프랄리독심 염화물

해독제 - 콜린에스테라아제 재활성화제

프랄리독심(흔히 **2-PAM**으로 불림)은 수의학에서 주로 **유기인계(OP) 중독**을 치료하는 데 사용되는 특이적 해독제입니다. 유기인계 화합물은 구형 살충제, 농약 및 일부 신경 작용제에서 흔히 발견됩니다. 이들은 아세틸콜린에스테라아제(AChE)에 비가역적으로 결합하고 억제하여 신경 시냅스와 신경근 접합부에 아세틸콜린이 대량으로 축적되게 합니다. 프랄리독심은 **콜린에스테라아제 재활성화제**로 작용하여, 결합이 영구적으로 변하기 전(이 과정을 "노화(aging)"라고 함)에 효소에서 유기인계 분자를 효과적으로 떼어냅니다. > **임상 요점:** 프랄리독심은 거의 항상 **아트로핀**과 함께 사용됩니다. 아트로핀은 아세틸콜린 과다로 인한 무스카린성 효과(SLUDDE 증상: 유연, 눈물, 배뇨, 배변, 호흡곤란, 구토)를 차단하는 반면, 프랄리독심은 **니코틴성 효과**(특히 심각한 근육 떨림, 쇠약 및 호흡근을 포함한 마비)를 완화하는 데 필요합니다. 카바메이트 중독의 경우 카바메이트-AChE 결합이 옥심계 재활성화제 없이도 자발적으로 가역화되므로 일반적으로 **권장되지 않습니다**.

작용 기전: Pralidoxime works by directly reactivating the acetylcholinesterase enzyme that has been inhibited by organophosphates. * **Organophosphates** bind to the esteratic site of **acetylcholinesterase (AChE)** via phosphorylation, inactivating the enzyme. * Accumulation of **acetylcholine (ACh)** occurs at muscarinic and nicotinic receptors → severe overstimulation. * **Pralidoxime** possesses a high affinity for the AChE enzyme. * Via **nucleophilic attack**, the oxime group of pralidoxime binds to the offending phosphoryl group of the organophosphate. * The pralidoxime-organophosphate complex breaks away from the enzyme → **AChE is reactivated** and resumes breaking down ACh. > **Important Mechanistic Note:** If the phosphorylated enzyme undergoes a chemical change (loss of an alkyl group) before pralidoxime is administered, the bond becomes permanent. This is known as **"aging"**. Therefore, pralidoxime is most effective when given **within 24 hours** of exposure, though some benefit may be seen up to 36-48 hours in massive exposures.

동물 종별 용량

Cats

Organophosphate poisoning · 20 mg/kg · IM or slow IV · 2-3 times a day · Works best when combined with atropine. Initial dose IM or slow IV; subsequent doses IM or SC.
Organophosphate poisoning · 10-15 mg/kg · IM or SC · q8-12h · 36 hour minimum
Organophosphate poisoning · 50 mg/kg · slow IV · May repeat in one hour if severe · Recovery should occur gradually over 48 hours · Give atropine first. Dilute in 10% glucose. May administer IM or IP. Reduce dose in renal failure.
Organophosphate poisoning · 20 mg/kg · IV · Repeat in one hour if signs persist, then q8h · 24-48 hours · Give slowly or with fluids over a 30-minute period.
Organophosphate poisoning · 20 mg/kg · IM or IV · May repeat q6-8h · Give within first 24 hours of exposure. Combine with atropine or give separately. Do not use in carbamate toxicity.

Cattle

Organophosphate poisoning · 30 mg/kg · IM · q8h · FARAD recommends a 28-day meat and a 6-day milk withdrawal time.
Organophosphate poisoning · 25-50 mg/kg · IV · Single dose, or maximum of 100 mg/kg/day as an IV drip · Give as a 20% solution over 6 minutes.

Horses

Organophosphate poisoning · 20 mg/kg (may require up to 35 mg/kg) · IV · q4-6h

Birds

투여 경로

IVIMSCIP

금기

Hypersensitivity to pralidoxime
Carbamate poisoning (generally not recommended as inhibition is rapidly reversible)

이상반응

Tachycardia (especially with rapid IV injection)
Muscle rigidity
Transient neuromuscular blockade
Laryngospasm

약물 상호작용

Barbiturates · Anticholinesterases can potentiate the action of barbiturates; use with caution.
Cimetidine · Use should be avoided in patients with organophosphate toxicity.
Succinylcholine · Use should be avoided in patients with organophosphate toxicity.
Theophylline · Use should be avoided in patients with organophosphate toxicity.
Reserpine · Use should be avoided in patients with organophosphate toxicity.
Respiratory Depressants (e.g., narcotics, phenothiazines) · Use should be avoided in patients with organophosphate toxicity.

모니터링

Clinical signs associated with organophosphate poisoning (SLUDDE signs, muscle fasciculations, weakness)
Heart rate and rhythm (especially during IV administration)
Respiratory rate and effort

과용량

The acute LD50 of pralidoxime in dogs is 190 mg/kg. At high dosages, it causes signs associated with its own anticholinesterase activity. Clinical signs of toxicity in dogs may be exhibited as: * Muscle weakness * Ataxia * Vomiting * Hyperventilation * Seizures * Respiratory arrest * Death

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