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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 plant, known as Kratom in Thailand or Biak-Biak in Malaysia, has long been used locally as treatment for pain, fever reduction, diarrhea, and even depression.
Kratom and Other Mitragynines: The Chemistry and Pharmacology of Opioids from a Non-Opium Source presents an introduction to the chemical and biological properties of alkaloids isolated from M. speciosa as well as their synthetic analogs. The book covers various topics including phytochemistry, medicinal chemistry, and pharmacology. Current research, analgesic effects, and addiction potential are also discussed. As the first extensive text on the basic science and clinical use of Kratom, the book provides readers with a concise yet comprehensive introduction to nature’s "other opioid."
- Sales Rank: #1470910 in Books
- Published on: 2014-10-29
- Original language: English
- Number of items: 1
- Dimensions: 9.20" h x .80" w x 6.20" l, .0 pounds
- Binding: Hardcover
- 366 pages
Review
"This is a novel foray into the realm of reviews on non-poppy-derived opioids and their pharmacology and … provides very solid information about the chemistry of the mitragynines…The editor, Robert Raffa, is a widely known expert in the pharmacology of opioid drugs with significant knowledge and respect in the field."
―Kenneth E. McCarson, BChE, PhD, University of Kansas Medical Center for Doody's Review Service
"This book should be an indispensable single-volume information source for anyone working in the fields of opioid chemistry, pharmacology and toxicology. Some chapters would be of particular interest to … specialists working in addiction treatment and drug regulation. The book would also be an excellent addition to any library collection specialized in natural products or drugs of abuse."
―Journal of Addition Research and Therapy
About the Author
Robert B. Raffa is a professor of pharmacology in the Department of Pharmaceutical Sciences at Temple University School of Pharmacy as well as a research professor in the Department of Pharmacology at Temple University School of Medicine. He has bachelor’s degrees in chemical engineering and in physiological psychology, master’s degrees in biomedical engineering and toxicology, and a doctorate in pharmacology. Dr. Raffa was co-leader for analgesics discovery at Johnson & Johnson and was pivotal in the elucidation of the mechanism of action and development of the analgesic drug tramadol (Ultram™). He is the co-holder of several patents, including the combination of tramadol plus acetaminophen (Ultracet™). He has published more than 280 scientific articles in peer-reviewd journals and is the co-author or editor of several books.
Most helpful customer reviews
25 of 25 people found the following review helpful.
Excellent Book. Needs to be Affordable.
By juki654
I've just read Kratom and Other Mitragynines: The Chemistry and Pharmacology of Opioids from a Non-Opium Source, ed. by Robert B. Raffa. In the preface, Professor Raffa explains the book evolved from an elective course taught at Temple University School of Pharmacy, and is a collection of essays by experts in various fields (chemistry, biology, pharmaceutics, forensic toxicology, etc.).
First of all, this is a valuable book, and my only real criticism of it is that it is priced much too high. Perhaps the hardback needs to be so expensive, but why can’t the e-book be a reasonable price?
Also, I didn't have the background to understand all of the essays. I found myself looking up terms every couple of minutes while reading. Many of the essays are descriptions of the chemical and biological elements of kratom, and I pretty much skipped these, as they were very dense reading, and I was more concerned with the way kratom functioned as a drug.
Short Review:
Kratom has enough opioid properties that it should be classified as an opioid, albeit a new one. Kratom has significant pain-relieving properties. It also seems to suppress coughs, has some anti-depressive properties, and can produce euphoria at high doses. It does suppress breathing but less so than classic opioids. It also causes much less constipation. It seems to be less toxic than classic opioids, as there are no verified reports of it acting alone to cause deaths. There are anecdotal reports, and worry, that it can cause dependence and addiction. Most of the chapters call for more research to be done.
Notes from the Chapters I Read:
Chap 2
Makes the case that kratom can be classified as an opioid. Has two alkaloids—mitragynine (MG) and 7-hydroxymitragynine (7-OH-MG)—that show binding affinity for opioid receptors. Also shows pain relief, miosis (constriction of pupils), constipation, respiratory depression, and tolerance. Also, when an alkaloid is injected into mice, and then an opioid antagonist (blocks opioid action) is also injected, the mice show signs of opioid withdrawal.
A non-opioid property is that very high doses injected into rodents did not seem to poison them. No evidence of toxicity was found. In addition, the compounds in kratom “appear to produce less emesis (vomiting) and respiratory depression than does codeine, although much more detailed investigation is needed.”
The chapter concludes by asserting that “these alkaloids are a novel (or at least distinct) class of opioids. It appears that biodiversity has provided an alternative natural source of opioid compounds.”
Chapter 13
Points out that the pain-relieving effects of kratom cannot be explained by just the MG alkaloid, which is less potent than morphine. The 7-OH-MG alkaloid (small amount present in kratom) produces the strongest pain-relieving effect, maybe ten times stronger than morphine. The chapter urges more research into all of the alkaloids in kratom, concluding that “unknown ancient treasures are still hidden in the Thai traditional medicine M. speciosa, and we should hunt for them.”
