Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists

A Gillis, AB Gondin, A Kliewer, J Sanchez, HD Lim… - Science …, 2020 - science.org
Agonists of the μ-opioid receptor (MOR), such as morphine and the synthetic opioid fentanyl…
Unfortunately, MOR agonists also elicit several on-target adverse effects that severely limit …

Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: a randomized, double-blind …

DG Soergel, RA Subach, N Burnham, MW Lark… - Pain, 2014 - journals.lww.com
… To determine whether differential activation of μ-opioid pathways dissociates analgesia from
adverse effects, we discovered TRV130, a “G protein-biased” μ-opioid ligand with G protein…

[PDF][PDF] Opioid pharmacology

R Centers, NC Conover - Pain Physician, 2008 - academia.edu
… by intolerable dose-related adverse effects. In contrast, opioid agonists/antagonists and
opioid partial agonists (buprenorphine, … Opioid Agonists Most of the most common opioids are …

[PDF][PDF] Dissecting the relative contribution of central versus peripheral opioid analgesia: Are the analgesic and adverse effects of opioids inseparable?

M Ringkamp, SN Raja - European Journal of Pain, 2012 - academia.edu
… may be a useful strategy to boost the analgesic effects of peripheral opioid effects and separate
the beneficial effects of opioids from their adverse CNS effects, this approach may not be …

Are peripheral opioid antagonists the solution to opioid side effects?

JJ Bates, JF Foss, DB Murphy - Anesthesia & Analgesia, 2004 - journals.lww.com
… administration, opioid agonists will produce both acute and chronic effects. Opioids alter the
… The only serious adverse effects of MNTX and alvimopan observed have been abdominal …

Side effects of opioid analgesics and narcotic antagonists

MS D'Souza, H Pham, SD Ray - Side Effects of Drugs Annual, 2022 - Elsevier
… from opioid dependence. This chapter will describe some of the adverse effects associated
with opioid agonist analgesics and narcotic antagonists. These adverse effects were reported …

Management of mood and anxiety disorders in patients receiving opioid agonist therapy: Review and meta‐analysis

AN Hassan, AS Howe, AV Samokhvalov… - … American Journal on …, 2017 - Wiley Online Library
… As expected, our review showed that studies that used TCAs had considerably high reported
adverse effects than those that used SSRIs as a pharmacotherapy. Adverse effects and …

[PDF][PDF] Combination opioid analgesics

HS Smith - Pain physician, 2008 - painphysicianjournal.com
… minimize adverse effects; 4.) combinations to diminish opioid effectsopioid effects); 5.)
combinations to reduce opioid tolerance/… Opioid agonists are initially inhibitory, but may become …

[PDF][PDF] Adverse Effects of Opioid Therapy

KE KHOR - healthxchange.sg
… This chapter will discuss general opioid adverse effects and classify them based on body
systems, the mechanism of their generation and general management strategies. …

A bifunctional-biased mu-opioid agonist–neuropeptide FF receptor antagonist as analgesic with improved acute and chronic side effects

AD La Rochelle, K Guillemyn, M Dumitrascuta… - Pain, 2018 - journals.lww.com
… of opioid-induced analgesic tolerance and other adverse effects. … analgesic effect of morphine,
56 and to potentiate opioid … prevents the development of opioid-induced hyperalgesia (…