톨라졸린

알파-아드레날린 수용체 차단제 / 역전제

톨라졸린은 비선택적 경쟁적 **알파-아드레날린 수용체 차단제**로, 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.

동물 종별 용량

Sheep

For reversal of xylazine effects · 2-4 mg/kg slow IV ; titrate to effect · IV · once · Slaughter withdrawal: 30 days. Not FDA-approved in the USA for use in food animals.
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

Goats

For reversal of xylazine effects · 2-4 mg/kg slow IV ; titrate to effect · IV · once · Slaughter withdrawal: 30 days. Not FDA-approved in the USA for use in food animals.
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

Cats

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 · 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.

Cattle

For reversal of xylazine effects · 2-4 mg/kg slow IV ; titrate to effect · IV · once · Slaughter withdrawal: 30 days. Not FDA-approved in the USA for use in food animals.
For reversal of xylazine effects (Emergency) · 2 mg/kg IM · IM · once · 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.

투여 경로

IVIM

금기

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)

이상반응

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)

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)

과용량

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.

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