activity life Aldosterone 0.2 800 30 m 11-deoxy 0 40 60 m corticosterone Fludrocortisone 10 800 300+ m MEDC 603 Steroids

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