Osteoporosis and Gout Drugs (Wolff) Flashcards
What are the category of drugs used to treat osteoporosis?
Calcium salts
Vitamin D
Calcitonin
PTH
Bisphonates
SERMS
RANKL inhibitor
What are the two forms of Vitamin D?
ergocalciferol (D2) - plants
cholecalciferol (D3) - sunlight
What is the calcitonin agent used to treat osteoporosis?
calcitonin-salmon
What is the parathyroid hormone analog used to treat osteoporosis?
teriparatide
What are the bisphosphonates used to treat osteoporosis?
alendronate and other “drenate’s”
zoledronic acid (IV once a year) - avoids GI probs (esophagitis)
What is the one SERM agent used to treat osteoporosis?
raloxifene
What is the one RANKL inhibitor used to treat osteoporosis?
denosumab
Calcium salts in the treatment of osteoporosis?
mild hypocalcemia (oral calcium salts)
severe hypocalcemia (parenteral calcium salts)
toxicity - constipation, lethargy and kidney stones
Too much calcium intake via calcium salt treatment can result in what side effects?
constipation, lethargy and kidney stones
ergocalciferol
Vitamin D2 - found in plants
cholecalciferol
Vitamin D3 - sunlight
calcitonin-salmon
calcitonin agent used to treat established osteoporosis (NOT PREVENTION); longer half life than human calcitonin; intranasal spray; very safe
alendronate
bisphosphonates used to treat osteoporosis; DRUG OF CHOICE; inhibits bone resorption; can cause esophagitis (prevent by waiting 30 mins before any liquids or food); can cause osteonecrosis of the jaw and atypical femur fractures
What are some side effects of alendronate?
esophagitis (prevent by waiting 30 mins before any liquids or food); can cause osteonecrosis of the jaw and atypical femur fractures
What is the drug of choice for osteoporosis?
alendronate; inhibits bone resorption
osteonecrosis of the jaw; commonly caused by bisphosphonates (alendronate) used to treat osteoporosis
atypical femur fracture; commonly caused by bisphosphonates (alendronate) used to treat osteoporosis
raloxifene
SERM; blocks estrogen receptors in the breast and uterus but agonist to receptors in the bone; also reduces the risk of estrogen dependent breast cancer; risk for DVT, PE and stroke; contraindicated in pregnancy (fetal death)
Which drug used to osteoporosis also has some benefit to reduce the risk of developing estrogen dependent breast cancer?
raloxifene; SERM; blocks estrogen receptors in the breast and uterus but agonist to receptors in the bone
teriparatide
truncated parathyroid hormone analog used to treat osteoporosis; ONLY drug for osteoporosis that increases bone formation; given in pulsed therapy (continuously given will cause osteoclast to predominate = worsen OA); add once daily and generally well tolerated
What is the ONLY drug for osteoporosis that increases bone formation?
teriparatide; truncated parathyroid hormone analog
How is teriparatide administered and why?
given in pulsed therapy (continuously given will cause osteoclast to predominate = worsen OA)
denosumab
monoclonal antibody RANKL inhibitor used to treat osteoporosis; decreases the formation of functional osteoclasts; should be taken with calcium and Vitamin D; injected every 6 months; found to delay fracture healing and increases risk of new fractures and osteonecrosis of the jaw
What does RANKL stand for?
Receptor activator of nuclear factor kappaB ligand (RANKL)
What are the adverse effects of denosumab?
delay fracture healing and increases risk of new fractures and osteonecrosis of the jaw
Treatment for osteoporosis in men?
testosterone replacement (hypogonadism)
glucocorticoids and androgen-deprivation therapy (decrease prostate cancer risk)
bisphophonates are the agent of choice
Cinacalcet
a calcimimetic drugs used to primary hyperparathyroidism and secondary hyperparathyroidism due to CKD (unable to eliminate phosphate = hypocalcemia = increased PTH = bone resorption); most common side effect is n/v and diarrhea
What is the drug used to treat secondary hyperparathyroidism due to CKD?
Cinacalcet; a calcimimetic drugs; (unable to eliminate phosphate = hypocalcemia = increased PTH = bone resorption); most common side effect is n/v and diarrhea
What are the category of drugs used to treat gout?
NSAIDs
Glucocorticoids
Xanthine oxidase inhibitors
Recombinant uricase
Microtubule formation disrupter
Uricosurics
What are the 3 NSAIDs used to treat gout?
naproxen (non-selective)
indomethacin (COX 1 > COX 2)
celecoxib (COX 2)
What are the 3 glucocorticoids used to treat gout?
betamethasone
methylprednisone
triamcinolone
What is the one microtubule formation disrupter used to treat gout?
colchicine
What are the two xanthine oxidase inhibitors used to treat gout?
allopurinol (competitive inhibitor)
febuxostat (non-competitive inhibitor)
What are the two recombinant uricase agents used to treat gout?
“case”
pegloticase
rasburicase (also used in high-risk lymphoma)
What are the two uricosuric agents used to treat gout?
probenecid
sulfinpyrazone
How does alcohol affect gout?
alcohol increases purine synthesis which then increases the rate concentration in the plasma (worsens gout symptoms)
Drugs used to increase uric acid renal excretion in recurrent gout?
uricosuric agents; probenecid and sulfinpyrazone
Drugs used to reduce uric acid renal production in recurrent gout?
xanthine oxidase inhibitors (allopurinol and febuxostat)
recombinant uricase agents “case’s” (pegloticase and rasburicase)
colchicine
microtubule formation disrupter used to treat gout; blocks formation of MTs (inhibits movement of inflammatory cells); contraindicated in renal and hepatic impairments; adverse effects of GI symptoms n/v and diarrhea
colchicine is contraindicated in which patients?
contraindicated in patients with renal and hepatic impairments
allopurinol
competitive xanthine oxidase inhibitors used to treat gout; hypoxanthine and xanthine are excreted; toxicity can cause a skin rash, a severe hypersensitivity reaction (fatal); there is increased risk if patient is HLA-B 5801 positive
allopurinol toxicities
skin rash, a severe hypersensitivity reaction (fatal); there is increased risk if patient is HLA-B 5801 positive
severe skin rash seen in allopurinol toxicity
febuxostat
non-competitive xanthine oxidase inhibitor used to treat gout; hypoxanthine and xanthine are excreted; used in those who cannot tolerate allopurinol; generally well tolerated but has been seen to have increased CV death
febuxostat toxicity
generally well tolerated but has been seen to have increased CV death
pegloticase
recombinant uricase agents used to treat gout; converts uric acid to allantoin (more soluble); watch for infusion reactions (VERY EXPENSIVE)
Which gout drug works by converting uric acid into allantoin (a more soluble compound)?
pegloticase; a recombinant uricase agent; (VERY EXPENSIVE)
probenecid
uricosuric agent used to treat gout; blocks rate of reabsorption more than of rate secretion; CANNOT BE USED IN OVERPRODUCERS!!; GFR > 60 ml/min and no kidney stones; is a sulfa drug (watch for hypersensitivity)
probenecid cannot be used in what patient populations?
CANNOT BE USED IN OVERPRODUCERS!!; GFR > 60 ml/min and no kidney stone
