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CORTOCOSTEROIDS   - Dr. N.R. BISWAS -
ADRENOCORTICOID   HORMONES ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
HORMONES OF ADRENAL CORTEX ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
MECHANISM   OF   ACTION   ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
ACTIONS OF CORTICOSTEROIDS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
GLUCOCORTICOID ACTIONS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
GLUCOCORTICOID   ACTIONS ,[object Object],[object Object],[object Object],[object Object]
Glucocorticoid  actions   ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Glucocorticoid    actions   ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Glucocorticoid    actions   ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Glucocorticoid    actions   ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
 
Relative potencies and equivalent doses of corticosteroids __________________________________________________________________________________________________________________________   RELATIVE  ANTI-    RELATIVE    APPROXIMATE    INFLAMMATORY    Na+-    DURATION OF  EQUIVALENT COMPOUND  POTENCY    RETAINING  ACTION*  DOSE  †       POTENCY    (mg)   __________________________________________________________________________________________________________________________ Cortisol (Hydrocortisone)  1 1 S   20 Tetrahydrocortisol 0 0 -   - Prednisone (∆ 1 -Cortisone) 4 0.8 I   5 Prednisolone (∆ 1 -Cortisol) 4 0.8 I   5 6  -Methylprednisolone 5 0.5 I   4 Fludrocortisone (9  -Fluorocortisol) 10 125 S   - 11-Desoxycortisol) 0 0 -   - Cortisone (11-Dehydrocortisol) 0.8 0.8 S   25 Corticosterone 0.35 15 S   - Triamcinolone (9  -Fluoro-16  -hydroxyprednisolone) 5 0 I   4 Paramethasone (6  -Fluoro-16  -methylprednisolone) 10 0 L   2 Betamethasone (9  -Fluro-16  -methylprednisolone) 25 0 L   0.75 Dexamethasone (9  -Fluoro-16  -methylprednisolone) 25 0 L   0.75 _________________________________________________________________________________________________________________________ *S=Short, or 8 to 12 hour biological half-life; I=intermediate, or 12 to 36 hour biological half-life; L=long, or 36 to 72 hour biological half-life.  †   These dose relationships apply only to oral or intravenous administration; relative potencies may differ greatly when injected intramuscularly or into joint spaces.
CORTICOSTEROIDS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
HYDROCORTISONE ACETATE ,[object Object],[object Object],[object Object],[object Object],[object Object]
SYNTHETIC GLUCOCORTICOIDS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
ADVERSE EFFECTS of prolonged use of glucocorticoids ,[object Object],[object Object],[object Object]
CONTRAINDICATIONS   of   Corticosteroids ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],Adverse skin reactions to topical glucocorticoids
Drug interactions of glucocorticoids    Glucocorticoid dosage is decreased:   Antibiotics (erythromycin, trioleandomycin), cyclosporin, isoniazid and ketoconazole reduce the metabolic clearance of glucocorticoids.  Estrogens increase the levels of corticosteroid binding protein and thus reduce the free fraction; they also reduce the clearance.  Cholestyramine decreases the intestinal absorption. Antiepileptic drugs(barbiturates, phenytoin, carbamazemine), rifampicin,, aminoglutethimide increase the metabolism by inducing hepatic microsomal enzymes.  Antianxiety and antipsychotic drugs: Recurrent or poor control of CNS symptoms due to inherent glucocorticoid effects.     Glucocorticoid dosage is increased:      Glucocorticoid dosage needs adjustment:      Anticholinesterases:   May precipitate myasthenic crisis    Anticoagulants:   Effectiveness of anticoagulants decreases    Antihypertensives:   Their effectiveness decreases    Oral hypoglycemics:   Their effectiveness decreases    Sympathomimetics:   Their effectiveness increases    Salicylates:   Their clearance is increased
THERAPEUTIC   USES   of   glucocoricoids ,[object Object],[object Object],[object Object],[object Object]
USES  ( Contd .) ,[object Object],[object Object],[object Object],[object Object],[object Object]
USES  ( Contd .) ,[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],Principles of treatment of acute adrenal insufficiency
Precautions during glucocorticoid therapy  Before starting therapy    Enquire about and check for: peptic ulcer, diabetes mellitus,  tuberculosis, any other infection (especially one not amenable  to chemotherapy). During therapy    Prescribe the drug with food    Diet low in calories and sodium, and high in potassium ,[object Object],[object Object],[object Object],[object Object]
MINERALOCORTICOIDS ,[object Object],[object Object],[object Object],[object Object],[object Object]
Therapeutic Uses of Mineralocortcoids ,[object Object],[object Object],[object Object],[object Object],[object Object]

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Corticosteroides Mdpm 408

  • 1. CORTOCOSTEROIDS - Dr. N.R. BISWAS -
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  • 13. Relative potencies and equivalent doses of corticosteroids __________________________________________________________________________________________________________________________ RELATIVE ANTI- RELATIVE APPROXIMATE INFLAMMATORY Na+- DURATION OF EQUIVALENT COMPOUND POTENCY RETAINING ACTION* DOSE † POTENCY (mg) __________________________________________________________________________________________________________________________ Cortisol (Hydrocortisone) 1 1 S 20 Tetrahydrocortisol 0 0 - - Prednisone (∆ 1 -Cortisone) 4 0.8 I 5 Prednisolone (∆ 1 -Cortisol) 4 0.8 I 5 6  -Methylprednisolone 5 0.5 I 4 Fludrocortisone (9  -Fluorocortisol) 10 125 S - 11-Desoxycortisol) 0 0 - - Cortisone (11-Dehydrocortisol) 0.8 0.8 S 25 Corticosterone 0.35 15 S - Triamcinolone (9  -Fluoro-16  -hydroxyprednisolone) 5 0 I 4 Paramethasone (6  -Fluoro-16  -methylprednisolone) 10 0 L 2 Betamethasone (9  -Fluro-16  -methylprednisolone) 25 0 L 0.75 Dexamethasone (9  -Fluoro-16  -methylprednisolone) 25 0 L 0.75 _________________________________________________________________________________________________________________________ *S=Short, or 8 to 12 hour biological half-life; I=intermediate, or 12 to 36 hour biological half-life; L=long, or 36 to 72 hour biological half-life. † These dose relationships apply only to oral or intravenous administration; relative potencies may differ greatly when injected intramuscularly or into joint spaces.
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  • 20. Drug interactions of glucocorticoids  Glucocorticoid dosage is decreased: Antibiotics (erythromycin, trioleandomycin), cyclosporin, isoniazid and ketoconazole reduce the metabolic clearance of glucocorticoids. Estrogens increase the levels of corticosteroid binding protein and thus reduce the free fraction; they also reduce the clearance. Cholestyramine decreases the intestinal absorption. Antiepileptic drugs(barbiturates, phenytoin, carbamazemine), rifampicin,, aminoglutethimide increase the metabolism by inducing hepatic microsomal enzymes. Antianxiety and antipsychotic drugs: Recurrent or poor control of CNS symptoms due to inherent glucocorticoid effects.  Glucocorticoid dosage is increased:  Glucocorticoid dosage needs adjustment:  Anticholinesterases: May precipitate myasthenic crisis  Anticoagulants: Effectiveness of anticoagulants decreases  Antihypertensives: Their effectiveness decreases  Oral hypoglycemics: Their effectiveness decreases  Sympathomimetics: Their effectiveness increases  Salicylates: Their clearance is increased
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