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Biomedical subjects

H Meguro

Publications and source records attributed to H Meguro.

At least 109 records · Page 6Linked to original sources
PubMed1988

[Appraisal of rokitamycin in the pediatric field].

In a study of rokitamycin (RKM) dry syrup for its usefulness in pediatric infections, the following results were obtained: 1. Frequencies of RKM-resistant strains among fresh isolates from sick children were very low, and 4.4% of 68 isolates of Staphylococcus aureus, 4.2% of 48 isolates of Streptococcus pneumoniae, and none of 96 isolates of Streptococcus pyogenes were found to be RKM-resistant. 2. Hypo- to achlorhydria was found in 2 (3.77%) of 53 children. 3. When children were administered once orally with 5, 10 and 15 mg/kg of RKM dry syrup at fasting, mean peak values of plasma concentration were 0.25, 0.55 and 0.74 micrograms/ml with a T1/2 (beta) of 2.18, 1.97 and 2.00 hours, respectively. Urinary recovery rates during the first 0-6 hours were quite low, and values were 1.21, 1.38 and 2.23%, respectively. 4. The clinical efficacy of RKM dry syrup was studied on children chiefly with acute pneumonia, mycoplasmal pneumonia and tonsillitis. Among 379 children from whom pathogens had been determined, responses to the treatment were excellent in 186, good in 144, fair in 24, poor in 20 and unknown in 5 patients, the overall efficacy rate being 88.2%. Among all 598 treated patients, including those with undetermined pathogens, responses were excellent in 247, good in 269, fair in 42, poor in 35 and unknown in 5 patients, the efficacy rate being 87.0%. 5. The clinical efficacy of the drug in treating Chlamydia infection in 12 patients including a Chlamydia carrier and the clinical efficacy in treating Campylobacter enteritis in 36 patients were studied. All the cases showed "good" responses. Among 66 patients with mycoplasmal pneumonia, responses were excellent in 33 and good in 27 patients, with an efficacy rate of 90.9%. 6. The optimal dose of RKM dry syrup seemed to be in the range between 20 and 40 mg/kg. It appeared, however, that a dose of about 40 mg/kg would be required to eradicate the pathogen from the pharynx in S. pyogenes infection. 7. Adverse reactions to RKM dry syrup were found in 9 (1.45%) of 622 patients. The reactions were gastrointestinal symptoms except eruption occurred in 1 patient, but they were all mild. Laboratory examinations revealed eosinophilia in 19 and abnormal hepatic enzyme activities in 8 of 455 patients studied, but such abnormalities were all transient and mild.

Bacterial Infections↗
PubMed1988

[Clinical and pharmacokinetic studies of rokitamycin in children].

Rokitamycin dry syrup (RKM), a new macrolide antibiotic preparation, was evaluated for its safety, efficacy and pharmacokinetics in 19 children. RKM was effective in mycoplasmal pneumonia, Chlamydia trachomatis pneumonitis and Campylobacter gastroenteritis. Efficacies of RKM in streptococcal pharyngitis and Haemophilus influenzae pneumonia, however, were insufficient. Pharmacokinetic observations seemed to indicate that RKM achieved higher blood concentrations than older macrolides, but a large individual variation was observed. Diarrhea which was the only type of side effect observed in our cases, was encountered in 2 of 17 evaluable cases. From these data, RKM seems to have a place in the treatment of pediatric infectious diseases.

Campylobacter Infections↗
PubMed1988

[Clinical evaluation of sultamicillin fine granules in pediatric infections].

Sultamicillin fine granules (SBTPC), a mutual prodrug of sulbactam (SBT) and ampicillin (ABPC), were administered to 16 pediatric patients with bacterial infections. The efficacy rate was 93.3%. MICs (10(6) cells/ml) of SBTPC against beta-lactamase non-producing strains were not significantly different from those of ABPC, and ranged from less than or equal to 0.05 to 1.56 micrograms/ml. MICs of SBTPC, however, were 2-4 fold smaller than MICs of ABPC against beta-lactamase producing strains. Diarrhea and loose stool as side effects were observed in 4 (25%) of 16 patients, but none of them were severe. After oral administration of SBTPC (10 mg/kg), serum levels of ABPC and SBT peaked at 3.41 micrograms/ml and 2.43 micrograms/ml after 0.6 hour, and declined with half-lives of 1.79 and 1.00 hours, respectively.

