Probenecid
Revision as of 18:03, 27 January 2026 by Ostermayer (talk | contribs) (Created page with "==General== *Type: Is DrugClass::Uricosuric Agent Is DrugClass::Antibiotic Adjuvant *Dosage Forms: Tablet *Dosage Strengths: 500mg *Routes of Administration: PO *Common Trade Names: Benemid, Probalan ==Adult Dosing== ===General=== *Determine indication (Gout vs Adjuvant) ===Hyperuricemia (Gout)=== *Start: 250mg PO bid x 1 week *Maintenance: 500mg PO bid *May increase by 500mg/day q4weeks if not controlled *Max: 2g/day ===Pelvic Inflammatory Disease (PID)...")
General
- Type: Uricosuric Agent Antibiotic Adjuvant
- Dosage Forms: Tablet
- Dosage Strengths: 500mg
- Routes of Administration: PO
- Common Trade Names: Benemid, Probalan
Adult Dosing
General
- Determine indication (Gout vs Adjuvant)
Hyperuricemia (Gout)
- Start: 250mg PO bid x 1 week
- Maintenance: 500mg PO bid
- May increase by 500mg/day q4weeks if not controlled
- Max: 2g/day
Pelvic Inflammatory Disease (PID)
- 1g PO x 1
- Given concurrently with Cefoxitin 2g IM x 1
Neurosyphilis (Adjunct)
- 500mg PO q6h
- Given concurrently with Procaine Penicillin G 2.4 million units IM daily x 10-14 days
Pediatric Dosing
General (< 2 years)
- Contraindicated
General (2 - 14 years)
- Adjunct to antibiotic therapy (limited data/use)
- Initial: 25mg/kg PO x 1
- Maintenance: 40mg/kg/day divided q6h
Special Populations
- Pregnancy: B
- Lactation: Excreted in breast milk; safety not established
- Renal
- Adult
- CrCl <30: Avoid use (likely ineffective for uricosuric effect; may typically be used for simple antibiotic adjuvant effect if necessary, but risk of toxicity increases)
- Pediatric
- Not defined
- Adult
- Hepatic
- No specific guidelines defined, but metabolized by liver
Contraindications
- Allergy to Probenecid
- Children < 2 years of age
- Concomitant use with ketorolac (increases ketorolac plasma levels significantly)
- Concomitant use with salicylates (aspirin antagonizes uricosuric action)
- Uric acid lithiasis (kidney stones)
- Acute Gout attack (do not initiate therapy during acute attack)
- Blood dyscrasias
- G6PD Deficiency (risk of hemolytic anemia)
Adverse Reactions
Serious
- Anaphylaxis
- Hemolytic Anemia (associated with G6PD deficiency)
- Aplastic Anemia
- Hepatic Necrosis
- Nephrotic Syndrome
- Seizures
Common
- Headache
- Nausea and Vomiting
- Anorexia
- Dizziness
- Flushing
- Rash (Urticaria/Pruritus)
- Gingival soreness
- Urinary frequency
Pharmacology
- Half-life: 3-8h (dose dependent)
- Metabolism: Liver
- Excretion: Urine
- Mechanism of Action:
- Uricosuric: Inhibits tubular reabsorption of urate, increasing urinary excretion of uric acid.
- Adjuvant: Inhibits renal tubular secretion of beta-lactam antibiotics (penicillins, cephalosporins), thereby increasing their plasma concentrations and half-life.