[Erythromycin estolate in treatment of genital tract infections in obstetrics and gynecology].
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Administration, Oral↗
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Efficacy of fixed combination antibiotics versus separate components in otitis media. Effectiveness of erythromycin estrolate, triple sulfonamide, ampicillin, erythromycin estolate- triple sulfonamide, and placebo in 280 patients with acute otitis media under two and one-half years of age.
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Acetaminophen↗
Cytotoxicity of macrolide antibiotics in a cultured human liver cell line.
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.
Anti-Bacterial Agents↗
Treatment of acute bacterial infections of the upper respiratory tract.
An open comparative study was carried out to assess the effectiveness of 4 antibiotic regimens in eradicating acute bacterial infections of the upper respiratory tract. Patients in each treatment group had similar physical parameters, severity of disease and bacterial pathogens, and were treated for 10 days with either erythromycin estolate, erythromycin stearate, ampicillin or oxytetracycline in the recommended dosage. Each patient was reviewed daily by physical examination and the bacteriological findings from throat swab and salivary washings. The results showed that erythromycin stearate produced more rapid bacterial eradication and clinical resolution of symptoms and fever than with the other antibiotic preparations, and was well tolerated by most patients.
Acute Disease↗
Erythromycin and clindamycin absorption and elimination in pregnant women.
Thirty-nine pregnant women admitted for therapeutic abortions during early or mid pregnancy were given erythromycin estolate, erythromycin base, or clindamycin hydrochloride orally in single or multiple doses. Peak serum levels of clindamycin were 3.4 to 9.0 mug/ml following a single dose of 450 mg, whereas peak serum levels of erythromycin were 0.29 to 7.2 mug/ml following 500 mg in a single dose. The individual variability of serum concentrations of erythromycin was greater than that reported in normal men and nonpregnant women, whereas the serum levels of clindamycin were rather uniform, and similar to what has been reported in nonpregnant individuals. Following multiple doses of each antibiotic, high serum levels were obtained in virtually all subjects, and urine levels were also higher. Following single doses the mean urinary recovery was 2% for erythromycin and 16.8% for clindamycin.
Abortion, Therapeutic↗
Treatment and prevention of pertussis by antimicrobial agents (Part II).
Suitable antimicrobials given during the catarrhal stage of whooping cough can attenuate the course of the disease. The efficacy of antibiotics administered prophylactically during the incubation period remains controversial but appears to be beneficial. Currently, erythromycin given for two weeks is the antibiotic of choice for pertussis. No treatment failures were observed with erythromycin estolate. Erythromycin ethylsuccinate and stearate must be given at high dosages (50-60 mg/kg/day) in order to achieve sufficient concentrations in the respiratory secretions. With ampicillin and amoxicillin treatment failures have been observed. The role of josamycin and co-trimoxazole in pertussis remains open.
Anti-Bacterial Agents↗
Concentrations of antimicrobial agents in middle ear fluid, saliva and tears.
Antibiotics concentrations in middle ear fluid (MEF), saliva and tears were measured in children with persistent middle ear effusions undergoing tympanostomy tube placement. In 31 children given cefaclor, specimens of serum, saliva and MEF were collected at 0.5, 1, 2, 3 or 5 h after a dose. Another group of 37 children were randomized to receive a single dose of penicillin V, amoxicillin, ampicillin, erythromycin estolate, erythromycin ethylsuccinate, trimethoprim-sulfamethoxazole or cefaclor. Concentrations of antibiotics in saliva and tears bore no consistent relationship to those in MEF. Mean concentrations of all drugs in MEF were several-fold greater than the usual minimal inhibitory concentrations (MIC) of pneumococci, but only with trimethoprim and cefaclor were they greater than in usual MIC's for Haemophilus influenzae. Concentrations of antibiotics in MEF in persistent effusions were comparable to those previously reported in acute purulent effusions.
Amoxicillin↗
Preparation and evaluation of a new erythromycin derivative -- erythromycin taurate.
Erythromycin taurate, a new derivative of erythromycin, was prepared by reacting erythromycin base with tauric acid and its physico-chemical and biological properties were evaluated. The derivative has reasonably good solubility in organic solvents. The partition coefficient values in chloroform/water 1.17 and octanol/water 1.16 systems indicate its good distribution in various tissues in vivo. The in vitro antimicrobial potency of the derivative (833.33 microg mg(-1)) is higher than that of the existing derivatives such as erythromycin estolate, erythromycin stearate, erythromycin ethyl succinate, erythromycin gluceptate, erythromycin lactobionate. The antimicrobial spectrum is comparable to that of the parent compound. Our results indicate that erythromycin taurate has a high potential for possible clinical application and is more efficient against Escherichia coli and Klebsiella pneumoniae than the parent base.
Animals↗
Pharmacologic evaluation of orally administered antibiotics in infants and children: effect of feeding on bioavailability.