Age Factors↗
PubMed1987

[Comparative, controlled study on an ampicillin suppository (KS-R 1) with an oral form of ampicillin in urinary tract infections].

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.

Administration, Oral↗
PubMed1987

[Clinical evaluation of flomoxef in children].

Flomoxef (FMOX, 6315-S), a new parenteral oxacephem antibiotic, was evaluated for its safety, efficacy and pharmacokinetics in children. Twenty-six patients with bacterial infections were treated with FMOX. Clinical efficacy rate was 92% and bacteriological cure rate was 85%. Three cases of infections due to methicillin-resistant Staphylococcus aureus were cured with FMOX therapy. No severe adverse reactions or abnormalities of laboratory test data were associated with FMOX therapy, although loose stools and diarrhea occurred frequently (23%). Serum half-lives of FMOX after a single bolus injection of 9 infants and children were 0.77 +/- 0.31 hour and excretion into urine was rapid. From these experiences, FMOX appeared to be a safe and effective antibiotic when used in children with susceptible bacterial infections.

Age Factors↗
PubMed1987

[Clinical and pharmacokinetic evaluations of cefuzonam in children].

A new parenteral cephalosporin antibiotic, cefuzonam (L-105, CZON), was evaluated for its safety, efficacy and pharmacokinetics in children. Twenty-two cases of bacterial infections including pneumonia, lung abscess, sepsis, urinary tract infection and soft tissue infections were treated with CZON. Clinical effective rate was 95%. Serum half-lives of CZON were 1.04-1.33 hours in children with normal renal and hepatic functions. Significant depressions of the normal fecal flora were observed and diarrhea or loose stool was encountered in 7 of the 22 treated cases (32%).

Adolescent↗
PubMed1987

[Pharmacokinetics and clinical effects of aspoxicillin in pediatric patients].

Since the efficacy and the safety of aspoxicillin (ASPC, TA-058) have been established on adult patients and the need of ASPC use on pediatric patients was anticipated, we performed a 16 center study on the clinical utility of ASPC in pediatric patients. 1. Pharmacokinetics ASPC was intravenously administered to 45 patients at a dose of 10, 20 or 40 mg/kg by one shot. Serum concentrations of ASPC were dependent of dose levels, and maximum levels of 58.4-230.8 micrograms/ml and half-lives (beta) of 1.08-1.16 hours were observed. Urinary recovery rates were 62.7-67.2% in 6 hours. Results obtained upon drip infusions (0.5-1 hour) were similar to one shot injections. 2. Clinical results (1) Clinical effectiveness Of 318 evaluable patients including 175 boys and 143 girls, 18.2% were nurslings and 61% were young children under 4 years of age. One hundred eighty six patients from whom causative organisms were isolated were classified as A group. Among them were 5 patients suffered with sepsis, but the ASPC treatment eradicated all the bacteria but Salmonella java in 1 case. All of 4 patients with meningitis were cured and all causative organisms (3 cases with Haemophilus influenzae and 1 case with Gram-positive coccus) were eradicated. Cure rates were 90% for 130 patients with respiratory tract infection, 88.6% for 35 with urinary tract infection, 85.7% for 7 with skin soft tissue infection and 89.8% for all the A group patients. Meanwhile, no causative organisms were isolated from 132 patients (B group patients) but cure rate of 91.7% was obtained for this group. No statistical difference was observed between A and B groups. For all the patients (318), the cure rate was 90.6%. (2) Bacteriological effects Of 63 Gram-positive bacteria isolated as pathogens, 58 strains were eradicated. Of 117 Gram-negative bacterial, 101 were eradicated. The eradication rate on all 180 strains was 88.3%. Overall, ASPC showed excellent effects against Streptococcus. Among strains of Staphylococcus aureus, 18 of 20 strains were eradicated. Of 59 strains of H. influenzae, 52 were eradicated and 3 decreased. Among strains of Escherichia coli, 25 of 28 strains were eradicated. Of Pseudomonas aeruginosa, 2 strains were decreased and one was unchanged. (3) ASPC was effective in 93.3% of 30 patients with serious infections and 79.2% of 72 patients with underlying diseases. Cure rates for patients with and without underlying disease were significantly different statistically (chi 2: P less than 0.005).(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1986

[Clinical evaluation of imipenem/cilastatin sodium in children].

