Rheumatology Book

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UricosuricAka: Probenecid, Sulfapyrazine

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  1. Indication
    1. Rarely used now due to toxicity
      1. Allopurinol used most often for gout prophylaxis
    2. Gout for Uric Acid under-excreter
      1. Indicated for Urine Uric Acid < 700 mg/24h
  2. Mechanism
    1. Increases Uric Acid excretion in Gout
  3. Requirements for use
    1. Age <60 years
    2. Normal Renal Function
    3. No history of renal stone
    4. No overproduction of Uric Acid
  4. Preparations
    1. Use concurrent NSAID or Colchicine when starting
    2. Probenecid (Consider Allopurinol instead)
      1. Dose: 250 mg PO bid
      2. Maximum: 1500 mg PO bid
    3. Sulfapyrazine (Rarely used)
      1. Dose: 50 mg PO bid
      2. Maximum: 100 mg PO bid
  5. Adverse effects
    1. Dermatitis
    2. Cytopenias
    3. Reduces excretion of other drugs (e.g. Penicillin)

Probenecid (C0033209)

Definition (MSH)The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.
Definition (CSP)USP lists as a uricosuric, an agent that promotes uric acid secretion in urine.
Definition (NCI)A substance that is being studied as a treatment for cancer. It belongs to the family of drugs called antibiotic therapy adjuncts.
Definition (PDQ)A benzoic acid derivative with antihyperuricemic property. Probenecid competitively inhibits the active reabsorption of urate at the proximal tubule in the kidney thereby increasing urinary excretion of uric acid and lowering serum urate concentrations. This prevents urate deposition and promotes resolution of existing urate deposits. In addition, probenecid modulates the transport of organic acids and acidic drugs at the proximal and distal renal tubule, thereby increasing the drug serum concentration. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40223&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=40223&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C772" NCI Thesaurus)
Definition (NCI)A benzoic acid derivative with antihyperuricemic property. Probenecid competitively inhibits the active reabsorption of urate at the proximal tubule in the kidney thereby increasing urinary excretion of uric acid and lowering serum urate concentrations. This prevents urate deposition and promotes resolution of existing urate deposits. In addition, probenecid modulates the transport of organic acids and acidic drugs at the proximal and distal renal tubule, thereby increasing the drug serum concentration.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
EnglishMajor Brand of Probenecid, Martec Brand of Probenecid, Parmed Brand of Probenecid, PROB, Probenecid, Probenecid Major Brand, Probenecid Martec Brand, Probenecid Parmed Brand, PROBENECID PREPARATION, Probenecid Zenith Brand, Zenith Brand of Probenecid
Spanishprobenecid
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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