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PubMed2004

Direct inhibition of rat detrusor muscle contraction by erythromycin.

PURPOSE: Detrusor instability is a common problem in the elderly, which is usually treated with anti-cholinergic medication. This study investigates the effect of erythromycin on rat detrusor muscle contractile response to characterise its potential as an alternative inhibitor of bladder muscle contraction. MATERIALS AND METHODS: Strips of rat detrusor muscle were suspended in a perfusion organ bath. The contractile response to direct muscle stimulation, electrical field stimulation (EFS, 0.5-60 Hz), carbachol (10(-5) M), and potassium (10-80 x 10(-3) M) were determined before and after the addition of erythromycin (10(-4)-10(-3) M). The contractile response to carbachol (10(-5) M) in the presence of nifedipine (10(-8) or 10(-6) M) or in calcium-free Kreb's solution was also determined in the absence and presence of erythromycin. RESULTS: Erythromycin 5 x 10(-4) M inhibited the maximum contractile response to EFS, carbachol, and potassium by 38% (P < 0.01), 62% (P < 0.001), and 17% (P < 0.05), respectively, but did not significantly reduce the response to direct muscle stimulation. The atropine-resistant component of EFS-evoked contraction was inhibited by 19.5% (P < 0.01) in the presence of erythromycin. In calcium-free Krebs solution, the maximum contractile response to carbachol was reduced by 42% of control (P < 0.0001) and nifedipine 10(-8) M had no additional effect. When erythromycin 5 x 10(-4) M was added together with nifedipine 10(-8) M, the response to carbachol was inhibited by a further 25% (P < 0.005). CONCLUSIONS: Erythromycin inhibits rat detrusor muscle contraction through the inhibition of calcium influx and the modulation of intracellular calcium movement.

Adenosine Triphosphate↗
PubMed1981

The effects of erythromycin on the absorption and disposition of kinetics of theophylline.

The effects of erythromycin on the kinetics of theophylline were investigated in eight female patients with documented asthma in a crossover study. Theophylline pharmacokinetics were determined at steady state before and after one-week treatment with erythromycin stearate 250 mg given four times a day. Multiple serum samples were collected for 12 h after an aminophylline dose in the two drug treatment phases and assayed by high performance liquid chromatography. The resultant serum theophylline concentration-time data were analyzed by weighted, nonlinear regression analysis to obtain various pharmacokinetic parameters. In this study, the elimination half-live increased from 7.8 +/- 1.7 h on the control day to 9.5 +/- 1.4 h following treatment with antibiotic (p less than 0.02). The estimated apparent volume of distribution for theophylline (V/F) was also observed to increase from 0.42 +/- 0.09 l/kg before treatment with erythromycin to 0.53 +/- 0.15 l/kg after antibiotic treatment (0.05 less than p less than 0.10). In this study, no difference was demonstrated in the apparent clearance rate (Clapp), apparent first-order absorption rate constant (ka), maximum serum drug concentration (Cmax), time of maximum drug concentration (Tmax) or absorption lag time (tlag) for theophylline before and after treatment with erythromycin. With no apparent alteration in theophylline clearance following erythromycin coadministration, the decrease in the first-order elimination rate constant suggested that the apparent volume of distribution of theophylline is increased in the presence of erythromycin. It is concluded that patients maintained on theophylline derivatives should be closely monitored when erythromycin is coadministered.

Adult↗
PubMed1987

The interaction of erythromycin with theophylline.

