Overview
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.
Indication
For the reduction of serum uric acid concentrations in chronic gouty arthritis and tophaceous gout in patients with frequent disabling gout attacks. Has also been effectively used to promote uric acid excretion in hyperuricemia secondary to the administration of thiazide and related diuretics.
Associated Conditions
- Bacterial Infections
- Chronic Gouty Arthritis
- Elevated Serum Uric Acid
- Gout Chronic
- Hyperuricemia
- Infection
Research Report
A Comprehensive Monograph on Probenecid (DB01032): Pharmacology, Clinical Utility, and Safety Profile
Executive Summary
Probenecid is a small molecule drug classified as a prototypical uricosuric and renal tubular blocking agent. A sulfonamide derivative, its development was initially driven by the need to extend the therapeutic efficacy of limited penicillin supplies during World War II by inhibiting the antibiotic's renal excretion.[1] This dual-action profile defines its modern clinical utility. Probenecid is primarily indicated for the long-term management of hyperuricemia associated with chronic gout and gouty arthritis, where it promotes the excretion of uric acid.[3] Concurrently, it serves as an adjuvant to therapy with certain β-lactam antibiotics and other medications, elevating their plasma concentrations to enhance therapeutic effects.[5] The pharmacological basis for these actions is its competitive inhibition of organic anion transporters (OATs) in the renal tubules, which simultaneously blocks the reabsorption of urate and the secretion of various acidic drugs.[7] While effective, its use is complicated by a significant potential for drug-drug interactions stemming from this mechanism and a notable risk of promoting uric acid nephrolithiasis, which necessitates specific patient management strategies.[2] This report provides a comprehensive examination of Probenecid's chemical properties, pharmacological profile, clinical applications, and safety considerations.
Chemical Identity and Physicochemical Properties
The precise identification and characterization of Probenecid's chemical and physical properties are fundamental to understanding its formulation, biological activity, and disposition within the body.
Nomenclature and Identifiers
Probenecid is recognized across scientific and regulatory domains by a variety of names and unique identifiers.
Clinical Trials
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Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2022/03/15 | Phase 1 | UNKNOWN | |||
2021/10/19 | Phase 1 | Completed | |||
2021/09/16 | Phase 1 | Completed | CSPC ZhongQi Pharmaceutical Technology Co., Ltd. | ||
2021/06/25 | Phase 2 | Recruiting | |||
2021/02/10 | N/A | Active, not recruiting | |||
2020/09/16 | Phase 2 | Recruiting | |||
2019/05/29 | Phase 4 | Completed | |||
2019/05/03 | Phase 1 | Completed | |||
2019/01/11 | Phase 1 | Completed | |||
2018/03/15 | Phase 1 | Completed |
FDA Drug Approvals
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Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Rising Pharma Holdings, Inc. | 16571-831 | ORAL | 500 mg in 1 1 | 11/28/2023 | |
| Aphena Pharma Solutions - Tennessee, LLC | 43353-839 | ORAL | 500 mg in 1 1 | 5/28/2014 | |
| Medstone Pharma LLC | 71626-999 | ORAL | 500 mg in 1 1 | 2/12/2021 | |
| Quality Care Products, LLC | 83008-020 | ORAL | 500 mg in 1 1 | 5/24/2023 | |
| Westminster Pharmaceuticals, LLC | 69367-154 | ORAL | 500 mg in 1 1 | 7/27/2016 |
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