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Chapter 5
Drug biotransformation or metabolism entails chemical alteration of xenobiotics, either activating or deactivating their pharmacological properties. ...
Phase I biotransformation or functionalization entails the chemical transformation of drugs into metabolites via oxidative, reductive, and or hydrolytic ...
Phase I biotransformation primarily involves microsomal enzymes that catalyze oxidative reactions, using molecular oxygen and NADPH. Notably, only one ...
Carbon-nitrogen systems, encompassing aliphatic and alicyclic amines, undergo oxidative reactions. Secondary and tertiary amines primarily undergo ...
Reductive reactions introduce electrons to drug molecules, affecting polar functional groups like hydroxy and amino, allowing subsequent biotransformation ...
Hydrolysis is a chemical process where a compound is decomposed by reacting with water without altering its oxidation state. This process plays a vital ...
Conjugation involves the covalent linkage of a conjugating reagent to drugs or their metabolites in the presence of a transferase enzyme. These reagents ...
Glucuronidation, a key phase II biotransformation reaction, involves the conjugation of glucuronic acid to xenobiotics or metabolites. This process is ...
Sulfation, a phase II biotransformation reaction, involves the addition of a polar sulfate group to a drug. The process is catalyzed by nonmicrosomal ...
Glutathione is a tripeptide consisting of three amino acids – glutamic acid, cysteine, and glycine. It plays a pivotal role in detoxification via ...
Acetylation is a crucial phase II biotransformation process involving the addition of an acetyl group to a substrate. It is similar to α-amino acid ...
Phase II methylation reactions involve the attachment of a methyl group to a substrate. This reaction is the reverse of the phase I demethylation. ...
Phase II biotransformations primarily involve detoxification processes where xenobiotics conjugate with endogenous substances. The cyanide ion's ...
Drug metabolism can be influenced by a drug's physicochemical properties, like molecular size and shape, which dictate the drug's interaction with ...
Drug metabolism varies among species due to distinct enzyme systems and metabolic pathways. Even within the same species, diverse strains can exhibit ...
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