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Antimicrobial Agents and Chemotherapy Jun 1981Concentrations of cyclacillin in serum over a 6-h period were similar in fasted and milk-fed infants who received 25-mg/kg doses of cyclacillin suspension. Measured by... (Comparative Study)
Comparative Study
Concentrations of cyclacillin in serum over a 6-h period were similar in fasted and milk-fed infants who received 25-mg/kg doses of cyclacillin suspension. Measured by the concentration in serum after oral administration of 15-mg/kg doses, cyclacillin was absorbed more rapidly, reached larger concentrations, and was cleared more promptly than was amoxicillin.
Topics: Amoxicillin; Bacteria; Child, Preschool; Cyclacillin; Female; Half-Life; Humans; Infant; Kinetics; Male; Penicillins
PubMed: 7271275
DOI: 10.1128/AAC.19.6.1086 -
Antimicrobial Agents and Chemotherapy Sep 1973Cyclacillin is a semisynthetic penicillin produced from the penicillin nucleus (6-aminopenicillanic acid) by acylation with 1-aminohexanecarboxylic acid. The absorption... (Clinical Trial)
Clinical Trial Comparative Study
Cyclacillin is a semisynthetic penicillin produced from the penicillin nucleus (6-aminopenicillanic acid) by acylation with 1-aminohexanecarboxylic acid. The absorption and excretion characteristics of cyclacillin were defined in one completely randomized and three three-way crossover experiments. Mean peak serum cyclacillin levels appeared earlier and were fivefold higher than those obtained with equal doses of ampicillin. High serum cyclacillin concentrations were reached at 0.5 h and by 2 h were lower than ampicillin. Serum ampicillin concentrations peaked at 1.5 h, remaining slightly higher than those for cyclacillin for the next 4.5 h. The mean area for the cyclacillin curve was significantly superior to either of the ampicillin formulations. Mean serum concentrations of cyclacillin exhibited a smooth dose-response, approximately doubling in each instance as the dose was doubled from 250 to 500 and from 500 to 1,000 mg. High concentrations of cyclacillin were also demonstrated in urine. Neither ratio of drug to metabolite in the urine nor the percent of excretion was significantly affected by the dose level. Sixty-seven percent of the drug was excreted unchanged, and 17% was excreted as penicilloic acid, with most of the excretion occurring within 6 h of administration. In subjects given 500 mg of cyclacillin (four times daily) for 6 days, 2% of the drug was excreted as 1-aminocyclohexanecarboxylic acid, and approximately 55% (24 to 91%) was unchanged. Neither formation nor excretion of the former was sex dependent.
Topics: Adult; Ampicillin; Analysis of Variance; Clinical Trials as Topic; Cyclohexylamines; Dose-Response Relationship, Drug; Female; Humans; Intestinal Absorption; Male; Middle Aged; Penicillanic Acid; Penicillins; Time Factors
PubMed: 4357182
DOI: 10.1128/AAC.4.3.361 -
Antimicrobial Agents and Chemotherapy Sep 1986Cyclacillin, a new aminosalicylic semisynthetic penicillin, was compared with amoxicillin for the therapy of acute bacterial maxillary sinusitis in 80 patients (ages, 12... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Cyclacillin, a new aminosalicylic semisynthetic penicillin, was compared with amoxicillin for the therapy of acute bacterial maxillary sinusitis in 80 patients (ages, 12 to 70 years) in a prospective, double-blind, randomized clinical trial. Direct sinus aspirations for quantitative culture were done for all patients before and after 10 days of therapy. Both drugs were administered at a dosage of 500 mg orally three times daily. Among culture-positive patients, clinical cure was achieved in 23 of 26 patients and 25 of 27 patients treated with cyclacillin and amoxicillin, respectively, for an overall cure rate of 91%. Bacteriologic failure occurred in 9% (4 of 44 patients); 3 of the 4 failures were in the cyclacillin group. There was no correlation between clinical or bacteriologic cure and the results of sinus transillumination (clear, dark) at follow-up. Initial direct sinus aspirates were positive in 57 of 80 cases (70%): 25 (44%) of these were the result of Streptococcus pneumoniae and 23 (40%) were the result of Haemophilus influenzae. All of these isolates were susceptible (MIC, less than or equal to 0.5 microgram/ml) to both study drugs; no ampicillin-resistant H. influenzae was recovered. On day 10 of therapy, mean concentrations of both drugs in serum were 2.5 to 2.7 micrograms/ml, but no antibiotic was detectable in 20 of 21 simultaneous sinus aspirates. Adverse effects (rash, diarrhea) were infrequent and similar in both groups. Cyclacillin appears equivalent to amoxicillin in the therapy of acute maxillary sinusitis.
