Oxazaphosphorine metabolites
WebThe initial metabolism of the oxazaphosphorine cytostatic ifosfamide (IF) consists of two different pathways: ring oxidation at carbon-4 forms the cytostatically active metabolite 4-hydroxyifosfamide (4-OH-IF, “activated ifosfamide”), whereas side-chain oxidation with liberation of the presumably neurotoxic compound chloroacetaldehyde (CAA) that may … WebSep 28, 2024 · In vitro, toxic acrolein is formed during the formation of the cytotoxic metabolite phosphoreamidemustard (PAM), whereas in vivo proapoptotic hydroxypropanal (HPA) is formed. The CP metabolites formed in sequence 4-hydroxycyclophosphamide (OHCP) are the main cause of toxicity, aldophosphamide (ALDO) is the pharmacologically …
Oxazaphosphorine metabolites
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WebNov 25, 2001 · The metabolism of oxazaphosphorines can be divided into three stages: activation, toxification, and deactivation. The initial activation is based on hydroxylation of the ring at C-4 by mixed function oxidases in the liver (cytochrome P-450) to give 4-hydroxyoxazaphosphorines. WebThe formation and rapid urinary excretion of conjugates of the activated (4-hydroxylated) oxazaphosphorine metabolites with mesna has been suggested as the pharmacological …
WebThe active metabolites of cyclophosphamide are highly protein bound and distributed to all tissues, are assumed to cross the placenta and are known to be present in breast milk. … WebOXAZAPHOSPHORINE METABOLISM BY THE HUMAN CYTOCHROME P450s AND SOME COMMONLY EXPRESSED P450 POLYMORPHIC VARIANTS by Diane M. Calinski A dissertation submitted in partial fulfillment of the requirements for the degree of Doctor of Philosophy (Pharmacology) in the University of Michigan 2013 Doctoral Committee: …
WebJan 1, 1989 · Abstract. The development of the oxazaphosphorine cytostatics cyclophosphamide, ifosfamide, and trofosfamide was based on the idea of applying the transport form/active form principle to the highly reactive nitrogen mustard group. A critical analysis and synopsis of the available results and knowledge will include examination of … WebMesna is a synthetic compound that protects the bladder from the urotoxic metabolites of oxazaphosphorine derivatives (e.g., ifosfamide, cyclophosphamide) by chemically interacting with them and their metabolites as a ... by 48% of the oxazaphosphorine dose PO at hour 3 and 7 Intravenous: N/A2,3,10 20% of the oxazaphosphorine dose at hour 0, 4, ...
http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Mesna_monograph_1Nov07.pdf
WebThe active metabolites of cyclophosphamide are highly protein bound and distributed to all tissues, are assumed to cross the placenta and are known to be present in breast milk. [40] It is specifically in the oxazaphosphorine group of medications. [41] hallway stairs ideasWebThat the oxazaphosphorines continue to be the subject of intensive investigation over 30 years after their introduction into clinical practice is partly because of their antitumour activity. The 2 most commonly used oxazaphosphorines are cyclophosphamide and ifosfamide, although other bifunctional mustard analogues continue to be investigated. … buried on the fens joy ellisWebThe P450 metabolites of CPA and IFA, CA (formed by the N-dechloroethylation pathway) and acrolein (formed by the 4-hydroxylation pathway), were determined in parallel using a single incubation tube [27]. Incubations were carried out for 30 min in a total volume of 100 mL, and included 50 mM potassium phosphate buffer, pH 7.4, 0.1 buried on the fens kindleWebMay 1, 2002 · CAA, a byproduct of oxazaphosphorine metabolism, displayed appreciable cytotoxic activity in cell culture (EC 50 ϳ 2.5 M, compared with EC 50 values of 3-5 M for the 4-hydroxy derivatives of CPA ... hallway standWebJul 1, 2005 · Oxazaphosphorine metabolism is affected by a number of factors associated with the drugs (e.g., dosage, route of administration, chirality, and drug combination) and patients (e.g., age, gender ... hallway stands furnitureWebMay 6, 2010 · Importance of the field: The oxazaphosphorines (cyclophosphamide, ifosfamide and trofosfamide) are widely used in clinical practice for their antitumor and … buried on the fens kindle unlimitedWebThe formation and rapid urinary excretion of conjugates of the activated (4-hydroxylated) oxazaphosphorine metabolites with mesna has been suggested as the pharmacological basis for the selective detoxification, but separation and identification of such metabolites in vivo have been extremely difficult due to their high polarity and chemical ... hallway standard size in meters