II. 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

III. Mechanism

  1. Increases Uric Acid excretion in Gout

IV. Indications: Requirements for use

  1. Age <60 years
  2. Normal Renal Function
  3. No history of renal stone
  4. No overproduction of Uric Acid

V. 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
  4. Lesinurad (Zurampic)
    1. Dose: 200 mg orally each morning
    2. Risk of Acute Renal Failure (should not be used as Uric Acid monotherapy)
    3. Must be taken with Xanthine Oxidase Inhibitor (Allopurinol or Febuxostat)
      1. Allopurinol dose must be at least 300 mg/day (at least 200 if CrCl <60 ml/min)
    4. Available as Duzallo (Allopurinol with Lesinurad)
      1. As of 2017, costs $12/day (compared with $3/day for Allopurinol and probenacid)
    5. (2017) Presc Lett 24(11): 64

VI. Adverse effects

  1. Dermatitis
  2. Cytopenias
  3. Reduces excretion of other drugs (e.g. Penicillin)

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Cost: Medications

probenecid (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
PROBENECID 500 MG TABLET Generic $0.49 each
PROBENECID-COLCHICINE TABS Generic $0.75 each

Ontology: Probenecid (C0033209)

Definition (NCI_NCI-GLOSS) A drug that is used to treat gout and is used together with some antibiotics to make them work better. It is being studied in the treatment of cancer. It belongs to the family of drugs called antibiotic therapy adjuncts.
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.
Definition (CSP) USP lists as a uricosuric, an agent that promotes uric acid secretion in urine.
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 (PSY) Agent that promotes the urinary excretion of uric acid.
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)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D011339
SnomedCT 387365004, 66094001
LNC LP16260-9, MTHU007603
English probenecid, Benzoic acid, 4-((dipropylamino)sulfonyl)-, Major Brand of Probenecid, Martec Brand of Probenecid, Parmed Brand of Probenecid, Probenecid Major Brand, Probenecid Martec Brand, Probenecid Parmed Brand, Probenecid Zenith Brand, Zenith Brand of Probenecid, PROB, probenecid (medication), Probenecid [Chemical/Ingredient], PROBENECID, Probenecid (product), Probenecid (substance), Probenecid
Swedish Probenecid
Czech probenecid
Finnish Probenesidi
Russian PROBENETSID, PROBETSID, ПРОБЕНЕЦИД, ПРОБЕЦИД
Japanese プロベネシッド, プロベシド, プロベネシド
Spanish Probenecid, Probenecida, probenecid (producto), probenecid (sustancia), probenecid
Polish Probenecyd
French Probénécide
German Probenecid
Italian Probenecid
Portuguese Probenecid

Ontology: Uricosuric Agents (C0041983)

Definition (MSH) Gout suppressants that act directly on the renal tubule to increase the excretion of uric acid, thus reducing its concentrations in plasma.
Concepts Pharmacologic Substance (T121)
MSH D014528
SnomedCT 371344006, 372758007, 49157004
English Agents, Uricosuric, Uricosuric Agents, uricosuric agents, Uricosuric product (product), Uricosuric agent, Uricosuric agent (substance), Uricosuric agent (product), Uricosuric product, uricosuric agent, Uricosuric agent, NOS, Hyperuricaemia Agents, Uricosuric Agent
French Médicaments uricosuriques, Agents uricosuriques, Uricosuriques
Swedish Utsöndring av urinsyra, medel för
Czech urikosurika
Finnish Urikosuurisesti vaikuttavat aineet
Russian MOCHEVOI KISLOTY VYVEDENIE, LEKARSTVENNYE SREDSTVA, SREDSTVA, SNIZHAIUSHCHIE KONTSENTRATSIIU MOCHEVOI KISLOTY, МОЧЕВОЙ КИСЛОТЫ ВЫВЕДЕНИЕ, ЛЕКАРСТВЕННЫЕ СРЕДСТВА, СРЕДСТВА, СНИЖАЮЩИЕ КОНЦЕНТРАЦИЮ МОЧЕВОЙ КИСЛОТЫ
Polish Leki moczanopędne
Portuguese Uricosúricos, Agentes Uricúricos, Agentes Uricosúricos, Uricúricos
Spanish Uricosúricos, producto con agente uricosúrico, producto con agente uricosúrico (producto), Agentes Uricosúricos, agente uricosúrico (sustancia), agente uricosúrico, agente uricosúrico (producto)
German Urikosurika
Italian Preparati favorenti l'escrezione di acido urico