1. Steroidal hormones synthesized by the adrenal glands
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).
9/18/2018
MEDC 603 Steroids

2. Adrenocorticoids Hydrocortisone Aldosterone (11b,17a,21-trihydroxy-
pregn-4-ene-3,20-dione)
Aldosterone
(11b,21-dihydroxy-
pregn-4-ene-3,18,20-trione)
9/18/2018
MEDC 603 Steroids

3. Overall Equilibrium in Aldosterone
Opened form hemi-acetal form
Aldosterone
9/18/2018
MEDC 603 Steroids

4. Adrenocorticoids  Biological Activities 1. Glucocorticoid Activity
1.1 Effects on Metabolism
Stimulation of gluconeogenesis, particularly in the liver
Mobilization of amino acids from extrahepatic tissues
Inhibition of glucose uptake in muscle and adipose tissue
Stimulation of fat breakdown in adipose tissue
1.2 Effects on Inflammation and Immune Function
Anti-inflammatory properties
Immunosuppressive properties
1.3 Other Effects of Glucocorticoids
Multiple effects on fetal development (promote maturation of the lung)
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
Effect on Water
2.2.1 Increased re-absorption of water
9/18/2018
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)
9/18/2018
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
9/18/2018
MEDC 603 Steroids

7. Biochemical Mechanism of Action
Cortisol Aldosterone
Anti-inflammatory
Action
Mineralocorticoid
Action
Receptor Receptor
Lipocortin Aldosterone-
induced protein
Phospholipase A2
Cell membrane
phospholipids
Prostaglandins
leucotrienes
Regulates
Na+-K+-ATPase Pump
Na+ Influx
9/18/2018
MEDC 603 Steroids

8. Biosynthesis of Adrenocorticoids
Corticosterone
9/18/2018
MEDC 603 Steroids

9. Metabolism of Adrenocorticoids
9/18/2018
MEDC 603 Steroids

10. Structure-Activity Relationships
Anti Salt Plasma
inflammatory retaining half
activity activity life
Hydrocortisone m
Cortisone m
9/18/2018
MEDC 603 Steroids

11. Structure-Activity Relationships
Anti Salt Plasma
inflammatory retaining half
activity activity life
Prednisone m
Prednisolone m
9/18/2018
MEDC 603 Steroids

12. Structure-Activity Relationships
Anti Salt Plasma
inflammatory retaining half
activity activity life
6a-methyl m
prednisolone
Triamcinolone m
9/18/2018
MEDC 603 Steroids

13. Structure-Activity Relationships
Anti Salt Plasma
inflammatory retaining half
activity activity life
Dexamethasone m
Betamethasone m
9/18/2018
MEDC 603 Steroids

14. Structure-Activity Relationships
Anti Salt Plasma
inflammatory retaining half
activity activity life
Aldosterone m
11-deoxy m
corticosterone
Fludrocortisone m
9/18/2018
MEDC 603 Steroids