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PubMed1994

Evaluation of pertussis treatment with erythromycin ethylsuccinate and stearate according to age.

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.

Administration, Oral↗
PubMed1988

High-performance liquid chromatography of erythromycin propionyl ester and erythromycin base in biological fluids.

The simultaneous determination of erythromycin propionate and erythromycin base in serum and urine by high-performance liquid chromatography using oleandomycin as internal standard is described. The separation was achieved on a reversed-phase C18 column employing acetonitrile-0.05 M phosphate buffer (65:35), adjusted to pH 7.0, as the mobile phase with coulometric detection. Hydrolysis of the ester during blood sample collection was minimised by immediate high-speed centrifugation of collected blood samples, followed by separation and immediate freezing of the serum fraction. A solid-phase extraction procedure, combined with a simple phase-separation step was used prior to chromatographic analysis. The method has the necessary precision, sensitivity and accuracy to allow the simultaneous determination of both components in serum and urine following a single 500-mg oral dose of erythromycin estolate.

Chromatography, High Pressure Liquid↗
PubMed1992

Absorption of various erythromycin esters and salts in mice after intragastric intubation.

Erythromycin base and its different salts and esters were given intragastrically to mice. Serum concentrations of erythromycin and its 2'-esters were determined by the bacterial growth inhibition method. Acetyl and propionyl erythromycin were the best absorbed 2'-esters, and differed significantly from butyryl erythromycin and erythromycin base. Erythromycin estolate yielded a larger area under the concentration curve than acistrate or stearate. Among the syrup preparations, erythromycin acistrate was significantly better absorbed than 2'-ethylsuccinyl erythromycin. Absorption of 2'-esters decreased with increasing number of esterified carbon atoms and increasing hydrophobicity and increasing log P value (the logarithm of octanol-water partition coefficient). In addition to sufficient lipophilicity, the optimum absorption of erythromycin esters seems to require a high hydrophilicity.

Animals↗
PubMed1988

Immunochemical similarity of P-450 HFLa, a form of cytochrome P-450 in human fetal livers, to a form of rat liver cytochrome P-450 inducible by macrolide antibiotics.

A protein immunochemically related to P-450 HFLa, a form of cytochrome P-450 purified from human fetal livers, was detected in rat liver microsomes. The content of the immunoreactive protein in rat liver microsomes was increased by treatments with phenobarbital, pregnenolone 16 alpha-carbonitrile (PCN), erythromycin, erythromycin estolate, and oleandomycin but not with 3-methylcholanthrene, imidazole, ethanol, isosafrole, josamycin, midecamycin, or miocamycin. The activity of erythromycin N-demethylase correlated with the content of the immunoreactive protein in rat liver microsomes (r = 0.72). In addition, anti-P-450 HFLa IgG inhibited erythromycin N-demethylase in liver microsomes from erythromycin- or oleandomycin-pretreated rats. Furthermore, the content of the immunoreactive protein highly correlated with that of P-450 PB-1, which is distinct from Waxman's terminology, and is one of the forms of PCN-inducible cytochrome P-450s (r = 0.95). From these results and the results reported so far, it seems possible that P-450 HFLa is one of the forms of cytochrome P-450 inducible by glucocorticoids.

Animals↗
PubMed2006

Investigation of the hepatotoxicity profile of chemical entities using Liverbeads and WIF-B9 in vitro models.

