妥拉蘇林

Tolazoline

Tolazoline hydrochloride

α-腎上腺素受體阻斷劑 / 鎮靜劑逆轉藥IVIM狗貓鳥馬牛羊山羊

別名: Tolazine · Priscoline · Vaso-Dilatan · benzazoline hydrochloride · tolazolinium chloratum

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 mg/kg slow IV (4 mL/220 lb. of body weight); administration rate should approximate 1 mL/secondIV· once

體重— 🐕

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
For reversal of xylazine effects	4 mg/kg slow IV (4 mL/220 lb. of body weight); administration rate should approximate 1 mL/second	IV	once	—	🌎 NA

For reversal of xylazine effects: High concentration (100 mg/mL) makes accurate dosing difficult; yohimbine or human-labeled tolazoline (25 mg/mL) may be safer alternatives. Not FDA-approved for dogs.

貓

適應症	劑量	途徑	頻次	療程	地區
For reversal of xylazine effects	4 mg/kg slow IV (4 mL/220 lb. of body weight); administration rate should approximate 1 mL/second	IV	once	—	🌎 NA

For reversal of xylazine effects: High concentration (100 mg/mL) makes accurate dosing difficult; yohimbine or human-labeled tolazoline (25 mg/mL) may be safer alternatives. Not FDA-approved for cats.

鳥

適應症	劑量	途徑	頻次	療程	地區
As a reversal agent for alpha2-adrenergic agonists (e.g., xylazine, detomidine, etc.)	15 mg/kg IV	IV	once	—	🌎 NA

馬

適應症	劑量	途徑	頻次	療程	地區
For reversal of xylazine effects	4 mg/kg slow IV (4 mL/220 lb. of body weight); administration rate should approximate 1 mL/second	IV	once	—	🌎 NA

For reversal of xylazine effects: FDA-approved for use in horses.

牛

適應症	劑量	途徑	頻次	療程	地區
For reversal of xylazine effects	2-4 mg/kg slow IV ; titrate to effect	IV	once	—	🌎 NA
For reversal of xylazine effects (Emergency)	2 mg/kg IM	IM	once	—	🌎 NA

For reversal of xylazine effects: Slaughter withdrawal: 30 days. Not FDA-approved in the USA for use in food animals.
For reversal of xylazine effects (Emergency): Should not be administered IV rapidly as this can result in cardiac asystole. Effects of reversal should start to become evident about 10 minutes following IM administration.

羊

適應症	劑量	途徑	頻次	療程	地區
For reversal of xylazine effects	2-4 mg/kg slow IV ; titrate to effect	IV	once	—	🌎 NA
For reversal of xylazine effects	1-2 mg /kg IM. Give 50% of initial dose slow IV or IM and then determine if more is needed.	IM/IV	once	—	🌎 NA

For reversal of xylazine effects: Slaughter withdrawal: 30 days. Not FDA-approved in the USA for use in food animals.

山羊

適應症	劑量	途徑	頻次	療程	地區
For reversal of xylazine effects	2-4 mg/kg slow IV ; titrate to effect	IV	once	—	🌎 NA
For reversal of xylazine effects	1-2 mg /kg IM. Give 50% of initial dose slow IV or IM and then determine if more is needed.	IM/IV	once	—	🌎 NA

For reversal of xylazine effects: Slaughter withdrawal: 30 days. Not FDA-approved in the USA for use in food animals.

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概覽

妥拉蘇林 (Tolazoline) 是一種非選擇性競爭型 α-腎上腺素受體阻斷劑，在獸醫學中主要用於逆轉甲苯噻嗪 (Xylazine) 在馬和反芻動物中所引起的鎮靜、鎮痛及心血管效應。

臨床要點：雖然對逆轉甲苯噻嗪非常有效，但對於較新的高選擇性 α2-致效劑（如右美托咪啶或得托咪啶），其專一性與效果不如阿替美唑 (Atipamezole)。
由於它同時阻斷 α1 和 α2 受體並具有直接的血管擴張特性，其心血管效應可能較為複雜且有時難以預測，因此必須緩慢且謹慎地給藥。

作用機制

Tolazoline acts as a competitive antagonist at both α1- and α2-adrenergic receptors.

