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  1. Article ; Online: Update on Functional Inhibitors of Acid Sphingomyelinase (FIASMAs) in SARS-CoV-2 Infection

    Gwenolé Loas / Pascal Le Corre

    Pharmaceuticals, Vol 14, Iss 691, p

    2021  Volume 691

    Abstract: The SARS-CoV-2 outbreak is characterized by the need of the search for curative drugs for treatment. In this paper, we present an update of knowledge about the interest of the functional inhibitors of acid sphingomyelinase (FIASMAs) in SARS-CoV-2 ... ...

    Abstract The SARS-CoV-2 outbreak is characterized by the need of the search for curative drugs for treatment. In this paper, we present an update of knowledge about the interest of the functional inhibitors of acid sphingomyelinase (FIASMAs) in SARS-CoV-2 infection. Forty-nine FIASMAs have been suggested in the treatment of SARS-CoV-2 infection using in silico, in vitro or in vivo studies. Further studies using large-sized, randomized and double-blinded controlled clinical trials are needed to evaluate FIASMAs in SARS-CoV-2 infection as off-label therapy.
    Keywords functional inhibitors of acid sphingomyelinase (FIASMAs) ; acid sphingomyelinase ; COVID-19 ; SARS-CoV-2 ; mortality ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
    Language English
    Publishing date 2021-07-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  2. Article ; Online: Association between Functional Inhibitors of Acid Sphingomyelinase (FIASMAs) and Reduced Risk of Death in COVID-19 Patients

    Gil Darquennes / Pascal Le Corre / Olivier Le Moine / Gwenolé Loas

    Pharmaceuticals, Vol 14, Iss 3, p

    A Retrospective Cohort Study

    2021  Volume 226

    Abstract: Given the current scarcity of curative treatment of COVID-19, the search for an effective treatment modality among all available medications has become a priority. This study aimed at investigating the role of functional inhibitors of acid ... ...

    Abstract Given the current scarcity of curative treatment of COVID-19, the search for an effective treatment modality among all available medications has become a priority. This study aimed at investigating the role of functional inhibitors of acid sphingomyelinase (FIASMAs) on in-hospital COVID-19 mortality. In this retrospective cohort study, we included adult in-patients with laboratory-confirmed COVID-19 between 1 March 2020 and 31 August 2020 with definite outcomes (discharged hospital or deceased) from Erasme Hospital (Brussels, Belgium). We used univariate and multivariate logistic regression models to explore the risk factors associated with in-hospital mortality. We included 350 patients (205 males, 145 females) with a mean age of 63.24 years (SD = 17.4, range: 21–96 years). Seventy-two patients died in the hospital and 278 were discharged. The four most common comorbidities were hypertension (184, 52.6%), chronic cardiac disease (110, 31.4%), obesity (96, 27.8%) and diabetes (95, 27.1%). Ninety-three participants (26.6%) received a long-term prescription for FIASMAs. Among these, 60 (64.5%) received amlodipine. For FIASMAs status, multivariable regression showed increasing odds ratio (OR) for in-hospital deaths associated with older age (OR 1.05, 95% CI: 1.02–1.07; p = 0.00015), and higher prevalence of malignant neoplasm (OR 2.09, 95% CI: 1.03–4.22; p = 0.039). Nonsignificant decreasing OR (0.53, 95% CI: 0.27–1.04; p = 0.064) was reported for FIASMA status. For amlodipine status, multivariable regression revealed increasing OR of in-hospital deaths associated with older age (OR 1.04, 95% CI: 1.02–1.07; p = 0.0009), higher prevalence of hypertension (OR 2.78, 95% CI: 1.33–5.79; p = 0.0062) and higher prevalence of malignant neoplasm (OR 2.71, 95% CI: 1.23–5.97; p = 0.013), then secondarily decreasing OR of in-hospital death associated with long-term treatment with amlodipine (OR 0.24, 95% CI: 0.09–0.62; p = 0.0031). Chronic treatment with amlodipine could be significantly associated with low mortality of ...
    Keywords functional inhibitors of acid sphingomyelinase (FIASMAs) ; COVID-19 ; SARS-CoV-2 ; mortality ; amlodipine ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
    Language English
    Publishing date 2021-03-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  3. Article ; Online: Association of Amlodipine with the Risk of In-Hospital Death in Patients with COVID-19 and Hypertension

    Gwenolé Loas / Philippe Van de Borne / Gil Darquennes / Pascal Le Corre

    Pharmaceuticals, Vol 15, Iss 380, p

    A Reanalysis on 184 COVID-19 Patients with Hypertension

    2022  Volume 380

    Abstract: Association between calcium channel blockers (CCBs) or functional inhibitors of acid sphingomyelinase (FIASMAs) use and decreased mortality in people with COVID-19 has been reported in recent studies. Since amlodipine is both a CCB and a FIASMA, the aim ... ...

