PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
probenecid

2D structure

Overview

Trade Names: Apurina; Benecid; Benemid; Benuryl; Col-Probenecid; Colbenemid; Polycillin-PRB; Probalan; Probampacin; Probecid; Proben; Proben-C; Probenecid Acid; Probenemid; Probexin; Prolongine; Synergid R; Tubophan; Uricosid
PharmGKB Accession Id: PA451106

Description

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. PubChem (source: Drug Bank)

Indication

For the treatment of gout and high levels of uric acid in the blood (source: Drug Bank)

ATC Therapeutic Category

  • M04AB:Preparations increasing uric acid excretion

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Probenecid inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. (source: Drug Bank)

Pharmacology

Probenecid is a uricosuric and renal tubular blocking agent and is used in combination with colchicine to treat chronic gouty arthritis when complicated by frequent, recurrent acute attacks of gout. It inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Effective uricosuria reduces the miscible urate pool, retards urate deposition, and promotes resorption of urate deposits. (source: Drug Bank)

Food Interactions

Increase liquid intake, avoid alcohol.
Take with food to reduce irritation. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Protein Binding

75-95% (source: Drug Bank)

Isomeric SMILES Code:

CCCN(CCC)S(=O)(=O)c1ccc(cc1)C(=O)O (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ABCC1
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SLC22A11
  •   
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SLC22A6
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
SLC22A8
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SLC22A9
  •   
  •   
  •   
  • FA
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ABCC1 Uncurated Annotation (source: Drug Bank)
ALB Uncurated Annotation (source: Drug Bank)
SLC22A8 Uncurated Annotation (source: Drug Bank)
SLC22A11 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
ezetimibe
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
oseltamivir
  •   
  •   
  •   
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
aspirin Uncurated Annotation The salicylate decreases the uricosuric effect of probenecid (source: Drug Bank)
cefadroxil Uncurated Annotation Probenecid increases the antibiotic's level (source: Drug Bank)
cefamandole Uncurated Annotation Probenecid increases the antibiotic's level (source: Drug Bank)
cefazolin Uncurated Annotation Probenecid increases the antibiotic's level (source: Drug Bank)
cefotaxime Uncurated Annotation Probenecid increases the antibiotic's level (source: Drug Bank)
cefoxitin Uncurated Annotation Probenecid increases the antibiotic's level (source: Drug Bank)
cefradine Uncurated Annotation Probenecid increases the antibiotic's level (source: Drug Bank)
cefuroxime Uncurated Annotation Probenecid increases the antibiotic's level (source: Drug Bank)
cephalexin Uncurated Annotation Probenecid increases the antibiotic's level (source: Drug Bank)
diflunisal Uncurated Annotation Probenecid increases toxicity of diflunisal (source: Drug Bank)
ganciclovir Uncurated Annotation Probenecid increases the effect and toxicity of ganciclovir/valganciclovir (source: Drug Bank)
indomethacin Uncurated Annotation Probenecid increases the effect/toxicity of indomethacin (source: Drug Bank)
ketorolac Uncurated Annotation Probenecid increases toxicity of ketorolac (source: Drug Bank)
methotrexate Uncurated Annotation Probenecid increases the effect and toxicity of methotrexate (source: Drug Bank)
salicylate-magnesium Uncurated Annotation The salicylate decreases the uricosuric effect of probenecid (source: Drug Bank)
salicylate-sodium Uncurated Annotation The salicylate decreases the uricosuric effect of probenecid (source: Drug Bank)
valganciclovir Uncurated Annotation Probenecid increases the effect and toxicity of ganciclovir/valganciclovir (source: Drug Bank)
zidovudine Uncurated Annotation Rash, malaise, myalgia (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Influenza, Human
  •   
  •   
  • PK
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Leukemia
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Leukemia, Myeloid
  • CO
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Leukemia, Myeloid, Acute
  • CO
  •   
  •   
  • FA
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Neoplasms
  • CO
  •   
  •   
  • FA
  •   
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Curated Phenotype Datasets

These datasets are sorted alphabetically by title.

  1. SLC22A6 Functional Protein Variants
    • Genotype data available
    • Phenotype data available
    • No literature annotations
    • Not annotated
    • FA
    Submitted by Kathleen M. Giacomini, PhD involving SLC22A6, , aminohippurate, methotrexate, ochratoxin A and probenecid

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Physicochemical determinants of human renal clearance
  2. The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease

Downloads

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LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01032
KEGG Compound ID:
C07372
KEGG Drug ID:
D00475
PubChem Compound ID:
4911
PubChem Substance ID:
9576

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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