Prostigmine (Neostigmine)

Anticholinesterase drug

• Reduces breakdown of Acetylcholine in the neuromuscular junction by inhibiting acetylcholinesterase
• Reversibly binds to and inactivates acetylcholinesterase
• Has less effect on the eye, heart and brain than physostigmine but has more effect on GI tract and bladder
• Acetylcholine Effects

To diagnose Myasthenia Gravis

• 1mg for 70kg Adult (or 0.02 mg/kg) IM, Give with 0.4 mg Atropine IM

To treat Myasthenia Gravis

• Start with 15 mg PO Q8h, Max 375 mg/day
• 15 mg PO = 0.5 mg SC/IM/IV

• Creatinine Clearance 10-50 decrease dose by 50%
• Creatinine Clearance <10 decrease dose by 75%

• Urine (50% unchanged)
• Recommended Creatinine level at baseline

Common Reactions

• hypersalivation
• fasciculation
• abdominal bloating/cramps
• loose stools/diarrhea
• flatulence
• dyspepsia
• headache
• dizziness
• diaphoresis
• lacrimation increase
• rhinorrhea
• pulmonary secretions increase
• dyspnea
• nausea/vomiting
• urinary frequency/urgency
• muscle weakness/cramps
• miosis
• visual changes
• rash
• drowsiness

Serious Reactions

• Cholinergic crisis:
  • overstimulation at the neuromuscular junction leading to
    • flaccid paralysis
    • respiratory failure
    • increased sweating
    • salivation
    • bronchial secretions
    • mitosis
  • treated with Atropine
• bradycardia
• AV block
• arrhythmias
• hypotension
• severe syncope
• cardiac arrest
• bronchospasm
• respiratory depression
• respiratory arrest
• respiratory paralysis
• paralysis
• anaphylaxis
• hypersensitivity reaction
• seizures