Term
|
Definition
-familial metabolic disease
-recurrent episodes of acute arthritis due to inflammation bc of deposits of monossodium urates in joints and cartalidge
-can also lead to deposition of uric acid calculi in kidney
-tophi precipitate in cooler areas of the body |
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|
Term
| gout trophi (uric acid accumulations) often found where? |
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Definition
| toe, foot, elbow, earlobe, scrotum |
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Term
| Colchicine (generic) pharmacokinetics |
|
Definition
microtubule inhibitor
-rapidly absorbed after oral admin
-peak value within 2 hours
-exccreted primarily in feces and 10-20% in urine |
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Term
| Colchicine pharmacodynamics |
|
Definition
-binds to intracellular tubulin, thus prevents polymerization of microtubules, leading to inhibition of leukocyte migration and phagocytosis
-also inhibits synthesis of LTB4, which is implicated as a chemotactic agent |
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Term
| colchicine fda labeled indications |
|
Definition
it is non-analgesic
-treatment of acute gouty arthritis |
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Term
| colchicine non-FDA labeled indications |
|
Definition
| -prophylaxis of recurrent episodes of gouty arthritis |
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Term
| colchicine adverse effects |
|
Definition
-often-diarrhea
-occasionally-nausea, vomitting, and abdominal pain
-rarely- hair loss, bone marrow depression, peripheral neuritis, myopathy |
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|
Term
|
Definition
not used because irreversibly binds..
--? what else? |
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Term
| indomethacin labeled indications |
|
Definition
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|
Term
| uricosuric agents , eg Probenecid, description |
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Definition
| decrease the body pool of uric acid, esp in patients with tophaceous gout |
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|
Term
| Probenecid pharmacokinetics |
|
Definition
completely absorbed by oral admin
-peak concentrations achieved 2 to 4 hours
-t1/2 is dose dependent, varies from 5-8 hours
-85-95% plasma protein bound
-both filtered and actively secreted into forming urine |
|
|
Term
| probenecid pharmacodynamics |
|
Definition
| -decreases the net reabsorption of uric acid |
|
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Term
| probenecid FDA indications |
|
Definition
-therapy should be started 2-3 weeks after an attack
-hyperuricemia; prophylaxis |
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Term
| probenecid adverse effects |
|
Definition
-renal stones-prevention requires maintenance of a large urine volumee
-gastric irritation
-allergic dermititis |
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|
Term
| Uric acid synthesis inhibitor, eg allopurinol, description |
|
Definition
| inhibitor of uric acid synthesis by inhibition of xanthine oxidase |
|
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Term
| Allopurinol (zyloprim) pharmacokinetics |
|
Definition
-about 80% absorbed after oral admin.
-metabolized by xanthine oxidase to alloxanthine, which also inhibits xanthine oxidase |
|
|
Term
| allopurinol pharmacodynamics |
|
Definition
| major source of purines are from "de novo" (not scavenger) synthesis and not from dietary sources |
|
|
Term
| allopurinal fda labeled indications |
|
Definition
-gout
-hyperuricemia--tumor lysis syndrome
-hyperuricemia-thiazide induced
-cancer-hyperuricemia |
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|
Term
| allopurinol adverse effects |
|
Definition
-may exacerbate gouty attacks
-gi intolerance
-peripheral neuritis
-necrotizing vasculitis
-depression of bone marrow element
-rarely- aplastic anemia |
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|
Term
| Febuxostat (Uloric) description |
|
Definition
| newly FDA approved nonpurine inhibitor of xanthine oxidase |
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Term
| Febuxostat pharmacokinetics |
|
Definition
-80% absorbed after oral dose
-t max occues at 1 hour
-exensive hepatic metabolism |
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|
Term
| Febuxostat vs allopurinol |
|
Definition
| feb is more effective than allo in lowering serum uric acid |
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|
Term
|
Definition
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|
Term
| Rasburicase mechanism of action |
|
Definition
-administered by IV
-enzyme taht oxidatelively cinverts uric acid to allantoin and hydrogen peroxide |
|
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Term
|
Definition
| hyperuricemia due to malignancy, in patients with risk for tumor lysis syndrome |
|
|
Term
| rasburicase adverse effects |
|
Definition
-may cause severe hypersensitivity reactions in patients with G6P Gehydrogenase deficiency
-may cause degredation of uric acid in blood samples left at room temp, which would give abnormally low uric acid levels |
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|
Term
| Pegloticase indications and info |
|
Definition
info: recombinant, PEGylated form of uricase
indications: gout refractory to conventional therapy |
|
|
Term
| pegloticase black box warning and contraindication |
|
Definition
-anaphylaxis and infusion reaction, discontinue treatment if blood levels of uric acid are greater than 6mg/dL
-GSP Dehydroxgenase deficiencyt--risk of hemolysis and methemoglobinemia |
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Term
|
Definition
--immunosuppressive drug
-at anti-cancer doses is potent immunosuppressive
-at anti-rheumatic doses, action is related to the inhbition of the enzymes and to increased release of adenosine |
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Term
| Methotrexate pharmacokinetics |
|
Definition
| 70% absorbed after oral administration |
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Term
| Methotrexate fda labeled indication |
|
Definition
-sever rheumatoid arthtitis
-juvenile rhem arth, polyarticular course |
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|
Term
| Methotrexate adverse effect |
|
Definition
-nausea
-mucosal ulcers
-frequent progressive dose related hepatoxicity
-rarely cirrhosis
-hypersensitivity lung reaction
-pseudolymphomatous reaction |
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|
Term
| Methotrexate toxicity may be ameliorated by: |
|
Definition
administering leucovorin for weeks prior to the admin
-adminstering leucovorin after each weekly dose
-daily folic acid therapy |
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