グラピプラント
グラピプラントは、ピプラントクラスに属する非ステロイド性、非シクロオキシゲナーゼ(COX)阻害性の抗炎症薬です。プロスタグランジンE2(PGE2)によって引き起こされる疼痛および炎症の主要なメディエーターである**EP4受容体**を特異的に遮断します。 > **臨床のポイント:** COX酵素を阻害しないため、理論的には胃腸、腎臓、血小板の恒常性に関与する有益なプロスタグランジンの産生を維持し、長期的な変形性関節症の管理においてより安全なプロファイルを提供する可能性があります。
作用機序: Grapiprant is a highly selective **EP4 receptor antagonist**. Arachidonic acid → COX enzymes → PGE2 → binds to **EP4 receptors** (mediating pain/inflammation). By blocking the EP4 receptor, grapiprant inhibits PGE2-mediated vasodilation, vascular permeability, and sensory nerve sensitization without disrupting the synthesis of PGE2 or other prostanoids.
動物種別の用量
- Management of mild to moderate pain caused by osteoarthritis · 2 mg/kg · PO · sid · As directed by veterinarian · For dogs >9 months of age and >3.6 kg.
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
- Hypersensitivity to grapiprant
- Concurrent use with other NSAIDs or corticosteroids
- Breeding, pregnant, or lactating dogs
- Dogs under 9 months of age or weighing less than 3.6 kg
- Dogs under 9 months of age
- Dogs weighing less than 3.6 kg
- Cats (not authorized for use)
- Known hypersensitivity to grapiprant
有害事象
- Vomiting
- Diarrhea
- Anorexia
- Lethargy
- Decreased serum albumin
- Soft-formed faeces
- Diarrhoea
- Inappetence
- Mild decreases in serum albumin and total protein
- Haematemesis (very rare)
- Haemorrhagic diarrhoea (very rare)
薬物相互作用
- Other NSAIDs · Increased risk of gastrointestinal toxicity · major
- Corticosteroids · Increased risk of gastrointestinal ulceration · major
- Highly protein-bound drugs · Potential competition for protein binding sites · moderate
- Other NSAIDs (e.g., meloxicam, carprofen) · Increased risk of gastrointestinal toxicity and adverse effects. Concurrent use should be avoided. · major
- Corticosteroids (e.g., prednisolone, dexamethasone) · Increased risk of gastrointestinal ulceration and adverse effects. Concurrent use should be avoided. · major
モニタリング
- Clinical response (pain scoring)
- Fecal consistency
- Appetite
- Baseline and periodic CBC, serum biochemistry (especially albumin, BUN, creatinine, liver enzymes)
- Clinical response to pain management
- Signs of gastrointestinal upset or ulceration (vomiting, diarrhoea, melaena)
- Serum albumin and total protein levels
- Baseline and periodic renal and hepatic panels, especially in older or compromised patients
過量投与
Overdoses up to 15x the recommended dose for 9 months resulted in mild, transient GI signs (vomiting, soft feces) and mild decreases in total protein and albumin. No specific antidote exists; treat symptomatically with GI protectants and supportive care.
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。