피조스티그민
Physostigmine
Physostigmine salicylate
다른 이름: Antilirium · Anticholium · Eserine salicylate · Physostigmine monosalicylate
VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료
감사 완료 v13 용량 근거
검토된 비계산 근거검토된 비계산 근거 (1)
근거 표시 전용 — 자동 계산 불가
May ameliorate flaccid paralysis from ivermectin or levamisole toxicosis
TABLE 128.6. Agent: Physostigmine (ophthalmic drops). Dosage: 1 drop/50 g topically q1–2h to effect52. Species/Comments: May ameliorate flaccid paralysis from ivermectin or levamisole toxicosis.
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
개요
피조스티그민은 가역적 콜린에스테라아제 억제제로, 수의학에서는 주로 이버멕틴 중독의 보조 치료, 개와 말의 기면증/탈력발작 진단을 위한 유발제, 그리고 중추성 항콜린성 독성의 해독제로 사용됩니다.
임상 요점:
- 4차 아민계 콜린에스테라아제 억제제(예: 네오스티그민)와 달리 피조스티그민은 3차 아민입니다.
- 이러한 구조적 차이로 인해 혈액뇌장벽(BBB)을 쉽게 통과할 수 있어 '중추성' 항콜린성 독성 치료에 특히 효과적입니다.
- 중추신경계로 진입하기 때문에 중추성 독성 부작용(예: 발작)의 위험이 더 높습니다.
- 치료 지수가 좁고 심각한 부작용의 가능성이 있어, 일반적으로 생명을 위협하는 중추신경계 독성 치료에만 제한적으로 사용됩니다.
작용 기전
Physostigmine reversibly inhibits the enzyme acetylcholinesterase → prevents the hydrolysis and destruction of acetylcholine (ACh) → increases the concentration of ACh at both muscarinic and nicotinic receptor sites.
Because it is a lipophilic tertiary amine, it crosses the blood-brain barrier and exerts its cholinergic effects both centrally and peripherally. This widespread cholinergic stimulation leads to miosis, bronchoconstriction, hypersalivation, and increased gastrointestinal motility.
안전성·주의사항
금기사항
- Prior hypersensitivity reactions to physostigmine or sulfites
- Bronchoconstrictive disease (asthma)
- Gangrene
- Diabetes mellitus
- Cardiovascular disease
- Mechanical obstruction of the GI or urinary tract
- Any vagotonic state
- Concurrent use of choline esters or depolarizing neuromuscular blocking agents
부작용
- Miosis
- Bronchial constriction
- Hypersalivation
- Muscle weakness
- Sweating (in species with sweat glands)
- Seizures
- Bradycardia
- Tachycardia
- Asystole
- Nausea
- Vomiting
- Diarrhea
- Depolarizing neuromuscular block
- Pulmonary edema
- Respiratory paralysis
주의
WARNING: Toxic effects from this drug can be serious and life-threatening. Must be administered with direct patient supervision.
- Cholinergic Crisis Risk: Increased risk when used in the absence of anticholinergic toxicity or to treat tricyclic/tetracyclic antidepressant overdoses.
- Administration Rate: Rapid IV administration increases the potential for bradycardia, hypersalivation, or seizures. Must be given slowly.
- Antidote Availability: Atropine must be readily available when administering physostigmine.
- Neonatal Toxicity: The injection contains benzyl alcohol, which may be toxic to neonatal animals.
- Pregnancy: Weigh potential risks versus benefits. Teratogenic effects have been observed in mice.
약물 상호작용
May cause additive adverse cholinergic effects.
May cause additive adverse cholinergic effects.
High doses of physostigmine may cause muscle fasciculations or depolarization block, which may be additive to the effects of succinylcholine-like neuromuscular blockers.
모니터링
- Direct patient supervision is required
- Blood pressure
- ECG/Heart rhythm (especially if heart rate is abnormal)
- Signs of cholinergic crisis (salivation, lacrimation, urination, defecation, dyspnea, emesis)
약동학
흡수
Rapidly absorbed from the GI tract (though no oral dosage form is available), subcutaneous tissue, or mucous membranes. Peak effects occur within 5 minutes after IV administration and about 25 minutes after IM dosing.
분포
Readily crosses the blood-brain barrier into the CNS due to its tertiary amine structure.
대사
The majority of the administered drug is rapidly destroyed via hydrolysis by cholinesterases.
배설
Very small amounts can be eliminated unchanged into the urine. Duration of pharmacologic effects ranges from 30 minutes to 5 hours (average duration is 30-60 minutes).
과다투여
Overdoses or acute toxicity can be life-threatening and may result in a severe cholinergic crisis (seizures, bradycardia, asystole, respiratory paralysis).
- Supportive Care: Because of the short duration of effect, supportive care (including mechanical ventilation and repeated bronchial aspiration) may be sufficient in some cases.
- Antidote (Muscarinic): Administration of IV atropine is the primary treatment for cholinergic toxicity. Re-administration may be required.
- Antidote (Nicotinic): Pralidoxime (2-PAM) may be useful in reversing the ganglionic and skeletal muscle effects of physostigmine.
- Contact an animal poison control center for case management assistance.
제품
제형
- Injection
인용의약품
- Physostigmine Salicylate Injection: 1 mg/mL (contains benzyl alcohol 2% and 0.1% sodium metabisulfite) in 2 mL ampules
규제 현황
규제 데이터 없음: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
보관·안정성
Store ampules below 40°C, preferably between 15-30°C. Protect from light and freezing. It should be administered IV undiluted and should not be added to IV solutions.
보호자 정보
이 약물은 임상 환경에서만 사용해야 합니다.
- 직접 감독: 수의사의 직접적인 감독과 응급 모니터링이 가능한 동물병원에서 투여해야 합니다.
- 가정 내 사용 금지: 심각하고 생명을 위협할 수 있는 부작용의 위험이 있으므로, 보호자가 집에서 투여하도록 처방되는 일은 절대 없습니다.
VetSheet 의약품 참고자료는 수의사 전문가의 임상 의사결정 지원을 위한 것이며, 전문적 판단이나 제조사의 최신 약물 정보를 대체할 수 없습니다.
