Intravenous inoculation of a penicillin-resistant, phage type 80/81 staphylococcus caused lethal infection in 8 of 15 untreated monkeys. Daily intragastric administration of 50 mg/kg of triacetyloleandomycin, erythromycin estolate, and erythromycin ethylsuccinate was followed by mortalities of 0 of 16, 3 of 16, and 3 of 10, respectively. At dose levels of 25 and 12.5 mg/kg, none of 7 and 4 of 7 receiving triacetyloleandomycin and erythromycin estolate, respectively, died, as compared to 3 of 4 deaths in controls. In vitro sensitivity data and serum antibacterial levels would suggest that triacetyloleandomycin would be the least effective therapeutically. However, this prediction was not fulfilled in these studies of experimental infections in monkeys wherein triacetyloleandomycin was a very effective antimicrobial agent.
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It was concluded that erythromycin is an effective prokinetic agent for diabetic gastroparesis, and that corrected gastric emptying may improve glycemic control.
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Noncompliance with a prescribed therapy is a common problem in ambulatory pediatrics.
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Erythromycin, sulfonamides, and tetracyclines are associated with acute symptomatic hepatitis resulting in hospitalization. Given the widespread use of these drugs, they will be among the more common drugs associated with hepatitis.
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A method is described for the determination of erythromycin estolate by liquid chromatography. A C18 reversed-phase column (25 x 0.46 cm i.d.) was used with acetonitrile-tetrabutylammonium sulphate (pH 6.5, 0.2 M)-phosphate buffer (pH 6.5, 0.2 M)-water [x:5:5:(90-x), v/v/v/v] as mobile phase. The proportion of acetonitrile (x) has to be adapted to the type of stationary phase used. For RSil C18 LL 42.5% (v/v) was used. The column was heated at 35 degrees C, the flow rate was 1.5 ml min-1 and UV detection was performed at 215 nm. The main component, erythromycin A propionate, was separated from all other components which were present in commercial samples. The impurities most frequently observed were the propionate ester of erythromycin C and the amide N-propionyl-N-demethyl-erythromycin A. Erythromycin A was shown to be present in specialties.
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One hundred two children with group A streptococcal pharyngitis were treated on a randomized basis with either 15 mg/kg of erythromycin estolate or 25 mg/kg of erythromycin ethylsuccinate given twice daily for ten days. Twelve patients, including 11 erythromycin ethylsuccinate-treated patients and one erythromycin estolate-treated patient, were dropped from the study at the request of their parents because of abdominal cramping and/or nausea and vomiting that occurred 15 to 45 minutes after ingestion of drug. Eighteen other patients (12 treated with erythromycin ethylsuccinate and six treated with erythromycin estolate) had similar gastrointestinal (GI) tract symptoms that resolved or abated. Excluding patients with reinfections with new streptococcal serotypes and those with resistant strains, the bacteriologic failure rates were 4.3% and 17.5%, and the total failure rates were 6.4% and 35.3% with erythromycin estolate therapy and with erythromycin ethylsuccinate therapy, respectively. The high rate of GI tract intolerance associated with the erythromycin ethylsuccinate appears to be dose related.
ilosone drug study
Pre- and post-extraction blood cultures were taken from 242 patients. The post-extraction ones were taken from 100 unpremedicated patients, from 42 with an erythromycin estolate cover, and from 100 patients after protection with pyrrolidino methyl tetracycline. The 100 post-extraction blood cultures from unpremedicated patients gave 64 positive results which yielded 155 strains, 88 of which were not aerobes. One hundred and fifteen representative strains were tested for sensitivity to 22 antibiotics. Of the 42 patients who received the erythromycin orally, 16 yielded positive blood cultures of mixtures of aerobes and anaerobes and of the 100 given one intravenous injection of the tetracycline three only developed a bacteraemia of a single type of aerobe. The serum concentrations obtained with the tetracycline given intravenously were 15 to 20 times higher than the serum levels obtained with the erythromycin given orally. There is a strong indication for using this kind of efficient antibiotic cover for dental extractions and other operative procedures known to be followed by a bacteraemia.
