톨라졸린

Tolazoline

Tolazoline hydrochloride

알파-아드레날린 수용체 차단제 / 역전제IVIM개고양이새말소양염소

다른 이름: Tolazine · Priscoline · Vaso-Dilatan · benzazoline hydrochloride · tolazolinium chloratum

VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료

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

체중— 🐕

용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.

동물 종별 용량

🌎 NA — North America🌍 EU — Europe

개

적응증	용량	경로	빈도	기간	지역
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.

고양이

적응증	용량	경로	빈도	기간	지역
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.

새

적응증	용량	경로	빈도	기간	지역
As a reversal agent for alpha2-adrenergic agonists (e.g., xylazine, detomidine, etc.)	15 mg/kg IV	IV	once	—	🌎 NA

말

적응증	용량	경로	빈도	기간	지역
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.

소

적응증	용량	경로	빈도	기간	지역
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.

양

적응증	용량	경로	빈도	기간	지역
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.

염소

적응증	용량	경로	빈도	기간	지역
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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개요

톨라졸린은 비선택적 경쟁적 알파-아드레날린 수용체 차단제로, 수의학에서는 주로 말과 반추동물에서 자일라진(xylazine)의 진정, 진통 및 심혈관계 효과를 역전시키는 데 사용됩니다.

임상 요점: 자일라진 역전에는 매우 효과적이지만, 덱스메데토미딘이나 데토미딘과 같은 새롭고 선택성이 높은 α2-작용제에 대해서는 특이성과 효과가 떨어지는 것으로 간주됩니다(이 경우 아티파메졸이 선호됨).
α1 및 α2 수용체를 모두 차단하고 직접적인 혈관 확장 특성을 가지고 있기 때문에 심혈관계에 미치는 영향이 복잡하고 때로는 예측하기 어려울 수 있으므로 천천히 주의해서 투여해야 합니다.

작용 기전

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.

안전성·주의사항

금기사항

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)

부작용

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)

주의

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.

약물 상호작용

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.

모니터링

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

약동학

반감기

말Approximately 1 hour

흡수

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

분포

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

과다투여

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.

제품

제형

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

동물용의약품

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

규제 현황

규제 데이터 없음: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

보관·안정성

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

보호자 정보

톨라졸린은 수술이나 검사 후 동물을 '깨우기(진정제 역전)' 위해 수의학 전문가가 독점적으로 투여하는 약물입니다.

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지속 시간: 이러한 효과는 대개 경미하며 투여 후 2시간 이내에 줄어들고 사라져야 합니다.
안전성: 심박수와 혈압의 급격한 변화가 발생할 수 있으므로, 회복 기간 동안 수의료 팀이 동물을 면밀히 모니터링할 것입니다.

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