Imipenem/cilastatin sodium (MK-0787/MK-0791) was evaluated for its safety, efficacy and pharmacokinetics in children. Thirty cases of bacterial infections were treated with MK-0787/MK-0791 at a daily dose of 40 to 222 mg/kg for 2.25 to 13 days. Clinical cure rate was 93% and bacteriological efficacy rate was 88%. Treated diseases included severe tonsillitis due to mixed anaerobic infections, pneumonia, sepsis, brain abscess and soft tissue infections. Two cases, one with periosteomyelitis due to methicillin-resistant S. aureus and the other with pulmonary abscess due to Haemophilus influenzae (other than type b), failed to respond to the MK-0787/MK-0791 therapy. The serum half-life of MK-0787 was 0.892 hour in children with normal renal functions. An episode of convulsions in a case of sepsis with bacterial croup and brain edema was considered to be associated with the MK-0787/MK-0791 therapy. From the present study, MK-0787/MK-0791 appears a safe and effective antibiotic when used in children with a variety of bacterial infections.

Bacteria↗
PubMed1986

[Pharmacokinetic and clinical studies with imipenem/cilastatin sodium in the pediatric field. Pediatric Study Group for Imipenem/Cilastatin Sodium].

Pharmacokinetic and clinical studies of imipenem/cilastatin sodium (MK-0787/MK-0791), a new carbapenem antibiotic and a dehydropeptidase-I inhibitor, respectively, were carried out in a joint study in the pediatric field by a study group consisting of investigators at 16 institutions. The results were summarized below. Pharmacokinetic studies Peak plasma concentrations of MK-0787/MK-0791 were 27.7-190.0/28.3-216.4 micrograms/ml at doses of 10/10-50/50 mg/kg administered by a 30 or 60-minute drip infusion. The above findings proved that dose response was clearly observed. Over a period of 6 or 7 hours, the urinary excretion of MK-0787 and MK-0791 totaled 54.2-88.0% and 53.6-89.0% of the dose administered, respectively. Plasma half-lives of MK-0787 and MK-0791 in the beta-phase were 0.87-1.05 hours and 0.59-0.95 hour, respectively. The cerebrospinal fluid (CSF) levels of MK-0787 in patients with purulent meningitis were 2.0-14.4 micrograms/ml; however, the penetration rate of the drug into the CSF was relatively poor in patients with normal meninges. Clinical study Clinical efficacy was evaluated in 283 patients. In 112 patients the daily dosage ranged from 30/30 mg/kg to 59/59 mg/kg, and in 138 patients it ranged from 60/60 mg/kg to 99/99 mg/kg. The maximum dose administered was 222/222 mg/kg. The drug was administered either 3 or 4 times per day. The clinical efficacy rate was 92.5% among 187 patients with identified etiologic pathogens. The drug was effective in 3 out of 4 patients with purulent meningitis and in 7 out of 10 patients with septicemia. The clinical efficacy rate was 96.7% in 90 patients with respiratory tract infection (pneumonia, lung abscess, etc.), 96.5% in 57 patients with urinary tract infection, 90.9% in 11 patients with SSTI. The clinical efficacy rate in those with no identified etiologic pathogen was 97.0% among 101 patients. Bacteriologically, the eradication rate for S. aureus was 87.9% of 33 isolates. Comprehensively, the eradication rate for Gram-positive bacteria was 94.7% of 75 isolates. The eradication rate for P. aeruginosa was 87.5% of 8 isolates. Including these strains, the eradication rate for Gram-negative bacteria was 90.3% of 134 isolates. The MK-0787/MK-0791 exhibited an eradication rate of 91.9% among a total of 211 Gram-positive and Gram-negative bacteria including anaerobes.(ABSTRACT TRUNCATED AT 400 WORDS)

Bacterial Infections↗
PubMed1986

[A comparative, well-controlled study of ceftizoxime suppository against ceftizoxime intravenous injection in infantile acute pneumonia].

