The role of a pharmacist in prevention and detection of OTC drug interactions: Nominal group technique

Introduction: Nowadays number of newly approved OTC medicines continuously increases, which can make certain difficulties in drug dispensing process. This fact particularly relates to drug-drug interactions-problems due to lack of data and insufficient of knowledge about the interactions. Aim: To identify the problems pharmacists face when dispensing OTC drugs and to recommend concrete ideas and methods for improving system for detecting OTC drugs interactions. Participants and method: The study was carried out in accordance with methodological principles of nominal group technique. Two meetings of nominal group were conducted, enrolling pharmacists employed in public pharmacies. During the meetings, moderator imposed aset of questions to participants, who gave answers in the form of individual statements. In order to examine agreement of the participants about the individual statements, at the end of both sessions the statements were rated on a Likert's scale. Meetings were recorded and audio recordings later used for qualitative analysis. Results: Nine pharmacists of both sex (7/2 females/males) participated in this study. Average age of the participants was 25.0±1.0 years. During nominal group meetings, participants presented 30 statements on 7 research questions, and after the second meeting agreement was reached about 29 of them. Qualitative analysis of data indicated three categories of statements: (1) pharmacists' knowledge of OTC drugs interactions, (2) problems pharmacists face when dispensing OTC drugs and (3) options of improving system for prevention and detection of OTC drugs interactions. Conclusion: For adequate prevention of potential OTC drugs interactions it is necessary to make guidelines with recommendations referring to proper dispensing procedure and to use regularly available online interaction checkers

Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen

The aim of the study was a synthesis and investigation of the dose-dependent anti-inflammatory effect of new thiourea derivatives of naproxen with selected aromatic amines and esters of aromatic amino acids. The results of the in vivo study indicate that derivatives of m-anisidine (4) and N-methyl tryptophan methyl ester (7) showed the most potent anti-inflammatory activity four hours after injection of carrageenan, with the percentage of inhibition of 54.01% and 54.12%, respectively. In vitro assays of COX-2 inhibition demonstrated that none of the tested compounds achieved 50% inhibition at concentrations lower than 100 µM. On the other hand, the aromatic amine derivatives (1–5) accomplished significant inhibition of 5-LOX, and the lowest IC50 value was observed for compound 4 (0.30 μM). High anti-edematous activity of compound 4 in the rat paw edema model, together with potent inhibition of 5-LOX, highlight this compound as a promising anti-inflammatory agen

Selected thiourea derivatives of naproxen as potential anti-inflammatory agents: in vivo, in vitro, and in silico approach

The aim of the conducted study was to develop new potential dual COX-2 and 5-LOX inhibitors based on naproxen scaffold. We performed the evaluation of in vivo and in vitro anti-inflammatory activity of newly synthesized thiourea derivatives of naproxen containing m-anisidine and N-methyl tryptophan methyl ester in a side chain. An in vivo study was carried out using a carrageenan-induced paw edema model of acute inflammation. COX-2 and 5-LOX inhibitory potential of synthesized compounds was evaluated using fluorometric inhibitor screening kits. In silico study was performed in OEDocking 3.2.0.2 software with the FRED tool. Two investigated derivatives exhibited comparable anti-inflammatory activity to naproxen (56.32%) four hours after injection of carrageenan, with the percentage of inhibition being 54.01% (m-anisidine derivative) and 54.12% (N-methyl tryptophan methyl ester derivative). In vitro studies of COX-2 inhibition demonstrated that none of the tested compounds achieved 50% inhibition at concentrations below 100 μM, whereas the m-anisidine derivative accomplished comparable inhibition of 5-LOX (IC50 = 0.30 μM) to commercial 5-LOX inhibitor zileuton (IC50 = 0.36 μM). Inability of the tested compounds to form three hydrogen bonds with ARG120 and TYR355 could be a reason why these compounds showed weak COX-2 inhibition. The m-anisidine derivative formed a more stable complex with the 5-LOX enzyme (−8.39 kcal/mol), compared to N-methyl tryptophan methyl ester derivative (−7.98 kcal/mol), with the absence of the iron ion chelation in the active site in both cases. The significant in vivo anti-inflammatory activity of the m-anisidine derivative, together with the potent inhibition of 5-LOX, highlighted this compound as a promising anti-inflammatory agent

Synthesis, Characterization, and Investigation of Anti-Inflammatory and Cytotoxic Activities of Novel Thiourea Derivatives of Naproxen

The objective of this study was to synthesize seven novel thiourea derivatives of naproxen (8–14), examine the anti-inflammatory activity of the newly synthesized compounds, investigate the cytotoxic potential of both sets of synthesized compounds (1–7 and 8–14), and select the most promising anti-inflammatory and antitumor drug candidates. The results of the in vivo anti-inflammatory study clearly showed that compounds 8 and 9 were capable of decreasing paw edema, as evident from a high percentage of inhibition (44.83% and 49.29%, respectively). In addition, the results of in vitro enzyme inhibition assays demonstrated that neither of the newly synthesized compounds reached 50% inhibition of 5-LOX at concentrations lower than 100 μM. In terms of antitumor potential, derivatives 3 and 8 exhibited strong cytotoxic effects on the HeLa cell line, suggesting the involvement of the extrinsic pathway of apoptosis. According to the overall results obtained for both sets of synthesized molecules, derivatives 4 and 8 can be underlined as molecules with the strongest anti-inflammatory activity, while derivatives 3 and 8 are the most promising cytotoxic agents

Formulation and Evaluation of Helichrysum italicum Essential Oil-Based Topical Formulations for Wound Healing in Diabetic Rats

As proper wound management is crucial to reducing morbidity and improving quality of life, this study evaluated for the first time the wound healing potential of H. italicum essential oil (HIEO) prepared in the form of ointment and gel in streptozotocin-induced diabetic wound models in rats. After creating full-thickness cutaneous wounds, forty-eight diabetic rats were divided into six groups: (1) negative control; (2) positive control; (3) ointment base; (4) gel base; (5) 0.5% HIEO ointment (6) 0.5% HIEO gel. Wound healing potential was determined by the percentage of wound contraction, hydroxyproline content, redox status, and histological observation. A significant decrease in the wound size was observed in animals treated with HIEO formulations compared with other groups. The HIEO groups also showed a higher level of total hydroxyproline content, and more pronounced restitution of adnexal structures with only the underlying muscle defect indicating the incision site. Hence, our results legitimate the traditional data of the pro-healing effect of HIEO because HIEO in both formulations such as gel and ointment exhibited the significant wound repairing effect in the incision wound model