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PubMed1994

[Azithromycin in the treatment of syphilis].

The results of the use of azithromycin (sumamed) in the treatment of 100 patients with fresh syphilis were analyzed. The antibiotic was used in accordance with two treatment schemes: 500 mg daily for 10 days and 500 mg every two days. The total course dose was 5 g in both the cases. The results of the treatment with azithromycin were compared with those of the treatment with erythromycin (30 g) and penicillin (300,000 U every 3 hours for 16-28 days depending on the disease stage). The results were estimated by the rate of the elimination of Treponema pallidum and syphilids as well as by the time course of the seroreactions. The analysis provided a conclusion that the therapeutic efficacy of sumamed in the treatment of patients with fresh manifest syphilis was high: by comparison with penicillin and erythromycin it more rapidly eliminated the clinical signs of syphilis and in the majority of the cases induced negativation of the cutaneous serological reactions within the first 4 months of the treatment.

Adolescent↗

PubMed1994

Azithromycin in the treatment of pneumonia caused by Chlamydia pneumoniae: report of a case.

We report a 67-year-old male with pneumonia in which Chlamydia pneumoniae was identified by serologic studies as the causative agent. After initial treatment failure with amoxicillin + clavulanic acid, pneumonia was successfully treated with the administration of oral azithromycin, 500 mg per day, for three days. Azithromycin is a new macrolide which has a long half-life and superior action to erythromycin. It provides a new and alternative choice in the treatment of Chlamydia pneumoniae infection in the future.

Aged↗

PubMed1994

[Effectiveness of and tolerance to azithromycin versus roxithromycin in the treatment of patients with acute infections of the upper respiratory tract].

A multicenter open prospective comparative study was carried out during two years enrolling 60 patients with upper respiratory infections. Thirty were treated with single daily 500 mg doses of azithromycin for three days, and 30 received two daily doses of roxithromycin of 150 mg each for seven days. Both treatments were equally well tolerated, and there was no substantial difference concerning clinical recovery. However, azithromycin treatment was more practical and of shorter duration.

Acute Disease↗

PubMed1995

[Effect of the molecular structure of azithromycin on pharmacokinetics and the antimicrobial activity].

Azithromycin possesses in position 9 of the lactone cycle a nitrogen atom which provides a second site of protonation. Hence, and compared to erythromycin, azithromycin is more stable in the gastric environment, enjoys improved digestive absorption and improved digestive toleration, displays much higher intracellular accumulation responsible for prolonged serum and tissue half-lives, which allows simplified therapeutic schedules. It is also postulated that improved activity against Gram negative isolates such as H. influenzae and B. catarrhalis results from the same structural particularities.

Anti-Bacterial Agents↗

PubMed1995

Azithromycin drug interactions.

Pre clinical work in vivo and in vitro have suggested that azithromycin has a low potential for significant drug interactions. Clinical studies conducted thus far have generated results in accordance with the preclinical science [6]. Direct comparisons with the most modern macrolides have been published and evidence suggests that azithromycin is likely to be associated with fewer significant drug interactions. However, as a final point, I wish to point out that proof of an absolute negative is not possible and therefore in any patient, on multiple medication with adverse findings, a drug interaction should be considered as part of the differential diagnosis.

Anti-Bacterial Agents↗

PubMed1995

[Use of azithromycin in ORL].

If the demonstration of the interest to treat beta-haemolytic streptococcal pharyngitis is not to be done, the recommended antibiotics, most of the time, display the drawback of a treatment with one to three intakes daily for 10 days. The azithromycin, with its numerous properties, allows for the required treatment duration, to decrease the intakes number, thus facilitating the compliance. Its in vitro activity is very good on streptococci with a MIC90 of 0.06 mg/l. Its in vivo activity in animal, with experimental Streptococcus pyogenes infection models is identical to the amoxicillin activity, and better than those of other tested macrolides. One of the major characteristics of azithromycin in man is its most peculiar pharmacokinetic with an extended half life and very high tonsillar concentrations, for at least 10 days after the administration of the product at the 1.5 g dose regimen over 3 days. In streptococcal acute tonsillitis clinical studies, with a 1.5 g dose regimen over 5 days, clinical results and bacterial eradication are identical to those obtained in the Penicillin V groups. This administration facility should greatly improve the treatment compliance and lower the risks of a prematurely discontinued treatment.

Animals↗

PubMed1995

[Effects of azithromycin on the virulence of Pseudomonas aeruginosa].

