Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C12H19N2O2.CH3O3S |
| Molecular Weight | 318.389 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CS([O-])(=O)=O.CN(C)C(=O)OC1=CC=CC(=C1)[N+](C)(C)C
InChI
InChIKey=UQDIHHVDTJLVSO-UHFFFAOYSA-M
InChI=1S/C12H19N2O2.CH4O3S/c1-13(2)12(15)16-11-8-6-7-10(9-11)14(3,4)5;1-5(2,3)4/h6-9H,1-5H3;1H3,(H,2,3,4)/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 |
|
| Myasthenia syndrome during penicillamine treatment. | 1975 Jun 28 |
|
| 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 |
|
| Refractory bradycardia after reversal of muscle relaxant in a diabetic with vagal neuropathy. | 1986 Nov |
|
| Propofol bradycardia. | 1991 Jan |
|
| Reversal of antihypertensive agent-induced postural hypotension with physostigmine. | 1991 May-Jun |
|
| Excitatory modulation by a spinal cholinergic system of a descending sympathoexcitatory pathway in rats. | 1992 Mar |
|
| 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 |
|
| [Prevention and release of epidural-morphine-induced urinary retention with phenoxybenzamine and neostigmine]. | 2000 Dec |
|
| Low-dose clonidine and neostigmine prolong the duration of intrathecal bupivacaine-fentanyl for labor analgesia. | 2000 Feb |
|
| Safety of enteral naloxone and i.v. neostigmine when used to relieve constipation. | 2003 Jun 15 |
|
| Measurement of gastric contraction activity in dogs by means of AC biosusceptometry. | 2003 May |
|
| Cardiac responses of Pacific oyster Crassostrea gigas to agents modulating cholinergic function. | 2004 Dec |
|
| Ciguatera fish poisoning in industrial ship crewmembers: a retrospective study in a seaport general practice in Trinidad and Tobago. | 2004 Sep |
|
| [Myasthenia in elderly patients: a series of 23 cases]. | 2005 Dec |
|
| Ocular myasthenia gravis and auto-immune thyroiditis in children. | 2005 Nov |
|
| Myasthenia gravis accompanied with hypokalemic periodic paralysis. | 2006 May |
|
| 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 |
|
| 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 |
|
| Determining the neurotransmitter concentration profile at active synapses. | 2009 Dec |
|
| Myasthenia gravis and autoimmune Addison disease in a patient with thymoma. | 2009 Sep |
|
| 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
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
11659722
Created by
admin on Sat Dec 16 11:01:05 GMT 2023 , Edited by admin on Sat Dec 16 11:01:05 GMT 2023
|
PRIMARY | |||
|
873090-02-9
Created by
admin on Sat Dec 16 11:01:05 GMT 2023 , Edited by admin on Sat Dec 16 11:01:05 GMT 2023
|
PRIMARY | |||
|
6F5UW4E5CF
Created by
admin on Sat Dec 16 11:01:05 GMT 2023 , Edited by admin on Sat Dec 16 11:01:05 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD
