ロベナコキシブ
**ロベナコキシブ (Robenacoxib)** は、犬および猫用に特別に認可された高選択的コキシブ系非ステロイド性抗炎症薬(NSAID)です。 主な臨床的特徴: * **組織選択性**:血中からは速やかに消失する一方で、活動性の炎症部位(炎症を起こした関節など)には高濃度で長時間とどまるという独自の薬物動態プロファイルを示します。この「組織特異的」な作用により、全身性の副作用を最小限に抑えつつ有効性を最大化します。 * **高いCOX-2選択性**:COX-1と比較して、犬では約140倍、猫では約500倍のCOX-2選択性を示し、獣医療において最もCOX-2に特異的なNSAIDの一つです。 * **適応症**:主に犬の慢性変形性関節症の疼痛管理、猫の急性筋骨格系疼痛、および両動物種の軟部組織または整形外科手術に伴う周術期疼痛の管理に使用されます。
作用機序: Robenacoxib exerts its anti-inflammatory and analgesic effects by selectively inhibiting the **Cyclooxygenase-2 (COX-2)** enzyme. **Arachidonic Acid** → **COX-2 Enzyme** → **Prostaglandin E2 (PGE2)** and other inflammatory mediators. By specifically targeting the inducible **COX-2** isoform, robenacoxib effectively blunts the production of prostaglandins responsible for pain, inflammation, and fever. Because it largely spares the constitutive **COX-1** enzyme, it preserves the homeostatic prostaglandins that are crucial for maintaining gastrointestinal mucosal integrity, renal blood flow, and normal platelet function.
動物種別の用量
- Acute pain and inflammation associated with musculoskeletal disorders · 1 mg/kg; with a range of 1-2.4 mg/kg · PO · once daily · up to 6 days · Equates to 1 tablet for cats weighing 2.5-<6 kg and 2 tablets for cats weighing 6 kg-<12 kg. Give either without food or with a small amount of food; tablets should not be divided or broken.
- Pain and inflammation associated with chronic osteoarthritis (Note: Label likely intended for surgical pain based on injection formulation) · 2 mg/kg · SC · once · Administer approximately 30 minutes before the start of surgery.
- Perioperative analgesia · 2 mg/kg · SC · q24h · Maximum of 2 doses · Administer approximately 30 minutes before the start of surgery.
- Acute and chronic musculoskeletal pain and inflammation · 1-2 mg/kg · PO · q24h · As directed by veterinarian · May be mixed with a small amount of food. Monitoring is recommended for long-term treatment (>12 weeks).
- Pain and inflammation associated with chronic osteoarthritis · 1 mg/kg with a range of 1-2 mg/kg · PO · once daily · Discontinue after 10 days if no clinical improvement seen · Give at the same time every day. For long term treatment, can adjust to lowest effective dose.
- Pain and inflammation associated with orthopedic or soft tissue surgery · 2 mg/kg · SC · once · Administer approximately 30 minutes before the start of surgery.
- Perioperative analgesia (orthopaedic and soft tissue surgery) · 2 mg/kg · SC · q24h · Maximum of 2 doses · Administer approximately 30 minutes before the start of surgery.
投与経路
禁忌
- Patients with active gastrointestinal ulcers
- Hypersensitivity to robenacoxib or its excipients
- Dogs with hepatic disease
- Dehydrated, hypovolaemic, or hypotensive patients
- Patients with pre-existing gastrointestinal disease or ulceration
- Patients with blood clotting disorders
- Pregnant or lactating animals
- Dogs < 12 weeks of age or < 2.5 kg body weight
- Cats < 16 weeks of age or < 2.5 kg body weight
- Perioperative use in animals with renal disease (not advisable)
有害事象
- Decreased appetite
- Vomiting
- Soft feces
- Diarrhea
- Blood in feces (melena/hematochezia)
- Mild gastrointestinal signs (vomiting, soft feces, diarrhea)
- Gastrointestinal ulceration or bleeding (rare but severe)
- Renal toxicity (especially if hypotensive or dehydrated)
- Hepatic accumulation (in patients with pre-existing liver disease)
薬物相互作用
- ACE Inhibitors (e.g., enalapril, benazepril) · Some NSAIDs can reduce effects on blood pressure
- Aspirin · May increase the risk of gastrointestinal toxicity (e.g., ulceration, bleeding, vomiting, diarrhea)
- Corticosteroids (e.g., prednisone) · May increase the risk of gastrointestinal toxicity (e.g., ulceration, bleeding, vomiting, diarrhea)
- Digoxin · NSAIDs may increase serum levels
- Fluconazole · Administration has increased plasma levels of celecoxib in humans and potentially could also affect robenacoxib levels in dogs
- Furosemide · NSAIDs may reduce the saluretic and diuretic effects
- Highly Protein Bound Drugs (phenytoin, valproic acid, oral anticoagulants, salicylates, sulfonamides, etc.) · As robenacoxib is highly bound to plasma proteins (>99%), it may displace other highly bound drugs or be displaced by them, potentially leading to increased serum levels and toxicity
- Methotrexate · Serious toxicity has occurred when NSAIDs have been used concomitantly; use together with extreme caution
- Nephrotoxic Drugs (e.g., aminoglycosides, amphotericin B) · May enhance the risk of nephrotoxicity development
- Other NSAIDs · Increased risk of severe gastrointestinal ulceration and renal toxicity. Require a 3-5 day wash-out period. · major
- Glucocorticoids · Increased risk of severe gastrointestinal ulceration and bleeding. · major
モニタリング
- Baseline and periodic physical examinations to assess clinical efficacy and adverse effects
- Baseline and periodic CBC, serum biochemistry (liver and renal function), electrolytes, and urinalysis
- For long-term therapy in dogs: Monitor liver enzymes at the start of therapy, and after 2, 4, and 8 weeks; then every 3-6 months
- Discontinue therapy if liver enzymes increase markedly or if accompanied by clinical signs (anorexia, apathy, vomiting)
- Clinical response (reduction in pain and inflammation)
- Gastrointestinal signs (monitor for vomiting, diarrhea, or melena)
- Renal parameters (BUN, Creatinine, USG) and hepatic enzymes, especially prior to anesthesia or during long-term therapy (>12 weeks)
過量投与
Acute overdoses may potentially cause **gastrointestinal, kidney, or liver toxicity**. Interestingly, chronic toxicity studies in healthy young dogs (up to 10 mg/kg/day for 6 months) and cats (up to 10 mg/kg SC for 3 days) did not produce signs of toxicity. **Treatment**: If an acute overdose occurs, symptomatic and supportive therapy is recommended. This may include the administration of gastrointestinal protective agents (e.g., sucralfate, omeprazole), IV fluid therapy for forced diuresis and renal support, and contacting an animal poison control center for guided management.
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。