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Background: Some antibiotic agents, including cotrimoxazole, inhibit the metabolism of warfarin sodium and possibly increase the risk of hemorrhage. We examined the risk of upper gastrointestinal (UGI) tract hemorrhage in older patients receiving warfarin in combination with antibiotics commonly used to treat urinary tract infection, with a focus on cotrimoxazole., Methods: This population-based, nested case-control study using health care databases in Ontario, Canada, between April 1, 1997, and March 31, 2007, identified residents 66 years or older who were continuously treated with warfarin. Cases were hospitalized with UGI tract hemorrhage. For each case, we selected up to 10 age- and sex-matched control subjects. We calculated adjusted odds ratios (aORs) for exposure to cotrimoxazole, amoxicillin trihydrate, ampicillin trihydrate, ciprofloxacin hydrochloride, nitrofurantoin, and norfloxacin within 14 days before the UGI tract hemorrhage., Results: We identified 134 637 patients receiving warfarin, of whom 2151 cases were hospitalized for UGI tract hemorrhage. Cases were almost 4 times more likely than controls to have recently received cotrimoxazole (aOR, 3.84; 95% confidence interval [CI], 2.33-6.33). Treatment with ciprofloxacin was also associated with increased risk (aOR, 1.94; 95% CI, 1.28-2.95), but no significant association was observed with amoxicillin or ampicillin (1.37; 0.92-2.05), nitrofurantoin (1.40; 0.71-2.75), or norfloxacin (0.38; 0.12-1.26). Compared with amoxicillin or ampicillin, cotrimoxazole prescription was associated with an almost 3-fold risk (ratio of ORs, 2.80; 95% CI, 1.48-5.32)., Conclusions: Among older patients receiving warfarin, cotrimoxazole is associated with a significantly higher risk of UGI tract hemorrhage than other commonly used antibiotics. Whenever possible, clinicians should prescribe alternative antibiotics in patients receiving warfarin.

Treatment options for bacterial vaginosis are numerous, however for urinary tract infection (UTI) by Gardnerella vaginalis have been not reported. Our purpose was to compare the efficacy and treatment complications of oral metronidazole versus oral ampicillin for treatment of this condition in a prospective randomized, nonblinded study. Fifty-seven women who had symptoms of UTI and a positive culture for G. vaginalis were enrolled in the study. Only forty-five subjects were considered valuable: 25 treated with oral metronidazole 500 mg twice daily for 7 days, and 20 with oral ampicillin 2 g for 10 days. Positive culture was defined as the presence of 10(4) or 10(5) UFC/ml of G. vaginalis in pure culture in HBT media. The clinical and bacteriological cure rates were 92% and 96% respectively for metronidazole and 90% in both for ampicillin. Chi-squared analysis reveals no statistical significance between two treatments. Adverse events were common in-patients treated with metronidazole whereas relatively few side effects were experienced in-patients treated with ampicillin. Ampicillin is effective, safe and well-tolerated therapy for UTI by G. vaginalis. In contrast oral metronidazole is effective but no safe and bad-tolerated therapy for the same condition.

