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PubMed1975

Relationship between the chemotherapeutic effectiveness of ciclacillin and ampicillin and the time of their administration in experimental infections.

In an attempt to explain the discrepancy between the weak in vitro activity and good clinical efficacy of ciclacillin, a time-dosage-efficacy study was made in order to investigate the relationship of the effectiveness of this antibiotic to the interval between experimental infection and administration in comparison to ampicillin, which because of its similar antimicrobial spectrum and completely different pharmacokinetic properties was particularly suitable for use in the study. Various single oral doses of both antibiotics were administered once to NMRI (SPF) mice at various intervals (0, 1, 2 or 3 h) following experimental infection with E. coli WT 102, E. coli 3033 or E. coli 026:B6 and the CD50's determined and compared statistically. It was demonstrated that the chemotherapeutic effectiveness of both antibiotics was markedly dependent on the interval between experimental infection and administration. Whereas ampicillin was superior to ciclacillin when drug and infective organism were administered simultaneously (0 h), ciclacillin was superior to ampicillin when it was administered 3 h after experimental infection. Both antibiotics were about equally effective when administered 1 or 2 h after infection. The difference in the serum concentrations and rates of absorption and excretion of the two drugs is assumed to be the reason for this phenomenon, and the pharmacokinetic characteristics of ciclacillin, in particular its rapid and almost complete absorption and rapid attainment of high peak serum levels, are discussed as at least a partial explanation of the difference in its in vitro and in vivo activities.

Administration, Oral↗
PubMed1976

[Evaluation of exanthemas following high-dosage intravenous penicillin combinations in intensive care].

118 patients of a non specialized intensive care unit have been studied, all of them under high dose bactericidal cover (10 MIU of Na-Penicillin G and 2,0 Ciclacillin q 12 hrs.) for a period of days to 4 weeks. In 17 (14,4%) a skin rash was observed. 10 of these could be studied using special techniques (radial immunodiffusion, passive hemagglutination, RIST and RAST), however in none of these cases there was a hint of the existence of penicillin specific antibodies. In 6 patients also skin tests were performed. There was no immediate type reaction, only twice delayed type reactions occured to Na Pencillin G.6 patients had continuing treatment on spite of the rash and without further steps the effluorescences vanished within 3-6 days. Therefore continuation of the antibiotic therapy in spite of rash along with strict clinical and laboratory monitoring seems to be preferable to a hastened change of antibiotic regime

Adolescent↗
PubMed1977

[In vitro examination on antibacterial activity of ciclacillin (ACPC) against clinically isolated strains (author's transl)].

(1) The antibacterial acivity of ciclacillin (ACPC) with inoculum size of 10(6) cells/ml was four times less potent than that of ampicillin (ABPC) and 4 approximately 8 times less potent than that of AMPC, but was 4 approximately 8 times more potent than that of CEX against Streptococcus pyogenes. For Streptococcus pneumoniae, ACPC was 2 approximately 4 times less active than ABPC and AMPC, but 16 approximately 32 times more active than CEX. Staphylococcus aureus was 4 approximately 8 times less susceptible to ACPC than to ABPC and AMPC, but 1 approximately 2 times more susceptible than to CEX. Against E. coli, ACPC was as active as CEX, 2 approximately 4 times less active than ABPC, and 4 approximately 8 times less active than AMPC. (2) It was suposed that ACPC was more resistant to penicillinase and more antibacterial with inoculum size of 10(6) cells/ml cells/ml than with 10(6) cells/ml. ACPC was 4 approximately 8 times less active than ABPC, and AMPC against Staphylococcus aureus with 10(8) cells/ml, while with 10(6) cells/ml, it was 2 times less active than ABPC and AMPC. (3) ACPC-resistant strains (greater than or equal to 3.13 microng/ml) of Streptococcus pyogenes and Streptococcus pneumoniae were not found. (4) A difference was noted in MIC of three semi-synthetic penicillins, ACPC, ABPC and AMPC, against Staphylococcus aureus, and E. coli between the sources from which their strains were isolated. (5) There were many strains resistant to erythromycin (EM) and josamycin (JM) (greater than 60%, respectively to both antibiotics) in Stretpococcus pyogenes and pus-isolated Staphylococcus aureus. No strains of Streptococcus pyogenes, were found resistant to EM and JM.

Amoxicillin↗
PubMed1986

Penetration of ciclacillin into bronchial secretions.

The penetration of ciclacillin into bronchial secretions was investigated in 105 patients undergoing bronchoscopy after a single oral dose of 500 mg ciclacillin. Comparison was made with 26 patients who received 500 mg ampicillin by mouth. Over a 6 to 8 hour period, ciclacillin achieved significantly higher levels in bronchial secretions but no statistically significant difference between serum ampicillin and ciclacillin levels was detected.

Adolescent↗
PubMed1980

[Studies on the distributions of antibiotics in the oral tissues: Experimental staphylococcal infection in rats, and effect of serratiopeptidase on the distributions of antibiotics (author's transl)].

1) A focal infection was prepared by inoculation of staphylococci into rat gingiva. Then, concentrations in oral tissues (gingiva, tongue and masseter), serum and liver of the infected rats which were given ciclacillin, ampicillin, cephalexin and minocycline in a dose of 100 mg/kg p.o. were investigated and effects of serratiopeptidase (20 mg/kg) on these concentrations were studied. 2) Concentrations of ciclacillin in the oral tissues were approximately 10% of a serum level. A gingival concentration was elevated 8.5-fold by pretreatment with serratiopeptidase. A concentration in infected gingiva was 2.5-fold of that of another side of gingiva. 3) Concentrations of ampicillin in the oral tissues were approximately 15% of a serum level. A gingival concentration was elevated 5.7-fold by pretreatment with serratiopeptidase. A concentration in infected gingiva ws 2.2-fold of that of another side of gingiva. 4) Concentrations of cephalexin in the oral tissues were approximately 3 to 5-fold of a serum level except that in masseter. A gingival concentration was slightly elevated (1.1-fold) by pretreatment with serratiopeptidase. A concentration in infected gingiva was 1.7-fold of that of another side of gingiva. 5) Concentrations of minocycline in the oral tissues were 1.3 to 7.2-fold of a serum level. A gingival concentration was elevated 2.2-fold by pretreatment with serratipeptidase. A concentration in infected gingiva was 3.1-fold of that of another side of gingiva. 6) Gingival concentrations of antibiotics were higher than those of tongue and masseter and serratiopeptidase elevated gingival concentrations.

Ampicillin↗
PubMed1975

[Ciclacillin therapy for diseases of the urinary tract].

In our own controlled bacteriological investigations, ciclacillin showed a good effect in urological infections at a daily dosage of 3 g for 10 days. The efficacy is comparable to that of ampicillin and corresponds to that of the double blind trials bescribed in the literature. The specially good tolerance is worthy of note.

Adult↗