Lecture 41+42: Osteoporosis Flashcards
Action of Drug therapies for Osteopororsis
-ensure adequate Ca and Vit D
-antiresorptive action
-anabolic action
Romosozumab
-sclerostin inhibitor
-antiresorptive action AND anabolic action
-drug therapy for osteoporosis
Antiresorptive action
-inhibits bone resorption
-maintain/inc bone mass
-reduce fracture risk
Drug therapies with antiresorptive action
-romosozumab*
-bisphosphonates
-SERMs
-calcitonin
-Estrogen replacement therapy (ERT)
-RANK ligand inhibitor
Anabolic action of osteoporosis drug therapy
-stimulate bone formation
-inc bone mass
-reduce frac risk
Osteoporosis drug therapies with anabolic action
-Romosozumab*
-Parathyroid hormones (teriparatide, abaloparatide)
Bisphonates products
-Alendronate (Fosamax)
-Risedronate (Actonel)
-Ibandronate (Boniva)
-Zoledronic acid (Reclast)
Bisphonates use
-treatment/prevention of POSTmenopausal osteoporosis
-treatment of osteoporosis to inc bone mass in males
-treatment of glucocorticoid-induced osteoporosis in males and females
Bisphosphonates contraindications
-hypocalcemia
-renal insufficiency
-esophageal abnormalities (except IV formulations)
-inability to sit/stand for at least 30 min (at least 60 min)
-avoid alendronate oral solution in patients at risk for aspiration
-avoid oral after bariatic surgery
-pregnancy or breast feeding (IV zoledronic acid)
Absorption of Bisphosphates
-reduced w coffe/joice
-reduced before breakfast
-reduced taken during breakfast
Metabolism of Bisphosphates
-does not affect hepatic CYP 450 system
Elimination of Bisphosphates
-50% bone
-50% renal
->10 year half life in bone
Adverse effects of oral bisphosphonates
-esophogeal irritation/ulceration
-ab pain
-musculoskeletal pain
-headache
-nausea
-thigh fracture
-occular inflammation
-aFib
-esophogeal cancer?
-osteonecrosis of the jaw
Osteonecrosis of the jaw
-necrotic maxillary bone and sequestrum formation
Bisphosphonates counseling
-must be taken on empty stomach 1st thing in the morning
-take delayed release after breakfast
-Full glass of water for tablet
-do not lie down at least 30 minutes after ingestion and until after first food of day (60 min for ibandronate)
-wait at least 30 min before eating, drinking, taking other meds (60 for ibandronate)
-avoid minaeral water w high calcium
-do NOT chew
discontinue bisphosphonate use if
-dysphagia (trouble swallowing)
-odynophagia (painful swallowing)
-retrosternal pain
-heartburn
Oral Bisphosphonate drug interations
-chelates w multivalent cations (Al, Ca, Fe, Mg)
-antacids
-mineral supplements
-vitamins
-osmotic laxatives (not magaldrate or sodium bicarbonate tho
-also inc GI side effects w NSAIDs
Bisphosphonate dosing
Menopausal Hormone Therapy for osteoporosis recommended for
-prevention of postmenopausal osteoporosis for women with SIGNIFICANT RISK
SERMs for osteoporosis
-Raloxifene
-Bazedoxifene + conjugated estrogens
Raloxifene use
-SERM
-prevent/treat postmenopausal osteoporosis
-breast cancer prophylaxis for postmenopausal women at high risk
Bazedoxifene + conjugated estrogen (Duavee) use
-SERM
-prevention of osteoporosis in women w a UTERUS
SERM contraindications
-active or past history of venous thromboembolic events
-pregnancy/lactating
Raloxifene BLACK BOX warning
-inc risk of deep vein thrombosis and pulmonary embolism
-inc risk of stroke
Raloxifene common side effects
-host flashes
-leg cramps
-weight gain
-peripheral edema
SERM mech of action on hypothalamus
-act as antiestrogens
-disrupts thermoregulation
=hot flashes