Novel pharmaceutical molecules against emerging resistant gram-positive cocci

INTRODUCTION: methicillin- and also vancomycin (glycopeptide)-resistant Gram-positive organisms have emerged as an increasingly problematic cause of hospital-acquired infections, also spreading into the community. Vancomycin (glycopeptide) resistance has emerged primarily among Enterococci, but the MIC values of vancomycin for the entire Staphylococcus species are also increasing worldwide. MATERIAL AND METHODS: the aim of our review is to evaluate the efficacy and tolerability of newer antibiotics with activity against methicillin-resistant and glycopeptide-resistant Gram-positive cocci, on the ground of our experience at a tertiary care metropolitan Hospital, and the most recent literature evidences in this field. RESULTS: Quinupristin-dalfopristin, linezolid, daptomycin, and tigecycline show an excellent in vitro activity, comparable to the activity of vancomycin and teicoplanin for methicillin-resistant staphylococci, and superior to the one that vancomycin for vancomycin-resistant isolates. Dalbavancin, televancin, and oritavancin are new lipoglycopeptide agents with excellent activity against Gram-positive cocci, and have superior pharmacodynamics properties compared to vancomycin. We review the bacterial spectrum, clinical indications and practical use, pharmacologic properties, and expected adverse events and contraindications associated with each of these novel antimicrobial agents, compared with the present standard of care. DISCUSSION: linezolid activity is substantially comparable to that of vancomycin in patients with methicillin-resistant Staphylococcus aureus (MRSA) pneumonia, although its penetration into the respiratory tract is exceptionally elevated. Tigecycline has activity against both Enterococus species and MRSA; it is also active against a broad spectrum of Enterobacteriaceae and anaerobes, which allows for use intraabdominal, diabetic foot and surgical infections. Daptomycin has a rapid bactericidal activity for ...

A Randomized, Phase IV, Comparison Study on the Efficacy and Safety of Tapocin(R) and Targocid(R) in Treating Infections Caused by Multi-Resistant Gram Positive Cocci / 감염과화학요법

BACKGROUND: Tapocin(R) is a recently produced Teicoplanin in Korea. To evaluate its clinical usefulness, we compared clinical outcome and safety of Tapocin(R) with those of Teicoplanin (Targocid(R)) against infection caused by multi-drug resistant gram positive cocci. MATERIALS AND METHODS: Twenty-four adult patients infected with multi-drug resistant gram positive cocci were enrolled and randomized into each treatment arm after informed consents were obtained. All patients were given one of the test articles for 7 to 14 days intravenously. Clinical outcome and safety were compared between the two groups. Statistical analysis was done by Chi-square test, Student's t-test, and Fisher's exact test. RESULTS: Twenty out of 24 enrolled patients could be evaluated for clinical efficacy and safety (10 patients for each treatment arm). The baseline characteristics were not significantly different between the two groups in terms of mean age, sex ratio, underlying diseases, site of infections, and causative microorganisms. MRSA was the most common organism: 66.67% in Tarpocin(R) and 91.67% in Targocid(R) groups. Total doses of Targocid(R) and Tapocin(R) administered were 24 and 23 vials, respectively. Fever resolved in 90% of treated subjects and there were no significant differences between the two groups. Bacteriological response shows that the causative microorganisms were eradicated except for one MRSA isolate from each group. Drug fever, as a side effect, was reported from one subject in each group. CONCLUSION: Efficacy and safety of Tapocin(R) is comparable to those of Targocid(R) for the treatment of infections with multi-drug resistant gram-positive cocci.

A Randomized, Phase IV, Comparison Study on the Efficacy and Safety of Tapocin(R) and Targocid(R) in Treating Infections Caused by Multi-Resistant Gram Positive Cocci / 감염과화학요법

BACKGROUND: Tapocin(R) is a recently produced Teicoplanin in Korea. To evaluate its clinical usefulness, we compared clinical outcome and safety of Tapocin(R) with those of Teicoplanin (Targocid(R)) against infection caused by multi-drug resistant gram positive cocci. MATERIALS AND METHODS: Twenty-four adult patients infected with multi-drug resistant gram positive cocci were enrolled and randomized into each treatment arm after informed consents were obtained. All patients were given one of the test articles for 7 to 14 days intravenously. Clinical outcome and safety were compared between the two groups. Statistical analysis was done by Chi-square test, Student's t-test, and Fisher's exact test. RESULTS: Twenty out of 24 enrolled patients could be evaluated for clinical efficacy and safety (10 patients for each treatment arm). The baseline characteristics were not significantly different between the two groups in terms of mean age, sex ratio, underlying diseases, site of infections, and causative microorganisms. MRSA was the most common organism: 66.67% in Tarpocin(R) and 91.67% in Targocid(R) groups. Total doses of Targocid(R) and Tapocin(R) administered were 24 and 23 vials, respectively. Fever resolved in 90% of treated subjects and there were no significant differences between the two groups. Bacteriological response shows that the causative microorganisms were eradicated except for one MRSA isolate from each group. Drug fever, as a side effect, was reported from one subject in each group. CONCLUSION: Efficacy and safety of Tapocin(R) is comparable to those of Targocid(R) for the treatment of infections with multi-drug resistant gram-positive cocci.