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Chapter 5

Pharmacokinetics: Drug Biotransformation

药物生物转化:概述
药物生物转化:概述
Drug biotransformation or metabolism entails chemical alteration of xenobiotics, either activating or deactivating their pharmacological properties. ...
I 期氧化反应:概述
I 期氧化反应:概述
Phase I biotransformation or functionalization entails the chemical transformation of drugs into metabolites via oxidative, reductive, and or hydrolytic ...
第一阶段反应:脂肪族和芳香族含碳体系的氧化
第一阶段反应:脂肪族和芳香族含碳体系的氧化
Phase I biotransformation primarily involves microsomal enzymes that catalyze oxidative reactions, using molecular oxygen and NADPH. Notably, only one ...
第一阶段反应:碳杂原子和其他体系的氧化
第一阶段反应:碳杂原子和其他体系的氧化
Carbon-nitrogen systems, encompassing aliphatic and alicyclic amines, undergo oxidative reactions. Secondary and tertiary amines primarily undergo ...
I 期反应:还原反应
I 期反应:还原反应
Reductive reactions introduce electrons to drug molecules, affecting polar functional groups like hydroxy and amino, allowing subsequent biotransformation ...
I 期反应:水解反应
I 期反应:水解反应
Hydrolysis is a chemical process where a compound is decomposed by reacting with water without altering its oxidation state. This process plays a vital ...
II 期偶联反应:概述
II 期偶联反应:概述
Conjugation involves the covalent linkage of a conjugating reagent to drugs or their metabolites in the presence of a transferase enzyme. These reagents ...
II 期反应:葡萄糖醛酸化
II 期反应:葡萄糖醛酸化
Glucuronidation, a key phase II biotransformation reaction, involves the conjugation of glucuronic acid to xenobiotics or metabolites. This process is ...
II 期反应:硫酸化和与 α-氨基酸偶联
II 期反应:硫酸化和与 α-氨基酸偶联
Sulfation, a phase II biotransformation reaction, involves the addition of a polar sulfate group to a drug. The process is catalyzed by nonmicrosomal ...
II 期反应:谷胱甘肽偶联和巯基酸形成
II 期反应:谷胱甘肽偶联和巯基酸形成
Glutathione is a tripeptide consisting of three amino acids – glutamic acid, cysteine, and glycine. It plays a pivotal role in detoxification via ...
II 期反应:乙酰化反应
II 期反应:乙酰化反应
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 ...
II 期反应:甲基化反应
II 期反应:甲基化反应
Phase II methylation reactions involve the attachment of a methyl group to a substrate. This reaction is the reverse of the phase I demethylation. ...
II 期反应:其他偶联反应
II 期反应:其他偶联反应
Phase II biotransformations primarily involve detoxification processes where xenobiotics conjugate with endogenous substances. The cyanide ion's ...
影响药物生物转化的因素:药物的物理化学和化学性质
影响药物生物转化的因素:药物的物理化学和化学性质
Drug metabolism can be influenced by a drug's physicochemical properties, like molecular size and shape, which dictate the drug's interaction with ...
影响药物生物转化的因素:生物
影响药物生物转化的因素:生物
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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