Download Drug Metabolism: Current Concepts by Mino R. Caira, Corina Ionescu PDF

By Mino R. Caira, Corina Ionescu

Drug Metabolism: present Concepts

Corina Ionescu and Mino R Caira

Drug Metabolism: present ideas presents a entire figuring out of the techniques that ensue following ingestion of a medicinal agent or xenobiotic, with an emphasis at the the most important function of metabolism (biotransformation). How a legitimate wisdom of those phenomena is included into the layout of powerful new drug applicants can be defined. The simple textual content makes a speciality of suggestions instead of extraneous info and is supported by means of many illustrated examples of biotransformations in addition to widespread references to present severe experiences and articles highlighting the character of analysis goals during this vivid zone of medicinal improvement. the ultimate subject on concepts for drug layout depends on the heritage supplied by means of the remainder of the book.

The e-book comprises chapters on

ADME (drug absorption, distribution, metabolism and removal)

Pathways of biotransformation (Phase I and section II metabolic reactions)

Enzymatic platforms thinking about biotransformation

Induction and inhibition of drug-metabolising enzymes

Factors that effect drug biotransformation

The function of pharmacogenetics

Drug-drug interactions and opposed reactions

Strategies for drug layout.

This publication is best as a complicated textual content for classes in drug metabolism for college kids of medication, pharmacy, pharmacology, biochemistry; and for classes in drug layout and drug supply for college students of medicinal chemistry. it's also applicable for pro seminars or classes that relate to the destiny of a drug within the physique, drug interactions, adversarial reactions and drug design.

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Additional resources for Drug Metabolism: Current Concepts

Example text

9]. There is a third class of metabolites, recognized as xenobioticmacromolecule adducts (also called macromolecular conjugates), formed when a xenobiotic binds covalently to a biological macromolecule [9]. As a very recent example of sequential metabolism, we mention that of 2,3,7-trichlorodibenzo-p-dioxin (2,3,7-triCDD) by cytochrome P450 and UDP-glucuronosyltransferase in human liver microsomes [10]. This study investigated the glucuronidation of 2,3,7-triCDD by rat CYP1A1 and human UGT. The ability of ten human liver microsomes to metabolise this polychlorinated compound was assessed.

Pharmacokinetic modelling attempts to quantify not only this distribution phase but also simultaneous clearance of the drug (by metabolism and excretion). Depending on the drug and the level of accuracy required, models of different degrees of sophistication are employed to formulate mathematical equations describing these processes. 2 Kinetic aspects For the purposes of modelling drug distribution, it is convenient to consider the body as being divided into discrete ‘compartments’, separated by boundaries.

2000. Absorption, distribution, metabolism and excretion of intravenously and dermally administered triethanolamine in mice. Food Chem Toxicol 38:1043-1051. 1 INTRODUCTION Drug metabolism is a complex and important part of biochemical pharmacology. The pharmacological activity of many drugs is reduced or nullified by enzymatic processes, and drug metabolism is one of the main mechanisms by which drugs may be inactivated. Metabolism, or the biotransformation of a drug, is the process whereby living organisms effect chemical changes to a molecule [1-8].

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