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Adrenal corticosteroids
Pharm III
22
Science
Professional
09/18/2011

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Term
Adrenal output of cortisol?
Definition
~10 mg per day
Term
Levels of glucocorticoids during the day?
Definition
Circadian rhythm, peak levels around 8am. Levels rise after meals
Term
Glucorticoids numerous physiological effects
Definition
effects:
intermdiary metabolism, cardiovascular function, growth and immunity
Term
Glucocorticoids effects on inflammation
Definition
-induce expression of annexin--a protein which inhibits phospholipase A2 and thus decreasese the sythesis of eicosanoids, inlcuding PG's and LT's
-reduce release of proteases, eg collagenase and stromelysin
-suppress release of pro-inflamm cytokines,, eg IL1, IL6 and TNF from macrophages
-suppress events in lymphocyte activiation
-block IgE mediated release of histamine and LTC4 by basophils
Term
Glucocorticoid pharmacokinetics
Definition
well-absorbed, highly protein bound and eliminated primarily by liver
Term
Major use of glucocorticoids
Definition
replacement therapy and anti-inflammatory agents
Term
glucocorticoid common indications
Definition
asthma, allergic rhinitis, psoriasis, eczema and hypersensitivity dermatidies, vasculitis, coinnective tissue diseases, IBD, nephrotic syndrome, immunosuppreseive agent in organ transplant, promotion of fetal lung development
Term
the synthetic corticosteroids
Definition
hydrocortisone (cortisol)
cortisone
prednisone
dexamethasone
Term
Source of synthetic corticosteroids
Definition
synthesized with modifications to create steroids with special characterisitcs
Term
synthetic corticosteroids pharmacokinetics
Definition
-similar to cortisol and other steroids
-may have different ratios of glucocorticoid potency to mineralocorticoid potency
Term
Hydrocortisone indications
Definition
-allergic disorder
-disorder of endocrine system
-inflammatory disorder of the musculoskeletal system
-disorder of teh respiratory system
-disorder if the skin
Term
Cortisone (cortone acetate)indications
Definition
same as hydrocortisone plus
Adrenal insufficiency

-allergic disorder
-disorder of endocrine system
-inflammatory disorder of the musculoskeletal system
-disorder of teh respiratory system
-disorder if the skin
Term
Prednisone indications
Definition
Same as cortisone plus:
Allergic disorders, intractable to adequate trials of conventional treatment
-asthma
-inflammatory disease of musculoskelatal system
-polyyositis
-rheum arthritis
Term
Dexamethasone (Decadron) indications
Definition
same as hydrocortisone plus:
-cerebral edema--associated with primary or metastatic brain tumor craniotomyor head injury
-Cushing's sydrome diagnosis
Term
Clinical uses of adrenocorticosteroids
Definition
-diagnosis and treatment of disturbed Adrenal function
-adrenocortical hypo- and hyperfunction
-diagnostic purposes
-stimulation of lung maturation in teh fetus
-corticosteroids and nonadrenal disorders
Term
synthetic corticosteroid ACUTE toxicities
Definition
hypertension, hyperglycemia, mood disturbance, myopathy, psychosis, masked fever, fluid retention, hypokalemic metabolic alkalosis
Term
synthetic corticosteroids SUB-ACUTE CHRONIC toxicity
Definition
moon facies, stria, delayed wound healing, acne, hirsutism, ecchymoses, ulcers and GI bleeding, gluacoma, cataracts, infection, osteopenia
Term
Stategies for minimizing synthetic toxicity
Definition
-use drugs with low mineralocorticoid activity
-use of alternate day therapy
-topical administration reduces systemic effects
Term
Mineralocorticoids eg?
Definition
aldosterone, deoxycorticosterone, fludrocortisone
Term
Aldosterone?
Definition
-synthesized in teh zona glomerulosa of adrenal cortex
-action-promotes reabsorption of Na from distal convoluted and proximal collecting tubules
Term
Fludrocortisone
Definition
Indications: Addison's disease, adrenogenital disorder

-treatment of adrenocortical insufficiency associated with mineralocorticoid deficiencey.
Term
Ketoconazole (Nizoral)
Definition
-inhibits cholesterol side chain cleavage
-inhibit steroid synthesis only seen at high doeses

-anti fungal imidazole derivative
-potent and non-selective inhibition of adrenal and gonadol steroid synthesis
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