Ilosone update.
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Chemical and Drug Induced Liver Injury↗
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Results for “Erythromycin Estolate”
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Cholestatic hepatitis caused by esters of erythromycin and oleandomycin. 1962.
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Chemical and Drug Induced Liver Injury↗
Evaluation of bacitracin ointment in the treatment of impetigo.
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Adolescent↗
Erythromycin in the treatment of streptococcal infections.
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)
Drug Administration Schedule↗
Treatment of syphilis in pregnancy.
Only penicillin has been adequately studied in treating syphilis during pregnancy. It is safe for the fetus and highly effective in doses currently recommended by the USPHS. Since these schedules appear to represent a minimal effective dose, smaller amounts should never be used. Whether higher doses would produce higher cure rates is not known. Penicillin is the drug of choice and the standard against which all others must be measured. Tetracyclines in any dose or form should not be used because of toxicity to both mother and child. Erythromycin (except the estolate) and cephalosporins are promising because of low toxicity, but their efficacy has not been established.
Cephalosporins↗
Erythromycin in the aqueous. Comparative concentrations form the estolate and from the base.
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Aqueous Humor↗
Another look at erythromycin.
The erythromycins are broadly reviewed from a clinical viewpoint. The antimicrobial spectrum, clinical indications, pharmacokinetics and toxicity are dealt with. The usefulness of erythromycin for respiratory tract infections is stressed. New evidence to support bactericidal activity of this antibiotic is noted. There seems little reason to use the potentially hepatotoxic estolate form of erythromycin. The safety of the other forms of this antibiotic available in this country is emphasized.
Bacteria↗
Effects of in vivo treatment with a new fluorinated macrolide (P-0501A) and other erythromycins on drug clearance and hepatic functions in perfused rat liver.
The hepatic clearance and the effects of a new fluorinated macrolide (P-0501A) on the functions of the isolated, perfused rat liver were compared with two known erythromycins--the base and the estolate--after 7 days of treatment (1.36 mmol/kg po daily). The in vitro metabolism of the antibiotics was induced to different extent but only the base and P-0501A were cleared from the perfusate and the liver faster than in untreated animals. In untreated rats the therapeutically active form of P-0501A was excreted in the bile more than the base and the estolate; after pretreatment, biliary excretion of all erythromycins was nearly double. The content of inactive, complexed cytochrome P-450 was increased only by the base and estolate, with various effects on microsomal activities (some induced, e.g. aminopyrine demethylation, other reduced, e.g. pentobarbital clearance). The clearance and biliary excretion of sulphobromophthalein was not affected by treatment with P-0501A or the base, but was significantly reduced by estolate.
Animals↗
Use of erythromycin for nonsurgical female sterilization in West Bengal, India: a study of 790 cases.
OBJECTIVE: Determine if erythromycin is an effective agent for achieving occlusion of the Fallopian tube for nonsurgical female sterilization. METHODS: Two studies of 100 healthy volunteers requesting sterilization were planned, one in Julpia Andhermanik and the other in Kolkata (Calcutta). A readily available marketed tablet preparation containing 500 mg of the estolate salt of erythromycin was used for the trial. In one study (Bishnupur), the tablet was crushed before placing in a copper-T IUD inserter for placement at the fundus. In the other study (Kolkata), crushed tablets were processed into 50 mg pellets of the same diameter as standard quinacrine pellets and 10 pellets were inserted at the fundus using aseptic precautions. Procedures in each study were repeated at 30 days. Oral contraceptives were prescribed for three cycles following first insertion. No incentive was offered for participation in the trial. Follow-up treatment, including first-trimester abortion for pregnancy due to failure of the sterilization procedure, was assured without charge. Due to extraordinary patient demand, one study (Bishnupur) was expanded to 690 cases for reasons of compassion. RESULTS: At 12 months of use, the failure rate of the sterilization procedure for the crushed 500 mg tablets was 35.8% (SE = 1.8) with 417 women at risk. At 12 months of use, the failure rate for the erythromycin pellets was 28.6% (SE = 5.0) with 43 women at risk. There were no serious complications reported in either trial. All pregnancies resulting from failure of the sterilization procedure were terminated by menstrual regulation within 10 weeks gestation. CONCLUSIONS: The failure rate in this study is unacceptably high for erythromycin to be used as a sterilization method.