Chapter 14
Compares the non-pain relieving aspects of kratom and other opioids
Both inhibit coughs. They were “equipotent.”
Both produce respiratory depression, but kratom’s effect is milder.
Euphoria: the authors note that kratom users report that a high dose of kratom is needed to produce euphoria and they speculate there is some compound in kratom that blocks euphoria at low doses.
Animals didn’t show as marked a preference for places where they received kratom, as they did for places where they got other opioids. Authors concluded the kratom extract used either did not have a sufficiently high concentration of active compounds, or that it contained some compound that blocked its effects.
They found some antidepressant activity in kratom.
Chapter 15
There is a discussion on opioid-induced constipation here. They found that morphine and the 7-OH-MG alkaloid in kratom slowed the travel of food through the large intestine to the same degree. However, since 7-OH-MG is ten times more potent than morphine for pain relief, you would need ten times less 7-OH-MG and therefore constipation would not be such a problem. When the MG alkaloid is compared to morphine and codeine as far as causing constipation, it was found that MG didn’t slow the food down nearly as much as morphine and codeine. So both of the pain-reducing elements in kratom cause less constipation than traditional opioids. The authors present this as a “possible clinical benefit, as opioids are commonly associated with constipation.”
Chapter 16
The authors quote fragments from postings by kratom users to a site called Erowid. Most of the quotes are from people trying to use kratom to detox from harsher opioids, or to feel euphoria, or to manage chronic pain. There was also some discussion of withdrawal symptoms. The authors also publish what they say is a “small number” of people who feel they may have caused themselves temporary liver or gall-bladder problems by using kratom.
Chapter 18
This is a long chapter detailing “adverse effects and toxicity” of opioids from the poppy plant—not kratom.
Chapter 19
This is on the “Toxicology of Mitragynine and Analogs.”
The chapter begins by pointing out that “To date, there have been no reports of fatal overdose of kratom per se. If there are such occurrences, they are probably the result of kratom products contaminated with synthetic adulterants.”
Most of the studies are with animals. One interesting thing found was that the Mitragynine content in the kratom extracts vary significantly by geographic origin. So the kratom in Thailand reported a higher mitragynine content than an extract from Malaysia.
The researchers tested the safety of MG by giving higher and higher doses to the rats. They concluded that it was only at the highest doses that any liver or kidney damage was found, and even then, “there were no significant effects of other biochemical parameters, such as cholesterol, triglycerides, total protein, creatinine, albumin, alkaline phosphates, or glucose levels.”
There don’t seem to have been any studies on humans but “despite informal and unsupervised widespread use of kratom, there are no reports of mortalities after ingestion of kratom alone, even after chronic and high-dosage consumption, but serious adverse reactions have been reported in several cases.” The cases referred to involve people who took adulterated kratom products, or mixed kratom with other substances. The chapter concludes by calling for more studies, so the “risk-benefit” equation for kratom can be more fully known.
One interesting point that came up in this chapter is that MG is a “poorly water-soluble drug . . . and has an acid-degradable nature.” That must be why it seems to dissolve in orange juice but not in water.
Chapter 20
This chapter is really looking ahead, to talk about what kinds of studies should be done. It recommends animal studies to see the abuse potential of the alkaloids in kratom. This chapter was very difficult to read, but I think it essentially said that pain-relieving properties have been established so now studies should focus on the dangers of the drug. It concludes that “many strides . . .have been made . . . regarding its potential therapeutic uses as an analgesic, anti-inflammatory agent, and muscle relaxant.” It also concludes that kratom can produce tolerance and physical dependence. It asks for studies “to assess the positive reinforcing and drug-seeking effects of mitragynine and drug discrimination assays to assess mechanistic similarities between mitragynine and prototypic drugs of abuse.”
Chapter 21
The author of this chapter, Professor Aziz Zoriah from the University of Malaya in Malayasia, gives the background of kratom. It was exclusive to Southeast Asia until around 1990, when the Internet made it easy to order. In Southeast Asia it is widely used, mostly as a stimulant to increase work production and treatment for opioid withdrawal symptoms. He cites a Malaysian study and a Thai study that both show a large percentage of the users reported they had trouble stopping. Professor Zoriah thinks this is because kratom is so easily available there, and so cheap, that users regularly take large doses. Along with all of the other researchers, he calls for more substantive research to be done on this drug.
Final Thoughts:
This is clearly a drug that needs to remain legal. It has many medical uses and has not caused one death yet—as opposed to alcohol, which new research shows causes an average of six deaths every day.
1 of 2 people found the following review helpful.
Fantastic.
By Casey Jones
The title says it all. I am working on a Ph.D. in a pharmacology-related field and wanted to write a research proposal on mitragynine. This book was an incredible investment for that purpose. It is somewhat specialized, although a determined average reader could reap plenty of benefit from it. Citations and references are thorough and extremely helpful. Great book, through and through.
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