Iniciar sesión

Phase I biotransformation reactions are integral to drug metabolism, predominantly involving oxidative, reductive, and hydrolytic transformations. Chief among these are oxidative reactions, which enhance the hydrophilicity of xenobiotics and introduce polar functional groups to facilitate their elimination from the body.

Oxidation reactions are fundamental in aromatic carbon-containing systems. An example is the hydroxylation of phenobarbital, a process that transforms it into hydroxyphenobarbital. This reaction exemplifies how aromatic carbon atoms undergo oxidation, and other drugs like phenytoin undergo similar processes.

Aliphatic carbon-containing systems also undergo oxidation reactions; p-hydroxy phenytoin is a product of the hydroxylation of phenytoin. This exemplifies the oxidation of aliphatic carbon atoms, a process also witnessed in drugs such as hexobarbital.

Oxidation reactions also occur in benzylic and allylic carbon atoms and carbon atoms alpha to carbonyl and imines. An illustration of this is the conversion of codeine to morphine, which involves oxidation at the benzylic carbon atom. Other drugs, like diazepam, also undergo comparable reactions. However, it's important to underscore that oxidative reactions can sometimes produce reactive metabolites, potentially leading to the toxicological activation of drugs. A classic example is acetaminophen (paracetamol), whose conversion to reactive metabolites can instigate hepatic necrosis.

Oxidative reactions play a pivotal role in phase I metabolism. They act as a detoxifying mechanism, transforming lipophilic drugs into polar metabolites that the body can readily excrete. The complexity of these reactions underscores their importance in drug metabolism, highlighting the need for continued research and understanding in this field.

Tags

Phase I ReactionsBiotransformationDrug MetabolismOxidative ReactionsAliphatic Carbon SystemsAromatic Carbon SystemsHydroxylationXenobioticsReactive MetabolitesDetoxificationLipophilic DrugsPolar MetabolitesToxicological Activation

Del capítulo 5:

article

Now Playing

5.3 : Phase I Reactions: Oxidation of Aliphatic and Aromatic Carbon-Containing Systems

Pharmacokinetics: Drug Biotransformation

109 Vistas

article

5.1 : Drug Biotransformation: Overview

Pharmacokinetics: Drug Biotransformation

147 Vistas

article

5.2 : Phase I Oxidative Reactions: Overview

Pharmacokinetics: Drug Biotransformation

210 Vistas

article

5.4 : Phase I Reactions: Oxidation of Carbon-Heteroatom and Miscellaneous Systems

Pharmacokinetics: Drug Biotransformation

44 Vistas

article

5.5 : Phase I Reactions: Reductive Reactions

Pharmacokinetics: Drug Biotransformation

152 Vistas

article

5.6 : Phase I Reactions: Hydrolytic Reactions

Pharmacokinetics: Drug Biotransformation

45 Vistas

article

5.7 : Phase II Conjugation Reactions: Overview

Pharmacokinetics: Drug Biotransformation

108 Vistas

article

5.8 : Phase II Reactions: Glucuronidation

Pharmacokinetics: Drug Biotransformation

141 Vistas

article

5.9 : Phase II Reactions: Sulfation and Conjugation with α-Amino Acids

Pharmacokinetics: Drug Biotransformation

107 Vistas

article

5.10 : Phase II Reactions: Glutathione Conjugation and Mercapturic Acid Formation

Pharmacokinetics: Drug Biotransformation

86 Vistas

article

5.11 : Phase II Reactions: Acetylation Reactions

Pharmacokinetics: Drug Biotransformation

118 Vistas

article

5.12 : Phase II Reactions: Methylation Reactions

Pharmacokinetics: Drug Biotransformation

70 Vistas

article

5.13 : Phase II Reactions: Miscellaneous Conjugation Reactions

Pharmacokinetics: Drug Biotransformation

25 Vistas

article

5.14 : Factors Affecting Drug Biotransformation: Physicochemical and Chemical Properties of Drugs

Pharmacokinetics: Drug Biotransformation

109 Vistas

article

5.15 : Factors Affecting Drug Biotransformation: Biological

Pharmacokinetics: Drug Biotransformation

68 Vistas

JoVE Logo

Privacidad

Condiciones de uso

Políticas

Investigación

Educación

ACERCA DE JoVE

Copyright © 2025 MyJoVE Corporation. Todos los derechos reservados