Cholinesterase inhibitors increase activity at acetylcholine receptors by blocking the breakdown of acetylcholine by the enzyme acetylcholinesterase. The result of blocking this enzyme is that theres a buildup of acetylcholine in the synapse and continuous activation of the cholinergic receptors.

Cholinesterase inhibitors are used to treat Alzheimers disease and myasthenia gravis. In both of these conditions, theres a severe decrease in the amount of acetylcholine receptor stimulation. Cholinesterase inhibitors, including donepezil (Aricept®), rivastigmine (Exelon®) and galantamine (Razadyne®), increase cholinergic transmission by inhibiting cholinesterase at the synapse. This action provides modest symptomatic benefits in some people with dementia.

Botulinum toxin  used to treat muscle spasticity, cosmetic wrinkles and migraines  works by preventing acetylcholine release from the end of nerve cells.