A total of 124 patients with lower respiratory tract (44) or urinary tract infections (80) were enrolled in an open, multicenter study to evaluate the efficacy and tolerability of sulbactam/ampicillin, administered at the dosage of 3 g/die by intramuscular route. Pretreatment pathogens from patients with lower respiratory tract infections included: Streptococcus alpha-haemolyticus in 8 cases, Streptococcus beta-haemolyticus in 2 cases, Staphylococcus albus in 7 cases, Haemophilus influenzae in 7 cases, Staphylococcus aureus in 6 cases, Klebsiella oxytoca in 5 cases, Staphylococcus epidermidis in 3 cases, Streptococcus pneumoniae in 3 cases, Escherichia coli in 2 cases; in one subject (2.75%), no microorganisms were isolated. In vitro, 36 isolates (84%) were sensitive to SA and 7 (16%) were resistant. At the end of therapy, all the causative pathogens sensitive to sulbactam/ampicillin were eliminated. In patients with urinary tract infections, pretreatment pathogens were: E. coli in 40 cases, S. albus in 16 cases, Proteus mirabilis in 8 cases, Enterobacter agglomerans in 6 cases, Proteus vulgaris in 3 cases, Streptococcus faecalis in 3 cases, Streptococcus liquefaciens in 2 cases, Pseudomonas aeruginosa in 2 cases. In vitro, 64 isolates (80%) were sensitive to sulbactam/ampicillin and 16 (20%) were resistant. At the end of therapy, 63 out of the 64 pathogens sensitive to sulbactam/ampicillin were eliminated; in one case the therapy was interrupted due to adverse effect. Clinical efficacy: in subjects with lower respiratory tract infections, sulbactam/ampicillin cured 32 patients (72.72%) and ameliorated the clinical status of 8 patients (18.18%); efficacy rate: 90.9%).(ABSTRACT TRUNCATED AT 250 WORDS)

Unasyn is a combination of ampicillin, a bactericidal antibiotic, and sulbactam, an inhibitor of beta-lactamases. It was used in treatment of 36 patients with urogenital infections. The combination was administered intravenously and in the main intramuscularly. The treatment course amounted to 7-10 days. The average daily dose was 6 to 9 g. 22 patients with acute nonocclusive pyelonephritis were treated with the combination and its clinical and bacteriological efficacy was stated in 95 per cent of the cases. An excellent clinical effect of the combination was observed in 6 patients with acute epididymitis. A clinical improvement was also observed in the treatment of the patients with acute prostatitis and chronic renal infections. Unasyn proved to be a highly efficient antibacterial combination with regard to gram-positive flora and colon bacilli as representatives of gram-negative organisms. Satisfactory results were also stated in the treatment of infections caused by Proteus spp. Complete elimination of the pathogen was achieved in 57.7 per cent of the cases. No adverse reactions to Unasyn except pain in the site of the injection were recorded.

An unblinded, randomized, prospective clinical trial of cefaclor, 250 mg twice daily, versus ampicillin, 500 mg four times daily, for a total of ten days of therapy, was conducted with 100 patients presenting to an emergency department with signs, symptoms, and urinalysis results suggestive of urinary tract infection (UTI). Eighty patients had a UTI proven by pre-therapy urine culture. Significantly more of the bacteria isolated were sensitive to cefaclor (96.3%) than to ampicillin (78.0%), P less than 0.01. Seventy-one patients returned for all follow-up visits and urine cultures. The overall success rate in the cefaclor group was 75.7% and in the ampicillin group 79.4%. There was a 10% failure rate in treating clinical cystitis with both regimens, and the satisfactory outcome rate for pyelonephritis and cystitis was similar in both treatment groups.

Sixty-eight patients with urinary infection were allocated at random to receive treatment with either 500 mg ampicillin 4-times daily or a trimethoprim (250 mg)/sulfamethopyrazine (200 mg) combination given once daily after a double, loading dose on the first day. All patients complained of urinary symptoms and showed significant bacteriuria, E. coli being the pathogen most frequently recovered. Clinical and microbiological assessments were carried out on entry and, as a rule, after 3 to 4 days and 1 to 2 weeks of treatment. In the 35 patients receiving trimethoprim/sulfamethopyrazine, 40 (95%) of the 42 original infecting organisms were eradicated. In the 33 patients on ampicillin, the eradication rate was 32 (89%) out of 36 organisms. The course of urinary symptoms was similarly favourable in the two groups. Overall response was considered as 'excellent' or 'good' in 89% of the patients receiving the combination preparation and in 82% of those given ampicillin. Clinical and biological tolerance was satisfactory under both regimens. A longer follow-up control should confirm the value of the new combination in the treatment of urinary infections.

