地洛他派
Dirlotapide
5-[(4'-trifluoromethyl-biphenyl-2carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide
別名: Slentrol · CP-742,033
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 |
|---|---|---|---|---|---|
| Weight Loss Phase (First 14 days) | 0.01 mL/kg (0.05 mg/kg) | PO | q24h | 14 days | 🌎 NA |
| Weight Loss Phase (Days 15 to 28) | 0.02 mL/kg (0.1 mg/kg) | PO | q24h | 14 days | 🌎 NA |
| Weight Loss Phase (Subsequent Months) | Adjust volume monthly to maintain a target percent weight loss of ≥ 0.7% per week. Max dose: 0.2 mL/kg (0.09 mL/lb) | PO | q24h | Until desired weight is reached | 🌎 NA |
| Weight Management Phase | Adjust dose volume by -50%, 0%, or +50% based on last month's weight loss, then +/- 25% in subsequent months. Max dose: 0.2 mL/kg (0.09 mL/lb) | PO | q24h | 3 months recommended | 🌎 NA |
- Weight Loss Phase (First 14 days): Initial assessment required prior to therapy.
- Weight Loss Phase (Days 15 to 28): Double the initial dose volume.
- Weight Loss Phase (Subsequent Months): If target not met: increase dose by 100% (first adjustment) or 50% (subsequent adjustments). If food consumption is greatly reduced, withhold 1-2 days.
- Weight Management Phase: Establish optimal food intake and physical activity to stabilize body weight.
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
地洛他派 (Dirlotapide) 是一種選擇性腸道微粒體三酸甘油酯轉移蛋白 (GMTP) 抑制劑，專門用於犬隻的肥胖管理。它主要在胃腸道局部作用，減少膳食脂肪吸收並促進飽足感，有效降低食慾和乞食行為。
臨床要點： 地洛他派需要基於每週減重目標進行高度結構化、經數學計算的劑量調整方案。由於快速減重會引發貓咪脂肪肝的高風險，因此嚴禁用於貓隻。
雖然該藥物會被全身吸收，但其主要療效來自於腸道的局部作用。全身吸收程度與不良反應（毒性）的相關性較高，而與減重療效的相關性較低。成功的長期體重管理需要同時配合飲食和生活方式的改變。
作用機轉
Dirlotapide selectively inhibits microsomal triglyceride transfer protein (GMTP) in the enterocytes of the gut.
- Lipid Blockade: Inhibits GMTP → blocks the assembly and release of lipoproteins into systemic circulation → reduces dietary fat absorption.
- Satiety Signaling: The accumulation of lipids within enterocytes triggers the release of Peptide YY (PYY) into the systemic circulation → signals the central nervous system to decrease appetite and induce satiety.
- Action Site: Primarily acts locally in the gut. Systemic blood levels do not directly correlate with efficacy, but rather with systemic toxicity.
安全性與警告
禁忌症
- Cats (high risk of hepatic lipidosis)
- Dogs with liver disease
- Dogs receiving long-term corticosteroid therapy
- Unmanaged endocrine disease (e.g., hyperadrenocorticism/Cushing's disease)
不良反應
- Vomiting (especially during the first month or 3-4 hours post-dose)
- Diarrhea
- Lethargy
- Anorexia
- Salivation
- Constipation
- Dehydration
- Elevated serum hepatic transaminases
注意事項
Important Precautions:
- Species Restriction: Do NOT use in cats. Rapid weight loss in obese cats significantly increases the risk of fatal hepatic lipidosis.
- Endocrine Disease: Pre-existing endocrine diseases (like Cushing's or hypothyroidism) must be managed prior to initiating dirlotapide therapy.
- Duration of Use: Safe use for longer than one year has not been evaluated.
- Reproductive Safety: Safety in breeding, pregnant, or lactating dogs has not been established.
- Hepatic Effects: May cause mild to moderate elevations in serum hepatic transaminases early in treatment.
藥物交互作用
Potential altered absorption rate and extent; administer at least 2 hours prior to dirlotapide.
Decreased plasma concentrations during the initial treatment phase; levels typically stabilize and recover during the weight stabilization phase.
監測
- Patient weight (monthly, to guide dose adjustments)
- Adverse gastrointestinal effects (vomiting, diarrhea, anorexia)
- Liver enzymes (baseline and occasional monitoring)
藥物動力學
半衰期
吸收
Highly variable (22-41%). Presence of food in the gut increases bioavailability.
分佈
Highly protein bound. Volume of distribution (Vd) is 1.3 L/kg.
代謝
Systemically absorbed drug is metabolized in the liver.
排除
Excreted primarily in bile (undergoes enterohepatic circulation) and feces. Renal excretion accounts for <1%.
過量
Toxicity Profile: Oral doses of 0.5, 1, and 2 mL/kg (2.5X, 5X, and 10X the maximum labeled dose) administered to normal weight Beagles for two weeks were generally tolerated.
Clinical Signs of Overdose:
- Vomiting and diarrhea
- Anorexia and lethargy
- Transient elevations in liver enzymes (transaminases)
Note: No histopathologic evidence of hepatic necrosis was observed at these doses.
可用產品
劑型
- Oral solution
獸醫用
- Dirlotapide Oral Solution 5 mg/mL (Slentrol)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store in the original container at room temperature 15-30°C (59-86°F).
飼主須知
寵物主人重要須知：
- 並非萬靈丹： 地洛他派透過降低食慾和減少脂肪吸收來幫助您的狗狗減重。然而，成功的長期體重管理需要永久改變飲食和運動習慣。
- 暫時性效果： 食慾降低是暫時的，在停藥後 1-2 天內就會消失。如果在停藥後不控制進食量，您的狗狗將會復胖。
- 副作用： 約有四分之一的狗狗偶爾會出現嘔吐或腹瀉，通常發生在治療的第一個月或增加劑量後。如果發生嘔吐，您可以嘗試在不同時間給藥，或改變與食物一起給予的方式。
- 何時該聯絡獸醫： 如果您的狗狗完全不吃東西超過一天，或者嘔吐嚴重或持續超過 2 天，請聯絡您的獸醫師。
- 給藥方式： 請使用隨附的口服給藥針筒。可以直接餵入狗狗口中，或滴在少量食物上。使用後請用乾布將針筒擦拭乾淨——請勿用水清洗。
- 安全警告： 請放置於兒童接觸不到的地方。如果不慎接觸到眼睛，請立即用清水沖洗。
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