Recent Advances in the Synthesis of Morphine and Related Alkaloids; by N. Chida * Opioids in Preclinical and Clinical Trials; by H. Nagase and H. Fujii * Synthesis of 14-Alkoxymorphinan Derivatives and Their Pharmacological Actions; by H. Schmidhammer and M. Spetea * 14-Amino-4,5-Epoxymorphinan Derivatives and Their Pharmacological Actions; by J. W. Lewis and S. M. Husbands * Nonpeptidic Delta (δ) Opioid Agonists and Antagonists of the Diarylmethylpiperazine Class: What Have We Learned?; by S. N. Calderon * Synthesis of Neoclerodane Diterpenes and Their Pharmacological Effects; by K. M. Lovell, K. M. Prevatt-Smith, A. Lozama and T. E. Prisinzano * Synthesis of Novel Basic Skeletons Derived from Naltrexone; by H. Nagase and H. Fujii * Twin and Triplet Drugs in Opioid Research; by H. Fujii * 3D-Pharmacophore Identification for κ-Opioid Agonists Using Ligand-Based Drug-Design Techniques; by N. Yamaotsu and S. Hirono
The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general.
Opioids such as morphine, codeine, and oxycodone are extracts or analogs isolated from a single source: the opium poppy. For a long time, it was believed to be nature's only source of opioids. But it now appears that biological diversity has evolved an alternative source of opioid compounds-those derived from the plant Mitragyna speciosa. This plan
This pocketbook summarizes the recent developments in this important and controversial aspect of pain management, looking at the benefits and adverse effects of opioids in non-cancer pain.
Drug overdose, driven largely by overdose related to the use of opioids, is now the leading cause of unintentional injury death in the United States. The ongoing opioid crisis lies at the intersection of two public health challenges: reducing the burden of suffering from pain and containing the rising toll of the harms that can arise from the use of opioid medications. Chronic pain and opioid use disorder both represent complex human conditions affecting millions of Americans and causing untold disability and loss of function. In the context of the growing opioid problem, the U.S. Food and Drug Administration (FDA) launched an Opioids Action Plan in early 2016. As part of this plan, the FDA asked the National Academies of Sciences, Engineering, and Medicine to convene a committee to update the state of the science on pain research, care, and education and to identify actions the FDA and others can take to respond to the opioid epidemic, with a particular focus on informing FDA's development of a formal method for incorporating individual and societal considerations into its risk-benefit framework for opioid approval and monitoring.
Synthesis of Essential Drugs describes methods of synthesis, activity and implementation of diversity of all drug types and classes. With over 2300 references, mainly patent, for the methods of synthesis for over 700 drugs, along with the most widespread synonyms for these drugs, this book fills the gap that exists in the literature of drug synthesis. It provides the kind of information that will be of interest to those who work, or plan to begin work, in the areas of biologically active compounds and the synthesis of medicinal drugs. This book presents the synthesis of various groups of drugs in an order similar to that traditionally presented in a pharmacology curriculum. This was done with a very specific goal in mind – to harmonize the chemical aspects with the pharmacology curriculum in a manner useful to chemists. Practically every chapter begins with an accepted brief definition and description of a particular group of drugs, proposes their classification, and briefly explains the present model of their action. This is followed by a detailed discussion of methods for their synthesis. Of the thousands of drugs existing on the pharmaceutical market, the book mainly covers generic drugs that are included in the WHO's Essential List of Drugs. For practically all of the 700+ drugs described in the book, references (around 2350) to the methods of their synthesis are given along with the most widespread synonyms. Synthesis of Essential Drugs is an excellent handbook for chemists, biochemists, medicinal chemists, pharmacists, pharmacologists, scientists, professionals, students, university libraries, researchers, medical doctors and students, and professionals working in medicinal chemistry. * Provides a brief description of methods of synthesis, activity and implementation of all drug types* Includes synonyms* Includes over 2300 references
Comprehensive and authoritative, Opioid Receptors and Antagonists: From Bench to Clinic offers neuroscientists, pharmacologists and interested clinicians a unique survey of the extensive and diverse research efforts currently employed with opioid antagonists to develop novel innovative drug therapies. Summarizes the present understanding of the chemistry, pharmacology and molecular biology of opioid receptors and their subtypes Highlights differences and similarities between the opioid pharmacology of animals and human Describes current and potential therapeutic areas for opioid antagonists, including substance abuse, alcohol and ingestive behaviors, behavioral disorders and other medical indications, supported by nonclinical and clinical evidence Focuses on the development of exciting and innovative drug delivery approaches that are being used with opioid antagonists for the above medical indications
This reference book covers all analgesics that are currently in use or in development. Pharmacological, therapeutical and mechanistical aspects are discussed along with valuable information on chemical properties and synthesis schemes. The latest information on novel drugs currently under development is provided.
