caa a22 4500 47705787X CHVBK 20180405111351.0 cr unu---uuuuu 170330e19960301xx s 000 0 eng 10.1007/BF00195933 doi (NATIONALLICENCE)springer-10.1007/BF00195933 A pharmacokinetic and pharmacodynamic evaluation of buffered sublingual captopril in patients with congestive heart failure [Elektronische Daten] [J. McElnay, T. Al-Furaih, C. Hughes, M. Scott, D. Nicholls] 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. Springer-Verlag, 1996 Congestive heart failure nationallicence Captopril nationallicence sublingual nationallicence pharmacokinetic nationallicence pharmacodynamic nationallicence McElnay J. Pharmacy Practice Research Group, School of Pharmacy, The Queen's University of Belfast, 97 Lisburn Road, BT9 7BL, Belfast, N. Ireland, UK aut Al-Furaih T. Pharmacy Practice Research Group, School of Pharmacy, The Queen's University of Belfast, 97 Lisburn Road, BT9 7BL, Belfast, N. Ireland, UK aut Hughes C. Pharmacy Practice Research Group, School of Pharmacy, The Queen's University of Belfast, 97 Lisburn Road, BT9 7BL, Belfast, N. Ireland, UK aut Scott M. Pharmacy Practice Research Group, School of Pharmacy, The Queen's University of Belfast, 97 Lisburn Road, BT9 7BL, Belfast, N. Ireland, UK aut Nicholls D. The Royal Victoria Hospital, BT12 6BA, UK aut European Journal of Clinical Pharmacology Springer-Verlag 49/6(1996-03-01), 471-476 0031-6970 49:6<471 1996 49 228 https://doi.org/10.1007/BF00195933 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00195933 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- McElnay J. Pharmacy Practice Research Group, School of Pharmacy, The Queen's University of Belfast, 97 Lisburn Road, BT9 7BL, Belfast, N. Ireland, UK aut NATIONALLICENCE 700 1- Al-Furaih T. Pharmacy Practice Research Group, School of Pharmacy, The Queen's University of Belfast, 97 Lisburn Road, BT9 7BL, Belfast, N. Ireland, UK aut NATIONALLICENCE 700 1- Hughes C. Pharmacy Practice Research Group, School of Pharmacy, The Queen's University of Belfast, 97 Lisburn Road, BT9 7BL, Belfast, N. Ireland, UK aut NATIONALLICENCE 700 1- Scott M. Pharmacy Practice Research Group, School of Pharmacy, The Queen's University of Belfast, 97 Lisburn Road, BT9 7BL, Belfast, N. Ireland, UK aut NATIONALLICENCE 700 1- Nicholls D. The Royal Victoria Hospital, BT12 6BA, UK aut NATIONALLICENCE 773 0- European Journal of Clinical Pharmacology Springer-Verlag 49/6(1996-03-01), 471-476 0031-6970 49:6<471 1996 49 228 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer