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At least 19 recordsLinked to original sources
PubMed2006

Simultaneous analysis of thiamphenicol and its prodrug thiamphenicol glycinate in human plasma and urine by high performance liquid chromatography: application to pharmacokinetic study.

A simple and sensitive method for simultaneous determination of the active compound, thiamphenicol (TAP) and its prodrug, thiamphenicol glycinate (TG) in human plasma and urine is described. The procedure involved extraction of TG and TAP with ethyl acetate (plasma) or 100-fold dilution with the mobile phase (urine) followed by determination by reversed-phase high performance liquid chromatography (HPLC) with UV detection at 224 nm. Separation of the compounds was achieved on a column packed with Hypersil ODS2. The mobile phase consisted of acetonitrile-water containing 0.003 M tetrabutyl ammonium bromide and 0.056 M ammonium acetate (87:13, v/v) with a flow rate of 1.0 ml/min. The chromatograms did not contain interfering peaks due to the suitable extraction procedure and chromatographic conditions. The calibration curves of TG and TAP were linear ranging from 0.78 to 100 microg/ml in plasma and in urine. The intra-day and inter-day relative standard deviations (S.D.) were less than 10%. The recoveries of TG and TAP in plasma and urine were above 80%. TG was not stable in plasma samples and after extraction at ambient temperature or in freeze-thaw cycles, and hence the samples for injection on HPLC column should be stored in refrigerator or under ice cooling prior to analysis, and the plasma samples should not experience the freeze-thaw cycle more than one time. Unlike TAP, TG could not be detected in most urine samples. Application of this method demonstrated that it was feasible for the clinical pharmacokinetic study.

Chromatography, High Pressure Liquid↗
PubMed2001

Comparative in vitro activity of thiamphenicol-glycinate and thiamphenicol-glycinate-acetylcysteinate and other antimicrobials against respiratory pathogens.

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.

Acetylcysteine↗
PubMedDate not supplied

Comparative effect of thiamphenicol glycinate, thiamphenicol glycinate N-acetylcysteinate, amoxicillin plus clavulanic acid, ceftriaxone and clarithromycin on pulmonary clearance of Haemophilus influenzae in an animal model.

BACKGROUND: Thiamphenicol glycinate (TG) and its derivative thiamphenicol glycinate N-acetylcysteinate (TGA) could be a valid therapeutic option in the treatment of respiratory tract infections. METHODS: Time-kill curves of TG and TGA and pulmonary clearance in Haemophilus influenzae infected guinea pigs were compared with those of clarithromycin, ceftriaxone and amoxicillin plus clavulanic acid. RESULTS: The bacterial activities of the tested antibiotics were comparable. When compared to the control group, lung bacterial counts were significantly lower for the TGA group at 3 h vs. controls, while for the other treatments, significant decreases were recorded after 6 h. All drugs showed a log count of <2.0 at 24 h with respect to the control while at 48 h all groups demonstrated a log count of <2.0. CONCLUSIONS: Although the in vitro activity of the tested drugs evaluated by time-kill curves seemed comparable, some pharmacokinetic and pharmacodynamic characteristics of TGA contribute to improving the resolution of the infective process.

Acetylcysteine↗
PubMed2002

Recent clinical evidence of the efficacy and safety of 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.

Acetylcysteine↗
PubMed1999

In vitro antibacterial activity of thiamphenicol glycinate acetylcysteinate against respiratory pathogens.

After 30 years of therapeutic use, thiamphenicol glycinate acetylcysteinate (CAS 20192-91-0) is still widely employed in the treatment of upper and lower respiratory tract infections. This is due to its particular characteristic to exert at pulmonary level, either the antibacterial activity of thiamphenicol (CAS 15318-45-3) and the mucolytic activity of N-acetylcysteine (CAS 616-91-1). The aim of this study was to evaluate the present pattern of susceptibility of several clinical isolates to thiamphenicol and the interference of N-acetylcysteine on this parameter. The studies have been performed in vitro. Equimolar concentrations of N-acetylcysteine and even higher concentrations did not interfere with the antibacterial activity of thiamphenicol against Streptococcus pneumoniae, Streptococcus pyogenes and Haemophilus influenzae. The spectrum of activity of thiamphenicol was similar to that observed in the past and was superior to that of erythromycin and amoxicillin. The activity of thiamphenicol was greater than that of erythromycin against H. influenzae and streptococci and equivalent versus Branhamella catarrhalis. In comparison with amoxicillin the activity of thiamphenicol was higher against H. influenzae and B. catarrhalis and slightly lower against streptococci. The results demonstrate that thiamphenicol maintains its therapeutic value confirming the importance of thiamphenicol glycinate acetylcysteinate in the treatment of respiratory tract infections.