We have attempted to clinically define the therapeutic usefulness of ceftizoxime suppository (CZX-S) in children with bacterial pneumonia, in a randomized trial. Intravenous injection of ceftizoxime (CZX) was used as the control. The results are summarized below. Subjects were inpatients with bacterial pneumonia, ranging in age from 9 months to 7 years and 10 months. As a rule, the daily dose was either four 250 mg (in potency) suppositories given at 6-hour intervals or 60 mg/kg body weight intravenous CZX (control) given in 4 injections at 6-hour intervals over a period of 7 days. The number of children in the study was 67. These children were divided into 2 dosage groups (suppository, 35; injection, 32) with matching pretreatment background factors. The severity of the target disease in the majority of the children was "moderate". The rate of therapeutic effectiveness was 97.1% for the suppository and 93.8% for the injection, and did not differ significantly between the 2 groups. Rates of efficacy by severity, presence or absence of underlying diseases, daily dose and/or complications were high without exception, and did not differ significantly between the 2 groups. Eradication rates for causative microorganisms, as studied in 16 children of each group, were both 93.8%. The 2 most frequently isolated causative organisms were Haemophilus influenzae and Streptococcus pneumoniae. Side effects were examined for 36 children of each group. The frequency of side effects did not differ significantly between the suppository group (2 with diarrhea and 1 with abdominal pain) and the injection group (1 with urticaria), and 8.3% and 2.8%, respectively. The frequency of abnormal laboratory test findings differed significantly (P less than 0.01) with respect to eosinophilia which occurred in 7 (20.6%) of the injected subjects but was not encountered in the subjects treated with suppositories. Other abnormal laboratory findings included thrombocytosis in 3 (14.3%) of the injection group and increased GOT in 1 (3.2%) of the suppository group. The suppository formulation of CZX appears to be a highly useful substitute for the injectable form, and should find a special use in children whose treatment with injections experiences some difficulty.

Abdomen↗
PubMed1986

[Bacteriological, pharmacokinetic and clinical evaluations of ceftriaxone in the pediatric field. Pediatric study group of ceftriaxone].

UNLABELLED: Ceftriaxone (CTRX), a new injectable cephem antibiotic agent, was evaluated bacteriologically and clinically for its efficacy and safety in the pediatric field by a study group organized with pediatricians from all over the country. The following are a summary of the results of the evaluation. Antibacterial effects: The inhibition of growth was attained for over 90% of strains of K. pneumoniae, H. influenzae and Salmonella spp. at the concentration of 0.10 micrograms/ml and of strains of S. pneumoniae and E. coli at the concentration of 2.0 micrograms/ml. The CTRX was proved to have excellent antibacterial effects. Absorption and excretion: Thirty minutes after one shot intravenous administration with 10, 20, 40 and 50 mg/kg of CTRX, its serum levels were 73, 124, 169 and 190 micrograms/ml, respectively, a clear tendency of dose-response relationship being noticed. The serum levels decreased only gradually and stayed as high as 10 to 20 micrograms/ml even after 12 hours. The half-lives of the drug were 5.5, 6.3, 6.0 and 4.7 hours for the 4 different dose levels, respectively. Following the intravenous injection with 10, 20 and 40 mg/kg, the urinary excretion rates were 55, 52 and 54%, respectively. Following the one shot intravenous administration or by the drip infusion for 30 minutes with about 50 mg/kg, CTRX levels in the cerebrospinal fluid ranged from 1 to 20.3 micrograms/ml in case of purulent meningitis (5 to 10 micrograms/ml in most cases). CLINICAL RESULTS: A total of 322 cases was enrolled. The efficacy of CTRX was evaluated in 295 cases out of the 322, excluding drop-outs and the cases which did not meet the protocols. The clinical efficacy rate was 94% of 191 cases where the causative bacteria were identified, CTRX being "excellent" in 108 cases and "effective" in 72. In the remaining 104 cases where the causative bacteria were not identified, the efficacy rate was 92%, CTRX being "excellent" in 42 cases and "effective" in 54. Furthermore, the efficacy rate was 89% of 18 cases infected with more than one kind of bacteria. The drug showed "excellent" or better effectiveness in 88% of 75 cases which had not responded to other antibiotics. Bacteriologically, 174 out of 216 strains (93%) which were judged to be causative bacteria disappeared with the use of CTRX. Eighty-five percent of 53 strains which had not responded to other antibiotics disappeared by the CTRX treatment.(ABSTRACT TRUNCATED AT 400 WORDS)

Adolescent↗
PubMed1986

Synthesis of C-5' chirally deuterated nucleosides with 100% optical purity.