A four-year investigation into the world of synthetic drugs—from black market factories to users & dealers to harm reduction activists—and what it revealed. A deeply human story, Fentanyl, Inc. is the first deep-dive investigation of a hazardous and illicit industry that has created a worldwide epidemic, ravaging communities and overwhelming and confounding government agencies that are challenged to combat it. “A whole new crop of chemicals is radically changing the recreational drug landscape,” writes Ben Westhoff. “These are known as Novel Psychoactive Substances (NPS) and they include replacements for known drugs like heroin, cocaine, ecstasy, and marijuana. They are synthetic, made in a laboratory, and are much more potent than traditional drugs” —and all-too-often tragically lethal. Drugs like fentanyl, K2, and Spice—and those with arcane acronyms like 25i-NBOMe—were all originally conceived in legitimate laboratories for proper scientific and medicinal purposes. Their formulas were then hijacked and manufactured by rogue chemists, largely in China, who change their molecular structures to stay ahead of the law, making the drugs’ effects impossible to predict. Westhoff has infiltrated this shadowy world. He tracks down the little-known scientists who invented these drugs and inadvertently killed thousands, as well as a mysterious drug baron who turned the law upside down in his home country of New Zealand. Westhoff visits the shady factories in China from which these drugs emanate, providing startling and original reporting on how China’s vast chemical industry operates, and how the Chinese government subsidizes it. Poignantly, he chronicles the lives of addicted users and dealers, families of victims, law enforcement officers, and underground drug awareness organizers in the United States and Europe. Together they represent the shocking and riveting full anatomy of a calamity we are just beginning to understand. From its depths, as Westhoff relates, are emerging new strategies that may provide essential long-term solutions to the drug crisis that has affected so many. “Timely and agonizing. . . . An impressive work of investigative journalism.” —USA Today “Westhoff explores the many-tentacled world of illicit opioids, from the streets of East St. Louis to Chinese pharmaceutical companies, from music festivals deep in the Michigan woods to sanctioned ‘shooting up rooms’ in Barcelona, in this frank, insightful, and occasionally searing exposé. . . . Westhoff’s well-reported and researched work will likely open eyes, slow knee-jerk responses, and start much needed conversations.” —Publishers Weekly “Our 25 Favorite Books of 2019” —St. Louis Post-Dispatch “Best Books of 2019” —Buzzfeed “Best Nonfiction of 2019” —Kirkus Reviews “50 Best Books of 2019” —Daily Telegraph “Best Nonfiction Books of 2019” —Tyler Cowen “Best Books of 2019” —Yahoo Finance
In recent years our understanding of molecular mechanisms of drug action and interindividual variability in drug response has grown enormously. Meanwhile, the practice of anesthesiology has expanded to the preoperative environment and numerous locations outside the OR. Anesthetic Pharmacology: Basic Principles and Clinical Practice, 2nd edition, is an outstanding therapeutic resource in anesthesia and critical care: Section 1 introduces the principles of drug action, Section 2 presents the molecular, cellular and integrated physiology of the target organ/functional system and Section 3 reviews the pharmacology and toxicology of anesthetic drugs. The new Section 4, Therapeutics of Clinical Practice, provides integrated and comparative pharmacology and the practical application of drugs in daily clinical practice. Edited by three highly acclaimed academic anesthetic pharmacologists, with contributions from an international team of experts, and illustrated in full colour, this is a sophisticated, user-friendly resource for all practitioners providing care in the perioperative period.
