Tigecycline: a new glycylcycline antimicrobial

Townsend, Mary L.; Pound, M. W.; Drew, Richard H.

doi:10.1111/j.1742-1241.2006.01188.x

Cited by 41 publications

(25 citation statements)

References 79 publications

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“…The drug demonstrated a limited activity, similar to other tetracyclines, only against P. aeruginosa. Other authors reported such a restricted activity also against Proteus mirabilis [8,13,26,[41][42][43] : the AcrAB transport system appears to be associated with the intrinsically reduced susceptibility to tigecycline in this microorganism [10] .…”

Section: Discussionmentioning

confidence: 99%

Tigecycline in vitro Activity against Gram-Negative and Gram-Positive Pathogens Collected in Italy

2007

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Background: In this study (part of the global TEST program), the in vitro activity of tigecycline, a member of a new class of antimicrobial agents, the glycylcyclines, against clinical isolates collected in Italy was evaluated. Methods: A total of 200 clinical isolates were collected and identified in our institution during 2005. Minimum inhibitory concentrations (MICs) of the antimicrobial agents were determined by the broth microdilution method recommended by the CLSI in 2005. Results: Globally, 135 Gram-negative and 65 Gram-positive pathogens were evaluated. Tigecycline demonstrated excellent inhibitory activity against Acinetobacter spp., Haemophilus influenzae, Escherichia coli, Enterococcus spp., Staphylococcus aureus, Streptococcus agalactiae and Streptococcus pneumoniae with MIC₉₀ ≤1 mg/l. Conclusion: Tigecycline exhibited potent in vitro antibacterial activity (comparable to or greater than most commonly employed antimicrobials) against both Gram-positive and Gram-negative clinical pathogens. These data suggest that tigecycline, with an expanded broad-spectrum antimicrobial activity, may be an effective empiric therapeutic option for the treatment of serious infections caused by clinically relevant pathogens.

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Section: Discussionmentioning

confidence: 99%

Tigecycline in vitro Activity against Gram-Negative and Gram-Positive Pathogens Collected in Italy

2007

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“…In patients with severe hepatic impairment (Child-Pugh class C) the systemic clearance of tigecycline is decreased by approximately 55%, and the elimination t 1/2 is prolonged by approximately 43% compared to healthy subjects [33]. In patients with moderate hepatic impairment (Child-Pugh class B) the systemic clearance of tigecycline decreases by nearly 25% compared to healthy subjects [34].…”

Section: Non-enzymatic Degradation Into Epimermentioning

confidence: 98%

Clinical Significance of the Pharmacokinetic and Pharmacodynamic Characteristics of Tigecycline

Falagas¹,

Karageorgopoulos²,

Dimοpoulos

2009

CDM

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Tigecycline is a novel antibacterial agent with a wide spectrum of antimicrobial activity that includes pathogens with clinically significant resistance patterns. The clinical effectiveness of tigecycline has been evaluated in several non-inferiority, phase III, randomized, double-blind, controlled clinical trials regarding, mainly, complicated skin and skin structure infections and complicated intra-abdominal infections. Clinical data regarding the effectiveness of tigecycline against infections caused by multidrug-resistant pathogens that commonly affect severely ill patients as well as community acquired pneumonia are favorable, yet limited. The consideration of the pharmacokinetic and pharmacodynamic properties of tigecycline may aid in further understanding the therapeutic role of this agent. Respectively, the utility of tigecycline in the treatment of severe infections involving the bloodstream has not been substantiated, particularly regarding pathogens with borderline susceptibility. Moreover, the fact that a relatively small proportion of the administered tigecycline dose is excreted unchanged in the urine may compromise the effectiveness of this agent in serious urinary tract infections. Increasing the dose of tigecycline to maximize effectiveness against severe infections appears as an appealing therapeutic option, considering the linear pharmacokinetics exhibited by this agent. However, gastrointestinal toxicity (nausea and vomiting) is usually dose-limiting. Further research is recommended on therapeutic strategies to optimize the effectiveness and safety of tigecycline therapy in severely ill patients.