Orally administered bacampicillin (400 mg twice daily for 10 days) was as effective as orally administered amoxicillin (250 mg thrice daily for 10 days) for the treatment of acute, uncomplicated infections of the urinary tract in young women. A satisfactory clinical response was produced by bacampicillin in 71 (98.6%) of 72 patients and by amoxicillin in 73 (98.6%) of 74 patients. A satisfactory bacteriologic response was produced by bacampicillin in 69 (95.8%) of 72 patients and by amoxicillin in 72 (97.3%) of 74 patients. In a subset of the patients, bacampicillin and amoxicillin were equally effective in the treatment of infections of the upper and lower urinary tract, as determined by the fluorescent antibody-coated bacterial test of localization. Both bacampicillin and amoxicillin were well tolerated. Allergic skin reactions occurred in two (2.7%) of 74 patients receiving amoxicillin but in none of the patients receiving bacampicillin. Mild diarrhea occurred in two (2.8%) of 72 patients receiving bacampicillin and in two (2.7%) of 74 patients receiving amoxicillin. Bacampicillin administered twice daily may offer several advantages over drugs given three times a day (e.g., amoxicillin) or four times a day (e.g., ampicillin). These advantages might include lower cost, better compliance with treatment regimen, and fewer allergic episodes and adverse reactions.

Blood levels of ampicillin (ABPC) were measured in 10 childish patients with heart disease after the rectal administration of KS-R1 at doses of 125 mg and 250 mg. Average blood levels of ABPC at 15, 30 minutes, 1, 2 hours and 4 hours after the administration of KS-R1 were 6.8, 6.9, 3.1, 1.1 mcg/ml and 0.1 mcg/ml with half-life of 0.64 hours in patients of age from 1 year to 4 years 7 months old (dose level 8.9 approximately 13.9 mg/kg, average 10.5 mg/kg), and 5.2, 6.1, 3.4, 1.0 mcg/ml and 0.1 mcg/ml with half-life of 0.65 hours in patients of age from 7 years 10 months to 10 years 7 months old (dose level 8.3 approximately 13.9 mg/kg, average 9.8 mg/kg), respectively. Clinical effective rate (excellent and good) was 87% in 55 childish patients with infections. Bacteriologically, 13 strains (74%) out of 18 strains which were isolated from the patients were eradicated. No severe side effects were observed. Diarrhea was observed in 3 cases.

The following results were obtained in clinical trials of new ampicillin suppository (KS-R1) in the pediatric infection. Twenty-four patients comprising 15 with respiratory tract infection, 9 with urinary tract infection were received KS-R1 at the dose ranging from 31 mg/kg to 75 mg/kg divided 3 or 4 times a day. The results in the respiratory tract infection were "excellent" in 8 and "good" in 6, and the efficacy rate was 93.3%. The results in the urinary tract infection were "excellent" in 4 and "good" in 3, and the efficacy rate was 77.8%. Diarrhea were observed in 4 patients, and anal pain was observed in 1. But the symptoms were transient. No abnormal laboratory findings were observed.

Clinical evaluations of ampicillin (ABPC) suppository (KS-R1) were performed in 9 cases with infectious diseases in the pediatric field and the following results were obtained; When 2.7 mg/kg of KS-R1 was rectally administered to 1 case, the plasma levels of ABPC were 3.9 micrograms/ml at 15 minutes, 2.2 micrograms/ml at 30 minutes and 1.2 micrograms/ml at 60 minutes after administration. The urinary excretion rate within 6 hours was 5.0%. Clinical effects of KS-R1 were examined in 6 cases (4 cases of tonsillitis and 2 cases of urinary tract infection) at the dose of 20 approximately 50 mg/kg/day for 3 approximately 7 days. Clinical responses were excellent in 4 cases, good in 1 case and poor in 1 case (tonsillitis). As to the side effects, slight increase of eosinophil was observed in 1 case, but no diarrhea, perianal redness and eruption were observed. Since discharge ratio of KS-R1 within 5 minutes was 11.0%, the tolerance of KS-R1 was considered to be good. From the above results, KS-R1 is useful for treating the pediatric patients with various infections, who refuse to oral administration or are impossible to give oral administration because of vomiting and are multiple handicapped ones.