We have studied the interaction of erythromycin with theophylline. We gave ten healthy volunteers theophylline as an intravenous loading dose (5 mg X kg-1) over 1 h, followed by a maintenance infusion (0.5 mg X kg-1 X h-1) for 5 h. A second infusion of theophylline was given after 9 days of treatment with 1 g erythromycin base daily, and the concentrations of theophylline were determined during the infusion periods. The concentrations of erythromycin were measured for 8 h, after one week of treatment, and also after the last erythromycin dose, simultaneously with the second theophylline infusion. Concentrations within the therapeutic range were obtained with both drugs. A significant increase in both AUC and mean plasma concentrations of theophylline was seen during erythromycin treatment. The plasma clearance of theophylline was reduced in 9 of the 10 subjects. Renal clearance increased correspondingly, but the change was not statistically significant. Serum concentrations of erythromycin fell significantly, by more than 30%, with concurrent theophylline medication. We conclude that an interaction between theophylline and erythromycin, affecting both drugs, can be shown with concentrations of the drugs within the therapeutic range.

Adult↗
PubMed1982

[Binding, distribution and efficacy of erythromycin (author's transl)].

The significance of the binding of antibiotics in humans in still a controversial question. In principle, only free, unbound antibiotic is considered to be diffusible and biologically active. With unimpaired measurements and a binding balance within the normal therapeutic concentration range, the free portion of erythromycin in the human serum is found to depend significantly on the total concentration of erythromycin. For example, for concentrations of 1, 16 and 24 mg/l, approx. 74%, 54% and 46% are bound (+38 degrees C). binding is temperature-dependent and decreases with decreasing temperature. At +4 degrees C, 44% of 1 mg/l and 30% of 16 mg/l are bound. These binding characteristics are based in part on the properties of erythromycin's major binding partner in the serum - acidic alpha1-glycoprotein. Albumin only contributes slightly to the overall binding and is not concentration-dependent in the therapeutic range, i.e. it cannot be saturated. Binding phenomena have a decisive influence on the distribution of an antibiotic within an organism. In the case of erythromycin, the tissue levels in nearly every organ are higher, sometimes considerably higher, than the corresponding serum levels. We have shown the binding of erythromycin to cytosol and particle fractions in certain organs and compared this to the binding in the serum. The antibacterial principle regarding the efficacy of erythromycin is also based primarily on a binding reaction which maintains the concentration gradient for the intake of erythromycin in microorganisms. The kinetics ofintake (microorganism) are compared to those of binding (macroorganism) and referred to the minimum inhibitory concentration.

Erythromycin↗
PubMed1992

Possible risk for cardiac arrhythmia related to intravenous erythromycin.

OBJECTIVE: To evaluate the incidence of prolongation of the rate-corrected electrocardiographic QT interval (QTc) and of ventricular arrhythmia associated with intravenous administration of erythromycin lactobionate. DESIGN: A consecutive series of 7 critically ill patients treated with intravenous erythromycin for severe pneumonia. SETTING: A medical intensive care unit of a university hospital. MEASUREMENTS AND RESULTS: Registration of QTc duration before and after intravenous administration of erythromycin as a short infusion. Blood chemistry, hemodynamic variables, arrhythmias, and co-medications were recorded. Evaluation of at least 10 ECG intervals by 2 experienced investigators who were blinded as to the time of drug administration. If several measurements were performed in the same patient, only the mean value was used for further analysis. During 12 of 13 drug administrations studied in 7 patients QTc prolongation was observed. The extent of QTc prolongation was significantly correlated with the infusion rate (mg/min, r = 0.765, p = 0.05). In 3 patients ventricular arrhythmia occurred in close temporal relation to the erythromycin infusion; two of them developed ventricular fibrillation shortly after the first and second dose of erythromycin, respectively, and died within 3 h. CONCLUSION: In critically ill patients erythromycin-induced QTc prolongation is a frequent pharmacologic effect correlated with erythromycin infusion rate. To avoid changes in electrocardiographic intervals and thereby possibly potentially life-threatening ventricular arrhythmia administration with the lowest possible infusion rate and close cardiac rhythm monitoring are advisable in these patients.

Aged↗
PubMed1994

Motilin agonist erythromycin increases human lower esophageal sphincter pressure by stimulation of cholinergic nerves.

