ArticleJournal of pharmaceutical health care and sciences2022
Voriconazole injection may induce delayed methotrexate excretion: a case report and experimental study.
Article in Journal of pharmaceutical health care and sciences, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.
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1 citing paper in PubMed, 1 citations in OpenAlex.
- Methotrexate-Cyclodextrin Systems: Molecular Recognition, Formulation Design, and Translational Perspectives.Current issues in molecular biology · 2026Review
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7 authors at 1 institution in 1 country.
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Abstract
backgroundWe report a case of delayed excretion of methotrexate (MTX) in a pediatric patient on high-dose MTX therapy in response to a change in the concomitant dosage of voriconazole from oral to intravenous. As the intravenous, but not the oral formulation of voriconazole includes sulfobutylether-β-cyclodextrin (SBECD), which has an anionic residue, we hypothesized that SBECD inhibits the renal excretion of anionic compounds.
methodsWe evaluated the inhibitory effects of SBECD on renal excretion of phenolsulfonphthalein (PSP), which is eliminated in urine via organic anion transport systems. PSP was administered intravenously to rats at 2.5 and 25 mg/kg with or without SBECD pretreatment (320 mg/kg).
resultsThe plasma concentration of PSP at the dosage of 2.5 mg/kg were comparable between control and SBECD groups. On the other hand, at 25 mg/kg the elimination of PSP was delayed. The clearance of PSP at the dosage of 25 mg/kg was 9.71 ± 1.65 and 4.13 ± 0.76 mL/min/kg in control and SBECD groups, respectively (p < 0.05). This suggested that SBECD partly inhibits the renal excretion of anionic drugs.
conclusionThe present case report discusses the delayed elimination of MTX in high dose therapy and possible mechanism involving SBECD as an excipient in concomitant drugs. It seems better to avoid choosing injection containing SBECD for patients undergoing HD-MTX treatment. Further studies are needed to confirm the inhibitory effects of SBECD on the renal excretion of MTX, especially in high-dose regimens.
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