A clinical study of PC-904 was performed and the following results were obtained. 1) PC-904 was intravenously administered at the daily dosage of 20 approximately 120 mg/kg to 13 children; urinary tract infection (10 cases), acute pneumonia (1 case), sepsis (1 case) and purulent meningitis (1 case). The overall efficacy rate was 46.2%. 2) As to adverse reaction, eosinophilia was noted only in 2 patients. One neonate was treated with this drug, but no side effects were observed. 3) It was considered that PC-904 was a useful antibiotic drug for the second choice rather than the first.

Clinical effects of ampicillin suppository (KS-R1) were examined in 24 children (11 male and 13 female) aged from 5 months to 7 years 5 months with urinary tract infection. KS-R1 was rectally given to the patients at doses of average 45.6 mg/kg/day divided into 3 to 4 times for average 8 days. Clinical effectiveness was 95.8%. Bacteriologically, the eradication of isolated organisms was observed in 10 (71.4%) out of 14 cases, the decrease in 3 (21.4%) and the persistence in 1 (7.1%). The discharge of suppository within 5 minutes after insertion was observed in 8.7% of patients without diarrhea and in 6.9% of patients with diarrhea. The evacuation rate of the bowels within 10 minutes after insertion was observed in 5.9% of patients without diarrhea and in 41.9% of patients with diarrhea. It was suggested that the administration of KS-R1 to childish patients with diarrhea should be careful. As to the side effects, diarrhea was observed in 2 cases (7.1%) and the elevation of GPT and GOT in 1 case (3.6%).

Pharmacokinetic and clinical studies of ampicillin suppository (KS-R1) was performed in children. The results were as follows. Peak serum level of ampicillin (ABPC) after single administration of KS-R1 contains 125 mg or 250 mg of ABPC in potency was 6.03 micrograms/ml after 15 minutes and 5.78 micrograms/ml after 30 minutes, respectively. The half-life was 30.4 minutes and 30.9 minutes, respectively. Urinary excretion rate was 34.2-70.1% within 6 hours. A clinical study of KS-R1 was performed in 40 patients including purulent tonsillitis (10 cases), pharyngitis (9 cases), bronchitis (6 cases), bronchopneumonia (2 cases), scarlet fever (8 cases), otitis media (1 case) and urinary tract infection (4 cases). The clinical effects, excellent and good responses, were showed in 37 cases (efficacy rate; 92.5%). No side effects and abnormal laboratory findings were observed.

A total of 100 hospitalized patients with upper and lower urinary tract infections were treated with bacampicillin or ampicillin. The treatment was double-blind and 50 patients were randomly allocated to each group, receiving 800 mg of bacampicillin or 2 g of ampicillin t. i. d. for ten days. The distribution by age and sex was similar in the two groups. Assessments of therapeutic response and tolerance were made two and six weeks after initiation of therapy. In 89% of the patients treated with bacampicillin and 68% of the ampicillin-treated patients both the bacteria and the symptoms were eliminated at the first follow-up visit three days after end of therapy. Relapse of reinfection occurred in 44% of the ampicillin-treated patients as compared to 7% in the bacampicillin-treated patients. Side-effects occurred significantly less frequently with bacampicillin compared with ampicillin (p less than 0.05). Treatment had to be stopped on account of side-effects in 16 patients treated with ampicillin compared with only four patients treated with bacampicillin.