The clinical pharmacology of orally administered antibiotics was investigated in 106 infants and children. The antibiotic suspensions studied were ampicillin, cephalexin, erythromycin estolate, erythromycin ethylsuccinate, penicillin G, and penicillin V. The feeding status of the patients was evaluated in relation to the concentrations of drugs in serum, saliva, and tears. Peak concentrations and area-under-the-curve values of cephalexin, penicillin V, and penicillin G were reduced 40% to 60% in patients given milk and drug concurrently. Absorption was enhanced when erythromycin ethylsuccinate was given milk. After administration of both erythromycin formulations, penicillin V and ampicillin, salivary concentrations exceeded the minimal inhibitory concentrations for most pneumococci and group A streptococci and for many meningococci. The clinical implications of these pharmacokinetic data are discussed.
Administration, Oral↗
Otitis media of infancy and early childhood. A double-blind study of four treatment regimens.
A double-blind, randomized trial of four antimicrobial regimens was conducted in 383 infants and children with acute otitis media. The drugs used were penicillin V, amoxicillin trihydrate, erythromycin estolate, and erythromycin estolate with trisulfapyrimidines. Aspiration of middle ear fluid for culture was done before treatment and repeated during treatment if fluid persisted. Etiologic bacteria were most commonly pneumococci (31%) or Haemophilus sp (22%), and an additional 5% of patients had both organisms. Amoxicillin was the most effective in promoting initial response in pneumococcal infection. For Haemophilus infections, the cure rates with amoxicillin and the erythromycin-trisulfapyrimidines mixture were significantly better than with the other two regimens, and serous otitis did not occur during the follow-up period; however, new episodes of otitis were comparable in the four groups. Amoxicillin and the erythromycin estolate-trisulfapyrimidines combination appear to be somewhat more effective than penicillin V or erythromycin estolate.
Acute Disease↗
Erythromycin jaundice: diagnosis by an in vitro challenge test.
A 53-year-old housewife who had developed severe cholestatic hepatitis following the administration of erythromycin estolate therapy two-and-a-half years previously, was studied by an in vitro "challenge" test in which peripheral venous lymphocytes were cultured in the presence of erythromycin estolate, erythromycin stearate and erythromycin base. Evidence of blastogenesis was observed in response to erythromycin estolate, but not to erythromycin stearate of erythromycin base. This test thus provided evidence that the patient was "sensitized" to erythromycin estolate without exposing her to the risk of in vivo challenge. Furthermore, in contrast to previous studies, the findings provide evidence that erythromycin estolate jaundice is mediated by immunological mechanisms.
Drug Hypersensitivity↗
Effect of tetrahydrocurcumin on erythromycin estolate-induced lipid peroxidation in rats.
Erythromycin estolate (EME), a potent macrolide antibiotic, generates free radicals, but their role in the development of liver toxicity is not yet well understood. The present study was carried out to investigate the effect of the antioxidant drug tetrahydrocurcumin (a metabolite of curcumin, the main component of turmeric) against EME-induced lipid peroxidation in rats. The oral administration of combined THC (80 mg/kg body weight) and EME (800 mg/kg body weight) for 15 days significantly decreased lipid peroxidation and enhanced cellular antioxidant defenses when compared with the group treated with EME alone. Supplemental histopathological examination of liver sections revealed that THC had a better antioxidant effect than Silymarin (200 mg/kg body weight), a reference drug. The results of this study indicate that THC affords significant protection against EME-induced lipid peroxidation.
Animals↗
Protective effect of Sesbania grandiflora against erythromycin estolate-induced hepatotoxicity.
Sesbania grandiflora, commonly known as 'sesbania', is widely used in Indian folk medicine for the treatment of liver disorders. Oral administration of an ethanolic extract of S. grandiflora leaves (200 mg/kg/day) for 15 days produced significant hepatoprotection against erythromycin estolate (800 mg/kg/day)-induced hepatotoxicity in rats. The increased level of serum enzymes (aspartate transaminase, alanine transaminase, alkaline phosphatase), bilirubin, cholesterol, triglycerides, phospholipids, free fatty acids, plasma thiobarbituric acid reactive substances and hydroperoxides observed in rats treated with erythromycin estolate were significantly decreased in rats treated concomitantly with sesbania extract and erythromycin estolate. The sesbania extract also restored the depressed levels of antioxidants to near normal. The results of the study reveal that sesbania could afford a significant protective effect against erythromycin estolate-induced hepatotoxicity. The effect of sesbania was compared with that of silymarin, a reference hepatoprotective drug.
Administration, Oral↗
Therapy of staphylococcal infections in monkeys. IV. Further comparison of triacetyloleandomycin and erythromycins.
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.
Animals↗
Treatment of Staphylococcus aureus infections in children in office practice.
