Sign In

Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be formed. Glucuronidation occurs at the luminal side of the endoplasmic reticulum. This process requires an activated endogenous cofactor, which transfers glucuronic acid to the substrate's reactive functional group. The enzyme responsible for facilitating this transfer is UDP-glucuronyl transferase. The resulting metabolites have high molecular weights and are typically excreted through bile. Sulfation, on the other hand, takes place within the cytosol of the cell. This reaction involves the formation of an active endogenous cofactor called phosphoadenosyl phosphosulfate (PAPS). PAPS transfers a sulfate group to the substrate's reactive site in the presence of the sulfotransferase enzyme.

Tags
Drug MetabolismPhase II ReactionsDetoxificationConjugationHydrophilic Drug ConjugatesSulfationGlucuronidationBiologically Inactive MetabolitesProdrugsUDP glucuronyl TransferaseBile ExcretionPhosphoadenosyl Phosphosulfate PAPSSulfotransferase Enzyme

From Chapter 3:

article

Now Playing

3.18 : Drug Metabolism: Phase II Reactions

Pharmacokinetics

3.1K Views

article

3.1 : Pharmacokinetics: Overview

Pharmacokinetics

3.1K Views

article

3.2 : Drug Absorption Mechanism: Passive Membrane Transport

Pharmacokinetics

2.8K Views

article

3.3 : Drug Absorption Mechanism: Carrier-Mediated Membrane Transport

Pharmacokinetics

2.9K Views

article

3.4 : Drug Absorption: Factors Affecting GI Absorption

Pharmacokinetics

3.2K Views

article

3.5 : Bioavailability: Overview

Pharmacokinetics

2.0K Views

article

3.6 : Factors Influencing Bioavailability: First-Pass Elimination

Pharmacokinetics

5.3K Views

article

3.7 : Bioequivalence: Overview

Pharmacokinetics

723 Views

article

3.8 : First Pass Effect

Pharmacokinetics

4.4K Views

article

3.9 : Time Course of Drug Effect

Pharmacokinetics

1.7K Views

article

3.10 : Drug Distribution: Tissue Binding

Pharmacokinetics

2.2K Views

article

3.11 : Physiological Barriers

Pharmacokinetics

3.0K Views

article

3.12 : Drug Distribution: Plasma Protein Binding

Pharmacokinetics

2.9K Views

article

3.13 : Compartment Models: Single-Compartment Model

Pharmacokinetics

1.8K Views

article

3.14 : Compartment Models: Two-Compartment Model

Pharmacokinetics

4.3K Views

See More

JoVE Logo

Privacy

Terms of Use

Policies

Research

Education

ABOUT JoVE

Copyright © 2025 MyJoVE Corporation. All rights reserved