B6.052 - CBCL Osteoporosis Prework 6 Pharmacology Flashcards
prevention and treatment of post menopausal osteoporosis
appropriate calcium and vit D intake (especially prior to achieving peak bone mass)
exercise
pharmacologic agents
calcium and vitamin D for tx
clinical trials report benefit
1000 vit d + 1000 Ca for adults >65
bisphosphonates
alendronte (w)
risedronate (w,m)
ibandronate (m, IV)
zolendronic acid (IV ann)
mechanism of bisphosphonates
direct inh of bone resorption
concentrate at sites of active remodeling, remains in matrix until bone is remodeled
released in acid environment of resorption lacunae and induces apoptosis in osteoclasts
also inh cholesterol biosynthetic pathway contributing to resorptive activty
AEs of bisphosphonates
hypocalcemio
osteonecrosis of the jaw
atypical femur fractures
GI sx
denosumab
fully human mab to RANKL
binds/inhibits ability of RANKL to mature osteoclasts from osteoclast precursors (similar to OPG)
reduces survival of osteoclasts
how is denosumbab administeredand AEs
2x yearly inj if stopped bone lost rapidly if another agent not used osteonecrosis of jaw atypical femur fractures hypocalcemia skin infx dermatitis
raloxifene
SERM
not pure agonists of estrogen receptor, have diff effect on diff tissues
produce diff structural changes in receptor upon bidning, alters cofactros with which ER interacts
partially replaces missing estrogen post menopause with respect to bone remodeling
no effect on heart disease or other rfx
65% reduction in invasive breast cx
what does PTH do
stimulates osteoclasts , bone resorption, Ca++ mobilized, inhibits osteoblasts
increases Ca resorption in distal tubules
calcitrol release, calcium absorption in intestine
what does calcitonin do
stimulates osteoblast activity
inhibits osteoclasts
transient increase in Ca secretion
teriparatide
AA 1-34 of PTH
stimulates osteoblastic bone formation
PTH on a longer time scale stimulates both osteoblasts and osteoclasts
bone formation is stimulated more than resorption
teriparatide impact on bone
increases predominantly trabecular bone at lumbar spine and femoral neck
administered once a day sub q
calcitonin MOA and administration
injection or nasal spray stimulates osteoblast activity and inhibits osteoclast activity