Neostigmine
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Neostigmine, sold under the brand name Bloxiverz, among others, is a medication used to treat myasthenia gravis, Ogilvie syndrome, and urinary retention without the presence of a blockage.[3][4] It is also used in anaesthesia to end the effects of non-depolarising neuromuscular blocking medication.[3] It is given by injection either into a vein, muscle, or under the skin.[3] After injection effects are generally greatest within 30 minutes and last up to 4 hours.[3][5]
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Trade names | Bloxiverz, Prostigmin, Vagostigmin, others |
AHFS/Drugs.com | Monograph |
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Routes of administration | Intramuscular, intravenous, subcutaneous, by mouth |
Drug class | Cholinesterase inhibitor |
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Bioavailability | Unclear, probably less than 5% |
Metabolism | Slow hydrolysis by acetylcholinesterase and also by plasma esterases |
Onset of action | Within 10-20 min (injection),[3] with 4 hrs (by mouth) [citation needed] |
Elimination half-life | 50–90 minutes |
Duration of action | up to 4 hrs[3] |
Excretion | Unchanged drug (up to 70%) and alcoholic metabolite (30%) are excreted in the urine |
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ECHA InfoCard | 100.305.602 |
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Formula | C12H19N2O2+ |
Molar mass | 223.296 g·mol−1 |
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Common side effects include nausea, increased saliva, crampy abdominal pain, and slow heart rate.[3] More severe side effects include low blood pressure, weakness, and allergic reactions.[3] It is unclear if use in pregnancy is safe for the baby.[3] Neostigmine is in the cholinergic family of medications.[3] It works by blocking the action of acetylcholinesterase and therefore increases the levels of acetylcholine.[3]
Neostigmine was patented in 1931.[6] It is on the World Health Organization's List of Essential Medicines.[7] The term is from Greek neos, meaning "new", and "-stigmine", in reference to its parent molecule, physostigmine, on which it is based.[8] It is available as a generic medication.[9]