A randomized controlled trial of rectal versus intramuscular diclofenac for post-operative analgesia after open myomectomy
To determine the efficacy and safety of rectal versus intramuscularly administered Diclofenac in reducing post-operative pain in the first 24  h after open-myomectomy. (Source: European Journal of Obstetrics, Gynecology, and Reproductive Biology)
Source: European Journal of Obstetrics, Gynecology, and Reproductive Biology - November 29, 2023 Category: OBGYN Authors: John C. Irechukwu, George U. Eleje, Bobbie C. Iwe, Okechukwu C. Ikpeze, Arinze C. Ikeotuonye, Eziaha E. Ede, Chidinma C. Okafor, Divinefavour E. Malachy, Chigozie G. Okafor Tags: Full length article Source Type: research

A premature stop codon in the CYP2C19 gene may explain the unexpected sensitivity of vultures to diclofenac toxicity
Toxicol Appl Pharmacol. 2023 Nov 25:116771. doi: 10.1016/j.taap.2023.116771. Online ahead of print.ABSTRACTThe unintended environmental exposure of vultures to diclofenac has resulted in the deaths of millions of old-world vultures on the Asian subcontinent. While toxicity has been since associated with a long half-life of elimination and zero order metabolism, the actual constraint in biotransformation is yet to be clarified. For this study we evaluated if the evident zero order metabolism could be due to defects in the CYP2C9/2C19 enzyme system. For this, using whole genome sequencing and de-novo transcriptome alignment,...
Source: Toxicology and Applied Pharmacology - November 28, 2023 Category: Toxicology Authors: Emmanuel Oluwasegun Adawaren Christiaan Labuschagne Aron Abera Vinny Naidoo Source Type: research

A premature stop codon in the CYP2C19 gene may explain the unexpected sensitivity of vultures to diclofenac toxicity
Toxicol Appl Pharmacol. 2023 Nov 25:116771. doi: 10.1016/j.taap.2023.116771. Online ahead of print.ABSTRACTThe unintended environmental exposure of vultures to diclofenac has resulted in the deaths of millions of old-world vultures on the Asian subcontinent. While toxicity has been since associated with a long half-life of elimination and zero order metabolism, the actual constraint in biotransformation is yet to be clarified. For this study we evaluated if the evident zero order metabolism could be due to defects in the CYP2C9/2C19 enzyme system. For this, using whole genome sequencing and de-novo transcriptome alignment,...
Source: Toxicology and Applied Pharmacology - November 28, 2023 Category: Toxicology Authors: Emmanuel Oluwasegun Adawaren Christiaan Labuschagne Aron Abera Vinny Naidoo Source Type: research

Urolithin A conjugation with NSAIDs inhibits its glucuronidation and maintains improvement of Caco-2 monolayers' barrier function
Biomed Pharmacother. 2023 Nov 23;169:115932. doi: 10.1016/j.biopha.2023.115932. Online ahead of print.ABSTRACTUrolithin A (UA) is an ellagitannin-derived postbiotic metabolite which emerged as a promising health-boosting agent, promoting mitophagy, improving skeletal muscle function, and suppressing the inflammatory response. However, phase II intestinal metabolism severely limits its biopotency, leading to the formation of nonactive glucuronides. To address this constraint, a set of new UA derivatives (UADs), conjugated with nonsteroidal anti-inflammatory drugs (NSAIDs), was synthesized. The bioavailability and inhibitory...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - November 24, 2023 Category: Drugs & Pharmacology Authors: Maciej Korczak Piotr Roszkowski Weronika Skowro ńska Klaudia M Żołdak Dominik Popowski Sebastian Granica Jakub P Piwowarski Source Type: research

Urolithin A conjugation with NSAIDs inhibits its glucuronidation and maintains improvement of Caco-2 monolayers' barrier function
Biomed Pharmacother. 2023 Nov 23;169:115932. doi: 10.1016/j.biopha.2023.115932. Online ahead of print.ABSTRACTUrolithin A (UA) is an ellagitannin-derived postbiotic metabolite which emerged as a promising health-boosting agent, promoting mitophagy, improving skeletal muscle function, and suppressing the inflammatory response. However, phase II intestinal metabolism severely limits its biopotency, leading to the formation of nonactive glucuronides. To address this constraint, a set of new UA derivatives (UADs), conjugated with nonsteroidal anti-inflammatory drugs (NSAIDs), was synthesized. The bioavailability and inhibitory...
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - November 24, 2023 Category: Drugs & Pharmacology Authors: Maciej Korczak Piotr Roszkowski Weronika Skowro ńska Klaudia M Żołdak Dominik Popowski Sebastian Granica Jakub P Piwowarski Source Type: research

