Azithromycin (AZM), a new macrolide antibiotic, in fine granules and in capsules was studied for pharmacokinetic and clinical evaluation in the pediatric patients.
Antibacterial activity of AZM against 43 clinical isolates: AZM exhibited slightly lower activity against Gram-positive bacteria and 2-8-fold higher activity against Gram-negative bacteria than erythromycin or clarithromycin.
Plasma or urine samples were collected from eight patients receiving the drug in fine granular form, and two patients receiving it in capsules for the determination of drug levels. The elimination half-lives of AZM after administration at dose of 10mg/kg/day for 3 days were 50.0 and 51.2 hours for fine granules, and 41.5 hours for capsules. AUC0.was 11.7 and 24.3μg·Ehr/ml for fine granules, and 8.3μg·Ehr/ml for capsules. The cumulative excretion rates up to 120 hours after the start of treatment were 8.24 and 13.84% for fine granules, and 3.83% for capsules.
AZM was administered to 123 patients once daily at 3.7-20.0mg/kg body weight over 3 to 5days with reference to the standard dose of 10mg/kg. The drug was used to treat patients with pharyngitis, tonsillitis, scarlet fever, pneumonia, mycoplasmal pneumonia, chlamydial pneumonia, otitis media, pertussis, intestinal infection, and SSTI. The effectiveness of AZM was evaluated in 109 cases. The drug was rated “excellent” in 65.1% of the patients and “good” in 29.4%, resulting in an efficacy rate of 94.5%. Furthermore, AZM eradicated 43 of 46 (93.5%) bacteria that had been identified before the treatment.
Three patients complained of side effects of urticaria (1 case) and diarrhea (2 cases).
Abnormal laboratory changes were reported as follows: decreased leukocyte (3 cases), increased eosinophil (5), increased platelet (2), increased eosinophil and platelet, elevated GPT (1), and elevated GOT and GPT (1). The abnormalities, however, were mild enough to raise no clinically significant problems.
In conclusion, AZM in once daily regimen was effective and safe in treatment of pediatric infections.

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Azithromycin (AZM) was studied for its clinical efficacy in pediatric infections.
The study on AZM was carried out in 43 patients whose diagnoses were given as follows: pharyngitis in five cases, tonsillitis in one, bronchitis in four, pneumonia in four, Mycoplasma pneumonia in 14, scarlet fever in nine, impetigo in four, pyodermia in one and Campylobacter enteritis in one. The patients received AZM once daily at 1.6-20.0mg/kg body weight for three to five days. Effectiveness of AZM was evaluated in 39 cases and the drug was rated “excellent” in 15,“good” in 19,“fair” in one,“poor” in four, resulting in an efficacy rate of 87.2%.
Twenty bacterial isolates were identified as causative isolates in 19 patients: Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Haemophilus influenzae, Campylobacter jejuni and Mycoplasma pneumoniae. AZM eradicated 16 isolates but four persisted after therapy.
One patient complained of loose stool, while two patients were found with decreases in white blood cell counts, and seven showed increases in eosinophils. However, no serious case of adverse event was reported.

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Azithromycin (AZM), a newly developed azalide antibiotic, was administered at a standard dose of 10mg/kg once daily for 3 days to pediatric patients with bacterial infections and the therapeutic efficacy of AZM was investigated.
1. A total of 12 patients with the following diseases was evaluated: pharyngitis in two, tonsillitis in four, bronchitis in one, Mycoplasma pneumonia in one, scarlet fever in two and enteritis in two. The drug was rated “excellent” in eight cases and “good” in four.
2. Eleven strains were isolated from patients: five strains of Streptococcus pyogenes, four strains of Haemophilus influenzae, and two strains of Haemophilus parainfluenzae. Isolated bacteria were eradicated in eight strains and persisting in one, resulting in 88.9% in eradication rate. No follow-up examinations in post-treatment were performed in two cases.
3. No adverse reaction was reported, while one case of eosinophilia was noted as an abnormal laboratory test value.
4. As far as compliance is concerned, patients claimed that the formulation of the drug is “easy to take” or “ordinary”.
With the results presented as above, we have concluded that AZM is a useful antibiotic in pediatric patients with bacterial infections.

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Azithromycin (AZM) was orally administered to 12 pediatric patients with the following bacterial infections: pharyngitis in four cases, tonsillitis in one, pharyngo-bronchitis in two, and mycoplasmal pneumonia in five.
In eleven of the twelve cases (91.7%) was the drug found effective. Neither abnormal clinical findings nor abnormal laboratory test results changes were observed.
Eleven of the twelve pediatric patients claimed that the formulation of the drug is easy to take.
The above results suggest that AZM is a useful antibiotic drug in the treatment of pediatric patients with bacterial infections.

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Fine granules or capsules of azithromycin (AZM) were given to 32 pediatric patients for the treatment of the following diseases: pharyngitis in three cases; tonsillitis in one; bronchitis in six; pneumonia in six; mycoplasmal pneumonia in 14; pertussis and enteritis in one, each. Effectiveness of AZM was evaluated in 30 cases and the drug was rated “excellent” in 18 patients, “good” in 11 and “fair” in one, resulting in a total efficacy rate of 96.7%.
Three strains of bacteria were isolated from 3 patients as the causative organisms including: Streptococcus pneumoniae, Haemophilus influenzae and Haemophilus parainfluenzae, from three different patients, respectively.
One patient complained of mild diarrhea, another patient mild urticaria. Abnormal laboratory test results were reported as follows: one patient showed a slight decrease in leukocyte count, three patients showed slight increases in eosinophils, and one patient had slight elevations in GOT and GPT.
The above results suggest that AZM is a useful antibiotic drug in the treatment of pediatric patients with various bacterial infections.

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[in Japanese]

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Cefetamet pivoxil (CEMT-PI), a drug of pivaloyloxymethyl group, was investigated for its impact on the carnitine blood homeostasis and renal excretion upon administering CEMT-PI alone, and CEMT-PI simultaneously with carnitine.
500mg of CEMT-PI (group A) and 500mg of CEMT-PI and an equimolar amount (200mg of carnitine) of levocarnitine chloride (group B) were administered twice a day for 7 and 1/2 consecutive days to 5 healthy volunteers (group A) and 3 healthy volunteers (group B).
No serious side effects nor abnormal values in physical and laboratory tests were observed throughout the study in both groups.
During the treatment period, plasma total carnitine decreased slowly down to 25.5μm (group A) and 38.8μm (group B) and plasma free carnitine reached steady state levels at 17.7μm (group A) and 29.2μm (group B) on day 5. These concentrations represent 45 and 37% in group A, 66and 58% in group B of the average pre-treatment baseline levels. Plasma pivaloylcarnitine quickly reached plateau levels of 6.12μm (group A) and 4.05μm (group B) on day 4. After treatment stop, plasma total and free carnitine returned to the pretreatment baseline level within 5 days (group A) and 3 days (group B), and plasma pivaloylcarnitine was detectable until day 7 of the treatment-free follow up in both groups. Although carnitine was given concurrently at a dose equimolar to the ingested amount of pivalic acid in group B, the plasma total and free carnitine exhibited a decrease. This was considered attributable to the fact that the bioavailability of carnitine is as low as 16% when administered orally, which is considerably less compared to the 55% bioavailability of cefetamet pivoxil.

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