格拉匹侖
格拉匹侖（Grapiprant）是一種非類固醇、非環氧合酶（COX）抑制劑的抗發炎藥物，屬於piprant類。它專一性地阻斷**EP4受體**，這是前列腺素E2（PGE2）引發疼痛和發炎的主要媒介。 > **臨床提示：** 由於它不抑制COX酵素，理論上格拉匹侖能保留參與胃腸道、腎臟和血小板恆定性的有益前列腺素，為長期的骨關節炎管理提供更安全的選擇。
作用機制: 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.
各物種劑量
- 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.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新藥品仿單及個別病患確認。
給藥途徑
禁忌症
- 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
不良反應
- 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)
藥物相互作用
- 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
監測
- 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
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 藥物參考供持牌獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠方最新藥品說明書。