Basic & Clinical Pharmacology, 14e > Drug Biotransformation

 
Bertram G. Katzung+
 TABLE 4–3Phase II reactions.  
 
Type of Conjugation Endogenous Reactant Transferase (Location) Types of Substrates Examples

Nitrophenol, morphine,
UDP glucuronosyl-transferase Phenols, alcohols, carboxylic acids, acetaminophen, diazepam, N-
Glucuronidation UDP glucuronic acid (UDPGA)
(microsomes) hydroxylamines, sulfonamides hydroxydapsone, sulfathiazole,
meprobamate, digitoxin, digoxin

Sulfonamides, isoniazid, clonazepam,
Acetylation Acetyl-CoA N-Acetyltransferase (cytosol) Amines
dapsone, mescaline

GSH-S-transferase (cytosol, Epoxides, arene oxides, nitro groups, Acetaminophen, ethacrynic acid,

Glutathione conjugation Glutathione (GSH)
microsomes) hydroxylamines bromobenzene

Salicylic acid, benzoic acid, nicotinic
Acyl-CoA glycinetrans-ferase Acyl-CoA derivatives of carboxylic
Glycine conjugation Glycine acid, cinnamic acid, cholic acid,
(mitochondria) acids deoxycholic acid

Estrone, aniline, phenol, 3-
Phosphoadenosyl phosphosulfate
Sulfation Sulfotransferase (cytosol) Phenols, alcohols, aromatic amines hydroxycoumarin, acetaminophen,
(PAPS) methyldopa

Dopamine, epinephrine, pyridine,
Methylation S-Adenosylmethionine (SAM) Transmethylases (cytosol) Catecholamines, phenols, amines
histamine, thiouracil

Arene oxides, cis-disubstituted and Benzopyrene 7,8-epoxide, styrene
Water conjugation Water Epoxide hydrolase (microsomes)
monosubstituted oxiranes 1,2-oxide, carbamazepine epoxide

(cytosol) Alkene oxides, fatty acid epoxides Leukotriene A4

Date of download: 05/21/19 from AccessMedicine: accessmedicine.mhmedical.com, Copyright © McGraw-Hill Education. All rights reserved.