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Pharmacology of Opioids
Published in Pamela E. Macintyre, Stephan A. Schug, Acute Pain Management, 2021
Pamela E. Macintyre, Stephan A. Schug
Opium contains more than 25 different alkaloids. Only two of these have any analgesic action—morphine and codeine. Thebaine, another alkaloid, is used in the manufacture of other opioids including oxycodone, oxymorphone, hydrocodone, hydromorphone, buprenorphine, naloxone, and naltrexone.
Disposition and Metabolism of Drugs of Dependence
Published in S.J. Mulé, Henry Brill, Chemical and Biological Aspects of Drug Dependence, 2019
Extensive research in the area of tolerance to and physical dependence482-486 on opiates and barbiturates has led to the general belief that physical dependence on these agents does not develop outside the cerebrospinal axis, and the matrix of the central nervous system is critically involved in the genesis of these two parameters. Dependence varied from drug to drug even within the same chemical class, and the development of tolerance was a frequent but not invariable accompaniment of physical dependence. Compounds closely related to morphine, e.g., thebaine, and others such as cocaine and amphetamine with predominantly stimulant properties, did not produce physical dependence. Narcotic antagonists as cyclazocine and nalorphine produced tolerance and physical dependence without drug-seeking behavior.175 Ethanol dependence was not a manifestation of dependence upon any endogenous opiate as proposed recently.487-489
Pain and psychiatry
Published in Ad (Sandy) Macleod, Ian Maddocks, The Psychiatry of Palliative Medicine, 2018
Ad (Sandy) Macleod, Ian Maddocks
A semi-synthetic opioid which targets the kappa as well as the mu receptors, oxycodone has been in clinical use since 1917. Derived from thebaine, it is twice as potent as morphine. Fewer hallucinations than with morphine have been reported.77 The rapid-acting oxycodone has proved very popular as a street drug of abuse. The combination of oxycodone with an oral opioid antagonist causes less constipation and it may also find a role in managing opioid addiction.
Current and emerging pharmacotherapies for opioid dependence treatments in adults: a comprehensive update
Published in Expert Opinion on Pharmacotherapy, 2022
Jonna M. Leyrer-Jackson, Amanda M. Acuña, M. Foster Olive
Opium is a naturally occurring substance derived from the opium poppy Papaver somniferum, and contains various bioactive opioid alkaloids, such as morphine, codeine, thebaine, papaverine, and others. Recorded history of use of opium for relief of pain and a variety of other medical ailments date back more than six millennia. In the latter half of the 19th century, chemical isolation of morphine from opium, the discovery of its conversion to diacetylmorphine (heroin) by boiling in acetic anhydride, and the invention of the hypodermic syringe, collectively led to widespread intravenous opioid use which revealed the high abuse dependence of these otherwise therapeutic compounds [1]. Over the next century, a multitude of synthetic and semisynthetic opioids were developed for use in the treatment of chronic pain, cough, and diarrhea, the most commonly prescribed being hydrocodone, hydromorphone, oxycodone, oxymorphone, fentanyl, tramadol, and meperidine.
Detection of opioids in umbilical cord lysates: an antibody-based rapid screening approach
Published in Toxicology Mechanisms and Methods, 2019
Stuart J. Knight, Alexander D. Smith, Tricia E. Wright, Abby C. Collier
Pure codeine spiked into UC lysate approximated the commercial-spiked curve closely, with an LLOQ of 5.7 ng/ml (Figure 1C). However, absolute quantitation of opioids in UC lysate is not possible because several analytes have cross reactivity in excess of 100% in the commercial ELISA. In particular 6-acetylmorphine and 6-acetyl-codeine cross reactivity is 636% and 442% respectively, with thebaine (uncommonly seen in the real world) at 151%. Additionally, several other metabolites are detected at less than 100% cross-reactivity, including morphine 3βD glucuronide (46%), morphine 6βD glucuronide (35%), hydrocodone (22%), hydromorphone (20%), dihydrocodeine (15%), norcodeine (0.8%) and normorphine (0.6%), according to the manufacturer’s product literature. If testing occurred shortly (minutes to hours) after ingestion, results would initially be several fold higher than true as 6-acetyl morphine is produced quickly, but after this, results would be under predictive of ingestion as the poorly detected glucuronides become more abundant. Despite this, relative levels of quantification can be detected as ‘high’ or ‘low’, an improvement on the ‘yes’ or ‘no’ previously reported (Montgomery et al. 2006; Wright et al. 2011).
Opioid exposure associated with poppy consumption reported to poison control centers and the U.S. Food and Drug Administration
Published in Clinical Toxicology, 2021
Eva Greenthal, Peter Lurie, Suzanne Doyon
The opium poppy, Papaver somniferum, naturally produces opiate alkaloids including morphine, codeine, and thebaine [1]. For this reason, Papaver somniferum cannot be legally cultivated in the United States. Its seeds may be imported as food or craft products, as they are not expected to contain opiate alkaloids, but the other parts of the plant (referred to as “poppy straw”) and its sap (referred to as poppy “latex”) are considered controlled substances under Schedule II of the Controlled Substances Act because of their opiate content [2]. Poppy seeds can only be cultivated in select countries, and Turkey, the Czech Republic, the Netherlands, China, and Slovakia were the top exporters in 2018 [3].