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Comparison of Pharmacokinetics of Long-Acting Local Analgesics: CPL-01, a Novel Extended-Release Ropivacaine, Demonstrates Consistent and Predictable Exposure Compared with Liposomal Bupivacaine.
Clin Drug Investig
January 2025
Cali Biosciences, US, LLC, San Diego, CA, USA.
Background And Objective: There is a significant medical need for improved long-acting local anesthetics to decrease postsurgical pain and reduce postoperative opioid use. While ropivacaine is considered a safer local anesthetic than bupivacaine, no long-acting ropivacaine formulation is currently marketed. Available formulations of bupivacaine show inconsistent pharmacokinetics (PK) among different surgical models, and inconsistency in PK may lead to a reluctance to use the medication owing to fear of local anesthetic systemic toxicity (LAST) or unreliable efficacy.
View Article and Find Full Text PDFThe role of weak interactions in evaluation of inhibitory potential of Indinavir as an HIV protease inhibitor and its comparison with innovative drug candidates.
Comput Biol Med
January 2025
Department of Chemistry, Graduate University of Advanced Technology, Kerman, Iran.
Designing and employing enzyme inhibitors against viral enzymes is one of the innovative and efficient approaches to treating viral diseases. These inhibitors can disrupt the viral replication cycle by deactivating vital enzymes, thereby curbing the spread of viral infections by reducing their population. So far, inhibitors have been designed, validated, and introduced for these enzymes.
View Article and Find Full Text PDFChemical Profiling, Antioxidant, and Antiproliferative Activities of Algerian Cistus creticus L. Leaf Extracts: Evidence from In vitro and In Silico Studies.
Curr Top Med Chem
January 2025
Medicinal Chemistry Department, Theodor Bilharz Research Institute Kornaish El Nile, Warrak El-Hadar, Imbaba (P.O. 30), Giza 12411, Egypt.
Background: Research into oxidative stress, cancer, and natural products revealed promising avenues for therapeutic intervention. Natural products are considered potent pharmaceuticals in combating oxidative stress and its relationship with cancer.
Methods: This study was carried out to evaluate the chemical profile and antioxidant activities using DPPH, ABTS, Phenanthroline, Cupric, Phosphomolybdenum, FRAP, Hydroxyl, Iron chelation in vitro assays, and anticancer properties by MTT method of Cistus creticus extracts.
Thigh Injections of Cabotegravir + Rilpivirine in Virally Suppressed Adults With Human Immunodeficiency Virus Type 1: A Substudy of the Phase 3b ATLAS-2M Study.
Clin Infect Dis
January 2025
ViiV Healthcare, Durham, North Carolina, USA.
Article Synopsis
- CAB + RPV is the first long-acting HIV treatment regimen using thigh injections, showing promising results in maintaining viral suppression.
- The study involved 118 participants and compared pharmacokinetic changes and tolerability between thigh and gluteal injections, finding no significant differences in effectiveness.
- Results indicated that a majority of participants preferred thigh injections, with potential plans for more flexible dosing schedules to enhance treatment convenience.
Evidence for the anxiolytic- and antidepressant-like effects of three semi-synthetic derivatives of xylopic acid in mice.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Pharmacology and Toxicology, School of Pharmacy, University of Health and Allied Sciences, Ho, Ghana.
Purpose: Major depressive disorder is one of the most common and burdensome psychiatric disorders worldwide. This study evaluated the anxiolytic- and antidepressant-like activity of three semi-synthetic derivatives of xylopic acid (XA) to identify the most promising derivative based on mechanism(s) of action, in vivo pharmacokinetics and in vitro cytotoxicity.
Methods: The anxiolytic potential and the involvement of GABAergic mechanisms were assessed in the elevated plus-maze and open field tests in mice.
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