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Opioid antagonists remain the standard treatment for respiratory depression following opioid overdose, with naloxone being by far the most commonly used, although the longer acting antagonist nalmefene may be used for treating overdoses of long-acting opioids such as methadone, and diprenorphine is used for reversing the effects of extremely ...
Carbonate derivatives of 14β-hydroxycodeine "viz., 14β-hydroxy-6-O-(methoxycarbonyl)codeine, 6-O-methoxycarbonyl-14β-(methoxycarbonyloxy)codeine, and 14β-acetoxy-6-O-methoxy-carbonylcodeine, potential substrates for ring C modification in morphinane (sic) alkaloids, were synthesized for the first time."
Opioids act upon opioid receptors that are coupled to inhibitor G protein coupled receptors (GPCR). These receptors fall into 3 classes: μ (mu), δ (delta), and κ (kappa) receptors. [36] More than 70% of opioid receptors are μ receptors, predominantly located on the central terminals of nociceptors in the dorsal horn of the spinal cord.
Morphine is highly addictive and prone to abuse. [12] If one's dose is reduced after long-term use, opioid withdrawal symptoms may occur. [12] Caution is advised for the use of morphine during pregnancy or breastfeeding, as it may affect the health of the baby. [12] [2] Morphine was first isolated in 1804 by German pharmacist Friedrich Sertürner.
The opioid epidemic, also referred to as the opioid crisis, is the rapid increase in the overuse, misuse/abuse, and overdose deaths attributed either in part or in whole to the class of drugs called opiates/opioids since the 1990s. It includes the significant medical, social, psychological, demographic and economic consequences of the medical ...
Opioid agonist therapy; Opioid excess theory; Opioid food peptides; Opioid overdose; Opioid rotation; Opioid withdrawal; Opioid-induced endocrinopathy; Opioid-induced hyperalgesia; Opioidergic; Opioids and pregnancy; Opium; Oxycodone; Oxymorphone-3-methoxynaltrexonazine
The structure-activity relationship of the drug class has been explored to a reasonable extent. The optimal substitution pattern is fairly tightly defined (i.e. N,N-diethyl on the amine nitrogen, 4-ethoxy on the benzyl ring and 5-nitro on the benzimidazole ring), but even derivatives incorporating only some of these features are still potent opioids.
Morphine, the archetypal opioid, and other opioids (e.g., codeine, oxycodone, hydrocodone, dihydromorphine, pethidine) all exert a similar influence on the cerebral opioid receptor system. Buprenorphine is a partial agonist of the μ-opioid receptor, and tramadol is a serotonin norepinephrine reuptake inhibitor (SNRI) with weak μ-opioid ...