Prostigmin - General Information:A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Prostigmin, unlike physostigmine, does not cross the blood-brain barrier. [PubChem]
Pharmacology:Prostigmin is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Prostigmin, unlike physostigmine, does not cross the blood-brain barrier.
Prostigmin for patients
Certain antibiotics, especially neomycin, streptomycin and kanamycin, have a mild but definite nondepolarizing blocking action which may accentuate neuromuscular block. These antibiotics should be used in the myasthenic patient only where definitely indicated, and then careful adjustment should be made of adjunctive anticholinesterase dosage.
Local and some general anesthetics, antiarrhythmic agents and other drugs that interfere with neuromuscular transmission should be used cautiously, if at all, in patients with myasthenia gravis; the dose of Prostigmin may have to be increased accordingly.
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.
Additional information about ProstigminProstigmin Indication: For the symptomatic treatment of myasthenia gravis.
Mechanism Of Action: Prostigmin is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors. It does not cross the blood-brain barrier.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Neostigmine
Synonyms: Not Available
Drug Category: Cholinesterase Inhibitors; Parasympathomimetics
Drug Type: Small Molecule; Approved
Other Brand Names containing Neostigmine: Neostigmine omega; Prostigmin;
Absorption: Neostigmine bromide is poorly absorbed from the gastrointestinal tract following oral administration
Toxicity (Overdose): Overdosage of Neostigmine can cause cholinergic crisis, which is characterized by increasing muscle weakness, and through involvement of the muscles of respiration, may result in death. The LD 50 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 LD 50 is 0.315 ± 0.019 mg/kg intravenously, 0.445 ± 0.032 mg/kg subcutaneously, and 0.423 ± 0.032 mg/kg intramuscularly.
Protein Binding: Protein binding to human serum albumin ranges from 15 to 25 percent.
Biotransformation: Neostigmine undergoes hydrolysis by cholinesterase and is also metabolized by microsomal enzymes in the liver.
Half Life: The half-life ranged from 42 to 60 minutes with a mean half-life of 52 minutes.
Dosage Forms of Prostigmin: Tablet Oral
Chemical IUPAC Name: [3-(dimethylcarbamoyloxy)phenyl]-trimethylazanium
Chemical Formula: C12H19N2O2+
Neostigmine on Wikipedia: http://en.wikipedia.org/wiki/Neostigmine
Organisms Affected: Humans and other mammals
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