Topics: Acute Disease; Adolescent; Adult; Aged; Amoxicillin; Child; Clinical Trials as Topic; Cyclacillin; Double-Blind Method; Humans; Maxillary Sinus; Microbial Sensitivity Tests; Middle Aged; Penicillins; Random Allocation; Sinusitis
PubMed: 3535660
DOI: 10.1128/AAC.30.3.350 -
The Journal of Biological Chemistry Oct 1995This study was initiated to determine if there are differences in the recognition of beta -lactam antibiotics as substrates between intestinal and renal peptide... (Comparative Study)
Comparative Study
This study was initiated to determine if there are differences in the recognition of beta -lactam antibiotics as substrates between intestinal and renal peptide transporters, PEPT 1 and PEPT 2. Reverse transcription-coupled polymerase chain reaction and/or Northern blot analysis have established that the human intestinal cell line Caco-2 expresses PEPT 1 but not PEPT 2, whereas the rat proximal tubule cell line SKPT expresses PEPT 2 but not PEPT 1. Detailed kinetic analysis has provided unequivocal evidence for participation of PEPT 2 in SKPT cells in the transport of the dipeptide glycylsarcosine and the aminocephalosporin cephalexin. The substrate recognition pattern of PEPT 1 and PEPT 2 was studied with cefadroxil (a cephalosporin) and cyclacillin (a penicillin) as model substrates for the peptide transporters constitutively expressed in Caco-2 cells (PEPT 1) and SKPT cells (PEPT 2). Cyclacillin was 9-fold more potent than cefadroxil in competing with glycylsacosine for uptake via PEPT 1. In contrast, cefadroxil was 13-fold more potent than cyclacillin in competing with the dipeptide for uptake via PEPT 2. The substrate recognition pattern of PEPT 1 and PEPT 2 was also investigated using cloned human peptide transporters functionally expressed in HeLa cells. Expression of PEPT 1 or PEPT 2 in HeLa cells was found to induce H(+)-coupled cephalexin uptake in these cells. As was the case with Caco-2 cells and SKPT cells, the uptake of glycylsarcosine induced in HeLa cells by PEPT 1 cDNA and PEPT 2 cDNA was inhibitable by cyclacillin and cefadroxil. Again, the PEPT 1 cDNA-induced dipeptide uptake was inhibited more potently by cyclacillin than by cefadroxil, and the PEPT 2 cDNA-induced dipeptide uptake was inhibited more potently by cefadroxil than by cyclacillin. It is concluded that there are marked differences between the intestinal and renal peptide transporters in the recognition of beta -lactam antibiotics as substrates.
Topics: Animals; Anti-Bacterial Agents; Biological Transport; Blotting, Northern; Carrier Proteins; Cefadroxil; Cells, Cultured; Cephalexin; Cephalosporins; Cyclacillin; Dipeptides; Dose-Response Relationship, Drug; Humans; Intestine, Small; Kidney; Penicillins; Peptide Transporter 1; Polymerase Chain Reaction; RNA, Messenger; Rats; Recombinant Proteins; Symporters; Vaccinia virus
PubMed: 7592745
DOI: 10.1074/jbc.270.43.25672 -
Bulletin of the New York Academy of... Jun 1983
Comparative Study
Topics: Administration, Oral; Amoxicillin; Ampicillin; Child, Preschool; Cyclacillin; Food; Humans; Infant; Kinetics; Penicillins
PubMed: 6576831
DOI: No ID Found -
Antimicrobial Agents and Chemotherapy Jan 1979A double-blind study was performed to compare the clinical response and the incidence of side effects in 2,581 patients administered ampicillin or cyclacillin for... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
A double-blind study was performed to compare the clinical response and the incidence of side effects in 2,581 patients administered ampicillin or cyclacillin for infections of the genitourinary or respiratory tract, infections of the skin and soft tissues, or for otitis media. There was no significant difference in clinical response and bacterial eradication. All side effects, including diarrhea and skin rash, were approximately twice as frequent in patients treated with ampicillin.
Topics: Administration, Oral; Ampicillin; Clinical Trials as Topic; Cyclacillin; Double-Blind Method; Female; Genital Diseases, Female; Genital Diseases, Male; Humans; Male; Penicillins; Respiratory Tract Infections; Urinary Tract Infections
PubMed: 371540
DOI: 10.1128/AAC.15.1.55 -
Applied Microbiology Nov 1971Intravenous inoculation of a penicillin-resistant phage type 80/81 staphylococcus caused lethal infection in seven of eight untreated monkeys. Daily intragastric... (Comparative Study)
Comparative Study
Intravenous inoculation of a penicillin-resistant phage type 80/81 staphylococcus caused lethal infection in seven of eight untreated monkeys. Daily intragastric administration of 50 mg/kg given in two equal morning and afternoon doses of cyclacillin and nafcillin was followed by mortalities of four of four and two of four monkeys, respectively. After 100 mg per kg per day, three of four and one of four monkeys receiving cyclacillin and nafcillin, respectively, died. Thus, mortality in controls and cyclacillin-treated monkeys was seven of eight as compared to three of eight after nafcillin treatment. Although the staphylococcus was more resistant to cyclacillin (minimal inhibitory concentration = 7.80 mug/ml) than to nafcillin (minimal inhibitory concentration = 0.31 mug/ml), regular rapid absorption and high levels of the former suggested potential efficacy. However, the similar mortality in cyclacillin-treated and control monkeys indicated that the in vitro data did not, in this instance, conform to the in vivo observations.
