Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

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.
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PMID:Telithromycin: a new ketolide antimicrobial for treatment of respiratory tract infections. 1117 47

Telithromycin is the first member of a new family of the macrolide-lincosamide-streptogramin-B (MLS(B)) class of antimicrobials, the ketolides. It has a good spectrum of activity against respiratory pathogens, including penicillin- and erythromycin-resistant pneumococci, as well as intracellular and atypical bacteria. Furthermore, it has a low potential to select for resistance or induce cross-resistance among other MLS(B) antimicrobials. At the recommended dosage of 800 mg orally once daily, telithromycin reaches maximal plasma concentrations of about 2 mg/L. It penetrates rapidly into bronchopulmonary, tonsillar, sinus and middle ear tissues and/or fluids and achieves high concentrations at sites of infection. It also concentrates within polymorphonuclear neutrophils. In clinical trials in patients with community-acquired pneumonia (CAP), acute exacerbations of chronic bronchitis (AECB) or pharyngitis/tonsillitis caused by group A beta-haemolytic streptococci, telithromycin 800 mg once daily achieved clinical cure rates of 86 to 95%. In acute maxillary sinusitis (AMS), cure rates were 73 to 91%. A 7- to 10-day regimen of telithromycin was as effective as a 10-day course of amoxicillin 1000 mg 3 times daily, clarithromycin 500 mg twice daily or a 7- to 10-day course of trovafloxacin 200 mg once daily for treating CAP. A 5-day regimen of telithromycin was as effective as a 10-day regimen of cefuroxime axetil 500 mg twice daily or amoxicillin/clavulanic acid 500/125 mg 3 times daily in AECB. A 5-day regimen of telithromycin was as effective as a 10-day regimen of clarithromycin 250 mg twice daily or phenoxymethylpenicillin 500 mg 3 times daily in pharyngitis/tonsillitis, or a 10-day regimen of amoxicillin/clavulanic acid 500/125 mg 3 times daily in patients with AMS. Telithromycin was well tolerated across all patient populations. Adverse events associated with telithromycin were generally mild to moderate in intensity and seldom led to treatment discontinuation. The most frequent adverse events were diarrhoea (13.3%) and nausea (8.1%). Other adverse events included dizziness and vomiting.
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PMID:Telithromycin. 1139 13

Telithromycin, the first ketolide antibacterial, was developed for the treatment of community-acquired respiratory tract infections. This multicenter, open-label, uncontrolled study assessed the efficacy and safety of 800 mg, once-daily telithromycin in adults with community-acquired pneumonia (CAP). Based on bacteriologic eradication rates, telithromycin was shown to be effective for the treatment of CAP. Telithromycin was generally well tolerated, with gastro-intestinal adverse events observed most frequently (diarrhea 4/218 [1.8%], nausea 4/218 [1.8%], vomiting 5/218 [2.3%]). These results were consistent with those observed in randomized, active-controlled studies.
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PMID:Efficacy and safety of telithromycin in community-acquired pneumonia. 1248 5

A randomised, double-blind study of adults with community-acquired pneumonia (CAP) resulted in clinical cure rates of 90.0% for telithromycin and 94.2% for trovafloxacin. Bacteriological eradication rates were also comparable for both treatments. All high-risk patients (i.e. > or = 65 years old [n=25], Pneumonia Severity Index score > or = 111 [n=16], pneumococcal bacteraemia [n=4]) were clinically cured. In infections caused by Mycoplasma pneumoniae and Chlamydophila (Chlamydia) pneumoniae, clinical cure rates were 93.3% (14/15) for telithromycin and 100% (16/16) for trovafloxacin. Possibly drug-related, treatment-emergent adverse events (TEAEs) were considered mild and occurred in 47.2% of telithromycin and 33.0% of trovafloxacin patients. The most frequently reported, possibly drug-related, TEAEs were diarrhoea and nausea for telithromycin and diarrhoea and headache for trovafloxacin. Serious TEAEs occurred in 1.9% of telithromycin and 1.8% of trovafloxacin subjects and were considered not drug related. No deaths occurred during the study. Telithromycin and trovafloxacin were safe and comparable in efficacy in these patients with CAP.
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PMID:Efficacy and tolerability of once-daily oral therapy with telithromycin compared with trovafloxacin for the treatment of community-acquired pneumonia in adults. 1284 41

Telithromycin, the first member of the ketolide antibacterials, has good activity against community-acquired respiratory pathogens, including multiple-drug-resistant strains of Streptococcus pneumoniae. Telithromycin 800 mg once daily has been US FDA approved for the treatment of acute bacterial sinusitis (ABS; treatment duration 5 days), acute bacterial exacerbations of chronic bronchitis (AECB; 5 days) and mild-to-moderate community-acquired pneumonia (CAP; 7-10 days). In patients with CAP, telithromycin was as effective as amoxicillin 1000 mg three times daily for 10 days, clarithromycin 500 mg twice daily for 10 days or trovafloxacin 200 mg once daily for 7-10 days. In patients with AECB, telithromycin was as effective as a 10-day regimen of amoxicillin/clavulanic acid 500/125 mg three times daily, cefuroxime axetil 500 mg twice daily or clarithromycin 500 mg twice daily. In patients with ABS, telithromycin was as effective as a 10-day course of amoxicillin/clavulanic acid 500/125 mg three times daily or cefuroxime axetil 250 mg twice daily. Telithromycin was generally well tolerated and most adverse events were of mild-to-moderate severity and transitory. The most common adverse events with telithromycin were diarrhoea and nausea (10.8% and 7.9% of 2702 patients in clinical trials); these events occurred in 8.6% and 4.6% of 2139 comparator-treated patients.
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PMID:Telithromycin. 1525 29

Telithromycin (Ketek), Aventis Pharma), a ketolide, belongs to a new class of antibiotics that was developed for the treatment of upper and lower respiratory tract infections. The prevalence of penicillin and macrolide resistance among respiratory pathogens is increasing in the USA. Telithromycin is highly active against beta-lactam, macrolide and fluoroquinolone reduced-susceptibility pathogens. Its efficacy has been shown to be equal or superior to comparator agents in numerous studies. It has a broad in vitro spectrum versus usual respiratory pathogens and oral once-daily dosing that increases patient compliance. Telithromycin penetrates rapidly into neutrophils in bronchopulmonary tissue, with peak levels obtained in 1 to 2 h. Results of clinical trials show clinical-esponse rates similar to comparator agents. The most frequent adverse events involve the gastrointestinal system, with mild to moderate diarrhea and nausea. A low rate of discontinuation was observed in the studies. Telithromycin is an effective first-line treatment for mild to moderate respiratory infections in adults.
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PMID:Telithromycin. 1548 32