異丙腎上腺素
Isoproterenol
Isoproterenol hydrochloride
別名: Isuprel · Imuprel · Isolin · Lenoprel · Norisodrine Aerotrol · Proterenal · Saventrine · Vapo-iso · Isoprenaline hydrochloride · Isopropylarterenol hydrochloride · Isopropylnoradrenaline 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。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Sinoatrial arrest, sinus bradycardia, complete AV block | 0.4 mg in 250 mL D5W drip slowly to effect | IV | to effect | — | 🌎 NA |
| Sinoatrial arrest, sinus bradycardia, complete AV block | Isuprel Glossets 5-10 mg | sublingual or rectal | q4-6h | — | 🌎 NA |
| Sinoatrial arrest, sinus bradycardia, complete AV block | 0.04-0.08 micrograms/kg/min | IV | CRI | — | 🌎 NA |
| Sinoatrial arrest, sinus bradycardia, complete AV block | 0.1-0.2 mg | IM, SC | q4h | — | 🌎 NA |
| Sinoatrial arrest, sinus bradycardia, complete AV block | 0.4 mg in 250 mL D5W slowly | IV | slowly | — | 🌎 NA |
| Adjunctive treatment for bradycardia associated with calcium channel blocker overdose | Mix 0.4 mg in 250 mL of D5W and give via slow IV drip to effect. | IV | to effect | — | 🌎 NA |
- Sinoatrial arrest, sinus bradycardia, complete AV block: Infusion
- Adjunctive treatment for bradycardia associated with calcium channel blocker overdose: Alternative to atropine
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Sinoatrial arrest, sinus bradycardia, complete AV block | 0.4 mg in 250 mL D5W drip slowly to effect | IV | to effect | — | 🌎 NA |
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Short-term bronchodilatation | Dilute 0.2 mg in 50 mL of saline and administer 0.4 micrograms/kg as an IV infusion, monitor heart rate continuously and discontinue when heart rate doubles. | IV | once | Effects may only last for an hour | 🌎 NA |
- Short-term bronchodilatation: ARCI UCGFS Class 2 Drug
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。
概覽
異丙腎上腺素 (Isoproterenol) 是一種強效的非選擇性 β-腎上腺素受體激動劑，主要用於獸醫急診醫學。
主要臨床特徵包括：
- 心臟支持： 用於治療嚴重的緩慢型心律不整，如完全性房室傳導阻滯或竇房結停搏，藉由增加心率和心肌收縮力來發揮作用。
- 支氣管擴張： 過去曾用於急性支氣管收縮，但目前已大多被更具選擇性的 $\beta_2$ 激動劑（如特布他林或沙丁胺醇）取代，以避免心臟副作用。
- 休克/心臟衰竭： 偶爾作為輔助治療，但由於其強烈的致心律不整潛力及引起心搏過速的傾向，使用受到限制。
臨床要點： 由於其強烈的心臟刺激特性，加上目前已有更安全、更具針對性的療法（例如用於房室傳導阻滯的心律調節器，或用於氣喘的選擇性支氣管擴張劑），異丙腎上腺素目前已較少使用。它的作用時間非常短，這意味著一旦停止輸注，副作用會迅速消退。
作用機制
Isoproterenol is a synthetic sympathomimetic amine that acts as a potent, non-selective agonist at both $\beta_1$ and $\beta_2$ adrenergic receptors, with virtually no $\alpha$-adrenergic activity.
Mechanism Pathway: Drug binds to $\beta_1$ and $\beta_2$ receptors → activates Gs-proteins → stimulates adenylyl cyclase → increases intracellular cyclic-AMP (cAMP) → activates Protein Kinase A (PKA).
- Cardiac Effects ($\beta_1$): Increased cAMP leads to increased intracellular calcium influx → positive inotropy (increased contractility) and positive chronotropy (increased heart rate and pacemaker discharge rate).
- Smooth Muscle Effects ($\beta_2$): Increased cAMP inhibits myosin light-chain kinase (MLCK) → relaxation of bronchial smooth muscle (bronchodilation) and peripheral vasculature (vasodilation).