Topics: Animals; Biological Assay; Blood Bactericidal Activity; Blood Urea Nitrogen; C-Reactive Protein; Haplorhini; Macaca; Nafcillin; Penicillin Resistance; Penicillins; Sarcina; Staphylococcal Infections; Staphylococcus
PubMed: 5002313
DOI: 10.1128/am.22.5.865-869.1971 -
The Journal of Physiology Aug 19771. Using an in vitro everted gut sac method based on that of Wilson & Wiseman (1954), a number of amino penicillins were tested in order to identify the involvement of...
1. Using an in vitro everted gut sac method based on that of Wilson & Wiseman (1954), a number of amino penicillins were tested in order to identify the involvement of any specialized transport mechanisms in their absorption across rat intestine. 2. Only one of the amino penicillins, cyclacillin (1-amino-cyclohexyl penicillin) was shown to be actively transported. The other penicillins appeared to diffuse passively across the intestine. 3. Cyclacillin was found to concentrate against a gradient at 37 degrees C but not at 19 degrees C. 4. Transport of cyclacillin across the mucosal membrane was saturated at mucosal concentrations greater than 1000 microgram/ml. 5. The rate of the forward flux of cyclacillin was many times that of its back flux. 6. No relationship between the active transport of cyclacillin and that of amino acids could be demonstrated.
Topics: Amoxicillin; Ampicillin; Animals; Biological Transport, Active; Cyclacillin; In Vitro Techniques; Intestinal Absorption; Intestinal Mucosa; Intestine, Small; Male; Mucous Membrane; Penicillins; Rats
PubMed: 894604
DOI: 10.1113/jphysiol.1977.sp011914 -
Antimicrobial Agents and Chemotherapy Dec 1986A predictable 6- to 7-day course of a fatal Leptospira interrogans serovar bataviae infection in experimentally infected mature 110- to 150-g hamsters was used to...
A predictable 6- to 7-day course of a fatal Leptospira interrogans serovar bataviae infection in experimentally infected mature 110- to 150-g hamsters was used to evaluate the therapeutic efficacy of conventionally used and newer antibiotics. Active drugs were ampicillin, bacampicillin, cyclacillin, piperacillin, mezlocillin, doxycycline, chlortetracycline, cefotaxime, and moxalactam. Cephalexin, cefadroxil, cefamandole, and cefoperazone showed little or no activity in preliminary studies. In delayed treatment studies, all nine active drugs prevented death of hamsters even when treatment was delayed until 1 to 2.5 days before expected time of death. Leptospires in kidneys of surviving animals could be demonstrated in one or more hamsters treated with doxycycline, chlortetracycline, cyclacillin, and piperacillin, but in none of the animals treated with ampicillin, bacampicillin, mezlocillin, cefotaxime, and moxalactam. The potential usefulness of newer penicillins and cephalosporins, as well as ampicillin, chlortetracycline, and doxycycline, for treatment of severe leptospirosis is reported.
Topics: Animals; Cephalosporins; Cricetinae; Leptospira interrogans; Mesocricetus; Penicillins; Tetracyclines; Weil Disease
PubMed: 3813511
DOI: 10.1128/AAC.30.6.835 -
Antimicrobial Agents and Chemotherapy Jan 1980The pharmacokinetic properties of cyclacillin administered as a 3.0-g oral dose, with and without progenecid, have been studied and correlated with in vitro activity of... (Comparative Study)
Comparative Study
The pharmacokinetic properties of cyclacillin administered as a 3.0-g oral dose, with and without progenecid, have been studied and correlated with in vitro activity of the drug against 109 isolates of Neisseria gonorrhoeae. By 8 h after dosage, levels of cyclacillin in serum declined below the minimal inhibitory concentration and the inferior antibacterial activity of cyclacillin (compared with that of amipicillin) suggest that cyclacillin is not a promising alternative to ampicillin for single-dose treatment of gonorrhea.
Topics: Adolescent; Adult; Ampicillin; Cyclacillin; Gonorrhea; Humans; Male; Microbial Sensitivity Tests; Neisseria gonorrhoeae; Penicillins
PubMed: 6766294
DOI: 10.1128/AAC.17.1.89