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An analgesic drug, also called simply an analgesic, pain reliever, or painkiller, is any member of the group of drugs used for pain management. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects.
Pharmacology is the science of medical drugs and medications, including a substance's origin, composition, pharmacokinetics, therapeutic use, and toxicology. More specifically, it is the study of the interactions that occur between a living organism and chemicals that affect normal or abnormal biochemical function. If substances have medicinal properties, they are considered pharmaceuticals.
Opioids are a class of drugs that derive from, or mimic, natural substances found in the opium poppy plant. Opioids work in the brain to produce a variety of effects, including pain relief. As a class of substances, they act on opioid receptors to produce morphine-like effects.
Pethidine, also known as meperidine and sold under the brand name Demerol among others, is a fully synthetic opioid pain medication of the phenylpiperidine class. Synthesized in 1938 as a potential anticholinergic agent by the German chemist Otto Eisleb, its analgesic properties were first recognized by Otto Schaumann while working for IG Farben, in Germany. Pethidine is the prototype of a large family of analgesics including the pethidine 4-phenylpiperidines, the prodines, bemidones and others more distant, including diphenoxylate and analogues.
Buprenorphine, sold under the brand name Subutex among others, is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection, as a skin patch (transdermal), or as an implant. For opioid use disorder, the patient must have moderate opioid withdrawal symptoms before buprenorphine can be administered under direct observation of a health-care provider.
Medicinal plants, also called medicinal herbs, have been discovered and used in traditional medicine practices since prehistoric times. Plants synthesize hundreds of chemical compounds for various functions, including defense and protection against insects, fungi, diseases, and herbivorous mammals.
Midwestern University (MWU) is a private medical and professional school with campuses in Downers Grove, Illinois and Glendale, Arizona. As of the 2022–23 academic year, a total of 2,758 students were enrolled at the Downers Grove campus and 3,782 were enrolled at the Glendale campus.
Mitragyna speciosa is a tropical evergreen tree in the coffee family native to Southeast Asia. It is indigenous to Cambodia, Thailand, Indonesia, Malaysia, Myanmar, and Papua New Guinea, where it has been used in herbal medicine since at least the 19th century. It has also historically been used for chewing, smoking, and tea. Kratom has opiate properties and some stimulant-like effects.
Carfentanil or carfentanyl, sold under the brand name Wildnil, is an extremely potent opioid analgesic used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses. It is typically administered in this context by tranquilizer dart. Carfentanil has also been used in humans to image opioid receptors. It has additionally been used as a recreational drug, typically by injection, insufflation, or inhalation. Deaths have been reported in association with carfentanil.
Solomon Halbert Snyder is an American neuroscientist who has made wide-ranging contributions to neuropharmacology and neurochemistry. He studied at Georgetown University, and has conducted the majority of his research at the Johns Hopkins School of Medicine. Many advances in molecular neuroscience have stemmed from Snyder's identification of receptors for neurotransmitters and drugs, and elucidation of the actions of psychotropic agents. He received the Albert Lasker Award for Basic Medical Research in 1978 for his research on the opioid receptor, and is one of the most highly cited researchers in the biological and biomedical sciences, with the highest h-index in those fields for the years 1983–2002, and then from 2007 to 2019.
Dihydromorphine is a semi-synthetic opioid structurally related to and derived from morphine. The 7,8-double bond in morphine is reduced to a single bond to get dihydromorphine. Dihydromorphine is a moderately strong analgesic and is used clinically in the treatment of pain and also is an active metabolite of the analgesic opioid drug dihydrocodeine. Dihydromorphine occurs in trace quantities in assays of opium on occasion, as does dihydrocodeine, dihydrothebaine, tetrahydrothebaine, etc. The process for manufacturing dihydromorphine from morphine for pharmaceutical use was developed in Germany in the late 19th century, with the synthesis being published in 1900 and the drug introduced clinically as Paramorfan shortly thereafter. A high-yield synthesis from tetrahydrothebaine was later developed.
Phenoperidine, is an opioid analgesic which is structurally related to pethidine and is used clinically as a general anesthetic.
Desmetramadol, also known as O-desmethyltramadol (O-DSMT), is an opioid analgesic and the main active metabolite of tramadol. Tramadol is demethylated by the liver enzyme CYP2D6 to desmetramadol in the same way as codeine, and so similarly to the variation in effects seen with codeine, individuals who have a less active form of CYP2D6 will tend to have reduced analgesic effects from tramadol. Because desmetramadol itself does not need to be metabolized to induce an analgesic effect, it can be used in individuals with low CYP2D6 activity unlike tramadol.
Lt. Gen. (Ret.) Ronald Ray Blanck, D.O. was the 39th Surgeon General of the United States Army, from 1996 to 2000. He is a Doctor of Osteopathic Medicine (D.O.) and is the only such physician ever appointed Surgeon General of the Army. He was also president of the University of North Texas Health Science Center at Fort Worth from 2000 to 2006. He is the former Chairman of the Board of Regents of the Uniformed Services University of the Health Sciences.
