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Pyridostigmine is a medication used to treat myasthenia gravis.
Common side effects include nausea, diarrhea, frequent urination, and abdominal pain.
Pyridostigmine was patented in 1945 and came into medical use in 1955.
1 Medical uses
2 Contraindications
3 Side effects
4 Mechanism of action
5 Names
6 References
Medical uses
Pyridostigmine is used to treat muscle weakness in people with myasthenia gravis or forms of congenital myasthenic syndrome and to combat the effects of curariform drug toxicity. Pyridostigmine bromide has been FDA approved for military use during combat situations as an agent to be given prior to exposure to the nerve agent Soman in order to increase survival. Used in particular during the first Gulf War, pyridostigmine bromide has been implicated as a causal factor in Gulf War syndrome.
Pyridostigmine sometimes is used to treat orthostatic hypotension.
It is also being prescribed ‘off-label’ for the postural tachycardia syndrome as well as complications resulting from Ehlers–Danlos syndrome.
Pyridostigmine bromide is contraindicated in cases of mechanical intestinal or urinary obstruction and should be used with caution in patients with bronchial asthma.
Side effects
Common side effects include:
Abdominal cramps
Increased salivation
Increased bronchial secretions
Constricted pupils
Facial flushing due to vasodilation
Erectile dysfunction
Mechanism of action
Pyridostigmine inhibits acetylcholinesterase in the synaptic cleft, thus slowing down the hydrolysis of acetylcholine. It is a quaternary carbamate inhibitor of cholinesterase that does not cross the blood–brain barrier which carbamylates about 30% of peripheral cholinesterase enzyme. The carbamylated enzyme eventually regenerates by natural hydrolysis and excess ACh levels revert to normal.
In a synapse, action potentials are conducted along motor nerves to their terminals where they initiate a Ca 2+ influx and the release of acetylcholine (ACh). The ACh diffuses across the synaptic cleft and binds to receptors on the post synaptic membrane, causing an influx of Na +, resulting in depolarization. If large enough, this depolarization results in an action potential. To prevent constant stimulation once the ACh is released, an enzyme called acetylcholinesterase is present in the endplate membrane close to the receptors on the post synaptic membrane, and quickly hydrolyses ACh.
Pyridostigmine bromide is available under the trade names Mestinon ( Valeant Pharmaceuticals ), Regonol and Gravitor (SUN Pharma).

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