Disease Related

NEOSTIGMINE

Neostigmine is a reversible acetylcholinesterase inhibitor used primarily in the treatment of myasthenia gravis and to reverse the effects of neuromuscular blocking agents after surgery. Unlike physostigmine, neostigmine does not cross the blood-brain barrier, making it more suited for peripheral applications. It increases acetylcholine levels at neuromuscular junctions, enhancing muscle contraction and improving strength in affected patients. Neostigmine is also used in the management of urinary retention and to stimulate gastrointestinal motility.

Neostigmine is a cholinergic agent that inhibits the breakdown of acetylcholine (ACh) in the body, thereby increasing its levels and duration of action.

Chemical Structure:

  • Molecular Formula: C12H19N2O2
  • Chemical Name: 3-(dimethylcarbamoyloxy)-N,N-diethyl-2-[(phenylmethyl)amino]ethanaminium

Pharmacological Effects:

  • Inhibits acetylcholinesterase, leading to:
    • Increased muscle contraction
    • Increased salivation and sweating
    • Pupil constriction (miosis)
    • Increased gastrointestinal motility and secretion
    • Urinary bladder contraction
    • Bronchoconstriction

Clinical Uses:

  • Treatment of:
    • Myasthenia gravis
    • Reversal of neuromuscular blockade
    • Postoperative ileus
    • Urinary retention
  • Diagnostic tool for:
    • Myasthenia gravis

Side Effects:

  • Nausea, vomiting, and diarrhea
  • Headache, dizziness, and weakness
  • Abdominal cramps and discomfort
  • Flushing, sweating, and hypersalivation
  • Bronchospasm and respiratory distress (rare)

Contraindications:

  • Asthma and other respiratory conditions
  • Peptic ulcer disease
  • Hyperthyroidism
  • Pregnancy and lactation
  • Hypotension and cardiac arrhythmias

Note: Neostigmine is a potent cholinergic agent and should be used with caution, under medical supervision.

Neostigmine is commonly used in anesthesia to reverse the effects of non-depolarizing neuromuscular blockers, and in the treatment of myasthenia gravis.