Raymond L. Woosley is an American pharmacologist who is the founding president and chairman of the board for AZCERT, a not-for-profit organization dedicated to improved outcomes from the use of medications. Prior to leading AZCERT, he was founder and President of Critical Path Institute (C-Path). C-Path is an independent, non-profit organization created by the U.S. Food and Drug Administration (FDA) and the University of Arizona to help launch the critical path initiative. Previously, he has served as Vice-President for Health Sciences and Dean of the College of Medicine at the University of Arizona. He is Professor of Medicine and Biomedical Informatics in the University of Arizona College of Medicine - Phoenix, Arizona.
MT-45 (IC-6) is an opioid analgesic drug invented in the 1970s by Dainippon Pharmaceutical Co. It is chemically a 1-substituted-4-(1,2-diphenylethyl) piperazine derivative, which is structurally unrelated to most other opioid drugs. Racemic MT-45 has around 80% the potency of morphine, with almost all opioid activity residing in the (S) enantiomer. It has been used as a lead compound from which a large family of potent opioid drugs have been developed, including full agonists, partial agonists, and antagonists at the three main opioid receptor subtypes. Fluorinated derivatives of MT-45 such as 2F-MT-45 are significantly more potent as μ-opioid receptor agonists, and one of its main metabolites 1,2-diphenylethylpiperazine also blocks NMDA receptors.
U-47700, also known as U4, pink heroin, pinky, and pink, is an opioid analgesic drug developed by a team at Upjohn in the 1970s which has around 7.5 times the potency of morphine in animal models.
Furanylfentanyl (Fu-F) is an opioid analgesic that is an analog of fentanyl and has been sold as a designer drug. It has an ED50 value of 0.02 mg/kg in mice. This makes it approximately one fifth as potent as fentanyl.
Mitragynine is an indole-based alkaloid and the most abundant active alkaloid in the Southeast Asian plant Mitragyna speciosa, commonly known as kratom. The total alkaloid concentration in dried leaves ranges from 0.5 to 1.5%. In Thai varieties, mitragynine is the most abundant component while 7-hydroxymitragynine is a minor constituent. In Malaysian kratom varieties, mitragynine is present at lower concentration. Such preparations are orally consumed and typically involve dried kratom leaves which are brewed into tea or ground and placed into capsules. Mitragynine consumption for medicinal and recreation purposes dates back centuries, although early use was primarily limited to Southeast Asian countries such as Indonesia and Thailand where the plant grows indigenously. Recently, mitragynine use has spread throughout Europe and the Americas as both a recreational and medicinal drug. While research into the effects of kratom have begun to emerge, investigations on the active compound mitragynine are less common.
Frank LoVecchio is an American emergency medicine physician, medical toxicologist, academic and researcher. He is the medical director of Clinical Research at College of Health Solutions, the Director of Good Samaritan Regional Poison Center, the Research Director of Maricopa Medical Center Emergency Medicine Program, and clinical professor at Arizona College of Osteopathic Medicine. He also serves as an attending physician at Valleywise Health, Phoenix Children's Hospital, and in the Department of Medical Toxicology at Banner University Medical Center.
References
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- ↑ "Walter C. Prozialeck | Semantic Scholar". www.semanticscholar.org.
- 1 2 Scaccia, Annamarya (October 21, 2016). "Kratom: Deadly Drug or Herbal Cure for Opioid Epidemic?". Rolling Stone.
- ↑ "Obituary for Walter Prozialeck". Harris Funeral Home. May 22, 2017.
- ↑ "Distinguished Alumni". Juniata College.
- ↑ Prozialeck, Walter. "Mechanisms of Cadmium Toxicity in LLC-PK1 Cells" – via grantome.com.
{{cite journal}}: Cite journal requires|journal=(help) - ↑ Prozialeck, Walter C.; Edwards, Joshua R. (October 24, 2012). "Mechanisms of Cadmium-Induced Proximal Tubule Injury: New Insights with Implications for Biomonitoring and Therapeutic Interventions". The Journal of Pharmacology and Experimental Therapeutics. 343 (1): 2–12. doi:10.1124/jpet.110.166769. PMC 3464032 . PMID 22669569.
- ↑ Prozialeck, Walter C.; Jivan, Jateen K.; Andurkar, Shridhar V. (December 1, 2012). "Pharmacology of kratom: an emerging botanical agent with stimulant, analgesic and opioid-like effects". The Journal of the American Osteopathic Association. 112 (12): 792–799. ISSN 1945-1997. PMID 23212430.
- ↑ "Walter Prozialeck Archives". Narcotica.
- ↑ Gerald Gianutsos. "The DEA Changes Its Mind on Kratom". www.uspharmacist.com.
- ↑ "Ruggers Request Partying Personnel". Ariel. 8 (4). Thomas Jefferson University: 11. March 1, 1978.