リシノプリル
リシノプリルは**アンジオテンシン変換酵素(ACE)阻害薬**であり、獣医療においては主に**うっ血性心不全(CHF)**および**全身性高血圧**の管理における血管拡張薬として使用されます。 主な臨床的特徴: * **直接活性型**:エナラプリルとは異なり、リシノプリルはプロドラッグではないため、活性化のために肝臓での生体内変化を必要としません。これは重度の肝機能障害を併発している患者において有利となる可能性があります。 * **1日1回投与**:他のいくつかのACE阻害薬と比較して作用時間が長いため、多くの患者で便利な1日1回投与が可能です。 * **腎保護作用**:慢性腎臓病(CKD)や蛋白漏出性腎症の患者において、蛋白尿を減少させ、腎機能を維持するためにしばしば使用されます。 * **血行動態への利点**:総末梢血管抵抗、肺血管抵抗、および肺毛細血管楔入圧を低下させると同時に、心拍出量と運動耐容能を増加させます。 > **臨床のポイント**:獣医療ではエナラプリルやベナゼプリルの方が一般的に使用され、広く研究されていますが、リシノプリルは特に1日1回投与が好まれる場合において、有効で多くの場合より安価な代替薬となります。
作用機序: Lisinopril exerts its effects by interfering with the **Renin-Angiotensin-Aldosterone System (RAAS)**. * **Mechanism**: It competitively binds to and inhibits **angiotensin-converting enzyme (ACE)**. * **Pathway**: **Angiotensin I** → (blocked by ACE inhibition) → Decreased **Angiotensin II**. * **Physiological Effects**: 1. **Vasodilation**: Reduction in Angiotensin II (a potent vasoconstrictor) leads to decreased systemic vascular resistance (afterload) and venous tone (preload). 2. **Decreased Aldosterone**: Lower Angiotensin II levels reduce the secretion of **aldosterone** from the adrenal cortex → decreased sodium and water retention. 3. **Bradykinin Preservation**: ACE is also responsible for the breakdown of bradykinin. Inhibition leads to increased bradykinin levels, contributing to vasodilation (but also potentially causing a mild cough). * **Net Result**: Decreased blood pressure, reduced cardiac workload, and decreased proteinuria due to efferent arteriolar vasodilation in the glomerulus.
動物種別の用量
- Adjunctive treatment of heart failure · 0.25-0.5 mg/kg · PO · q24h
- Adjunctive treatment of heart failure · 0.5 mg/kg · PO · q12-24h
- Adjunctive treatment of heart failure · 0.5 mg/kg · PO · q24h
- Adjunctive treatment of heart failure · 0.25-0.5 mg/kg · PO · q24h · Highest recommended doses should be used unless not tolerated by patient.
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
- Known hypersensitivity to ACE inhibitors
- Pregnancy (especially 2nd and 3rd trimesters)
有害事象
- Anorexia
- Vomiting
- Diarrhea
- Lethargy or weakness
- Hypotension
- Renal dysfunction (azotemia)
- Hyperkalemia
- Cough (rare in animals compared to humans)
薬物相互作用
- Antidiabetic Agents (insulin, oral agents) · Possible increased risk for hypoglycemia; enhanced monitoring recommended.
- Diuretics (e.g., furosemide, hydrochlorothiazide) · Potential for increased hypotensive effects; reducing furosemide doses (by 25-50%) is often recommended when initiating ACE inhibitors in CHF.
- Potassium-Sparing Diuretics (e.g., spironolactone, triamterene) · Increased risk of hyperkalemia; enhanced monitoring of serum potassium recommended.
- Other Hypotensive Agents · Potential for additive hypotensive effects.
- Lithium · Increased serum lithium levels possible; increased monitoring required.
- NSAIDs · May reduce the anti-hypertensive or positive hemodynamic effects of lisinopril; may increase the risk of acute renal failure.
- Potassium Supplements · Increased risk for hyperkalemia.
モニタリング
- Clinical signs of CHF (respiratory rate/effort, exercise tolerance)
- Blood pressure (especially upon initiation or dose changes)
- Serum electrolytes (specifically potassium)
- Renal panel (BUN, Creatinine)
- Urine protein
- Periodic CBC with differential
過量投与
The primary concern with overdosage is **hypotension**. * **Toxicity Thresholds**: In dogs, the lowest dosage documented to cause hypotension is 27 mg/kg. Dosages below 20 mg/kg generally cause only mild signs (vomiting, lethargy). In cats, hypotension was noted at 4.9 mg/kg in a single case. In birds, mild somnolence occurred at 41 mg/kg. * **Clinical Signs**: Hypotension, lethargy, vomiting, and tachycardia. * **Treatment**: Recent overdoses should be managed using gut-emptying protocols when warranted. Supportive treatment with **volume expansion using normal saline** is recommended to correct blood pressure. Due to the drug's long duration of action, prolonged monitoring and treatment may be required.
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。