During phases II and III of the migrating motor complex, there is an increase in plasma motilin level that is synchronous with phasic and tonic contractile activity of the lower esophageal sphincter and of the stomach. The action of motilin on human lower esophageal sphincter is proposed to be mediated by cholinergic mechanisms. Recently, it has been shown that erythromycin was a motilin agonist. This study evaluated the pharmacological effects and the mechanisms of action of intravenous erythromycin on esophageal motility in humans. Healthy volunteers were studied three times at seven-day intervals in a randomized, double-blind fashion. Subjects were first studied for 10 min before drug administration. Afterwards, they received blindly and randomly an intravenous injection of placebo or atropine (12 micrograms/kg) followed by a 20-min continuous intravenous administration of placebo or erythromycin (150 mg). The difference (delta) between lower esophageal sphincter pressure and the duration, amplitude, and velocity of peristaltic contractions during the control period and after administration of drugs was compared. Erythromycin significantly increased (P < 0.05) the lower esophageal sphincter pressure (16.8 +/- 4.7 mm Hg) compared to placebo (-0.029 +/- 1.4 mm Hg). Erythromycin significantly decreased peristaltic contraction velocity compared to placebo (P < 0.05). The effects of erythromycin on lower esophageal sphincter pressure were completely blocked by previous administration of intravenous atropine. Erythromycin increased the number of fundic contractions compared to the placebo, but this effect was not blocked by the previous administration of atropine.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1993

Antibiotic treatment of sinusitis in general practice. A double-blind study comparing ofloxacin and erythromycin.

The present study compared ofloxacin and erythromycin in a double-blind study with parallel groups for clinical efficacy and the number and severity of adverse reactions in patients treated in general practice for acute or chronic sinusitis. All patients lived in medium-sized to large towns and rural districts in the northern and western parts of Sealand, Funen and eastern Jutland, Denmark. Three hundred and nineteen patients were enrolled in the study, of whom 280 were clinically evaluable. From this total number, 136 patients were treated with ofloxacin (31 males and 105 females) and 144 patients were treated with erythromycin (40 males and 104 females). Following administration of either ofloxacin 400 mg once daily or erythromycin 500 mg twice daily for 7-14 days, 94.9% of the ofloxacin-treated group and 94.4% of the erythromycin-treated group were cured of their infections. There was no difference in clinical efficacy. Complications occurred in 18 of 155 patients in the ofloxacin-treated group and 32 of 164 in the erythromycin-treated group (P < 0.05), corresponding to 27 and 45 symptoms respectively (P < 0.01). This difference in adverse reactions principally involved gastrointestinal symptoms, i.e. 19 in the ofloxacin-treated group and 41 in the erythromycin-treated group (P < 0.01). Present findings show that the two antibiotics are comparable as to clinical efficacy, but the frequency of adverse reactions is significantly higher in the erythromycin-treated group due to the greater incidence of gastrointestinal adverse reactions.

Adolescent↗
PubMed2005

Effect of multiple-dose erythromycin on everolimus pharmacokinetics.

OBJECTIVE: We sought to quantify the influence of the CYP3A inhibitor erythromycin on the pharmacokinetics of everolimus, a CYP3A substrate. METHODS: This was a two-period, single-sequence, crossover study in 16 healthy subjects. In period 1, subjects received the reference treatment of a single 2-mg dose of everolimus. In period 2, they received the test treatment of erythromycin 500 mg three times daily for a total of 9 days and a single 2-mg dose of everolimus coadministered on the fifth day of erythromycin therapy. The test/reference ratio and 90% confidence interval (CI) were derived for everolimus C (max) and AUC. RESULTS: During erythromycin coadministration, everolimus C (max) increased 2.0-fold (90% CI, 1.8-2.3) from 20+/-5 ng/ml to 40+/-10 ng/ml. Everolimus AUC increased 4.4-fold (90% CI, 3.5-5.4) from 116+/-37 ng h/ml to 524+/-225 ng h/ml. Everolimus half-life was prolonged by 39% from 32+/-6 h to 44+/-6 h. Erythromycin predose concentrations were not changed after single-dose administration of everolimus. CONCLUSION: Multiple-dose erythromycin increased single-dose everolimus blood levels by an average 4.4-fold (range, 2.0-12.6). During erythromycin treatment, a compensatory everolimus dose reduction should be made guided by everolimus therapeutic drug monitoring.