The cytotoxicity profile of various chemical entities was evaluated using two in vitro hepatocyte models. Liverbeads is a cryopreserved model consisting of primary hepatocytes entrapped in alginate beads. WIF-B9 is a hybrid cell line obtained by fusion of rat hepatoma (Fao) and human fibroblasts (WI38). Various reference hepatotoxicants were tested and ranked according to their equivalent concentration 50 (EC50) for various biochemical endpoints (lactate dehydrogenase (LDH) release, 3-(4,5 dimethylthiazol 2yl)-2,5-diphenyl-2H tetrazolium bromure (MTT) activity, adenosine triphosphate (ATP) and glutathione (GSH) levels). The ranking obtained was comparable in both models and consistent with previously published results on hepatocyte monolayers. Ketoconazole, erythromycin estolate, retinoic acid, telithromycin and alpha-naphthyl-isothiocyanate were among the most toxic chemicals in both models, with an EC50 < 200 microM. Troleandomycin, spiramycin, erythromycin, diclofenac, taurodeoxycholate, warfarin, galactosamine, valproic acid and isoniazid were found to be less toxic. Few marked differences, potentially linked to metabolism pathways, were observed between EC50s in the two models for compounds such as cyclosporine A (10 and > 831 microM) and warfarin (5904 and 1489 microM) in WIF-B9 and Liverbeads, respectively. The results obtained indicate that Liverbeads and WIF-B9 cells are reliable in vitro models to evaluate the hepatotoxic potential of a wide range of chemicals, irrespective of structure and pharmaceutical class.

Adenosine Triphosphate↗
PubMed1990

Pharmacokinetic evaluation of erythromycin and caffeine administered with bromocriptine.

A study was performed to determine if the pharmacokinetics of bromocriptine is altered by factors that have been shown to interact with other ergot compounds. The effects on bromocriptine plasma concentrations by bromocriptine coadministration with caffeine and erythromycin were evaluated in five male volunteers. Serial blood samples were obtained during a 12-hour period after a single 5 mg oral dose of bromocriptine (alone and after 4-day treatments of either erythromycin estolate, 250 mg four times/day, or caffeine, 200 mg four times/day). There were no significant alterations of bromocriptine pharmacokinetic parameters after caffeine, although statistical power was very low. With the use of erythromycin, the bromocriptine area under the concentration-time curve standardized to body weight increased significantly by 268%, whereas peak bromocriptine plasma concentration (Cmax) increased to 4.6 times the Cmax from bromocriptine alone. Time to achieve Cmax was not altered by erythromycin. We conclude that erythromycin can markedly increase the systemic bioavailability of bromocriptine, which can lead to increased therapeutic or adverse effects, whereas the effects of caffeine require further study.

Adult↗
PubMed1977

Tetracyclines, chloramphenicol, erythromycin, and clindamycin.

Tetracyclines are active in vitro against most urinary tract pathogens, Chlamydia, Mycoplasma pneumoniae, Brucella, rickettsiae, and Nocardia. Chloramphenicol is used primarily for anaerobic infections, Haemophilus influenzae meningitis, and infections due to Salmonella typhi. Erythromycin is active in vitro against M. pneumoniae, Streptococcus pneumoniae, and group A beta-hemolytic streptococci. Erythromycin may be used as prophylactic therapy for subacute bacterial endocarditis and for recurrence of acute rheumatic fever in patients who are allergic to penicillin. Clindamycin should be used only for the treatment of anaerobic infections. Tetracycline may cause gastrointestinal upset; phototoxic dermatitis; hepatitis, especially in pregnant females; discoloration of teeth and bone dysplasia in the human fetus and children; and suprainfections, especially oral and anogenital candidiasis. Tetracycline should be used with caution in patients with renal insufficiency. The most important toxic effect of chloramphenicol is bone marrow suppression, which is dose related and idiosyncratic. The incidence of undesirable side effects associated with the use of erythromycin is low. Gastrointestinal irritation is the most common; cholestatic hepatitis may occur with erythromycin estolate. Pseudomembranous colitis is the most important toxic effect associated with clindamycin.

Anaerobiosis↗
PubMed1995

Effect of oral erythromycin on patients with diabetic gastroparesis.

