Stratification of cephalosporins based on physicochemical and pharmacokinetic variables using multivariate statistical tools

Abstract

Introduction: Cephalosporins, a class of beta-lactam antibiotics, are commonly used in medical practice. However, their potential advantages, based on physicochemical and pharmacokinetic variables, are often overlooked. This research, proposing strategies based on multivariate statistics to stratify different cephalosporins, is a significant step towards providing the prescribing team with more rational and effective options. The potential benefits of this research are promising, as it has the potential to significantly improve the efficacy and safety of cephalosporin therapy.

Method: Exploratory study and review of pharmacokinetic parameters of cephalosporins. Data were extracted from DrugBank go.drugbank.com, and multivariate statistical techniques such as Pearson correlation and cluster analysis were applied. This approach allowed the identification of groupings of cephalosporins with similar characteristics, thus facilitating their rational selection in clinical practice.

Results: The results reveal that cefazolin, cefotetan, cefoperazone, and ceftriaxone form the conglomerate with the most favorable properties for reaching effective concentrations at the site of action due to their high solubility, high percentage of binding to plasma proteins, and adequate residence times in the organism. Solubility, protein binding, half-life, MRT, molecular weight, volume of distribution, number of interactions, and pKa are all critical factors that influence the efficacy and safety of cephalosporin therapy.

Conclusions: It is relevant to highlight the use of multivariate statistics as a tool for drug selection and rational use. In the present study, cefazolin, cefotetan, cefoperazone, and ceftriaxone were highlighted as the best therapeutic alternatives according to the variables selected for the study.

Keywords

Principal component analysis (PCA) / Pharmacological variable / Principal component (PC) / Cefalosporins / Conglomerate

References

[1] Maxwell SR . Rational prescribing: the principles of drug selection. CME Clinic Pharmacol. 2016; 16 (5): 459- 464.

[2] Dorati CM , Buschiazzo PM , Marín GH , et al. Indicadores de prescripción racional de medicamentos: factibilidad de aplicación en instituciones de las Américas. Revista Panamericana de Salud Publica/Pan Am J Public Health. 2021; 45: e152.

[3] Turabián-Fernández JL , Pérez-Franco B . Prescripción de medicamentos en medicina de familia: ¿racional, razonable o relevante? Aten Primaria. 2005; 36 (9): 507- 509.

[4] Romero David E . Principios para la prescripción racional de los medicamentos. Medellin. 1992; 5 (3): 225- 229.

[5] Garjón Parra J . Evaluación y selección de medicamentos. Farmacéuticos de Atención Primaria. 2011; 9 (3): 89- 94.

[6] Carlos Zuluaga . Análisis Estadístico Multivariado: una Herramienta Estratégica para el Control de Procesos y Calidad en la Industria Agroalimentaria. Publicaciones e Investigación. 2011; 5 (1): 143- 157.

[7] ZTMBILLMA Rodríguez-Riera . Antibióticos Cefalosporánicos: Actualidades Y Perspectivas. La Habana. 2013; 44 (1).

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The Authors. Publishing services by Elsevier B.V. on behalf of Higher Education Press and KeAi Communications Co. Ltd.