Adult↗
PubMedDate not supplied

Hyperglycemia attenuates erythromycin-induced acceleration of solid-phase gastric emptying in healthy subjects.

BACKGROUND: Acute hyperglycemia has been associated with delayed gastric emptying of solid foods in healthy control subjects. Erythromycin has been found to be a gastrointestinal prokinetic agent in humans. We examined whether acute steady-state hyperglycemia reduces the erythromycin-induced acceleration of gastric emptying of a solid meal after a fasted state in healthy subjects. METHODS: Twelve healthy subjects ate standard solid meals that had been radiolabeled. Gastric emptying was measured by scintigraphy during normoglycemia (5-8.9 mmol/L glucose) and hyperglycemia induced by intravenous glucose (16-19 mmol/L glucose) after administration of placebo or 200 mg of erythromycin intravenously. Emptying was measured randomly on 4 different days. RESULTS: Administration of erythromycin during normoglycemia or induced hyperglycemia compared with placebo accelerated the gastric emptying of the solid meal but did not completely normalize the delay caused by hyperglycemia versus normoglycemia (p < 0.001). In both conditions, erythromycin versus placebo significantly reduced the lag-phase duration (9.7 +/- 2.3 min and 22.0 +/- 3.9 min vs. 38.3 +/- 5.7 min and 49.5 +/- 6.0 min, respectively; p < 0.001), gastric emptying of the half meal (39.2 +/- 4.0 min and 52.0 +/- 7.1 min vs. 75.7 +/- 11.8 min and 94.0 +/- 13.4 min, respectively; p < 0.001), and the percentage of meal retained in the stomach 120 min postprandially (p < 0.001). CONCLUSION: The erythromycin-induced acceleration effect on gastric emptying was related to the plasma glucose level. Hyperglycemia might have chosen a cholinergic antagonist pathway that delayed gastric emptying of solids. Even though induced hyperglycemia inhibited gastric emptying, erythromycin accelerated the gastric emptying rate through two distinct pathways: cholinergic and noncholinergic.

Adult↗
PubMed2002

High frequency of erythromycin A resistance and distribution of mefE and ermB genes in clinical isolates of Streptococcus pneumoniae in Japan.

The ermB and mefE genes are important in terms of their responsibility for macrolide resistance in Streptococcus pneumoniae. We investigated the distribution of the ermB and mefE genes in erythromycin A-resistant S. pneumoniae isolated in our hospital during the period 1995-1998. All amoxicillin-low-susceptible isolates were considered to be resistant to erythromycin A. All isolates with resistance to erythromycin A (minimum inhibitory concentrations [MICs], > or =0.5 microg/ml) possessed ermB or mefE genes. The MICs of erythromycin A for most mefE-positive isolates ranged from 0.5 to 2 microg/ml. On the other hand, approximately 85% of ermB-positive isolates demonstrated high-level resistance to erythromycin A (MICs, > or =4 microg/ml) while the others showed low-level resistance (MICs, 0.5 to 2 microg/ml). In ermB-positive isolates with low-level resistance, high-level resistant mutants were selected with a frequency of 3.1 x 10(-6)-1.8 x 10(-3) on agar containing 4-32 MIC of erythromycin A, whereas in mefE-positive isolates, no high-level resistant mutants were detected. Mutants from ermB-positive isolates with low-level resistance showed reversibility and heterogeneity. Our data indicated a wide distribution of erythromycin A-resistant isolates with mefE or ermB genes among amoxicillin-low-susceptible S. pneumoniae in Japan. In addition, it is likely that ermB-positive isolates with low-level resistance show heterogeneous high-level resistance.

