Drugs online research references
J Med Chem. 1988 May;31(5):976-83.
Coupling products of amino acids to penicillin V and cephalothin: synthesis and susceptibility to carboxypeptidases and lysosomal enzymes.
Bounkhala Z, Renard C, Baurain R, Marchand-Brynaert J, Ghosez L, Tulkens PM.
Laboratoire de Chimie Organique de Synthese, Universite Catholique de Louvain, Louvain-La-Neuve, Belgium.
Amino acids have been coupled to the carboxyl group of penicillin V and cephalothin by methods that keep the beta-lactam ring intact. Derivatives were successfully obtained with both neutral (Leu, Val, Ala, Ile, Trp, Tyr, Gly) and one acidic (Glu) amino acids. The new compounds were inactive in vitro against Staphylococcus aureus or Micrococcus luteus. Incubation in the presence of purified carboxypeptidases (A, B), soluble lysosomal fractions from liver, or cellular homogenates from liver, kidney, fibroblasts, and macrophages did not allow recovery of the antibacterial activity. Injection in mice also failed to cause liberation of microbiologically active compounds. HPLC studies confirmed that the amide linkage between the antibiotic and the amino acid was not hydrolyzed in the presence of soluble lysosomal fractions from liver. However, conversion of cephalothin and cephalothin-leucine to desacetyl derivatives was observed in the presence of soluble lysosomal fractions and extracts from liver and semipurified orange peel acetylesterase(s). It is concluded that amino acid derivatives of beta-lactam antibiotics do not offer potential chemotherapeutic use as prodrugs.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3129562&dopt=Abstract
Arch Otolaryngol Head Neck Surg. 1988 Jun;114(6):667-70.
Emergence and persistence of beta-lactamase-producing bacteria in the oropharynx following penicillin treatment.
Brook I.
Department of Pediatrics, Uniformed Services University of the Health Sciences, Bethesda, Md.
The emergence and persistence of aerobic and anaerobic beta-lactamase-producing bacteria (BLPB) were investigated in 26 children treated with penicillin for otitis media or pharyngitis and in 28 nontreated control children. beta-Lactamase-producers were isolated in three (12%) of the treated children before therapy, in 12 (46%) seven to ten days after completion of therapy, in nine (35%) 40 to 45 days after therapy, and in seven (27%) 85 to 90 days after therapy. These organisms were present in three (11%) of the nontreated children, and the number of patients harboring BLPB stayed constant throughout the three-month follow-up. The predominant BLPB were Bacteroides species (Bacteroides melaninogenicus group, Bacteroides oralis, and Bacteroides oris-buccae), Staphylococcus aureus, Haemophilus influenzae, and Branhamella catarrhalis. The emergence and persistence of BLPB after penicillin therapy may have important implications for the antimicrobial management of infections of the upper respiratory tract.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3130087&dopt=Abstract
Br J Clin Pharmacol. 1988 Jan;25(1):33-40.
Milk transfer of phenoxymethylpenicillin during puerperal mastitis.
Matheson I, Samseth M, Loberg R, Faegri A, Prentice A.
Department of Pharmacotherapeutics, University of Oslo, Norway.
1 The milk excretion of phenoxymethylpenicillin (PMP) was studied from both breasts in patients with mastitis (n = 12) and healthy volunteers (controls, n = 4) to investigate the hypothesis that milk transfer of PMP is higher in mastitic than in non-mastitic breasts. 2 Patients were included according to clinical symptoms of mastitis. Milk (and serum from controls) were sampled 0, 1, 2, 3, 4, 6 and 8 h after a single oral dose of 1320 mg PMP. Penicillin concentrations in milk and serum were measured by an agar diffusion technique. 3 Maximum milk concentrations (Cmax) of PMP in patients were higher (P less than 0.05) in mastitic than in non-mastitic breasts. The latter concentrations were higher (P less than 0.05) than those in breast milk from healthy controls. In milk from the mastitis patients (both breasts) the Cmax was reached after 2 h with a subsequent rapid decline in concentration. In milk from the healthy controls the PMP concentration reached a plateau after 4 h. The area under the milk concentration vs time curve (AUC0-8h) was not different for mastitic vs non-mastitic breast milk in patients nor for mastitic vs control breast milk. This can be explained by higher rates of appearance and disappearance of PMP in the breast milk of mastitis patients compared with healthy controls. In mastitic breast milk there was a moderate (P less than 0.01) increase in sodium and albumin compared with non-mastitic milk. However, milk potassium, glucose and lactose values were within normal limits.(ABSTRACT TRUNCATED AT 250 WORDS)
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3130891&dopt=Abstract
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