Plasma levels of ampicillin (ABPC) after the single rectal insertion of KS-R1 at doses of 125 and 250 mg in 154 children reached a peak at 11 approximately 15 minutes in children of age less than 1 year old, at 16 approximately 20 minutes in children of 1 approximately 3 years, 4 approximately 6 years and more than 7 years old with the highest levels of 11.50, 8.69, 10.33 and 8.30 micrograms/ml, respectively. Highest plasma levels of ABPC were 6.48, 8.00, 12.32 and 17.83 micrograms/ml by the administration of KS-R1 at doses of less than 10.9 mg/kg, 11.0 approximately 15.9, 16.0 approximately 20.9 mg/kg and more than 21.0 mg/kg, respectively, with dose-dependent response which were observed at 11 approximately 15 minutes or 16 approximately 20 minutes. There was no difference of plasma levels between the administration of 125 and 250 mg of KS-R1. The pain of insertion was observed in 0.6% of total 167 cases, the feeling of defecation in 2.4% and the discharge of suppository or its dissolved material or defecation within 30 minutes after insertion in 12.6%, without the influence of patients ages and dosage level. These figures were almost the same as those after the insertion of other suppositories such as erythromycin suppository or antipyretic suppository. Clinical effectiveness of KS-R1 was examined in 51 childish patients with various infections. KS-R1 was rectally given to them at doses of average 41.6 mg/kg/day divided into 3 to 4 times for 7 days. All cases showed excellent and good effects. Bacteriologically, all pathogens which were isolated from 12 patients were eradicated.

We compared the efficacy of orally administered ampicillin, 2 g/d, with that of trimethoprim-sulfamethoxazole, 320 mg/d-1600 mg/d, given for 2 or 6 weeks for outpatient management of acute uncomplicated renal infection in women. Of 98 women participating in the trial, 60 had renal infections with susceptible strains, complied with drug therapy, and completed 6 weeks of follow-up. Before treatment, 39 women had symptoms and signs of acute pyelonephritis; 21 had symptoms of cystitis but positive tests for antibody-coated bacteria. All 60 women had alleviation of symptoms and resolution of bacteriuria after 7 days of therapy. Subsequent recurrences occurred in 12 of 27 women given ampicillin, compared with 4 of 33 given trimethoprim-sulfamethoxazole (p = 0.008). Serotyping showed that most recurrences were reinfections with ampicillin-resistant strains. With each drug, a 2-week regimen of therapy proved as efficacious as a 6-week regimen, but the longer regimen was less well tolerated. We conclude that a 2-week treatment regimen is sufficient to manage acute pyelonephritis in outpatients and that trimethoprim-sulfamethoxazole is preferable to ampicillin therapy.

The results of a clinical trial of sultamicillin, a novel mutual pro-drug combination of ampicillin and the beta-lactamase inhibitor sulbactam, in ampicillin-resistant urinary tract infections are reported. The majority of infections treated occurred in elderly geriatric in-patients. Two dosage schedules were investigated, both resulting in the same total daily dosage (1500 mg sultamicillin). These were 750 mg sultamicillin, 12-hourly (series I) and 500 mg sultamicillin, 8-hourly (series II), each administered orally for seven days. Short term cure rates (after exclusion of superinfections and reinfections) of 79.5% (series I) and 82% (series II) were obtained one week after therapy, falling to 69% and 50%, respectively, at three to six week follow up. Sultamicillin was well tolerated. Pharmacokinetic studies confirmed intestinal absorption of both constituents in young volunteers and in the elderly.

Twenty-five children (16 females and 9 males) aged from 8 months to 10 years with clinical and laboratory evidence of UTI were treated with sulbactam + ampicillin (SBT/AMP). Twenty-four of them were suffering from cystitis and one from pyelonephritis. Four of them were treated unsuccessfully prior to entry in the trial. The mean final dose of SBT/AMP was 47.69 mg/kg/die (ratio of SBT-AMP was 1:2). The patients were treated for 3 to 8 days (mean: 4.76 days). 84% were treated by i.m. route. No side effects or adverse experience were reported. Clinical cure was achieved in 25 patients (100%).

30 outpatients suffering from acute urinary infections underwent oral treatment with pivaloyloxymethyl-(2S,5R,6R)-6-(perhydroazepin-1-ylmethylenamino)penicillinate (pivmecillinam) (n = 15) or ampicillin (n = 15) in a first study. In a second study 6-beta-(hexahydro-1H-azepin-1-yl)-methylenamino penicillanic acid (mecillinam) (n = 16) or ampicillin (n = 14) were applied i.v. to 30 patients with pretreated urinary infections. The tolerance of the drugs proved to be comparatively good in both studies. The clinical and antibacterial effectiveness were equally good in the first study. However, in the second study the effectiveness of mecillinam However, in the second study the effectiveness of mecillinam seemed to be comparatively inferior.