One hundred five Staphylococcus aureus infections occurring in 79 children who were seen in a private office practice were evaluated for response to antibiotic therapy. The value of in vitro disk susceptibility testing in directing antibiotic selection in treatment failures was also examined. Of the total episodes studied, the types of infection studied included vesicular pyoderma (48%), secondary pyoderma (13%), bullous pyoderma (5%), furunculosis (14%), carbunculosis (12%), cellulitis (3%), suppurative otitis media (4%), and paronychia (2%). Comparative treatment efficacy was obtained with perioral erythromycin estolate and erythromycin ethylsuccinate, cefaclor and cephalexin, and clindamycin hydrochloride and dicloxacillin sodium. Penicillin V potassium, ampicillin, and topical bacitracin were generally ineffective. In 23 patients, 27/105 infections were initial treatment failures. Antibiotic disk susceptibility testing predicted these clinical failures and/or the antibiotic that would produce a clinical response in 21 of these 23 patients, suggesting that this office procedure can be of considerable value.
Adolescent↗
[Effect of pretreatment with bacterial endotoxin on erythromycin estolate-induced cholestasis].
The effect of acute and chronic endotoxin (LPS) treatment on the erythromycin estolate (EE) induced cholestasis, was studied using the isolated perfused rat liver. Addition of EE markedly reduced bile and perfusate flows in livers from control rats but did not alter these parameters in livers from endotoxin pretreated rats or in vitro treated with LPS. We suggest that changes in membrane organization induced by LPS may alter the diplay of EE toxicity.
Animals↗
Antibiotics for whooping cough (pertussis).
BACKGROUND: Whooping cough is a highly contagious disease. Infants are the population at highest risk of severe disease and death. Erythromycin for 14 days is recommended for treatment and contact prophylaxis but this regime is considered inconvenient and prolonged. The value of contact prophylaxis is uncertain. OBJECTIVES: To study the benefits and risks of antibiotic treatment of and contact prophylaxis against whooping cough. SEARCH STRATEGY: The Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library Issue 1, 2004); MEDLINE (January 1966 to February 2004); EMBASE (January 1974 to August 2003); conference abstracts and reference lists of articles were searched. Study investigators and pharmaceutical companies were approached for additional information (published or unpublished studies). There were no constraints based on language or publication status. SELECTION CRITERIA: All randomised and quasi-randomised controlled trials of antibiotics for treatment of and contact prophylaxis against whooping cough were included in the systematic review. DATA COLLECTION AND ANALYSIS: At least three reviewers independently extracted data and assessed the quality of each trial. MAIN RESULTS: Twelve trials with 1,720 participants met the inclusion criteria. Ten trials investigated treatment regimens and two investigated prophylaxis regimens. The quality of the trials was variable. Results showed that short-term antibiotics (azithromycin for three days, clarithromycin for seven days, or erythromycin estolate for seven days) were equally effective with long-term antibiotic treatment (erythromycin estolate or erythromycin for 14 days) in the microbiological eradication of Bordetella pertussis (B. pertussis) from the nasopharynx. The relative risk (RR) was 1.02 (95% confidence interval (CI) 0.98 to 1.05). Side effects were fewer with short-term treatment (RR 0.66; 95% CI 0.52 to 0.83). There were no differences in clinical improvement or microbiological relapse between short and long-term treatment regimens. Contact prophylaxis (of contacts older than six months of age) with antibiotics did not significantly improve clinical symptoms or the number of cases that developed culture positive B. pertussis. AUTHORS' CONCLUSIONS: Antibiotics are effective in eliminating B. pertussis from patients with the disease, rendering them non-infectious, but do not alter the subsequent clinical course of the illness. Effective regimens include: three days of azithromycin, seven days of clarithromycin, seven or 14 days of erythromycin estolate, and 14 days of erythromycin ethylsuccinate. Considering microbiological clearance and side effects, three days of azithromycin or seven days of clarithromycin are the best regimens. Seven days of trimethoprim/sulfamethoxazole also appeared to be effective for the eradication of B. pertussis from the nasopharynx and may serve as an alternative antibiotic treatment for patients who cannot tolerate a macrolide. There is insufficient evidence to determine the benefit of prophylactic treatment of pertussis contacts.
Anti-Bacterial Agents↗
Protective role of tetrahydrocurcumin against erythromycin estolate-induced hepatotoxicity.
Tetrahydrocurcumin (THC), one of the major metabolites of curcumin, was investigated for its possible hepatoprotective effect in Wistar rats against erythromycin estolate-induced toxicity. Oral administration of THC significantly prevented the occurrence of erythromycin estolate-induced liver damage. The increased level of serum enzymes (aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP)), bilirubin, cholesterol, triglycerides, phospholipids, free fatty acids and plasma thiobarbituric acid reactive substances (TBARS) and hydroperoxides observed in rats treated with erythromycin estolate were very much reduced in rats treated with THC and erythromycin estolate. This biochemical observation were supplemented by histopathological examination of liver section. Results of this study revealed that THC could afford a significant protection against erthromycin estolate-induced hepatocellular damage. Tetrahydrocurcumin had a better protective effect when compared with Silymarin, a reference drug.
Administration, Oral↗