Acetylcysteine↗
PubMed1981

In vitro antibacterial activity of fluorinated analogs of chloramphenicol and thiamphenicol.

We evaluated the in vitro antimicrobial activity of Sch 24893, Sch 25298, and Sch 25393, three novel analogs of chloramphenicol and thiamphenicol. All of the analogs had minimal inhibitory concentrations of less than or equal to 10 micrograms/ml for 18 chloramphenicol-thiamphenicol-resistant strains of Shigella dysenteriae and 21 strains of resistant Salmonella typhi. The analogs were also more active than were chloramphenicol and thiamphenicol against chloramphenicol-resistant enteric bacteria, including six strains of Escherichia coli, seven strains of Klebsiella pneumoniae, and two strains of Enterobacter cloacae. Fifty-three strains of ampicillin-resistant Haemophilus influenzae were uniformly susceptible to chloramphenicol, thiamphenicol, and the three analogs. Sch 25298 was the most active compound tested (minimal inhibitory concentration, 0.5 microgram/ml for all strains). Four of seven chloramphenicol-thiamphenicol-resistant Haemophilus strains were susceptible to the fluorinated analogs. Of the three Haemophilus strains which were resistant to chloramphenicol, thiamphenicol, and the analogs, two contained less than 10% of the chloramphenicol acetyltransferase activity of the strains which were resistant to only chloramphenicol and thiamphenicol. We conclude that fluorinated analogs of chloramphenicol and thiamphenicol have considerable in vitro activity against a broad spectrum of chloramphenicol-thiamphenicol-resistant, gram-negative bacteria.

Acetyltransferases↗
PubMedDate not supplied

Comparative study of treatment of uncomplicated gonorrhea with thiamphenicol and cefotaxime.

Results of treatment of uncomplicated urogenital gonorrhea caused by penicillinase- and non-penicillinase-producing Neisseria gonorrhoeae were compared. In The Hague treatment consisted of thiamphenicol (2.5 g given orally), whereas the treatment in Rotterdam was cefotaxime (1 g given im). All isolates were tested for production of penicillinase and sensitivity to cefotaxime and thiamphenicol. Special attention was given to possible hematological effects of treatments with thiamphenicol. Of 55 patients treated with thiamphenicol, 87.3% were cured; however, all of 55 patients treated with cefotaxime were cured. The frequency of postgonococcal urethritis among male patients was 34.1% after thiamphenicol and 39.5% after cefotaxime treatment. The only adverse effect seen after cefotaxime treatment was a rash (2%). After treatment with thiamphenicol, 10.9% of patients had diarrhea. No significant changes in hematologic tests were seen after treatment with thiamphenicol. There was a remarkable and significant difference in sensitivity to thiamphenicol between the two treatment groups; this fact could point to the importance of specific local factors in comparison of different treatments for gonorrhea.

Adult↗
PubMed1977

[Susceptibility to Thiamphenicol and Chloramphenicol of Anaerobic Bacteria (author's transl)].

