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Modulation of morphine antinociceptive and rewarding effect by mirtazapine in an animal model of osteoarthritic pain.
Eur J Pharmacol
January 2025
Area of Pharmacology, Nutrition and Bromatology, Department of Basic Health Sciences, Rey Juan Carlos University (URJC), Associated R+D+i Unit to the Institute of Medicinal Chemistry (IQM), Scientific Research Superior Council (CSIC), Alcorcón, Spain; High Performance Research Group in Experimental Pharmacology (PHARMAKOM) of the Rey Juan Carlos University, Alcorcón, Spain.
People with chronic pain mitigate their suffering by the action of opioids. Adverse reactions aside, opioids are not exempt from potential complications like addiction and abuse, which have posed a global public health problem lately. Finding new therapeutic strategies to improve analgesia and to reduce opioid side effects has become a priority.
View Article and Find Full Text PDFNaltrexone blocks alcohol-induced effects on kappa-opioid receptors in the plasma membrane.
Transl Psychiatry
November 2024
Department of Clinical Neuroscience, Center for Molecular Medicine, Karolinska Institutet, Stockholm, SE-17176, Sweden.
Naltrexone (NTX), a homolog of the opiate antidote naloxone, is an orally active long-acting general opioid receptor antagonist used in the treatment of opiate dependence. NTX is also found to relieve craving for alcohol and is one of few FDA-approved medications for treatment of alcohol use disorder (AUD). While it was early on established that NTX acts by blocking the binding of endogenous opioid peptide ligands released by alcohol, experimental evidence emerged that could not be fully accounted for by this explanation alone, suggesting that NTX may have additional modes of action.
View Article and Find Full Text PDFA Single-Dose Study to Evaluate the Relative Bioavailability, Safety, and Tolerability of Monthly Extended-Release Buprenorphine at Alternative Injection Locations in Adult Participants with Opioid Use Disorder.
Clin Drug Investig
December 2024
Research and Development, Indivior Inc., North Chesterfield, VA, USA.
Background And Objectives: Buprenorphine extended-release monthly formulation (BUP-XR, SUBLOCADE) is approved for treatment of moderate-to-severe opioid use disorder (OUD) following subcutaneous injection in the abdomen. This open-label pharmacokinetic study assessed three alternative injection locations (upper arm, thigh, buttocks) to offer additional flexibility considering the chronic nature of the disease and patient preferences.
Methods: Following stabilization on 12/3 mg/day of sublingual buprenorphine/naloxone for ≥ 7 days, participants with moderate-to-severe OUD were randomized to receive a single 300-mg BUP-XR injection in the upper arm, thigh, buttocks, or abdomen (reference).
Physiologically based pharmacokinetic modeling of long-acting extended-release naltrexone in pregnant women with opioid use disorder.
CPT Pharmacometrics Syst Pharmacol
November 2024
Division of Maternal Fetal Medicine, Department of Gynecology & Obstetrics, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA.
Article Synopsis
- * A new study developed a pharmacokinetic model to analyze how XR-NTX behaves in pregnant women, predicting appropriate dosing by simulating maternal plasma levels during different pregnancy trimesters.
- * Results showed that lowering the XR-NTX dose to 285 mg in the first/second trimester and 190 mg in the third trimester could maintain control comparable to non-pregnant women, providing important data for future clinical decisions
Stimulation of kappa opioid receptors in the nucleus accumbens promotes feeding behavior in mice: Acute restoration of feeding during anorexia induced by 5-fluorouracil.
Eur J Pharmacol
December 2024
Department of Pathophysiology and Therapeutics, Hoshi University School of Pharmacy and Pharmaceutical Sciences, 2-4-41 Ebara, Shinagawa-ku, Tokyo, Japan. Electronic address:
Article Synopsis
- Scientists studied how a type of receptor in the brain called kappa (κ) opioid receptors affects eating and sugar levels in the body.
- They found that a drug called nalfurafine increased how much food animals ate, but only when they weren't hungry.
- This study suggests that nalfurafine might help people with a loss of appetite caused by cancer treatment.
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