Adrenal/Bone Pharm Flashcards
What are the 3 adrenocorticosteroids?
1-Glucocorticoids (regulation of intermediary metabolism/immunity)
2-Mineralcorticoids (aldosterone-salt retention)
3-Androgens (dehydroepiandrosterone-can be converted to estrogens)
What drugs are used for their rapid and dramatic effect on inflammation and slows bone erosion and rheumatoid arthritis?
Glucocorticoids
*may cause loss of muscle mass and diabetogenesis
What is the half-life of cortisol (hydrocortisone)?
60-90 minutes
*synthesized from cholesterol
When plasma cortisol levels exceed ______ mug/dL CBG is saturated and the concentration of free cortisol rises rapidly
20-30
Steroids interact with _______ to regulate and transcribe target genes
promoters
What do glucocorticoids stimulate in the fasting state?
Gluconeogenesis and glycogen synthesis
How do glucocorticoids affect fat deposits?
Has a net increase in fat deposition
How do glucocorticoids affect bone?
They have catabolic and anti-anabolic effects on bone causing osteoporosis
*major limitation of long term steroid use
How is inflammation reduces by glucocorticoids?
They affect leukocytes and suppress inflammatory cytokines/chemokines
What are 3 short-medium acting glucocorticoids?
1-Hydrocortisone
2-Cortisone
3-Prednisone
Which glucocorticoid is long-acting?
dexamethasone
What are 7 conditions steroids can be used for?
1-Allergic rxns 2-GI disease 3-Systemic inflammation 4-Infection 5-Inflammatory conditions of bones/joints 6-Pulmonary disease 7-Skin disease
Which disease is a result of adrenal glands producing too little cortisol, often has insufficient levels of aldosterone and may have weakness and weight loss?
Addison’s disease
What is the typical treatment for Addison’s disease?
20-30 mg of hydrocortisone daily
*fludrocortisone may be added for salt-retention
Which disease has chronic high levels of cortisol usually due to a ACTH secreting tumor?
Cushing syndrome
*fatty hump between shoulders, round face, stretch marks, osteoporosis and hypertension
What are 3 cushings medications?
1-Ketoconazole (nizoral)
2-Metyrapone (Metopirone)
3-Mifepristone (korlym)
Which drug is an inhibitor of adrenal and gonadal steroid synthesis by inhibiting side chain cleavage required for steroid hormone synthesis?
Ketoconazole (Nizoral)
Which drug has a relatively selective inhibitor of steroid 11-hydroxylaiton and interferes with cortisol and corticosterone synthesis?
Metyrapone (Metopirone)
Which drug is an antagonist to steroid receptors?
Mifepristone (Korlym)
_______ Is abnormal loss of bone whereas ______ is uncontrolled osteoclastic bone resorption and poor bone formation
Osteoporosis
Paget’s disease
What drug is secreted by thyroid, is 32 AA peptide, administered by injection or spray and inhibits osteoclastic bone resorption?
Calcitonin
What are the three main regulators of Ca homeostasis?
1-Parathyroid Hormone (PTH)
2-Fibroblast growth factor 23 (FGF23)
3-Vit D
*Calcitonin is less critical
Which group of drugs suppress activity of osteoclasts in part through the inhibition os farnesyl pyrophosphate synthesis?
Bisphophonates
*inhibit bone resorption. used to prevent osteoporosis and pagets disease
What are the two main bisphosphonate drugs?
1-Ibandronate (Boniva)-monthly
2-Alendronate sodium (Fosamax)-daily/weekly
What are 4 drugs that secondarily regulate bone mineral homeostasis?
1-Calcitonin
2-Glucocorticoids (reverse hypercalcemia)
3-Estrogens (prevent bone loss)
4-Selective estrogen Receptor Modulators
Which drug is an antibody to the osteoclast stimulating RANK?
Denosumab (XGEVA)
*Blocks osteoclast number and activity
Which drug is a recombinant form of parathormone segment and activates osteoblasts to stimulate new bone formation?
Terparatide (Forteo)
