Drugs online research references
Acta Paediatr Scand. 1976 Mar;65(2):253-6.
The bioavailability of oral penicillin V. A comparative study of the absorption of different salts of penicillin V in children.
Bolme P, Eriksson M.
Different salts of penicillin V (pc-V): potassium pc-V (Calciopen and Kavepenin), calcium pc-V (Penicals) and benzathine pc-V (Meropenin) were given to 37 children (age 2 months to 4 years) with upper respiratory infections. The gastro-intestinal absorption of the drug given in a mixture was followed for three hours after administration by determination of the serum levels from capillary samples. Administration of the mixtures containing the potassium pc-V resulted in a more rapid absorption and in significantly higher plasma concentrations at 30 min than did administration of the preparations containing the calcium and benzathine salts. In four children with coeliac disease, verified by intestinal biopsy, the absorption of potassium pc-V (Calciopen) was compared with that of calcium pc-V (Penicals). A decreased absorption was found and this was most pronounced when the calcium salt was given.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=816174&dopt=Abstract
J Biol Chem. 1994 Apr 22;269(16):12067-73.
Purification, properties, and kinetics of enzymatic acylation with beta-lactams of soluble penicillin-binding protein 2a. A major factor in methicillin-resistant Staphylococcus aureus.
Roychoudhury S, Dotzlaf JE, Ghag S, Yeh WK.
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.
Intrinsic resistance toward beta-lactams in methicillin-resistant Staphylococcus aureus strains, a major source of nosocomial infections, is believed to be caused mainly by penicillin-binding protein 2a (PBP2a). This protein resembles other penicillin-binding proteins that are involved in bacterial cell wall biosynthesis and are the targets of active site acylation by beta-lactam antibiotics. PBP2a, however, presumably remains active at therapeutic concentrations of beta-lactams. In this paper, we describe a three-step purification of a soluble form of PBP2a (PBP2a') to apparent homogeneity using anion-and cation-exchange, and dye-ligand affinity chromatographies. Purified PBP2a' was a 74-kDa monomeric protein that appeared to be folded. The protein was evaluated for its enzymatic acylation with beta-lactams initially by fluorescence quenching and then kinetically by radioactive labeling. Using a modified 125I-labeled penicillin V-acylation assay, the apparent Km of PBP2a' for penicillin V was 1.2 mM. Three other beta-lactams, each of which exhibited significant fluorescence quenching, acted as strong competitive inhibitors of penicillin V with apparent Ki values of 123.4, 36.1, and 12.4 microM, respectively. By a new beta-lactam preincubation analysis, these compounds could function as substrates with similar Km values. Also, the acylation rates of different beta-lactams could be readily ascertained. The enzymatic acylation data substantiate the major causative role of PBP2a in the bacterial resistance. The quantitative radioactive acylation assays are potentially useful in screening for a potent inhibitor of the enzyme.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8163510&dopt=Abstract
Infect Immun. 1976 Mar;13(3):808-12.
Bacterial interference: effects of oral antibiotics on the normal throat flora and its ability to interfere with group A streptococci.
Sanders CC, Sanders WE Jr, Harrowe DJ.
The effects of orally administered penicillin and tetracycline on the composition of the normal throat flora and its interference with the growth of group A streptococci were evaluated by throat culture and an agar overlay technique. Tetracycline caused only a slight, transient quantitative decrease in the composition of the flora and interference activity. Penicillin caused significant quantitative and qualitative decreases in both the composition of the flora and interference activity. The diminution in interference activity persisted up to 3 weeks after therapy. The differences observed between the antibiotic regimens correlated with differences in initial susceptibility of the flora to the antibiotic used and emergence of the resistance during therapy. Results indicated that although effects of antibiotics on the composition of the flora are transient, effects on its ability to interfere with group A streptococci may persist long after therapy is discontinued. It is thus possible that penicillin therapy may enhance susceptibility of certain individuals to subsequent infection with group A streptococci.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=818017&dopt=Abstract
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