Central & Peripheral α2 Blockade → Reverses the sedation, analgesia, and bradycardia induced by α2-agonists (like xylazine).
Direct Smooth Muscle Relaxation → Exerts a direct relaxant effect on vascular smooth muscle → peripheral vasodilation → decreases total peripheral resistance.
Onset: Rapid acting (usually within 5 minutes of IV administration), but has a short duration of action, meaning repeat doses may occasionally be required if re-sedation occurs.

安全性與警告

禁忌症

Horses exhibiting signs of stress, debilitation, or shock
Cardiac disease or coronary artery disease
Sympathetic blockage
Hypovolemia
Cerebrovascular disease
Known hypersensitivity to the drug
Foals (relative contraindication; adverse reactions and fatalities reported)

不良反應

Transient tachycardia
Peripheral vasodilation (sweating, injected mucous membranes of gingiva and conjunctiva)
Hyperalgesia of the lips (licking, flipping of lips)
Piloerection
Clear lacrimal and nasal discharge
Muscle fasciculations
Apprehensiveness and anxiety
Gastrointestinal hypermotility (flatulence, diarrhea, mild colic)

注意事項

WARNING: Rapid IV Administration Acute death and cardiac asystole have been reported after rapid IV administration of tolazoline at high dosages, particularly in camelids and cattle. Always administer IV slowly (e.g., 1 mL/second) or consider the IM route.

High Concentration Risk: The veterinary formulation is highly concentrated (100 mg/mL), making accurate dosing difficult in small animals (dogs/cats). Yohimbine or atipamezole are generally safer alternatives for small animals.
Human Safety: Humans with coronary artery or cerebrovascular disease should use extra caution when handling this agent.

藥物相互作用

Alcohol

Accumulation of acetaldehyde can occur if tolazoline and alcohol are given simultaneously.

Epinephrine

If large doses of tolazoline are given with epinephrine, a paradoxical drop in blood pressure can occur followed by a precipitous increase in blood pressure.

Norepinephrine

If large doses of tolazoline are given with norepinephrine, a paradoxical drop in blood pressure can occur followed by a precipitous increase in blood pressure.

監測

Reversal effects (efficacy of waking up/recovery)
Heart rate and rhythm
Blood pressure
Adverse effects (sweating, GI hypermotility, anxiety)

藥物動力學

半衰期

馬Approximately 1 hour

吸收

Rapid acting after IV administration (usually within 5 minutes).

分佈

Widely distributed. Animal studies have demonstrated that tolazoline is concentrated in the liver and kidneys.

過量

Overdoses can cause severe cardiovascular and gastrointestinal disturbances.

Horses (5X overdose): Gastrointestinal hypermotility resulting in flatulence, defecation, mild colic, and transient diarrhea. Intraventricular conduction may be slowed (prolongation of the QRS-complex). Ventricular arrhythmias and death may occur at higher overdoses.
Camelids (5X overdose in a llama): Anxiety, hyperesthesia, profuse salivation, GI tract hypermotility, diarrhea, convulsions, hypotension, and tachypnea. Successfully treated with IV diazepam, phenylephrine, IV fluids, and oxygen.
Human Treatment Note: Ephedrine (NOT epinephrine or norepinephrine) has been recommended to treat serious tolazoline-induced hypotension.

可用產品

劑型

Injection: 100 mg/mL (Veterinary)
Injection: 25 mg/mL (Human-labeled, historically)

獸醫用

Tolazoline HCl Injection: 100 mg/mL in 100 mL multi-dose vials (Tolazine®)

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

Commercially available injection products should be stored between 15-30°C and protected from light. Reportedly physically compatible with commonly used IV solutions.

飼主須知

妥拉蘇林主要由獸醫專業人員給藥，用於在手術或檢查後「喚醒」您的動物（逆轉鎮靜劑）。

預期反應：當您的動物甦醒時，您可能會注意到暫時的副作用，例如流汗、舔嘴唇、焦慮或肌肉顫抖。
持續時間：這些影響通常是輕微的，應在給藥後 2 小時內減弱並消失。
安全性：由於心跳速率和血壓可能會發生快速變化，獸醫團隊會在恢復期間密切監測您的動物。

VetSheet 藥物參考供持牌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方最新藥品說明書。