Author Topic: Opioid Analgesics  (Read 2012 times)

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Opioid Analgesics
« on: December 10, 2001, 10:51:00 PM »
I must wholeheartedly reccommend the book "Opioid Analgesics - Chemistry and Receptors" by Alan F. Casy & Robert T. Parfitt for anyone interested in the chemistry of opiates and opioids. The book is 500 pages, full of references, synthetic routes to most known opiates/opioids along with SAR information and discussions on how and why they fit into the different opiate receptors. It is a veritable OIKAL (Opioids I Have Known...) - the only downside is the $200 pricetag from


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A new book on Analgesics
« Reply #1 on: November 26, 2003, 12:07:00 AM »
Analgesics. From Chemistry and Pharmacology to Clinical Application
Edited by H. Buschmann, T. Christoph, E. Friderichs, C. Maul, and B. Sundermann.
Wiley-VCH, Weinheim, Germany. 2002. ix + 604 pp. 18 × 25 cm. ISBN 3527304037. $185.00.
David S. Fries

10.1021/jm030187f S0022-2623(03)00187-0

This book is edited and written by scientists at Grenthal GmbH, Achen, Germany. Scientists at Grenthal discovered and brought to market the analgesic tramadol, and the company has retained a research focus on the discovery of new analgesics. No biographical information on the editors or the authors of the individual chapters is given other than their affiliation with Grenthal. The book attempts to give a thorough review of drugs in use, and current developments in the search for new drugs, for the clinical management of pain in humans.

The book is divided into four parts. Part 1, Introduction, consists of one chapter entitled "What Is Pain?". Part 2 is devoted to the broad topic of "Pain Therapy Today" and makes up nearly half of the book's content. Part 2 contains chapters on cyclooxygenase inhibitors, opioids (five subchapters), and NA and 5-HT reuptake inhibition, and 2 agonists. Part 3 is on "New Approaches to Pain Therapy" and consists of 12 chapters, covering nearly every potential mechanistic target that has been identified as being involved in the transmission, modulation, and perception of pain. Part 4 is a short chapter on the outlook for the discovery of new analgesics. The chapters are referenced and include citations through early 2002. The attention paid to the patent literature and to the status of agents currently undergoing clinical trials is especially complete and useful. The book contains a convenient glossary of terms and a subject index.

Medicinal chemists will find the writing approach taken by the authors much to their liking. Drugs and investigational new agents are presented in chapters related to their mechanism of action. Structures of important compounds are given, and for marketed drugs, the Chemical Abstracts identification numbers, chemical nomenclature, and some general physicochemical properties are included. General structure-activity relationships for a drug class are frequently included. Routes to the synthesis of many marketed agents are included; however, the inclusion of synthetic data varies markedly among the chapters. The metabolism of many of the drugs is included, but again, the coverage is inconsistent among the chapters.

The book is not without faults. Numerous errors exist in the structures and synthetic schemes presented in the book, and one should be cautious when using them. A second annoying error is the references to non-salt dosage forms of carboxylic acids as "free bases". The coverage of the important literature is sometimes incomplete. There are often inconsistencies in the organizational placement of material within and among the chapters. Overall, the book is highly informative and will be of value to teachers and students as well as to researchers in the area of analgesics and pain management. The approach to reviewing drug development of analgesic drugs is especially suited to the medicinal chemist. I recommend the book to individuals researching, teaching, or desiring to become informed about analgesic drugs and the status of drug development in this area. The book should be included in the holdings of all research libraries serving scientists and professionals dealing with the use and discovery of pharmaceutical agents.