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During a 24-month period, throat-swab cultures were obtained on 1,362 well children who were 3 months to 14 years of age. The overall incidence of positive cultures for group-A beta-hemolytic Streptococcus was 3.3%; in those children older than 1 year, it was 4.4%. The largest incidence of positive cultures occurred in the 5- to 7-year-old (8.3%) and 8- to 10-year-old (4.5%) age groups. No positive cultures were obtained from 339 infants younger than 1 year of age. There was no relation between positive cultures and the month of the year. There were no significant differences between the age, sex, presence of tonsils, previous group-A streptococcal infections, or the presence in a daycare center or school of children with positive cultures compared with those children with negative cultures. Follow-ups were obtained on 29 of 45 children with positive throat cultures; all of the children were asymptomatic and had normal results of physical examinations. Group-A streptococci of the same serotype as the original isolate were isolated from 19 of these children. Three to four days after a ten-day course of erythromycin estolate, five of 19 children again had positive cultures. Twenty-six of the 29 children had a total of 43 siblings residing in the home. Serotypically identical group-A streptococci were isolated from five siblings (11%). Only one of 29 patients from whom paired serum samples were obtained showed a fourfold rise or fall in the Streptozyme titers.
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A randomized crossover study in 16 healthy volunteers given multiple doses of erythromycin base enteric-coated tablets or erythromycin estolate capsules revealed essentially no difference in the resultant plasma concentration of bioactive erythromycin. This similarity in bioactivity persisted despite the fact that total eryghromycin levels (bioactive erythromycin base plus bioinactive erythromycin propionate) were at least three times higher after administration of the estolate than after administration of the base.
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Although a possible microbial etiology was identified in 43% of the evaluable patients, clinical findings and results of blood cultures, chest radiographs and white blood cell and differential counts did not distinguish patients with a defined etiology from those without a known cause for pneumonia. There were no differences in the clinical responses of patients to the antimicrobial regimens studied.
ilosone suspension dosage
Using primary cultures of parenchymal hepatocytes as a model system, the cytotoxic potential of dantrolene sodium (DS) was compared with that of erythromycin estolate (EE)--a known hepatotoxin. Parallel morphological and functional comparisons were made, following 4-, 8-, or 24-h exposures of hepatocyte cultures, using phase contrast microscopy and lactate dehydrogenase (LDH) leakage, respectively. Four-hour exposures of cultures to rather low concentrations of EE (i.e. 50 microM) resulted in cellular necrosis and significantly elevated LDH release. As the concentration of this hepatotoxin was increased, the changes were more pronounced. However, even 4- or 8-h exposures of cultures to a maximum of 100 microM DS did not affect LDH leakage or morphological integrity, although marginally detectable morphological changes did not occur at the highest concentration after 24-h. The value of using primary parenchymal hepatocyte cultures as a model system for the assessment of xenobiotic-induced hepatotoxicity was confirmed.
Food was withheld from foals overnight before intragastric administration of erythromycin estolate (25 mg/kg of body weight; n = 8) and erythromycin phosphate (25 mg/kg; 7). Four foals received both drugs with 2 weeks between treatments. Plasma erythromycin concentrations were determined at various times after drug administration by use of high-performance liquid chromatography. Maximum plasma peak concentrations, time to maximum concentrations, area under plasma concentration versus time curves, half-life of elimination, and mean residence times were determined from concentration versus time curves.
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Capillary electrophoresis was utilized in the study of the macrolide antibiotics (i.e. pharmaceutical glycoconjugates) clarithromycin, erythromycin, oleandomycin, troleandomycin, and spiramycin. In order to assist in analyte solubilization, two buffer systems using acetonitrile were developed. The first system involved 30 mM sodium cholate and 20% acetonitrile in 80 mM sodium phosphate, pH 6. This buffer permitted the baseline resolution of all five glycoconjugated antibiotics. In addition, erythromycin was separated from its derivatives estolate and ethylsuccinate. In the absence of surfactants, a higher acetonitrile quantity, 65%, was used in the second buffer system, with 35 mM sodium phosphate, pH 6. Selectivity between oleandomycin and clarithromycin was reversed in this system compared to the cholate buffer, indicating solute interaction with the cholate micelles in the previous system. Calibration linearity and detection sensitivity were improved in the high acetonitrile buffer, due to decreased background absorbance. It was demonstrated that both buffer systems can be utilized for the visualization of minor components that may be present in bulk pharmaceuticals.
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Dissolution percentage in thirty minutes reached 28.9% and in sixty minutes erythromycin was completely released. The parameters of the delayed release tablets were Tlag 2.3 hr, Tmax.4.5 hr, and Cmax 2.123 g/ml Ka 0.38048 hr(-1) T (1/2) 1.8 hr, V*C/F 49.721 AUC 12.9155. The relative bioavailability of erythromycin delayed release tablet to erythromycin capsules was 105.31%
In this large, multicenter, randomized trial, we found that azithromycin is as effective as erythromycin estolate for the treatment of pertussis in children. Gastrointestinal adverse events were much more common with erythromycin treatment than azithromycin. Compliance with therapy was markedly better with azithromycin than with erythromycin in this study.
