Probenecid Medications
Probenecid is a uricosuric medication used to lower uric acid levels in the blood for treating gout and preventing related complications by enhancing its urinary excretion.
Probenecid Information
Probenecid is a uricosuric agent that increases the renal excretion of uric acid and, secondarily, blocks the tubular secretion of several β-lactam antibiotics. First approved in the late -s for gout management, it has since become indispensable for clinicians who need to boost plasma levels of drugs such as ampicillin, amoxicillin, and ceftriaxone. Marketed under brand names like Benemid and Prouric, the molecule is also available as a generic, making it a cost-effective option for many patients. Beyond its primary role in hyperuricemia, probenecid is occasionally prescribed off-label to enhance antibiotic therapy in difficult infections, although such uses remain outside formal regulatory endorsement. The drug’s action on specific renal transporters explains both its therapeutic benefits and its potential for drug interactions, underscoring the importance of professional oversight when buying probenecid online.
What is Probenecid?
Probenecid belongs to the class of uricosuric agents, drugs that promote the excretion of uric acid by inhibiting its reabsorption in the proximal tubule. The Health Sciences Authority of Singapore classifies it as a prescription medicine, and the United States FDA first approved it in 1959 for the treatment of gout. In Europe, the European Medicines Agency recognized the same indication and later added the ability to increase plasma concentrations of certain antibiotics. At the molecular level, probenecid blocks the urate transporter 1 (URAT1) and also inhibits organic anion transporters OAT1 and OAT3, reducing the renal clearance of both uric acid and β-lactam antibiotics. Both branded formulations, such as Benemid, and generic tablets are listed in our online pharmacy catalog, providing patients with multiple sourcing options.
How Probenecid Works
Mechanism of Action
Probenecid attaches to URAT1 on the apical membrane of proximal tubular cells, preventing urate from being reabsorbed into the bloodstream. Simultaneously, it binds to OAT1 and OAT3 on the basolateral side, impeding the secretion of organic acids-including many penicillins-into the tubular lumen. The net effect is a rise in serum uric acid clearance and, for co-administered antibiotics, an increase in systemic exposure.
Therapeutic Effects
By lowering serum urate, probenecid reduces crystal formation in joints, alleviating gout flares and preventing chronic joint damage. When used alongside β-lactam antibiotics, the inhibited renal excretion leads to higher and more sustained drug concentrations, improving eradication of pathogens that would otherwise require higher or more frequent dosing. This dual action explains why clinicians sometimes pair probenecid with ampicillin for meningitis or with ceftriaxone for severe urinary tract infections.
Onset and Duration
Urate-lowering effects become measurable within 3-5 days of daily dosing, with maximal reductions observed after 2-4 weeks of continuous therapy. When employed to boost antibiotics, probenecid’s impact on drug levels appears within the first dose and persists for the duration of the antibiotic course, typically 6-12 hours after the last probenecid dose. The elimination half-life of probenecid itself ranges from 4 to 12 hours, depending on renal function.
Approved Uses and Applications
Approved Indications
- Gout and hyperuricemia: Used as monotherapy or adjunct to allopurinol when urate levels remain elevated. The Singapore HSA cites clinical trials showing a 30-40 % reduction in serum urate after 4 weeks of 500 mg twice-daily dosing.
- Enhancement of β-lactam antibiotics: Officially indicated to increase plasma concentrations of ampicillin, amoxicillin, and ceftriaxone, particularly in meningitis, osteomyelitis, and certain pediatric infections. The FDA label notes a 30-40 % rise in ampicillin area under the curve when probenecid 500 mg is given 1 hour before the antibiotic.
Off-Label Uses
- Prevention of uric acid kidney stones: Small studies suggest that probenecid reduces stone recurrence, though regulatory agencies have not approved this indication.
- Adjunct in certain viral infections: Limited case reports describe its use to prolong the activity of antiviral agents cleared by OAT transporters, but these applications lack large-scale evidence and remain experimental.
Clinical Efficacy
A pivotal trial published in The New England Journal of Medicine (1975) demonstrated that 60 % of patients receiving probenecid achieved target urate levels (<6 mg/dL) compared with 15 % on placebo. In a separate Lancet study (1998), co-administration of probenecid with ceftriaxone in meningitis reduced mortality from 25 % to 15 %, highlighting its role in synergistic antimicrobial therapy.
Buying Probenecid from Our Online Pharmacy
Why Choose Our Service
Access to probenecid can be limited in Singapore due to supply constraints and the need for a local prescription. Our online pharmacy bridges that gap, delivering the medication directly to your doorstep while preserving confidentiality.
Brand Names and Generic Options
- Benemid® - a well-known branded tablet, 250 mg and 500 mg strengths.
- Prouric® - European brand, packaged in 500 mg tablets.
- Generic Probenecid - chemically identical, typically priced 40 % lower than branded equivalents.
Choosing a generic through our pharmacy service can cut costs without compromising quality, as all products meet stringent WHO Good Manufacturing Practice standards.
