新斯狄明
Neostigmine
Neostigmine metilsulfate
別名: Prostigmin · Robinul-Neostigmine · Neostigmine metilsulfate · Neostigmine bromide
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
Crocodiles/gallamine reversal; may cause emesis and lacrimation; fast 24–48 hr before use; effects enhanced if combined with 75 mg hyaluronidase per dose when administered SC, IM188
TABLE 127.5. Agent: Neostigmine. Dosage: 0.03–0.25 mg/kg IM188 0.063 mg/kg IV188 0.07–0.14 mg/kg IM235. Species/Comments: Crocodiles/gallamine reversal; may cause emesis and lacrimation; fast 24–48 hr before use; effects enhanced if combined with 75 mg hyaluronidase per dose when administered SC, IM188.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
新斯狄明是一種可逆的乙醯膽鹼酯酶抑制劑，在獸醫學中主要用於診斷和控制重症肌無力，以及拮抗非去極化神經肌肉阻斷劑的作用。由於其極性結構，它對中樞神經系統（CNS）的穿透力較差。
臨床警告： 給藥可能會引發危及生命的膽鹼能危機。強烈建議使用與格隆溴銨（glycopyrronium）的複方製劑，或準備好阿托品（atropine）以便立即靜脈注射，以控制嚴重的毒蕈鹼副作用（例如嚴重心搏過緩、心搏停止、支氣管收縮）。
作用機制
Neostigmine acts as a reversible inhibitor of the enzyme acetylcholinesterase at the neuromuscular junction (NMJ) and autonomic synapses.
Inhibition of acetylcholinesterase → Decreased breakdown of acetylcholine (ACh) → Accumulation of ACh in the synaptic cleft → Prolonged and enhanced stimulation of nicotinic and muscarinic receptors → Improved muscle contraction (in myasthenia gravis) and reversal of non-depolarizing neuromuscular blockade.
安全性與警告
禁忌症
- Mechanical gastrointestinal obstruction
- Mechanical urinary tract obstruction
- Peritonitis
不良反應
- Nausea and vomiting
- Increased salivation (ptyalism)
- Diarrhoea
- Muscle fasciculations and cramps
- Weakness and paralysis (with overdose)
- Severe bradyarrhythmias or asystole
- Miosis and nystagmus
- Hypotension
- Bronchoconstriction and increased bronchial secretions
注意事項
Use with extreme caution in patients with:
- Bronchial disease (especially feline asthma)
- Bradycardia and other arrhythmias
- Hypotension
- Renal impairment
- Epilepsy
Always have atropine (0.05 mg/kg IV) available for immediate administration when using neostigmine to diagnose myasthenia gravis.
藥物相互作用
May antagonize the neuromuscular effects of neostigmine
May antagonize the neuromuscular effects of neostigmine
May antagonize the neuromuscular effects of neostigmine
May increase clinical severity of myasthenia gravis and reduce neostigmine effectiveness
May reduce effectiveness in myasthenia gravis; concurrent use may result in severe bradycardia
Neostigmine inhibits its metabolism, prolonging and enhancing its clinical effect (combined use not recommended)
Neostigmine antagonizes their effect (therapeutic use)
Antagonizes the muscarinic effects of neostigmine (used therapeutically to manage side effects)
監測
- Heart rate and rhythm (ECG monitoring recommended during IV administration)
- Respiratory rate, effort, and airway patency
- Signs of cholinergic crisis (excessive salivation, urination, defecation, miosis)
- Muscle strength and fasciculations
藥物動力學
吸收
Poorly absorbed orally. Low CNS penetration due to its polar structure.
分佈
Does not readily cross the blood-brain barrier.
代謝
Metabolized by cholinesterases at the neuromuscular junction and in the liver.
排除
Excreted primarily in the urine.
過量
Cholinergic Crisis can occur with overdosage, presenting with both muscarinic and nicotinic effects (SLUDGE signs: Salivation, Lacrimation, Urination, Defecation, Gastrointestinal distress, Emesis), miosis, bradycardia, hypotension, muscle cramps, fasciculations, weakness, paralysis, bronchoconstriction, ataxia, seizures, and coma.
Management:
- Maintenance of respiration is the absolute priority.
- Administer Atropine to control muscarinic signs (note: atropine does not antagonize nicotinic effects like muscle weakness and paralysis).
- If muscle twitching is severe, control with small doses of a competitive neuromuscular blocker.
- The cholinesterase reactivator pralidoxime can be used as an adjunct to atropine.
- Provide intensive supportive care as required.
可用產品
劑型
- Injectable: 2.5 mg/ml solution
- Injectable: Glycopyrronium bromide 0.5 mg/ml and neostigmine metilsulfate 2.5 mg/ml solution
- Oral: 15 mg tablets
獸醫用
- Neostigmine 2.5 mg/ml injection (special order)
- Glycopyrronium bromide 0.5 mg/ml / Neostigmine metilsulfate 2.5 mg/ml injection
人用標示
- Neostigmine 15 mg tablets
各地核准狀態
Available as POM (Prescription Only Medicine)
Available as POM-V. Injectable often requires special order.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store at room temperature. Protect from light. Keep out of reach of children.
飼主須知
此藥物用於幫助診斷或治療稱為重症肌無力（一種導致嚴重肌肉無力的疾病）的病症，或用於逆轉麻醉期間使用的某些肌肉鬆弛劑。
- 密切觀察副作用： 如果您的寵物開始過度流口水、嘔吐、腹瀉，或出現呼吸困難或嚴重虛弱的跡象，請立即聯繫您的獸醫。
- 這種藥物可能會導致心率突然下降，因此通常在診所內給藥，以便密切監測您的寵物。
- 在未諮詢獸醫的情況下，請勿給予任何其他藥物，因為許多藥物可能會與新斯狄明產生交互作用。
VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠方最新藥品說明書。