Disposition of intravenous pyrimethamine in healthy volunteers. NLM AIDSLINE Important note: Information in this article was accurate in 2000. The state of the art may have changed since the publication date.

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Disposition of intravenous pyrimethamine in healthy volunteers.

Antimicrob Agents Chemother. 2000 Jun;44(6):1691-3. Unique Identifier : AIDSLINE MED/20277902
Almond DS; Szwandt IS; Edwards G; Lee MG; Winstanley PA; Department of Pharmacology and Therapeutics, University of; Liverpool, Liverpool L69 3GE, United Kingdom.

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.
Keywords: JOURNAL ARTICLE Acquired Immunodeficiency Syndrome/DRUG THERAPY Antimalarials/*ADMINISTRATION & DOSAGE/*PHARMACOKINETICS Encephalitis/DRUG THERAPY Human Infusions, Intravenous Male Pyrimethamine/*ADMINISTRATION & DOSAGE/*PHARMACOKINETICS Support, Non-U.S. Gov't

KWDjournalarticleacquiredimmunodeficiencysyndrome/drugtherapyantimalarials/KWDadministration&dosage/KWDpharmacokineticsencephalitis/drugtherapyhumaninfusions,intravenousmalepyrimethamine/KWDadministration&dosage/KWDpharmacokineticssupport,non-uKWDsKWDgov't
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A0090766

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