Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?

All drugs have both favorable therapeutic and untoward adverse effects. Conventional opioid analgesics possess both analgesia and adverse reactions, such as nausea, vomiting, and respiratory depression. The opioid ligand binds to µ opioid receptor and non-selectively activates two intracellular signaling pathways: the G protein pathway induce analgesia, while the β-arrestin pathway is responsible for the opioid-related adverse reactions. An ideal opioid should activate the G protein pathway while deactivating the β-arrestin pathway. Oliceridine (TRV130) has a novel characteristic mechanism on the action of the µ receptor G protein pathway selective (µ-GPS) modulation. Even though adverse reactions (ADRs) are significantly attenuated, while the analgesic effect is augmented, the some residual ADRs persist. Consequently, a G protein biased µ opioid ligand, oliceridine, improves the therapeutic index owing to increased analgesia with decreased adverse events. This review article provides a brief history, mechanism of action, pharmacokinetics, pharmacodynamics, and ADRs of oliceridine.

Opioid-induced hyperalgesia: a review of epidemiology, mechanisms and management

There has been a growing interest in opioid-induced hyperalgesia (OIH), which is an increased sensitivity to pain caused by opioid exposure. Multiple underlying pathways may contribute to the development of OIH, and the mechanism may vary with the duration of opioid exposure, dose, type and route of administration. In addition, the distinction between OIH, tolerance and withdrawal should be made in both the basic and clinical science literature so as to help translate findings to the clinical phenomenon and to help determine the best strategies to prevent or treat OIH.

Spinal cord stimulation for chronic pain

Spinal cord stimulation (SCS) is one of the most effective modalities for management of refractory neuropathic pain unresponsive to conservative therapies. The SCS has been successful in providing analgesia, improving function, and enhancing quality of life for patients suffering from chronic pain conditions such as failed back surgery syndrome, complex regional pain syndrome, ischaemic and phantom limb pain, and coronary artery disease. This technique has proven to be cost effective in the long term despite its high initial cost. In this review article, we discuss the history of SCS development, mechanism of action, and indications for SCS.

Permanent Peripheral Nerve Stimulation for Chronic Occipital Neuralgia: Case reports / 대한통증학회지

This report presents the application of occipital nerve stimulation in two patients with severe and disabling bilateral occipital neuralgia. Pain persisted despite the use of several procedures and the administration of medication in the patients. The patients underwent peripheral nerve stimulation for the treatment of headache. Peripheral nerve stimulation was accomplished via implantation of a subcutaneous electrode to stimulate the peripheral nerve in the occipital area. The patients reported a 90% improvement in overall pain. These cases illustrate the possible utilization of peripheral nerve stimulation for the treatment of occipital neuralgia.