Review of Pharmacology - 9E (2015)

Review of Pharmacology
• Effect on CVS and CNS: Glucocorticoids prevent the increase in the permeability
of capillaries. These have mild euphoric effect and high doses can lower seizure
threshold.
• Effect on GIT: These hormones may aggravate peptic ulcer by increasing the
secretion of HCl and pepsin in stomach.
• Effect on hematopoietic system: Glucocorticoids cause destruction of T cells and
B cells (less sensitive) in malignancies whereas little effect is exerted on normal
cells. These drugs cause sequestration of lymphocytes, eosinophils, monocytes and
basophils in tissues (and thus decrease circulating levels of these cells) whereas
circulating neutrophils are increased due to release from bone marrow.
• Effect on inflammatory response: Glucocorticoids are powerful anti-inflammatory
agents. Most important mechanism is the inhibition of chemotaxis (recruitment of
the cells at the site of inflammation). These hormones also induce the production of
annexins (previously called, lipocortins) that are responsible for the inhibition of
phospholipase A 2
(involved in the production of prostaglandins and leukotrienes).
They also delay the healing of wounds and scar formation.
• Effect on immunity: These hormones suppress cell mediated immunity (CMI)
more than humoral immunity. Main effect is due to inhibition of recruitment of
immune cells, but they also inhibit the release of IL-1 and IL-2. Antibody production
is affected at high doses and continuous administration of glucocorticoids can
result in catabolism of IgG. Immunosuppressive effect of glucocorticoids is the basis
of their use in graft rejection and various hypersensitivity reactions.
Endocrinology
Important Pharmacokinetic Properties
Glucocorticoids Duration of Action G Activity M Activity Potency (eq. Dose) in mg
1. HYDROCORTISONE
(CORTISOL)
Short 1 1 20
2. CORTISONE Short Minimum (0.8) 0.8 Least potent G. (25)
3. PREDNISONE Intermediate 4 0.5 5
4. PREDNISOLONE Intermediate 5 0.5 5
5. MEPREDNISONE Intermediate 5 0 4
6. METHYLPREDNISOLONE Intermediate 5 0 4
7. TRIAMCINOLONE Intermediate 5 0 4
8. FLUPREDNISOLONE Intermediate 15 0 1.5
9. PARAMETHASONE Long 10 0 2
10. BETAMETHASONE Long 25 0 Most potent G.(0.6)
11. DEXAMETHASONE Long Maximum (30) 0 0.75
MINERALOCORTICOIDS
12. DOCA 0 20
13. FLUDROCORTISONE 10 250 Most potent M.
14. ALDOSTERONE 0.3 3000 (max.) Not used clinically
248
G. = Glucocorticoid, M. = Mineralocorticoid
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