Osteoporosis Pharmacology Flashcards
Two OTC supplements commonly used that affect calcium regulation
Calcium salts
Vitamin D supplements
Similar in structure and function to human calcitonin synthesized by thyroid, but has a longer half-life and greater potency
Calcitonin-salmon
Effects of calcitonin-salmon on calcium regulation
Inhibits activity of osteoclasts to decrease bone resorption
Inhibits renal tubular resorption of calcium to increase calcium excretion
Clinical applications of calcitonin-salmon
Used for tx of established osteoporosis, but not prevention
Also used in Paget disease of bone
Can treat hypercalcemia but not a preferred target
AEs of calcitonin salmon
Generally very safe
Intranasal dosing can cause dryness and irritation
Parenteral dosing can cause inflammatory reaction at the injection site
Neutralizing antibodies appear in some pts over time
Name the bisphosphonates used to inhibit bone resorption in osteoporosis
Alendronate Risedronate Ibandronate Tiludronate Zolendronic acid
MOA of the bisphosphonates (i.e., alendronate)
Structural analogs of pyrophosphate, a normal constituent of bone
Undergo incorporation into bone, then inhibit bone resorption by decreasing both the number and activity of osteoclasts
Clinical applications of the bisphosphonates
Drugs of first choice for:
Postmenopausal osteoporosis
Osteoporosis in men
Glucocorticoid-induced osteoporosis
Paget disease of bone
Hypercalcemia of malignancy
AEs of the bisphosphonates
Esophagitis +/- ulceration (minimized by taking with glass of water on empty stomach)
Ocular inflammation
Osteonecrosis of the jaw
Atypical femur fractures
Atrial fibrillation
Bisphosphonate most commonly associated with osteonecrosis of the jaw (often occurring after tooth extraction or some other dental procedure in cancer pts), and is also associated with dose-dependent kidney damage and rarely atrial fibrillation
Zolendronic acid
MOA of raloxifene
Selective estrogen receptor modulator (SERM)
Exerts estrogen effects in bone
Anti-estrogenic in breast and uterus
SERM that is not generally used to tx osteoporosis
Tamoxifen
Clinical applications of raloxifene
Due to its estrogen agonist effects on bone, it is used to prevent AND treat postmenopausal osteoporosis
Due to its antiestrogenic effects on the breast, used to reduce the risk for development (but not treat) estrogen-dependent breast cancer
AEs of raloxifene
Increased risk of DVT, PE, and stroke (discontinue in anticipation of prolonged immobilization)
Pregnancy risk category X — leads to many fetal anomalies and fetal death
Can cause hot flashes in women previously asymptomatic
What is the only drug for osteoporosis that increases bone formation?
Teriparatide (PTH 1-34)
[Clinical indications include tx of postmenopausal osteoporosis, osteoporosis in men, and glucocorticoid-induced osteoporosis]