瑞芬太尼

Remifentanil

Remifentanil hydrochloride

超短效鴉片類鎮痛藥IV狗貓

別名: Ultiva · Remicit · GI-87084B · remifentanilo · rémifentanil · remifentanili

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

4 micrograms/kg bolus IV, followed by 6-20 micrograms/kg/hr CRI.IV· CRI

這是依速率計算的持續輸注（CRI）劑量；須計算輸注速率，不能只依體重換算。

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
Analgesic adjunct to general anesthesia	4 micrograms/kg bolus IV, followed by 6-20 micrograms/kg/hr CRI.	IV	CRI	—	🌎 NA
Analgesic adjunct to general anesthesia	1 microgram/kg IV loading dose slowly over 2-3 minutes, followed by a 0.1-0.2 microgram/kg/minute CRI.	IV	CRI	—	🌎 NA

Analgesic adjunct to general anesthesia: Do not confuse mcg/kg/hr with mcg/kg/min.
Analgesic adjunct to general anesthesia: Do not confuse mcg/kg/hr with mcg/kg/min.

貓

適應症	劑量	途徑	頻次	療程	地區
Analgesic adjunct to general anesthesia	0.2 micrograms/kg/minute (for OHE) to 0.3 micrograms/kg/minute (to reduce stimulus-induced movement)	IV	CRI	—	🌎 NA

Analgesic adjunct to general anesthesia: In propofol-anesthetized (0.3 mcg/kg/min) cats.

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。

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概覽

瑞芬太尼 (Remifentanil) 是一種強效、超短效的合成mu-鴉片類促效劑，結構上與芬太尼相似。在獸醫學中，它主要作為全身麻醉期間的鎮痛輔助劑，特別適用於全靜脈麻醉 (TIVA) 方案。

主要藥理特點包括：

非器官依賴性代謝：與大多數依賴肝臟代謝和腎臟排泄的鴉片類藥物不同，瑞芬太尼會被血漿、紅血球和組織中的非特異性酯酶迅速降解。這使其對患有嚴重肝腎功能不全的病患極為安全。
作用消退迅速：其極短的作用時間使得無論輸注時間多長，病患都能快速且可預測地甦醒，減少了其他鴉片類藥物常見的長時間鎮靜副作用。
天花板效應：與其他作為麻醉輔助劑的鴉片類藥物一樣，它具有天花板效應，即增加劑量不會進一步增強鎮痛效果，但可能會增加不良反應。

臨床要點：由於停止輸注後瑞芬太尼不會提供任何殘留的術後鎮痛效果，因此在停止輸注前，必須給予長效鎮痛藥（如 NSAIDs、丁丙諾啡或局部神經阻斷），以防止急性甦醒期譫妄和疼痛。

作用機轉

Remifentanil acts as a selective agonist at mu-opioid receptors (G-protein coupled receptors) located primarily in the pain-regulating areas of the central nervous system (limbic system, spinal cord, thalamus, midbrain).

Mechanism Pathway: Remifentanil binds to mu-receptors → inhibits adenylate cyclase → decreases intracellular cAMP → promotes opening of potassium channels and inhibits voltage-gated calcium channels → hyperpolarization of nociceptive neurons → suppression of substance P release and profound analgesia.

Metabolism: It is rapidly metabolized via hydrolysis of its propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases (not plasma pseudocholinesterase). The principal carboxylic acid metabolite (GR90291) is virtually inactive (4000 times less potent in dogs).

安全性與警告

禁忌症

Hypersensitivity to remifentanil or other fentanyl analogs
Epidural or intrathecal administration (contraindicated due to the presence of glycine in the formulation)

不良反應

Respiratory depression
Apnea
Bradyarrhythmias
Hypotension
Hyperthermia (noted in cats)
Anaphylaxis (rare)

注意事項

Because of the high risk of significant respiratory depression (including apnea) and bradycardia, remifentanil must ONLY be administered in a closely monitored anesthesia care setting with intubation and mechanical ventilation capabilities.

Administration: Continuous infusions should strictly be administered via a calibrated syringe pump or infusion device.
Obesity: In morbidly obese patients, the dosage should be calculated based on ideal body weight rather than actual body weight.
Pregnancy: Weigh potential risks versus benefits. FDA Category C for humans. No teratogenic effects observed in limited animal studies, but fetal respiratory depression is possible.

