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Adrenocorticoids

Adrenocorticoids. Adrenocorticoids. Aldosterone (11 b ,21-dihydroxy- pregn-4-ene-3,18,20-trione). Hydrocortisol (11 b ,17 a ,21-trihydroxy- pregn-4-ene-3,20-dione). Adrenocorticoids. Addison’s Disease Cushing’s Disease Conn’s Syndrome.  Disease States. Adrenocorticoids.

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Adrenocorticoids

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  1. Adrenocorticoids MEDC 603 Steroids

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

  3. Adrenocorticoids • Addison’s Disease • Cushing’s Disease • Conn’s Syndrome  Disease States MEDC 603 Steroids

  4. Adrenocorticoids  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

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

  6. Overall Structure of Adrenocorticoids ~ planar A ring Differences in the substitution pattern 3D structure of hydrocortisol 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. Reduction C-20 Reduction C-4 Reduction C-3 Metabolism of Adrenocorticoids MEDC 603 Steroids

  9. Oxidation C-11 Reduction at C-3, C-4 and C-20 positions 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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