In 16 controlled, randomized, comparative studies a total of 953 patients were treated for urinary tract infection, sinusitis, otitis media or chronic bronchitis. The aim was to evaluate the efficacy and safety of bacampicillin in a twice daily dosage, compared with three times daily dosages of bacampicillin, ampicillin, amoxycillin and a twice daily dosage of co-trimoxazole. Bacampicillin was given in amounts of either 400 or 800 mg to 422 of the patients in these studies. The twice daily dosage of bacampicillin eradicated 89% of the causative bacteria of urinary tract infections compared to 86% with the other regimens. In acute sinusitis 92% and 96% of the patients were either cured or improved when treated with 400 and 800 mg bacampicillin twice daily respectively. Similar percentages occurred in the groups given the three times daily dosages. In exacerbation of chronic bronchitis, 800 mg bacampicillin twice daily was the minimum effective dosage and 84% of the patients were either cured or improved with this regimen. Adverse drug reactions due to bacampicillin at all dose levels were less frequent than those of other anti-microbials. The lowest frequency of diarrhoea, 2.4%, was seen in the group given 400 mg bacampicillin twice daily. Dosages of 400 or 800 mg bacampicillin twice daily had a reliable efficacy combined with a low frequency of adverse reactions in respiratory and urinary tract infections.

This general practice study compared a 3-day course of a new preparation, Mictral, with a standard 7-day course of ampicillin in the treatment of uncomplicated urinary tract infection. Mictral achieved bacteriological cure in all infected patients by Day 4 while only 69% of infected patients in the ampicillin group were abacteriuric by Day 8. Symptomatic relief and the incidence of side-effects were similar for both groups. It is concluded that Mictral appears to be a useful addition to currently available therapy for urinary tract infection and merits further investigation.

In this double-blind study, the clinical tolerance of high doses of bacampicillin hydrochloride (800 mg t. i. d.) and of pivampicillin base (700 mg t. i. d.) administered for ten days were compared in out-patients with acute urinary tract infections. The clinical response was comparable with that previously reported for those antibiotics. Upper gastrointestinal side-effects were more common after treatment with pivampicillin and were reported in 9/38 patients compared to 3/34 patients treated with bacampicillin. The duration of the symptoms of the side-effects was also more prolonged after pivampicillin than after bacampicillin.

Blood level of ampicillin (ABPC) after the administration of ABPC suppository (KS-R1) reached a peak in 15 approximately 60 minutes with the level of 300 ng/ml at a dose of 1 mg/kg/day. This level was almost the same as that after the intramuscular injection of ABPC, and higher than that after the oral administration of ABPC which were reported. The clinical effective rate (excellent and good) of KS-R1 was more the 95%, and the overall effective rate including bacteriological effect was more than 95%. It is concluded that KS-R1 is a useful drug for the treatment of bacterial infections in pediatric field.

A double-blind trial was carried out comparing cephradine and ampicillin in the treatment of urinary tract infections in 42 females attending a hospital Department of Obstetrics and Gynaecology. Results showed that patients did better in the cephradine group than the ampicillin group, both bacteriologically and clinically. The numbers in each group were small, however, and did not reach statistical significance.

In order to evaluate effectiveness of ABPC suppository (KS-R1) in the treatment of bacterial infections of children, the clinical studies were carried out. KS-R1 was given in rectum to 14 patients in doses of 24.2 approximately 65.8 mg/kg (average 38.5 mg/kg) in 3 approximately 4 divided doses for 3 approximately 8 days (average 4.0 days); 6 with acute tonsillitis, 3 with pneumonia, 1 with otitis media, 4 with UTI. The overall efficacy rate was 100%. Bacterial efficacy was good, i.e. 8 of the 8 strains disappeared. Any clinical side effects and laboratory abnormalities were not observed during treatment. The above results suggested that KS-R1 is a useful antibiotics for pediatric bacterial infections.

