Disposition of intravenous pyrimethamine in healthy volunteers.

Abstract:

:A proportion of patients with AIDS and toxoplasmic encephalitis (TE) sustain low plasma pyrimethamine concentrations during oral treatment, possibly because of incomplete and variable bioavailability. We wanted to develop a safe, practicable intravenous (i.v.) formulation of pyrimethamine and characterize its disposition in healthy volunteers. A neutral, aqueous, sterile solution of pyrimethamine was produced and presented in sealed glass ampoules. Pyrimethamine (1 mg/kg) was given to eight healthy male volunteers by i.v. infusion over 2 h, and blood was sampled over a 2 week period. Pyrimethamine levels in plasma were measured by high-performance liquid chromatography. The drug was well tolerated by all volunteers, and there were no changes in vital signs, electrocardiogram, hematology, or biochemical parameters. The maximum pyrimethamine concentration of 2,089+/-565 ng ml(-1) (mean +/- standard deviation) was achieved shortly after the end of the infusion; thereafter, concentrations declined in a log-linear manner, with a half-life of 140+/-31 h.

authors

Almond DS,Szwandt IS,Edwards G,Lee MG,Winstanley PA

doi

10.1128/aac.44.6.1691-1693.2000

subject

Has Abstract

pub_date

2000-06-01 00:00:00

pages

1691-3

issue

6

eissn

0066-4804

issn

1098-6596

journal_volume

44

pub_type

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