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PubMedDate not supplied

Liposomes as carriers of macrolides: preferential association of erythromycin A and azithromycin with liposomes of phosphatidylglycerol containing unsaturated fatty acid(s).

To assess the most favourable phospholipid composition of a liposomal carrier for antibiotics, small multilamellar liposomes were prepared from phosphatidylcholine, phosphatidylethanolamine and phosphatidylglycerol of varying fatty acid composition in the presence of erythromycin A and azithromycin. Crude liposomes were subjected to Sepharose CL-4B column chromatography, and liposomes containing antibiotics were well separated from free antibiotics. These experiments established that the greatest association of antibiotics was achieved with liposomes prepared from phosphatidylglycerol rather than phosphatidylcholine or phosphatidylethanolamine. Furthermore, the composition of fatty acids in phosphatidylglycerol liposomes influenced the amount of antibiotics associated with liposomes; the highest amount was obtained with dioleoylphosphatidylglycerol followed by phosphatidylglycerol of fatty acid composition similar to that of egg yolk lecithin. It was established that purified liposomes, prepared from [3H]phosphatidylglycerol containing unsaturated fatty acid(s) bind about 25 per cent of originally present antibiotic. Both antibiotics, erythromycin A and azithromycin, were similar in respect to the amount of their association with liposomes. Determination of the size of phosphatidylglycerol/antibiotic liposomes established that the mean diameter of liposomes containing antibiotics was 200-350 nm, very close to that of liposomes without them.

Anti-Bacterial Agents↗
PubMed1998

Partial regression of advanced cyclosporin-induced gingival hyperplasia after treatment with azithromycin. A case report.

Gingival hyperplasia is a well recognised complication of cyclosporin A therapy. Although its pathogenesis is still debated in several recent reports a second generation macrolide antibiotic-azithromycin induced partial or even complete regression of hyperplasia. We present a patient after kidney transplantation treated with cyclosporin who developed very advanced gigival overgrowth (stage 3+). The patient received a 3-day treatment with azithromycin which was repeated after 3 months. The first course of the drug caused a partial regression of gingival hyperplasia during following months but the repeated treatment did not provide a further regression of the changes.

Adult↗
PubMed1999

Ethanol feeding does not affect the efficacy or pharmacokinetics of azithromycin, trovafloxacin, or ceftriaxone in a rat model of pneumococcal pneumonia.

A rat model of ethanol feeding was used to study the effects of ethanol on antibiotic therapy of pneumococcal pneumonia. Male Sprague-Dawley rats (150 g) received a liquid diet containing 36% of total calories as ethanol. Controls were pair-fed a liquid diet without ethanol or received rat chow. Diets began 7 days pre- and continued postinfection. Rats were infected transtracheally with type 3 Streptococcus pneumoniae and then treated with azithromycin (50 mg/kg), trovafloxacin (50 mg/kg), or ceftriaxone (100 mg/kg) injected subcutaneously twice daily for 5 days. Antibiotic levels in serum, lung cells, and lavage fluid were measured by HPLC. Ethanol- and pair-fed rats had depressed baseline peripheral neutrophil counts but were able to generate adequate numbers of peripheral and pulmonary polymorphonuclear leukocytes early in the course of their infection. Ethanol feeding did not alter the pharmacokinetics of azithromycin, trovafloxacin, or ceftriaxone. All three antibiotics were equally effective in curing experimental pneumococcal pneumonia, and survival rates were similar in treated ethanol-fed and control rats.

Animals↗
PubMed1999

Evaluation of lansoprazole (an H+/K+-ATPase inhibitor) and azithromycin (an antibiotic) for control of gastric ulceration in swine during periods of feed deprivation.