Amoxicillin↗
PubMed2007

Pharmacokinetic profile of erythromycin after intramammary administration in lactating dairy cows with specific mastitis.

The pharmacokinetics of erythromycin was studied in five lactating dairy cows following single intramammary infusion of 300 mg erythromycin in each of two quarters per cow with specific mastitis. Levels of erythromycin in plasma and quarter milk samples were measured by agar plate diffusion assay using Micrococcus luteus (ATCC 9341) as the test organism. Erythromycin level in plasma reached a peak concentration value (C(max)) of 0.07 +/- 0.01 microg/ml at 30 min; thereafter, levels declined gradually to reach 0.05 +/- 0.00 microg/ml 12 h post drug administration. The pharmacokinetic profile of the drug revealed mean absorption half life (t(1/2 ka)) as 0.26 +/- 0.05 h. The drug was eliminated slowly with elimination half-life (t(1/2 beta)) of 13.75 +/- 0.35 h and elimination rate constant (k(el)) of 0.04 +/- 0.00 h(-1). The volume of distribution based on the zero-time plasma concentration intercept of the least-squares regression line of the elimination phase (V(d(B))) was 0.032 L/kg. The drug crossed to untreated quarters also; mean drug levels of 0.20 +/- 0.07, 0.23 +/- 0.07, 0.17 +/- 0.04, and 0.17 +/- 0.04 microg/ml were found at 3, 6, 8 and 12 h, respectively. The mean drug concentration for treated quarters was measured as 22.97 +/- 2.31 microg/ml milk at first milking (12 h) following drug infusion. No apparent adverse reaction was seen in cows administered erythromycin. It is concluded that following intramammary infusion erythromycin diffuses readily and extensively in various body fluids and tissues and adequate concentration is maintained in udder tissues for at least 12 h post intramammary administration. Thus, erythromycin may be recommended for local therapy of acute mastitis caused by Gram-positive bacteria in lactating dairy cows.

Animals↗
PubMed1991

Erythromycin enhances delayed gastric emptying in dogs after Roux-Y antrectomy.

Delayed gastric emptying occurs in up to 50% of patients after truncal vagotomy and Roux-Y antrectomy and is often resistant to nonsurgical therapy. This study evaluates the effect of erythromycin, metoclopramide, and motilin on delayed gastric emptying in four dogs after Roux-Y antrectomy. Solid food gastric emptying was measured using a radionuclide technique. Study groups were: (1) saline control; (2) erythromycin 1 mg/kg intravenously over 1 hour; (3) erythromycin 3 mg/kg by mouth 45 minutes prior to feeding; (4) metoclopramide 0.6 mg/kg intravenously over 1 hour; and (5) motilin 500 ng/kg intravenously over 1 hour. After Roux-Y antrectomy, saline control dogs had 73% +/- 5% (SEM) gastric retention at 2 hours. After intravenous and oral erythromycin, gastric emptying improved at 2 hours to 27% +/- 6% and 39% +/- 5% (p less than 0.01 compared with control). Erythromycin intravenously and by mouth improved gastric emptying compared with metoclopramide (64% +/- 8%, p less than 0.05). Motilin enhanced gastric emptying to a similar degree as erythromycin, with a 2-hour gastric retention of 37% +/- 4% (NS). Erythromycin improved gastric emptying in dogs with severe Roux-Y gastroparesis and may have clinical application.

Administration, Oral↗
PubMed1986

The binding protein of erythromycin in human serum.

Erythromycin binding to human serum albumin and to alpha 1-acid glycoprotein was measured under conditions of binding equilibrium. At therapeutical concentrations of erythromycin the binding to albumin is not saturable. The fraction of total erythromycin bound to alpha 1-acid glycoprotein is proportionally related to the protein concentration and is bound to a single class of binding sites with an apparent association constant Ka = 0.16 X 10(6) M-1 (38 degrees). About one mole of erythromycin is bound per mole of alpha 1-acid glycoprotein. The binding affinity can be enhanced and vice versa lowered by increasing the concentrations of NaCl and urea, respectively. The semilogarithmic plot of bound/free ratios vs log concentration of NaCl or urea exhibits linear relationships. Erythromycin binding can be competitively inhibited by mersalyl (Ki = 11-16 microM) but not by other SH-reagents or by neuraminidase treatment. A marked reduction of erythromycin binding to alpha 1-acid glycoprotein is seen with dithiothreitol. alpha 1-acid glycoprotein is the main erythromycin binding protein in human serum.