Erythromycin↗
Gonococcal tenosynovitis-dermatitis and septic arthritis. Intravenous penicillin vs oral erythromycin.
Twenty-three patients with disseminated gonococcal infections--15 with acute tenosynovitis, six with septic monoarticular arthritis, and two with both--were randomly given five days of erythromycin stearate or estolate, 500 mg orally every six hours (13 patients), or crystalline aqueous penicillin G potassium, 1 million units intravenously every three hours for three days (ten patients). There were no treatment failures. Cultures taken one and seven days and two and four weeks after completion of therapy were uniformly negative. Clinical resolution was rapid in both groups, as judged by response of fever, joint tenderness, and disappearance of joint effusion. Orally administered erythromycin is a useful alternative to penicillin in the treatment of disseminated gonococcal infections, particularly in penicillin-allergic pregnant women.
Administration, Oral↗
Effects of a new fluorinated macrolide (P-0501A) and other erythromycins on drug metabolizing enzymes in rat liver.
The effects of a new fluorinated macrolide (P-0501A) on drug metabolizing enzymes of rat liver were compared with three erythromycins--the base, the stearate and the estolate--after 7 days of dosing (1.36 mmol/kg po daily). The three erythromycins induced the synthesis of microsomal enzymes, but the products of their metabolism inactivated cytochrome P-450 in the order base less than or equal to stearate less than estolate. N-Demethylation of erythromycin and aminopyrine increased, while O-demethylation of 4-nitroanisole was reduced and hydroxylation of aniline was not changed after in vivo treatment. Pentobarbital sleeping time was prolonged and liver glutathione levels were lower in treated rats than in controls. In contrast to the three erythromycins, P-0501A did not induce the synthesis of microsomal enzymes, did not form an inactive complex with cytochrome P-450 and did not affect mono-oxygenase activities or pentobarbital narcosis.
Administration, Oral↗
Bioavailability and stability of erythromycin delayed release tablets.
BACKGROUND: Erythromycin is available as the free base, ethylsuccinate, estolate, stearate, gluceptate, and lactobionate derivatives. When given orally erythromycin and its derivatives except the estolate are inactivated to some extent by the gastric acid and poor absorption may result. OBJECTIVES: To establish whether delayed release erythromycin tablets meet the bioequivalent requirement for the market. METHODS: Sectrophotometric analysis was used to determine the dissolution percentage of the tablets in vitro. High performance liquid chromatography and IBM/XT microcomputer was used to determine the bioavailability and pharmacokinetic parameters in vivo. RESULTS: 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% CONCLUSION: The content, appearance, and dissolution bioavailability of delayed release erythromycin tablets conforms to the United States pharmacopoeia standards. The tablets should be stored in a cool and dry place in airtight containers and the shelf life is temporarily assigned two years.
Administration, Oral↗
Effects of roxithromycin, a new semisynthetic macrolide, and two erythromycins on drug metabolizing enzymes in rat liver.
The effects of a new semisynthetic macrolide, roxithromycin, on drug metabolizing enzymes of rat liver were compared with two erythromycins, the base (EB) and the estolate (EE), after 7 days' treatment with high oral doses (400 and 800 mg/kg daily). Dose-related higher concentrations of roxithromycin were reached in serum and liver than after EB or EE. The two reference erythromycins induced the synthesis of microsomal enzymes and formed inactive cytochrome P-450-metabolite complexes. N-Demethylation of erythromycin itself and aminopyrine was increased by the treatment. Liver microsomal enzyme activities were not induced and the inactive cytochrome P-450-metabolite complex was not formed after 400 mg/kg of roxithromycin and only to a very limited extent after 800 mg/kg (10% vs. 50% after EE). At the higher dose microsomal activities were not changed by roxithromycin and only aminopyrine N-demethylation was reduced.
