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dc.contributor.author
Talevi, Alan
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dc.contributor.author
Bellera, Carolina Leticia
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dc.contributor.other
Talevi, Alan
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dc.date.available
2022-05-03T18:41:45Z
dc.date.issued
2021
dc.identifier.citation
Talevi, Alan; Bellera, Carolina Leticia; Drug Metabolism Functionalization (Phase I) Reactions; Springer Nature Switzerland AG; 2021; 1-7
dc.identifier.isbn
978-3-030-51519-5
dc.identifier.uri
http://hdl.handle.net/11336/156392
dc.description.abstract
Functionalization (or Phase I) reactions of drug metabolism are those that introduce a functional drug to their substrates (for instance, in hydroxylation) or modify an existing one (e.g., in hydrolysis). The term functionalization is sometimes preferred to Williams’ classic Phase I denomination. Williams’ nomenclature reflects the usual scheme of sequential metabolism, where the parent drug is converted to a primary, or first-generation, metabolite, which in turn is subjected to a second biotransformation reaction that yields a secondary, or second-generation, metabolite. Whereas it is true that functionalization reactions often “prepare” their substrate to undergo a conjugation (Phase II) reaction (because they provide the substrate with a chemical “anchor” site for a conjugation to occur, such as a -OH or a -NH function), there are many deviations from this too general scheme. For instance, many Phase I metabolites are excreted without experiencing Phase II reactions. Similarly, the intact drug may directly undergo a Phase II transformation without a previous Phase I reaction. A drug may undergo one or more subsequent Phase I reactions before being conjugated (see Fig. 1 for figures). Finally, drug metabolism tends to operate in parallel and not only serially, since many different biotransformations occur simultaneously to different drug molecules of the same compound.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Springer Nature Switzerland AG
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dc.rights
info:eu-repo/semantics/restrictedAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
DRUG METABOLISM
dc.subject
CLEARENCE
dc.subject
CYP450
dc.subject
CYPS
dc.subject.classification
Otras Ciencias Biológicas
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dc.subject.classification
Ciencias Biológicas
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dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
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dc.title
Drug Metabolism Functionalization (Phase I) Reactions
dc.type
info:eu-repo/semantics/publishedVersion
dc.type
info:eu-repo/semantics/bookPart
dc.type
info:ar-repo/semantics/parte de libro
dc.date.updated
2022-03-02T15:54:41Z
dc.journal.pagination
1-7
dc.journal.pais
Reino Unido
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dc.journal.ciudad
Basignstoke
dc.description.fil
Fil: Talevi, Alan. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina. Universidad Nacional de La Plata. Facultad de Ciencas Exactas. Laboratorio de Investigación y Desarrollo de Bioactivos; Argentina
dc.description.fil
Fil: Bellera, Carolina Leticia. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata; Argentina. Universidad Nacional de La Plata. Facultad de Ciencas Exactas. Laboratorio de Investigación y Desarrollo de Bioactivos; Argentina
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://link.springer.com/referenceworkentry/10.1007/978-3-030-51519-5_63-1
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1007/978-3-030-51519-5_63-1
dc.conicet.paginas
1500
dc.source.titulo
The ADME Encyclopedia
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