ディルロタピド
ディルロタピドは、犬の肥満管理に特化して使用される選択的**腸管ミクロソームトリグリセリド転送タンパク質（GMTP）阻害薬**です。主に消化管で局所的に作用し、食事からの脂肪吸収を抑え、満腹感を促進することで、食欲や食べ物をねだる行動を効果的に減少させます。 > **臨床上のポイント：** ディルロタピドは、毎週の減量目標に基づいた、数学的に計算された厳密な投与プロトコルを必要とします。急激な減量による猫の肝リピドーシス（脂肪肝）を誘発するリスクが高いため、猫への使用は**厳禁**です。 この薬は全身に吸収されますが、主な有効性は腸管での局所作用によるものです。全身への吸収は減量効果よりも副作用（毒性）と強く相関します。長期的な体重管理を成功させるには、食事や生活習慣の改善を併用する必要があります。
作用機序: 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.
動物種別の用量
- 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.
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
- 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)
有害事象
- Vomiting (especially during the first month or 3-4 hours post-dose)
- Diarrhea
- Lethargy
- Anorexia
- Salivation
- Constipation
- Dehydration
- Elevated serum hepatic transaminases
薬物相互作用
- 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.
モニタリング
- Patient weight (monthly, to guide dose adjustments)
- Adverse gastrointestinal effects (vomiting, diarrhea, anorexia)
- Liver enzymes (baseline and occasional monitoring)
過量投与
**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.*
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。