[Clinical results of latamoxef on pertussis].
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Biomedical subjects
Publications and source records attributed to M Minamitani.
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Pharmacokinetic and clinical studies on cefotetan (CTT), a new cephamycin antibiotic, were carried out and the following results were obtained. Pharmacokinetic study Two patients, 7 years and 10 months of age (22 kg of body weight) and 9 years of age (28 kg of body weight), were administered 20 mg/kg of CTT by 30 minutes intravenous drip infusion. Serum levels of CTT were 148 micrograms/ml and 92 micrograms/ml immediately after the end of drip, 118 micrograms/ml and 63 micrograms/ml at 1 hour after the drip infusion. 76 micrograms/ml and 39 micrograms/ml at 2 hours after, 34 micrograms/ml and 18.2 micrograms/ml at 4 hours after and 18 micrograms/ml and 8.2 micrograms/ml at 6 hours after. Serum half-lives calculated were 1.92 hours and 1.78 hours respectively. Clinical study CTT was administered to a total of 14 patients, 3 with pneumonia, 2 with acute pyelonephritis, 2 with acute enteritis, each one with acute tonsillitis, acute bronchitis, acute bronchiolitis, sepsis, acute lymphadenitis, stomatitis and measles. Because that stomatitis and measles, however, were not indications of CTT, 2 cases with those diseases were excluded. CTT was administered at daily dose of 40 to 73 mg/kg in 2 to 4 portions for 3 to 5.5 days by intravenous drip infusion. Marked response was seen in 2 cases, moderate response in 9 and no response in 1, thus effectiveness rate was 91.7%. Neither side effects nor abnormal clinical laboratory findings were observed.
After the intravenous injection of cefpiramide (CPM) at a dose of 10 mg/kg to 2 children, the average blood levels of CPM were 77.7 micrograms/ml at 15 minutes, 64.6 micrograms/ml at 30 minutes, 41.9 micrograms/ml at 1 hour, 31.9 micrograms/ml at 2 hours, 10.7 micrograms/ml at 4 hours and 3.28 micrograms/ml at 12 hours. The half-lives were 3.0 hours and 5.8 hours. When CPM was given to 22 pediatric patients with mainly acute respiratory tract infection at doses of 20 approximately less than 50 mg/kg/day divided into 2 times by intravenous injection (12 cases) and drip-infusion (10 cases) for 2 approximately 3 days (10 cases) or 4 approximately 6 days (12 cases), the effective rate was 90.9%. No side effects were observed except slight increase of eosinophil in 1 case slight elevation of GOT in 1 case. It was concluded that CPM is a useful drug for the treatment of infection in pediatric field.
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We have studied clinically on 9,3"-diacetylmidecamycin (MOM), a new macrolide antibiotic derived from midecamycin. The following results were obtained. 1) Serum concentration. To the the same child weighing 15 kg and aged 4 years, the MOM dry syrup was administered orally at single doses of 150 mg (10 mg/kg) and 300 mg (20 mg/kg) and then the MDM fine granules at a single dose of 300 mg (20 mg/kg). At dosages of 10 mg/kg and 20 mg/kg of MOM dry syrup and 20 mg/kg of MDM fine granules, the serum concentrations were 0.5 microgram/ml, 0.8 microgram/ml and not detectable (N.D.) respectively, at 45 minutes after administration; 0.4, 0.6 and N.D. at 1 hour; 0.12; 0.2 and N.D, at 2 hours; N.D., less than 0.1, N.D. at 4 hours; N.D. in all the cases at 6 hours. 2) Clinical results. MOM dry syrup was administered to 25 children. The efficacy rate was 68.75% except for 1 dropout case and the elimination rate of 11 isolated strains of group A Streptococcus was 9.09% in 16 cases of scarlet fever and 1 of acute pharyngitis caused by group A Streptococcus. With 6 cases of pertussis were eradicated. The clinical response to 1 with acute bronchitis and 1 with Mycoplasma pneumonia were good and poor respectively. 3) Side effect. No clinical side effect and abnormal laboratory findings were observed in any of the 25 cases administered MOM dry syrup.
Pharmacokinetic and clinical evaluations of cefsulodin (CFS) were made and the following results were obtained. 1. Pharmacokinetic study Three hundred fifty grams of CFS (20 mg/kg) was administered by 30 minutes intravenous drip infusion to 7 years old child (17.5 kg in weight). Serum concentrations of CFS at the end of the infusion and 1,1.5,2.5,6.5 hours thereafter were 46.0,44.9,23.0,11.9 mcg/ml and 0.6 mcg/ml respectively. Urinary recovery rate until 6 hours from the start of infusion was 66.2%. 2. Clinical study CFS was administered to the case of bronchitis with cystic fibrosis of the pancreas and bronchiectasia (treatment was made 2 times), and each 1 case of pyelonephritis with renal calculus and measles pneumonia with infantile spasm. All infections were caused by P. aeruginosa and administration and dosage of CFS was 47 to 86 mg/kg/day, 2 to 4 times daily by intravenous injection or intravenous drip infusion for 5 to 11 days. Result was good in 3 infections (2 cases) and fair in 1 case, i.e. measles pneumonia. Effectiveness rate was 75.0%. Side effect as well as abnormal change of laboratory findings were not observed. Thus, CFS is considered to be the useful drug for the treatment of pediatric infection caused by P. aeruginosa.
