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毒扁豆鹼

Physostigmine

Physostigmine salicylate

膽鹼酯酶抑制劑IVIMSC狗馬牛

別名: Antilirium · Anticholium · Eserine salicylate · Physostigmine monosalicylate

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

經審核的 v13 劑量證據

經審核的非計算證據
經審核的非計算證據 (1)

只供證據參考，不會自動計算

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.

topically
高風險須由已驗證獸醫確認drug_regimen方案年份 2019審核 dose-audit-mader-reviewed-v1

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概覽

毒扁豆鹼是一種可逆的​膽鹼酯酶抑制劑​，在獸醫學中主要用於伊維菌素 (ivermectin) 中毒的輔助治療、作為犬馬猝睡症/猝倒症的誘發診斷試劑，以及中樞性抗膽鹼藥物中毒的解毒劑。

​臨床要點：​

  • 與四級胺類膽鹼酯酶抑制劑（如新斯狄明 neostigmine）不同，毒扁豆鹼是一種​三級胺​。
  • 這種結構差異使其能夠輕易穿透​血腦屏障 (BBB)​，因此對治療「中樞性」抗膽鹼毒性特別有效。
  • 由於能進入中樞神經系統，其引發中樞毒性副作用（如癲癇）的風險也較高。
  • 由於治療指數狹窄且可能產生嚴重副作用，通常僅保留用於危及生命的中樞神經毒性治療。

作用機制

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.

安全性與警告

禁忌症

  • 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

不良反應

  • 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

注意事項

​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.

藥物相互作用

Choline esters (bethanechol, carbachol, methacholine)

May cause additive adverse cholinergic effects.

Organophosphates

May cause additive adverse cholinergic effects.

Succinylcholine

High doses of physostigmine may cause muscle fasciculations or depolarization block, which may be additive to the effects of succinylcholine-like neuromuscular blockers.

監測

  • 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)

藥物動力學

吸收

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.

分佈

Readily crosses the blood-brain barrier into the CNS due to its tertiary amine structure.

代謝

The majority of the administered drug is rapidly destroyed via hydrolysis by cholinesterases.

排除

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).

過量

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.

可用產品

劑型

  • Injection

人用標示

  • Physostigmine Salicylate Injection: 1 mg/mL (contains benzyl alcohol 2% and 0.1% sodium metabisulfite) in 2 mL ampules

各地核准狀態

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儲存與穩定性

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.

飼主須知

本藥物僅限於臨床環境中使用。

  • ​直接監督：​ 必須在有獸醫師直接監督及具備急救監測設備的獸醫院內給藥。
  • ​不可居家使用：​ 由於具有引發嚴重且可能危及生命副作用的風險，本藥物絕對不會交由飼主帶回家自行投藥。

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