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“…2,4 Uma única restrição a estas drogas refere-se às mulheres grávidas e crianças em fase de crescimento, uma vez que tetraciclinas são depositadas nos ossos e dentes durante a calcificação, o que pode levar a um descoloramento dos dentes e a uma inibição do crescimento ósseo em crianças. 55 Outros efeitos menos comuns são fotossensibilidade, que é caracterizada pelo aparecimento de manchas tipo queimadura de sol na pele, urticária, dor de cabeça, dor abdominal, hipertensão, febre, leucopenia leve, anemia, trombocitopenia. 4 Tetraciclinas são fortes agentes quelantes e as suas propriedades antibacterianas e farmacocinéticas são afetadas pela coordenação de íons metálicos presentes no meio biológico.…”

Section: Efeitos Adversos E Interação Com Outras Drogasunclassified

Tetraciclinas e glicilciclinas: uma visão geral

Pereira-Maia¹,

Silva²,

Almeida³

et al. 2010

Quím. Nova

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Recebido em 18/5/09; aceito em 4/9/09; publicado na web em 22/2/10 TETRACYCLINES AND GLYCYLCYCLINES: AN OVERVIEW. Tetracyclines exhibits activity to a broad range of Gram-negative and Gram-positive bacteria and this fact allied to the low toxicity, low cost, and the advantage of administration by oral route led to their indiscriminate use, which caused the appearance of bacterial resistance to these agents, wich has restricted its clinical utility, though new applications have emerged. On the other hand, the glycylcyclines, semi-synthetic products are similar to tetracyclines, which are active against many bacteria resistant to tetracycline and other classes of antibiotics. The purpose of this paper is to give an overview of this important class of antibiotics focusing on its coordination chemistry and possible applications.Keywords: tetracyclines; glycylcyclines; antibacterial activity. INTRODUÇÃOA descoberta do primeiro membro da família das tetraciclinas em 1945 por Benjamin Duggar, a clortetraciclina, que é um produto da fermentação natural de uma bactéria do solo, Streptomyces aureofaciens, provocou uma corrida na pesquisa e obtenção de novas tetraciclinas com grande sucesso. Assim, de 1950 a 1970, vários membros da família das tetraciclinas haviam sido desenvolvidos, uns como produtos naturais, outros como produtos semissintéticos e, neste mesmo período, as tetraciclinas figuraram entre os antibióticos mais usados nos Estados Unidos. 1-3Após a descoberta da minociclina em 1972, um longo tempo se passou sem que novas tetraciclinas fossem descobertas até que, no ano de 1993, as glicilciclinas, foram sintetizadas. As glicilciclinas são produtos semissintéticos análogos às tetraciclinas, que são ativos contra inúmeras bactérias resistentes às tetraciclinas e a outras classes de antibióticos. 4 Em 2005, o composto denominado tigeciclina (tygacil TM ), uma glicilciclina derivada da minociclina, que possui um grupo glicilamido na posição C9, foi aprovado para uso clínico pela FDA e, recentemente, o composto denominado PTK-0796, um derivado semissintético da minociclina, tem chamado a atenção, pois entrou em fase I de testes clínicos. 5,6 Tetraciclinas possuem diversas propriedades favoráveis, tais como amplo espectro de ação, baixa toxicidade, baixo custo, e podem ser, na maioria dos casos, administradas por via oral.1,2 Devido a essas propriedades, tetraciclinas em geral têm sido utilizadas indiscriminadamente, o que tem levado ao aparecimento de resistência em um grupo variado de bactérias, principalmente às tetraciclinas de primeira geração, descobertas no período compreendido entre 1950 e 1970, e isto provocou e tem provocado restrições na utilidade clínica destes compostos.3 No entanto, tetraciclinas ainda são bastante úteis na clínica médica e têm sido usadas no tratamento de diversos tipos de infecção.7-9 Além do uso em humanos, tetraciclinas são utilizadas na terapia animal para tratar infecções e promover o crescimento.7 Além disso, tigeciclina e minociclina têm sido indicadas no tratamento de MRSA (Stap...

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Tigecycline: a new glycylcycline antimicrobial

Cited by 41 publications

References 79 publications

Tigecycline in vitro Activity against Gram-Negative and Gram-Positive Pathogens Collected in Italy

Tigecycline in vitro Activity against Gram-Negative and Gram-Positive Pathogens Collected in Italy

Clinical Significance of the Pharmacokinetic and Pharmacodynamic Characteristics of Tigecycline

Tetraciclinas e glicilciclinas: uma visão geral

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