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Farmacocinética, farmacodinâmica e monitorização sérica de β-lactâmicos
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Os β-lactâmicos constituem a família mais numerosa de antibióticos e a mais utilizada em antibioterapia na prática clínica. Todos os compostos deste grupo (penicilinas, cefalosporinas, carbapenemos, monobactamos e inibidores das β-lactamases) são caracterizados por possuírem um anel β-lactâmico com uma cadeia lateral variada, que explica as características e espetros de ação de cada antibiótico. Têm ação bactericida lenta, com atividade dependente do tempo. Em geral têm boa distribuição e escassa toxicidade. No entanto, há mais de três décadas que não há entrada no mercado de nenhum novo β-lactâmico. Estes antibióticos satisfazem algumas das condições referenciadas para a monitorização terapêutica de fármacos (TDM), nomeadamente a relação direta entre a concentração e o efeito farmacológico e a elevada variabilidade farmacocinética. Esta abordagem permite, assim, uma otimização da terapêutica através do ajuste da dose dos fármacos para um valor terapêutico ótimo, tendo por base as características do doente em particular. A monitorização correta dos fármacos pode ser uma mais valia tanto em termos de segurança como de efetividade, não só reduzindo a ocorrência de efeitos adversos como contribuindo para atingir as concentrações desejadas, nos tempos desejados, aumentando o sucesso do tratamento e diminuindo a ocorrência de resistências ao fármaco e a necessidade de substituição por outro antibiótico. Apesar destas vantagens, esta metodologia não está amplamente implementada na prática clínica. Verificam-se algumas dificuldades para pôr em prática esta abordagem, como o estabelecimento de margens terapêuticas e a escassez de dados publicados de ensaios clínicos bem delineados. No entanto, há alguns fármacos β-lactâmicos para os quais estas limitações já estão ultrapassadas. Esta monografia faz uma compilação da literatura acerca da monitorização sérica de β-lactâmicos, suas características físicas e químicas, farmacológicas, farmacocinéticas e farmacodinâmicas.
The β-lactams are the most numerous family of antibiotics and the most used in antibiotic therapy in clinical practice. All the compounds in this group (penicillins, cephalosporins, carbapenems, monobactams and β-lactamases inhibitors) are characterized by having a β-lactam ring with a varied side chain, which explains the characteristics and action spectrum of each antibiotic. They have a slow bactericidal action, with time-dependent activity. In general they have good distribution and low toxicity. However, no new β-lactam has entered the market for more than three decades. These antibiotics satisfy some of the conditions referenced for the therapeutic drug monitoring (TDM), namely the direct relationship between concentration and pharmacological effect and the high pharmacokinetic variability. This approach allows therapy optimization by adjusting the dose of drugs to an optimal therapeutic value, based on the characteristics of the patient. The correct monitoring of drugs can be an advantage in terms of safety and effectiveness, not only reducing the occurrence of adverse effects but contributing to achieve the desired concentrations at the desired times, increasing the success of the treatment and decreasing the occurrence of resistance to drug and the need for replacement by another antibiotic. However, it is not widely implemented in daily clinical practice. There are some difficulties in implementing this approach, such as establishment of therapeutic margins and the lack of published data from well-designed clinical trials. However, there are some β-lactam drugs for which these limitations are overcome. This monograph compiles the literature on the serum monitoring of β-lactams, their pharmacological, pharmacokinetic, pharmacodynamic, physical and chemical characteristics.
The β-lactams are the most numerous family of antibiotics and the most used in antibiotic therapy in clinical practice. All the compounds in this group (penicillins, cephalosporins, carbapenems, monobactams and β-lactamases inhibitors) are characterized by having a β-lactam ring with a varied side chain, which explains the characteristics and action spectrum of each antibiotic. They have a slow bactericidal action, with time-dependent activity. In general they have good distribution and low toxicity. However, no new β-lactam has entered the market for more than three decades. These antibiotics satisfy some of the conditions referenced for the therapeutic drug monitoring (TDM), namely the direct relationship between concentration and pharmacological effect and the high pharmacokinetic variability. This approach allows therapy optimization by adjusting the dose of drugs to an optimal therapeutic value, based on the characteristics of the patient. The correct monitoring of drugs can be an advantage in terms of safety and effectiveness, not only reducing the occurrence of adverse effects but contributing to achieve the desired concentrations at the desired times, increasing the success of the treatment and decreasing the occurrence of resistance to drug and the need for replacement by another antibiotic. However, it is not widely implemented in daily clinical practice. There are some difficulties in implementing this approach, such as establishment of therapeutic margins and the lack of published data from well-designed clinical trials. However, there are some β-lactam drugs for which these limitations are overcome. This monograph compiles the literature on the serum monitoring of β-lactams, their pharmacological, pharmacokinetic, pharmacodynamic, physical and chemical characteristics.
Descrição
Trabalho Final de Mestrado Integrado, Ciências Farmacêuticas, 2020, Universidade de Lisboa, Faculdade de Farmácia.
Palavras-chave
Farmacocinética Farmacodinâmica ß-lactâmicos TDM Monitorização de fármacos Mestrado integrado - 2020