American Journal of Pharmacotherapy and Pharmaceutical Sciences最新文献

{"title":"Emerging therapies targeting cardiovascular risk factors to prevent or delay the onset of heart failure","authors":"Olisaemeka Zikora Akunne, Ogochukwu Emilia Anulugwo","doi":"10.25259/ajpps_2024_013","DOIUrl":"https://doi.org/10.25259/ajpps_2024_013","url":null,"abstract":"Cardiovascular disease (CVD) poses a significant global health concern, contributing to nearly 30% of global deaths. Its prevalence is on the rise, necessitating a deeper understanding of associated risk factors including hypertension, cardiac hypertrophy, and diabetes. Addressing these risk factors is crucial in preventing or slowing the onset of heart failure (HF), a complex chronic condition with high morbidity and mortality rates. This review aims to explore innovative strategies for preventing or delaying HF, focusing on cardiovascular risk (CV) factors. Specifically, it delves into the link between hypertension, cardiac hypertrophy, diabetes, and HF emphasizing the importance of identifying new therapeutic approaches. A comprehensive examination of existing literature, clinical trials, and experimental models forms the basis of this review providing insights into the interconnected nature of cardiovascular risk factors and the efficacy of combination therapies. Evidence from diverse sources supports the adoption of a multifaceted approach to HF prevention. The review underscores the complex associations between hypertension, cardiac hypertrophy, diabetes, and HF highlighting the need for innovative therapeutic interventions. Clinical trials demonstrate promising outcomes with synergistic therapies such as angiotensin-converting enzyme (ACE) inhibitors, beta-blockers, and sodium-glucose cotransporter-2 (SGLT-2) inhibitors showcasing improved efficacy over single-agent interventions. In conclusion, adopting a multifaceted approach to HF prevention considering the interplay of various risk factors. Such an approach holds the potential for substantial benefits including simultaneous targeting of multiple pathways, individualized care, enhanced patient motivation, and reduced healthcare costs. Further research should focus on optimizing combination therapies and identifying patient population that stands to gain the most from these interventions providing a pathway towards improved cardiovascular health globally.","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"98 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141663959","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Assessment of β-lactamase inhibition and antioxidant potential of ethanolic and aqueous leaf extracts of Irvingia gabonensis using GC-MS method","authors":"Stanley Chukwuma Okereke, Valentine Chibuike Edom, C. J. Nwaogwugwu, Chinomso Friday Aaron, Prince oko Ifegwu, Bruno Obinna Iwuchukwu, George Ugochukwu Ekechukwu, Stanley Udochukwu Alugbuo, Ugoaghalam Uche James","doi":"10.25259/ajpps_2024_014","DOIUrl":"https://doi.org/10.25259/ajpps_2024_014","url":null,"abstract":"\u0000\u0000This study aimed to investigate the antibiotic and antioxidant potential of aqueous and ethanol extracts from Irvingia gabonensis leaves, with a specific focus on their ability to inhibit β-lactamase enzyme activity. Both in vitro and in vivo approaches were employed to comprehensively assess the characteristics of the leaf extracts. Irvingia gabonensis, known for its medicinal properties, has been of interest due to its reported pharmacological activities. In the face of rising antimicrobial resistance, exploring natural sources for antimicrobial and antioxidant agents is crucial. This study builds upon existing knowledge by evaluating the phytochemical composition and potential therapeutic applications of Irvingia gabonensis leaf extracts.\u0000\u0000\u0000\u0000Gas chromatography-mass spectrometry (GC-MS) analysis was employed to identify the chemical components present in ethanolic leaf extracts. Antioxidant activities were assessed through various assays, including DPPH, FRAP, nitric oxide radical scavenging, and MDA scavenging assays. In vivo experiments involved the administration of different concentrations of leaf extracts to albino rats over a 28-day period. Blood samples collected were utilized for serum separation, enabling the analysis of antioxidant assays in vivo, including β-lactamase inhibition, lipid peroxidation (MDA), superoxide dismutase (SOD), and catalase (CAT) activity.\u0000\u0000\u0000\u0000The ethanolic extracts exhibited a significant 65.96% inhibition rate against β-lactamase enzyme activity. Additionally, there was an increase in the concentrations of glutathione (GSH) and glutathione peroxidase (GPx), as well as heightened catalase (CAT) activity. Simultaneously, a decrease in malondialdehyde (MDA) concentration indicated the extracts’ potential to mitigate lipid peroxidation. These results highlight the robust antimicrobial and antioxidant properties of Irvingia gabonensis leaf extracts.