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• W2098521826 abstract "OPC-18790, a nonglycosidic intropic agent, is now under clinical development for treatment of congestive heart failure. Two separate studies (one placebo-controlled) were conducted to evaluate its pharmacokinetics and pharmacodynamics after intravenous administration to a total of 36 healthy male subjects. The drug was administered both rapidly as a .05-, .1-, .2-, or .4-mg/kg intravenous dose, and as a 1-hour infusion of .5, 1.0, 2.5, 5.0,10.0, or 15.0 μg/kg/minute. Echocardiograms (ECHO) were evaluated before and immediately and 4 hours after the rapid administrations. Blood pressure (BP), heart rate (HR), and QTc in the electrocardiogram also were monitored in the rapid administration study. OPC-18790 was generally well tolerated by all subjects. Maximum peak plasma concentration and area under the curve increased linearly with dose in both studies. The t1/2, total body clearance of drug from plasma (CL), and the dose fraction excreted unchanged in the urine (fe) were comparable and dose-independent at the doses tested in both studies. The overall mean values of t1/2α, t1/2β, CL, and fe were .08 ± .01 hours, 3.64 ± .22 hours, .46 ± .01 L/kg, and 43.5 ± 1.0%, respectively. Echocardiograms showed that, immediately after rapid administration of up to .4 mg/kg, OPC-18790 increased left cardiac function dose-proportionally (P < .05 to .01): the ejection fraction by 21.1% and fractional shortening by 26.5% compared with the predose values, blood pressure, heart rate, and QTc did not differ between subjects given OPC-18790 and these receiving placebo. Intravenous OPC-18790 at the dose ranges used is considered to be safe and tolerable and exerts positive inotropic effects in a dose-proportional manner. This drug is potentially useful in the treatment of severe congestive heart failure." @default.
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• W2098521826 date "1994-02-01" @default.
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• W2098521826 title "Pharmacokinetics and Pharmacodynamics of Intravenous OPC-18790 in Humans: A Novel Nonglycosidic Inotropic Agent" @default.
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• W2098521826 doi "https://doi.org/10.1002/j.1552-4604.1994.tb03983.x" @default.
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