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UNLABELLED: The therapeutic effects of cefotiam (CTM) in the pediatric field were studied, and the following results were obtained: 1. Absorption and excretion: After 30 minutes intravenous drip infusion of 250 mg (14.7 mg/kg) of CTM to a 5-year old child weighing 17 kg, the serum levels and urinary excretion were measured. The serum levels were 47.8 mcg/ml at 30 minutes after administration, 23.9 mcg/ml after 1 hour, 12.5 mcg/ml after 1 hour and 30 minutes, 5.2 mcg/ml after 2 hours and 30 minutes, 0.3 mcg/ml after 6 hours and 30 minutes. Excretion rate in the urine was 48.8% at 6 hours after administration. 2. CLINICAL RESULTS: CTM was administered at a daily dose of 35 to 91 mg/kg b.i.d. to q.i.d. by intravenous or intravenous drip injection for 2 to 6.5 days to six patients i.e. two with bronchopneumonia, one with acute bronchitis, one with acute enteritis, one with impetigo and atopic dermatitis one with acute tonsillitis and acute cervical lymphadenitis. The responses were excellent in 2 cases and good in 4 cases. The response rate was 100%. No side effect was observed.
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Clinical effects were investigated on cefadroxil powder for syrup (containing 100 mg of cefadroxil per 1 g) for acute bacterial infections (mostly scarlet fever) in the field of pediatrics, and the results were obtained as follows. Cefadroxil was applied in 100 cases of scarlet fever. Among 49 cases administered 30-39 mg/kg/day, the results were excellent in 34 cases and good in 15 cases, efficacy ratio being thus 100%. Among 38 cases administered 40-49 mg/kg/day, the results were excellent in 33 cases, and good in 5 cases, efficacy ratio being thus 100%. Out of 4 cases administered 20-29 mg/kg/day, the results were excellent in 3 cases and good in 1 case, while out of 9 cases administered 50-59 mg/kg/day, excellent in 4 cases and good in 5 cases. Among 78 cases of scarlet fever from which beta-hemolytic Streptococcus was proven from swab liquid of palatal tonsil, 67 cases received cefadroxil at a daily dose of 30-49 mg/kg, and the bacteria turned to negative the next day of administration in 72 cases, 2 days later in 6 cases. Cefadroxil was administered at a daily dose of 46 mg/kg for 7 days in 1 case of SSS syndrome of which Staphylococcus aureus was proven from skin lesion, and local bacteria turned to negative, as well as clinical effect was excellent. No pathogen was proven in 1 case of acute tonsillitis, maybe because ampicillin (ABPC) and cefazolin (CEZ) were administered before cefadroxil treatment, and yet a clinical efficacy was judged by administering cefadroxil at a daily dose of 46 mg/kg, though no clinical improvement was observed with the prior antibiotics. As to the side effects of cefadroxil in 102 cases, a slight vomiting was noticed in 6 cases, though the administration could be continued, and a slight rise of GOT or GPT was observed respectively in 3 cases and 1 case, all of which were recovered without abnormal clinical findings. Among the patients of scarlet fever, after beta-hemolytic Streptococcus became negative, reelimination or recurrence was noticed in 2 cases, but these patients were cured completely by readministration of cefadroxil or administration of amoxicillin (AMPC). Cefadroxil powder for syrup was absorbed quite well, its serum levels were maintained for long, and it was easily administered in children. Considering from its superior antibacterial activity, cefadroxil may be expected to be useful for a remedy in slight or middle infections of children.
