Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C12H19N2O2.HO |
| Molecular Weight | 240.2988 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[OH-].CN(C)C(=O)OC1=CC=CC(=C1)[N+](C)(C)C
InChI
InChIKey=GTPJMRHVDZUPND-UHFFFAOYSA-M
InChI=1S/C12H19N2O2.H2O/c1-13(2)12(15)16-11-8-6-7-10(9-11)14(3,4)5;/h6-9H,1-5H3;1H2/q+1;/p-1
DescriptionSources: http://www.drugbank.ca/drugs/DB01400Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/pro/neostigmine-methylsulfate-injection.html
Sources: http://www.drugbank.ca/drugs/DB01400
Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/pro/neostigmine-methylsulfate-injection.html
Neostigmine is a cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike physostigmine, does not cross the blood-brain barrier. By inhibiting acetylcholinesterase, more acetylcholine is available in the synapse, therefore, more of it can bind to the fewer receptors present in myasthenia gravis and can better trigger muscular contraction. Neostigmine is used for the symptomatic treatment of myasthenia gravis by improving muscle tone.
CNS Activity
Sources: http://www.drugbank.ca/drugs/DB01400
Curator's Comment: Neostigmine, unlike physostigmine, does not cross the blood-brain barrier.
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
300 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/382915/ |
0.07 mg/kg single, intravenous dose: 0.07 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
NEOSTIGMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
69.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/382915/ |
0.07 mg/kg single, intravenous dose: 0.07 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
NEOSTIGMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
79.8 min EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/382915/ |
0.07 mg/kg single, intravenous dose: 0.07 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
NEOSTIGMINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1.5 h |
0.03 mg/kg single, intravenous dose: 0.03 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
NEOSTIGMINE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
75% |
0.03 mg/kg single, intravenous dose: 0.03 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
NEOSTIGMINE plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes | yes (co-administration study) Comment: information obtained from abstract: AUC of coadministered drug, parathion, parathion was significantly greater than control (65.1 versus 74.3 microg min/ml) |
PubMed
| Title | Date | PubMed |
|---|---|---|
| The prevention of muscle pains associated with the use of suxamethonium. | 1967 Dec |
|
| Myasthenia gravis syndrome associated with trimethadione. | 1970 Jun 29 |
|
| Prolonged curarization in a patient with renal failure. Case report. | 1971 May |
|
| Recurarization--fact or fiction. | 1971 Sep-Oct |
|
| Antagonism of succinylcholine paralysis in a patient with atypical pseudocholinesterase. | 1972 May |
|
| Thioridazine toxicity. Agranulocytosis and hepatitis with encephalopathy. | 1973 Apr 23 |
|
| On the interaction of drugs with the cholinergic nervous system--V. Characterization of some effects induced by physostigmine in mice: in vivo and in vitro studies. | 1978 Jan 15 |
|
| Neuropharmacology of the parasitic trematode, Schistosoma mansoni. | 1983 Jan |
|
| Effect of halogenated anaesthetics on heart rate changes during reversal of neuromuscular block with glycopyrrolate and neostigmine. | 1984 Nov |
|
| Abnormal responses to morphine-neostigmine in patients with undefined biliary type pain. | 1985 Dec |
|
| Refractory bradycardia after reversal of muscle relaxant in a diabetic with vagal neuropathy. | 1986 Nov |
|
| Prolonged bradycardia and hypotension after neostigmine administration in a patient receiving atenolol. | 1987 Dec |
|
| Spinal cholinergic neurons and the expression of morphine withdrawal symptoms in the rat. | 1987 Mar |
|
| Portal hypertension secondary to azathioprine in myasthenia gravis. | 1988 Dec |
|
| Impairment of the antagonism of vecuronium-induced paralysis and intra-operative disopyramide administration. | 1989 Jan |
|
| Complete heart block following glycopyrronium/neostigmine mixture. | 1989 May |
