Neostigmine
| Clinical data | |
|---|---|
| Trade names | Bloxiverz, Prostigmin, Vagostigmin, others |
| AHFS/Drugs.com | Monograph |
| License data |
|
| Pregnancy category |
|
| Routes of administration | Intramuscular, intravenous, subcutaneous, by mouth |
| Drug class | Cholinesterase inhibitor |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| 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) |
| 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 |
| Identifiers | |
IUPAC name
| |
| CAS Number | |
| PubChem CID | |
| DrugBank |
|
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEBI | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.305.602 |
| Chemical and physical data | |
| Formula | C12H19N2O2+ |
| Molar mass | 223.296 g·mol−1 |
| 3D model (JSmol) | |
SMILES
| |
InChI
| |
| (what is this?) (verify) | |
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]
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 the alkaloid, physostigmine, which inspired its design.[8] It is available as a generic medication.[9]
- ^ "Neostigmine Use During Pregnancy". Drugs.com. 3 January 2020. Retrieved 21 January 2020.
- ^ "Bloxiverz- neostigmine methylsulfate injection". DailyMed. 3 March 2021. Retrieved 15 July 2022.
- ^ a b c d e f g h i j k "Neostigmine Bromide". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
- ^ World Health Organization (2009). Stuart MC, Kouimtzi M, Hill SR (eds.). WHO Model Formulary 2008. World Health Organization. p. 428. hdl:10665/44053. ISBN 9789241547659.
- ^ "Neostigmine Methylsulfate Monograph for Professionals". Drugs.com. The American Society of Health-System Pharmacists. 19 September 2019. Retrieved 20 January 2020.
- ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 540. ISBN 9783527607495. Archived from the original on 20 December 2016.
- ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ^ "neostigmine: definition of neostigmine in Oxford dictionary (American English) (US)". www.oxforddictionaries.com. Archived from the original on 22 December 2015. Retrieved 17 December 2015.
- ^ "Competitive Generic Therapy Approvals". U.S. Food and Drug Administration (FDA). 29 June 2023. Archived from the original on 29 June 2023. Retrieved 29 June 2023.