thiamphenicol-glycinate-acetylcysteinate and thiamphenicol-glycinate

Thiamphenicol is a broad-spectrum antimicrobial agent active against penicillin-resistant Streptococcus pneumoniae, Staphylococcus aureus VISA strains, most methicillin-resistant isolates and atypical pathogens such as Mycoplasma pneumoniae and Chlamydia pneumoniae). Thiamphenicol is present as glycinate hydrochloride (TG) and glycinate acetylcysteinate (TGA) esters in the parenteral and aerosol dosage form. This multicenter, double-blind, randomized clinical trial aimed to evaluate the efficacy and tolerability of aerosol administration of TGA, compared to TG, in the treatment of acute and/or exacerbated infections of the respiratory tract. Results showed that both treatments ameliorated the symptoms (frequency and severity of cough, difficulty in expectoration) associated with the evaluated pathologies, i.e. tracheobronchitis, acute and exacerbated chronic bronchitis. The investigators rated both treatments Good or Very Good in 90% of patients at the end of treatment, with "Very Good" for patients treated with TGA (37%) compared to 28% of patients treated with TG. Both treatments were well tolerated with fewer than 5% of patients experiencing an adverse event.

Topics: Acetylcysteine; Administration, Inhalation; Anti-Bacterial Agents; Bronchitis; Cough; Double-Blind Method; Drug Combinations; Female; Humans; Italy; Male; Middle Aged; Severity of Illness Index; Thiamphenicol; Treatment Outcome

Thiamphenicol-glycinate-acetylcysteinate (TGA; CAS 20192-91-0) is widely used for the treatment of infections of varied aetiology. The aim of this study was to compare the antibacterial activity of thiamphenicol-glycinate (TG; CAS 15318-45-3), TGA, amoxicillin (CAS 61336-70-7) plus clavulanic acid (CAS 58001-44-8), azithromycin (CAS 83905-01-5) and ceftriaxone (CAS 104376-79-6). Minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined against Staphylococcus aureus, Klebsiella pneumoniae, Streptococcus pyogenes, Streptococcus pneumoniae, Moraxella catarrhalis and Haemophilus influenzae according to the National Committee for Clinical Laboratory Standards (NCCLS) methods. The effects of changes in assay conditions were also examined. The activity of TG and TGA was similar to that of amoxicillin plus clavulanic acid, with the exception of methicillin resistant S. aureus. Azithromycin and ceftriaxone were characterised by a limited activity against gram-positive cocci and methicillin resistant and cefinase-positive S. aureus, respectively. TG and TGA are characterized by a wide spectrum of activity, comparable to that of recent commercialized antibiotics for treatment of respiratory tract infections.

Topics: Acetylcysteine; Bacteria; Cations, Divalent; Culture Media; Drug Combinations; Hydrogen-Ion Concentration; Microbial Sensitivity Tests; Respiratory Tract Diseases; Thiamphenicol

In vitro thiamphenicol antibacterial activity in the presence of N-acetylcysteine as sodium salt proved to be enhanced when compared with that of the antibacterial alone against both Gram-positive and Gram-negative bacterial strains. The in vitro results were confirmed in vivo in the guinea-pig, where the sera from animals previously treated by i.m. route with thiamphenicol glycinate acetylcysteinate, showed a higher antibacterial activity than sera from animals treated with thiamphenicol glycinate hydrochloride. The observation, even after allowing for differences between species might be of some interest in view of use of this chemotherapeutic agent in the treatment of respiratory infections.

Topics: Acetylcysteine; Animals; Bacteria; Drug Combinations; Escherichia coli; Female; Guinea Pigs; Klebsiella pneumoniae; Pseudomonas aeruginosa; Staphylococcus aureus; Thiamphenicol