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- Jansson Löfmark, Rasmus,1979Gothenburg University,Göteborgs universitet,Institutionen för neurovetenskap och fysiologi, sektionen för farmakologi,Institute of Neuroscience and Physiology, Department of Pharmacology (author)
Enantiospecific Reassessment of the Pharmacokinetics and Pharmacodynamics of Oral Eflornithine against Late-Stage Trypanosoma brucei gambiense Sleeping Sickness
- Article/chapterEnglish2015
Publisher, publication year, extent ...
- American Society for Microbiology,2015
Numbers
- LIBRIS-ID:oai:gup.ub.gu.se/213502
- https://gup.ub.gu.se/publication/213502URI
- https://doi.org/10.1128/aac.04101-14DOI
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- Language:English
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Notes
- This study aimed to characterize the stereoselective pharmacokinetics of oral eflornithine in 25 patients with late-stage Trypanosoma brucei gambiense sleeping sickness. A secondary aim was to determine the concentrations of L-and D-eflornithine required in plasma or cerebrospinal fluid (CSF) for an efficient eradication of the T. brucei gambiense parasites. Patients were randomly allocated to receive either 100 (group I, n = 12) or 125 (group II, n = 13) mg/kg of body weight of drug every 6 h for 14 days. The concentrations of L-and D-eflornithine in the plasma and CSF samples were measured using a stereospecific liquid chromatographic method. Nonlinear mixed-effects modeling was used to characterize the plasma pharmacokinetics. The plasma concentrations of L-eflornithine were on average 52% (95% confidence interval [CI], 51, 54%; n = 321) of the D-enantiomer concentrations. The typical oral clearances of L-and D-eflornithine were 17.4 (95% CI, 15.5, 19.3) and 8.23 (95% CI, 7.36, 9.10) liters/h, respectively. These differences were likely due to stereoselective intestinal absorption. The distributions of eflornithine enantiomers to the CSF were not stereoselective. A correlation was found between the probability of cure and plasma drug exposure, although it was not more pronounced for the L-enantiomer than for that of total eflornithine. This study may explain why oral treatment for late-stage human African trypanosomiasis (HAT) patients with racemic eflornithine has previously failed; the more potent L-enantiomer is present at much lower concentrations in both plasma and CSF than those of the D-enantiomer. Eflornithine stereoselective pharmacokinetics needs to be considered if an oral dosage regimen is to be explored further.
Subject headings and genre
- MEDICIN OCH HÄLSOVETENSKAP Medicinska och farmaceutiska grundvetenskaper Farmakologi och toxikologi hsv//swe
- MEDICAL AND HEALTH SCIENCES Basic Medicine Pharmacology and Toxicology hsv//eng
- HUMAN AFRICAN TRYPANOSOMIASIS
- CEREBROSPINAL-FLUID
- ALPHA-DIFLUOROMETHYLORNITHINE
- ORNITHINE-DECARBOXYLASE
- COMBINATION
- THERAPY
- DRUG ABSORPTION
- MODEL
- MELARSOPROL
- ENANTIOMERS
- PLASMA
- Microbiology
- Pharmacology & Pharmacy
Added entries (persons, corporate bodies, meetings, titles ...)
- Na-Bangchang, K. (author)
- Bjorkman, S. (author)
- Doua, F. (author)
- Ashton, Michael,1955Gothenburg University,Göteborgs universitet,Institutionen för neurovetenskap och fysiologi, sektionen för farmakologi,Institute of Neuroscience and Physiology, Department of Pharmacology(Swepub:gu)xashmi (author)
- Göteborgs universitetInstitutionen för neurovetenskap och fysiologi, sektionen för farmakologi (creator_code:org_t)
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- In:Antimicrobial Agents and Chemotherapy: American Society for Microbiology59:2, s. 1299-13070066-48041098-6596
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