酮洛芬
Ketoprofen
2-(3-benzoylphenyl)propanoic acid
別名: Ketofen · Anafen · Comforion Vet · ketoprofenum · RP-19583 · Ketoprofeno
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
經審核的 v13 劑量證據
結構化劑量計算證據Anti-inflammatory/analgesic (extra-label)
須由已驗證獸醫確認
- q12-24h
NA
必須一併考量的臨床脈絡 (1)
- Ketoprofen injection should be stored below 25°C (77°F), with brief excursions permitted between 0°C and 40°C (32°F-104°F) and used within 4 months of first vial puncture. 13
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
酮洛芬 (Ketoprofen) 是一種強效的丙酸衍生物類非類固醇消炎止痛藥 (NSAID)，在結構上與布洛芬 (ibuprofen)、萘普生 (naproxen) 和卡洛芬 (carprofen) 相似。在獸醫學中，它被廣泛用於其強大的鎮痛、解熱和抗發炎特性。
主要藥理特點：
- 對映異構體特徵：市售的酮洛芬為消旋混合物。S(+) 對映異構體主要負責抗前列腺素活性（以及相關的胃腸道/腎臟毒性），而 R(-) 對映異構體則提供鎮痛作用且無明顯的胃腸道副作用。
- 物種應用：廣泛用於馬匹的肌肉骨骼疼痛，並被部分臨床獸醫師視為貓咪短期鎮痛的首選 NSAID 之一。它也可用於狗、牛、豬及各種特寵物種。
- 臨床要點：雖然非常有效，但酮洛芬是一種非選擇性的 COX 抑制劑。因此，與較新的 COX-2 選擇性 NSAIDs（如 coxibs）相比，它引起胃腸道潰瘍和腎臟毒性的風險較高，特別是在小動物中。其在犬貓的使用通常限制在短期療程（例如 1 至 5 天）。
作用機轉
Ketoprofen exerts its effects primarily through the inhibition of the cyclooxygenase (COX) enzymes.
- Arachidonic Acid Cascade: Cell membrane phospholipids → Phospholipase A2 → Arachidonic Acid.
- COX Inhibition: Ketoprofen non-selectively blocks COX-1 and COX-2 enzymes. This prevents the conversion of arachidonic acid into prostaglandin precursors (endoperoxides), thereby halting the synthesis of pro-inflammatory and hyperalgesic prostaglandins (e.g., PGE2) and thromboxanes.
- LOX Inhibition (Theoretical): Ketoprofen purportedly has inhibitory activity on lipoxygenase (LOX), which would theoretically block the formation of leukotrienes. However, in vitro studies have not definitively confirmed this dual-inhibition activity at therapeutic doses in veterinary species.
- Central and Peripheral Action: By reducing peripheral prostaglandins, it decreases nociceptor sensitization. It also acts centrally to reduce fever by inhibiting prostaglandin synthesis in the hypothalamus.
安全性與警告
禁忌症
- Known hypersensitivity to ketoprofen or other NSAIDs
- Active gastrointestinal ulceration or bleeding
- Significant renal or hepatic impairment
- Late pregnancy (due to risk of premature closure of the patent ductus arteriosus)
- Intra-arterial administration
- Dehydrated, hypovolaemic, or hypotensive patients
- Patients with pre-existing gastrointestinal disease
- Patients with blood clotting problems
- Pregnant animals
- Animals < 6 weeks of age
不良反應
- Horses: Gastric mucosal damage, GI ulceration, renal crest necrosis, mild hepatitis, injection site inflammation (IM)
- Dogs and Cats: Vomiting, anorexia, gastrointestinal ulceration, renal toxicity
- General: Masking of infection signs (inflammation, hyperpyrexia)
- Gastrointestinal signs (vomiting, diarrhea, anorexia)
- Gastrointestinal ulceration and bleeding
- Renal toxicity (especially in dehydrated/hypotensive patients)
- Hepatic accumulation (in patients with liver disease)
- Potential precipitation of cardiac failure (rare/unknown risk in animals)
注意事項
High Protein Binding: Because ketoprofen is highly protein-bound, patients with hypoproteinemia may have increased levels of free (active) drug, significantly increasing the risk of toxicity.
- GI and Renal Risks: Use only when potential benefits outweigh risks in patients with a history of GI ulceration or compromised renal/hepatic function.
- Masking Infection: May mask clinical signs of infection such as fever and inflammation. Use appropriate anti-infective therapy if a primary infectious process is present.
- Breeding Animals: Use with caution in breeding animals; effects on fertility and fetal health are not fully established. Avoid in late pregnancy.
- Administration Warnings: Avoid subcutaneous (SC) injections in horses. Do not administer intra-arterially in any species.
藥物交互作用
Increased risk for nephrotoxicity.
Increased risk for bleeding.
Plasma levels of ketoprofen could decrease; increased likelihood of GI adverse effects (blood loss). Concomitant use is not recommended.
May increase risk for GI ulceration.
Concomitant administration significantly increases the risks for GI adverse effects and ulceration.
May increase risk for nephrotoxicity.
May increase NSAID levels.
Ketoprofen may reduce the saluretic and diuretic effects of furosemide.
Ketoprofen is 99% protein-bound and may displace other drugs, leading to increased serum levels and duration of action.
