title: [Microbiological, pharmacokinetic and clinical studies of rokitamycin dry syrup in the pediatric field].
abstract: Rokitamycin (RKM), a newly developed macrolide antibiotic with a 16-membered ring, dissolves well under acidic conditions. It has been improved over other macrolides to minimize individual variations in its absorbability. We measured, using the GA-test, variations in gastric acidities of 43 children with ages between 1 to 14 years, and investigated the relationship between gastric acidities and pharmacokinetic values. Also activities (expressed in MICs) of antimicrobial agents were studied against clinically isolated 229 bacterial strains using an inoculum size of 10(6) cells/ml. Tested organisms included Streptococcus pyogenes (77 strains), Streptococcus agalactiae (29), Streptococcus pneumoniae (2), as Gram-positive cocci, and Haemophilus influenzae (1), Haemophilus parainfluenzae (1), Bordetella pertussis (12), Salmonella sp. (4) and Campylobacter jejuni (103) as Gram-negative bacilli. Against stock strains of bacteria, MICs of 10 drugs (RKM, erythromycin (EM), josamycin (JM), midecamycin (MDM), midecamycin acetate (MOM), clindamycin (CLDM), amoxicillin (AMPC), cefaclor (CCL), minocycline, ofloxacin (OFLX] were determined. Against isolates from patients who underwent treatment with RKM, MICs of only 4 drugs (RKM, EM, JM, MOM) were determined. Measurements were made on plasma and urinary concentrations of RKM and its urinary recovery rates after patients including 6 boys with ages between 5 years 1 month and 11 years 6 months were administered with RKM (dry syrup). Two groups of 6 boys were administered between meals with RKM at dose levels of 5 and 10 mg/kg, respectively. Clinical and bacteriological effects of RKM were evaluated for 175 patients including 5 cases of pharyngitis, 3 tonsillitis, 32 pneumonia, 17 mycoplasmal pneumonia, 34 atypical pneumonia, 28 streptococcal infections, 29 Campylobacter enteritis, 4 Salmonella gastroenteritis, and 23 enteritis due to unknown organisms. Five drop-out cases were excluded from the evaluations. In the evaluable cases, an average dose level used was 31.8 mg/kg/day, with a daily dose divided into 3 to 4 administrations and with an average treatment duration of 9 days. Adverse reactions of RKM and its effects on laboratory test values were investigated in these patients including the drop out cases. Obtained results of these studies are summarized below. 1. The GA-test produced pH values indicating that amounts of gastric acid were mostly either normal or high in 42 of the 43 subjects tested (97.7%), and only one low acid case (2.3%) was observed.(ABSTRACT TRUNCATED AT 400 WORDS)
mesh_terms: D000284:Administration, Oral; D001774:Blood Chemical Analysis; D002167:Campylobacter / Q000187:drug effects; D002169:Campylobacter Infections / Q000188:drug therapy; D002648:Child; D002675:Child, Preschool; D004341:Drug Evaluation; D004352:Drug Resistance, Microbial; D004751:Enteritis / Q000188:drug therapy; D005260:Female; D006801:Humans; D007223:Infant; D007933:Leucomycins / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D015644:Miocamycin / Q000031:analogs & derivatives*; D015337:Multicenter Studies as Topic; D011014:Pneumonia / Q000188:drug therapy; D011019:Pneumonia, Mycoplasma / Q000188:drug therapy; D012141:Respiratory Tract Infections / Q000188:drug therapy* / Q000378:metabolism / Q000382:microbiology; D013290:Streptococcal Infections / Q000188:drug therapy; D013291:Streptococcus / Q000187:drug effects; D014069:Tonsillitis / Q000188:drug therapy
chemical_list: D007933:Leucomycins; D015644:Miocamycin; C033383:rokitamycin