Musculoskeletal Flashcards
Calcipotriene (calcipotriol), calcitriol, and tacalcitol
Bind to and activate vitamin D receptor (nuclear transcription factor)
Causes inhibition of keratinocyte proliferation and stimulation of keratinocyte differentiation
Inhibits T cell proliferation and other inflammatory mediators
Used in psoriasis
Vemurafenib
RAF kinase inhibitor used in melanoma patients with BRAF V600E mutation
Leukotrienes
Bronchoconstriction, vasoconstriction, contraction of smooth muscle, and increase vascular permeability
Inhibited by zafirlukast
Prostacyclin
Decrease platelet aggregation, decrease vascular tone, decrease bronchial tone, decrease uterine tone
Damaged endothelial cells lose ability to produce prostacyclin predisposing to thrombi and hemostasis
Synthetic used in pulmonary hypertension, peripheral vascular disease, and Raynaud syndrome
Prostaglandins
Increase uterine tone
Decrease bronchial tone
Inhibited by NSAIDS, ACETAMINOPHEN and cox-2 inhibitors
Thromboxane
Increase platelet aggregation
Increase vascular tone
Increase bronchial tone
Inhibited by NSAIDS, ACETAMINOPHEN and cox-2 inhibitors
NSAIDs
Ibuprofen, naproxen, Indomethacin, ketorolac, diclofenac
MOA: reversibly inhibit COX-1 and COX-2 block prostaglandin synthesis
Clinical: antipyretic, analgesic, anti-inflammatory,
Indomethacin used to close PDA
Acute gout
Toxicity: interdigital nephritis, gastric ulcer, renal ischemia,
Celecoxib
Selective COX-2 inhibitor
Found in inflammatory cells and vascular endothelium
Maintains gastric mucosa
Spares platelet function
Clinical: rhematoid arthritis, and osteoarthrits
Toxicity: increase risk of thrombosis and sulfa allergy
Acetaminophen
Reversibly inhibits cyclooxygenase In CNS
Clinical: antipyretic, analgesics, but not anti inflammatory
Used in children with viral infection
Toxicity: hepatic necrosis (overdose)
Metabolite depletes glutathione and forms toxic tissue
N-acetylacysteine is antidote
Bisphosphonates
Alendronate -donates
MOA: pyrophosphate analog. Binds hydroxyapatite in bone inhibiting osteoclasts
Clinical: osteoporosis, hypercalcemia, Paget disease
Toxicity: corrosive esophagitis (remain upright and drink water for 30 mins), osteonecrosis of jaw
Allopurinol
MOA: inhibits Xanthine oxidase
Decreases conversion of xanthine to uric acid
Clinical: Gout, lymphoma and leukemia to prevent tumor lysis syndrome associated with urate nephropathy
AE: increased concentrations of azothioprine and 6-MP (normally metabolized by xanthine oxidase)
Do not give salicylates
Febuxostat
Inhibits Xanthine oxidase
Chronic gout
Probenicid
Inhibits reabsorption of uric acid in proximal convoluted tubule
Chronic gout
Colcichine
MOA: binds and stabilizes Tubulin and inhibits microtubule polymerization
Impairs leukocyte chemotaxis and degranulation
Acute and prophylactic gout, used with renal failure and or peptic ulcer disease
AE: diarrhea nausea vomiting
Etanercept
MOA: fusion protein produced by recombinant DNA
Receptor for TNF-a and IgG Fc
Decoy receptor for TNF-a
Clinical: rheumatoid arthritis, psoriasis, ankylosing spomdolytis
AE: immunosuppression including reactivation of TB