Literature DB >> 3243326

Pharmacokinetic and metabolic studies of busulfan in rat plasma and brain.

M Hassan1, H Ehrsson, I Wallin, S Eksborg.   

Abstract

Busulfan kinetics were studied in the rat plasma and brain after an I.P. dose of 14C-busulfan or busulfan (15 mg/kg). The distribution of busulfan to the brain was rapid and the ratio brain/plasma concentration was 0.74 during the time-course of busulfan. The elimination half-lives in plasma and brain were 3h for intact busulfan and 8h for the 14C-radioactivity. The radioactivity remaining in plasma and brain after 24h was mostly busulfan metabolites e.g. sulfolane, 3-hydroxysulfolane and tetrahydrothiophene-1-oxide as identified by gas chromatography-mass spectrometry. The protein binding to rat plasma was low (9.2 +/- 4.4%).

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Year:  1988        PMID： 3243326     DOI： 10.1007/BF03190094

Source DB:  PubMed          Journal:  Eur J Drug Metab Pharmacokinet        ISSN： 0378-7966            Impact factor:   2.441


  17 in total

1.  Hydrophobicity and central nervous system agents: on the principle of minimal hydrophobicity in drug design.

Authors:  C Hansch; J P Björkroth; A Leo
Journal:  J Pharm Sci       Date:  1987-09       Impact factor: 3.534

2.  Distribution and metabolic fate of S35-labeled myleran (busulfan) in normal and tumor-bearing rats.

Authors:  C T PENG
Journal:  J Pharmacol Exp Ther       Date:  1957-06       Impact factor: 4.030

3.  Pentazocine binding to blood cells and plasma proteins.

Authors:  M Ehrnebo; S Agurell; L O Boréus; E Gordon; U Lönroth
Journal:  Clin Pharmacol Ther       Date:  1974-09       Impact factor: 6.875

4.  Comparative brain and plasma pharmacokinetics and anticancer activities of chlorambucil and melphalan in the rat.

Authors:  N H Greig; D J Sweeney; S I Rapoport
Journal:  Cancer Chemother Pharmacol       Date:  1988       Impact factor: 3.333

5.  Gas chromatographic determination of busulfan in plasma with electron-capture detection.

Authors:  M Hassan; H Ehrsson
Journal:  J Chromatogr       Date:  1983-10-14

6.  Degradation of melphalan in aqueous solutions--influence of human albumin binding.

Authors:  H Ehrsson; U Lönroth
Journal:  J Pharm Sci       Date:  1982-07       Impact factor: 3.534

7.  Bone marrow transplantation for leukemia following a new busulfan and cyclophosphamide regimen.

Authors:  P J Tutschka; E A Copelan; J P Klein
Journal:  Blood       Date:  1987-11       Impact factor: 22.113

8.  Busulfan and total body irradiation as antihematopoietic stem cell agents in the preparation of patients with congenital bone marrow disorders for allogenic bone marrow transplantation.

Authors:  R Parkman; J M Rappeport; S Hellman; J Lipton; B Smith; R Geha; D G Nathan
Journal:  Blood       Date:  1984-10       Impact factor: 22.113

9.  Methotrexate: distribution in cerebrospinal fluid after intravenous, ventricular and lumbar injections.

Authors:  W R Shapiro; D F Young; B M Mehta
Journal:  N Engl J Med       Date:  1975-07-24       Impact factor: 91.245

10.  Urinary metabolites of busulfan in the rat.

Authors:  M Hassan; H Ehrsson
Journal:  Drug Metab Dispos       Date:  1987 May-Jun       Impact factor: 3.922
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  8 in total

Review 1.  The role of busulfan in bone marrow transplantation.

Authors:  M Hassan
Journal:  Med Oncol       Date:  1999-09       Impact factor: 3.064

2.  In vivo distribution of [11C]-busulfan in cynomolgus monkey and in the brain of a human patient.

Authors:  M Hassan; G Oberg; K Ericson; H Ehrsson; L Eriksson; M Ingvar; S Stone-Elander; J O Thorell; B Smedmyr; N Warne
Journal:  Cancer Chemother Pharmacol       Date:  1992       Impact factor: 3.333

3.  Influence of prophylactic anticonvulsant therapy on high-dose busulphan kinetics.

Authors:  M Hassan; G Oberg; M Björkholm; I Wallin; M Lindgren
Journal:  Cancer Chemother Pharmacol       Date:  1993       Impact factor: 3.333

4.  Flavin-containing monooxygenase 3 (FMO3) role in busulphan metabolic pathway.

Authors:  Ibrahim El-Serafi; Ylva Terelius; Manuchehr Abedi-Valugerdi; Seán Naughton; Maryam Saghafian; Ali Moshfegh; Jonas Mattsson; Zuzana Potácová; Moustapha Hassan
Journal:  PLoS One       Date:  2017-11-09       Impact factor: 3.240

5.  The effect of N-acetyl-l-cysteine (NAC) on liver toxicity and clinical outcome after hematopoietic stem cell transplantation.

Authors:  Ibrahim El-Serafi; Mats Remberger; Ahmed El-Serafi; Fadwa Benkessou; Wenyi Zheng; Eva Martell; Per Ljungman; Jonas Mattsson; Moustapha Hassan
Journal:  Sci Rep       Date:  2018-05-29       Impact factor: 4.379

6.  Population pharmacokinetic modelling of busulfan and the influence of body composition in paediatric Fanconi anaemia patients.

Authors:  Matthijs W van Hoogdalem; Chie Emoto; Tsuyoshi Fukuda; Tomoyuki Mizuno; Parinda A Mehta; Alexander A Vinks
Journal:  Br J Clin Pharmacol       Date:  2020-01-23       Impact factor: 4.335

7.  Vitamin D levels and busulphan kinetics in patients undergoing hematopoietic stem cell transplantation, a multicenter study.

Authors:  Ahmed El-Serafi; Rui He; Wenyi Zheng; Fadwa Benkossou; Sandra Oerther; Ying Zhao; Karin Mellgren; Britt Gustafsson; Carsten Heilmann; Jukka Kanerva; Kourosh Lotfi; Jacek Toporski; Mikael Sundin; Martin Höglund; Jonas Mattsson; Ibrahim El-Serafi; Moustapha Hassan
Journal:  Bone Marrow Transplant       Date:  2020-10-21       Impact factor: 5.483

Review 8.  Treosulfan Pharmacokinetics and its Variability in Pediatric and Adult Patients Undergoing Conditioning Prior to Hematopoietic Stem Cell Transplantation: Current State of the Art, In-Depth Analysis, and Perspectives.

Authors:  Michał Romański; Jacek Wachowiak; Franciszek K Główka
Journal:  Clin Pharmacokinet       Date:  2018-10       Impact factor: 6.447
  8 in total

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