Binding Sites↗
PubMed1991

The inhibition of drug oxidation by anhydroerythromycin, an acid degradation product of erythromycin.

The inhibition of steroid 6 beta-hydroxylase activity by anhydroerythromycin, an acid breakdown product of erythromycin, has been studied and compared to the effects of erythromycin using liver microsomes from control and dexamethasone pretreated rats and human liver microsomes. Both anhydroerythromycin and erythromycin were found to be demethylated, thus both fulfil the prerequisites for possible metabolite-cytochrome P450 complex information. The formation of a metabolite-cytochrome P450 complex was demonstrated for anhydroerythromycin by preincubating NADPH fortified microsomes with anhydroerythromycin. This complex formation could be reversed by incubating the microsomes in 50 microM potassium ferricyanide. Anhydroerythromycin was a more potent inhibitor of androst-4-ene-3,17-dione (androstenedione) 6 beta-hydroxylation than erythromycin. Kinetic analysis shows that there are probably two cytochromes P450 involved in androstenedione 6 beta-hydroxylation in control rat microsomes both of which are inhibited by anhydroerythromycin. There are at least two forms of cytochrome P450 responsible for androstenedione 6 beta-hydroxylation in microsomes from dexamethasone pretreated rats but only the high affinity form is inhibited by anhydroerythromycin. "Atypical" kinetics were observed in human microsomes but inhibition of androstenedione 6 beta-hydroxylation was observed with 5 microM anhydroerythromycin at all androstenedione concentrations used. Inconsistencies have been observed in the literature with respect to clinical interactions observed with erythromycin. Since anhydroerythromycin appears to be a more potent inhibitor of androstenedione 6 beta-hydroxylation than erythromycin, we speculate that the variable blood levels of anhydroerythromycin found after dosing with erythromycin may explain these discrepancies.

Animals↗
PubMed1995

Loratadine administered concomitantly with erythromycin: pharmacokinetic and electrocardiographic evaluations.

OBJECTIVE: To evaluate the effects of coadministration of loratadine and erythromycin on the pharmacokinetics and electrocardiographic repolarization (QTc) pharmacodynamics of loratadine and its metabolite descarboethoxyloratadine in healthy volunteers. METHODS: Twenty-four healthy volunteers were studied in a prospective, double-blind crossover design while confined in a Clinical Research Center. The primary pharmacodynamic end point of the study was the difference between baseline and day 10 mean QTc intervals obtained from surface electrocardiograms. Plasma concentrations of loratadine, descarboethoxyloratadine, and erythromycin were measured on treatment day 10 for pharmacokinetic analysis. Subjects received in random sequence the following three treatments for 10 consecutive days during three separate study periods: 10 mg loratadine every morning plus 500 mg erythromycin stearate every 8 hours, or 10 mg loratadine every morning plus placebo every 8 hours, or placebo every morning plus 500 mg erythromycin stearate. RESULTS: Concomitant administration of loratadine and erythromycin was associated with increased plasma concentrations of loratadine (40% increase in area under the plasma concentration-time curve [AUC]) and descarboethoxyloratadine (46% increase in AUC) compared with loratadine alone. Analysis of variance showed no difference between the treatment groups in effect on QTc intervals compared with baseline, and no significant change from baseline was observed. No clinically relevant changes in the safety profile of loratadine were observed, and there were no reports of sedation nor syncope. CONCLUSION: Although concomitant administration of loratadine and erythromycin was associated with increased plasma concentrations of loratadine and descarboethoxyloratadine, no clinically relevant changes in the safety profile of loratadine were observed. In this study, 10 mg loratadine administered orally for 10 consecutive days was well tolerated when coadministered with therapeutic doses of erythromycin stearate.

