マバコキシブ
Mavacoxib
4-[5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
別名: Trocoxil · mavacoxibum · PHA 739,521 · UNIIYFT7X7SR77
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
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 degenerative joint disease in dogs aged 12 months or more in cases where continuous treatment exceeding one month is indicated | 2 mg/kg PO given immediately before or with the dog's main meal. The treatment should be repeated 14 days later; thereafter the dosing interval is one month. | PO | Day 1, Day 14, then monthly | A treatment cycle should not exceed 7 consecutive doses (6.5 months). | 🌎 NA |
| Pain and inflammation associated with degenerative joint disease (osteoarthritis) | 2 mg/kg | PO | q14d for 2 doses, then q1month | Maximum of 7 doses total | 🌍 EU |
- Pain and inflammation associated with degenerative joint disease in dogs aged 12 months or more in cases where continuous treatment exceeding one month is indicated: Care should be taken to ensure that the tablet is ingested. THIS IS not a daily NSAID.
- Pain and inflammation associated with degenerative joint disease (osteoarthritis): Should be given immediately before or with the dog's main meal. Treatment can potentially be re-started after a 1-month break from dosing.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Any | Do not use | PO | N/A | N/A | 🌍 EU |
- Any: Contraindicated in cats.
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。
概要
マバコキシブ（Mavacoxib）は、コキシブ系に属する非常にユニークな超長時間作用型非ステロイド性抗炎症薬（NSAID）です。従来の毎日の投薬とは異なり、月1回の投与で済むように設計されており、毎日の投薬が困難な飼い主にとって優れた選択肢となります。
臨床上のポイント： 半減期が非常に長い（平均16〜17日）ため、副作用が発生した場合、休薬後も数週間にわたって持続する可能性があります。したがって、慎重な患者選択が不可欠であり、通常は急性疼痛ではなく慢性の変形性関節症の管理に限定して使用されます。
作用機序
Mavacoxib is a COX-2 selective inhibitor (coxib).
- Arachidonic Acid Cascade: It selectively inhibits the cyclooxygenase-2 (COX-2) enzyme → decreases the production of pro-inflammatory prostaglandins (such as PGE2) → reduces pain, inflammation, and fever.
- COX-1 Sparing: At therapeutic dosages, it relatively spares COX-1, the constitutive enzyme responsible for synthesizing prostaglandins that protect the gastric mucosa, support platelet function, and maintain normal renal blood flow. However, COX-selectivity is relative and can be lost at higher doses or in susceptible individuals.
安全性・警告
禁忌
- Dogs less than 12 months of age
- Dogs less than 5 kg body weight
- Gastrointestinal disorders including ulceration and bleeding
- Evidence of a hemorrhagic disorder
- Impaired renal or hepatic function
- Cardiac insufficiency
- Hypersensitivity to mavacoxib, sulfonamides, or excipients
- Pregnant, breeding, or lactating animals
- Dehydrated, hypovolemic, or hypotensive animals
- Dehydrated, hypovolaemic, or hypotensive patients
- Gastrointestinal disease or ulceration
- Blood clotting disorders
- Liver disease (prolongs metabolism and causes accumulation)
- Renal disease (requires careful evaluation, generally avoid)
- Pregnant or lactating animals
- Dogs < 12 months of age
- Dogs < 5 kg body weight
- Cats
有害事象
- Inappetence
- Diarrhea
- Depression
- Gastrointestinal ulceration or bleeding
- Vomiting and diarrhoea
- Renal toxicity (especially if dehydrated or hypotensive)
- Hepatic accumulation (in poor metabolizers)
- Theoretical risk of precipitating cardiac failure
注意事項
Do not use concomitantly with glucocorticoids or other NSAIDs. Do not administer other NSAIDs within 1 month of the last administration of mavacoxib. Avoid use in any dehydrated, hypovolemic, or hypotensive animal, as there is a potential risk of increased renal toxicity. Concurrent administration of potentially nephrotoxic medicinal products should be avoided. Animals should not become dehydrated when receiving this or other NSAIDs.