Pseudomonas aeruginosa is a saprophyte opportunistic bacteria which frequently colonizes the respiratory tract of patients presenting a severe chronic bronchitis pathology. Secreting a number of exotoxins and enzymes inducing an inflammation and necrosing of the surrounding tissues, it provokes irreversible pulmonary lesions. Different experimental in vitro works evidenced macrolides activity on the production and/or secretion of these factors, with a diminution of elastase, protease, lecithinase and D-nase synthesis. Among the macrolides, azithromycin seems to have the most pronounced activity. In vivo, some patients suffering from bronchiolitis or cystic fibrosis have been clinically improved with a treatment using erythromycin, or clarithromycin or azithromycin. These very preliminary results demand to be confirmed but the macrolides could allow a decrease of Pseudomonas aeruginosa pathogenicity and thus stop the deterioration of pulmonary functions.

Anti-Bacterial Agents↗

PubMed1997

Azithromycin in the treatment of chlamydial cervicitis and eradication of Ureaplasma urealyticum in female lower genital tract.

From May 1995 to May 1996, thirty-six females with chlamydial cervicitis were enrolled at Bangrak Hospital's Venereal Disease Clinic in an open study to assess the efficacy and safety of a single, 1-gram oral dose of azithromycin. Thirty-five had positive C. trachomatis and one had a positive Gen-probe test. Twenty-two returned for their first and second follow-ups and 18 came back for their final follow-up (visit 4). Eradication rate was 100 per cent on all visits. Fourteen patients were excluded from the final analysis- three had dropped out from the beginning, ten had sexual intercourse without a condom and one had a positive Gen-probe test but negative C. trachomatis culture. U. urealyticum was isolated from the vaginal wall of 15 of the 36 cases and eradication rate was 0 per cent at visit 2 and visit 4. In conclusion, this study shows that a single, 1-gram oral dose of azithromycin is an effective and well-tolerated alternative therapy for chlamydial cervicitis.

Adolescent↗

PubMed1997

Intracellular activity of azithromycin against Mycobacterium avium complex in human macrophages.

In the concentration range examined (0.5-16 micrograms/ml) the azalide antibiotic azithromycin (CAS 83905-01-5, Zithromax) inhibited the growth of mycobacteria in macrophages over 7 days. The higher concentrations of azithromycin, 8 and 16 micrograms/ml, reduced the number of phagocytized bacteria in macrophages by at least 1 log unit within 4 days. The system used, macrophages from healthy volunteers, is suitable for testing the intracellular activity of drugs against the Mycobacterium avium complex.

Anti-Bacterial Agents↗

PubMed1997

Azithromycin in non-gonococcal urethritis.

The efficacy and safety of a single 1 g oral dose of azithromycin was evaluated in 100 male patients with non-gonococcal urethritis (NGU). Enrolled were men with > or = 5 polymorphonuclear leukocytes (PMNL)/high power field (HPF) (x 1000 magnification) in a Gram-stained smear of urethral discharge with or without symptoms and signs of NGU. Of the 66 evaluable patients, Chlamydia trachomatis was isolated from 18 cases (27.3%) and Ureaplasma urealyticum from 12 cases (18.2%). After treatment, signs and symptoms disappeared from 59 cases (89.4%). Forty-four cases (66.7%) showed reduced PMNL/HPF. C. trachomatis was eradicated in 18 cases (100%) and U. urealyticum in 12 cases (83.3%). One patient complained of mild dizziness, moderate nausea, and palpitations. Single 1 g oral dose of azithromycin appears to be effective and safe for treating chlamydial, non-chlamydial, and ureaplasmal NGU. In addition, its ease of use encourages patient compliance.

Administration, Oral↗

PubMed1997

[Omeprazole and azithromycin with and without metronidazole in the eradication of Helicobacter pylori in duodenal ulcer disease].

This prospective, single blind, randomized study was designed to compare the efficacy and tolerance of two therapeutic schedules for eradication of H. pylori in patients with duodenal ulcer. Patients were randomized into two groups. Group 1 (n = 25) was treated with omeprazole 20 mg each morning for 28 days, azithromycin 500 mg/day for 5 days and metronidazole 3 x 500 mg/day for 5 days. Group 2 (n = 25) was treated with omeprazole 20 mg/day for 28 days and azithromycin 500 mg/day for 5 days. H. pylori status was determined by rapid urease test and histology before and 1, 6 and 12 months after the therapy. After 4 weeks of treatment ulcers healed in 96% (24/25) of patients in the first group and in 92% (23/25) of patients in the second group. One and 12 months after the treatment, eradication of Helicobacter pylori was achieved in 72% (18/25) of patients in the first group and in 64% (16/25) of patients in the second group. In 12 months after the treatment ulcer recurred in 43.7% (7/16) of patients in whom H. pylori was not eradicated and in 2.9% (1/34) of patients with eradicated H. pylori. The side effects were minor and/or transitory and did not require discontinuation of the treatment.

