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PubMed1993

[Reaction mechanism of macrolide 2'-phosphotransferase from Escherichia coli to the 2'-modified macrolide antibiotics].

Reaction mechanism of macrolide 2'-phosphotransferase [MPH(2')] from Escherichia coli to the 2'-modified macrolide antibiotics was analyzed by using microbioassay, nuclear magnetic resonance (NMR) spectrometric assay and mass spectrometry. It was found by microbioassay that the 2'-modified macrolide antibiotics as triacetyloleandomycin (TAO), erythromycin ethyl succinate (EME) and erythromycin estolate were inactivated with adenosine triphosphate (ATP) by MPH(2'). The NMR spectrometric assay for the analysis of the reaction with the 2'-modified macrolide antibiotics and MPH(2') was established using guanosine triphosphate, which was higher reaction rate than ATP, as a cofactor. It was clearly shown by NMR spectrometric assay and mass spectrometry that the C2'-side chain of TAO and EME was naturally released in phosphate buffer solution, and then, the C2' position was phosphorylated with GTP by MPH(2').

Anti-Bacterial Agents↗
PubMed1993

The increased risk of hospitalizations for acute liver injury in a population with exposure to multiple drugs.

We conducted a nested case-control study to estimate and compare the relative risks for hospitalizations for newly diagnosed acute liver injury associated with the use of non-steroidal antiinflammatory drugs (NSAIDs) and other hepatotoxic drugs and their interaction. The source population comprised 228,392 members of the Saskatchewan Health Plan from 1982 to 1986. We used hospital records and the databases of the Department of Health. Thirty-four cases with confirmed liver injury were hospitalized. We randomly selected 500 controls from the source population. Crude risks ranged from 1 case per 100,000 prescriptions in current users of methyldopa, ampicillin, or NSAIDs to 14 cases per 100,000 prescriptions in current users of erythromycin estolate. The age-adjusted odds ratios for current users of NSAIDs was 1.8 [95% confidence interval (CI) = 0.8-3.7] and for other hepatotoxic drugs 5.9 (95% CI = 2.8-12.4). The adjusted relative excess risk due to the interaction between current exposure to both categories of drugs was 3.6, accounting for 31% of the cases of acute liver injury among those with exposure to both types of drugs. We conclude that the risk of hospitalization for acute noninfectious liver injury is different among users of various individual potentially hepatotoxic drugs. Concomitant current exposure to two or more drugs increases this risk above what would merely be expected from the sum of the individual risks.

Acute Disease↗
PubMedDate not supplied

[Immunotoxicity of drugs].

Immunotoxicity of drugs represents an important problem for 10 to 12% of the overall population. There are 4 types immunotoxicological manifestations of drugs: immediate hypersensitivity, cytotoxic reactions, immune complexes reactions and delayed-type hypersensitivity. The most frequently concerned drugs are penicillins, cephalosporins, anesthetics (type I), erythromycin estolate, nitrofurantoin, sulfonamids, antitubercular agents (type II), quinidine, ticarcillin, valproate, pyramidon (type III) and finally for type IV, topical drugs (antihistaminic products, oestradiol, s.c. heparin).

Drug Hypersensitivity↗
PubMed1988

Selection of an erythromycin for the treatment of pertussis.

Pertussis is one of the most communicable diseases of the respiratory tract and the incidence of this disease has increased substantially in recent years. Bordetella pertussis is the major pathogen implicated and erythromycin is considered the drug of choice. Because more studies have reported bacteriological and clinical relapses with ethylsuccinate and stearate formulations than with the estolate preparation, erythromycin estolate 50 mg/kg/d in divided doses over a 14-day period is recommended for the treatment of pertussis. None of the studies, however, have directly compared various forms of erythromycin in these patients to establish superiority of one form over the others. Treatment should be initiated as soon as possible and patients should be followed closely to achieve maximal efficacy and minimize the spread of the disease.

Erythromycin↗
PubMed1984

Erythromycin therapy for group A streptococcal pharyngitis. Results of a comparative study of the estolate and ethylsuccinate formulations.

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.

Adolescent↗
PubMed1980

Selection of an oral erythromycin product.

The chemistry, bioavailability, and adverse effects of erythromycin base, stearate, estolate, and ethylsuccinate are reviewed. Criteria for the evaluation of erythromycin bioavailability studies include study design, patient population, meal composition and timing, and assay methodology. Based on these criteria, the bioavailability of individual erythromycin products are evaluated in this paper. Compared with other antibiotics, the erythromycins have a good safety record. However, both the estolate and ethylsuccinate forms of erythromycin may cause hepatotoxity. Considering bioavailability and adverse effect data, a specific brand of enteric-coated erythromycin base tablets is recommended for erythromycin-sensitive infections in adults. For pediatric patients, a liquid formulation of erythromycin estolate or erythromycin ethylsuccinate is recommended.

Administration, Oral↗
PubMed1994

Comparison of oral erythromycin formulations in the horse using pharmacokinetic profiles.

The pharmacokinetic properties of four erythromycin formulations were compared in six adult horses after administration of single and multiple oral doses. Formulations of erythromycin administered were estolate and phosphate given 37.5 mg/kg every 12 h and 25 mg/kg every 8 h, and stearate and ethylsuccinate given 25 mg/kg every 8 h. Areas under the curve (AUC) and maximum plasma erythromycin concentrations (Cmax) were equal or greater (P > or = 0.05) following administration of erythromycin phosphate and stearate compared with those values following administration of erythromycin estolate or ethylsuccinate. In comparing an 8 h vs. a 12 h dosage interval for multiple doses of erythromycin phosphate or estolate, there were no significant differences observed in AUC(24-28 h), peak-trough plasma concentrations or duration that plasma concentrations exceeded the minimal inhibitory concentration (MIC) for Rhodococcus equi. Comparisons of pharmacokinetic parameters between single and multiple doses were made for each formulation. Differences in Cmax, tmax, or t1/2 beta between single and multiple doses were demonstrated for erythromycin ethylsuccinate and estolate. Based on equivalent plasma antibiotic concentrations, erythromycin phosphate or stearate could be substituted for estolate in the treatment of Rhodococcus equi pneumonia. Furthermore, there was no advantage of an 8-h interval, compared with an interval of 12 h.