Animals↗
Absorption of erythromycin. A cross-over study in healthy volunteers.
The absorptions of 6 erythromycin preparations were compared in a cross-over study in healthy humans. In a single-dose study, 500 mg of each preparation was, after an overnight fast, given to 10 volunteers. The two enterosoluble preparations of erythromycin base studied were absorbed slowly, and the peak serum concentration (1.5-2 mg/l) was achieved only at 4 h. The absorption of the stearates was quick, but especially one of them was poorly absorbed, the serum concentration being always below 1 mg/l. Both of the two estolates gave highest apparent concentrations, and the maximum serum level (2-2.5 mg/l) was achieved at 2 h, but the concentration of active erythromycin remains unknown. In the second part of the study, two erythromycin stearates and one base preparation were given at 6-h interval in a cross-over fashion, each for 4 days. On the 4th day, blood samples were analyzed. The erythromycin base gave higher serum concentrations than did the two stearates, which were equivalent. It seems doubtful that the erythromycin stearate at the dose of 250 mg every 6th hour would give satisfactory serum levels of erythromycin which would be effective against most bacteria during the whole treatment.
Biopharmaceutics↗
Analysis of macrolide antibiotics by capillary electrophoresis.
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.
Acetonitriles↗
Plasma and salivary concentrations of erythromycin after administration of three different formulations.
In a 6-volunteer cross-over study the pharmacokinetics of 3 erythromycin preparations were compared. A single oral dose of 500 mg of each preparation was administered at each occasion and the levels measured in timed samples of plasma and saliva. Markedly higher blood concentrations of the estolate and propionate were obtained compared to the stearate. Comparison of serum and plasma concentration of the drugs from each split sample showed no significant differences. Plasma concentrations always exceeded those in saliva but for any one preparation a similar ratio was obtained at different times. This may be useful to ascertain compliance and to measure concentration of the compounds where direct measurement in plasma is not practicable.
Adult↗
Review article: erythromycin as a prokinetic agent in infants and children.
Erythromycin has been used as an antibiotic for more than four decades, but only in the last 10 years have other therapeutic benefits of this agent been exploited. Animal and human studies have demonstrated a prokinetic effect on the gastrointestinal tract at sub-antimicrobial doses (typically a quarter or less of the antibiotic dose). A limited number of studies have been performed in children to investigate this action. A review of this literature is particularly pertinent given the frequency of clinical problems related to gastrointestinal dysmotility in children and the limited availability of prokinetic agents in paediatric practice, compounded by the recent withdrawal of cisapride. The prokinetic effects of erythromycin have been investigated in infants with dysmotility associated with prematurity, in low birth-weight infants recovering from abdominal surgery, and in older children with a variety of other gastrointestinal disorders. Only one randomized placebo-controlled trial has been conducted. All except one of these studies have shown a beneficial effect of erythromycin in either promoting tolerance of enteral feeds or enhancing a measured index of gastrointestinal motility. Erythromycin appears to be equally effective when given orally (as ethylsuccinate or estolate) or intravenously (as lactobionate). Significantly, no serious adverse effects have been reported in studies in which erythromycin has been used for its prokinetic effects, although fatal reactions have followed the intravenous administration of erythromycin to neonates in antibiotic doses.
Administration, Oral↗
A new look at erythromycin.
This article reviews the current place of erythromycin in antibiotic therapy. Overall, erythromycin is thought to be underused because: (1) the fear of resistance has been exaggerated; (2) significant toxicity has been associated with only one derivative (the estolate); (3) newer antibiotics have very rarely been demonstrated to be superior to erythromycin. Erythromycin has an important place in treating acute upper and lower respiratory tract infections, acute otitis media, sinusitis, skin and soft tissue, osteomyelitis, prostatitis, infections due to Mycoplasma spp. and Chlamydia organisms, and infections due to anaerobes.
Bacterial Infections↗