The syntheses of chirally pure (5R)- and (5S)-[5-2H1]-D-ribose and (5R)-(5-2H1)-3-C-methyl-D-ribose and the syntheses of chirally pure (5'R)- and (5'S)-[5-2H1]-adenosine and (5'R)-[5'-2H1]-3'-C-methyladenosine are described. The 1H-NMR characteristics of these nucleosides and the mechanism of the reaction of adenosine and thionyl chloride-hexamethyl phosphoric triamide (HMPA) are also described. The stereospecific presence of deuterium in these nucleosides permits specific assignments for the resonances of 5'-protons. From the observed spin-spin coupling between H5' and H4', the estimates have been made of the rotamer population of the exocyclic 5'-carbinol groups of these nucleosides. It is shown that these nucleosides exist in gauche-gauche rotamer (ca. 70%) in aqueous solution. The SN2 mechanism of the chlorination reaction is suggested.

Deuterium↗
PubMed1986

[Clinical evaluation of cefixime in children].

A new beta-lactamase-stable oral cephem antibiotic, cefixime (CFIX), was evaluated for safety, efficacy and pharmacokinetics in children. CFIX was effective in 19 of 20 cases (95%) with bacterial infections. The drug was especially effective against the cases of pneumonia due to beta-lactamase-producing H. influenzae or B. catarrhalis. Pharmacokinetic parameters of CFIX (3 mg/kg) with premeal administration were as follows: Kel 0.328 +/- 0.066 hr-1, T 1/2 2.14 +/- 0.36 hrs, AUC 10.9 +/- 8.7 micrograms X hr/ml, and Vd/F 1.64 +/- 1.42 L/kg. In most of the cases tested, the urinary excretion rate in 12 hours was 5 to 17%. A dose of 3 mg/kg twice daily seems to be adequate for a regular treatment.

Bacterial Infections↗
PubMed1986

[Pharmacokinetic and clinical studies on cefuzonam in the pediatric field].

A multi-center open study was conducted to investigate cefuzonam (L-105, CZON), a newly developed cephalosporin from pharmacokinetic, bacteriological and clinical aspects, in the pediatric field with the participation of 17 institutions and their related facilities. The results are summarized as follows. Serum concentrations and urinary excretion. The pharmacokinetics in pediatric patients was investigated with a dose of 20 mg/kg, via one shot intravenous injection or intravenous drip infusion over 1 hour. The results were nearly the same as those in adult patients. Mean serum concentrations 5 minutes after one shot intravenous injections were: 52.8 micrograms/ml with the dosage of 10 mg/kg, 135 micrograms/ml with 20 mg/kg, and 317 micrograms/ml with 40 mg/kg, and T1/2 beta's for the 3 dosages were 1.07 hours, 0.91 hour, and 1.01 hours, respectively. With 1-hour intravenous drip infusion, mean serum concentrations at the end of infusion were: 22.4 micrograms/ml with 10 mg/kg, 46.3 micrograms/ml with 20 mg/kg, 72.5 micrograms/ml with 40 mg/kg, and 69.2 micrograms/ml with 50 mg/kg, and T1/2 beta's for these dosages were 1.31 hours, 1.45 hours, 0.84 hour, and 0.66 hour, respectively. In 6 hours after administration of CZON, urinary excretion rates were 43.5-51.4% for one shot intravenous injections of 10-40 mg/kg, and 42.7-58.6% for 10-50 mg/kg drip infusions. Concentrations in cerebrospinal fluid Penetrations into cerebrospinal fluids in patients with purulent meningitis achieved levels of 2.80-6.40 micrograms/ml with the administration of CZON at 100 mg/kg in acute cases of within 6 days after onset. When the administration of the drug was done at the earlier stage, the greater penetration occurred. However, rates of penetration were 3.10% to 5.03% within 4 days after a drug administration, thus, the penetration was not thought to be as good as other beta-lactam agents which achieve higher penetration rates. Clinical results Of 407 cases treated with CZON, 18 cases were excluded from the statistical analysis. The remaining 389 cases plus 8 cases each of which had 2 complicated diseases, with a total of 397, were statistically analyzed for the clinical effectiveness of this drug against various infections. The efficacy was evaluated as "good" or "excellent" in 248 out of 266 cases from which pathogens were isolated, for an efficacy rate of 93.2%. The efficacy rate was 88.5% for 131 cases for which pathogens were unidentified, thus no statistically significant difference was noted between the 2 groups.(ABSTRACT TRUNCATED AT 400 WORDS)

Ceftizoxime↗
PubMed1985

Taste response to 2,5-anhydro-D-hexitols; rigid stereospecificity of the furanose site in the sugar receptor of the flesh fly.

