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吡啶斯的明

Pyridostigmine

Pyridostigmine bromide

抗膽鹼酯酶劑POIVIM狗貓

別名: Mestinon · Distinon · Kalymin · Regonol · pyridostigmini bromidum · Pyridostigmine 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

0.5-3 mg/kg PO q8-12 hours with food.PO· q8-12h
— 🐕

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。

各物種劑量

🌎 NA — North America🌍 EU — Europe

狗

適應症劑量途徑頻次療程地區
Myasthenia gravis (MG)1-3 mg/kg PO q8-12h. For animals that cannot tolerate oral medications, it may be used as an IV constant rate infusion at 0.01-0.03 mg/kg/hour.PO/IVq8-12h or CRI—🌎 NA
Myasthenia gravis (MG)0.5-3 mg/kg PO q8-12 hours with food.POq8-12h—🌎 NA
Acquired Myasthenia gravis (MG)7.5-30 mg PO two times a day.POBID—🌎 NA
Myasthenia gravis (MG)0.5-3 mg/kg PO two to three times a day.POBID-TID—🌎 NA
Myasthenia gravis (MG)0.5-1 mg/kg PO two to three times a dayPOBID-TID—🌎 NA
Myasthenia gravis0.2-5 mg/kgPOq8-12h—🌍 EU
  • Myasthenia gravis (MG): Titrate to effect to minimize adverse effects and maximize muscle strength.
  • Myasthenia gravis (MG): Start low and increase slowly. Liquid formulation recommended for easy adjustment. An H2 antagonist (e.g., famotidine 5 mg/kg/day) may reduce nausea/GI irritation.
  • Acquired Myasthenia gravis (MG): Begin after oral regurgitation is abolished with parenteral neostigmine. Once stable, begin corticosteroids for 2 weeks, then gradually reduce pyridostigmine.
  • Myasthenia gravis (MG): If no response, add prednisone.
  • Myasthenia gravis (MG): With or without prednisone (2 mg/kg PO twice daily). Spontaneous remission is not uncommon.
  • Myasthenia gravis: Dose should be incrementally adjusted to maximize muscle strength and minimize adverse effects.

貓

適應症劑量途徑頻次療程地區
Myasthenia gravis (MG)0.5-3 mg/kg daily PO in divided dosesPODivided daily—🌎 NA
Myasthenia gravis (MG)1-3 mg/kg PO q8-12hPOq8-12h—🌎 NA
Myasthenia gravis (MG)0.5-3 mg/kg PO per dayPODaily—🌎 NA
Myasthenia gravis0.25 mg/kgPOq8-12h—🌍 EU
  • Myasthenia gravis (MG): Dose depending on response.
  • Myasthenia gravis (MG): Given with corticosteroids.

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。

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概覽

溴化吡啶斯的明是一種合成的季銨類抗膽鹼酯酶藥物，在獸醫學中主要用於控制犬（偶爾用於貓）的​重症肌無力 (Myasthenia Gravis, MG)​。

  • ​臨床要點：​ 由於其季銨結構，吡啶斯的明在標準治療劑量下不易穿透血腦屏障。這使其非常適合針對如重症肌無力等周邊神經肌肉接合處疾病，而不會引起明顯的中樞神經系統 (CNS) 副作用。
  • 通常認為它對​後天性重症肌無力​的療效遠優於先天性。
  • 由於其吸收不穩定且治療指數狹窄，必須根據療效仔細調整劑量，在改善肌肉力量與膽鹼能毒性風險之間取得平衡。

作用機制

Pyridostigmine acts as a reversible, competitive inhibitor of the enzyme ​acetylcholinesterase (AChE)​ at the neuromuscular junction.

  • ​Mechanism:​ Pyridostigmine competes directly with ​acetylcholine (ACh)​ for attachment to AChE. The resulting pyridostigmine-AChE complex is hydrolyzed much more slowly than the natural ACh-AChE complex.
  • ​Pathway:​ Inhibition of AChE → Decreased breakdown of ACh → Accumulation of ACh in the synaptic cleft → Prolonged and increased stimulation of nicotinic ACh receptors on the motor endplate → Enhanced skeletal muscle contraction and improved strength in myasthenic patients.

安全性與警告

禁忌症

  • Hypersensitivity to anticholinesterase compounds or bromides
  • Mechanical or physical obstructions of the urinary tract
  • Mechanical or physical obstructions of the gastrointestinal (GI) tract
  • Mechanical gastrointestinal obstruction
  • Mechanical urinary tract obstruction
  • Peritonitis

不良反應

  • Nausea
  • Vomiting
  • Diarrhea
  • Excessive salivation (ptyalism)
  • Sweating (in species with sweat glands)
  • Increased bronchial secretions
  • Bronchospasm
  • Pulmonary edema
  • Respiratory paralysis
  • Miosis (pupil constriction)
  • Blurred vision
  • Lacrimation (tearing)
  • Bradycardia
  • Tachycardia
  • Cardiospasm
  • Hypotension
  • Cardiac arrest
  • Muscle cramps
  • Weakness (can indicate cholinergic crisis)
  • Increased salivation (ptyalism)
  • Diarrhoea
  • Abdominal cramps
  • Bronchoconstriction
  • Involuntary defecation and micturition
  • Nystagmus
  • Heart block
  • Arrhythmias
  • Agitation
  • Muscle weakness
  • Fasciculations

注意事項

​High-Risk Patients:​ Use with extreme caution in patients with bronchospastic disease, epilepsy, hyperthyroidism, bradycardia or other arrhythmias, vagotonia, or GI ulcer diseases.