\u0000\u0000\u0000\u0000Irvingia gabonensis leaf extracts demonstrate substantial potential as antimicrobial and antioxidant agents, emphasizing their role in combating antimicrobial resistance. The significant inhibition of β-lactamase enzyme activity and the modulation of key antioxidant markers suggest the extracts’ therapeutic relevance. This study contributes to the understanding of Irvingia gabonensis phytochemical composition and supports its potential application as an antioxidant supplement and β-lactamase inhibitor.\u0000","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"65 17","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-07-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141663379","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antipsychotic initiation in mechanically ventilated patients in a medical intensive care unit","authors":"Hannah R. Ritchie, Taylor J. Hodle, Hannah E. Spinner","doi":"10.25259/ajpps_2024_001","DOIUrl":"https://doi.org/10.25259/ajpps_2024_001","url":null,"abstract":"\u0000\u0000Guidelines for the prevention and management of pain, agitation/sedation, delirium, immobility, and sleep disruption in adult patients (PADIS) in the intensive care unit (ICU) promote use of analgosedation to minimize pain, reduce anxiety, and facilitate care. They also suggest against routine use of antipsychotics (APs) for delirium. Our institution’s adaptation incorporates assessment-driven, protocol-based pain, and sedation management and suggests a short course of APs in patients with agitated delirium, defined as Confusion Assessment Method for the ICU (CAM-ICU) positive with Richmond Agitation Sedation Scale (RASS) ≥ +2. While the use of APs in the ICU is typically for delirium, a recent study assessed whether quetiapine reduced sedative requirements among non-delirious patients. The purpose of this study was to assess adherence to our institutional guideline for AP use and to describe sedative and opioid use in relation to AP initiation.\u0000\u0000\u0000\u0000This retrospective study included patients who were mechanically ventilated and received ≥ 3 new start AP doses. The primary outcome was adherence to our guideline for use of APs in agitated delirium. The secondary outcomes were CAM-ICU and RASS scores in relation to AP initiation and change in sedative and analgesic infusion rates following AP initiation.\u0000\u0000\u0000\u0000Thirty-eight patients were included in the study. Five had APs initiated appropriately per our guideline. There was no clinically significant change in continuous infusion rates in the 24 h before and after AP initiation.\u0000\u0000\u0000\u0000Overall, AP use was liberal with patients being started on APs who did not have agitated delirium, thus indicating potential alternative indications for initiation. APs did not result in a clinically significant change in continuous infusion requirements in the 24 h following initiation.\u0000","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"8 6","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139380677","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A post-COVID-19 IDEA to strengthen research, innovation, and development in Africa","authors":"Solomon Nwaka, Muhammadou M. O. Kah, Christian Chikelu Anieke","doi":"10.25259/ajpps_2023_021","DOIUrl":"https://doi.org/10.25259/ajpps_2023_021","url":null,"abstract":"Globally, research, innovation, and the associated education and entrepreneurship are essential for youth and socioeconomic development. Governments, universities, research institutions, and private sector play various roles in the innovation value chain. The weak research and innovation systems in Africa are often linked to the overarching challenges of poor financing, inadequate capacity, weak infrastructure, and processes. Many African universities and research institutions are challenged to validate and transition their ideas and discoveries from the laboratory to field evaluation, and downstream development, registration, and commercialization processes. The critical discovery–development interface that is normally driven by the private sector is also not well developed. Overcoming these constraints require concerted local and global partnerships, sharing of available resources and assets, and training and use of suitable Information and Communications Technology and digital tools to boost productivity. Importantly, this requires private sector engagement and development. We discuss how the Innovation Development and