エスモロール
Esmolol
Esmolol hydrochloride
別名: Brevibloc · Miniblock · ASL-8052 · Esmolol HCl · Esmololum · Esmolol hydrochloride
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| Ultra-short acting beta blockade (ventricular arrhythmias) - Normal cardiac function | An initial loading dose of 0.25-0.5 mg/kg (250-500 micrograms/kg) administered IV as slow bolus over 1-2 minutes, then followed by a constant rate infusion of 10-200 micrograms/kg/minute; or Start CRI at 10-200 micrograms/kg/minute without the bolus loading dose. | IV | CRI | — | 🌎 NA |
| Ultra-short acting beta blockade - Severe dilated cardiomyopathy or severe mitral regurgitation | Start CRI at 10-20 micrograms/kg/min and titrate upward every 10 minutes to an effective endpoint. | IV | CRI | — | 🌎 NA |
| SVTs | 0.05-0.1 mg/kg (50-100 micrograms/kg) IV bolus over 2 minutes; repeat every 5 minutes to a maximum of 0.5 mg/kg (500 micrograms/kg). | IV | q5m | — | 🌎 NA |
| Arrhythmia conversion | Give in incremental IV bolus doses of 0.05-0.1 mg/kg every 5 minutes up to a maximum dose of 0.5 mg/kg. | IV | q5m | — | 🌎 NA |
- Ultra-short acting beta blockade (ventricular arrhythmias) - Normal cardiac function: If no loading dose, maximal effect should occur in 10-20 minutes.
- Ultra-short acting beta blockade - Severe dilated cardiomyopathy or severe mitral regurgitation: Do not give loading dose.
- Arrhythmia conversion: Because esmolol's effects are short-lived, if arrhythmia conversion does not occur, other negative inotropes (e.g., diltiazem, or verapamil) can be safely used 30 minutes after esmolol.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| HCM (to determine if beta-blockers will reduce dynamic left-ventricular outflow tract obstruction) | An initial loading dose of 0.25-0.5 mg/kg (250-500 micrograms/kg) administered IV as slow bolus over 1-2 minutes, then followed by a constant rate infusion of 10-200 micrograms/kg/minute. | IV | CRI | — | 🌎 NA |
| Critical Arrhythmias | Loading dose of 200-500 micrograms/kg IV over 1 minute; followed by a constant rate IV infusion of 25-200 micrograms/kg/minute | IV | CRI | — | 🌎 NA |
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
エスモロールは、超短時間作用型で心臓選択性のあるベータ1アドレナリン受容体拮抗薬です。
獣医療では主に、心房細動、心房粗動、洞性頻脈などの上室性頻脈性不整脈（SVT）の急性かつ短期的な管理のための静脈内持続点滴として使用されます。また、より長時間作用する経口ベータ遮断薬に移行する前に、ベータ遮断薬療法が有効かつ忍容性があるかを判断するための診断用テスト薬としても非常に有用です。これは特に肥大型心筋症（HCM）の猫において、ベータ遮断が動的左室流出路狭窄を軽減するかどうかを評価するのに役立ちます。
臨床のポイント: エスモロールは赤血球のエステラーゼによって急速に代謝されるため、点滴終了後10〜20分以内に効果が消失します。そのため、重症患者における試験的治療において極めて安全性が高い薬剤です。
作用機序
Esmolol competitively blocks beta-1 adrenergic receptors in the myocardium with minimal to no effect on beta-2 receptors at clinical doses.
- Negative Chronotropy: Decreases heart rate by slowing sinoatrial (SA) node firing and increasing sinus cycle length.
- Negative Dromotropy: Slows conduction velocity through the atrioventricular (AV) node and prolongs sinus node recovery time.
- Negative Inotropy: Decreases myocardial contractility, which reduces myocardial oxygen demand.
Unlike propranolol, esmolol lacks intrinsic sympathomimetic activity (ISA) and does not possess membrane-stabilizing (quinidine-like) or bronchoconstrictive effects.
