Neostigmine

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Normastigmin; Belgium: Prostigmine; Bulgaria: Syntostigmin; Cyprus: Neostigmin; Czech Republic: Syntostigmin; France: Prostigmine; Germany: Jorinda, Konstigmin, Neostig, Neostigmin, Sylvemid; Greece: Neostigmine, Normastigmin, Prostigmine; Hungary: Stigmosan; Ireland: Neostigmine; Italy: Intrastigmina, Prostigmina; Lithuania: Syntostigmin; Luxembourg: Prostigmine; Malta: Neostigmine; Netherlands: Neostigmine, Prostigmin; Poland: Polstigminum; Portugal: Intrastigmina, Neostigmine; Romania: Neostigmina; Slovakia: Syntostigmin; Spain: Neostigmina, Prostigmine; Sweden: Neostigmin; UK: Neostigmine.

North America

Canada: Neostigmine, Prostigmin.

Latin America

Argentina: Fadastigmina, Neostigmina; Brazil: Normastig, Prostigmine; Mexico: Prostigmine.

Asia

Japan: Neostigmine, Vagostigmin.

Drug combinations

Neostigmine and Glycopyrrolate

Chemistry

Neostigmine Bromide: C~12~H~19~BrN~2~O~2~. Mw: 303.20. (1) Benzenaminium, 3-[[(dimethylamino)carbonyl]oxy]-N,N,N-trimethyl-, bromide; (2)(m-Hydroxyphenyl)trimethylammonium bromide dimethylcarbamate. CAS-114-80-7; CAS-59-99-4 (neostigmine).

Neostigmine Methylsulfate: C~13~H~22~N~2~O S. Mw: 334.39. Benzenaminium, 3-[[(dimethylamino)carbonyl]oxy]-N,N,N-trimethyl-, methyl sulfate. CAS-51-60-5.

Pharmacologic Category

Parasympathomimetic (Cholinergic) Agents; Acetylcholinesterase Inhibitor. Diagnostic Agents; Myasthenia Gravis. (ATC-Code: N07AA01; S01EB06).

Mechanism of action

Inhibits destruction of acetylcholine by acetylcholinesterase, which facilitates transmission of impulses across myoneural junction.

Therapeutic use

Diagnosis and treatment of myasthenia gravis. Prevention and treatment of postoperative bladder distention and urinary retention. Reversal of effects of nondepolarizing neuromuscular-blocking agents after surgery.

Pregnancy and lactiation implications

Use with caution in pregnancy. Excretion in breast milk unknown (not recommended in nursing women).

Unlabeled use

Contraindications

Hypersensitivity to neostigmine, bromides, or any component of the formulation. Gastrointestinal or genitourinary obstruction.

Warnings and precautions

Anticholinesterase insensitivity can develop for brief or prolonged periods. Overdosage may result in cholinergic crisis. Hypersensitivity reactions might occur. Use with caution in asthma, hyperthyroidism, bradycardia and cardiac arrhythmias, and gastrointestinal disease, including peptic ulcer disease; also in history of seizure disorder. Not generally recommended for use in vagotonia. Does not antagonize and may prolong phase I block of depolarizing muscle relaxants (e.g. succinylcholine).

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