Drug/Small Molecule:
neostigmine

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
Trade Names
  • Neostigmine omega
  • Prostigmin
Brand Mixture Names

PharmGKB Accession Id:
PA450611

Description

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.

Source: Drug Bank

Indication

Neostigmine is used for the symptomatic treatment of myasthenia gravis by improving muscle tone.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. The drug inhibits acetylcholinesterase which is responsible for the degredation of acetylcholine. So, with acetylcholinesterase inhibited, more acetylcholine is present By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors which are involved in muscle contraction.. It does not cross the blood-brain barrier.

Source: Drug Bank

Pharmacology

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.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Neostigmine undergoes hydrolysis by cholinesterase and is also metabolized by microsomal enzymes in the liver.

Source: Drug Bank

Protein Binding

Protein binding to human serum albumin ranges from 15 to 25 percent.

Source: Drug Bank

Absorption

Neostigmine bromide is poorly absorbed from the gastrointestinal tract following oral administration

Source: Drug Bank

Half-Life

The half-life ranged from 42 to 60 minutes with a mean half-life of 52 minutes.

Source: Drug Bank

Toxicity

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.

Source: Drug Bank

Chemical Properties

Chemical Formula

C12H19N2O2

Source: Drug Bank

Isomeric SMILES

CN(C)C(=O)OC1=CC(=CC=C1)[N+](C)(C)C

Source: Drug Bank

Canonical SMILES

CN(C)C(=O)OC1=CC(=CC=C1)[N+](C)(C)C

Source: Drug Bank

Average Molecular Weight

223.2915

Source: Drug Bank

Monoisotopic Molecular Weight

223.144652862

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
ACHE (source: Drug Bank)

Drug Interactions

Drug Description
neostigmine The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
neostigmine The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, neostigmine. (source: Drug Bank)
neostigmine The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, neostigmine. (source: Drug Bank)
neostigmine The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
neostigmine The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, neostigmine. (source: Drug Bank)
neostigmine The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
neostigmine The corticosteroid, prednisolone, may decrease the effect of the anticholinesterase, neostigmine. (source: Drug Bank)
neostigmine The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
neostigmine The corticosteroid, prednisone, may decrease the effect of the anticholinesterase, neostigmine. (source: Drug Bank)
neostigmine The corticosteroid decreases the effect of anticholinesterases (source: Drug Bank)
neostigmine The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, neostigmine. (source: Drug Bank)

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01400
ChEBI:
7514
KEGG Compound:
C07258
PubChem Compound:
4456
PubChem Substance:
46509161
9467
Drugs Product Database (DPD):
868906
ChemSpider:
4301
Therapeutic Targets Database:
DAP000563

Clinical Trials

These are trials that mention neostigmine and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.