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The absorption, excretion, and metabolism of [1-14C]lauryl sulfate as either the sodium or propionyl erythromycin salt has been studied in the rat and man. In the rat 88% of the radiolabel from propionyl erythromycin [1-14C]lauryl sulfate was excreted in the urine in the 24-hr period following a single oral dose. More than 95% of the radiolabel was excreted as the metabolite butyric acid 4-sulfate. This metabolite was shown to be derived from carbons 1-4 of the lauryl sulfate moiety. There was no evidence of sulfate cleavage in the rat. In man 51-59% of the administered ratioactivity was recovered in the urine. The major excretion product was butyric acid 4-sulfate accounting for approximately 95% of urinary radioactivity. The remainder was unchanged lauryl sulfate. A significant portion of the radiolabeled propionyl erythromycin lauryl sulfate was converted to 14CO2 indicating that the sulfate linkage was cleaved. A minimum value of 9-16% of the dose was metabolized in this manner.
ilosone 250 suspension
Twenty patients of Type II (non-insulin-dependent) diabetes mellitus with typical symptoms of gastroparesis and delayed solid phase gastric emptying were studied. There were 18 males and 2 females, aged 49 to 72 years. Erythromycin (erythromycin estolate) was given orally at a dose of 250 mg, 3 times daily, 30 minutes before each meal. Radionuclide-labelled solid phase gastric emptying and fasting blood sugar (FBS) were studied after one day of erythromycin therapy, and again after 2 weeks of the therapy. The half time of gastric emptying (GETt1/2) represented the time needed for 50 percent of the initial radioactivity to leave the stomach, and was used to express the gastric emptying status.
ilosone 500 mg
Sustained release of antibiotics from hydrogel matrices in the eye was studied for the purpose of developing a new method for trachoma therapy. Copolymers of N-vinylpyrrolidone were moulded into an ocular insert and impregnated with erythromycin or erythromycin estolate. The antibiotic-hydrogel inserts completely suppressed the chlamydia trachomatis infection in the owl monkey eyes. The drug elution rates were a little lower in vivo than in vitro. By comparison of the drug elution rate in the human eye with that in the owl monkey eye, similar therapeutic effect is expected in the treatment of human trachoma.
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Although erythromycin estolate has been fully assessed for pertussis treatment, the evaluation of erythromycin ethylsuccinate and stearate, the main erythromycin preparations used in Japan and the US, is inadequate. We evaluated these preparations to establish an appropriate treatment for pertussis according to age. Sixty-six patients with culture-confirmed pertussis were treated with erythromycin administered at a dosage of 40-50 mg/kg/day (maximum, 1.2 g/day). Negative culture was obtained in 39% (15/38) of patients aged 0-2 years within one week and in 71% (27/38) within two weeks, in 78% (7/9) of those aged 3-15 years within one week and in 100% (9/9) within two weeks. All 12 adult patients had a negative culture within one week. The efficacy of erythromycin for the eradication of B. pertussis was significantly lower in children aged 0-2 years than in older children. In conclusion, it is desirable to administer erythromycin for three weeks to children aged 0-2 years, two weeks to those aged 3-15 years and one week to adults.
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Cytotoxicity of erythromycin base, erythromycin estolate, erythromycin-11,12-cyclic carbonate, roxithromycin, clarithromycin and azithromycin was compared in cultured human non-malignant Chang liver cells using reduction of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide and cellular protein concentration as end points of toxicity. Erythromycin estolate was the most toxic macrolide in all tests differing clearly from all the other macrolides studied. Erythromycin-11,12-cyclic carbonate was also more toxic than the other macrolides. Roxithromycin and clarithromycin were the next toxic derivatives, while erythromycin base and azithromycin were least toxic. Thus, cytotoxicity of the new semisynthetic macrolides, roxithromycin, clarithromycin and azithromycin, is not substantially different from that of erythromycin base. In view of the low level of hepatotoxicity of macrolides hitherto reported in humans, the results do not suggest any substantial risk for hepatic disorders related to the use of azithromycin, clarithromycin and roxithromycin.
