Gout drugs Flashcards
NSAIDs
MOA: COX inhibition so less PGs + inhibit phagocytosis of urate crystals
Decrease gouty infl. with pain relief
Use: 1st line in acute gout attack; consider celecoxib in pts with GI issues
AE:
GI: gastritis, n/v, ulcers
Renal: renal insuff., papillary necrosis
CV: fluid retention, HTN, edema (Celecoxib increases risk of thrombotic events)
CNS: HA, dizziness
Contraindicated in: PUD, CHF, HTN, renal dz
Colchicine
MOA: inhibits tubulin polymerization into microtubles + inhibits action of PMN leukocytes and mononuclear macrophages
Decrease gouty infl with pain resolution
Use: 2nd line in acute flare (NSAIDs are a no-go)
AE:
GI: n/v, abdominal pain, diarrhea
TOX: bloody diarrhea, burning throat pain, hematuria, oliguria, neutropenia, axonal neuromyopathy
Corticosteroids
GC-R binding to regulate gene transcription, affect distribution and function of leukocytes, suppress infl. cytokines and chemokines
Decrease gouty infl with pain resolution
Use: acute attack with contraindications to NSAIDs and colchicine, prednisone 5-10dd PO; triamcinolone is for joint injection
AE: well tolerated if short, CI in: DM, GI dz, CV dz, psych dz
Allopurinol and febuxostat
Irrev inhib of XO; allopurinol is a purine analog converted to alloxanthine in a suicide rxn; febuxostat is a non-purine inhib. lower urate production!
USE: 1st line in intercritical gout therapy (chronic)
For: chronic tophaceous gout, 24hr urinary urate >1.1g, stones, renal dz
AE:
Initial flares: so give with acute therapy
GI: diarrhea, n/v
Allopurinol only: skin severe (SJS-TEN), peripheral neuritis, necrotizing vasculitis, BM suppression, hep tox, AIN, aplastic anemia
Febuxostat: safer!
Probenecid
organic acid that inhibits organic anion transporter (OAT) in PCT by increasing secretion and decreasing resorption of urate
USE: 2nd line for chronic urate lowering tx in toph. gout or in frequent attacks, when XOIs fail or are CIed
AE: GI (give with food)
stone formation; alkalinize urine
start 2-3ww post attack
Lesinurad
URAT1 inhibitor (an OAT) in PCT by increasing secretion and decreasing resorption of urate
ONLY in combo with XOI in people failing monotherapy
AE: HA, flu, heartburn, elev. cr
Nephrotox, esp. as monotherapy (black box)
CI in pts with renal dz
Take with food and plenty of water
Pegloticase
Pegylated recombinant uricase converting urate to allantoin
lowers serum urate
USE: chronic gout refractory to others
Single IV does for 21dd q2ww need good renal fxn
AE: Infusion rxn, start on NSAID/colchicine before giving pegloticase, pretreatment with anti-H or CS to avoid infusion rxn