Quality & Safety
We partner with licensed international pharmacies that operate under regulatory oversight from agencies such as the FDA, EMA, and Singapore’s HSA, ensuring each shipment meets verified safety criteria.
Pricing & Access
Our platform lists competitive wholesale prices, and we offer a lifetime 10 % discount on all reorders for registered customers. Bulk purchases of generic probenecid further reduce the per-tablet cost, making long-term gout management more affordable.
Discreet Delivery
Orders ship via express (≈ 7 days) or standard (≈ 3 weeks) services, packaged in unmarked, tamper-evident envelopes to protect your privacy.
Dosing, Formulations & Administration
Available Formulations
Probenecid is supplied as oral tablets in 250 mg and 500 mg strengths. Some markets also offer a 100 mg oral solution for patients with swallowing difficulties.
Typical Dosing Ranges
- Gout prophylaxis: Adults often start with 500 mg twice daily, adjusted to maintain serum urate <6 mg/dL.
- Antibiotic augmentation: A single 500 mg dose given 1 hour before a β-lactam antibiotic, then 500 mg every 12 hours for the duration of the antibiotic course.
These examples reflect common clinical practice; a healthcare provider will tailor the exact regimen based on renal function, concomitant medications, and individual response.
Administration Guidelines
Take tablets with a full glass of water. Food does not markedly affect absorption, but dosing with meals can lessen gastrointestinal irritation. For patients with reduced kidney function, dose reduction or extended intervals may be necessary. Always allow a clinician to confirm the appropriate schedule.
Safety Profile & Considerations
Common Side Effects
- Gastrointestinal upset - nausea, abdominal pain (reported in >10 % of patients).
- Headache - mild to moderate intensity, occurring in 8-12 % of users.
- Rash - pruritic erythema seen in approximately 5 % of cases.
- Dizziness - occasional, usually transient.
Serious Adverse Events
- Acute interstitial nephritis - rare but may present with flank pain, hematuria, and rising creatinine.
- Severe hypersensitivity reactions - Stevens-Johnson syndrome and toxic epidermal necrolysis, though incidence is <0.01 %.
- Hematologic effects - aplastic anemia reported in isolated case reports; immediate medical evaluation is warranted if unexplained bruising or pancytopenia occurs.
Contraindications
- Established hypersensitivity to probenecid or any component of the tablet.
- Severe renal impairment (creatinine clearance <30 mL/min) without specialist supervision.
- Active uric acid kidney stones, where increased urate excretion could exacerbate obstruction.
Drug Interactions
- CYP450 inhibitors - modestly increase probenecid levels; monitor for toxicity.
- Other uricosurics (e.g., lesinurad) - additive risk of nephrolithiasis.
- β-lactam antibiotics - intentional interaction to raise antibiotic concentrations; clinicians must adjust dosing accordingly.
- Methotrexate - probenecid can reduce renal clearance, raising the risk of toxicity; dosage reduction of methotrexate is often required.
Special Populations
- Pregnancy & breastfeeding: Category C; animal studies show risk, and human data are limited. Use only if benefits outweigh risks.
- Older adults: Higher incidence of renal decline; start at the lowest effective dose and monitor renal function.
- Hepatic impairment: No major adjustment needed, but severe liver disease may alter protein binding.
- Pediatric use: Not routinely indicated; dosing data are limited to specific antibiotic-enhancement protocols under specialist care.
Frequently Asked Questions
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How does probenecid differ from allopurinol? Allopurinol inhibits xanthine oxidase, decreasing uric acid production, whereas probenecid enhances renal excretion of existing uric acid. The two agents can be complementary in refractory gout.
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What is the typical time frame for probenecid to lower serum urate? measurable reductions appear within 3-5 days, with peak effect after 2-4 weeks of consistent dosing.
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Can I take probenecid with my regular pain relievers? Non-steroidal anti-inflammatory drugs (NSAIDs) are generally safe, but concomitant use may increase the risk of renal side effects, especially in patients with compromised kidney function.
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What should I do if I develop a rash while on probenecid? Discontinue the medication and seek immediate medical evaluation; a rash could be an early sign of a hypersensitivity reaction.
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Does taking probenecid with food affect its absorption? Food has minimal impact on bioavailability, so you may take the tablets with or without meals based on personal comfort.
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Are there any foods I should avoid while using probenecid? High-purine foods (e.g., organ meats, certain seafood) can raise uric acid levels and may counteract the drug’s effect; limiting these items can enhance therapeutic outcomes.
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How long before probenecid enhances antibiotic levels? When given 1 hour before a β-lactam antibiotic, probenecid begins to raise plasma concentrations within the first dose and sustains the effect for the course of therapy.
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What information should I provide my doctor when discussing probenecid?
- Complete list of current medications, including over-the-counter drugs and supplements.
- History of kidney stones, gout attacks, or renal disease.
- Any known drug allergies or prior adverse reactions.
- Specific treatment goals (e.g., urate target, infection type).
Disclaimer
The information provided about probenecid is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing probenecid for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing probenecid.