The in vitro susceptibility to thiamphenicol and chloramphenicol of 272 anaerobes, most of which were recent clinical isolated, was determined by broth dilution tests, With chloramphenicol, 133 anaerobic gram-negative non-sporing rods (48 Bacteroides fragilis, 13 B. thetaiotaomicron, 14 B. oralis, 16 Sphaerophorus varius etc.) had MIC values of 0.03 through 16 microng/ml. Very similar results (MIC, 0.06-16 microng/ml) were obtained with thiamphenicol. In concentrations of 4 microng/ml or less chloramphenicol inhibited 90.2% and thiamphenicol 78.95% of the strains. Strains with only moderate sensitivity to both antibiotics (MIC, 8 or 16 microng/ml) belonged to B. fragilis or other Bacteroides species. Members of the Fusobacterium and Sphaerophorus group were susceptible to less than or equal to 2 microng chloramphenicol/ml and less than or equal to 4 microng thiamphenicol/ml respectively. With both antibiotics, 102 strains of gram-positive non-sporing anaerobes (P. acnes, Peptostreptococcus spp., Peptococcus spp.) were susceptible to less than or equal to 8 microng/ml. Of 37 Clostridium isolates, 35 (belonging to C. perfringens, C. septicum, C. cadaveris etc.) were inhibited by concentrations of 8 microng/ml or less of chloramphenicol and thiamphenicol. Only one strain each of C. perfringens and Clostridium sp. had an MIC of 16 microng thiamphenicol/ml. Accordingly, resistance to thiamphenicol or chloramphenicol was not observed. A standardized monodisk agardiffusion test was performed on 40 Bacteroidaceae, 18 Peptococcaceae and 20 C, (P.) acnes strains. Only a poor correlation was observed between MIC and zone size for thiamphenicol and chloramphenicol. Therefore, inhibition zone diameter measurement cannot be regarded as a reliable method to detect chloramphenicol or thiamphenicol resistance in anaerobes. Thiamphenicol, which is virtually as active against anaerobes as chloramphenicol but lacks serious toxicity, may well play an important role in the therapy of various anaerobic infections.

Anti-Bacterial Agents↗
PubMed2002

A comparative kinetic study of thiamphenicol in pre-ruminant lambs and calves.

Eight healthy Holstein-Friesian calves and 8 Massese lambs of either sex (10-15-days old) were used to evaluate the pharmacokinetics of thiamphenicol after intravenous (i.v.) and oral (p.o.) administration (30 mg/kg). Plasma concentrations of thiamphenicol were determined by high-performance liquid chromatography on blood samples collected over 24h following treatment. Pharmacokinetic variables of the drug were calculated for both species and after both administration routes. After intravenous administration of thiamphenicol, a rapid distribution phase was followed by a slower elimination phase and, when thiamphenicol was administered p.o., the bioavailability was about 60% in both species. The higher volume of distribution and the longer biological elimination half-lives in pre-ruminant compared with adult animals indicate that thiamphenicol distributes widely into the extravascular compartment of pre-ruminants. Interspecies differences were observed in the kinetic behaviour of thiamphenicol with respect to peak plasma concentration (C(max)), time of peak plasma concentration (T(max)), elimination half-life (T(1/2)) and total clearance (Cl(B)). In conclusion intravenous or oral administration of 30 mg/kg of thiamphenicol provides plasma concentrations higher than minimum effective concentrations inhibiting bacterial growth (MICs) against most pathogens in pre-ruminant lambs and calves.

Administration, Oral↗
PubMed2002

In vitro activity of thiamphenicol against multiresistant Streptococcus pneumoniae, Haemophilus influenzae and Staphylococcus aureus in Italy.

Thiamphenicol is a derivative of chloramphenicol characterized by a spectrum comparable to that of the parent compound against multiresistant pathogens but showing satisfactory tolerability. The in vitro activity of thiamphenicol and of 11 comparative drugs against 397 recently isolated antibiotic-resistant and/or invasive pneumococci and 52 multiply-resistant MRSA including 2 VISA strains was determined. Bactericidal activity against Haemophilus influenzae and the post-antibiotic effect on Streptococcus pneumoniae, H. influenzae, Staphylococcus aureus and Escherichia coli were also assessed. Against invasive pneumococci, thiamphenicol and chloramphenicol were the most potent non-beta-lactam molecules together with vancomycin and rifampin. Against high-level penicillin-resistant strains phenicol activities were superior to those of cefotaxime, ceftriaxone and imipenem. Against MRSA thiamphenicol and chloramphenicol were second only to the glycopetides and also inhibited the VISA strains. Thiamphenicol showed a significant PAE (0.33 to 2.9h) on all pathogens studied and a powerful bactericidal effect against beta-lactamase-positive and -negative H. influenzae. These results indicate a good in vitro activity of thiamphenicol against difficult-to-treat multiply resistant pathogens.

Anti-Bacterial Agents↗
PubMed2004

[Role of thiamphenicol in the treatment of community-acquired lung infections].

