Pharmacokinetics and oral bioavailability of pyridostigmine in man.

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Aquilonius SM, Eckernas SA, Hartvig P, Lindstrom B, Osterman PO

Pharmacokinetics and oral bioavailability of pyridostigmine in man.

Eur J Clin Pharmacol. 1980 Nov;18(5):423-8. doi: 10.1007/BF00636797.

PubMed ID

7439266 [ View in PubMed

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Abstract

The pharmacokinetics of pyridostigmine was evaluated after intravenous injection in two healthy male volunteers and after oral administration to five subjects. Plasma concentrations of pyridostigmine were determined after ion pair extraction from plasma and analysis by gas chromatography - mass spectrometry with chemical ionization, using d6-pyridostigmine as internal standard. Degradation of pyridostigmine in vitro was compensated for by use of the deuterated internal standard and by rapid cooling and separation of plasma after blood sampling. After intravenous administration of pyridostigmine 2.5 mg the plasma elimination half-life was 1.52 h, the volume of distribution was 1.43 l/kg and the plasma clearance 0.65 l/kg x h. The pharmacokinetic constants were very similar after oral administration of pyridostigmine 120 mg; the elimination half-life was 1.78 +/- 0.24 h, the volume of distribution 1.64 +/- 0.29 l/kg and the plasma clearance was 0.66 +/- 0.22 l/kg x h. The bioavailability was calculated to be 7.6 +/- 2.4%. When pyridostigmine was taken together with food, the time to reach the peak plasma concentration was prolonged from 1.7 to 3.2 h. Bioavailability, however, was not influenced by concomitant food intake. "Steady-state" plasma concentrations of pyridostigmine were measured in myasthenic patients on their ordinary dose schedule of cholinesterase inhibitor drugs. More than a seven-fold difference in steady-state plasma concentration was found between patients taking approximately the same daily dose of pyridostigmine.

DrugBank Data that Cites this Article

Drugs

Pyridostigmine

Food Interactions

Drug	Interaction
Pyridostigmine	Take with food. Food decreases irritation.