氟馬西尼

Flumazenil

1,4-imidazobenzodiazepine derivative

別名: Romazicon · Anexate · Fadaflumaz · Flumage · Flumanovag · Fluxifarm · Lanexat · flumazenilum · flumazepil · Ro-15-1788/000

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

經審核的 v13 劑量證據

經審核的非計算證據

經審核的非計算證據 (3)

只供證據參考，不會自動計算

Crocodilians, chelonians/reversal of zolazepam

TABLE 127.5. Agent: Flumazenil (Romazicon, Hoffman-LaRoche). Dosage: 1 mg/20 mg of zolazepam187 IM, IV275. Species/Comments: Crocodilians, chelonians/reversal of zolazepam.

IMIV

高風險須由已驗證獸醫確認drug_regimen方案年份 2019審核 dose-audit-mader-reviewed-v1

只供證據參考，不會自動計算

All species/reversal of midazolam; extrapolated from mammals and birds

TABLE 127.5. Agent: Flumazenil (Romazicon, Hoffman-LaRoche). Dosage: 0.05 mg/kg IM, SC, IV207. Species/Comments: All species/reversal of midazolam; extrapolated from mammals and birds.

IMIVSC

高風險須由已驗證獸醫確認drug_regimen方案年份 2019審核 dose-audit-mader-reviewed-v1

只供證據參考，不會自動計算

All species/reversal of benzodiazepines, including diazepam and midazolam; seldom indicated

TABLE 127.5. Agent: Flumazenil (Romazicon, Hoffman-LaRoche). Dosage: —. Species/Comments: All species/reversal of benzodiazepines, including diazepam and midazolam; seldom indicated.

高風險須由已驗證獸醫確認drug_regimen方案年份 2019審核 dose-audit-mader-reviewed-v1

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概覽

氟馬西尼是一種高度專一的苯二氮平類拮抗劑，在獸醫學中主要用於逆轉因治療或意外過量引起的苯二氮平類藥物（如地西泮、咪達唑侖、唑拉西泮）的中樞神經系統（CNS）抑制作用。

主要臨床應用：

逆轉鎮靜/麻醉： 快速逆轉苯二氮平類藥物引起的鎮靜作用。
肝性腦病： 可作為輔助療法，透過拮抗內源性苯二氮平類物質，暫時改善嚴重肝衰竭病患的神經功能。
毒性/過量： 有效治療苯二氮平類藥物及某些非苯二氮平類安眠藥（如 Zolpidem/Ambien®）的過量。

臨床要點： 當用於逆轉替來他明-唑拉西泮（Telazol®）麻醉組合時，氟馬西尼能成功逆轉唑拉西泮的成分（鎮痛、姿勢、聽覺效應），但不能逆轉替來他明（一種解離性麻醉劑）。這可能導致甦醒過程不平穩，出現殘留的解離效應（如肌肉僵硬、焦躁不安），而缺乏苯二氮平類的平緩作用。

作用機制

Flumazenil acts as a competitive antagonist at the benzodiazepine recognition site on the GABA-A/benzodiazepine receptor complex in the central nervous system.

Mechanism Pathway: Flumazenil binds to the receptor → competitively displaces benzodiazepine molecules → prevents the allosteric enhancement of GABA → prevents the opening of chloride (Cl-) channels → reverses GABAergic inhibitory effects (sedation, amnesia, muscle relaxation).

安全性與警告

禁忌症

Known hypersensitivity to flumazenil or other benzodiazepines
Patients receiving benzodiazepines for life-threatening conditions (e.g., status epilepticus, increased intracranial/CSF pressure)
Serious tricyclic antidepressant (TCA) overdose
Mixed overdoses where benzodiazepine reversal may precipitate seizures
Baclofen or carisoprodol overdoses (may worsen clinical signs)
Suspected tricyclic antidepressant overdose (can precipitate seizures)
Patients receiving long-term benzodiazepine administration for seizure control or sedation (relative contraindication)

不良反應

Injection site reactions
Vomiting
Cutaneous vasodilatation
Vertigo
Ataxia
Blurred vision
Seizures (especially in patients with a history of chronic benzodiazepine use or tricyclic antidepressant toxicity)
Potentially teratogenic at high dosages
Seizures (especially in patients receiving long-term benzodiazepine therapy)
Re-sedation (due to short half-life)
Agitation or anxiety upon rapid awakening

注意事項

Important Warnings:

Short Half-Life: Flumazenil has a shorter half-life (~1 hour) than many of the benzodiazepines it reverses. Re-sedation can occur once flumazenil wears off, requiring repeated dosing.
Seizure Risk: Use with extreme caution in patients with mixed drug overdoses or those dependent on benzodiazepines for seizure control, as rapid reversal can precipitate intractable seizures.
Not a Universal Antidote: It does not alter benzodiazepine pharmacokinetics (clearance/metabolism) and does not reverse opioids, alpha-2 agonists, or dissociative anesthetics.

藥物相互作用

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

Increased risk for seizures; concurrent use is contraindicated.

Neuromuscular Blocking Agents

Not recommended to use flumazenil until neuromuscular blockade has been fully reversed.

Tricyclic antidepressants (TCAs)Major

Can precipitate seizures in patients with suspected TCA overdose

Benzodiazepines (Diazepam, Midazolam, etc.)Major

Antagonizes therapeutic effects (intended interaction)

Tricyclic antidepressantsMajor

Increased risk of seizures if flumazenil is administered during a TCA overdose.

監測

Efficacy of reversal (level of consciousness, respiratory rate)
Monitor for re-sedation after 1-2 hours due to short half-life
Monitor for seizures in susceptible patients
Respiratory rate and depth
Level of consciousness and sedation (monitor for re-sedation after 1 hour)
Seizure activity

藥物動力學

半衰期

貓~1 hour狗~1 hour

吸收

Administered by rapid IV injection. Therapeutic effects are very rapid, typically occurring within 1-2 minutes of administration.

分佈

Rapidly distributed throughout the body and into the CNS.

代謝

Rapidly metabolized in the liver.

排除

Cleared primarily via hepatic metabolism.

過量

Large IV overdoses have rarely caused symptoms in otherwise healthy humans. If seizures are precipitated by an overdose or rapid reversal, they have been successfully treated with barbiturates, benzodiazepines, and phenytoin, usually with prompt responses.

可用產品

劑型

Injection
Injectable: 0.1 mg/ml solution (5 ml and 10 ml vials)

人用標示

Flumazenil Injection: 0.1 mg/mL in 5 mL & 10 mL vials (Romazicon®, generic)
Romazicon 0.1 mg/ml injectable solution

各地核准狀態

European Union✓ 已核准處方藥EMA

POM (Prescription Only Medicine)

United Kingdom✓ 已核准處方藥VMD

POM (Prescription Only Medicine)

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Store at 25°C (77°F); excursions are permitted from 15° to 30°C (59° to 86°F). Once drawn into a syringe or mixed with compatible IV solutions (Lactated Ringer's, D5W, or normal saline), discard after 24 hours.

飼主須知

寵物主人須知：

僅限醫院使用： 氟馬西尼是一種急救和麻醉逆轉藥物，嚴格限制在受控的獸醫醫院環境中由專業人員使用。
用途： 用於讓接受過苯二氮平類鎮靜劑（如 Valium/地西泮）的寵物快速「甦醒」，或用於治療這些藥物及人類安眠藥（如 Ambien）的意外過量。
監測： 由於該藥物代謝很快（約一小時內失效），您的寵物將在醫院接受密切監測，以確保在逆轉劑失效後不會再次陷入昏睡。

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