安全性・警告
禁忌
- Overt cardiac failure
- 2nd or 3rd degree AV block
- Sinus bradycardia
- Cardiogenic shock
- Second or third-degree AV block
- Uncompensated congestive heart failure
- Hypotension
有害事象
- Hypotension
- Bradycardia
- Heart block
- Exacerbation of congestive heart failure
- Bronchospasm (at high doses where beta-1 selectivity is lost)
注意事項
Use with caution (weigh benefit vs. risk) in patients with congestive heart failure (CHF), bronchoconstrictive lung disease, or diabetes mellitus. Esmolol may mask certain clinical signs of developing hypoglycemia (such as increased heart rate or blood pressure).
医薬品相互作用
Esmolol may increase serum digoxin levels up to 20%, but these drugs have been used together safely and effectively.
Concurrent use is not recommended due to potential risk of hypertension.
May increase steady-state esmolol serum concentrations up to 50%; titrate esmolol dosage carefully.
May see additive effects (hypotension, bradycardia) if used with esmolol.
If systemic vascular resistance is high, there is an increased risk for blocked cardiac contractility; esmolol is not recommended to control SVTs in patients receiving these drugs.
In humans, particularly with severe cardiomyopathy, cardiac arrest has occurred (rarely).
Additive negative inotropic and chronotropic effects; risk of severe bradycardia and hypotension
Increased risk of severe bradycardia
Mutual antagonism
Additive negative inotropic and chronotropic effects, increasing risk of severe bradycardia and hypotension.
監視
- Continuous Electrocardiogram (ECG)
- Direct or indirect blood pressure
- Heart rate and rhythm
- Clinical signs of heart failure
薬物動態
半減期
吸収
Steady-state blood levels occur in about 5 minutes if a loading dose was given or about 30 minutes if no load was given.
分布
Rapidly and widely distributed but not appreciably to the CNS, spleen or testes. The distribution half-life is about 2 minutes. It is unknown whether the drug crosses the placenta or enters milk.
代謝
Rapidly metabolized in the blood by esterases to a practically inactive metabolite.
消失
Renal or hepatic dysfunction do not appreciably alter elimination characteristics.
過剰投与
The IV LD50 in dogs is approximately 32 mg/kg.
- 2 mg/kg/min for 1 hour: No adverse effects.
- 3 mg/kg/min for 1 hour: Produced ataxia and salivation.
- 4 mg/kg/min for 1 hour: Caused muscular rigidity, tremors, seizures, ptosis, vomiting, hyperpnea, vocalizations, and prostration.
Management: These effects all resolved within 90 minutes of the end of infusion. Because of the short duration of action of the drug, discontinuation or dosage reduction may be all that is required; otherwise, symptomatic and supportive treatment may be initiated.
製品
製剤
- Injection
- Injectable: 10 mg/ml solution
ヒト用医薬品
- Esmolol HCl Injection: 10 mg/mL regular & preservative free in 10 mL vials
- Esmolol HCl Injection: 20 mg/mL preservative free in 5 mL vials & 100 mL bags
- Esmolol HCl Injection: 250 mg/mL in 10 mL ampules
- Brevibloc 10 mg/ml solution for injection
規制ステータス
POM (Prescription Only Medicine). Human-approved drug used under the cascade.
POM (Prescription Only Medicine). Human-approved drug used under the cascade.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
The concentrate for injection should be stored at room temperature; do not freeze and protect from excessive heat. After diluted to a concentration of 10 mg/mL esmolol HCl is stable (at refrigeration temperatures or room temperature) for at least 24 hours in commonly used IV solutions.
飼主向け情報
エスモロールは、動物病院内でのみ投与される救急用の超短時間作用型薬剤です。
- 継続的なモニタリング: この薬剤の投与中、ペットは心電図（ECG）や血圧計によって注意深く監視されます。
- 目的: 危険な不整脈を急速に安定させるため、あるいはペットの心臓の状態が長時間作用型の経口ベータ遮断薬に良好に反応するかを確認するための「テスト」としてよく使用されます。
- 安全性: 数分で血中から消失するため、低血圧や徐脈などの副作用が生じても、点滴を止めれば通常は非常に早く回復します。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。