Helicobacter-like organisms as well as fermentative bacteria have been implicated in gastric ulcer production in swine. Irregular feeding schedules are also considered a major risk factor. A research trial was conducted to determine whether medication with an acid secretion inhibitor (lansoprazole), either alone or in combination with an antibiotic (azithromycin), would protect pigs from gastric ulceration if the animals were subjected to a 48 h period of fasting. In a 2 x 3 factorial design, 48 pigs were fasted, while an equal number were fed ad libitum. Within these 2 study groups, pigs were randomly assigned to 1 of 3 treatments: control, 30 mg lansoprazole s.i.d. for 7 d, or lansoprazole (30 mg s.i.d. for 7 d) and azithromycin (500 mg s.i.d. for 3 d). Overall, fasted pigs were 1.9 times more likely to develop erosive or ulcerative lesions of the pars esophagea (chi2 = 9.89, P < 0.002). Treatment with an acid secretion inhibitor alone or in combination with an antibiotic did not protect pigs from developing gastric lesions. Helicobacter-like organisms were not detected in any of the stomachs. Possibly, the lansoprazole dose of 30 mg given once per day was insufficient to prevent pH levels from becoming low enough to cause damage to epithelial tissue. Alternatively other substances such as bile acids may have caused the ulcerative lesions, even though stomach acid production was suppressed.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2000

[Triple therapy of short-term with azithromycin, amoxycillin and omeprazole for the eradication of Helicobacter pylori].

BACKGROUND: The high cost and complexity of therapeutic schemes for the eradication of Helicobacter pylori has stimulated the search of simpler and cheaper treatment options. AIM: To evaluate the efficacy of 3 days of azithromycin 500 mg od, 7 days of amoxycillin 750 mg tid and omeprazole, 20 (Group A) or 40 mg (Group B) on randomization, as a treatment for Helicobacter pylori infection in patients with endoscopically diagnosed peptic ulcer. METHODS: H. pylori status of peptic ulcer patients was pathologically confirmed by the examination of five gastric biopsies using the Giemsa stain and by rapid urease testing in two gastric biopsies. H. pylori status was reassessed not less than 28 days after completing treatment. Adverse events and compliance were evaluated. RESULTS: Fifty four patients (29 men, 25 women, mean age 48 years) were enrolled, 28 in Group A and 27 in Group B. Per protocol the infection was cured in 58.8% of patients (30/51; 95% CI: 45-73%). On an intention to treat basis, H pylori infection was cured in 55%. Minor side effects including diarrhea and nausea were reported by 32% of patients. Ninety-five per cent of patients consumed more than 95% of prescribed medications. H. pylori was successfully eradicated in 61% of group A and 57% of group B patients (p = NS). CONCLUSION: Short term therapy with azithromycin was poorly effective in curing H. pylori infection. The compliance was excellent. Increasing Omeprazole from 20 to 40 mg/day did not improve treatment effectiveness.

Amoxicillin↗
PubMed2003

Comparison of two azithromycin distribution strategies for controlling trachoma in Nepal.

OBJECTIVE: The study compares the effectiveness of two strategies for distributing azithromycin in an area with mild-to-moderate active trachoma in Nepal. METHODS: The two strategies investigated were the use of azithromycin for 1) mass treatment of all children, or 2) targeted treatment of only those children who were found to be clinically active, as well as all members of their household. FINDINGS: Mass treatment of children was slightly more effective in terms of decreasing the prevalence of clinically active trachoma (estimated by clinical examination) and of chlamydial infection (estimated by DNA amplification tests), although neither result was statistically significant. CONCLUSION: Both strategies appeared to be effective in reducing the prevalence of clinically active trachoma and infection six months after the treatment. Antibiotic treatment reduced the prevalence of chlamydial infection more than it did the level of clinically active trachoma.

Anti-Bacterial Agents↗
PubMed2000

[Prospective, comparative study (1994-1998) of the influence of short-term prophylactic treatment with azithromycin on patients with advanced COPD].

Despite the advances in therapy, chronic obstructive pulmonary disease (COPD) requires frequent hospital admissions due to acute exacerbations. We carried out a prospective randomized study of two groups of patients with COPD, one (n = 54) treated with azithromycin (500 mg/day) for three days every 21 days during the winter months, and a control group (n = 40) without treatment. A statistically significant reduction in the number of acute infectious episodes (187) and hospital admissions (22) was observed in the treated group versus the control group (249 and 45, respectively). A short prophylactic treatment course with azithromycin is a good alternative in the management of patients with severe, advanced COPD, and could lead to an improvement in social and healthcare costs

Aged↗
PubMed2001

Azithromycin and doxycycline in the treatment of female patients with acute urethral syndrome caused by Ureaplasma urealyticum: significance of duration of clinical symptoms.

