Oxazaphosphorine metabolites

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August undefined, 2024

WebMay 6, 2010 · Importance of the field: The oxazaphosphorines (cyclophosphamide, ifosfamide and trofosfamide) are widely used in clinical practice for their antitumor and … WebOxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug …

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WebCyclophosphamide is an oxazaphosphorine that contributes alkyl groups to DNA, forming covalent linkages. It depletes T and B cells and suppresses antibody production. It is metabolized to 4-hydroxycyclophosphamide and its tautomer aldophosphamide by liver … Yanfeng Wang, Weiyang He, in The Liver, 2024. Introduction of mitochondria … WebJan 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 … thailande code insee

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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: … WebApr 1, 2012 · 2.1. Cytochrome P450. Prototypical oxazaphosphorine cytostatics such as CPA and IFO are chemically and pharmacologically inactive transport forms of alkylating nitrogen mustards that are biotransformed to their active forms predominantly in the liver 47; 48.As one of the key mechanisms of action, hepatic metabolism of CPA, has been … WebDec 20, 1999 · 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 … thaïlande circuits circuits en thaïlande

Oxazaphosphorines: new therapeutic strategies for an old …

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WebThe formation and rapid urinary excretion of conjugates of the activated (4-hydroxylated) oxazaphosphorine metabolites with mesna has been suggested as the pharmacological … WebImportance of the field: The oxazaphosphorines (cyclophosphamide, ifosfamide and trofosfamide) are widely used in clinical practice for their antitumor and … thailande code paysWebOxazaphosphorine metabolism and transport have a major impact on pharmacokinetic variability, pharmacokinetic-pharmacodynamic relationship, toxicity, resistance, and drug … sync hotstuff

"Webthe 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, " - Oxazaphosphorine metabolites

Oxazaphosphorine metabolites

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, ... WebOXAZAPHOSPHORINE METABOLISM BY THE HUMAN CYTOCHROME P450s AND SOME COMMONLY EXPRESSED P450 POLYMORPHIC VARIANTS by Diane M. Calinski A …

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http://www.bccancer.bc.ca/drug-database-site/Drug%20Index/Mesna_monograph_1Nov07.pdf 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 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 ...

WebMay 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 ... 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]

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.

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 … thailande cofaceWebThe 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 sync hp envy bluetoothWebApr 1, 2015 · 1. Name of the medicinal product 2. Qualitative and quantitative composition 3. Pharmaceutical form 4. Clinical particulars 5. Pharmacological properties 6. … thailande climatWebJul 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 ... synch photos to itunes libraryWebMafosfamide (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 synch productionWebThe metabolism of oxazaphosphorines is auto-inducible, with the activation of the orphan nuclear receptor pregnane X receptor (PXR) being the major mechanism. 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 ... sync hp printer to wifiWebThe 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. … synch pictures on phone to windows10 photos