Adult↗

PubMed1998

[Treatment of pneumonia caused by Legionella with azithromycin].

Nineteen patients with pneumonia caused by Legionella, who did not need to be admitted to ICU were treated with 500 mg/day of azithromycin. The etiological diagnosis was made retrospectively by detecting Legionella pneumophila in the urine of nine patients and/or by serology (seroconversion or single titer 1/256) in 19 cases. None of them met the criteria for ICU admittance nor had received prior treatment with antibiotics which were potentially active against L. pneumophila. Serology tests and radiography of the thorax were carried out on all the patients in the study during their convalescence period. The average age (+/- SD) of the group was 58.5 +/- 16.2 years. The average respiratory frequency (+/- SD) 26 +/- 6 breaths per minute; the radiologic extension was of one lobule in 18 cases and two lobules in one case. No patients showed bilateral disease. Arterial gasometry (FiO2 0.21) showed a pO2 average of (+/- SD) 53 +/- 14 mmHg and the hemogram an average of 6.700 leukocytes/mm3 (range: 4,200-41-800). All the patients progressed favorably. The average duration of fever was 1.8 days; the average stay (+/- SD) was 6.1 +/- 2 days. The treatment was well tolerated. One month after discharge radiographies were clear for all patients. There were no relapses. In conclusion, 3-day administration of azithromycin was found to be a useful guide in the treatment of community acquired pneumonia caused by Legionella in patients whose clinical situation does not require ICU administration and allows for oral administration.

Adult↗

PubMed1998

In-vitro susceptibility of group A beta-haemolytic streptococci (GABHS) to penicillin, erythromycin, clarithromycin and azithromycin in Styria, Austria.

248 Strains of group A beta-haemolytic streptococci (GABHS) were tested against penicillin and the macrolide antibiotics, erythromycin, clarithromycin and azithromycin. 213 (85.9%) GABHS isolates were taken from throat swabs from patients with pharyngotonsillitis, 35 isolates (14.1%) were from other body sites or from invasive infections. The age of the patients ranged from 9 months to 89 years, 155 of the patients (62.5%) were below 10 years of age. The results of the E-test method and a disk diffusion assay were compared; to classify the phenotype of the erythromycin-resistant strains, a disk induction test was carried out. None of the 248 GABHS strains showed resistance to penicillin, whereas 53 GABHS isolates (21.4%) were resistant to the macrolide antibiotics included in the test. There were only minor discrepancies between the two testing methods. The MIC data obtained with the E-test method suggested that among the macrolides, erythromycin and clarithromycin had slightly higher antistreptococcal activity than azithromycin in vitro. 50 (94.3%) of the erythromycin-resistant GABHS showed the pattern of novel resistance (M phenotype), 2 (3.8%) strains showed inducible resistance (IR) and 1 (1.9%) strain exhibited consecutive resistance (CR).

Adolescent↗

PubMed1993

Susceptibility of Mycobacterium kansasii to ofloxacin, sparfloxacin, clarithromycin, azithromycin, and fusidic acid.

The MICs of ofloxacin, sparfloxacin, clarithromycin, azithromycin, and fusidic acid for clinical isolates of Mycobacterium kansasii were determined by the radiometric (BACTEC) method. All drugs except azithromycin elicited MICs for 90% of the strains tested that were lower than previously reported achievable maximum concentrations in serum. Ofloxacin, sparfloxacin, and clarithromycin had the largest maximum concentration in serum/MIC for 90% of strains ratio of the drugs tested.

4-Quinolones↗

PubMed1994

Susceptibility of Neisseria gonorrhoeae associated with pelvic inflammatory disease to cefoxitin, ceftriaxone, clindamycin, gentamicin, doxycycline, azithromycin, and other antimicrobial agents.

We determined the susceptibilities, by the agar dilution method, of 84 recent clinical isolates of Neisseria gonorrhoeae obtained from women with pelvic inflammatory disease in the United States to the following antimicrobial agents: penicillin, cefoxitin, cefotetan, ceftriaxone, ceftizoxime, cefixime, tetracycline, doxycycline, ciprofloxacin, ofloxacin, erythromycin, azithromycin, clindamycin, and gentamicin. Twenty-five percent of the isolates were resistant to penicillin and 20% were resistant to tetracycline. In comparison, doxycycline was more active than tetracycline and azithromycin was more active than erythromycin in vitro. Ceftriaxone, ceftizoxime, and cefixime were equally active against penicillin-susceptible isolates, but they had different in vitro activities against gonococcal isolates possessing chromosomally mediated resistance to penicillin. Overall, cefoxitin was slightly more active than cefotetan and ciprofloxacin was more active in vitro than ofloxacin, especially against N. gonorrhoeae with chromosomally mediated resistance. Criteria for the interpretation of susceptibility data for N. gonorrhoeae are not available for clindamycin or gentamicin, but for at least half of all isolates, including penicillin-susceptible isolates, at least 4 micrograms of clindamycin or gentamicin per ml was required to inhibit growth in vitro.

