マバコキシブ
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.
動物種別の用量
- Any · Do not use · PO · N/A · N/A · Contraindicated in cats.
- 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). · 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) · 2 mg/kg · PO · q14d for 2 doses, then q1month · Maximum of 7 doses total · 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.
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
- 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
有害事象
- Inappetence
- Diarrhea
- Vomiting
- Depression
- Renal toxicity
- Gastrointestinal ulceration
- 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
薬物相互作用
- ACE Inhibitors (e.g., enalapril, benazepril) · NSAIDs can reduce effects on blood pressure and potentially reduce renal blood flow, increasing the risk for renal injury.
- Aspirin · May increase the risk of gastrointestinal toxicity (ulceration, bleeding, vomiting, diarrhea). Long washout periods are warranted when switching.
- Corticosteroids (e.g., prednisone) · May increase the risk of gastrointestinal toxicity (ulceration, bleeding, vomiting, diarrhea). Concurrent use is contraindicated.
- Digoxin · NSAIDs may increase serum levels of digoxin.
- Fluconazole · May increase plasma levels of mavacoxib (extrapolated from celecoxib data in humans).
- Furosemide · NSAIDs may reduce saluretic and diuretic effects.
- 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 · May increase the risk of gastrointestinal toxicity. Do not administer other NSAIDs within 1 month of the last administration of mavacoxib. · major
- Glucocorticoids · Increased risk of severe gastrointestinal ulceration and bleeding. · major
- Aminoglycosides · Increased risk of nephrotoxicity. · major
モニタリング
- 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)
過量投与
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.
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。