2,5-Anhydro-D-mannitol with a fixed furanose ring stimulated the sugar receptor of the flesh fly and reacted with the furanose site. This is the first direct evidence that a furanose can stimulate the sugar receptor and supports strongly the assumption that beta-D-fructofuranose is the only stimulatory component in the solution of D-fructose. Rigid stereospecificity of the furanose site in the sugar receptor is discussed according to the effectiveness of various synthetic 2,5-anhydro-D-hexitols and related compounds. At least four receptor sites are concluded to be in a single sugar receptor: a pyranose (P) site, a furanose (F) site, an aliphatic carboxylate (R) site and an aromatic amino acid (Ar) site.

Animals↗
PubMed1985

[Clinical and pharmacokinetic evaluations of ceftizoxime suppositories in children].

Ceftizoxime suppository (CZX-S) was evaluated for its safety, clinical efficacy and pharmacokinetics in pediatric patients. The Cmax, 4.8 to 9.5 micrograms/ml, was obtained 15 to 30 minutes after administration of CZX-S, and the serum half-life was 0.93 hour. Cross-over comparison with intramuscular CZX in a child showed approximately one-third bioavailability of the suppository against intramuscular injection. CZX-S was effective in all the 26 bacterial infections including acute pharyngitis, pneumonia, soft tissue infection, and urinary tract infections. The causative organisms were eradicated in 95%. Mild diarrhea (17%) was the only side effect observed in the study. The data suggest that CZX-S is an excellent alternative to oral and injectable antibiotics for the treatment of mild to moderate bacterial infections due to the susceptible organisms.

Bacteria↗
PubMed1985

[Bacteriological, pharmacokinetic and clinical studies on aztreonam in the pediatric field. Pediatric Study Group of Aztreonam].

This report summarizes the results of joint studies in pediatrics on aztreonam, the first monobactam antibiotic for practical use. Pharmacokinetics was studied in 53 cases administered with 10, 20, 40 and 50 mg/kg of aztreonam (AZT) by intravenous injection and 20 cases with 10, 20, 30, and 40 mg/kg by drip infusion. All the cases had normal hepatic and renal functions at the administration. T1/2 was in a relatively fixed range of 1.35-1.56 hours in intravenous injection cases and 1.30-1.55 hours in drip infusion. One hour after commencing administration of standard 20 mg/kg, the serum concentrations were 50.18 +/- 4.24 micrograms/ml in intravenous injection and 116.33 +/- 10.18 micrograms/ml in drip infusion and even 6 hours after the end of the administration, they were 5.80 +/- 1.16 micrograms/ml and 3.38 +/- 0.58 micrograms/ml, respectively. The cerebrospinal fluid penetration was studied on suppurative meningitis (5 cases) and nonbacterial meningitis (3 cases). The penetration was generally good with sufficient concentration for meningitis caused by E. coli and H. influenzae. Amount of the penetration decreased as the cases were improved. Twenty-nine (29) cases were excluded and 262 cases of total 291 were clinically assessed, and the pathogen-isolated 167 cases of 262 were principally analyzed. Efficacy of AZT was "excellent" for all 3 cases of E. coli sepsis and 1 case of N. meningitidis meningitis and "good" for 1 case of H. influenzae meningitis. The effective rate was 94.6% for 37 pneumonia cases, 94.7% for 76 UTI cases and 88.5% on the whole including as many as 98 "excellent" cases. However, the effective rate for 21 enteritis cases was only 52.4%. Similar trend was observed in the pathogen-unknown group and overall effective rate of total 267 cases was 86.8%. The clinical effect by pathogen was 97.7% for 44 E. coli cases and 97.1% for 34 H. influenzae cases, showing excellent results for the GNB group. AZT was also effective for 8 out of 11 P. aeruginosa cases. With regard to microbiological effect by pathogen, AZT showed a high rate of bacterial elimination for GNB, primarily 98.1% for E. coli and 100% for H. influenzae followed by 76.9% for P. aeruginosa. However, it was only 30.0% for Salmonella. Excluding the Salmonella cases, GNB elimination rate was 93.5%. Clinical and microbiological dose response was not clear partly because, same as the previous studies, the effective rate of AZT was high. It was considered, however, standard dose of 20 mg/kg X 3 approximately 4 times a day was recommendable.(ABSTRACT TRUNCATED AT 400 WORDS)

Age Factors↗