格拉匹侖
Grapiprant
N-[[[2-[4-(2-Ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]amino]carbonyl]-4-methylbenzenesulfonamide
別名: Galliprant · CJ-023423 · RQ-00000007
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Management of mild to moderate pain caused by osteoarthritis | 2 mg/kg | PO | sid | As directed by veterinarian | 🌍 EU |
- Management of mild to moderate pain caused by osteoarthritis: 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。請務必對照最新仿單及個別病患確認。
概覽
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。
作用機轉
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.
安全性與警告
禁忌症
- 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 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
- Inappetence
- Mild decreases in serum albumin and total protein
- Haematemesis (very rare)
- Haemorrhagic diarrhoea (very rare)
注意事項
Use with caution in dogs with pre-existing hepatic or renal disease, or those with a history of gastrointestinal disease. Monitor liver enzymes, kidney values, and clinical signs of GI upset.
Clinical Pearl: Although COX-sparing, gastrointestinal adverse effects (vomiting, diarrhea) remain the most commonly reported side effects in clinical practice.
藥物交互作用
Increased risk of gastrointestinal toxicity
Increased risk of gastrointestinal ulceration
Potential competition for protein binding sites
Increased risk of gastrointestinal toxicity and adverse effects. Concurrent use should be avoided.
Increased risk of gastrointestinal ulceration and adverse effects. Concurrent use should be avoided.
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
藥物動力學
半衰期
吸收
Rapidly absorbed following oral administration. Peak plasma concentration (Tmax) is reached within 1-2 hours.
分佈
Highly protein bound (>95%).
代謝
Hepatic metabolism.
排除
Excreted primarily in feces (via bile) and to a lesser extent in urine.
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.
可用產品
劑型
- Oral tablets (20 mg, 60 mg, 100 mg)
- 20 mg oral tablet
- 60 mg oral tablet
- 100 mg oral tablet
獸醫用
- Galliprant 20 mg tablets
- Galliprant 60 mg tablets
- Galliprant 100 mg tablets
各地核准狀態
Approved for control of pain and inflammation associated with osteoarthritis in dogs.
POM-V
POM-V
暫無法規資料: 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR
儲存與穩定性
Store at room temperature (below 30°C/86°F). Keep out of reach of children and animals.
飼主須知
請完全依照獸醫師的指示給予此藥物。可以與食物一起或空腹餵食。
請注意觀察是否有嘔吐、腹瀉或食慾不振等副作用。如果出現這些情況，請停止給藥並聯絡您的獸醫師。
在您的狗狗服用格拉匹侖期間，切勿給予任何其他止痛藥（如阿斯匹靈、布洛芬或其他獸醫用NSAIDs）。
VetSheet 藥物參考供合格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商最新仿單。