Clinical evaluation was carried out on cefroxadine dry syrup (containing 100 mg of cefroxadine per 1 g) for child use, and the following results were obtained. 1. Serum levels: Peak serum levels at 1 hour after single administration of CXD 100 mg (9.1 mg/kg) to a 4-year old child (11kg) and 300 mg (12.8 mg/kg) to a 8-year old child (23.5 kg) were 20.32 microgram/ml and 18.75 microgram/ml, respectively. They declined to 0.78 microgram/ml and 0.88 microgram/ml respectively after 6 hours and to undetectable levels after 8 hours. Half-life was 1 hour and 1.2 hours, respectively. CXD has shown the same concentration pattern as CEX, except for the fact that serum levels were peaked after 30 minutes and not detectable after 6 hours. 2. Clinical responses: CXD was administered, for 7 days, to 33 children with scarlet fever in the dosage of greater than or equal 20 approximately less than 60 mg/kg/day (7 children in greater than or equal to 20 approximately 30 mg/kg/day, 21 in greater than or equal to 30 approximately less than 40 mg/kg/day and 5 in greater than or equal to 40 approximately less than 60 mg/kg/day). Clinical responses were excellent in 19 cases and good in 14 cases, with an efficacy rate of 100%. All strains of group A Streptococcus isolated from the pharynx of 22 children were eradicated within 24 hours. In 1 case each of acute pharyngitis, acute tonsillitis, acute laryngotracheitis and staphylococcal scalded skin syndrome, the dosage of greater than or equal to 30 approximately less than 45 mg/kg/day produced a 100% good clinical response and eliminated the causative pathogens. 3. Side effect: Only 2 cases of eosinophilia were observed in hematologic study as well as in hepatic and renal function tests before and after administration.
From the studies on the stability of cefmetazole and cefazolin in feces of animals and children, and the determination of the fecal concentration of cefmetazole in three pediatric patients, the following results were obtained. 1) When cefmetazole was kept at 37 degrees C for 24 approximately 48 hours in feces of rats, rabbits, dogs and children, it showed no decrease of the potency. On the other hand, cefazolin kept in the same condition as that of cefmetazole showed a remarkable decrease of the potency. 2) Fecal excretions of cefmetazole were 0, 0.22 and 0.65% of total doses, respectively, in two pediatric patients of scarlet fever and one pediatric patient of serous meningitis.
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Cefuroxime (CXM), a new cephalosporin antibiotic, was used in pediatric field, and the following results were obtained. 1. Absorption and excretion CXM was administered by intravenous drip infusion to 3 patients aged 14 years, 1 year and 1 month, and 5 years and 3 months, respectively, at doses of 15.4 mg/kg, 14.1 mg/kg, and 13.2 mg/kg. The following blood levels were obtained; 71 micrograms/ml at the completion of infusion, 26.8 micrograms/ml at 30 minutes, 13.2 micrograms/ml at 1 hours, 5.05 micrograms/ml at 2 hours, 2.07 micrograms/ml at 4 hours, and less than 0.45 micrograms/ml at 6 hours after the infusion. Urinary excretion of the drug administered was measured in one of these cases. The urinary excretion rate at 1 approximately 6 hours after intravenous drip infusion was 50.4%. 2. Clinical result CXM 17 approximately 55 mg/kg were administered for 2 approximately 4 days to 6 patients with acute respiratory tract infection, 1 with acute cervical lymphadenitis, and 1 with acute enteritis. The clinical results was poor in the case with acute enteritis and good in the other 7 cases. No side effect was observed in 9 cases (the above 8 cases plus 1 unassessable case), and the laboratory examination results showed no abnormality, either.
Clinical study of PC-904 was performed in 8 children with infectious diseases and the following results were obtained. 1) The patients treated with PC-904 were each one case of acute pharyngitis, lacunar tonsillitis, scarlet fever, phlegmone, acute bronchitis and lung abscess, and 2 cases of bronchopneumonia. 2) The administration methods were drip infusion, one-shot intravenous injection and the combined use of these administrations. The daily dosage varied from 30 to 49 mg/kg in 3 cases and from 50 to 70 mg/kg in 3 cases, and was 227 mg/kg in 1 case. 3) Clinical evaluation was examined in 7 cases and 57.1% of effectiveness was obtained. Out of 2 cases of pneumonia, one case with the causative organism of My. pneumoniae was excluded from the clinical evaluation. 4) No side effects were observed in all 8 cases treated with PC-904.
Clinical study of sustained release cephalexin (granules, 200 mg/g, S-6437) was conducted in pediatric patients as follows: 1. For infants under 20 kg of body weight, 25 approximately 50 mg/kg/day of this preparation (or 50 approximately 100 mg/kg/day for severe diseases) were given in two divided doses, and for infants over 20 kg, 1 g (or 2 g for severe diseases) were administered at two divided doses. 2. Patients treated with this preparation were 27 cases with scarlet fever, 3 with acute pharyngitis, 2 with acute tonsillitis, 1 with acute laryngitis, 1 with acute cystitis and 1 with acute enteritis. 3. Out of the 35 patients, 11 showed "very good" response to this preparation, 18 "good", 3 "fair", 1 "poor", and 2 "unknown" indicating 87.9% of effectiveness. 4. Side effects of cheilitis in one patient and vomiting in 1 were observed, and other 2 patients had difficulty in taking this preparation. No other side effects were found.
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