Entrepreneurship Africa aims to use available assets in Africa to support institutions and youths to stimulate innovation. Redoubling efforts toward African development in the post COVID-19 era, in alignment with the African Union Agenda 2063 and the Sustainable Development Goals, will require investment in support of these ideals. We offer some policy recommendations in this context.","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"28 12","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138589251","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Neurostimulation as a potential modality for transitioning patients with chronic refractory pain syndromes off opioid analgesics: A systematic review","authors":"Kyle Blalock, Ngozi C Mezu-Patel, Nina Mezu-Nwaba","doi":"10.25259/ajpps_2023_020","DOIUrl":"https://doi.org/10.25259/ajpps_2023_020","url":null,"abstract":"Opioid analgesics are mu-opioid agonists used in practice for pain management which pose significant health risks including, but not limited to, abuse, dependence, respiratory depression, overdose, and death. Medical devices such as spinal cord stimulators (SCS) – which fall under the category of neurostimulators – may offer an alternative method for pain management. Four searches were conducted on PubMed and the Cochrane Trials database to assess the effects neurostimulation has on opioid consumption. Sixty-two (62) unique results originally populated, and six studies out of the 62 results met inclusion criteria. One result was a neurophysiological study which found transcranial magnetic stimulation (TMS) decreased mu-opioid receptor availability (P < 0.001), thereby suggesting TMS may activate the release of endogenous opioids. Five results were clinical studies utilizing SCS for chronic pain. These five studies cumulatively enrolled 330 participants, 57 of which were withdrawn and 139 of which were using opioids at the time of enrollment. Following neurostimulation, 41% of participants discontinued opioid use altogether, 26.6% of participants decreased opioid use, 26.6% of participants remained on the same opioid dose, and 5.8% of participants increased opioid use. Overall opioid use decreased by an estimated 45.6% ± 13 following SCS. The median trial duration was 1 year, and the median sample size was 23 participants. Although the results unanimously showed effectiveness for pain control and opioid dose reductions, the studies in this review were small, and none were placebo-controlled. The statistical fallbacks of the five SCS studies make it difficult to draw concrete conclusions. More research is needed to ascertain the risk-benefit profiles of neurostimulators in chronic pain patients.","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139240832","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bioequivalence assessment of two formulations of empagliflozin in healthy adult subjects","authors":"Evelyn Pena, Alfredo Inatti, Anyoli Taly, José Gregorio Chacón, Xenon Serrano-Martin","doi":"10.25259/ajpps_2023_019","DOIUrl":"https://doi.org/10.25259/ajpps_2023_019","url":null,"abstract":"The objective of the study was to evaluate the bioequivalence (BE) between Izaban® (test) and Jardiance® (reference) empagliflozin 25 mg, oral tablets, in healthy adult subjects. A randomized, open-label, two-sequence, and two-period crossover comparative oral bioavailability study was conducted on healthy adult subjects. It was tested BE in vivo using a comparative pharmacokinetic (PK) evaluation. Serial blood samples were collected up to 72 h following oral administration of the study drugs, plasma concentrations of empagliflozin were using liquid chromatography mass spectrometry (LC-MS-MS) method. The test and reference drug products were considered bioequivalent when the geometric means of the test (T)/reference (R) ratios and 90% confidence intervals (CIs) fall within the range of 80.00–125.00%. For PK parameters, % T/R ratios and 90% CIs were Cmax: 105.11% (100.28–110.18%), area under curve (AUC0-t): 103.25% (99.62–107.00%), and AUC0-∞ 102.71% (99.26–106.28%). Our study demonstrated in vivo BE between the two empagliflozin formulations tested in healthy subjects under fasting conditions.","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"66 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-11-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139265529","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and anti-tumor activity of piperonal substituted chalcone","authors":"Zahatu Muhammad, J. Yau, Abdulqadir U. Zezi, M. Magaji, A. Hamza","doi":"10.25259/ajpps_2023_011","DOIUrl":"https://doi.org/10.25259/ajpps_2023_011","url":null,"abstract":"\u0000\u0000Chalcones have been identified as potential antitumor agents with a novel target, the tubulin. The aim of the study was to synthesize a piperonal substituted chalcone and evaluate its in vivo antitumor activity.