MSK Drugs (Not including anti-inflammatories) Flashcards
Name the bisphosphonates
alendronate, other “-dronates”
Mechanism of bisphosphonates
pyrophosphate analogs
bind hydroxyapatite in bone, inhibiting osteoclast activity
Use of bisphosphonates
osteoporosis
hypercalcemia
Paget disease of bone
Toxicity of bisphosphonates
corrosive esophagitis (pts advised to take with water and remain upright for 30 minutes) osteonecrosis of jaw
Mechanism of teriparatide
recombinant PTH analog given subcutaneously daily –> increased osteoblastic activity
Use of teriparatide
osteoporosis
causes increased bone growth compared to antiresportive therapies (bisphosphonates)
Toxicity of teriparatide
transient hypercalcemia
may increase risk of osteosarcoma
Name the acute gout drugs
NSAIDs (naproxen, indomethacin)
Glucocorticoids (oral and intra-articular)
Colchicine
Mechanism of colchicine
binds and stabilizes tubulin to inhibit MT polymerization, impairing neutrophil chemotaxis and degranulation
Use of colchicine
acute and prophylactic value for gout
Toxicity of colchicine
GI side effects
Why not give salicylates in gout?
all doses but the HIGHEST dose depress uric acid clearance
even highest doses have only minor uricosuric activity
Name the chronic gout drugs (preventative
allopurinol, febuxostat, pegloticase, probenecid
Mechanism of allopurinol
inhibits xanthine oxidase after being converted to alloxanthine
decreases conversion of xanthine to uric acid
Use of allopurinol
gout prevention/chronic tx
Use of allopurinol in leukemia and lymphoma
to prevent tumor lysis-associated urate nephropathy
Mechanism of febuxostat
inhibits xanthine oxidase
Name the two antimetabolite drugs that need to be careful of dosing when using allopurinol/febuxostat
azathioprine and 6-mercaptopurine (6-MP)
because normally metabolized by xanthine oxidase
Mechanism of pegloticase
recombinant uricase that catalyzes metabolism of uric acid to allantoin (more water soluble product)
Mechanism of probenecid
inhibits reabsorption of uric acid in proximal convoluted tubule (also inhibits secretion of penicillin)
can precipitate uric acid calculi
NEED TO HAVE PRISTINE KIDNEYS TO USE
What do need to check before starting TNF-alpha inhibitor?
TB status because using TNF-alpha inhibitors could predispose to infection by reactivating latent TB
TNF-alpha is important in granuloma formation and stabilization
Mechanism of etanercept
fusion protein (receptor for TNF-alpha and IgG1 Fc receptor), produced by recombinant DNA
Use of etanercept
RA
psoriasis
ankylosing spondylitis
Mechanism of infliximab/adalimumab
anti-TNF-alpha monoclonal antibodies
Use of infliximab/adalimumab
IBD
RA
ankylosing spondylitis
psoriasis
