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Related Concept Videos

Pharmacogenetics of Drug Metabolism: Overview01:27

Pharmacogenetics of Drug Metabolism: Overview

Genetic polymorphism in drug metabolism is crucial to the inter-individual variability observed in drug responses. Drug metabolism primarily involves the chemical modification of drugs and other xenobiotics to enhance their elimination by increasing their polarity. Two main classes of enzymes mediate this biotransformation process: Phase I enzymes, primarily cytochrome P450s, catalyze oxidation and reduction reactions, while other enzymes, such as esterases, mediate hydrolysis, and Phase II...
Drug toxicity: Idiosyncratic Reactions01:16

Drug toxicity: Idiosyncratic Reactions

Idiosyncratic drug reactions represent abnormal chemical responses that vary significantly among individuals, ranging from extreme sensitivity to low doses to insensitivity to high doses. These reactions often occur due to the drug's covalent binding with serum proteins, forming a foreign hapten that triggers an immunotoxicological response. The variability in drug reactions has a strong pharmacogenetic foundation, with genetic differences crucial in how individuals metabolize drugs. For...
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Drug metabolism, a critical process in the liver, involves two primary phases: Phase I reactions and Phase II conjugation. Obesity introduces significant alterations in this metabolic process, primarily due to fatty infiltration of the liver, leading to conditions such as nonalcoholic fatty liver disease (NAFLD). This condition can modify the activities of both Phase I and II enzymes, impacting how drugs are metabolized in obese patients.Phase I metabolism sees variable effects across...
Drug Metabolism: Phase I Reactions01:17

Drug Metabolism: Phase I Reactions

A phase I reaction is a biochemical process that introduces a functionally reactive polar group to a substance. This transformation predominantly occurs in the liver, facilitated by the cytochrome P450 system of hemoproteins situated in the lipophilic endoplasmic reticulum of cells. The metabolite generated through this process can have varying polarities. If it is sufficiently polar, it can be easily excreted in the urine due to its water compatibility. However, if the metabolite is nonpolar,...
Drug Biotransformation: Overview01:28

Drug Biotransformation: Overview

Biotransformation, also known as drug metabolism, is a vital physiological process that chemically alters drugs, facilitating their elimination from the body and terminating their action. This process involves two main phases: phase I and phase II reactions. Phase I reactions, including oxidation, reduction, and hydrolysis, introduce or unmask polar functional groups on the drug molecule, thereby increasing its water solubility. By enhancing water solubility, the drug becomes more hydrophilic...
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Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...

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Identification and Quantification of Deranged Metabolites in Critically Ill Patients Using NMR-Based Metabolomics
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Metabolomics in drug intolerance.

Inmaculada Andreu1, Cristobalina Mayorga, Miguel A Miranda

  • 1Departamento de Química/Instituto de Tecnología Química UPV-CSIC, Universidad Politécnica de Valencia, Camino de Vera s/n, Valencia, Spain.

Current Drug Metabolism
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Adverse drug reactions, often caused by drug metabolites, pose significant health risks and hinder drug development. Understanding drug biotransformation is key to preventing these toxic effects.

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Area of Science:

  • Pharmacology
  • Toxicology
  • Immunology

Background:

  • Adverse drug reactions (ADRs) are a major cause of patient morbidity and mortality.
  • Idiosyncratic or hypersensitivity reactions can occur even at low drug doses.
  • The hapten hypothesis is the most accepted mechanism for immunological activation in ADRs.

Purpose of the Study:

  • To review the toxicological consequences of drug biotransformation.
  • To highlight the role of reactive metabolites in adverse drug reactions.
  • To provide examples of drugs associated with biotransformation-induced toxicity.

Main Methods:

  • Literature review of recent scientific publications (last decade).
  • Focus on drugs where bioactivation is a prerequisite for hypersensitivity.
  • Examination of toxicological consequences in liver and skin.

Main Results:

  • Drug metabolites can be more toxic and reactive than the parent drug.
  • Reactive metabolites bind to proteins, leading to hepatotoxicity (liver) and skin reactions.
  • Specific examples include nimesulide, paracetamol, and sulfamethoxazole, among others.

Conclusions:

  • Drug biotransformation is a critical factor in the development of adverse drug reactions.
  • Understanding metabolic pathways is essential for predicting and mitigating drug toxicity.
  • Further research into drug metabolism can improve drug safety and development.