BACKGROUND: Abnormal gastrointestinal motility is a well recognized complication of diabetes mellitus, and disordered gastric emptying may hamper glycemic control. The objects of this study were to investigate the effect of oral erythromycin on gastric emptying and to evaluate the effect of corrected gastric emptying on glycemic control in patients with diabetic gastroparesis. METHODS: 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. RESULTS: The GETt1/2 decreased from 198.0 +/- 58.9 minutes at baseline to 139.1 +/- 67.6 minutes following one day of erythromycin therapy (p < 0.01), and to 137.1 +/- 71.2 minutes after two weeks of treatment (vs. baseline p < 0.01). The FBS decreased from 159.0 +/- 40.2 mg/dl at baseline to 149.0 +/- 38.5 mg/dl following one day of therapy (p = 0.12, NS), and to 139.2 +/- 39.8 mg/dl after two weeks of treatment (vs. baseline p < 0.02). CONCLUSIONS: It was concluded that erythromycin is an effective prokinetic agent for diabetic gastroparesis, and that corrected gastric emptying may improve glycemic control.

Administration, Oral↗
PubMed1983

Tetracyclines, chloramphenicol, erythromycin, and clindamycin.

The tetracyclines are active in vitro against many urinary tract pathogens such as Chlamydia, Mycoplasma pneumoniae, Brucella, rickettsiae, and Nocardia. Chloramphenicol is used primarily for anaerobic infections, Haemophilus influenzae meningitis, and infections due to Salmonella typhi. Erythromycin is active in vitro against M. pneumoniae, Legionella spp., Streptococcus pneumoniae, and group A beta-hemolytic streptococci; it may also be used as prophylactic therapy for subacute bacterial endocarditis and for recurrence of acute rheumatic fever in patients who are allergic to penicillin. Clindamycin should be used primarily for the treatment of anaerobic infections. The tetracyclines may cause gastrointestinal upset; phototoxic dermatitis; hepatitis, especially in pregnant women; discoloration of the teeth and bone dysplasia in the human fetus and in children; and superinfections, especially oral and anogenital candidiasis. The tetracyclines should be used with caution in patients with renal insufficiency. The most important toxic effect of chloramphenicol is bone marrow suppression, which is dose related or idiosyncratic. The incidence of undesirable side effects associated with the use of erythromycin is low; gastrointestinal irritation is the most common, and cholestatic hepatitis may occur with the use of erythromycin estolate. Pseudomembranous colitis is the most important toxic effect associated with the use of clindamycin.

Bacterial Infections↗
PubMed1987

Effect on birth weight of erythromycin treatment of pregnant women.

To test the hypothesis that treatment with antibiotics prevents low birth weight, pregnant women whose vaginal cultures contained Ureaplasma urealyticum or Mycoplasma hominis (or both) and who gave written informed consent were treated with one of the following: identical looking capsules containing 250 mg of either erythromycin estolate or stearate (active against U urealyticum), or 150 mg of clindamycin hydrochloride (active against M hominis), or placebo, four times daily for six weeks in a randomized double-blind study. Treatment with clindamycin had no effect. Treatment with erythromycin initiated during the second trimester had no effect on mean birth weight or on the frequency of low-birth-weight infants. In contrast, women whose treatment with erythromycin was initiated in the third trimester gave birth to infants with a heavier mean birth weight (3331 g) than infants born to placebo-treated women (3187 g) (P = .042). Similarly, in women whose erythromycin was begun during the third trimester, the birth rate of infants weighing 2500 g or less was 3%, whereas in women treated with placebo, the birth rate for low-birth-weight infants was 12% (P = .047). These data suggest that treatment with erythromycin during the third trimester prevents low birth weight in mycoplasma-colonized pregnant women. Whether the effect is due solely to the action of erythromycin on U urealyticum is uncertain.

Birth Weight↗
PubMed1983

Pharmacokinetics of erythromycin in foals and in adult horses.