In an open, prospective clinical trial, we evaluated the safety and efficacy of apalcillin in the treatment of complicated urinary tract infection. 21 hospitalized adult patients received apalcillin 2 g IV Q8-12 h for 5-17 days. There were 8 upper tract and 13 lower tract infections. Of 25 functional or anatomic abnormalities of the GU tract among these patients, 9 (36%) were corrected during the study period. Effectiveness of apalcillin was determined by clinical and bacteriologic response. 16 (76.2%) patients had clinical cures, 4 (19.8%) had clinical improvement, and 1 (4.8%) had clinical failure. Based on 26 pretreatment isolates, there were 16 (61.5%) bacteriologic cures and 10 (38.5%) failures. Failures were due to 6 (23.1%) relapses, 2 (7.7%) superinfections, and 2 (7.7%) relapses with superinfection. Adverse reactions were mild, transient, and did not require discontinuation of treatment. Apalcillin appears to be a safe, although marginally effective single agent antibiotic for the treatment of complicated urinary tract infections.

The results of two studies on tolerability and efficacy of mezlocillin/oxacillin are reported. The pain caused by i.m. injection of 1 g (20% solution) of the fixed antibiotics combination mezlocillin/oxacillin is compared with that caused by 1 g ampicillin. The injection volume was 5 ml. The statistical analysis of the patients' statements indicates a better tolerance of the fixed antibiotics combination mezlocillin/oxacillin than of ampicillin. The second study was determined the clinical efficacy and tolerability of mezlocillin/oxacillin in the treatment of wound infections, biliary tract infections, urinary tract infections, appendicitis and peritonitis. 19/20 patients were clinically cured after about 7 days o treatment with i.m. injections of 1.5 g mezlocillin/oxacillin in 6 ml of a 25% aqueous solution t.i.d. Treatment had to be discontinued after 3 days in one case because of a generalized exanthema. No other side effects were reported. These studies show that both the i.m. injection o the 20% solution of 1 g mezlocillin/oxacillin combination and the 25% solution of 1.5 g of this combination are tolerated without problems.

Clinical and bacteriological effects of ampicillin suppository (KS-R1) were determined in 9 cases with urinary tract infection and 13 cases with upper respiratory tract infection in children. Clinical effects were excellent in 1 case, good in 18 cases, fair in 2 cases and poor in 1 case. Bacteriological effects were eradication in 6 cases, decrease in 1 case, persistance in 3 cases and replacement in 1 case among 11 cases which were measured the pathogens before and after treatment. As to the side effects, one patient showed watery diarrhea, and another one showed the elevation of GOT. KS-R1 is considered to be a useful drug for the treatment of infection in children both clinically and bacteriologically.

The safety and clinical efficacy of dosing twice a day with bacampicillin was evaluated in clinical trials conducted at various locations in Latin America, Switzerland, and Scandinavia, Bacampicillin (200, 400, 600, or 800 mg) given twice a day was compared with bacampicillin (400 mg) or ampicillin (500 or 556 mg) administered three times a day in eight double-blind and six open randomized trials involving 750 patients with respiratory and urinary tract infections. In a noncomparative study, 47 additional patients were treated with 600 mg of bacampicillin twice a day. High rates of clinical cure or improvement were achieved for all types of infections investigated. Microbiologic cure was observed in greater than 90% of respiratory infections due to beta-hemolytic streptococci, Streptococcus pneumoniae, or Hemophilus influenzae. There were no significant differences between the responses of groups treated twice and those treated three times a day. Adverse effects of both regimens of bacampicillin were similar and occurred less frequently than in patients treated with ampicillin. Dosing twice daily with bacampicillin appears to be effective against numerous gram-positive and gram-negative bacteria in a variety of mild clinical infections. Studies comparing identical dosage regimens of bacampicillin and other aminopenicillins are needed to determine whether bacampicillin given twice a day has a therapeutic advantage.

