corticosteroids.pptx

B. Pharm. 5th sem. 3rd year
Medicinal chemistry-II structures and chemistry of corticosteroid.

1. CHEMISTRY OF CORTICOSTEROIDS Raj K. Prasad (Gold Medalist) M. Pharm. ( P’ceutical Chemistry)

2. CORTICOSTEROIDS All corticosteroids are derivatives of cyclopentanophenanthrene with keto-groups at C3 and C20 and an unsaturated bond between C4 and C5. Corticosteroids do not heal illnesses, but they are widely used in various conditions when it is necessary to utilize their anti-inflammatory, immunosuppressant, and mineralocorticoid properties. They are used in replacement therapy for patients who have adrenal insufficiency.

3. Glucocorticoids (Moderate to low salt retention):

4. Glucocorticoids Glucocorticoids (GC) are endogenous compounds that have an effect on carbohydrate, lipid, and protein metabolism, and which exhibit anti-inflammatory, desensitizing, and antiallergy action. They are immunodepressants , and they also possess anti-shock and anti-toxic action.

5. example 11/22/2023 Sample Footer Text 5

6. Mineralocorticoids (High salt retention): 6

7. Mineralocorticoids (MC) Mineralocorticoids (MC) are endogenous compounds that have an effect on fluid and electrolytic balance in the body, mainly by promoting sodium retention in the kidney. Eg. aldosterone, 11-deoxycorticosterone, 11-deoxy-17-oxycorticosterone.

8. CORTISONE 8

9. CORTISONE It is a naturally occurring cortisone with good systemic anti-inflammatory activity and low-to-moderate salt-retention activity after its in vivo conversion to hydrocortisone acetate. This conversion is mediated by 11 β -hydroxysteroid dehydrogenase. Its plasma half-life is only about 30 minutes, compared with 90 minutes to 3 hours for hydrocortisone.

10. USES Cortisone is used for inflammatory processes, allergies, and adrenal insufficiency. It also used in collagen diseases, Addison disease, severe shock, allergic conditions, chronic lymphocytic leukemia, and many other indications. Cortisone acetate is relatively ineffective topically, mainly because it must be reduced in vivo to hydrocortisone.

11. HYDROCORTISONE (11β,17α,21-trihydroxypregn-4-en-3,20-dione)

12. Uses 11/22/2023 Sample Footer Text 13

13. Uses Hydrocortisone drugs are used for severe inflammation, shock, primary or secondary renal insufficiency, adrenal insufficiency, ulcerative colitis, and rheumatoid, gouty, and psoriatic arthritis, collagen and dermatological diseases, allergic conditions, ophthalmologic and gastrointestinal diseases, and respiratory tract diseases.

14. PREDNISOLONE (11β,17α,21-trihydroxypregna-1,4-dien-3,20-dione) 11/22/2023 Sample Footer Text 15

15. Prednisolone differs from prednisone in that the keto-group at C11 of prednisone is replaced by a hydroxyl group. Prednisolone is available in various salts and esters to maximize its therapeutic utility like Prednisolone acetate, Prednisolone sodium phosphate, Prednisolone sodium succinate etc.

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17. Uses Prednisolone is used for the same indications as all corticosteroids: Rheumatism, Polyarthritis, Bronchial asthma, Neurodermatitis, And eczema. raj 18

18. BETAMETHASONE Betamethasone, which differs from dexamethasone only in configuration of the 16-methyl group was made available for the treatment of rheumatic diseases and dermatologic disorders. 11/22/2023 raj 19

19. Structure 11/22/2023 Sample Footer Text 20

20. Uses B etamethasone is primarily used locally to treat dermatitis and eczema, and also as an anti-itch agent.

21. 11/22/2023 Sample Footer Text DEXAMETHASONE 22

22. Structure 11/22/2023 Sample Footer Text 23

23. The distinctive characteristic of dexamethasone is the presence of a fluorine atom at C9 of the steroid ring. A 16a-methyl group decreases the reactivity of the 20-keto group to carbonyl reagents and increases the stability of the drug in human plasma in vitro.

24. Uses Dexamethasone is used for the same indications as all corticosteroids; however, it exhibits a significantly more powerful anti-inflammatory and anti-allergic action. It is used for circulatory collapse—shock during or after surgical operations, trauma, blood loss, myocardial infarction, and burns. It is also used in severe infections—toxemia, vascular collapse in meningococcosis , septicemia, diphtheria, typhoid fever, and peritonitis. It is used in severe allergic conditions—asthmatic status, laryngeal edema, severe anaphylactic reactions to medicinal drugs, and pyrogenic reactions. Raj K. prasd 25

25. RAJ THANK YOU 26