Download Drug Name

Drug Name
Mechanism of Action
Pharmacology
Side Effects/Other
NSAIDS
Indomethacin, phenylbutazone
Inhibition of prostaglandin synthesis and
inhibition of urate crystal phagocytosis.
Tx of acute inflammation in gout.
Glucocorticoids
See Glucocorticoid chapter
For the Tx of a few gouty joints, single
glucocorticoid injections may prove
effective.
Other Anti-Inflammatory
Colchicine
It ONLY acts to suppress the inflammatory
process caused by urate crystals. It is antimitotic  binds tubulin preventing
polymerization for motility and secretory
events in neutrophils. It suppresses IL-8
induced neutrophil migration. Also
reduces leukotriene B4
Rapidly absorbed orally, can be IV. See
high levels in kidney, liver, spleen, GI; see
low levels in heart, skeletal muscle, brain.
Metabed by liver, elim in bile and feces.
Generally works within 18 hours
Effective ONLY against gout. Can see GI
irritation  N/V, diarrhea, abd pains
(dose related)  due to ability to suppress
the normally rapid cell turnover of the
intestine. Less often, see renal damage,
muscular weakness, paralysis, blood
dyscrasias, resp. depression.
Involve inhibition of the renal tubular
transport of a variety of weak organic acids
 increases plasma half-life of other drugs
that are weak org acids (ie penicillin).
It blocks active transport mechanisms for
urate reabsorption in the prox tubules at
site B, C and D.
Benzoic acid derivative. Orally active,
bound to plasma proteins, metabed in
liver. Enters renal tubules by weak acidic
transporter in prox tubules, can reduce
secretion of other weak acids.
Used to lower plasma urate levels only in
patients who are underexcretors of urate
(90% of pts with hyperuricemia). Must
increase water water and maintain alkaline
urine (with HCO3-) to minimize precip of
crystals in renal tubules. Can cause GI
irritation, other drug interactions (protein
bound drugs).
Well absorbed orally, rapidly cleared from
plasma with t1/2 1-3hr. Metabed in liver,
excreted in urine.
Used for overproducers and underexcretors. Indicated when high risk of uric acid
stone formation in kidney. Usually drug is
well tolerated, causes some GI irritation,
may see temporary increase in acute gout
attacks. Hypersensitivity rxns and
hepatox are rare. It interferes with 6mercaptopurine (anti-cancer).
Uricosuric Drugs
Probenecid
Inhibitors of Urate Synthesis
Allopurinol
Inhibits urate biosynthesis (structural
analog of hypoxanthine). Inhibits xanthine
oxidase  low levels competitively, at
high levels noncompetetively. Inhibits de
novo and salvage synth of purines.