Subjects were in-patients with bacterial urinary tract infections, ranging in age 4 months to 11 years 4 months. As a rule, daily dose was either four 125 mg (in potency) suppositories or four 125 mg (in potency) oral form given at 6-hour intervals over a period of 5 days. The number of children subjected to this study was 105. These children were divided into 2 groups (suppository 54; oral form 51) with matched pretreatment background factors. Therapeutic effectiveness rates were 70.4% for the suppository and 66.7% for the oral form, and no significant difference was observed between the 2 groups. Rates of efficacy by severity, presence or absence of underlying and/or complication diseases, daily dose and causative microorganisms did not differ significantly between the 2 groups. There was no significant difference in time-courses of improvement of clinical signs and symptoms between the 2 groups. Eradication rates for causative microorganisms were 65.9% for the suppository and 62.5% for the oral form. Most frequently isolated causative microorganisms were Escherichia coli and Proteus mirabilis. No significant differences were recognized in the therapeutic effect and usefulness evaluated by physicians in charge. The frequency of side effects did not differ significantly between the suppository group (6 with diarrhea and 1 with anal pain: 12.1%) and the oral form group (5 with diarrhea, 1 with displeasure and 1 with vomiting: 12.7%). Abnormal laboratory findings appeared in 6 cases (2 with eosinophilia, 2 with increased GOT and 2 with increased GPT) in the suppository group and 7 cases (2 with eosinophilia, 2 with thrombocytosis, 2 with increased GOT and 1 with increased GPT) in the oral form group.

A multicenter, prospective, double-blind, controlled study was performed to compare the efficacy of trimethoprim-sulfamethoxazole with that of ampicillin in the treatment of chronic urinary tract infections. The incidence of adverse clinical signs and symptoms as well as abnormal laboratory values were comparable in the two treatment groups. This study appears to establish the fact that trimethoprim-sulfamethoxazole is an acceptable alternative to ampicillin for the treatment of chronic urinary tract infections caused by susceptible Escherichia coli.

A total of 120 patients, including 53 pregnant women with significant bacteriuria, received 163 7-day courses of oral antimicrobial agents allocated in a randomised manner. The cure rates after 6 weeks' follow-up ranged from 73% to 86%, and there was no statistical difference between preparations of ampicillin, carbenicillin indanyl easter, and 2 different formulations of nifuratel. Side-effects occurred in 30% to 40% of the courses of penicillin drugs, but in under 15% of the course of nifuratel. It is concluded that the new oral preparation of carbenicillin is a useful addition to the list of antimicrobial agents which are effective in the treatment of urinary infections in domiciliary patients. Furthermore, nifuratel has been confirmed as a highly active non-toxic drug which is valuable in the treatment of urinary infections.

Cephazolin sodium was shown to be as effective as ampicillin in the treatment of respiratory and urinary system infections in patients who were infected with susceptible organisms and had a much less troublesome side reaction rate of hypersensitivity type. In addition, it was found that predictable blood levels of cephazolin could be obtained in patients with renal failure when dosage was regulated according to a nomogram calculated from the patient's serum half-life based on clearance of creatinine.

Clinical trials of KS-R1 have been carried out on 28 infections in children, including 8 pharyngitis, 11 tonsillitis, a pharyngolaryngobronchitis, 3 lymphadenitis and 5 urinary tract infections. The following results were obtained. KS-R1 30-50 mg/kg/day, was clinically effective in 27 out of 28 infections. Bacteriologically, the following routine clinical isolates were identified; Enterococci in 1 case, S. viridans 1 case, S. pneumoniae 1 case, S. pyogenes 2 cases, H. parainfluenzae 1 case, E. coli 5 cases and S. aureus + H. influenzae 1 case. Every isolated organism showed +++ sensitivity to the ABPC sensitivity disc in vitro without only 1 case of E. coli. The organisms were eradicated in 11 patients after the administration of KS-R1. Adverse effects did not occur in any patient without case 25, who complained of pollakiuria.