  • ​Pregnancy/Nursing:​ FDA Category C. Excreted in maternal milk; use with caution in nursing patients.
  • ​Dose Titration:​ Doses must be carefully titrated. High doses can cause a cholinergic crisis, which presents as profound weakness and can be difficult to distinguish from a myasthenic crisis.

藥物相互作用

Atropine

Antagonizes the muscarinic effects of pyridostigmine. Use cautiously as it can mask early clinical signs of a life-threatening cholinergic crisis.

Corticosteroids

May decrease the anticholinesterase activity of pyridostigmine. Discontinuing corticosteroids may suddenly increase anticholinesterase activity, requiring dose adjustments.

Dexpanthenol

Theoretically may have additive cholinergic effects when used concurrently.

Neuromuscular blocking drugs (e.g., aminoglycosides)

May necessitate increased dosages of pyridostigmine when treating or diagnosing myasthenic patients.

Magnesium (parenteral)

Can antagonize anticholinesterase therapy due to its direct depressant effect on skeletal muscle.

Muscle Relaxants

May prolong the Phase I block of depolarizing muscle relaxants (e.g., succinylcholine) and antagonize the actions of non-depolarizing agents (e.g., pancuronium, atracurium).

AminoglycosidesModerate

May antagonize the neuromuscular effects of pyridostigmine

ClindamycinModerate

May antagonize the neuromuscular effects of pyridostigmine

LincomycinModerate

May antagonize the neuromuscular effects of pyridostigmine

PropranololModerate

May antagonize the effects of pyridostigmine

SuxamethoniumMajor

Pyridostigmine may enhance the effect of depolarizing muscle relaxants

PancuroniumMajor

Pyridostigmine antagonizes the effect of non-depolarizing muscle relaxants

VecuroniumMajor

Pyridostigmine antagonizes the effect of non-depolarizing muscle relaxants

監測

  • Clinical signs of cholinergic toxicity (salivation, lacrimation, urination, defecation, GI upset, emesis, weakness)
  • Efficacy of therapy (improvement in muscle strength, reduction of megaesophagus/regurgitation)
  • Improvement in muscle strength and exercise tolerance
  • Signs of muscarinic toxicity (hypersalivation, vomiting, diarrhea, miosis)
  • Heart rate and rhythm
  • Respiratory rate and effort (especially in patients with megaoesophagus)

藥物動力學

吸收

Marginally absorbed from the GI tract. Absorption may be erratic, especially with sustained-release tablets. Onset of action after oral dosing is generally within one hour.

分佈

Distributed to most tissues, but does not cross into the brain (CNS), intestinal wall, fat, or thymus at usual doses due to its quaternary ammonium structure. Crosses the placenta.

代謝

Metabolized by the liver and hydrolyzed by cholinesterases.

排除

Excreted primarily via the kidneys (implied by class, though specific veterinary elimination data is sparse in the monograph).

過量

Overdosage of pyridostigmine can induce a life-threatening cholinergic crisis.

  • ​Clinical Signs (SLUDGE syndrome):​ GI effects (nausea, vomiting, diarrhea), excessive salivation, sweating, respiratory distress (increased bronchial secretions, bronchospasm, pulmonary edema, respiratory paralysis), ophthalmic effects (miosis, blurred vision, lacrimation), cardiovascular collapse (bradycardia, tachycardia, hypotension, cardiac arrest), severe muscle cramps, and profound weakness.
  • ​Diagnostic Challenge:​ Overdoses in myasthenic patients can be very difficult to distinguish from a myasthenic crisis (disease exacerbation). The time of onset of clinical signs or an edrophonium challenge (Tensilon test) may help differentiate the two.
  • ​Treatment:​ Consists of immediate respiratory and cardiac supportive therapy. Atropine should be administered to antagonize muscarinic effects (refer to atropine protocols for cholinergic toxicity).

可用產品

劑型

  • Extended-release tablets
  • Injection
  • 60 mg tablets
  • 60 mg/5 ml oral syrup (available on import licence)

人用標示

  • Pyridostigmine Bromide Tablets: 60 mg (Mestinon®, generic)
  • Pyridostigmine Bromide Extended-Release Tablets: 180 mg (Mestinon®)
  • Pyridostigmine Bromide Syrup: 12 mg/mL in 480 mL (Mestinon®)
  • Pyridostigmine Bromide Injection: 5 mg/mL in 2 mL ampules (Mestinon®)
  • Mestinon 60 mg tablets

各地核准狀態

European Union✓ 已核准處方藥EMA
🐕 Dogs🐈 Cats

Human registered products often used under the cascade.

United Kingdom✓ 已核准處方藥VMD
🐕 Dogs🐈 Cats

POM (Prescription Only Medicine). Oral syrup available on import licence.

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Store products at room temperature unless otherwise instructed. Protect oral solution and injection from light and freezing. Keep tablets in tight containers. Extended-release tablets may become mottled over time, but this does not affect potency. Injection is unstable in alkaline solutions.

飼主須知

吡啶斯的明是控制您寵物重症肌無力的關鍵藥物，但劑量必須非常精確。

  • ​嚴格給藥：​ 請完全按照獸醫師的指示給藥。未經諮詢請勿自行更改劑量，因為有效劑量與中毒劑量之間的差距非常小。
  • ​給藥方式：​ 與食物一起餵食有助於減少腸胃不適。通常建議使用液體劑型，以便進行微小的劑量調整。
  • ​注意毒性反應：​ 如果您發現寵物出現過量中毒的跡象，請​立即​聯繫您的獸醫師。症狀包括：過度流口水、嘔吐、腹瀉、極度虛弱、肌肉抽搐或呼吸困難。
  • ​自發性緩解：​ 在某些犬隻中，重症肌無力可能會隨著時間自行痊癒，因此您的獸醫師會密切監測您的寵物，以評估未來是否可以減少或停止用藥。

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