Anti-Bacterial Agents↗

PubMed2003

Treatment of cast bronchitis with low-dose oral azithromycin.

Cast or plastic bronchitis is an unusual disorder that is rarely encountered in the pediatric population. It is characterized by the expectoration of large, branching plugs of airway debris. These "casts" conform to the shape of portions of the tracheobronchial tree, and give the disorder its name. Cast bronchitis is typically seen in association with several primary pulmonary disorders and cyanotic congenital heart disease. It can be classified as inflammatory or acellular, based on the histologic characteristics of the casts. The presence of large, obstructive plugs filling the airways of lobes or entire lungs can result in a variety of clinical signs and symptoms, and may ultimately lead to respiratory failure and death. Conventional treatment of cast bronchitis has focused on the clearance of obstructing material from the airways combined with therapy for any underlying cardiopulmonary disease. Unfortunately, this approach has not proven very effective, and patient mortality remains high. We report on a case in which a patient with cast bronchitis was treated with long-term, low-dose oral azithromycin. This therapy resulted in clinical, spirometric, and radiographic improvement of the patient.

Adolescent↗

PubMed2002

Azithromycin, a lysosomotropic antibiotic, has distinct effects on fluid-phase and receptor-mediated endocytosis, but does not impair phagocytosis in J774 macrophages.

Pretreatment of J774 mouse macrophages by the dicationic macrolide antibiotic, azithromycin (AZ), selectively inhibited fluid-phase endocytosis of horseradish peroxidase and lucifer yellow, but not phagocytosis of latex beads. AZ delayed sequestration of receptor-bound transferrin and peroxidase-anti-peroxidase immune complexes into cell-surface endocytic pits and vesicles, but did not slow down the subsequent rate of receptor-mediated endocytosis. AZ down-regulated cell surface transferrin receptors, but not Fc gamma receptors, by causing a major delay in the accessibility of internalized transferrin receptors to the recycling route, without slowing down subsequent efflux, resulting in redistribution of the surface pool to an intracellular pool. Acidotropic accumulation of AZ was associated with an extensive vacuolation of late endosomes/lysosomes, and these compartments became inaccessible to horseradish peroxidase and immune complexes, but not to latex beads. The inhibitory profile of AZ cannot be solely accounted for by vacuolation and interference with acidification. AZ may help in dissecting various steps of the endocytic apparatus such as lateral mobility of receptors at the plasma membrane, formation of clathrin-independent endocytic vesicles, orientation of transferrin receptors into the recycling route, and fusogenicity with lysosomes.

Animals↗

PubMed1998

Function of human alveolar macrophages after a 3-day course of azithromycin in healthy volunteers.

Azithromycin (AZM) is a new macrolide antibiotic with a high intracellular/extracellular concentration ratio. Immunomodulatory and antiinflammatory properties have been reported with other macrolides, especially erythromycin. The aim of the present study was to evaluate the effect of AZM on the production of proinflammatory mediators by alveolar macrophages (AM) up to 4 weeks after a 3-day course of AZM (500 mg, once a day). Nineteen non-smoking healthy male subjects were investigated with bronchoscopy and bronchoalveolar lavage. Group 1 received no treatment. Groups 2, 3, and 4 were bronchoscoped 1, 7 and 30 days, respectively, after AZM administration. AZM concentrations were simultaneously measured in plasma and in AM extracts. In serum, AZM levels were higher in group 2 (32.8 +/- 14.2 micrograms/l), at the lower limit of detection in group 3 (2.8 +/- 1.7 micrograms/l), and no longer detectable in group 4. In AM extracts, the highest concentrations were measured in group 2 (51.6 +/- 28.3 ng/microliter) and in group 3 (31.8 +/- 17.2 ng/microliter), and were detected up to 30 days after treatment in group 4 (2.9 +/- 2.3 ng/microliter). There was no significant differences between groups for blood or BAL proinflammatory cytokines levels (TNF-alpha, IL-1 beta, IL-6), and for superoxide generation by AM. We conclude that a 3-day course of AZM 500 mg/day in healthy subjects does not alter the proinflammatory cytokine profile in blood and in AM despite the prolonged tissue impregnation by this drug.

Adolescent↗