One hundred ninety-two female patients with acute urethral syndrome caused by Ureaplasma urealyticum were examined. First, patients were divided into two groups: those with clinical symptoms present for less than 3 weeks before the start of treatment and those with clinical symptoms 3 weeks or longer before the beginning of therapy. The patients were then further divided into groups and randomized to receive azithromycin once daily in a single dose of 1 g or 500 mg once daily for 6 days, or to receive doxycycline 100 mg b.i.d. for 14 days or 100 mg b.i.d. for 7 days (eight study groups in all). Clinical and bacteriological efficacy were evaluated 3 weeks after the end of therapy. In the group of patients with disease symptoms lasting for 3 weeks or longer, eradication and clinical cure rates were significantly higher after the administration of azithromycin at a dose of 1 x 500 mg/6 days than after a single dose of 1 g (p < 0.001).

Acute Disease↗
PubMed2000

[Azithromycin in dentistry and oral surgery].

Azithromycin has adequate tissue levels for 7 days with a 3 day treatment regimen. The antibacterial activity is excellent. In dental infections, recurrence of infection happens when antibiotics cause a temporary improvement in symptoms but the etiologic agent is not eradicated. Azithromycin produces a "focused" cure and is an appropriate antibiotic for these infections. For this reason, the antibiotic was approved.

Anti-Infective Agents↗
PubMed2002

A comparative clinical trial of combinations of dihydroartemisinin plus azithromycin and dihydroartemisinin plus mefloquine for treatment of multidrug resistant falciparum malaria.

With the deteriorating situation of multidrug resistant falciparum malaria, a new drug or drugs in combinations are urgently needed. We conducted a study comparing a combination of dihydroartemisinin 240 mg and mefloquine 1,250 mg given over 3 days (Group 1) and a combination of dihydroartemisinin 240 mg and azithromycin 1,500 mg given over 3 days (Group 2), to determine safety, efficacy and tolerability. All of the patients stayed in a non-malaria endemic area during the study. By the third day after drug administration, most patients were free of parasites and none had serious adverse events. The cure rates at day 28 were 100% and 69.7% in Group 1 and Group 2, respectively (p<0.01). We conclude that a combination of dihydroartemisnin and azithromycin was safe and effective and may be another interesting regimen of the treatment of uncomplicated multidrug resistant Plasmodium falciparum malaria in Thailand.

Adolescent↗
PubMed1992

New macrolide antibiotics: clarithromycin and azithromycin.

Clarithromycin and azithromycin are new semisynthetic macrolide antibiotics structurally related to erythromycin. They are well absorbed and widely distributed, with excellent cellular and tissue penetration. Both have a broader spectrum of activity and fewer gastrointestinal side effects than erythromycin. Currently, clarithromycin and azithromycin are approved by the U.S. Food and Drug Administration for respiratory tract infections and skin infections, but they may also have use in mycobacterial and Toxoplasma infections in patients with acquired immunodeficiency syndrome.

Azithromycin↗
PubMed2003

[Comparative study of azithromycin pharmacokinetics in healthy volunteers in open cross randomized procedure].

A method of quantitative determination of azithromycin in HPLC with mass spectrometric detection was developed. The detection limit is 0.5 ng/ml. The method was used in the study of pharmacokinetics and bioequivalence of Zi-Factor (capsules of 250 mg of azithromycin made by Veropharm, Russia) vs. reference-drug. The pharmacokinetic study was performed by the open cross randomized procedure in 18 volunteers. The pharmacokinetic parameters required for estimation of the drug bioequivalence were calculated. The statistical analysis of the pharmacokinetic parameters revealed bioequivalence of Zi-Factor and the reference-drug.

Administration, Oral↗
PubMed2004

Comparison of ranitidine bismuth citrate, tetracycline and metronidazole with ranitidine bismuth citrate and azithromycin for the eradication of Helicobacter pylori in patients resistant to PPI based triple therapy.