The pharmacokinetic parameters of erythromycin in foals were determined following intravenous administration of 5.0 mg/kg to animals aged 1, 3, 5 and 7 weeks. The distribution of the drug was described by a two-compartment open model, and no significant differences were observed between coefficients on which the parameters were based. Pharmacokinetic values were also determined for four mares given 5.0 mg/kg intravenously and for six 10-12-week-old foals given 20.0 mg/kg intravenously. The half-life of erythromycin for all groups of animals (foals less than 7 weeks, mares, foals 10-12 weeks) was 1.0-1.1 h; the apparent volume of distribution was between 2.3 and 7.2 l/kg, and the clearance of the drug from the body was between 1.9 and 5.0 mg/kg/h. No drug could be detected in the serum following oral administration of 5.0 mg/kg erythromycin estolate; detectable levels were found for 5 h in mares given 12.5 mg/kg, and for 8 h in foals given 20.0 mg/kg orally. Peak levels in foals given the drug orally were 0.42 micrograms/ml at 120 min after administration. Foals given 10.0 mg/kg of erythromycin base intramuscularly had serum concentrations detectable 12 h later; the peak level achieved was 1.44 micrograms/ml serum 90 min after administration and concentrations exceeded 0.25 micrograms/ml for 6 h. In the mares the milk concentrations were approximately twice those in serum. Recommendations were made for drug dosage to be used in the treatment of Corynebacterium equi pneumonia of foals.

Administration, Oral↗
PubMed1974

Diphtheria carriers and the effect of erythromycin therapy.

One hundred and fourteen Corynebacterium diphtheriae, toxigenic, gravis type, pharyngeal carriers were identified during a diphtheria epidemic in Elgin, Texas. All carriers were treated with erythromycin estolate, 1 g/day in divided doses for 6 days. Serial pharyngeal cultures were obtained in order to monitor the bacteriological response. Seventy-two carriers had positive cultures immediately prior to the start of therapy, and only these individuals were considered in the analysis of the effects of erythromycin. Forty-eight hours after institution of therapy, 96% of the carriers had become culture negative; all were negative by the 4th day of therapy, and all remained culture negative while taking the drug. Two days after cessation of therapy, all but one (99%) were culture negative. However, upon reculture 2 weeks later, 15 (21%) had relapsed to the carrier state. There were no significant differences in the serum diphtheria antitoxin levels, immunization status, age, sex, or socioeconomic status of those who relapsed and those who remained culture negative. This study demonstrates that erythromycin is effective in converting carriers to culture-negative status, but when given for only 6 days it is associated with large numbers of relapses. Because previous studies have not included follow-up cultures 2 weeks after therapy, it is suggested that all C. diphtheriae carriers be treated with either erythromycin or penicillin and that all be recultured at a minimum of 2 weeks after completion of therapy to assure eradication of the diphtheria organisms.

Adolescent↗
PubMed1987

Diagnostic methods for Chlamydia trachomatis disease in neonates.

Chlamydia trachomatis is an obligate intracellular parasite responsible for many clinical syndromes, including neonatal conjunctivitis and pneumonia. The gold standard of diagnosis has been isolation in cell culture. However, this requires days of processing. Several rapid diagnostic tests are available. Giemsa staining of conjunctival smears, enzyme immunoassay, and the fluorescein-conjugated monoclonal antibody test. Both the EIA and the FA tests show promise as ideal rapid diagnostic tests. Treatment of chlamydial conjunctivitis must focus upon the eradication of nasopharyngeal carriage as well as cure of ophthalmic symptoms. The need for nasopharyngeal eradication is underscored by the fact that it is the source for chlamydial pneumonia as well as for conjunctival re-infection. Clinical studies have shown that oral erythromycin estolate or ethylsuccinate suspension 50 mg/kg/day twice-daily or four times a day for 14 to 21 days are the therapeutic regimens of choice. Neonatal ocular prophylaxis is currently under study. One per cent silver nitrate does not prevent chlamydial conjunctivitis but preliminary studies do show favorable results with topical erythromycin. Nevertheless, neither 1 per cent silver nitrate nor topical erythromycin eradicate nasopharyngeal carriage, elimination of which is necessary for the prevention of neonatal chlamydial pneumonia.

