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dc.contributor.authorLesko, Lawrence J.
dc.contributor.authorBenotti, Joseph R.
dc.contributor.authorAlpert, Joseph S.
dc.contributor.authorBrady, Priscilla M.
dc.contributor.authorMcCue, Jane E.
dc.contributor.authorWeiner, Bonnie H.
dc.contributor.authorOckene, Ira S.
dc.date2022-08-11T08:08:02.000
dc.date.accessioned2022-08-23T15:40:19Z
dc.date.available2022-08-23T15:40:19Z
dc.date.issued1986-10-01
dc.date.submitted2008-04-11
dc.identifier.citationJ Pharm Sci. 1986 Oct;75(10):952-4.
dc.identifier.issn0022-3549 (Print)
dc.identifier.pmid3491897
dc.identifier.urihttp://hdl.handle.net/20.500.14038/26373
dc.description.abstractThe pharmacokinetics of intravenous bepridil (1-[2-(N-benzylanilino)-1-(isobutoxymethyl)ethyl]pyrrolidine ) were studied in 16 patients undergoing cardiac catheterization for evaluation of coronary disease, all with normal base-line hemodynamic and renal functions. Ten patients received 3 mg/kg and six patients received 4 mg/kg of bepridil infused over a period of 30 min. Plasma bepridil concentrations were measured by HPLC and analyzed by model-dependent and model-independent methods. The mean (+/- SD) maximum plasma bepridil concentrations at the end of the infusion were 2047 +/- 820 ng/mL (3 mg/kg) and 2478 +/- 1426 ng/mL (4 mg/kg). Postinfusion bepridil concentrations were best described by a two-compartment open model. The model-dependent harmonic mean distribution and elimination half-lives were 1.7 h (range: 1.1-2.2 h) and 19.7 h (range: 8.0-61.9 h), respectively. The harmonic mean elimination half-life from model-independent analysis was 14.9 h (range: 7.4-64.0 h). The arithmetic means of other model-independent kinetic parameters were systemic clearance, 0.524 +/- 0.215 L X kg-1 X h-1; Vd, 15.3 +/- 10.9 L/kg; and Vdss, 10.1 +/- 6.0 L/kg. Model-dependent and model-independent estimates of half-life and clearance agreed reasonably well. Bepridil was well tolerated, effecting little or no change in central hemodynamics or EKG intervals. The extensive distribution and relatively slow clearance of bepridil account for its long elimination half-life. Intravenous bepridil appears to be a safe calcium (II) antagonist that is suitable for once-a-day dosing.
dc.language.isoen_US
dc.relation<a href="http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3491897&dopt=Abstract ">Link to article in PubMed</a>
dc.relation.urlhttp://dx.doi.org/10.1002/jps.2600751008
dc.subjectAged
dc.subjectBepridil
dc.subjectCalcium Channel Blockers
dc.subjectCoronary Disease
dc.subjectFemale
dc.subjectHumans
dc.subjectInjections, Intravenous
dc.subjectKinetics
dc.subjectMale
dc.subjectMiddle Aged
dc.subjectModels, Biological
dc.subjectPyrrolidines
dc.subjectCardiology
dc.subjectCardiovascular Diseases
dc.titlePharmacokinetics of intravenous bepridil in patients with coronary disease
dc.typeJournal Article
dc.source.journaltitleJournal of pharmaceutical sciences
dc.source.volume75
dc.source.issue10
dc.identifier.legacycoverpagehttps://escholarship.umassmed.edu/cardio_pp/58
dc.identifier.contextkey488240
html.description.abstract<p>The pharmacokinetics of intravenous bepridil (1-[2-(N-benzylanilino)-1-(isobutoxymethyl)ethyl]pyrrolidine ) were studied in 16 patients undergoing cardiac catheterization for evaluation of coronary disease, all with normal base-line hemodynamic and renal functions. Ten patients received 3 mg/kg and six patients received 4 mg/kg of bepridil infused over a period of 30 min. Plasma bepridil concentrations were measured by HPLC and analyzed by model-dependent and model-independent methods. The mean (+/- SD) maximum plasma bepridil concentrations at the end of the infusion were 2047 +/- 820 ng/mL (3 mg/kg) and 2478 +/- 1426 ng/mL (4 mg/kg). Postinfusion bepridil concentrations were best described by a two-compartment open model. The model-dependent harmonic mean distribution and elimination half-lives were 1.7 h (range: 1.1-2.2 h) and 19.7 h (range: 8.0-61.9 h), respectively. The harmonic mean elimination half-life from model-independent analysis was 14.9 h (range: 7.4-64.0 h). The arithmetic means of other model-independent kinetic parameters were systemic clearance, 0.524 +/- 0.215 L X kg-1 X h-1; Vd, 15.3 +/- 10.9 L/kg; and Vdss, 10.1 +/- 6.0 L/kg. Model-dependent and model-independent estimates of half-life and clearance agreed reasonably well. Bepridil was well tolerated, effecting little or no change in central hemodynamics or EKG intervals. The extensive distribution and relatively slow clearance of bepridil account for its long elimination half-life. Intravenous bepridil appears to be a safe calcium (II) antagonist that is suitable for once-a-day dosing.</p>
dc.identifier.submissionpathcardio_pp/58
dc.contributor.departmentDepartment of Medicine, Division of Cardiovascular Medicine
dc.source.pages952-4


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