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フィゾスチグミン

Physostigmine

Physostigmine salicylate

コリンエステラーゼ阻害薬IVIMSC犬馬牛

別名: Antilirium · Anticholium · Eserine salicylate · Physostigmine monosalicylate

VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス

監査済み v13 用量エビデンス

確認済み・計算対象外のエビデンス
確認済み・計算対象外のエビデンス (1)

エビデンス表示のみ（自動計算対象外）

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
高リスク認証済み獣医師の確認が必要drug_regimenプロトコル 2019監査 dose-audit-mader-reviewed-v1

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

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概要

フィゾスチグミンは可逆性の​コリンエステラーゼ阻害薬​であり、獣医療では主にイベルメクチン中毒の補助治療、犬や馬のナルコレプシー/カタプレキシーの誘発診断薬、および中枢性抗コリン薬中毒の解毒剤として使用されます。

​臨床上のポイント:​

  • 第4級アミン（ネオスチグミンなど）とは異なり、フィゾスチグミンは​第3級アミン​です。
  • この構造の違いにより​血液脳関門（BBB）​を容易に通過できるため、「中枢性」の抗コリン毒性の治療に特異的な効果を発揮します。
  • 中枢神経系に移行するため、中枢性の毒性作用（痙攣など）のリスクが高くなります。
  • 治療域が狭く重篤な副作用の可能性があるため、通常は生命を脅かす中枢神経毒性の治療に限定して使用されます。

作用機序

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・警告

禁忌

  • 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

有害事象

  • 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.

医薬品相互作用

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.

監視

  • 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)

薬物動態

吸収

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.

分布

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.

消失

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).

過剰投与

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.

製品

製剤

  • Injection

ヒト用医薬品

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

規制ステータス

規制データなし: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

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.

飼主向け情報

この薬は臨床環境でのみ使用されます。

  • ​直接の監督:​ 獣医師の直接の監督と緊急モニタリングが可能な動物病院で投与する必要があります。
  • ​自宅での使用不可:​ 重篤で生命を脅かす可能性のある副作用のリスクがあるため、飼い主が自宅で投与するために処方されることは決してありません。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。