藥物交互作用

CNS Depressants (e.g., propofol, isoflurane, thiopental)

Additive CNS and respiratory depression; remifentanil significantly reduces MAC and induction agent requirements.

Diuretics

Opiates may decrease diuretic efficacy in patients with congestive heart failure.

Monoamine Oxidase Inhibitors (e.g., amitraz, selegiline)

Severe and unpredictable opiate potentiation may occur; use is generally not recommended if an MAOI has been used within 14 days.

Skeletal Muscle Relaxants

Remifentanil may enhance neuromuscular blockade.

Nitrous Oxide

High doses of remifentanil combined with nitrous oxide may cause cardiovascular depression.

Tricyclic Antidepressants (e.g., clomipramine, amitriptyline)

May exacerbate the effects of tricyclic antidepressants.

Warfarin

Opiates may potentiate anticoagulant activity.

監測

Cardiac rate and rhythm (ECG)
Respiratory rate and depth / Capnography (ETCO2)
Pulse oximetry (SpO2) or arterial blood gas
Blood pressure (direct or indirect)
Body temperature (especially in cats)

藥物動力學

半衰期

貓17.4 minutes狗6 minutes

吸收

Rapid onset of analgesic action and peak effect (1-3 minutes) following IV administration.

分佈

Rapidly distributed into the CNS. In dogs, the blood-brain equilibration half-life is 2.3-5.2 minutes. In cats, it has a moderately high volume of distribution (7.6 L/kg in conscious cats, decreasing to 1.65 L/kg under isoflurane anesthesia).

代謝

Rapidly metabolized by hydrolysis of the propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases. It is not appreciably metabolized by the liver or by plasma cholinesterase (pseudocholinesterase).

排除

High clearance rate (766 mL/min/kg in cats). The principal carboxylic acid metabolite is virtually inactive and excreted.

過量

Overdosage manifests as an enhancement of the drug's pharmacological effects.

Clinical Signs:

Apnea and severe respiratory depression
Chest-wall rigidity
Hypoxemia
Hypotension and severe bradycardia
Seizures

Treatment:

Discontinue drug administration immediately.
Provide supportive therapy, primarily mechanical ventilation and oxygen administration. Because the drug is cleared so rapidly by tissue esterases, this is often the only intervention required.
Administer IV fluids, and use glycopyrrolate or atropine to manage bradycardia or hypotension.
Naloxone may be used to reverse mu-opioid activity, but caution is advised as it can lead to acute pain and sympathetic hyperactivity.

可用產品

劑型

Powder for injection (reconstitution)

人用標示

Remifentanil HCl Powder for reconstitution (IV use only): 1 mg (3 mL vial), 2 mg (5 mL vial), 5 mg (10 mL vial) as Ultiva® or generic equivalents. (Rx, C-II controlled substance)

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

Prior to reconstitution, store lyophilized powder between 2°-25°C (36°-77°F). To reconstitute, add 1 mL of diluent per mg of drug (yields ~1 mg/mL), then further dilute to 20-250 mcg/mL before administration. Stable for 24 hours at room temperature after dilution with sterile water, D5W, 0.9% NaCl, or 0.45% NaCl. Stable for 4 hours at room temperature when diluted with Lactated Ringer's Solution (LRS), though UK labeling advises against mixing with LRS.

飼主須知

瑞芬太尼是一種先進且強效的止痛藥和麻醉輔助劑，僅在獸醫院的手術環境中使用。

使用原因：它在手術過程中提供深度的疼痛緩解，並允許獸醫師減少其他麻醉氣體或藥物的使用劑量。
作用迅速：它最獨特的特點是排出體外的速度極快。一旦停止點滴，藥物會在幾分鐘內失效。這使得您的寵物能更快、更平穩地從麻醉中甦醒。
器官安全性高：因為它是由血液和組織中的酵素分解，而不是依賴肝臟或腎臟，所以對於患有肝臟或腎臟疾病的寵物來說非常安全。
術後疼痛管理：由於瑞芬太尼的藥效消退非常快，您的獸醫師會在寵物醒來之前給予長效的止痛藥，以確保牠們在術後保持舒適。

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