Actinomycetales Infections↗
PubMed1975

Comparison of erythromycin ethyl succinate, stearate and estolate treatments of group A streptococcal infections of the upper respiratory tract.

The microbiologic and clinical responses of acute Group A beta-hemolytic streptococcal infections of the upper respiratory tract to oral treatment with erythromycin ethyl succinate, stearate, and estolate were studied in 303 patients. Streptococcal M and T typing was done on all positive cultures. The overall cure rate was 95.4 per cent, with no statistically significant differences in clearing organisms from the pharynx. Of the 285 cured patients who completed the prescribed follow-up period, 11 had recurrences between the 12th and 31st day after initiation of therapy, and five developed new infections. No cases of rheumatic fever or glomerulonephritis were encountered during a follow-up study. Eight gastrointestinal reactions and one transient rash occurred. Results with these forms of erythromycin compare favorably with published results for similar infections treated with oral penicillins.

Administration, Oral↗
PubMed1987

High-performance liquid chromatographic assay of erythromycin and its esters using electrochemical detection.

A high-performance liquid chromatographic analysis of erythromycin and its esters in plasma, urine and saliva is presented. A diethyl ether extract of sample was chromatographed on a reversed-phase column and components of the column effluent were monitored by electrochemical detection at +0.9 V (vs. Ag/AgCl). The method sensitivity limit was 10 ng with inter-day coefficients of variation from 3.2 to 10.3%. In order to assess precisely the relative concentrations of erythromycin esters (ethylsuccinate or estolate) and their active by-product erythromycin base, it is necessary to adopt measures preventing their continuous hydrolysis in biological fluids and during sample preparation.

Chromatography, High Pressure Liquid↗
PubMed1976

Concentrations of erythromycin in serum and tonsil: comparison of the estolate and ethyl succinate suspensions.

Concentrations of erythromycin were measured in serum and tonsil from children who had received either the estolate or ethyl succinate suspension before surgery. The in vitro assay measured total erythromycin activity against a group A beta hemolytic streptococcus. Levels of erythromycin in serum and tonsil after single and multiple doses of the estolate were significantly higher than those after administration of the ethyl succinate. The therapeutic implications of these findings are unknown.

Biological Availability↗
PubMed1983

Therapeutic doses of erythromycin esteolate is not cholestatic in rats in vivo.

The effect of erythromycin esteolate (EE) on bile flow and bile acid secretion was studied in male Wistar rats in vivo. Daily oral treatment with a dose of up to 100 mg/kg for 1 week increased the bile flow and the bile acid secretion. Increasing the days of treatment to 4 weeks with a dose of 20 mg/kg did not alter the measured parameters significantly. Acute intravenous injection of erythromycin lactobionate (50 mg/kg) also increased bile flow and biliary bile acid secretion temporarily. The increase in bile flow may partly be due to the osmotic effect of the drug and its metabolites in bile. Since EE failed to produce cholestasis in the range of therapeutic doses, rats do not seem to be a suitable experimental model for studying EE-cholestasis.

Animals↗
PubMed1987

Regulation of testosterone hydroxylation by rat liver microsomal cytochrome P-450.

The pathways of testosterone oxidation catalyzed by purified and membrane-bound forms of rat liver microsomal cytochrome P-450 were examined with an HPLC system capable of resolving 14 potential hydroxylated metabolites of testosterone and androstenedione. Seven pathways of testosterone oxidation, namely the 2 alpha-, 2 beta-, 6 beta-, 15 beta-, 16 alpha-, and 18-hydroxylation of testosterone and 17-oxidation to androstenedione, were sexually differentiated in mature rats (male/female = 7-200 fold) but not in immature rats. Developmental changes in two cytochrome P-450 isozymes largely accounted for this sexual differentiation. The selective expression of cytochrome P-450h in mature male rats largely accounted for the male-specific, postpubertal increase in the rate of testosterone 2 alpha-, 16 alpha, and 17-oxidation, whereas the selective repression of cytochrome P-450p in female rats accounted for the female-specific, postpubertal decline in testosterone 2 beta-, 6 beta-, 15 beta-, and 18-hydroxylase activity. A variety of cytochrome P-450p inducers, when administered to mature female rats, markedly increased (up to 130-fold) the rate of testosterone 2 beta-, 6 beta-, 15 beta-, and 18-hydroxylation. These four pathways of testosterone hydroxylation were catalyzed by partially purified cytochrome P-450p, and were selectively stimulated when liver microsomes from troleandomycin- or erythromycin estolate-induced rats were treated with potassium ferricyanide, which dissociates the complex between cytochrome P-450p and these macrolide antibiotics. Just as the testosterone 2 beta-, 6 beta-, 15 beta-, and 18-hydroxylase activity reflected the levels of cytochrome P-450p in rat liver microsomes, so testosterone 7 alpha-hydroxylase activity reflected the levels of cytochrome P-450a; 16 beta-hydroxylase activity the levels of cytochrome P-450b; and 2 alpha-hydroxylase activity the levels of cytochrome P-450h. It is concluded that the regio- and stereoselective hydroxylation of testosterone provides a functional basis to study simultaneously the regulation of several distinct isozymes of rat liver microsomal cytochrome P-450.

Aging↗