Conjunctivitis, Inclusion↗
PubMed1987

An evaluation of tolerance of roxithromycin in adults.

This review deals with tolerance of a new macrolide, roxithromycin from data collected from a number of studies in adults. A total of 2917 adults, 2519 given roxithromycin 150 mg bid, were recruited into 17 multicentre comparative or non-comparative studies. Nine studies were double-blind, against doxycycline, erythromycin estolate (EES), lymecycline or cephradine. Overall the drug was well tolerated: side-effects possibly or probably related to roxithromycin were noted in only 4.1% (120/2917) of all patients, and in 3.1% (15/480) of elderly subjects. The gastrointestinal tolerance of roxithromycin was significantly better than that of doxycycline in four trials, and better than that of erythromycin ethylsuccinate in one study. The incidence of drug-related liver function test abnormalities following roxithromycin therapy was low and compared favourably with data published on erythromycin. Roxithromycin shows a satisfactory safety profile at the recommended daily dosage of 150 mg bid in adults.

Adult↗
PubMed1966

An effective antibiotic cover for the prevention of endocarditis following dental and other post-operative bacteraemias.

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.

Endocarditis, Bacterial↗
PubMed1993

Acute liver disease associated with erythromycins, sulfonamides, and tetracyclines.

OBJECTIVE: To determine whether erythromycins, sulfonamides, and tetracyclines are associated with an increased risk for acute hepatitis. DESIGN: Case-control study. SETTING: Medicaid billing data from Michigan and Florida between 1980 and 1987. PATIENTS: The 107 cases included patients hospitalized with acute symptomatic hepatitis without an identifiable cause of liver disease noted in the medical record. Four controls per case were randomly selected and were matched for age, sex, and state. RESULTS: Five cases (4.7%) and four controls (0.9%) were exposed to erythromycins, yielding an odds ratio of 5.2 (95% Cl, 1.1 to 26.6). No case or control was exposed to erythromycin estolate. Eight cases (7.5%) and three controls (0.7%) were exposed to oral sulfonamides, yielding an odds ratio of 11.4 (Cl, 2.7 to 67.8). All (except one control) had received trimethoprimsulfamethoxazole. Five cases (4.7%) and four controls (0.9%) were exposed to tetracyclines, yielding an odds ratio of 5.2 (Cl, 1.4 to 19.7). The results did not change substantively for erythromycin or sulfonamides after adjustment using multiple logistic regression for age, sex, state, and use of other hepatotoxic drugs. With tetracyclines, however, the odds ratio decreased to 3.6 (Cl, 0.9 to 14.3). Associations were also seen with isoniazid (P = 0.008) and rifampicin (P = 0.04). The number of patients developing acute symptomatic liver disease resulting in hospitalization for each million patients treated with a 10-day course of erythromycin was 2.28 cases; for sulfonamides, this figure was 4.8 cases; and for tetracycline, the figure was 1.56 cases. CONCLUSION: 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.

Acute Disease↗
PubMed1980

Factors determining the passage of drugs from blood into saliva.

1. Following single oral dosing of ampicillin, cephalexin, tetracycline, erythromycin estolate, clindamycin and rifampicin to six normal volunteers, antibacterial activity was measured at 1, 3 and 6 h in serum, gingival fluid and minor gland saliva from all subjects and in parotid and submandiabular saliva from three. 2. pH values of all gingival fluid and saliva specimens were noted. 3. Partition coefficients between n-octanol and water were measured for erythromycin, clindamycin and rifampicin. Published data were used for ampicillin, cephalexin and tetracycline. 4. All antibiotics, but particularly rifampicin, were detected in gingival fluid. Only rifampicin and to a lesser degree, clindamycin were present in the other salivary constituents. 5. In studies of secretion of drugs in saliva, both the physico-chemical characteristics of the drugs and the physiological differences between individual salivary components should be considered. 6. Parotid saliva samples are likely to be of greatest value.

Adult↗