\u0000\u0000\u0000\u0000Piperonal substituted chalcone was synthesized using Claisen-Schmidt condensation and characterized using various spectroscopic techniques. The lethal dose (LD50) of the synthesized compound was estimated using OECD-425 guidelines in rats. Antitumor activity of the synthesized compound was evaluated on 1-methyl nitrosourea (MNU)-induced mammary tumor in female Wistar rats. Histological evaluation was used to confirm tumor induction and assess treatment with the synthesized compound. The possible mechanism of action of the synthesized compound was elucidated in silico using molecular docking.\u0000\u0000\u0000\u0000The compound was synthesized and named C2. C2 was found to be relatively safe with LD50 >2000 mg/kg orally. Moreover, C2 exhibited remarkable antitumor activity, at all the tested doses in a dose dependent manner. Histological evaluation of the MNU-induced mammary tumor rats treated with C2 displayed fewer signs of hyperplasia and small numbers of connective tissue with larger lobules when compared with the untreated group. In silico tubulin-binding interactions revealed that the kinetics of C2 binding to tubulin was like that of colchicine. Comparison of crystal structures of tubulin-C2 and tubulin-colchicine complexes showed that the binding mode of C2 to tubulin was like that of colchicine to tubulin and produced the same conformational changes on the tubulin structure as colchicine.\u0000\u0000\u0000\u0000The synthesized chalcone demonstrated remarkable antitumor activities in MNU-induced mammary tumors in rats possibly through inhibition of tubulin polymerization.\u0000","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"11 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-07-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121979784","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Mass casualty incident response: Assessment of the level of preparedness among hospital pharmacists","authors":"U. Eze, Omolara F. Adebisi, Onyinye J. Uwaezuoke, S. Saka, M. Femi-oyewo, B. Ogbonna, Samuel A Lawal, Adaeze G. Eze","doi":"10.25259/ajpps_2023_010","DOIUrl":"https://doi.org/10.25259/ajpps_2023_010","url":null,"abstract":"\u0000\u0000Mass casualty incidents (MCIs) and outcomes depend on the resources of the admitting institutions and their preparedness, respectively. We assessed the preparedness of hospital pharmacists for MCIs.\u0000\u0000\u0000\u0000A cross-sectional survey was conducted among 132 pharmacists working in hospitals in Ogun State, Southwestern Nigeria, over 1 month, using a 26-item self-administered questionnaire. Data were analyzed using the Statistical Package for the Social Sciences (SPSS, version 21). A Chi-square test was used for further analysis. P <0.05 was considered statistically significant.\u0000\u0000\u0000\u0000The response rate was 79.5% (105/132). Most respondents were 26–30 years, 31.4%, had been practicing for <10 years, 44.8%, and were female, 59.0%. Overall, 42.9% of the respondents had >400 beds, 66 (62.9%), and 48 (45.7%) had general and pharmacy-specific disaster preparedness plans, respectively. Respondents agreed that the hospital committee consensus determined medications to be stocked, 64 (60.9%) and that disaster plans were mainly for natural disasters, 73 (35.4%). Only 7 (6.6%) respondents practiced mock disaster preparedness. There was a significant association between respondents’ year of practice and response on including disaster events in the institutional plan (χ2 = 95.637, df. = 72, P = 0.033). Most respondents, 95 (90.0%), were positive (mean ± SD: 4.42 ± 0.875) about the need for analgesics during disaster events.\u0000\u0000\u0000\u0000Preparation for disaster preparedness was suboptimal based on the number of beds, pharmacy-specific disaster preparedness plan, and practice for mock disasters. This calls for immediate awareness to address these shortfalls through orientation, training, and retraining on preparedness for MCIs.\u0000","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"46 2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-07-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114743137","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Patients’ perceptions of medication counseling and education provided by pharmacists","authors":"U. Eze, Monsurat O. Fasanya, O. C. Babalola, E. Onwuchuluba, Adebola I. Ajayi, Adaeze G. Eze","doi":"10.25259/ajpps_2023_009","DOIUrl":"https://doi.org/10.25259/ajpps_2023_009","url":null,"abstract":"\u0000\u0000Pharmacists can increase patients’ knowledge and understanding of their medications and assist them to make appropriate decisions. However, clients’ perception is a rate determining step to their accepting such Pharmacists roles. In this study we evaluated clients’ perceptions on pharmacists provided medication counseling and education.