Full Opioid Agonists and Tramadol: Pharmacological and Clinical Considerations

AuthorAmber N. Edinoffen
AuthorLeah A. Kaplanen
AuthorSami Khanen
AuthorMurray Petersenen
AuthorEmily Sauceen
AuthorChristopher D. Causeyen
AuthorElyse M. Cornetten
AuthorFarnad Imanien
AuthorOmid Moradi Moghadamen
AuthorAdam M. Kayeen
AuthorAlan D. Kayeen
OrcidAmber N. Edinoff [0000-0001-7436-6206]en
OrcidElyse M. Cornett [0000-0001-7961-3931]en
OrcidFarnad Imani [0000-0003-0814-0772]en
OrcidOmid Moradi Moghadam [0000-0003-4152-7397]en
OrcidAdam M. Kaye [0000-0002-7224-3322]en
OrcidAlan D. Kaye [0000-0003-2464-0187]en
Issued Date2021-08-31en
AbstractOpioids are mu receptor agonists and have been an important part of pain treatment for thousands of years. In order to use these drugs appropriately and successfully in patients, whether to control pain, to treat opiate-induced side effects, or opiate withdrawal syndromes, a solid understanding of the pharmacology of such drugs is crucial. The most recognized full agonist opioids are heroin, morphine, codeine, oxycodone, meperidine, and fentanyl. Phenanthrenes refer to a naturally occurring plant-based compound that includes three or more fused rings. The opioids derived from the opium plant are phenanthrene derivatives, whereas most synthetic opioids are simpler molecules that do not have multiple rings. Methadone acts as a synthetic opioid analgesic similar to morphine in both quality and quantity; however, methadone lasts longer and in oral form, has higher efficacy, and is considered a diphenylheptane. Fentanyl is a strong synthetic phenylpiperdine derivative that exhibits activity as a mu-selective opioid agonist approximately 50 to 100 times more potent than morphine. Meperidine is another medication which is a phenylpiperdine. Tramadol is considered a mixed-mechanism opioid drug, as it is a centrally acting analgesic that exerts its effects via binding mu receptors and blocking the reuptake of monoamines. Some of the most common adverse effects shared among all opioids are nausea, vomiting, pruritus, addiction, respiratory depression, constipation, sphincter of Oddi spasm, and miosis (except in the case of meperidine). Chronic opioid usage has also established a relationship to opioid-induced hypogonadism and adrenal suppression. Physicians must be stewards of opioid use and use opioids only when necessary.en
DOIhttps://doi.org/10.5812/aapm.119156en
KeywordOpioidsen
KeywordFull Agonistsen
KeywordTramadolen
KeywordMethadoneen
KeywordMeperidineen
KeywordFentanylen
PublisherBrieflandsen
TitleFull Opioid Agonists and Tramadol: Pharmacological and Clinical Considerationsen
TypeReview Articleen

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