    Abstract Association between calcium channel blockers (CCBs) or functional inhibitors of acid sphingomyelinase (FIASMAs) use and decreased mortality in people with COVID-19 has been reported in recent studies. Since amlodipine is both a CCB and a FIASMA, the aim of this study was to investigate the association between chronic amlodipine use and the survival of people with hypertension infected with COVID-19. This retrospective cohort study used data extracted from the medical records of adult inpatients with hypertension and laboratory-confirmed COVID-19 between 1 March 2020 and 31 August 2020 with definite outcomes (discharged from hospital or deceased) from Erasme Hospital (Brussels, Belgium). We re-analyzed the data of the retrospective cohort study using only the 184 patients (103 males, 81 females) with a mean age of 69.54 years (SD = 14.6) with hypertension. The fifty-five participants (29.9%) receiving a chronic prescription of amlodipine were compared with the 129 patients who did not receive a chronic prescription of amlodipine. Univariate and multivariate logistic regressions were used to explore the relationships between mortality and sex, age, comorbidities, smoking, and amlodipine status. Out of the 184 participants, 132 (71.7%) survived and 52 (28.3%) died. The mortality rates were, respectively, 12.73% ( n = 7) and 34.88% ( n = 45) for the amlodipine and non-amlodipine groups. Multivariate logistic regression was significant (Chi square (5) = 29.11; p < 0.0001). Chronic kidney disease and malignant neoplasm were significant predictors as well as amlodipine status. For chronic kidney disease and malignant neoplasm, the odds ratio with 95% confidence interval (95% CI) were, respectively, 2.16 (95% CI: 1.04–4.5; p = 0.039) and 2.46 (95% CI: 1.01–6.01; p = 0.047). For amlodipine status the odds ratio was 0.29 (95% CI: 0.11–0.74; p = 0.009). The result of the present study suggests that amlodipine may be associated with reduced mortality in people with hypertension infected with COVID-19. Further research ...
    Keywords functional inhibitors of acid sphingomyelinase (FIASMAs) ; COVID-19 ; SARS-CoV-2 ; mortality ; amlodipine ; calcium channel blockers (CCBs) ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
    Subject code 610
    Language English
    Publishing date 2022-03-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article ; Online: Preparação, caracterização e avaliação in vitro de microesferas de bupivacaína em excesso enantiomérico de 50% (S75-R25) Preparación, caracterización y evaluación in vitro de microesferas de bupivacaina en exceso enantiomérico de 50% (S75-R25) Preparation, characterization and in vitro evaluation of 50% enantiomeric excess bupivacaine (S75-R25)-loaded microspheres

    Pedro Paulo Tanaka / Jean Pierre Estèbe / Richard Campos / François Chevanne / Pascal Le Corre / Sérgio Bernardo Tenório / Maria Fernanda Torres

    Revista Brasileira de Anestesiologia, Vol 58, Iss 1, Pp 15-

    2008  Volume 22

    Abstract: JUSTIFICATIVA E OBJETIVOS: As microesferas podem ser utilizadas como um sistema de liberação controlada para prolongar a ação de anestésicos locais. Esse estudo teve como objetivo a preparação, caracterização e análise da liberação in vitro de ... ...

    Abstract JUSTIFICATIVA E OBJETIVOS: As microesferas podem ser utilizadas como um sistema de liberação controlada para prolongar a ação de anestésicos locais. Esse estudo teve como objetivo a preparação, caracterização e análise da liberação in vitro de microesferas de bupivacaína em excesso enantiomérico de 50% (S75-R25). MÉTODO: As micropartículas foram preparadas utilizando o co-polímero de ácido poliláctico-co-glicólico contendo bupivacaína em excesso enantiomérico de 50% pelo método spray-dryed. RESULTADOS: A caracterização das microesferas em relação ao seu tamanho e conteúdo foram similares aos valores teóricos. A liberação in vitro apresentou um padrão bifásico. CONCLUSÕES: O processo de fabricação de microesferas contendo bupivacaína em excesso enantiomérico de 50% pelo método spray-dryed é factível de ser realizado, com resultados semelhantes aos encontrados com microesferas de bupivacaína. JUSTIFICATIVA Y OBJETIVOS: Las micro esferas pueden ser utilizadas como un sistema de liberación controlada para prolongar la acción de anestésicos locales. Este estudio tuvo como objetivo la preparación, caracterización y el análisis de la liberación in vitro de micro esferas de bupivacaina en exceso enantiomérico de 50% (S75-R25). MÉTODO: Las micro partículas fueron preparadas utilizando el copolímero de ácido poliláctico-co-glicólico con bupivacaina en exceso enantiomérico de un 50% por el método spray-dryed. RESULTADOS: La caracterización de las micro esferas con relación a su tamaño y contenido fueron similares a los valores teóricos. La liberación in vitro presentó un estándar bifásico. CONCLUSIONES: El proceso de fabricación de micro esferas con bupivacaina en exceso enantiomérico de 50% por el método spray-dryed se puede realizar con resultados semejantes a los encontrados con micro esferas de bupivacaina. BACKGROUND AND OBJECTIVES: Microspheres can be used as a controlled delivery system to prolong the duration of action of local anesthetics. The objective of this study was the preparation, characterization and analysis of the in vitro release of 50% enantiomeric excess bupivacaine (S75-R25)-loaded microspheres. METHODS: Microspheres were prepared using the copolymer of polylactide-co-glycolic acid by the spray-dryed method. RESULTS: Characterization of microspheres regarding their size and content were similar to the theoretical values. The in vitro release demonstrated a biphasic pattern. CONCLUSIONS: Manufacturing of 50% enantiomeric excess bupivacaine-loaded microspheres by the spray-dryed method with results similar to bupivacaine-loaded microspheres can be done.
    Keywords ANESTÉSICOS ; Local ; ANESTHETICS ; Surgery ; RD1-811 ; Medicine ; R ; DOAJ:Surgery ; DOAJ:Medicine (General) ; DOAJ:Health Sciences
    Language English
    Publishing date 2008-02-01T00:00:00Z
    Publisher Sociedade Brasileira de Anestesiologia
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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