- Immunologic Effects: Inhibits the antigen-mediated release of histamine and slow-releasing substance of anaphylaxis (SRS-A).
安全性與警告
禁忌症
- Tachycardias or AV block caused by cardiac glycoside (digoxin) intoxication
- Ventricular arrhythmias that do not require increased inotropic activity
不良反應
- Tachycardia
- Ventricular arrhythmias (highly arrhythmogenic)
- Anxiety and excitability
- Tremors
- Headache
- Weakness
- Vomiting
注意事項
Warning: Isoproterenol is highly arrhythmogenic (more so than dopamine or dobutamine). Use with extreme caution.
- Disease States: Use with caution in patients with coronary insufficiency, hyperthyroidism, renal disease, hypertension, or diabetes.
- Shock: Isoproterenol is not a substitute for adequate fluid replacement in shock.
- Pregnancy: FDA Category C. Animal studies show adverse fetal effects. Use cautiously as a last resort when benefits clearly outweigh risks.
- Lactation: Rapidly deactivated in the gut, so it is unlikely to pose much risk to nursing offspring.
藥物相互作用
Increased risk of developing arrhythmias. Propranolol may be administered should these occur.
May antagonize isoproterenol's cardiac, bronchodilating, and vasodilating effects. Can be used to treat isoproterenol-induced tachycardia, but use with caution in bronchospastic disease.
Increased risk of arrhythmias.
Hypertension may result if used concurrently.
Should not be administered concurrently as increased toxicity may result.
May increase the risk for theophylline toxicity.
監測
- Cardiac rate and rhythm (ECG continuous monitoring highly recommended)
- Respiratory rate and auscultation (especially during anaphylaxis)
- Blood pressure
- Blood gases (if indicated and possible)
- Urine flow (if possible)
藥物動力學
吸收
Rapidly inactivated by the GI tract. Sublingual administration is not reliably absorbed (effects may take up to 30 minutes). IV administration results in immediate effects, but only persists for a few minutes after discontinuation.
分佈
Unknown if distributed into milk. Pharmacologic actions are ended primarily through tissue uptake.
代謝
Metabolized in the liver and other tissues by catechol-O-methyltransferase (COMT) to a weakly active metabolite.
排除
Primarily cleared via tissue uptake and enzymatic metabolism (COMT).
過量
High doses may cause an initial hypertension, followed by hypotension, as well as severe tachycardias and other arrhythmias.
Treatment:
- Halt or reduce the drug infusion (effects dissipate rapidly due to short half-life).
- Provide supportive care.
- If tachycardias persist, a beta-blocker could be considered for treatment, provided the patient does not have a bronchospastic disease.
可用產品
劑型
- Injection
- Sublingual tablets (historical)
- Rectal suppositories (historical)
人用標示
- Isoproterenol HCl for Injection: 1:5000 solution (0.2 mg/mL) 5 mL & 10 mL vials
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store in tight, light-resistant containers. Stable indefinitely at room temperature. Salts will darken with time upon exposure to air, light, or heat. Solutions may become pink or brownish-pink if exposed to air, alkalies, or metals. Do not use solutions that are discolored or contain a precipitate. If mixed with other drugs/fluids resulting in a pH > 6, use immediately.
飼主須知
寵物主人重要須知
- 僅限急診使用： 異丙腎上腺素是一種強效、速效的急救藥物。它只能由受過訓練的獸醫專業人員在醫院環境中給藥，並需持續監測您寵物的心率和血壓。
- 用途： 通常作為挽救生命的措施，用於治療危及生命的緩慢心率（心臟傳導阻滯）或（極少數情況下）嚴重的氣喘危機。
- 作用迅速： 藥物會立即生效，但一旦停止靜脈點滴，藥效會在幾分鐘內消退。這使得獸醫能夠精確控制其效果。
- 副作用： 由於它會強烈刺激心臟，可能會引起心跳過速、焦慮或發抖。獸醫團隊會密切監測這些情況，並在需要時立即調整劑量。
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