Full Opioid Agonists and Tramadol: Pharmacological and Clinical Considerations

Abstract

: Opioids 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.

Supraclavicular vs. Infraclavicular Brachial Plexus Nerve Blocks: Clinical, Pharmacological, and Anatomical Considerations

“…There has been a remarkable resurgence of regional anesthesia, especially peripheral nerve blocks (PNB), with widespread implementation of these in enhanced recovery pathways after surgery and pain management (1,2). Although, opioids are the cornerstone analgesics for perioperative pain relief, regional anesthesia has ameliorated postoperative pain, decreased opioid consumptions, and their potential complications (3)(4)(5)(6)(7)(8). Furthermore, some peripheral nerve entrapments and surgical conditions can be successfully treated by peripheral nerve blocks (9)(10)(11)(12).…”

The Effect of Pneumoperitoneum-induced Hypertension During Laparoscopic Cholecystectomy Under General Anesthesia on Postoperative Pain: A Randomized Clinical Trial

“…Non-steroid anti-inflammatory drugs (NSAIDs) and opioids administration have been shown to be effective in controlling pain in perioperative period; however, there are some concerns about their side effects (13)(14)(15)(16)(17). Therefore, adjuvant drugs such as ketamine and dexmedetomidine can play a special role in this regard (18)(19)(20)(21).…”

Adding Dexmedetomidine to Bupivacaine in Ultrasound-guided Thoracic Paravertebral Block for Pain Management after Upper Abdominal Surgery: A Double-blind Randomized Controlled Trial

“…Various methods have been used for postoperative pain relief, such as oral and intravenous opioid and nonopioid analgesics, as well as peripheral nerve blocks and neuraxial analgesia (1)(2)(3)(4). Although opioids are the most common pain killers used to control pain after surgery, there is always concern about their risk, such as dependence and complications (5,6).…”