피리도스티그민
Pyridostigmine
Pyridostigmine bromide
다른 이름: Mestinon · Distinon · Kalymin · Regonol · pyridostigmini bromidum · Pyridostigmine bromide
VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
동물 종별 용량
🌎 NA — North America🌍 EU — Europe
개
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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/IV | q8-12h or CRI | — | 🌎 NA |
| Myasthenia gravis (MG) | 0.5-3 mg/kg PO q8-12 hours with food. | PO | q8-12h | — | 🌎 NA |
| Acquired Myasthenia gravis (MG) | 7.5-30 mg PO two times a day. | PO | BID | — | 🌎 NA |
| Myasthenia gravis (MG) | 0.5-3 mg/kg PO two to three times a day. | PO | BID-TID | — | 🌎 NA |
| Myasthenia gravis (MG) | 0.5-1 mg/kg PO two to three times a day | PO | BID-TID | — | 🌎 NA |
| Myasthenia gravis | 0.2-5 mg/kg | PO | q8-12h | — | 🌍 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.
고양이
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| Myasthenia gravis (MG) | 0.5-3 mg/kg daily PO in divided doses | PO | Divided daily | — | 🌎 NA |
| Myasthenia gravis (MG) | 1-3 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Myasthenia gravis (MG) | 0.5-3 mg/kg PO per day | PO | Daily | — | 🌎 NA |
| Myasthenia gravis | 0.25 mg/kg | PO | q8-12h | — | 🌍 EU |
- Myasthenia gravis (MG): Dose depending on response.
- Myasthenia gravis (MG): Given with corticosteroids.
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
개요
브롬화 피리도스티그민은 합성 4급 암모늄 항콜린에스테라제 약물로, 수의학에서는 주로 개(드물게 고양이)의 중증 근무력증(MG) 관리에 사용됩니다.
- 임상 요점: 4급 암모늄 구조로 인해 표준 치료 용량에서는 혈액-뇌 장벽을 쉽게 통과하지 못합니다. 따라서 중추신경계(CNS) 부작용을 일으키지 않으면서 MG와 같은 말초 신경근 접합부 질환을 표적으로 삼는 데 이상적입니다.
- 일반적으로 선천성 질환보다 후천성 중증 근무력증에 훨씬 더 효과적인 것으로 간주됩니다.
- 흡수가 불규칙하고 치료 지수가 좁기 때문에 근력 개선과 콜린성 독성 위험 사이의 균형을 맞추어 효과에 따라 용량을 주의 깊게 조절해야 합니다.
작용 기전
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.
안전성·주의사항
금기사항
- 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
부작용
- 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
주의
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.
약물 상호작용
Antagonizes the muscarinic effects of pyridostigmine. Use cautiously as it can mask early clinical signs of a life-threatening cholinergic crisis.
May decrease the anticholinesterase activity of pyridostigmine. Discontinuing corticosteroids may suddenly increase anticholinesterase activity, requiring dose adjustments.
Theoretically may have additive cholinergic effects when used concurrently.
May necessitate increased dosages of pyridostigmine when treating or diagnosing myasthenic patients.
Can antagonize anticholinesterase therapy due to its direct depressant effect on skeletal muscle.
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).
May antagonize the neuromuscular effects of pyridostigmine
May antagonize the neuromuscular effects of pyridostigmine
May antagonize the neuromuscular effects of pyridostigmine
May antagonize the effects of pyridostigmine
Pyridostigmine may enhance the effect of depolarizing muscle relaxants
Pyridostigmine antagonizes the effect of non-depolarizing muscle relaxants
Pyridostigmine antagonizes the effect of non-depolarizing muscle relaxants
모니터링
- 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)
약동학
흡수
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.
분포
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.
대사
Metabolized by the liver and hydrolyzed by cholinesterases.
배설
Excreted primarily via the kidneys (implied by class, though specific veterinary elimination data is sparse in the monograph).
과다투여
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).
제품
제형
- Extended-release tablets
- Injection
- 60 mg tablets
- 60 mg/5 ml oral syrup (available on import licence)
인용의약품
- 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
규제 현황
Human registered products often used under the cascade.
POM (Prescription Only Medicine). Oral syrup available on import licence.
규제 데이터 없음: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
보관·안정성
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.
보호자 정보
피리도스티그민은 반려동물의 중증 근무력증을 관리하는 데 매우 중요한 약물이지만, 용량을 매우 정확하게 지켜야 합니다.
- 엄격한 투약: 수의사가 처방한 대로 정확하게 이 약을 투여하십시오. 유효 용량과 독성 용량의 차이가 매우 작으므로 수의사와 상의 없이 용량을 변경하지 마십시오.
- 투여 방법: 음식과 함께 약을 투여하면 위장 장애를 줄이는 데 도움이 될 수 있습니다. 미세한 용량 조절을 위해 액체 형태가 선호되는 경우가 많습니다.
- 독성 주의: 과도한 침 흘림, 구토, 설사, 극심한 쇠약, 근육 경련 또는 호흡 곤란과 같은 과다 복용의 징후가 나타나면 즉시 수의사에게 연락하십시오.
- 자연 관해: 일부 개의 경우 중증 근무력증이 시간이 지남에 따라 저절로 해결될 수 있으므로, 수의사는 반려동물을 면밀히 모니터링하여 궁극적으로 약물을 줄이거나 중단할 수 있는지 확인할 것입니다.
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