| A pharmacokinetic and pharmacodynamic evaluation of buffered sublingual captopril in patients with congestive heart failure. | |
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MedLine Citation:
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PMID: 8706772 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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OBJECTIVE: The pharmacokinetics and pharmacodynamics of buffered sublingual captopril were assessed in patients with congestive heart failure (CHF). METHODS: The study was carried out in a randomised single-blind cross-over fashion (n = 6, 4 males and 2 females) and involved two study days, at least 7 days apart. Baseline measurements were carried out for plasma renin activity (PRA), blood pressure (B.P.) and heart rate (H.R.). Captopril (12.5 mg) was administered sublingually with dibasic potassium phosphate which maintained salivary pH at 7, or perorally with 100 ml of water. Further B.P., H.R. measurements and venous blood samples were taken over a 3 hour period post-drug administration. Blood samples were analysed for captopril and PRA levels. RESULTS: tmax after buffered sublingual administration of captopril, which ranged from 40-60 min (median = 40 min), was significantly shorter than after peroral administration (range 60-120 min, median = 90 min). Cmax was slightly greater after buffered sublingual than after peroral administration with mean values of 108.2 vs. 94.0 ng.ml-1. AUC values were similar after both routes of administration. Systolic and diastolic B.P. vs. time profiles for each administration method were significantly different i.e. sublingual administration produced an earlier reduction in B.P., however, HR did not differ significantly between the two routes. CONCLUSION: The data indicate that this novel administration method of captopril leads to an increased rate, but an unchanged extent of captopril absorption, suggesting a modest therapeutic advantage with the use of buffered sublingual captopril if a rapid reduction in blood pressure is required. |
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Authors:
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J C McElnay; T A al-Furaih; C M Hughes; M G Scott; D P Nicholls |
Publication Detail:
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Type: Clinical Trial; Journal Article; Randomized Controlled Trial |
Journal Detail:
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Title: European journal of clinical pharmacology Volume: 49 ISSN: 0031-6970 ISO Abbreviation: Eur. J. Clin. Pharmacol. Publication Date: 1996 |
Date Detail:
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Created Date: 1996-09-09 Completed Date: 1996-09-09 Revised Date: 2010-03-24 |
Medline Journal Info:
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Nlm Unique ID: 1256165 Medline TA: Eur J Clin Pharmacol Country: GERMANY |
Other Details:
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Languages: eng Pagination: 471-6 Citation Subset: IM |
Affiliation:
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Pharmacy Practice Research Group, School of Pharmacy, Queen's University of Belfast, N. Ireland, UK. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Sublingual Aged Aged, 80 and over Analysis of Variance Angiotensin-Converting Enzyme Inhibitors / administration & dosage, pharmacokinetics, pharmacology, therapeutic use* Blood Pressure / drug effects Captopril / administration & dosage, pharmacokinetics, pharmacology, therapeutic use* Cross-Over Studies Female Heart Failure / drug therapy*, metabolism, physiopathology Heart Rate / drug effects Humans Male Middle Aged Phosphates / metabolism Potassium Compounds / metabolism Renin / blood Single-Blind Method |
| Chemical | |
Reg. No./Substance:
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0/Angiotensin-Converting Enzyme Inhibitors; 0/Phosphates; 0/Potassium Compounds; 16068-46-5/potassium phosphate; 62571-86-2/Captopril; EC 3.4.23.15/Renin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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