BACKGROUND/AIMS: Helicobacter pylori is the most common infectious disease all over the world. Ten to twenty percent of the patients remain infected despite treatment with proton pump inhibitors (PPIs), amoxicillin and clarithromycin. We compared PPI, bismuth, tetracycline and metronidazole with ranitidine bismuth citrate, tetracycline and metronidazole in cases resistant to PPIs-based triple therapies. METHODS: The study included 52 patients who underwent a triple therapy with PPI, clarithromycin and amoxicillin for 14 days between September 2001 and December 2002, and were found to be resistant to the therapy. They were randomized to take ranitidine bismuth citrate (Rb) 400 mg twice a day, tetracycline (T) 1 g twice a day and metronidazole (M) 500 mg three times a day for 14 days (RbTM), or ranitidine bismuth citrate (Rb) 400 mg twice a day for 14 days and azithromycin (A) 500 mg once a day for 7 days (RbA). Four weeks after the treatment, endoscopies were repeated, and patients were assessed with respect to changes in symptoms. When H. pylori was negative on histological analysis and urease test, eradication was achieved. RESULTS: A total of 52 patients, 32 females and 20 males with a mean age of 49+/-12 years, were included in the study. Eradication was achieved in 15 (28%) out of 52 patients in total. There was a significant difference between RbA and RbTM groups (p=0.01). In fact, H. pylori was eradicated in 3 (12%) out of 25 patients in the RbA group, whereas it was eradicated in 12 (44.4%) out of 27 patients in the RbTM group. Symptom scores significantly improved in both groups after the treatment, though there was not a significant difference between the groups (p=0.705). CONCLUSIONS: Triple therapy including azithromycin does not seem to be a good choice in cases resistant to the first line therapies; however, a similarly lower rate of eradication was achieved with the quadruple therapy proposed. Therefore, different treatment schemes should be applied in resistant patients, and further studies are needed as well.

Adult↗
PubMed2004

Ultrastructure of the hepatocytes after application of azithromycin (Sumamed).

Azithromycin (Sumamed, PLIVA Cracow) was administered intragastrically to rats in doses 10 times and 100 times bigger than the therapeutic dose (according to the indications for a 5-day treatment). Ultrastructural examinations of the liver were performed. Changes observed in the morphology of hepatocytes and Browicz-Kupffer cells (swelling of mitochondria, more numerous lysosomes, weaker RER content and granular material inside biliary canaliculi) may indicate temporary violation of the functional equilibrium in the liver due to the application of azithromycin.

Animals↗
PubMed2006

Stevens-Johnson syndrome as an unusual adverse effect of azithromycin.

Stevens-Johnson syndrome mostly involves the skin and mucous membranes. The diagnosis is made when the characteristic rash appears 1 to 3 weeks after exposure to a known stimulus and cannot be explained by some other diagnosis. A 62-year-old woman was admitted for evaluation of toxo-allergic dermatitis and collagenosis. Ten days prior to admission she was taking a course of azithromycin for upper respiratory tract infection. After a few days she was feeling better but maculopapular, erythematous rash developed over her palms, accompanied by fever and chills as well as reddish discoloration around her eyes. Within the next few days the rash progressed to the feet. Routine hematologic, biochemical and immunologic studies did not confirm the diagnosis of inflammatory rheumatic disease. Corticosteroid therapy with methylprednisolone (1 mg/kg) for the presumed Stevens-Johnson syndrome was started and her condition improved in several days; she became afebrile and her skin lesions gradually disappeared. There is only one report, in a child, documenting the association of Stevens-Johnson syndrome with azithromycin, as in this patient.

Anti-Bacterial Agents↗
PubMedDate not supplied

Chemotherapeutic effect of azithromycin and lasalocid on Cryptosporidium infection in mice.

Prednisolone-immunosuppressed mice (ICR, 7-wk-old female) were each inoculated with 1 x 10(5) oocysts of Cryptosporidium parvum. Medication with azithromycin (400 mg/kg/day) or lasalocid (64, or 128 mg/kg/day) was started 13 h after inoculation and continued for 3 days. The number of oocysts discharged by each mouse was calculated on days 4-12 post-inoculation. Compared with non-medicated controls, oocyst production by the medicated mice was markedly reduced; some mice did not discharge oocysts and the remaining mice discharged less than 1/100 the number of oocysts of the control mice. These results indicate that both azithromycin and lasalocid have prophylactic or therapeutic activity against Cryptosporidium.

Animals↗
PubMed2006

Azithromycin-induced QT prolongation in elderly patient.

The authors present a case of an elderly patient with idiopathic dilated cardiomyopathy who developed a significative prolongation of the QT interval after two days of treatment with azithromycin for a community-acquired pneumonia. QT prolongation is associated with a high risk of serious ventricular tachyarrhythmias. Three days after discontinuation of azithromycin, QT interval returned to the normal value.

Aged↗