\u0000\u0000\u0000\u0000A descriptive cross-sectional survey was conducted using a 27 item, three sectioned questionnaire among 405 respondents > 16years old for 10 weeks in secondary Health facility in Lagos state. Nigeria. Using Statistical Package for Social Sciences (SPSS) version 22, descriptive analysis (frequency), reliability (Cronbach alpha), correlation (spearman’s rho), association (chi-square) were conducted with P value< 0.05. Three (3) was used as a logical mid-point and a positive perception was assumed if an overall mean of above 3 was obtained.\u0000\u0000\u0000\u0000Majority of the respondents were female 267 (65.9%), 47.4% fall within the age range of 20-39 years, and the highest proportion of respondents (44%) have secondary school educational qualification. About half of the respondents strongly disagreed that pharmacists are responsible for providing information on disease condition and minor ailments 181(44.7%) and strongly agreed that pharmacists always indicate medication use in writing, 278 (68.6%), there was correlation between this and pharmacists usually re-emphasized information in writing using spearman’s rho (p=0.000). Most respondents strongly disagreed that pharmacy is only a business and of no benefit to patients 314 (78.9%) and 270 (66.7%) agreed that pharmacists should be an integral part of the health delivery system. Overall mean ± SD was 4.11 ± 0.841, while mean ± SD on patients’ knowledge of pharmacists’ roles and their opinion on usefulness of pharmacists counseling and education were 4.26 ± 0.839 and 3.95 ± 0.840 respectively. Overall value of 0.66 was obtained for reliability test using Cronbach’s’ alpha. There is significant association between the patients’ age and their perception on need to go back to physician for clarification on medication use after pharmacists counseling (P=0.000), also between respondents’ gender and their perception that counseling received from pharmacists has benefits to them. (P=0.007).\u0000\u0000\u0000\u0000Generally, respondents have positive perceptions on pharmacist provided medication counseling and education. Our study results showed that pharmacists are seen as important professionals in providing medication related information.\u0000","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"16 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"129717840","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bioequivalence study of two formulations of rivaroxaban in healthy adult subjects under fasting conditions","authors":"Evelyn Pena, Alfredo Inatti, Xenón S. Martín","doi":"10.25259/ajpps_2023_008","DOIUrl":"https://doi.org/10.25259/ajpps_2023_008","url":null,"abstract":"\u0000\u0000Oral anticoagulants exert their antithrombotic effect by disrupting the coagulation cascade. Rivaroxaban is the first oral agent to be developed that inhibits the coagulation process by binding directly to Factor Xa in a competitive manner. The aim of this study was to demonstrate the bioequivalence (BE) and safety of a generic formulation of rivaroxaban by comparing their pharmacokinetic (PK) parameters through statistical data and criteria of validation. Oral tablet formulations of 20 mg of a commercial product rivaroxaban reference (R) were tested against a generic product test (T) in 24 healthy adults under fasting condition.\u0000\u0000\u0000\u0000The study was an open label, balanced, randomized, two-treatment, two-period, two-sequence, single oral dose, and crossover study. Blood samples were collected pre-dose and at specified intervals up to 48-h post-dose to evaluate PK parameters by quantifying the concentration of rivaroxaban in plasma using a validated Liquid chromatography-mass spectrometry (LC-MS/MS) method of analysis. Statistics and confidence intervals (CIs) were calculated for BE purposes.\u0000\u0000\u0000\u0000The geometric means of the T/R ratios and 90% confidence intervals (CIs) were: Cmax 87.80% (82.74 –93.12%), AUC0-t 85.96% (81.88–90.24%), and AUC0-∞ 86.13% (82.2–90.35%). All PK parameters are within BE acceptance range of 80–125% for demonstration of average bioequivalence.\u0000\u0000\u0000\u0000The study demonstrates the BE and well tolerance of both formulations of rivaroxaban in healthy subjects under fasting conditions.\u0000","PeriodicalId":376259,"journal":{"name":"American Journal of Pharmacotherapy and Pharmaceutical Sciences","volume":"7 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"126628561","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}