地洛他派
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。
作用機制: 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.
各物種劑量
- Weight Loss Phase (First 14 days) · 0.01 mL/kg (0.05 mg/kg) · PO · q24h · 14 days · Initial assessment required prior to therapy.
- Weight Loss Phase (Days 15 to 28) · 0.02 mL/kg (0.1 mg/kg) · PO · q24h · 14 days · Double the initial dose volume.
- 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 · 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 · 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 · Establish optimal food intake and physical activity to stabilize body weight.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
給藥途徑
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
藥物相互作用
- Narrow therapeutic index oral drugs · Potential altered absorption rate and extent; administer at least 2 hours prior to dirlotapide.
- Fat-soluble vitamins (A, E, K) · 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)
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.*
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