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An Acute Dose‐Response Pharmacodynamic Evaluation of Orally Administered Isradipine (PN‐200‐110) in Hypertensive Patients
Author(s) -
McMahon F. Gilbert,
Vargas Ramon,
Ryan Jerome R.,
Miller Howard,
Faraday Susan
Publication year - 1988
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1988.tb03195.x
Subject(s) - isradipine , supine position , medicine , placebo , blood pressure , anesthesia , pharmacodynamics , dosing , washout , dihydropyridine , pharmacokinetics , pharmacology , calcium , alternative medicine , pathology
This study was conducted to assess acute oral dose‐responses of four dose levels (2.5,5,10, 20 mg) of isradipine, a new calcium channel blocking agent of the 1,4‐dihydropyridine group. Sixteen patients with mild essential hypertension were investigated using a randomized, four‐way cross‐over, double‐blind, placebo‐controlled design. After a 2‐week washout period, all patients were admitted to a research unit where they entered a 3‐day placebo equilibration, followed by 9 days of double‐blind single doses of isradipine. Drug administration was randomized, and baseline blood pressure values obtained preceding active medication doses were fairly constant. Dose‐related reductions in supine and in standing blood pressures were obtained. The mean peak supine blood pressure decrements to doses of 2.5, 5, 10, and 20 mg were 17/16, 25/19, 35/22, and 37/25 mm Hg, respectively. Pulse rates increased slightly. Similar responses were obtained with patients in the erect position. Peak hypotensive responses occurred within 3 hours after dosing. The duration of effect persisted as long as 21 hours, particularly after the 10‐ and 20‐mg doses (15/9 and 17/12 mm Hg mean supine blood pressure decrements, respectively).