艾司洛爾
Esmolol
Esmolol hydrochloride
別名: Brevibloc · Miniblock · ASL-8052 · Esmolol HCl · Esmololum · Esmolol hydrochloride
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 |
|---|---|---|---|---|---|
| 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.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| 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 |
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
艾司洛爾是一種超短效、具心臟選擇性的Beta-1 腎上腺素受體拮抗劑。
在獸醫學中，它主要作為靜脈輸注，用於急性、短期控制室上性心搏過速 (SVTs)，如心房顫動、心房撲動和竇性心搏過速。它也常被用作診斷性測試藥物，以評估病患在轉換為長效口服 Beta 阻斷劑前，是否能有效且耐受 Beta 阻斷劑治療。這在患有肥厚型心肌病 (HCM) 的貓中特別有用，可評估 Beta 阻斷是否能減少動態左心室出口阻塞。
臨床要點： 由於艾司洛爾會被紅血球酯酶迅速代謝，其作用在停止輸注後 10-20 分鐘內即會消退，這使其在重症病患的試驗性治療中具有極高的安全性。
作用機轉
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.
安全性與警告
禁忌症
- Overt cardiac failure
- 2nd or 3rd degree AV block
- Sinus bradycardia
- Cardiogenic shock
- Second or third-degree AV block
- Uncompensated congestive heart failure
- Hypotension
不良反應
- 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).
藥物交互作用
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.
監測
- Continuous Electrocardiogram (ECG)
- Direct or indirect blood pressure
- Heart rate and rhythm
- Clinical signs of heart failure
藥物動力學
半衰期
吸收
Steady-state blood levels occur in about 5 minutes if a loading dose was given or about 30 minutes if no load was given.
分佈
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.
排除
Renal or hepatic dysfunction do not appreciably alter elimination characteristics.
過量
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.
可用產品
劑型
- Injection
- Injectable: 10 mg/ml solution
人用標示
- 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
各地核准狀態
POM (Prescription Only Medicine). Human-approved drug used under the cascade.
POM (Prescription Only Medicine). Human-approved drug used under the cascade.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
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.
飼主須知
艾司洛爾是一種急救用的超短效藥物，僅在獸醫院環境中施打。
- 持續監測： 您的寵物在接受此藥物時，將會接受心電圖 (ECG) 和血壓設備的密切監測。
- 用途： 它通常用於迅速穩定危險的心律，或作為「測試」，以觀察您的寵物心臟狀況是否對長效口服 Beta 阻斷劑有良好反應。
- 安全性： 因為它在幾分鐘內就會從血液中清除，任何副作用（如低血壓或心跳過慢）通常在停止輸注後會非常迅速地消退。
VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠商最新仿單。