Levorphanol, termed “the forgotten opioid,” is a potent opioid analgesic available for the treatment of moderate to severe pain. It was first approved in 1953, and it has a wide range of ascending and descending pain pathway receptor-mediated pharmacological activities, including mu, delta, and kappa (kappa 1 and 3) opioid agonism; N-methyl-D-aspartate (NMDA) antagonism; and reuptake inhibition...

Identification of adaptations to chronic morphine that are causally associated with opioid tolerance formation has long been intensely pursued by the opioid research community. There is an impressive array of components of signaling pathways that are influenced by chronic opioid administration. This underscores the importance to tolerance mechanisms of the complex interplay of cellular adaptati...

People are living to older age. Demographic pressures are driving change. Opiate analgesics are the most powerful known pain relievers. Persistent pain, both cancer and non-cancer types is frequent in older adults. The use of opioid analgesics is appropriate in the treatment of moderate to severe persistent pain. The challenge of prescribing opioids in older adults is to understand the factors ...

Low molecular weight opioid peptide esters (OPE) could become a class of analgesics with different side effect profiles than current opiates. OPE may have sufficient plasma stability to cross the blood brain barrier (BBB), undergo ester hydrolysis and produce analgesia. OPE of dipeptides, tyr-pro and tyr-gly conjugated to ethanol have a structure similar to the anesthestic agent, etomidate. Bas...

Acute and chronic pain management in children is increasingly characterized by either a multimodal or a preventive analgesia approach, in which smaller doses of opioid and nonopioid analgesics, such as nonsteroidal anti-inflammatory drugs, local anaesthetics, N-methyl-D-aspartate antagonists, alpha(2)-adrenergic agonists, and voltage-gated calcium channel alpha-2 delta-proteins, are combined al...

Background In patients with serious illness or trauma, reduction of severe pain is a key therapeutic goal of emergency medical service (EMS) teams. In Germany, only physicians are allowed to use opioid analgesics. In the rural EMS area studied, the mean arrival time for paramedics is 8 minutes, 23 seconds, and for the rescue physician between 10 minutes, 30 seconds and 16 minutes, 59 seconds, d...

Morphine and structurally related derivatives are highly effective analgesics, and the mainstay in the medical management of moderate to severe pain. Pharmacological actions of opioid analgesics are primarily mediated through agonism at the µ opioid peptide (MOP) receptor, a G protein-coupled receptor. Position 17 in morphine has been one of the most manipulated sites on the scaffold and intens...

PURPOSE To compare the postoperative analgesic effects of lidocaine, morphine and lidocaine plus morphine administered by constant rate infusion (CRI) and analyzing their effects on opioid requirements after orthopedic surgery in dogs. METHODS Twenty-four dogs underwent fracture repairs were premedicated with IM acepromazine (0.05 mg/kg) combined with morphine (0.3mg/kg). Anesthesia was induc...

PURPOSE Low-dose naltrexone (LDN) is used in a wide range of conditions, including chronic pain and fibromyalgia. Because of the opioid antagonism of naltrexone, LDN users are probably often warned against concomitant use with opioids. In this study, based on data from the Norwegian prescription database, we examine changes in opioid consumption after starting LDN therapy. METHODS We included...

Objective Opioid abuse is a serious public health concern. In response, the Food and Drug Administration (FDA) determined that a risk evaluation and mitigation strategy (REMS) for extended-release and long-acting (ER/LA) opioids was necessary to ensure that the benefits of these analgesics continue to outweigh the risks. Key components of the REMS are training for prescribers through accredited...