Acetylcholinesterase, seen left, breaks down the neurotransmitter acetylcholine, eliminating it from the synaptic cleft. Anti-acetylcholinesterase agents are the first line of treatment in myasthenia gravis, and may be given initially to enhance the function of the remaining normal acetylcholine
receptors. The use of anti-acetylcholinesterase drugs is limited to the treatment
of mild myasthenia.

active for a longer duration at the motor endplate. With this increased
duration of action, the number of interactions between the transmitter and
receptors is increased, and muscular strength and response to repetitive
nerve stimulation is improved.The optimal dose and timing of administration of anticholinesterase drugs must be determined empirically for each individual. A beneficial affect is dose dependent.
Pyridostigmine Bromide (peer-id-oh-STIG-meen) [Mestinon, Regonol], given orally, is the most widely used anticholinesterase agent for the treatment of myasthenia gravis. It is given alone for mild muscle weakness, or in combination with corticosteroids for moderate to severe impairment. Dosage requirements vary among patients because of differences in absorption , metabolism, and excretion of the drug. Therefore, the dosage and timing of administration must be determined empirically.
Other anticholinesterase agents include ambenonium (am-be-NOE nee-um) chloride [Mytelase] and Neostigmine (nee-oh-STIG-meen) Bromide, Neostigmine Methylsulfate [Prostigmin].
All of the anticholinesterase agents are given by mouth or by injection. Before the myasthenic patient begins
the use of any of these drugs, the risks of taking the medicine must be
weighed against the good it will do. This decision is made by the patient
and their doctor, prior to which the following must be considered:
Allergies- any previous unusual or allergic reaction to ambenonium,
bromides, neostigmine, or pyridostigmine as well as allergies to other substances
such as foods, preservatives or dyes must be brought to the doctorís
attention.
Pregnancy- although these drugs have not been reported to cause birth
defects muscle weakness has occurred temporarily in some newborn babies
whose mothers took anticholinesterase agents during pregnancy, thus this
factor must be taken into consideration.
Breast-feeding- thusfar anticholinesterase agents have not been reported
to cause problems in nursing babies.
Age- these medicines are not expected to cause different side effects
or problems in children than they do in adults, nor are they expected to
cause different side effects or problems in older people than the do in
younger people, however there is no specific information comparing the use
of anticholinesterase agents among various age groups.
Concurrent use of Other Medications- inform your doctor if you are using
any of the following:
Other medical problems- may affect the use of the anticholinesterase
agent.
Side Effects- the most common adverse reactions to anticholinesterase
agents are caused by excessive cholinergic stimulation and include both
muscarinic and nicotinic effects.
Symptoms of overdose:
Rare symptoms:
More common symptoms: