VetSheet

阿替美唑

Atipamezole

Atipamezole hydrochloride

α2-腎上腺素受體拮抗劑IMIVSCIP狗貓小型哺乳類鳥爬蟲類牛羊山羊

別名: Antisedan · Revertidine · Alzane · Revertor · Sedastop · Tipafar · Atipamezole HCl · MPV-1248 · Atipamezole hydrochloride · Atipamezolum

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

結構化劑量計算證據

Reversal of dexmedetomidine constant rate infusion (extralabel)

15–30 mcg/kgIM

須由已驗證獸醫確認

  • once · discontinuation of dexmedetomidine CRI

NA

必須一併考量的臨床脈絡 (1)
  • Atipamezole HCl injection should be stored at room temperature of 15°C to 30°C (59°F-86°F) and protected from light. Use within 90 days of first vial puncture.
高風險須由已驗證獸醫確認formulary方案年份 2023審核 dose-audit-plumb-v13

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。

正在看診？VetSheet 的 AI 會把藥物、劑量與療程直接寫入結構化的看診紀錄。了解 VetSheet 如何運作

概覽

阿替美唑是一種高選擇性且強效的 ​α2-腎上腺素受體拮抗劑​，在獸醫學中主要用作美托咪定 (medetomidine) 和右美托咪定 (dexmedetomidine) 等 α2-激動劑的逆轉劑。它也可用於標示外用途，以逆轉其他 α2-激動劑（如甲苯噻嗪 xylazine、雙甲脒 amitraz 和可樂定 clonidine）。

​臨床要點：​

  • 阿替美唑的 α2:α1 選擇性比例為 8526:1，比育亨賓 (yohimbine) 或妥拉蘇林 (tolazoline) 等較舊的逆轉劑更具特異性。這種高特異性使其能快速、乾淨地逆轉鎮靜，且心血管副作用較少。
  • 由於它會迅速逆轉鎮靜​和鎮痛​作用，因此在給藥前必須評估病患的疼痛情況；如果病患接受了會引起疼痛的處置，應提供替代的鎮痛藥物（如鴉片類藥物、非類固醇消炎藥）。
  • 阿替美唑的半衰期相對較短（在狗體內約 2-3 小時）。在治療長效 α2-激動劑（如雙甲脒）中毒時，毒性物質的作用時間可能超過逆轉劑，導致再次鎮靜，此時可能需要重複給藥。

作用機轉

Atipamezole competitively binds to central and peripheral ​$\alpha_2$-adrenergic receptors​, displacing alpha-2 agonists.

By blocking these receptors, it inhibits the negative feedback loop on presynaptic neurons $\rightarrow$ increases the release of norepinephrine into the synaptic cleft $\rightarrow$ leads to rapid arousal, reversal of sedation, increased heart rate, increased blood pressure, and loss of analgesia. It also antagonizes the diuretic action of alpha-2 agonists like xylazine.

安全性與警告

禁忌症

  • Reptiles (Intravenous administration is contraindicated due to profound hypotension)

不良反應

  • Vomiting
  • Diarrhea
  • Hypersalivation
  • Tremors
  • Brief excitation or apprehensiveness
  • Aggression upon rapid waking
  • Profound hypotension (if given IV in reptiles)
  • Loss of analgesia

注意事項

​Pregnancy/Lactation:​ Not recommended in pregnant or lactating animals, or animals intended for breeding due to lack of safety data.

  • ​Rapid Emergence:​ Because reversal can occur rapidly, care should be exercised as animals emerging from sedation and analgesia may exhibit apprehensive or aggressive behaviors. Protect animals from falling or self-harm.
  • ​Loss of Analgesia:​ Additional analgesia (e.g., butorphanol, buprenorphine) should be considered, particularly after painful procedures.
  • ​Relapse of Sedation:​ When used as an antidote for alpha-2 agonist toxicity (e.g., amitraz), atipamezole's effects may subside before non-toxic levels of the offending agent are reached; repeat dosing may be necessary.
  • ​Geriatric/Debilitated Patients:​ Caution should be used in administration of anesthetic agents to elderly or debilitated animals.
  • ​Reptiles:​ Do NOT give IV to reptiles as profound hypotension can occur.

藥物交互作用

Alpha-1 adrenergic blockers (e.g., prazosin)

Atipamezole can partially block alpha-1 receptors and reduce the effects of prazosin.

Alpha-2 adrenergic agonists (e.g., detomidine, clonidine, brimonidine, xylazine, amitraz)

Atipamezole can reduce the effects (toxic or therapeutic) of these agents.

MedetomidineMinor

Reverses sedative, analgesic, and cardiovascular effects (intended therapeutic interaction)

DexmedetomidineMinor

Reverses sedative, analgesic, and cardiovascular effects (intended therapeutic interaction)

KetamineMajor

If atipamezole is given less than 30 minutes after a medetomidine/ketamine combination in cats, it can cause severe CNS excitation during recovery.

Other alpha-2 antagonistsModerate

Additive antagonistic effects

Hypotensive agentsMinor

May exacerbate transient hypotension

監測

  • Level of sedation and analgesia
  • Heart rate
  • Body temperature

藥物動力學

半衰期

狗2-3 hours

吸收

After IM administration in the dog, peak plasma levels occur in about 10 minutes.

代謝

Atipamezole is apparently metabolized in the liver.

排除

Eliminated in the urine.

過量

Dogs receiving up to 10X the listed dosage apparently tolerated the drug without major effects.

​Clinical signs of overdose:​

  • Panting
  • Excitement
  • Trembling
  • Vomiting
  • Soft or liquid feces
  • Vasodilatation of sclera
  • Muscle injury at the IM injection site

Specific overdose therapy should generally not be necessary as effects are typically transient.

可用產品

劑型

  • Injection: 5 mg/mL

獸醫用

  • Atipamezole HCl for Injection: 5 mg/mL in 10 mL multidose vials; Antisedan® (Pfizer); (Rx)

各地核准狀態

European Union✓ 已核准處方藥EMA
🐕 Dogs🐈 Cats

Approved for reversal of medetomidine and dexmedetomidine in dogs and cats.

United Kingdom✓ 已核准處方藥VMD
🐕 Dogs🐈 Cats

POM-V classification.

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

儲存與穩定性

Atipamezole HCl injection should be stored at room temperature (15°-30°C) and protected from light.

飼主須知

阿替美唑是一種逆轉劑，用於在鎮靜或麻醉後喚醒您的寵物。本藥物僅應由獸醫專業人員給藥。

​在家中需要注意的事項：​

  • 偶爾，寵物在接受此藥物後可能會出現嘔吐、腹瀉、流口水（唾液分泌過多）、過度興奮或發抖的情況。
  • 由於該藥物會迅速消除鎮靜和止痛效果，如果您的寵物接受了會引起疼痛的處置，牠們可能會顯得焦慮或不適。請確保按照指示給予任何處方的止痛藥。
  • 如果任何副作用很嚴重，或者您的寵物在離開診所後顯得過度焦躁或再次陷入昏睡，請立即聯繫您的獸醫。

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。