Neostigmine

Neostigmine is a reversible acetylcholinesterase inhibitor that increases acetylcholine at cholinergic synapses. It is used for myasthenia gravis and to reverse certain neuromuscular-blocking drugs.

Acetylcholinesterase: An enzyme that breaks down acetylcholine in cholinergic synapses. Neostigmine reversibly inhibits this enzyme, slowing acetylcholine breakdown.
Myasthenia gravis: An autoimmune disorder in which impaired neuromuscular transmission causes fluctuating weakness. Neostigmine can improve muscle strength by increasing acetylcholine at the neuromuscular junction.
Pyridostigmine: A reversible acetylcholinesterase inhibitor used chiefly for long-term symptomatic treatment of myasthenia gravis. It serves a similar role but is often preferred for ongoing treatment because its action lasts longer.
Cholinergic crisis: A severe state caused by excessive cholinergic activity, including weakness and potentially dangerous secretions or breathing impairment. Excessive acetylcholinesterase inhibition can cause this dangerous complication.
Acetylcholine: A neurotransmitter used by neurons at cholinergic synapses and by motor neurons at muscle end plates. Neostigmine increases its availability rather than binding directly to its receptors.
Neuromuscular-blocking drug: A drug that interrupts signaling between motor nerves and skeletal muscle, causing paralysis. Neostigmine can reverse blockade by increasing acetylcholine competing at muscle receptors.
Edrophonium: A short-acting acetylcholinesterase inhibitor formerly used to test for myasthenia gravis. Its brief action contrasts with neostigmine's therapeutic use and longer duration.
Bradycardia: A heart rate slower than the normal range for a person's age and circumstances. Muscarinic stimulation by increased acetylcholine can slow the heart rate.
Cholinergic synapse: A junction where a neuron releases acetylcholine to communicate with another cell. The drug alters signaling at cholinergic synapses throughout the body.
Rocuronium: A nondepolarizing neuromuscular blocker used to produce skeletal-muscle relaxation during anesthesia. Neostigmine can reverse rocuronium-induced blockade once sufficient spontaneous recovery has occurred.

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