|
| Sensitivity to both vecuronium and neostigmine in a sero-negative myasthenic patient. | 1989 Oct |
|
| Prolonged paralysis following suxamethonium and the use of neostigmine. | 1990 Sep |
|
| Propofol bradycardia. | 1991 Jan |
|
| Acetylcholinesterase fiber-optic biosensor for detection of anticholinesterases. | 1991 May |
|
| Reversal of antihypertensive agent-induced postural hypotension with physostigmine. | 1991 May-Jun |
|
| Intrathecal cholinergic agonists lessen bupivacaine spinal-block-induced hypotension in rats. | 1994 Jul |
|
| Interaction between intrathecal neostigmine and epidural clonidine in human volunteers. | 1996 Aug |
|
| Spinal neostigmine diminishes, but does not abolish, hypotension from spinal bupivacaine in sheep. | 1996 Nov |
|
| Subarachnoid neostigmine does not affect blood pressure or heart rate during bupivacaine spinal anesthesia. | 1996 Nov-Dec |
|
| Effect of long-term administration of berberine on scopolamine-induced amnesia in rats. | 1997 Jul |
|
| Postoperative reparalysis after rocuronium following nebulized epinephrine. | 1997 Mar |
|
| Effect of glyceryl trinitrate on the sphincter of Oddi spasm evoked by prostigmine-morphine administration. | 1997 Nov |
|
| A multi-center study of intrathecal neostigmine for analgesia following vaginal hysterectomy. | 1998 Oct |
|
| Ocular myasthenia gravis and auto-immune thyroiditis in children. | 2005 Nov |
|
| Myasthenia gravis accompanied with hypokalemic periodic paralysis. | 2006 May |
|
| Synthesis and screening for acetylcholinesterase inhibitor activity of some novel 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-ones: derivatives of irbesartan key intermediate. | 2007 Dec 1 |
|
| Fresh frozen plasma transfusion for reversal of prolonged post-anaesthesia apnoea. | 2008 Apr |
|
| Heart block and prolonged Q-Tc interval following muscle relaxant reversal: a case report. | 2008 Feb |
|
| Sphincter of Oddi and its dysfunction. | 2008 Jan |
|
| Neostigmine and pilocarpine attenuated tumour necrosis factor alpha expression and cardiac hypertrophy in the heart with pressure overload. | 2008 Jan |
|
| The role of Wnt signaling in neuronal dysfunction in Alzheimer's Disease. | 2008 Jul 24 |
|
| Prucalopride: the evidence for its use in the treatment of chronic constipation. | 2008 Jun |
|
| The effect of piroxicam on the formation of postoperative, intraabdominal adhesion in rats. | 2008 Oct |
|
| Interventions for heartburn in pregnancy. | 2008 Oct 8 |
|
| Neostigmine but not sugammadex impairs upper airway dilator muscle activity and breathing. | 2008 Sep |
|
| Neostigmine decreases bupivacaine use by patient-controlled epidural analgesia during labor: a randomized controlled study. | 2009 Aug |
|
| Determining the neurotransmitter concentration profile at active synapses. | 2009 Dec |
|
| A two cases clinical report of mandragora poisoning in primary care in Crete, Greece: two case report. | 2009 Dec 16 |
|
| Relationship between anti-acetylcholine receptor antibody titres and severity of myasthenia gravis. | 2009 May |
|
| Dr Lazar Remen (1907-74): a forgotten pioneer in the treatment of myasthenia gravis. | 2009 May |
|
| Myasthenia gravis and autoimmune Addison disease in a patient with thymoma. | 2009 Sep |
|
| The validation of an in vitro colonic motility assay as a biomarker for gastrointestinal adverse drug reactions. | 2010 Jun 15 |
|
| A comparative study of two different doses of epidural neostigmine coadministered with lignocaine for post operative analgesia and sedation. | 2010 Oct |
|
| Efficacy of bupivacaine-neostigmine and bupivacaine-tramadol in caudal block in pediatric inguinal herniorrhaphy. | 2010 Sep |
Patents
Sample Use Guides
The recommended dose range of Neostigmine Methylsulfate Injection is 0.03 mg/kg to 0.07 mg/kg administered as an intravenous bolus.
Route of Administration:
Intravenous
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5PJE4BX5PX
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12313247
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588-17-0
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ACTIVE MOIETY
SUBSTANCE RECORD
