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Drug Overdoses during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Propoxyphene or pentazocine overdose during pregnancy is not published. Nonspecific and supportive antidote therapy should be given because the effectiveness and safety of nalmefene for narcotic overdose have been demonstrated only in a pilot study. Naloxone and pentazocine combinations are used to treat moderate pain. Synthetic narcotic drugs are known to cross the placenta, and chronic use during pregnancy exposes the fetus to sufficient amounts to produce neonatal abstinence syndrome. Narcotics may cause fetal hepatic enzyme activity, and hasten liver enzyme maturation. Effects of potentially toxic doses of pentazocine are unknown. Adult half-lives of propoxyphene and pentazocine in the post-absorptive period are 8–24 hours and 2.1–3.5 hours, respectively (Baselt, 2017).
Improving the Old, Embracing the New: Implications of Alcohol Research for Future Practice
Published in Gary Rosenberg, Weissman Andrew, Behavioral and Social Sciences in 21st Century Health Care: Contributions and Opportunities, 2021
Researchers recently completed a clinical trial of a new opioid antagonist called “nalmefene” in which it significantly reduced relapse to heavy drinking among recovering alcoholics. In this trial, patients taking placebos were twice as likely to relapse as were patients taking nalmefene. Further, none of the 105 patients who took part in the trial suffered major adverse effects from nalmefene. In previous studies in which naltrexone and nalmefene were compared, nalmefene entered the bloodstream more quickly and had a somewhat lower risk of liver toxicity than did naltrexone. (It should be noted that at typical dosages, liver toxicity is not a significant problem with naltrexone.) In addition, data suggest that nalmefene may be more potent than naltrexone in that it binds more readily with the three subtypes of opioid receptors that are thought to reinforce alcohol consumption whereas naltrexone specifically binds to just one receptor subtype and may affect the other two only at high doses.
Opioids Analgesics and Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
R. Rachana, Tanya Gupta, Saumya Yadav, Manisha Singh
Nalmefene antagonizes opioids at other receptors but, do have a greater affinity for µ receptors like naloxone. It antagonizes µ receptors agonist effects four times vigorously as naloxone. If, given parenterally, it needs at least 4 h to act (dose dependent) but, it lasts up to 48 h if, given orally (Dixon et al., 1986).
Current pharmacotherapy for gambling disorder: a systematic review
Published in Expert Opinion on Pharmacotherapy, 2020
Shane W. Kraus, Repairer Etuk, Marc N. Potenza
Nalmefene is another opioid-receptor antagonist that has shown some encouraging results in the treatment of PG. In comparison to naltrexone, nalmefene also has significant affinity for mu-opioid receptors, differential affinity for kappa receptors, and lower likelihood of inducing hepatotoxicity. In a multicenter trial with a 16-week, double-blind, placebo-controlled design, 207 patients were randomized to receive placebo or nalmefene at flexible doses (25 mg, 50 mg, or 100 mg) [55]. The 25 mg and 50 mg nalmefene groups presented greater improvements in problem-gambling severity compared to the placebo group. Furthermore, 59.2% of patients receiving 25 mg of nalmefene were classified as responders which were significantly higher than the 34% of patients considered placebo-responders. Lastly, in 2010 a second multicenter trial was completed by Grant and colleagues [56] with a similar design that included 233 patients assigned to nalmefene (20 mg or 40 mg doses) or to placebo. This extension of their previous study provided less positive results for nalmefene, as in the initial analyses nalmefene failed to show treatment differences from placebo in the outcomes of problem-gambling severity, symptoms, or disability. However, in post-hoc analyses with only the patients who received dosing of the medication/placebo for at least 1 week, the 40-mg-nalmefene group had a greater reduction in problem-gambling severity than did the placebo group.
Safety of nalmefene for the treatment of alcohol use disorder: an update
Published in Expert Opinion on Drug Safety, 2020
Hugo López-Pelayo, Paola Zuluaga, Elsa Caballeria, Wim Van den Brink, Karl Mann, Antoni Gual
Within the safety and tolerability analysis of randomized phase III studies of nalmefene versus placebo – ESENSE1 [13], ESENSE2 [14], and SENSE [23]-, up to 75% of patients in the nalmefene group and 63% in the placebo group reported adverse events (AEs). These differences were statistically significant in the ESENSE1 and SENSE studies. Nausea, dizziness, headache, and insomnia were the most frequent symptoms in the nalmefene group, with 13% of the patients abandoning the medication, compared to 6% in the placebo group. Most AEs were transient, with an average length of 3 to 7 days and occurred during the first days of medication use. Psychiatric AEs were reported in 2.9% of the patients, mainly confusional symptoms, generally occurring after the first dose and with a short duration [17].
Psychotic Decompensation During Nalmefene Treatment in a Patient With Schizoaffective Disorder: A Case Report
Published in Journal of Dual Diagnosis, 2019
Juliette Salles, Camille Ponté, Laurent Schmitt
In 2015, the European Medicines Agency (EMA) approved nalmefene for the treatment of alcohol dependence. Nalmefene was approved in Europe to reduce alcohol intake after a Phase 3 trial (NCT00811720) and the ESENSE2 trial (NCT00812461) showed a significantly greater effect of nalmefene versus placebo in reducing the number of heavy drinking days after 6 months of treatment. In those studies, the most common adverse effects (AEs) related to nalmefene were gastrointestinal and central nervous system effects, particularly nausea, vomiting, anxiety, and dizziness (Gual et al., 2013). Data from the American National Epidemiologic Survey on Alcohol and Related Conditions (NESARC) cohort have shown that AUD was associated with mood and anxiety disorders in almost 40% of the participants (Jeanblanc, 2015; Hoertel et al., 2014). However, this high prevalence in “real-world” studies is not found in clinical trial samples, as alcohol-dependent patients with current psychiatric disorders are likely to be excluded from these studies (Hoertel et al., 2014).