Streptococcus pneumoniae and Haemophilus influenzae are the two main pathogens responsible for bacterial respiratory tract infections. Their antimicrobial susceptibility to antibiotics like beta-lactams, macrolides or fluoroquinolones has been largely studied, while it remains less known to other antibiotics like thiamphenicol, erythromycin, cotrimoxazole or tetracycline, often used in developing countries due to their availability. In this study, the activity of chloramphenicol and thiamphenicol on different respiratory tract pathogens was found to be equivalent. However, thiamphenicol was better in detecting resistant organisms. One hundred S. pneumoniae among which 69% had reduced susceptibility to penicillin (PRSP) and 87 H. influenzae isolates, 39.1% producing beta-lactamase, were recovered from sputum cultures in children. All H. influenzae and all penicillin susceptible S. pneumoniae strains were sensitive to thiamphenicol. Susceptibility of penicillin sensitive S. pneumoniae to erythromycin, cotrimoxazole and tetracycline was 70.9%, 83.9%, and 90.3% respectively. Susceptibility of PRSP to thiamphenicol, erythromycin, cotrimoxazole and tetracycline was 68.1%, 7.2%, 17.4% and 44.9% respectively. Thiamphenicol and chloramphenicol are still active against respiratory pathogens.

Anti-Bacterial Agents↗
PubMedDate not supplied

Salient features of thiamphenicol: review of clinical pharmacokinetics and toxicity.

This article reviews specific aspects of the pharmacokinetics and clinical toxicity of thiamphenicol. Studies on the systemic bioavailability in humans of 2.5 g of thiamphenicol given orally showed mean peak levels in plasma of 16.1-18.6 micrograms/ml after about 2 hr, and plasma concentrations of thiamphenicol of greater than 2 micrograms/ml for approximately 17-20 hr. The oral dose of 2.5 g appeared no less bioavailable than the usual 0.5-g parenterally administered dose. The distribution of thiamphenicol to selected urogenital tissues is also summarized. Clinical data on toxicity obtained during 1980-1982 confirmed that thiamphenicol does possess a hematopoietic suppressant potential of the dose-related type, which appeared to be observed only after repeated dosing. On the other hand, thiamphenicol does not appear to be associated with the dose-unrelated, delayed type of hemotoxicity known to occur after therapy with chloramphenicol.

Administration, Oral↗
PubMed1981

Placental transfer of thiamphenicol in the rat.

Measurement of thiamphenicol transfer to the rat embryo during organogenesis was performed as one step of the determination of possible drug embryotoxicity in man. Extrapolation of data on animal embryotoxicity to man will only become possible when data on the toxicokinetic properties of the substance under investigation are available for both animal and man. 1) Thiamphenicol, given between day 11.5 and 14 of rat gestation, rapidly reached the embryo; 4--6 h after single i.v. or s.c. injection, embryonic and maternal thiamphenicol levels became equal and decreased from that time on at the same rate. 2) No evidence was found for development of a placenta barrier with increasing placental function. The same dose applied at different developmental stages yielded the same embryonic drug concentrations. 3) Elimination via kidney (unchanged) or bile (glucuronide), may become rate-limiting for thiamphenicol excretion. Doses exceeding 50 mg/kg (i.v.) or approx. 100 mg/kg (s.c.) yielded thiamphenicol levels higher than those expected from linear dose-concentration relationships. 4) Drug concentrations (greater than 3--5 micrograms/g wet weight) obtained with dosing regimens (greater than 100 mg/kg/day) used for experimental induction of embryolethality in rats are equal to those necessary for inhibition of mitochondrial protein synthesis in vitro and to those necessary for treatment of bacterial infections in man.

Animals↗
PubMed1991

Determination of thiamphenicol residues in chicken muscles by column liquid chromatography.

A column liquid chromatographic (CLC) method for the determination of thiamphenicol residues in chicken muscles was developed. The drug is extracted from minced muscles with ethyl acetate and the extract is evaporated to dryness. The residue is dissolved in 10% sodium chloride solution and partitioned with n-hexane. Thiamphenicol is extracted with ethyl acetate and, after evaporation of the solvent, the residue is cleaned up by alumina column chromatography. CLC analysis is carried out on a Nucleosil C18 column with ultraviolet detection of thiamphenicol at 230 nm. The average recoveries of thiamphenicol added to muscles at 0.2 and 0.1 ppm were 92.8 and 90.0%, respectively. The detection limit was 5 ng for thiamphenicol standard, which corresponds to 0.05 ppm in muscles.

Animals↗