Neuroendocrine response to diclofenac in healthy subjects: a pilot study
ConclusionDiclofenac resulted in an increased ECF at 48  h, but this phenomenon seems to be associated with a greater renal sensibility to the action of vasopressin rather than with an increase in its secretion. Moreover, a partial inhibitory effect on cortisol secretion can be hypothesized. (Source: Journal of Endocrinological Investigation)
Source: Journal of Endocrinological Investigation - November 17, 2023 Category: Endocrinology Source Type: research

Diclofenac, ibuprofen, and paracetamol biodegradation: overconsumed non-steroidal anti-inflammatories drugs at COVID-19 pandemic
Front Microbiol. 2023 Oct 30;14:1207664. doi: 10.3389/fmicb.2023.1207664. eCollection 2023.ABSTRACTThe consumption of non-steroidal anti-inflammatory drugs (NSAIDs) have increased significantly in the last years (2020-2022), especially for patients in COVID-19 treatment. NSAIDs such as diclofenac, ibuprofen, and paracetamol are often available without restrictions, being employed without medical supervision for basic symptoms of inflammatory processes. Furthermore, these compounds are increasingly present in nature constituting complex mixtures discarded at domestic and hospital sewage/wastewater. Therefore, this review em...
Source: Cancer Control - November 15, 2023 Category: Cancer & Oncology Authors: Beatriz L Ferreira Dionisia P Ferreira Swanny F Borges Adriana M Ferreira Fabricio H Holanda Jo ão G M Ucella-Filho Rodrigo Alves S Cruz Willian G Birolli Rafael Luque Irlon M Ferreira Source Type: research

Ternary Deep Eutectic Solvents System of Colchicine, 4-Hydroxyacetophenone, and Protocatechuic Acid and Characterization of Transdermal Enhancement Mechanism
This study aimed to prepare colchicine (CO), 4-hydroxyacetophenone (HA), and protocatechuic acid (CA) contained in transdermal rubber plasters into a more releasable and acrylate pressure-sensitive adhesive (PSA) to optimize traditional Touguling rubber plasters (TOU) with enhanced transdermal permeability by using deep eutectic solvents (DES) technology. We compared the difference in the release behavior of CO between rubber plaster and PSA, determined the composition of the patch through pharmacodynamic experiments, explored the transdermal behavior of the three components, optimized the patch formula factors, and improv...
Source: AAPS PharmSciTech - November 14, 2023 Category: Drugs & Pharmacology Authors: Huiqing Piao Wanchen Xie Shiqi Li Jiaqi Wang Chao Liu Peng Quan Liang Fang Source Type: research

Ternary Deep Eutectic Solvents System of Colchicine, 4-Hydroxyacetophenone, and Protocatechuic Acid and Characterization of Transdermal Enhancement Mechanism
This study aimed to prepare colchicine (CO), 4-hydroxyacetophenone (HA), and protocatechuic acid (CA) contained in transdermal rubber plasters into a more releasable and acrylate pressure-sensitive adhesive (PSA) to optimize traditional Touguling rubber plasters (TOU) with enhanced transdermal permeability by using deep eutectic solvents (DES) technology. We compared the difference in the release behavior of CO between rubber plaster and PSA, determined the composition of the patch through pharmacodynamic experiments, explored the transdermal behavior of the three components, optimized the patch formula factors, and improv...
Source: AAPS PharmSciTech - November 14, 2023 Category: Drugs & Pharmacology Authors: Huiqing Piao Wanchen Xie Shiqi Li Jiaqi Wang Chao Liu Peng Quan Liang Fang Source Type: research

Curcuminoids-enriched extract and its cyclodextrin inclusion complexes ameliorates arthritis in complete Freund ’s adjuvant-induced arthritic mice via modulation of inflammatory biomarkers and suppression of oxidative stress markers
AbstractCurcuma longa extract and its marker curcuminoids have potential use in inflammatory conditions. However, curcuminoids solubility and bioavailability are major hindrances to their bioactivity. The current study investigated green extraction-based curcuminoids-enriched extract (CRE) prepared fromC. longa and its cyclodextrin inclusion complexes, i.e., binary inclusion complexes (BC) and ternary inclusion complexes (TC), in complete Freund ’s adjuvant (CFA)-induced mice for their comparative anti-arthritic efficacy. CRE, BC, and TC (2.5 and 5 mg/kg) with the standard drug diclofenac sodium (13.5 mg/kg) were orall...
Source: Inflammopharmacology - November 13, 2023 Category: Drugs & Pharmacology Source Type: research

Neuroendocrine response to diclofenac in healthy subjects: a pilot study
ConclusionDiclofenac resulted in an increased ECF at 48  h, but this phenomenon seems to be associated with a greater renal sensibility to the action of vasopressin rather than with an increase in its secretion. Moreover, a partial inhibitory effect on cortisol secretion can be hypothesized. (Source: Journal of Endocrinological Investigation)
Source: Journal of Endocrinological Investigation - November 9, 2023 Category: Endocrinology Source Type: research