Serious toxicity has occurred when NSAIDs are used concomitantly; use with extreme caution.
May cause a significant increase in serum levels and half-life of ketoprofen.
Increased risk of severe gastrointestinal ulceration and renal toxicity. Do not administer concurrently or within 24 hours.
Increased risk of severe gastrointestinal ulceration and bleeding. Do not administer concurrently or within 24 hours.
Increased risk of nephrotoxicity.
監測
- Clinical efficacy (reduction in pain, lameness, or fever)
- Adverse effects (monitor for vomiting, diarrhea, melena, or anorexia)
- Baseline and periodic liver and renal function tests (BUN, Creatinine, ALT, AST) are recommended with long-term therapy
- Clinical signs of gastrointestinal ulceration (vomiting, melena, anorexia)
- Renal parameters (BUN, Creatinine, USG) especially in older or compromised patients
- Hepatic enzymes
- Hydration status and blood pressure
藥物動力學
半衰期
吸收
Rapidly and nearly completely absorbed after oral administration in rats, dogs, and humans. Presence of food or milk decreases oral absorption. Oral absorption is poor in horses. IV and IM areas under the curve are relatively equivalent in horses.
分佈
Volume of distribution is low in adult horses, but higher in foals (doses may need to be 1.5X higher in neonates). Enters synovial fluid. Highly bound to plasma proteins (99% in humans, ~93% in horses).
代謝
Metabolized to a conjugated metabolite (primarily glucuronidation in dogs and horses). In cats, thioesterification is proposed as a major elimination mechanism.
排除
Eliminated via the kidneys both as a conjugated metabolite and unchanged drug.
過量
As with any NSAID, overdosage can lead to severe gastrointestinal and renal toxicity.
- Dogs: The LD50 after oral ingestion is reported to be 2000 mg/kg, but exposures as low as 0.44 mg/kg have caused GI ulcers. Common clinical signs of toxic exposure include vomiting.
- Cats: Highly sensitive; have developed renal toxicity at doses as low as 0.7 mg/kg.
- Horses: Generally tolerate higher doses. Doses up to 11 mg/kg IV once daily for 15 days showed no toxicity. However, severe laminitis occurred at 33 mg/kg/day (15X label dose) for 5 days. At 55 mg/kg/day (25X label dose), horses developed anorexia, depression, icterus, abdominal swelling, gastritis, nephritis, and hepatitis.
Treatment:
- Decontamination: Emetics and/or activated charcoal are appropriate for recent oral exposures.
- GI Protection: Use of gastrointestinal protectants (e.g., omeprazole, sucralfate, misoprostol) is strongly warranted if GI effects are expected.
- Renal Protection: Aggressive IV fluid diuresis is warranted to support renal perfusion if renal effects are expected.
可用產品
劑型
- Veterinary Injection: 100 mg/mL, 10 mg/mL
- Veterinary Tablets: 5 mg, 10 mg, 20 mg
- Human Capsules: 50 mg, 75 mg
- Human Extended-Release Capsules: 100 mg, 150 mg, 200 mg
- Injectable: 1% solution
- Oral: 5 mg tablets
- Oral: 20 mg tablets
獸醫用
- Ketoprofen Injection: 100 mg/mL (Ketofen, generic)
- Ketoprofen Injection: 10 mg/mL (Anafen, Ketofen - Canada/UK)
- Ketoprofen Tablets: 5 mg, 10 mg, 20 mg (Anafen, Ketofen - Canada/UK)
- Ketofen 1% injection
- Ketofen 5 mg tablets
- Ketofen 20 mg tablets
人用標示
- Ketoprofen Capsules: 50 mg, 75 mg
- Ketoprofen Extended-Release Capsules: 100 mg, 150 mg, 200 mg
- Oruvail
- Orudis
各地核准狀態
停藥期: pig meat 4 days · cattle meat 4 days · cattle milk 0 hours · horse meat 28 days
POM-V classification.
POM-V classification.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Oral capsules should be stored at room temperature in tight, light-resistant containers. Veterinary injection should be stored at room temperature.
飼主須知
酮洛芬 (Ketoprofen) 是一種用於減輕寵物疼痛、發炎和發燒的藥物。
重要安全指引：
- 與食物一起服用：如果您是口服給予酮洛芬，最好與食物一起餵食，以幫助減少腸胃不適的機會。
- 注意腸胃問題：最常見的副作用是嘔吐、食慾不振和腹瀉。如果您的寵物嘔吐、停止進食，或者您發現有黑色柏油狀糞便或嘔吐物/糞便中有血，請立即停止給藥並聯繫您的獸醫師。這些可能是胃潰瘍的徵兆。
- 請勿混合用藥：除非獸醫師特別指示，否則在寵物服用酮洛芬期間，絕對不要給予阿斯匹靈、布洛芬或其他止痛藥（如 Rimadyl、Metacam 或 Deramaxx）。混合使用這些藥物可能會導致致命的胃出血或腎衰竭。
- 嚴格遵守指示：請勿自行增加劑量或增加給藥頻率。犬貓對 NSAID 的過量非常敏感。
- 保持水分充足：確保您的寵物隨時有充足的新鮮飲水，這有助於保護牠們的腎臟。
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