케토프로펜

비스테로이드성 항염증제 (NSAID)

케토프로펜은 이부프로펜, 나프록센, 카프로펜과 구조적으로 관련된 강력한 **프로피온산 유도체 비스테로이드성 항염증제(NSAID)**입니다. 수의학에서는 강력한 **진통, 해열 및 항염증** 특성으로 인해 널리 사용됩니다. 주요 약리학적 특징: * **거울상 이성질체 특성**: 상업용 케토프로펜은 라세미 혼합물입니다. **S(+) 거울상 이성질체**는 주로 항프로스타글란딘 활성(및 관련 위장관/신장 독성)을 담당하는 반면, **R(-) 거울상 이성질체**는 심각한 위장관 부작용 없이 진통 효과를 제공합니다. * **사용 축종**: 말의 근골격계 통증에 널리 사용되며, 일부 임상 수의사들은 고양이의 단기 진통을 위한 최우선 NSAID 중 하나로 간주합니다. 개, 소, 돼지 및 다양한 특수 동물에도 사용됩니다. * **임상적 주의사항**: 매우 효과적이지만 케토프로펜은 비선택적 COX 억제제입니다. 따라서 특히 소동물에서 최신 COX-2 선택적 NSAID(콕시브계)에 비해 위장관 궤양 및 신장 독성의 위험이 더 높습니다. 개와 고양이에서의 사용은 일반적으로 단기(예: 1~5일)로 제한됩니다.

작용 기전: 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.

동물 종별 용량

Cats

Antiinflammatory/analgesic · 2 mg/kg (0.2 mL/kg) SC for one day, and continue with ketoprofen tablets PO at a lower maintenance dose of 1 mg/kg once a day for four more days · SC, PO · q24h · 5 days total · In severe cases, the parenteral loading dose of 2 mg/kg can be given for up to three consecutive days.
Antiinflammatory/analgesic · 1 mg/kg PO or SC once daily for up to 5 days, or 2 mg/kg SC as a single injection · PO, SC · q24h · Up to 5 days
Post-operative pain control · 1-2 mg/kg IV, SC once daily for 3 days duration after surgery; or 1 mg/kg PO once daily for 3 days, after surgery · IV, SC, PO · q24h · 3 days
Antiinflammatory/analgesic · 2 mg/kg SC once daily for up to 3 consecutive days. If preferred after one injection treatment may be followed on the next day with tablets at 1 mg/kg and continued on successive days for up to 4 days · SC, PO · q24h · Up to 5 days total
Acute pain from musculoskeletal and other painful disorders · 2 mg/kg · SC · q24h · up to 3 consecutive days · Oral dosing for 4 days may follow a single injection of ketoprofen on day one.
Acute pain from musculoskeletal and other painful disorders · 1 mg/kg · PO · q24h · up to 5 days · Oral dosing for 4 days may follow a single injection of ketoprofen on day one.

Swine

Antiinflammatory/analgesic · 3 mg/kg · IM · q24h · Up to 3 days · Withdrawal times (U.K.) for meat: 4 days

Ferrets

투여 경로

POIVIMSC

금기

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

이상반응

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)

약물 상호작용

Aminoglycosides (gentamicin, amikacin) · Increased risk for nephrotoxicity.
Anticoagulants (heparin, LMWH, warfarin) · Increased risk for bleeding.
Aspirin · Plasma levels of ketoprofen could decrease; increased likelihood of GI adverse effects (blood loss). Concomitant use is not recommended.
Bisphosphonates (alendronate) · May increase risk for GI ulceration.
Corticosteroids · Concomitant administration significantly increases the risks for GI adverse effects and ulceration.
Cyclosporine · May increase risk for nephrotoxicity.
Fluconazole · May increase NSAID levels.
Furosemide · Ketoprofen may reduce the saluretic and diuretic effects of furosemide.
Highly Protein Bound Drugs (phenytoin, valproic acid, sulfonamides) · Ketoprofen is 99% protein-bound and may displace other drugs, leading to increased serum levels and duration of action.
Methotrexate · Serious toxicity has occurred when NSAIDs are used concomitantly; use with extreme caution.
Probenecid · May cause a significant increase in serum levels and half-life of ketoprofen.
Other NSAIDs · Increased risk of severe gastrointestinal ulceration and renal toxicity. Do not administer concurrently or within 24 hours. · major

모니터링

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

과용량

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.

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