Oxazaphosphorine metabolites
WebIn order to reduce the oxazophosphorine-related urothelial toxicity, sodium mercaptoethane sulphonate (mesna) is used in different schedules following the administration of ifosfamide. The proposed mechanism of mesna activity is the binding of toxic oxazaphosphorine metabolites such as acrolein in the urine of the patients. WebMay 1, 2004 · Cyclophosphamide (CPA) and ifosfamide (IFA) are oxazaphosphorine anticancer prodrugs metabolized by two alternative cytochrome P450 (P450) pathways, drug activation by 4-hydroxylation and drug inactivation by N -dechloroethylation, which generates the neurotoxic and nephrotoxic byproduct chloroacetaldehyde.
Oxazaphosphorine metabolites
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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] 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 …
WebOxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug … WebMafosfamide (4-thioethane sulfonic acid salt of 4-hydroxy-cyclophosphamide, MAF) belongs to a new generation of the oxazaphosphorine agents. MAF is a cyclophosphamide analog which spontaneously degrades to 4-hydroxy-cyclophosphamide. The effects of
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 … WebMar 1, 2024 · On the basis of the discovery that the proapoptotic aldehyde 3-hydroxypropanal is a cyclophosphamide metabolite, a novel mechanism of action of oxazaphosphorine cytostatics is presented and ...
WebOxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug …
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. … pedigree dog food official siteWebJan 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 … meaning of tit for tat in hindiWebOXAZAPHOSPHORINE METABOLISM BY THE HUMAN CYTOCHROME P450s AND SOME COMMONLY EXPRESSED P450 POLYMORPHIC VARIANTS by Diane M. Calinski A … pedigree dog food nutritionWebwhich is caused by oxazaphosphorine metabolites such as 4-hydroxy-cyclophosphamide, 4-hydroxy-ifosfamide or acrolein, is sometimes the dose-limiting toxicity of these cytostatics (Brock et al. 1979, 1981). Mesna (sodium 2-mercaptoethane sulfonate, Fig. 1), which shows low toxicity, very limited tissue transfer and pedigree dog food petcoWebThe concentrations of the parent oxazaphosphorine and its principal metabolites were measured simultaneously in the plasma and CSF of 25 children. Twenty-one patients received CP for the treatment of either acute lymphoblastic leukemia, non-Hodgkin's lymphoma, or medulloblastoma, and 4 children received IF for the treatment of … pedigree dog food offersWebthe oxazaphosphorine metabolites. After oral or intravenous administration, mesna undergoes rapid oxidation in the plasma to dimesna. Only a small portion of the dose remains in the circulation as the physiologically active compound. Both mesna and dimesna are very hydrophilic and therefore remain in the intravascular compartment, meaning of tissue in biologyWebJan 1, 2005 · Oxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug interactions since the drug-metabolizing enzymes and drug transporters involved are key determinants of the pharmacokinetics and … meaning of tit for tat