丙磺舒
Probenecid
4-(dipropylsulfamoyl)benzoic acid
別名: Benemid · Benuryl · probenecidas · probenecidum
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
爬蟲類
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Gout | 250 mg PO q12h; can be increased as needed. | PO | q12h | — | 🌎 NA |
| Gout | 40 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Gout | 250 mg (total dose) PO twice daily; may increase as needed. | PO | twice daily | — | 🌎 NA |
- Gout: Suggested dosage based upon human data as dose is not established for reptiles.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
丙磺舒 (Probenecid) 是一種磺胺類衍生物，主要作為促尿酸排泄藥和腎小管分泌抑制劑。
- 獸醫用途：雖然在小型哺乳動物中的臨床使用有限，但它在爬行動物醫學中對治療痛風（高尿酸血症）特別有價值。
- 藥理效用：在歷史和藥理學上，丙磺舒以其抑制弱有機酸（特別是β-內醯胺類抗生素，如青黴素和頭孢菌素）腎臟排泄的能力而聞名。藉此，它能顯著延長這些藥物的半衰期並提高血清濃度。
- 臨床要點：在狗體內，丙磺舒的消除半衰期（約18小時）比人類（6.5小時）長得多，這在理論上有利於延長昂貴或快速清除藥物的給藥間隔，儘管目前仍缺乏針對狗的充分臨床試驗支持。
作用機制
Probenecid exerts its effects via competitive inhibition at the proximal renal tubules:
- Uricosuric Effect: Competitively inhibits the Urate Transporter 1 (URAT1) on the apical membrane of the proximal tubule → prevents the reabsorption of uric acid from the urine back into the blood → enhances uric acid excretion and lowers serum urate levels.
- Secretion Inhibition: Competitively inhibits Organic Anion Transporters (OAT1, OAT3) on the basolateral membrane → prevents the active tubular secretion of weak organic acids (e.g., penicillins, cephalosporins, NSAIDs) from the blood into the urine → prolongs the systemic half-life of these drugs.
安全性與警告
禁忌症
- Patients with or susceptible to uric acid renal or bladder calculus formation
- Urate nephropathy (e.g., cancer chemotherapy with rapidly cytolytic agents)
- Severe renal impairment (creatinine clearance < 30 mL/min)
- Gout in birds (can exacerbate the condition)
不良反應
- Headache (humans)
- Inappetence
- Nausea
- Mild vomiting
- Rashes
- Increased rate of gouty attacks initially (if no prophylaxis)
- Hypersensitivity (rare)
- Bone marrow suppression (rare)
- Hepatotoxicity (rare)
- Nephrotic syndrome (rare)
注意事項
Renal Function: Probenecid requires sufficient renal function to be effective; efficacy decreases with increasing renal function impairment. Avian Patients: Not usually recommended for treating gout in birds as it can exacerbate the condition. Laboratory Alterations: May cause false-positive urine glucose (cupric sulfate method), falsely elevated theophylline levels, decreased 17-ketosteroid urine concentrations, and altered renal clearance study results.
藥物相互作用
Increased acyclovir serum concentrations; probenecid can decrease renal excretion
Increased chance of uric acid nephropathy
Salicylates antagonize the uricosuric effects of probenecid
Probenecid may prolong action or reduce time for onset of action
Probenecid may increase serum concentrations by reducing renal excretion
Probenecid may increase serum concentrations by reducing renal excretion (does not affect clavulanic acid)
Probenecid decreases elimination; hypoglycemia is possible
Probenecid reduces renal tubular secretion of ciprofloxacin by about 50%. Significantly reduces renal excretion of enrofloxacin in goats.
Possible accumulation of dapsone or its active metabolites
Increased serum furosemide levels
Probenecid may increase and prolong heparin's effects
Probenecid may increase levels; increased risks for toxicity
Probenecid may increase plasma levels and increase risks for toxicity
Reduced urine levels; increased chance for systemic toxicity
Probenecid may increase serum concentrations by reducing renal excretion
Probenecid may reduce hepatic uptake of rifampin and serum levels can be increased; use together is not recommended
Decreases renal elimination of sulfonamides, may increase risks for sulfonamide toxicity without therapeutic benefit
Anesthesia may be extended or dose required for anesthesia decreased
監測
- Serum uric acid
- Urine uric acid
- Acid-base balance (if concomitant urine alkalinization is used)
藥物動力學
半衰期
吸收
Dogs: Oral bioavailability information not located. Mares: Oral bioavailability approximately 90%. Humans: Rapid and complete absorption after oral administration.
分佈
Dogs: Apparent volume of distribution at steady state is 0.46 L/kg. Exhibits biphasic concentration-dependent plasma protein binding (binds less to plasma proteins than in humans). Mares: Highly bound (99.9%) to equine plasma proteins.
代謝
Humans: Converted in the liver to glucuronidated, carboxylated, and hydroxylated compounds that have uricosuric and renal tubular secretion inhibition activity.
排除
Dogs: Plasma clearance is 0.343 mL/min/kg. Humans: Elimination half-life is dosage dependent (larger dosages have longer half-lives).
過量
Limited information is available in veterinary species.
- Human Data: One massive (>45 g) overdose caused CNS stimulation, seizures, protracted vomiting, and respiratory failure.
- Management: Handle initially using standardized protocols for removal of drug from the gut and preventing absorption. Treat supportively. Use caution co-administrating drugs that may compete with probenecid for tubular secretion. Consider contacting an animal poison control center for guidance.
可用產品
劑型
- Tablets
人用標示
- Probenecid Tablets: 500 mg
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Probenecid tablets should be stored at room temperature in well-closed containers. Expiration dates are generally 3-5 years after manufacture.
飼主須知
重要提示：丙磺舒很少用於犬貓，其在這些物種中的安全性尚未完全確立。它更常被處方用於特殊寵物，特別是爬行動物。
- 用途：用於治療爬行動物的痛風，或有意延長某些抗生素在體內的作用時間。
- 給藥：請嚴格按照獸醫的指示給藥。未經獸醫同意，請勿給予任何新藥物或保健品，因為丙磺舒會與許多常見藥物產生交互作用。
- 副作用：觀察是否有腸胃不適的跡象（食慾不振、噁心、嘔吐）。如果您發現任何異常行為或症狀，請聯繫您的獸醫。
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