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特波沙林

Tepoxalin

非類固醇消炎止痛藥 (NSAID)PO狗

別名: Zubrin · ORF-20485 · RWJ-20485

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

20 mg/kg PO (or 10 mg/kg PO) on first day; subsequently give 10 mg/kg PO once dailyPO· q24h· Based on clinical response and patient tolerance
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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

狗

適應症劑量途徑頻次療程地區
Pain and inflammation associated with osteoarthritis20 mg/kg PO (or 10 mg/kg PO) on first day; subsequently give 10 mg/kg PO once dailyPOq24hBased on clinical response and patient tolerance🌎 NA
  • Pain and inflammation associated with osteoarthritis: On first day of treatment give 20 mg/kg PO (or 10 mg/kg PO); subsequently give 10 mg/kg PO once daily.

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概覽

特波沙林 (Tepoxalin) 是一種獨特的​雙重抑制劑​，能同時抑制環氧合酶 (COX) 和脂氧合酶 (LOX) 途徑。主要用於治療​犬骨關節炎​相關的疼痛與發炎。

  • 具有快速崩解錠劑型（口溶錠），非常適合難以餵藥的犬隻。
  • 由於其對白三烯素的抑制作用，目前也有研究探討其作為犬過敏性疾病輔助治療的潛力。
  • ​臨床提示​：儘管抑制 LOX 理論上具有保護胃腸道的作用，但臨床數據顯示，與其他現代 FDA 核准的 COX-2 選擇性 NSAID 相比，它可能引起更多的嘔吐和腹瀉。

作用機制

Tepoxalin blocks the arachidonic acid cascade at two key points:

  • ​Cyclooxygenase (COX-1 and COX-2)​ → Decreases production of pro-inflammatory prostaglandins (mediators of pain, hyperpyrexia, and inflammation).
  • ​5-Lipoxygenase (5-LOX)​ → Decreases production of leukotrienes (e.g., LTB4).

Pharmacological Note: LTB4 is a potent chemoattractant for neutrophils and contributes to GI mucosal damage by increasing cytokine production and release of proteinases. By inhibiting LOX, tepoxalin theoretically mitigates the GI ulcerogenic effects typically seen with COX-1 inhibition, though clinical GI side effects still occur. LOX inhibition in dogs persists for only about 6 hours after dosing.

安全性與警告

禁忌症

  • Prior hypersensitivity reactions to tepoxalin
  • Active gastrointestinal ulcers
  • Dogs weighing less than 3 kg (cannot be accurately dosed)
  • Dogs less than 6 months old (safety not established)

不良反應

  • Diarrhea
  • Vomiting
  • Anorexia/inappetence
  • Enteritis
  • Lethargy
  • Incoordination (<1%)
  • Incontinence (<1%)
  • Increased appetite (<1%)
  • Eating grass (<1%)
  • Flatulence (<1%)
  • Hair loss (<1%)
  • Trembling (<1%)

注意事項

Use with caution in patients with impaired hepatic, cardiovascular, or renal function, or those at risk for developing nephrotoxic effects associated with NSAIDs (e.g., dehydrated patients or those on concomitant diuretic therapy). Safety has not been determined in pregnant, breeding, or lactating dogs; use with caution and informed consent. Discontinue if signs of inappetence, vomiting, fecal abnormalities, anemia, icterus, or lethargy are observed.

藥物相互作用

Aspirin

May increase the risk of gastrointestinal toxicity (e.g., ulceration, bleeding, vomiting, diarrhea)

Corticosteroids

May increase the occurrence of gastric ulceration; avoid concomitant use

Digoxin

NSAIDs may increase serum levels of digoxin

Fluconazole

May increase plasma levels of tepoxalin (extrapolated from human celecoxib data)

Furosemide

NSAIDs may reduce saluretic and diuretic effects

Methotrexate

Serious toxicity has occurred with concomitant NSAID use; use with extreme caution

Nephrotoxic Drugs (e.g., aminoglycosides, amphotericin B)

May enhance the risk of nephrotoxicity

Other NSAIDs

May increase the risk of gastrointestinal toxicity (e.g., ulceration, bleeding, vomiting, diarrhea)

Warfarin

Tepoxalin is highly protein bound (98-99%); may displace warfarin and increase bleeding risk. Monitor closely.

監測

  • Clinical efficacy (improvement in mobility/pain)
  • Baseline and periodic CBC
  • Chemistry panel (including bilirubin and serum creatinine)
  • Signs associated with adverse effects (GI effects, appetite, vomiting, diarrhea, etc.)

藥物動力學

半衰期

貓Tepoxalin: ~5 hours; Active metabolite: ~4 hours狗Tepoxalin: ~2 hours; Active metabolite: ~13 hours

吸收

Readily absorbed after oral administration. Peak levels occur between 2-3 hours post-dose. The presence of food in the gut increases bioavailability.

分佈

Tepoxalin and its active metabolite (tepoxalin pyrazole acid) are highly bound to plasma proteins (98-99%).

代謝

Rapidly metabolized to several metabolites, including the active metabolite tepoxalin pyrazole acid.

排除

Metabolites are eliminated primarily in the feces; only 1% of the drug is eliminated in the urine.

過量

Information on acute overdosage is limited. Chronic overdosage (300 mg/kg/day for 6 months) in dogs caused decreases in total protein, albumin, and calcium concentrations, with gastric lesions noted at necropsy.

An acute overdose may cause significant GI distress, ulceration, and GI bleeding.

  • Treatment: Treat supportively. Monitor CBC, hydration status, renal function, and for evidence of GI bleeding. Contact an animal poison control center for further guidance.

可用產品

劑型

  • Rapidly-disintegrating oral tablets

獸醫用

  • Tepoxalin Oral (rapidly-disintegrating) Tablets: 30 mg, 50 mg, 100 mg, 200 mg in foil blisters (Zubrin)

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

Tablets should be kept in their foil blister packs until used and stored at temperatures between 2-30°C (36-86°F).

飼主須知

  • ​給藥方式​：將藥錠直接放入狗狗口中，並將其嘴巴合攏約 4 秒鐘。藥錠設計為在唾液中快速崩解，可防止狗狗將藥吐出。
  • ​隨餐服用​：請與食物一起餵食，以促進吸收並可能減少腸胃不適。
  • ​水分補充​：確保狗狗隨時有乾淨的飲水。脫水會增加腎臟副作用的風險。

​重要提示​：如果您發現狗狗出現嚴重或持續的嘔吐、腹瀉、黑便/血便、食慾不振、嗜睡或牙齦/眼睛發黃（黃疸），請立即停藥並聯繫您的獸醫師。

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