医薬品相互作用
NSAIDs can reduce effects on blood pressure and potentially reduce renal blood flow, increasing the risk for renal injury.
May increase the risk of gastrointestinal toxicity (ulceration, bleeding, vomiting, diarrhea). Long washout periods are warranted when switching.
May increase the risk of gastrointestinal toxicity (ulceration, bleeding, vomiting, diarrhea). Concurrent use is contraindicated.
NSAIDs may increase serum levels of digoxin.
May increase plasma levels of mavacoxib (extrapolated from celecoxib data in humans).
NSAIDs may reduce saluretic and diuretic effects.
Serious toxicity has occurred when NSAIDs have been used concomitantly; use together with extreme caution.
May enhance the risk of nephrotoxicity development.
May increase the risk of gastrointestinal toxicity. Do not administer other NSAIDs within 1 month of the last administration of mavacoxib.
Increased risk of severe gastrointestinal ulceration and bleeding.
Increased risk of nephrotoxicity.
Synergistic risk of acute kidney injury.
監視
- Baseline and periodic CBC and serum chemistry (including BUN/serum creatinine, and liver function assessment)
- Baseline history and physical
- Efficacy of therapy
- Adverse effect monitoring via client
- Baseline and periodic renal function (BUN, Creatinine, SDMA, USG)
- Baseline and periodic hepatic function (ALT, ALP, Bilirubin)
- Clinical signs of GI ulceration (vomiting, melaena, anorexia)
- Hydration status and blood pressure (especially during anaesthesia)
薬物動態
半減期
吸収
Average bioavailability after oral dosing is about 46% when fasted, but nearly doubles (87%) when given with food. Peak levels occur in about 11 hours.
分布
Apparent volume of distribution (steady-state) averaged 1.6 L/kg. Highly bound to canine plasma proteins (98%).
代謝
Primarily cleared by biliary excretion.
消失
Total body clearance is a very low 2.7 mL/hour/kg.
過剰投与
In safety studies, repeated doses of 5 and 10 mg/kg did not demonstrate adverse events. At 15 mg/kg, vomiting, softened/mucoid feces, and decreased renal function were noted. Doses of 25 mg/kg caused GI ulceration, with one fatality from GI perforation and peritonitis.
- Management: Manage as with other NSAID toxicity (emetics, activated charcoal, GI protectants, fluid diuresis).
- Important: Because of the drug's very long duration of effect, prolonged monitoring and treatment may be required. Consulting a veterinary poison center is highly recommended.
製品
製剤
- Oral chewable tablets
- 6 mg chewable tablet
- 20 mg chewable tablet
- 30 mg chewable tablet
- 75 mg chewable tablet
- 95 mg chewable tablet
動物用医薬品
- Mavacoxib Oral Chewable Tablets: 6 mg, 20 mg, 30 mg, 75 mg, & 95 mg (Trocoxil)
- Trocoxil 6 mg chewable tablets
- Trocoxil 20 mg chewable tablets
- Trocoxil 30 mg chewable tablets
- Trocoxil 75 mg chewable tablets
- Trocoxil 95 mg chewable tablets
規制ステータス
Authorized for use in dogs >= 12 months old.
POM-V classification.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
Store in the original packaging at room temperature out of reach of pets and children.
飼主向け情報
重要： これは毎日服用する薬ではありません。獣医師の指示通りのスケジュール（通常、1日目、14日目に投与後、厳密に月1回）で正確に投与してください。余分に投与しないでください。
- 食事と一緒に投与： 犬の1日で最も量の多い食事と一緒に与えてください。食事と一緒に与えることで、胃からの吸収が大幅に向上します。
- 副作用の観察： 食欲不振、嘔吐、血便や黒色便、行動の変化、飲水量や尿量の変化に気づいた場合は、直ちに獣医師に連絡してください。注意：この薬は体内に長く留まるため、最後の投与から数週間後に副作用が現れる可能性があります。
- 安全な保管： このチュアブル錠は犬にとって非常に好ましい味がします。誤飲による過剰摂取を防ぐため、すべてのペットや子供の手の届かない場所に厳重に保管してください。
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。