Drugs online research references
Drug Metab Dispos. 1982 Mar-Apr;10(2):142-6.
Metabolism of minocycline in humans.
Nelis HJ, De Leenheer AP.
Metabolites of tetracycline antibiotics have not previously been isolated from human excreta. It is now demonstrated that minocycline is the first tetracycline to be metabolized in man. A two-step liquid chromatographic procedure was used to isolate three metabolites from human urine. The principal metabolite was tentatively identified as 9-hydroxyminocycline by mass spectral and spectrophotometric analysis and comparison with a synthetic compound. The latter was prepared by incubation of minocycline in a modified Udenfriend system, simulating an enzymatic oxygenase. Two other major metabolites are probably mono-N-demethylated derivatives. Substantial amounts of 4-epiminocycline, which probably resulted from minocycline epimerization rather than biotransformation, were also present.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6124399&dopt=Abstract
ogh.on.ca
Most Burkholderia cepacia strains are resistant to many, or all, of the antibacterial agents commonly used in cystic fibrosis (CF), and selection of appropriate antibiotics for treatment of pulmonary exacerbations is therefore difficult. We developed a technique for rapid in vitro testing of multiple antibiotic combinations for B. cepacia isolates. For each of 119 multi-drug-resistant isolates of B. cepacia, our multiple combination bactericidal test (MCBT) studied the bactericidal activity of 10 to 15 antimicrobial agents using 225 +/- 97 single, double, and triple antibiotic combinations. Of the 119 isolates, 50% were resistant to all single antibiotics tested, 8% were resistant to all two-drug antibiotic combinations, but all were inhibited by at least one bactericidal triple-drug combination. When used alone, meropenem, ceftazidime and high-dose tobramycin (200 microg/ml) were bactericidal against only 47, 15, and 14% of in vitro isolates, respectively. Using a double antibiotic combination improved bactericidal activity; meropenem-minocycline, meropenem-amikacin, and meropenem-ceftazidime combinations were bactericidal against 76, 73, and 73% of isolates, respectively. However, 47% of isolates demonstrated antagonism (growth of an organism when a second antibiotic was added to a bactericidal single antibiotic). Triple antibiotic combinations that contained tobramycin, meropenem, and an additional antibiotic were most effective, and were bactericidal against 81 to 93% of isolates. We conclude that triple-antibiotic combinations are more likely than double and single antibiotic combinations to be bactericidal against B. cepacia in vitro. MCBT testing is a useful technique to help clinicians decide on appropriate nonantagonistic combination antibiotic therapy for patients with CF infected with B. cepacia.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10764313&dopt=Abstract
Chemotherapy. 1978;24(1):17-23.
Tri-minocycline: a minocycline complex for parenteral use. I. Antibacterial activity and toxicity data.
Kahan IL, Szepesy GL, Pusztai R, Joo I.
Aqueous solutions of tri-minocycline (equivalent to 20--50 mg/ml minocycline HCl) and preconstituted ready-for-use injections were prepared at the pH of blood; these exert high antibiotic activities equal to those of the parent substance. The chloroform/water distribution coefficients of tri-minocycline in the different types of injections were somewhat lower, but in the same order of magnitude as that of the parent substance. The MIC values of tri-minocycline proved to be very low and the LD50 values very high, their separation covering more than 3 orders of magnitude.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=618721&dopt=Abstract
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