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テポキサリン

Tepoxalin

非ステロイド性抗炎症薬 (NSAID)PO犬

別名: Zubrin · ORF-20485 · RWJ-20485

VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス

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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用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

動物種別用量

🌎 NA — North America🌍 EU — Europe

犬

適応用量経路頻度期間地域
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.

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

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概要

テポキサリンは、シクロオキシゲナーゼ（COX）およびリポキシゲナーゼ（LOX）経路の両方を阻害するユニークな​二重阻害薬​です。主に​犬の変形性関節症​に伴う疼痛および炎症の管理に適応されます。

  • 口腔内崩壊錠（口の中で溶ける錠剤）として提供されており、投薬が困難な犬に非常に有用です。
  • ロイコトリエンに対する阻害作用があるため、犬のアレルギー疾患の補助治療としての可能性にも関心が寄せられています。
  • ​臨床のポイント​: LOX阻害による理論的な消化管保護作用にもかかわらず、臨床データでは他の最新のFDA承認COX-2選択的NSAIDと比較して嘔吐や下痢を引き起こす可能性が高いことが示唆されています。

作用機序

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・警告

禁忌

  • 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)

有害事象

  • 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.

医薬品相互作用

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.

監視

  • 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.)

薬物動態

半減期

猫Tepoxalin: ~5 hours; Active metabolite: ~4 hours犬Tepoxalin: ~2 hours; Active metabolite: ~13 hours

吸収

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

分布

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.

消失

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

過剰投与

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.

製品

製剤

  • Rapidly-disintegrating oral tablets

動物用医薬品

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

規制ステータス

規制データなし: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

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

飼主向け情報

  • ​投薬方法​: 錠剤を犬の口の中に直接入れ、約4秒間口を閉じたままにしてください。錠剤は唾液で急速に崩壊するように設計されており、犬が吐き出すのを防ぎます。
  • ​食事と一緒に​: 吸収を良くし、胃の不調を軽減する可能性があるため、食事と一緒に与えてください。
  • ​水分補給​: 常に新鮮な水が飲めるようにしてください。脱水は腎臓の副作用のリスクを高めます。

​重要​: 重度または持続的な嘔吐、下痢、黒色便、食欲不振、無気力、または歯茎や目の黄染（黄疸）に気づいた場合は、直ちに投薬を中止し、獣医師に連絡してください。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。