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Neostigmine

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Description

Generic Name

Neostigmine

Chemical names

3-Trimethylammoniumphenyl N, N-dimethylcarbamate

Brand names

Eustigmin, Eustigmine, Vagostigmin

IUPAC name

3-[(dimethylcarbamoyl)oxy]-N,N,N-trimethylanilinium

Pharmacokinetics

  • Poorly absorbed from the gastrointestinal tract following oral administration
  • Metabolized by microsomal enzymes in the liver.
  • Does not cross BBB

Actions

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. 

Dosage/Dosage form

  • Total daily dose is 75-300 mg in divided doses orally for myasthenia.
  • 50-70 mcg/kg by IV injection over 60 seconds 
  •  Instill 1-2 drops of 0.5% solution into the eyes 1-4 times daily for glaucoma.

Therapeutic uses

Myasthenia gravis, Paralytic ileus and postoperative urinary retention, Reversal of neuromuscular blockade.

Adverse effects/Side effects

Nausea and vomiting increased salivation and sweating, abdominal cramps, allergic reactions, diarrhea, rash, bradycardia, hypotension.

Interaction

Effects may be reduced by quinine, chloroquine, hydroxychloroquine, quinidine, propafenone, procainamide, lithium, β-blockers. 

Contraindications

Pregnancy, Lactation

Storage

Protect from light. Store at 15-30°C. Do not freeze. 

Information

Molecular weight

223.294

Molecular formula

C12H19N2O2

CAS number

59-99-4

Precautions

Frequently assess muscle strength and function in patient with myasthenia gravis or patient recovering from non depolarizing neuromuscular blocking agent.