Kinetics and metabolism of intramuscular neostigmine in myasthenia gravis

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Abstract
Neostigmine kinetics and metabolism were studied after intracellular administration to 8 patients with myasthenia gravis. The plasma neostigmine level declined monoexponentially from 21 ± 2 to 9 ± 1 ng/ml between 30 and 120 min. The data were interpreted in terms of a 1‐compartment model. Estimates of plasma half‐life (t½) ranged from 51.1 to 90.5 min; apparent volume of distribution varied from 32.0 to 60.6 l; and total body clearance from 434 to 549 ml/min. Approximately 80% of the drug was eliminated in urine within 24 hr either as unchanged neostigmine or its metabolites. Approximately 50% of the dose was eliminated as the unchanged drug, 15% as 3‐hydroxyphenyltrimethylammonium, and 15% as other unidentified metabolites. The neostigmine t½ based on the urinary excretion of the unchanged drug, ranged from 90.2 to 118.7 min. It was concluded that neostigmine was eliminated by renal and extrarenal mechanisms. Clinical Pharmacology and Therapeutics (1980) 28, 64–68; doi:10.1038/clpt.1980.132

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