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1 Gout
Scammell
43
Pharmacology
Graduate
04/26/2010

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Term
what is gout?
Definition
metabolic disease a/w recurrent episodes of acute arthritis due to deposits of monosodium urate in joints and cartilage
Term
gout is a/w deposits of what?
Definition
monosodium urate in joints and cartilage
Term
gout is usually a/w high serum levels of what?
Definition
uric acid - the major end product of purine metabolism
Term
what cell makes synovial fluid?
Definition
synoviocytes
Term
what happens to urate crystals in the joint space?
Definition
phagocytosed by synoviocytes
Term
when synoviocytes phagocytose urate crystals that stimulates them to do what?
Definition
secrete PGE --> amplifies the inflammatory response
Term
how is the inflammatory response in the joints amplified in gout?
Definition
1. synoviocytes secrete PGE after they phagocytose urate crystals
2. PMN leukocytes migrate to joint space
3. macrophages ingest urate crystals --> then release more inflammatory factors
Term
how do anti-inflammatory agents work in the treatment of gout?
Definition
1. relieve pain of acute gouty attack
2. prevent recurrent episodes
Term
what drugs are used to relieve pain of acute gouty attack and prevent recurrent episodes?
Definition
NSAIDs and corticosteroids
Term
what anti-inflammatory drugs are used in the treatment of gout?
Definition
NSAIDs and corticosteroids
Term
mechanism of action of indomethacin as treatment for gout?
Definition
inhibits PGE synthesis and urate crystal phagocytosis
Term
3 NSAIDs used to treat gout?
Definition
1. indomethacin
2. naproxen
3. etoricoxib
Term
what is a selective COX-2 inhibitor used in the treatment of gout?
Definition
etoricoxib
Term
mechanism of action of corticosteroids in the treatment of gout?
Definition
1. reduce the production of inflammatory mediators
2. inhibit COX and PLA2 --> inhibits production of arachadonic acid (precursor to PGE and leukotrienes)
Term
administration of corticosteroids for treatment of gout?
Definition
oral --> can lead to systemic side effects

poor local injection for single joint involvement --> less systemic side effects
Term
2 corticosteroids used for treatment of gout?
Definition
1. prednisone
2. methylprednisolosone
Term
what is colchicine?
Definition
an alkaloid isolated from autumn locus
Term
administration of colchicine?
Definition
readily absorbed orally; often used IV
Term
how is colchicine effective in treating gout?
Definition
dramatically relieves pain and inflammation
Term
mechanism of colchicine?
Definition
1. binds tubulin --> prevents polymerization into tubules
2. inhibits leukocyte migration and pro-inflammatory agents release (like PGE)
Term
why is colchicine now a 2nd line drug?
Definition
it is very effective but diarrhea is a common side effect that limits use
Term
what side effect of colchicine limits its use?
Definition
diarrhea
Term
colchicine is a substrate for what?
Definition
CYP3A4 and P-glycoprotein efflux transporter
Term
when can colchicine have fatal toxicities and why?
Definition
when the patient is also taking clarithromycin or cyclosporine

they are also substrates or block the same transporters and the amount of colchicine can reach toxic levels
Term
mechanism of probenecid and sulfinpyrazone?
Definition
enhance uric acid excretion by inhibiting renal reabsorption
Term
what usually happens to excreted uric acid?
Definition
reabsorbed in the proximal tubule of the kidney
Term
what must be maintained with use of probenecid and sulfinpyrazone?
Definition
urine volume
Term
patients taking probenecid and sulfinpyrazone are at increased risk for what?
Definition
urate nephrolithiasis
Term
probenecid and sulfinpyrazone are contraindicated in who?
Definition
individuals with kidney stones
Term
will probenecid and sulfinpyrazone alter the course of a gouty attack?
Definition
NO
Term
how long do probenecid and sulfinpyrazone take to be effective?
Definition
2-3 weeks
Term
2 xanthine oxidase inhibitors?
Definition
1. allopurinol
2. febuxostat
Term
mechanism of allopurinol and febuxostat?
Definition
lower serum uric acid by inhibiting xanthine oxidase enzyme
Term
xanthine oxidase inhibitors are effective how in the treatment of gout?
Definition
in preventing recurrence of acute gouty arthritis and treating urate nephrolithiases (uric acid kidney stones)
Term
how are xanthine oxidase inhibitors used in the treatment of gout?
Definition
not helpful short term --> used in long term therapy
Term
when are xanthine oxidase inhibitors used in the treatment of gout?
Definition
1. patients with high urine uric acid levels
2. impaired kidney function
3. allergies to probenecid or sulfapyrazone (S containing)
Term
adverse effects of xanthine oxidase inhibitors?
Definition
1. hypersensitivity reactions
2. liver enzyme abnormalities
Term
allopurinol can have significant drug interaction with what drug?
Definition
6-mercaptopurine - immunomodulator used in treatment of IBD
Term
6-mercaptopurine is normally inactivated by what?
Definition
xanthine oxidase
Term
what happens when allopurinol and 6-mercaptopurine are given together?
Definition
increased levels of 6-mercaptopurine can lead to very serious leukopenia
Term
synthesis of uric acid?
Definition
its synthesized from xanthine by xanthine oxidase
Term
what must be done when give allopurinol with 6-mercaptopurine?
Definition
dose of 6-mercaptopurine has to reduced >50%
Term
Uncle Bob has recently found out that he has gout. He also as diabetes and has been told that his kidney function isn’t stellar. After initial treatment with indomethacin, he has been placed long-term on a drug that does not require fully functioning kidneys. This drug is most likely:

a. Uric acid
b. Allopurinol
c. Probenicid
d. Propranolol
Definition
b. Allopurinol
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