Serum Protein Binding of Erythromycincand Erythromycin 2'-Propionate Ester

Wiegand, Ronald G.; Chun, Alexander

doi:10.1002/jps.2600610322

Cited by 36 publications

(8 citation statements)

References 9 publications

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“…Therefore, the in vivo activity must not be considered in terms of that found in in vitro (Tardrew, Mao and Kenny, 1969). The kinetic constants obtained are similar to those demonstrated in earlier studies (Stephens et al, 1969;Wiegand, 1972;Griffith, 1958).…”

Section: Discussionsupporting

confidence: 89%

Plasma and salivary concentrations of erythromycin after administration of three different formulations

Henry¹,

Turner²,

Garland³

et al. 1980

Postgraduate Medical Journal

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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.

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Section: Discussionsupporting

confidence: 89%

Plasma and salivary concentrations of erythromycin after administration of three different formulations

Henry¹,

Turner²,

Garland³

et al. 1980

Postgraduate Medical Journal

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“…Plasma protein binding of erythromycin is high and is in the range where its effects are important (Gordon, Regamey & Kirby, 1973;Wiegand & Chun, 1972).…”

Section: Discussionmentioning

confidence: 99%

“…Reasons for this apparent nonlinear behaviour were not investigated but may be related to changes in plasma protein binding over the concentration range encountered. Plasma protein binding of erythromycin is high and is in the range where its effects are important (Gordon, Regamey & Kirby, 1973;Wiegand & Chun, 1972).…”

Section: Discussionmentioning

confidence: 99%

Intersubject and dose‐related variability after intravenous administration of erythromycin.

Austin¹,

Mather²,

Philpot³

et al. 1980

Brit J Clinical Pharma

109

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1 It is well‐known that considerable variability and unpredictability in serum concentrations results from orally administered erythromycin. 2 Disposition kinetics and their variability were studies in 24 healthy subjects after a single dose of erythromycin lactobionate and four doses were studied to evaluate dose‐related variability in five other subjects. 3 Erythromycin kinetics were adequately described by a classical two compartment open model with little intersubject variability. 4 Dose‐related variability occurred. Clearance was independent of dose but T1/2 beta and Vdss increased with dose. 5 Data are presented to show that non‐invasive sampling of urine and saliva are of limited value in studying erythromycin pharmacokinetics.

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“…Erythromycin has been recovered in fecal samples 3.5 days after a dose (11). Presumably, this erythromycin was slowly released from tissues where it is thought to bind (17) and was then excreted from the central compartment. Enterohepatic recycling (6) may also have contributed to the presence of erythromycin in the fecal samples.…”

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics of single-dose erythromycin in normal and alcoholic liver disease subjects

Kroboth¹,

Brown²,

Lyon³

et al. 1982

Antimicrob Agents Chemother

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Six normal males and eight male subjects with alcoholic liver disease (ALD) and ascites were given a single 500-mg dose of erythromycin base. Twelve serum samples were collected at 0, 1, 2, 3, 4, 6, 8, 10, 12, 14, 16, and 24 h after dosing and assayed microbiologically for erythromycin concentration. Absorption was characterized by a zero-order model for both groups. ALD subjects demonstrated a shorter lag time (2.0 versus 3.0 h), an earlier peak (4.6 versus 6.3 h, P less than 0.05), and higher peak concentrations (2.04 versus 1.50 micrograms/ml) than normal subjects. Previously unreported biphasic elimination kinetics after oral dosing were observed in five and four ALD subjects. In the ALD group, the mean half lives for the first (alpha) and terminal (beta) phases were 1.6 and 4.5 h, respectively, and in normal subjects, were 1.3 and 6.6 h. The difference in alpha between groups was significant, P less than 0.05. The clinical significance of this finding for ALD patients receiving prolonged courses of erythromycin is discussed.

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Serum Protein Binding of Erythromycincand Erythromycin 2'-Propionate Ester

Cited by 36 publications

References 9 publications

Plasma and salivary concentrations of erythromycin after administration of three different formulations

Plasma and salivary concentrations of erythromycin after administration of three different formulations

Intersubject and dose‐related variability after intravenous administration of erythromycin.

Pharmacokinetics of single-dose erythromycin in normal and alcoholic liver disease subjects

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