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Comparison of serum antibacterial activity against a beta-hemolytic streptococcus and a penicillin-resistant staphylococcus was made in a cross-over study in volunteers after ingestion of oral suspensions and capsules of triacetyloleandomycin and erythromycin estolate. Oral suspensions yielded earlier peak titers, but ultimate peak titers and duration of activity were similar to those observed after ingestion of capsules. Antibacterial activity of serum against both organisms was consistently greater with both erythromycin estolate preparations than with the triacetyloleandomycin preparations. These in vitro data were comparable to observations made previously in monkeys infected with the same organisms, although comparative clinical efficacy in monkeys did not reflect these implied therapeutic differences.
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In a number of well-designed comparison studies since 1958, erythromycin has proved highly effective in the treatment of both streptococcal pharyngitis and skin infections. Of the two formulations most often prescribed, the estolate salt is better absorbed and achieves higher tissue concentrations than does the ethylsuccinate salt. For these reasons and based on results of the published clinical studies, the appropriate daily dosage for erythromycin estolate is 20 to 30 mg/kg/day and that for erythromycin ethylsuccinate is 40 mg/kg/day. Erythromycin estolate may be given in two, three or four daily doses in the treatment of streptococcal pharyngitis with efficacy rates equal to or better than that achieved with penicillin V. Erythromycin ethylsuccinate is as efficacious as penicillin V when given in three or four daily doses. Treatment of streptococcal pharyngitis should be for 10 days. Recent studies in the treatment of streptococcal skin infections have shown erythromycin to be superior to penicillin. This superiority may be due to increasing numbers of penicillin-resistant staphylococci found in these streptococcal skin lesions. Dosage and frequency of administration of erythromycin in the treatment of streptococcal skin infections is similar to that for the treatment for streptococcal pharyngitis. However, b.i.d. administration has not been well-established in the skin infection studies. Treatment should be given for 7 to 10 days. In conclusion erythromycin is a safe and effective antibiotic for the treatment of streptococcal pharyngitis. Penicillin remains the antibiotic of choice for these infections, but erythromycin is an effective alternate when penicillin allergy is suspected. The appropriate therapy for streptococcal skin infections is less clear.(ABSTRACT TRUNCATED AT 250 WORDS)
The activities of 11 5-nitroimidazole compounds have been compared against Giardia intestinalis in vitro using a 3H-thymidine incorporation assay. All the compounds were at least equipotent to, or more active than metronidazole with the exception of panidazole. Satranidazole, ronidazole and S75 0400 A were all about five times more active than metronidazole and warrant further study as potential chemotherapeutic agents for man. No major differences in the response to these compounds was found between two stocks of Giard. intestinalis with the exception of flunidazole. Several other antiprotozoal drugs showed activity against Giard. intestinalis. Berberine sulphate, paromomycin sulphate, erythromycin estolate and sulphasalazine, all of which have been used to treat human patients, showed no activity in vitro.
Of 456 patients enrolled during 17 consecutive months, 420 were evaluable. Clinical success at Study Days 15 to 19 was 94.6% in the azithromycin group and 96.2% in the comparative treatment group (P = 0.735) and at 4 to 6 weeks posttherapy 90.6 and 87.1%, respectively (P = 0.330). Evidence of infection was identified in 46% of 420 evaluable patients (1.9% bacteria, 29.5% M. pneumoniae and 15% C. pneumoniae). Microbiologic eradication was 81% for C. pneumoniae and 100% for M. pneumoniae in the azithromycin group vs. 100 and 57%, respectively, in the comparator group. Treatment-related adverse events occurred in 11.3% of the azithromycin group and 31% in the comparator group (P < 0.05).
To determine the etiology of community-acquired pneumonia in ambulatory children and to compare responses to treatment with azithromycin, amoxicillin-clavulanate or erythromycin estolate.
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Although 14 days of erythromycin is recommended for the treatment of Bordetella pertussis infection, there have been no prospective controlled studies to support the contention that this long course of therapy is required to eradicate the microorganism from the nasopharynx or to prevent bacteriological relapse. We randomly allocated children and adults with culture-positive community-acquired pertussis to either 7 or 14 days of erythromycin estolate treatment (40 mg/kg/d; maximum dose 1 g/d). Nasopharyngeal aspirate cultures were obtained by study nurses during home visits before and at the end of treatment, and 1 week after the completion of treatment. B pertussis-specific antibodies were measured before treatment and 1 month later. Information about clinical symptoms, adverse reactions, and compliance were collected at each scheduled contact.
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Mycoplasma pneumoniae and C. pneumoniae are common etiologic agents of CAP in older children from different latitudes. Children with CAP present with similar clinical and radiologic findings to those caused by other etiologic agents. Outcome was excellent for the three treatment regimens studied.
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Pityriasis lichenoides (PL) occurs in all age groups, although predominantly in younger individuals.