Prostigmin

Overdosage of Prostigmin (neostigmine) can cause cholinergic crisis, which is characterized by increasing muscle weakness, and through involvement of the muscles of respiration, may result in death. Myasthenic crisis, due to an increase in the severity of the disease, is also accompanied by extreme muscle weakness and may be difficult to distinguish from cholinergic crisis on a symptomatic basis. However, such differentiation is extremely important because increases in the dose of Prostigmin (neostigmine) or other drugs in this class, in the presence of cholinergic crisis or of a refractory or “insensitive” state, could have grave consequences. The two types of crises may be differentiated by the use of Tensilon® (edrophonium chloride) as well as by clinical judgment.

Treatment of the two conditions differs radically. Whereas the presence of myasthenic crisis requires more intensive anticholinesterase therapy, cholinergic crisis calls for the prompt withdrawal of all drugs of this type. The immediate use of atropine in cholinergic crisis is also recommended.

Atropine may also be used to abolish or minimize gastrointestinal side effects or other muscarinic reactions; but such use, by masking signs of overdosage, can lead to inadvertent induction of cholinergic crisis.

The LD50 of neostigmine methylsulfate in mice is 0.3 ± 0.02 mg/kg intravenously, 0.54 ± 0.03 mg/kg subcutaneously, and 0.395 ± 0.025 mg/kg intramuscularly; in rats the LD50 is 0.315 ± 0.019 mg/kg intravenously, 0.445 ± 0.032 mg/kg subcutaneously, and 0.423 ± 0.032 mg/kg intramuscularly.

This medication may cause blurred vision or impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert and able to see clearly.

Drinking alcohol can increase drowsiness caused by neostigmine.

Your pharmacist can provide more information about neostigmine.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

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Side effects are generally due to an exaggeration of pharmacological effects of which salivation and fasciculation are the most common. Bowel cramps and diarrhea may also occur.

The following additional adverse reactions have been reported following the use of either neostigmine bromide or neostigmine methylsulfate:

Allergic: Allergic reactions and anaphylaxis.

Neurologic: Dizziness, convulsions, loss of consciousness, drowsiness, headache, dysarthria, miosis and visual changes.

Cardiovascular: Cardiac arrhythmias (including bradycardia, tachycardia, A-V block and nodal rhythm) and nonspecific EKG changes have been reported, as well as cardiac arrest, syncope and hypotension. These have been predominantly noted following the use of the injectable form of Prostigmin (neostigmine) .

Respiratory: Increased oral, pharyngeal and brochial secretions, and dyspnea. Respiratory depression, respiratory arrest and bronchospasm have been reported following the use of the injectable form of Prostigmin (neostigmine) .

Dermatologic: Rash and urticaria.

Gastrointestinal: Nausea, emesis, flatulence and increased peristalsis.

Genitourinary: Urinary frequency.

Musculoskeletal: Muscle cramps and spasms, arthralgia.

Miscellaneous: Diaphoresis, flushing and weakness.

Read the entire FDA prescribing information for Prostigmin (Neostigmine)

Common side effects of neostigmine methylsulfate include a slower heart beat, nausea, and vomiting.

This is not a complete list of neostigmine methylsulfate side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
 

• It is used to treat myasthenia gravis.
• It may be given to you for other reasons. Talk with the doctor.

• Tell all of your health care providers that you take this medicine. This includes your doctors, nurses, pharmacists, and dentists.
• Talk with your doctor before you drink alcohol.
• If you are 65 or older, use Prostigmin with care. You could have more side effects.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

Neostigmine inhibits the hydrolysis of acetylcholine by competing with acetylcholine for attachment to acetylcholinesterase at sites of cholinergic transmission. It enhances cholinergic action by facilitating the transmission of impulses across neuromuscular junctions. It also has a direct cholinomimetic effect on skeletal muscle and possibly on autonomic ganglion cells and neurons of the central nervous system. Neostigmine undergoes hydrolysis by cholinesterase and is also metabolized by microsomal enzymes in the liver. Protein binding to human serum albumin ranges from 15 to 25 percent.

Neostigmine bromide is poorly absorbed from the gastrointestinal tract following oral administration. As a rule, 15 mg of neostigmine bromide orally is equivalent to 0.5 mg of neostigmine methylsulfate parenterally, due to poor absorption of the tablet from the intestinal tract. In a study in fasting myasthenic patients, the extent of absorption was estimated to be 1 to 2 percent of the ingested 30-mg single oral dose. Peak concentrations in plasma occurred 1 to 2 hours following drug ingestion, with considerable individual variations. The half-life ranged from 42 to 60 minutes with a mean half-life of 52 minutes.

Prostigmin is contraindicated in patients with known hypersensitivity to the drug. Because of the presence of the bromide ion, it should not be used in patients with a previous history of reaction to bromides. It is contraindicated in patients with peritonitis or mechanical obstruction of the intestinal or urinary tract.