Adult↗
PubMed1992

Erythromycin accelerates gastric emptying by inducing antral contractions and improved gastroduodenal coordination.

Erythromycin has been shown to act as a motilin agonist by binding to motilin receptors on gastrointestinal smooth muscle and to improve the severely impaired gastric emptying in patients with diabetic gastroparesis. To elucidate the motor pattern that accounts for this accelerated emptying, the effect of 200 mg erythromycin vs. placebo on postprandial motility of the stomach and the upper small intestine was examined in 13 normal subjects. Erythromycin significantly increased the amplitude of the antral contractions during the 2-hour postprandial study period (maximal difference in mean amplitude of distal antral contractions between erythromycin and placebo recorded from 80 to 90 minutes after meal: 123 +/- 17 vs. 44 +/- 12 mm Hg; P less than 0.005). The total number of antral contractions was not affected, but the contractions could be recorded manometrically higher up in the stomach after erythromycin than after placebo (9-12 vs. 3-6 cm above the pylorus). Antroduodenal coordination was significantly improved during the first postprandial hour, and the first normal phase 3 of the migrating motor complex, indicating the reappearance of fasting motility, occurred earlier after erythromycin than after placebo (128.3 +/- 14.3 vs. 173.4 +/- 16.1 minutes; P less than 0.05). These changes in postprandial motility induced by erythromycin may well account for its accelerating effect on gastric emptying.

Adult↗
PubMed1992

Effect of erythromycin on gastric motility in controls and in diabetic gastroparesis.

The effect of three doses of erythromycin on interdigestive gastrointestinal motility and on plasma motilin levels was studied in healthy volunteers and patients with diabetic gastroparesis. Abnormalities of interdigestive motility were observed in 40% of the patients. In healthy volunteers, 40 mg erythromycin elicited a premature phase 3 that started in the stomach. In contrast to the spontaneous gastric phase 3, this erythromycin-induced phase 3 was not accompanied by a motilin peak. In patients with diabetic gastroparesis, 40 mg erythromycin induced a premature phase 3 in three patients, no response in one patient, and a burst of antral contractions in another patient. Doses of 200 and 350 mg erythromycin elicited a burst of antral phase-3-like contractions in both volunteers and patients, which was not accompanied by a motilin peak. This phase-3-like activity did not migrate to the small intestine and was not followed by a phase 1, but by a prolonged period of antral contractile activity. The number and amplitude of antral contractions after 200 or 350 mg erythromycin were significantly higher than after 40 mg. The motor patterns induced by different doses of erythromycin offer potential therapeutic applications.

Adult↗
PubMed1989

Involvement of a Spiroplasma citri plasmid in the erythromycin-resistance transfer.

An erythromycin-resistant strain (M4 Er-1) was selected from Spiroplasma citri M4+. The transfer by transformation of the erythromycin-resistance character to the erythromycin-sensitive S. citri strain R8A2+ was studied. Transfer became effective and reproducible when cells were treated with alkali cations plus polyethylene glycol. Comparison of the efficiency of transformation of the erythromycin-sensitive strain S. citri R8A2+ by total and extrachromosomal DNA purified from the erythromycin-resistant strain M4 Er-1 showed that the plasmid pM42 was able to transfer the erythromycin-resistance. pM42 was mapped with restriction endonucleases and found to be related to the pMH1 plasmid previously isolated from S. citri MH. Hybridization analysis of DNA from sensitive and resistant strains has shown that a sequence from pM42, analogous to a sequence from pMH1, was integrated at a specific locus in the chromosome of the erythromycin-resistant cells, i.e., of the transformed R8A2 cells and of the spontaneous mutant M4 Er-1 strain.

DNA↗