ケトロラク
**ケトロラク**は、獣医学において主に短期的な鎮痛に使用される非常に強力な非ステロイド性抗炎症薬(NSAID)です。 - **臨床上のポイント**: ケトロラクは強力な鎮痛効果(ヒト医療ではオピオイドと比較されることが多い)を提供しますが、より安全な動物用NSAIDが利用可能であること、および犬や猫において**胃腸毒性**(潰瘍や穿孔)や**腎毒性**のリスクが非常に高いため、その使用は議論の余地があり、一般的には推奨されません。 - 犬に使用する場合、ほとんどの臨床医は治療を**3日未満**に厳しく制限し、**ミソプロストール**(スクラルファートの併用を問わず)などの胃腸保護薬の同時投与を強く推奨します。
作用機序: Ketorolac exerts its analgesic, anti-inflammatory, and antipyretic effects by non-selectively inhibiting **cyclooxygenase (COX-1 and COX-2)** enzymes. **Arachidonic Acid** → **COX-1/COX-2 Inhibition** → Decreased synthesis of **prostaglandins** and **thromboxanes**. By blocking prostaglandin production, it reduces inflammation and pain signaling. However, the profound inhibition of constitutive COX-1 also depletes protective prostaglandins in the gastric mucosa and kidneys, leading to its severe ulcerogenic and nephrotoxic side effect profile in small animals.
動物種別の用量
- As an analgesic · 0.25 mg/kg IM q8-12h for one or two doses · IM · q8-12h · 1-2 doses
- Anterior uveitis and ulcerative keratitis · 1 drop per eye · topical · q6-24h · Frequency depends on the severity of inflammation.
- As an analgesic (Mice) · 0.7-10 mg/kg PO once daily · PO · once daily
- As an analgesic (Rats) · 3-5 mg/kg PO once to twice a day; 1 mg/kg IM once to twice a day · PO, IM · once to twice a day
- As an analgesic · 0.3-0.7 mg/kg IV , IM, SC, PO three times daily · IV, IM, SC, PO · three times daily
- As an analgesic · 0.5 mg/kg IV three times daily or 0.3 mg/kg PO twice daily · IV, PO · TID (IV) or BID (PO) · < 3 days · Repeated doses have considerable potential for causing GI or renal toxicity. Treated dogs should receive misoprostol.
- As an analgesic · 0.3-0.5 mg/kg IV , IM q8-12h for one or two doses · IV, IM · q8-12h · 1-2 doses
- Anterior uveitis and ulcerative keratitis · 1 drop per eye · topical · q6-24h · Frequency depends on the severity of inflammation.
用量は獣医療従事者向けの臨床リファレンスです。必ず最新の添付文書と個々の患者で確認してください。
投与経路
禁忌
- Active GI ulcers
- History of hypersensitivity to ketorolac
- Pre-existing hematologic, renal, or hepatic disease (relative contraindication)
- Known hypersensitivity to NSAIDs
- Use with extreme caution in patients with deep or progressive corneal ulcers
有害事象
- Gastrointestinal ulceration and erosion
- Gastrointestinal perforation
- Renal toxicity
- Hepatic toxicity
- Platelet inhibition (increased bleeding risk)
- Local ocular irritation
- Delayed corneal epithelial healing
- Increased intraocular pressure (IOP)
- Corneal 'melting' (keratomalacia) - reported in humans, theoretical risk in animals
薬物相互作用
- ACE INHIBITORS · Increased risk for nephrotoxicity
- ALPRAZOLAM · Hallucinations reported in some human patients taking with ketorolac
- AMINOGLYCOSIDES (gentamicin, amikacin, etc.) · Increased risk for nephrotoxicity
- ANTICOAGULANTS (heparin, LMWH, warfarin) · Increased risk for bleeding possible
- ASPIRIN · Increased likelihood of GI adverse effects (blood loss)
- BISPHOSPHONATES (alendronate, etc.) · May increase risk for GI ulceration
- CORTICOSTEROIDS · Concomitant administration with NSAIDs may significantly increase the risks for GI adverse effects
- CYCLOSPORINE · May increase risk for nephrotoxicity
- FLUCONAZOLE · May increase NSAID levels
- FLUOXETINE · Hallucinations reported in some human patients taking with ketorolac
- FUROSEMIDE · Ketorolac may reduce the saluretic and diuretic effects of furosemide
- METHOTREXATE · Serious toxicity has occurred when NSAIDs have been used concomitantly; use together with extreme caution
- MUSCLE RELAXANTS, NONDEPOLARIZING · Ketorolac may potentiate effects
モニタリング
- Analgesic and anti-inflammatory efficacy
- Gastrointestinal signs (appetite, vomiting, diarrhea, occult blood in feces)
- Renal function parameters (BUN, creatinine, urinalysis) with repeated use
- Intraocular pressure (IOP), especially in predisposed breeds
- Corneal healing via fluorescein staining
- Signs of corneal melting or worsening ulceration
過量投与
Ketorolac has a narrow margin of safety in small animals. - **Cats**: Have developed renal toxicity at doses as low as 0.7 mg/kg. - **Mice**: The oral LD50 is 200 mg/kg. - **Clinical Signs**: GI effects, including severe GI ulceration and bleeding, are highly likely in overdoses in small animals. Metabolic acidosis has been reported in humans. - **Treatment**: Consider GI emptying for large, recent overdoses. Patients must be closely monitored for GI bleeding and renal impairment. Treat aggressively with GI protectants (sucralfate) and consider giving misoprostol early.
VetSheet の薬剤リファレンスは、獣医療従事者向けの臨床意思決定支援を目的としており、専門的判断やメーカーの最新添付文書に代わるものではありません。