R. Haerlin

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Urapidil is a selective alpha 1-adrenoceptor antagonist with central antihypertensive action which is increasingly used in the treatment of hypertension. Urapidil is readily absorbed, is subject to moderate first-pass metabolism and is eliminated primarily as metabolites of much lower antihypertensive activity than the parent drug. The influences of age,(More)
The study was designed to follow the haemodynamic effects and pharmacokinetics under steady-state conditions of three different doses of urapidil infused continuously. Nine male hypertensive patients received three randomly assigned intravenous infusions of 32.5, 65 and 130 mg urapidil, over 14 h during 6 consecutive days, in a change-over fashion. Blood(More)
The influence of food intake on the pharmacokinetics of a single dose (30 mg) of urapidil in a tablet and a sustained-release capsule form were examined in 12 healthy volunteers in a double crossover trial. Drug administration under fasting conditions requires that a standardized breakfast be eaten, 4 h after drug intake. Drug application with breakfast(More)
The pharmacokinetic parameters, including the relative bioavailabilities of two experimental batches of a 60-mg urapidil slow release-capsule and a 30-mg urapidil drinking ampoule (Ebrantil) had to be evaluated in a randomized, three-period change-over study with 12 healthy volunteers after single dosing. The appropriate parameters for the capsule(More)
In a multi-center, double-blind parallel-group study involving patients with essential hypertension (grade I/II), the antihypertensive effect and toleration of the postsynaptic alpha-1 receptor blocker, urapidil, was compared with that of the calcium antagonist, nifedipine. After a one-week wash-out, and one week period on placebo, the patients received(More)
The antihypertensive efficacy of urapidil, a postsynaptic alpha blocker with an additional central action, was compared with that of the angiotensin I converting enzyme inhibitor captopril under conditions of general practice (multicenter study). The study was performed in a double-blind, randomized, parallel-group fashion. After a 2-week washout and(More)
The effect produced by an inhibitor on an enzyme is characterized by the underlying mechanism and the molar inhibition coefficients Ki and Ki', respectively. The commonly used graphical estimation methods according to Lineweaver-Burk, Dixon and Cornish-Bowden do not always yield a differentiation between various possible mechanisms. According to our(More)