Prostigmine (Neostigmine)
Effects
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
Dosing
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
Renal dosing
- Creatinine Clearance 10-50 decrease dose by 50%
- Creatinine Clearance <10 decrease dose by 75%
Excretion
- Urine (50% unchanged)
- Recommended Creatinine level at baseline
Side Effects
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