441-Osteo only

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Author:
jgiantess
ID:
124287
Filename:
441-Osteo only
Updated:
2011-12-18 03:37:26
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drugs
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pharmacology
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  1. HRT
    • anti-resorptive (anti-catabolic).
    • considered for tx of mod-severe vasomotor symptoms of postmenopause only
    • osteoporosis prevention is a secondary benefit
  2. Etidronate
    • first-gen bisphosphonate, least potent anti-resorptive(anti-catabolic). R1 -CH3, R2 -OH
    • Incorporates into bone, released when hydroxyapatite dissolved by osteoclasts
    • Preferentially taken up by osteoclasts -> impair recruitment, differentiation, activity of osteoclasts. Increase osteoclast apoptosis.
    • Dose that inhibits bone resorption also impairs bone mineralization --> osteomalacia.
    • Therefore give: 400mg etid x14d, then 500mg CaCO3 x76d.
    • 1o px post-men: no effect
    • 2o px post-men: 50% RR vertebral fracture. NSS for non-vert, hip, wrist.
  3. Alendronate
    • 2nd gen bisphosphonate. anti-resorptive (anti-catabolic). R1 -OH, R2 -CH2CH2CH2NH2
    • Incorporates into bone, released when hydroxyapatite dissolved by osteoclasts
    • Preferentially taken up by osteoclasts -> impair recruitment, differentiation, activity of osteoclasts. Increase osteoclast apoptosis.
    • 1o px: 45% RR vertebral fracture (vs. NOT risedronate, and zolen was not tested)
    • 2o px: 50% RR in vert, non-vert, hip fx (all 3 drugs)
    • Orally, poorly absorbed (1-5%). Empty stomach, water only. t1/2 is 1 hour in plasma, 10 years in bone.
    • 10mg/d or 70mg/week
  4. Risedronate:
    • 2nd gen bisphosphonate. anti-resorptive (anti-catabolic). R1 -OH, R2 -CH2N-ring.
    • Incorporates into bone, released when hydroxyapatite dissolved by osteoclasts
    • Preferentially taken up by osteoclasts -> impair recruitment, differentiation, activity of osteoclasts. Increase osteoclast apoptosis.
    • 1o px: no effect
    • 2o px: 50% RR in vert, non-vert, hip fx (all 3 drugs)
    • Orally, poorly absorbed (1-5%). Empty stomach, water only. t1/2 is 1 hour in plasma, 10 years in bone.
    • 5mg/d, or 35mg/week, or 75mg/day x2 days/month.
  5. Zoledronate:
    • 3rd gen bisphosphonate. anti-resorptive (anti-catabolic). R1 -OH, R2 CH2N-ring.
    • Incorporates into bone, released when hydroxyapatite dissolved by osteoclasts
    • Preferentially taken up by osteoclasts -> impair recruitment, differentiation, activity of osteoclasts. Increase osteoclast apoptosis.
    • 1o px: not tested
    • 2o px: 50% RR in vert, non-vert, hip fx (all 3 drugs)
    • Injected 5mg once/year by IV infusion.
  6. Calcitonin
    • peptide hormone in calcium homeostasis; decreases Plasma Calcium. Anti-resorptive (anti-catabolic).
    • Suppresses activity of osteoclasts, decreases bone resorption.
    • 30% RR in vertebral fx, but not non-vertebral.
    • May have analgesic effect.
    • 2nd line tx for post-men osteo, 1st line tx for pain ass'd with acute vert fx.
  7. Denosumab (prolia)
    • osteoporosis anti-resorptive (anti-catabolic)
    • monoclonal Ab to RANKL that mimcs action of OPG, prevents RANKL from binding to RANK.
    • Decrease in osteoclast formation and bone resorption.
    • Px severe osteoporosis in post-men: 60% RR vertebral, 20% RR non-vertebral, 40% RR hip
    • May also be useful in conditions characterized by temporary rapid bone resorp (i.e. aromatase inhib tx)
    • Injection: 60mg SC q6mo.
  8. Teriparatide
    • recombinante human PTH.
    • Increases recruitment and differentioatn of osteoblasts and decreases apoptosis.
    • Given intermittently, get net bone forming effect: increases bone remodeling, with anabolic window: initial stimulation of bone formation before resorption takes place. Window lasts 12-18 months.
    • 2o post-men: 65% RR vert, 53% RR non-vert. No sig decrease in hip fx.
    • Also for glucocorticoid-induced osteo in high-risk pts.
    • Tx duration limited 2 years.Once daily injections.

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