Yassin H M, Dever L L
VA New Jersey Health Care System, East Orange, NJ and UMDNJ, New Jersey Medical School, Newark, NJ, USA.
Expert Opin Investig Drugs. 2001 Feb;10(2):353-67. doi: 10.1517/13543784.10.2.353.
Telithromycin is a new ketolide antimicrobial, specifically developed for the treatment of community-acquired respiratory tract infections. It has a wide spectrum of antibacterial activity against common respiratory pathogens including Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis and Streptococcus pyogenes. It also has activity against atypical pathogens, such as Chlamydia pneumoniae, Legionella pneumophila and Mycoplasma pneumoniae. Telithromycin maintains activity against beta-lactam and macrolide-resistant respiratory tract pathogens and does not appear to induce cross-resistance to other members of the macrolide-lincosamide-streptogramin (MLS) group of antimicrobials. It demonstrates bactericidal activity against S. pneumoniae and H. influenzae and has a prolonged concentration-dependent post-antibiotic effect (PAE) in vitro. The drug has favourable pharmacokinetics following oral administration. It is well absorbed, achieves good plasma levels and is highly concentrated in pulmonary tissues and white blood cells. In clinical trials, telithromycin given orally at a dose of 800 mg once daily for 5 - 10 days was as effective as comparator antimicrobials for the treatment of adults with community-acquired pneumonia, acute exacerbations of chronic bronchitis, acute maxillary sinusitis and group A-beta-haemolytic streptococcal pharyngitis or tonsillitis. The adverse events and safety profile were similar to comparator antimicrobials. The most common adverse events were diarrhoea, nausea, headache and dizziness. Telithromycin should provide an effective, convenient and well-tolerated once-daily oral therapy for treatment of respiratory infections.
泰利霉素是一种新型酮内酯类抗菌药物,专门用于治疗社区获得性呼吸道感染。它对常见呼吸道病原体具有广泛的抗菌活性,包括肺炎链球菌、流感嗜血杆菌、卡他莫拉菌和化脓性链球菌。它对非典型病原体也有活性,如肺炎衣原体、嗜肺军团菌和肺炎支原体。泰利霉素对β-内酰胺类和大环内酯类耐药的呼吸道病原体仍保持活性,且似乎不会诱导对大环内酯-林可酰胺-链阳菌素(MLS)组其他抗菌药物的交叉耐药性。它对肺炎链球菌和流感嗜血杆菌具有杀菌活性,并且在体外具有延长的浓度依赖性抗生素后效应(PAE)。该药物口服后具有良好的药代动力学特性。它吸收良好,能达到良好的血浆水平,并在肺组织和白细胞中高度浓缩。在临床试验中,口服泰利霉素,剂量为800mg,每日一次,持续5至10天,对于治疗患有社区获得性肺炎、慢性支气管炎急性加重、急性上颌窦炎以及A组β溶血性链球菌咽炎或扁桃体炎的成人,其疗效与对照抗菌药物相当。不良事件和安全性与对照抗菌药物相似。最常见的不良事件是腹泻、恶心、头痛和头晕。泰利霉素应为治疗呼吸道感染提供一种有效、方便且耐受性良好的每日一次口服疗法。