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What increases duration of action in glucocorticoids analogues
Highr plasma protein binding
Lower affinity for 11beta HSDII
Higher lipophilicity
Higher affinity for GR
Glucocorticoids and Pregnancy
Mother can be given prednisone without SEs in fetus
Metabolism: The mother's liver converts prednisone into prednisolone, which is a more active form of the medication. However, the placenta contains an enzyme called 11β-HSDII which can convert prednisolone back to the less active prednisone.
Fetal metabolism: The fetal liver is unable to convert prednisone back into prednisolone, which means that the active drug does not accumulate in the fetus, reducing potential side effects.
Dexamethasone or betamethasone give to promote fetal lung maturation
Immune suppression mechanisms
1)Inhibition of COX2 and phospholipase A2—>Inhibits conversion of arachidonic acid to prostaglandins and leukotrienes
2)Inhibition of cytokine production and release
3)Reduced expression of ELAM1 and ICAM 1 adhesion molecules—>reduces recruitment of immune cells
4)Inhibit histamine & leukotriene C4 release
Mitotane
Selectively adrenocortical cells
Must replace both cortisol & aldosterone deficit
Aminoglutethimide
Inhibits CYP11A1 to reduce all adrenosteroids
Inhibits CYP11B1 and aromatase
Glucocorticoid replacement encessary but do NOT use dexamethason
Ketoconazole
Inhibits CYP17 and CYP11A1
Serious drug interactions, hepatic dysfunction
treat cushings
Metyrapne
Selective CYP11B1 inhibitor
Mifepristone
Progesterone receptor antagonist at LOW concentrations
Glucocorticoid recepor antagonist at HIGH concentrations
use: treat life threatening glucocorticoid levels in ectopic ACTH syndrome
Emergency contraceptive
Aldosterone effects
Na reabsorption
K excretion
Aldosterone hypofunction effects
Salt wasting
Hyperkalemia
Acidosis
Aldosterone hyperfunction effects
Volume expansion
Hypokalemia
Alkalosis
Hypertension
Mineralocorticoid receptor antagonists
Spironolactone
Eplerenone
Fludrocortisone
Mineralocorticoid receptor agonist
High mineralocorticoid: glucocorticoid potency ratio
Aldosterone repalcement therapy
Congenital adrenal hyperplasia & PCOS
Increased DHEA- a precusor to testosterone