By W. Lochner (auth.), Professor Dr. Wilhelm Lochner, Wolfgang Braasch, Günther Kroneberg (eds.)
The First Adalat Symposium held in Tokyo in 1973, offered very important experimental and medical effects which have been amassed in Europe and Japan with the hot coronary healing agent. the eu scientists had a chance to debate the issues and effects in my view with their eastern colleagues. the second one Adalat Symposium used to be held in Amsterdam inside a yr with the aim of bringing jointly in most cases scientists inside Europe. the consequences mentioned in Tokyo were prolonged and supplemented via extra stories. Contributions in easy technology are awarded, yet most crucial are these medical stories, which aid and expand facts of the drug's efficacy in people. The editors desire to exhibit their appreciation to all these accountable for contributing to this record and, particularly, to Dr. M. SPENGLER, Dr. F. EBNER and Dr. ok. BRANDAU for his or her editorial support, and to Dr. W. BOTTGER for the training of the topic Index. we are hoping that this ebook may be a precious contribution towards conveying info to physicians and scientists. DiisseldorfjWuppertal, Autumn 1975 W. LOCHNER' W BRAASCH' G. KRONEBERG Contents creation: W. LOCHNER current foundation of Coronary treatment: W. LOCHNER. With eleven Figures 2 consultation I. Chemistry and Experimental Pharmacology (Chairmen: A. FLECKENSTEIN and okay. LANDMARK) Pharmacology of Nifedipine: G. KRONEBERG. With eight Figures 12 dialogue comments 19 The Chemistry of Nifedipine: F. BOSSERT. With nine Figures 20 Pharmacokinetics of Adalat in Animal Experiments: okay. PATZSCHKE, B.
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Additional resources for 2nd International Adalat® Symposium: New Therapy of Ischemic Heart Disease
Both the metabolites isolated from urine and the synthetic product were investigated in dogs. The dose required for an increase of oxygen in the coronary sinus blood of the dogs by 30 saturationpercent (ED) was measured . After intravenous administration the efficacy of the "free acid" and the lactone is WOO-fold weaker, as compared to nifedipine (Table 2). It is of interest that oxidation of nifedipine to the respective pyridine-derivative leads to a remarkable diminution of the pharmacologic potency (Table 2, substance BAY b 4759).
They have, however, the general disadvantage that satisfactory coronary dilation is achieved only by parenteral administration. Our own research target was therefore clear. In addition to improving the coronary activity, we had to develop a compound that could be taken orally in order to make reasonable prophylactic therapy possible. mo~ ~R' R500CCH2-oTO~Rl R4 1 Fig. 1 We first tackled this problem by varying the heteroatom in the six-membered heterocyclic ring. By this means a favorable change in the metabolization of the compounds could follow.
Oo )( ~I -so )( )C )C )C )( )( )( a, s, is. , ............. -a m ¢ Velocity of isometric tension development(dk/dt) Fig. 8. Isolated papillary muscle of guinea pig heart (electrically stimulated) (here to about 100%) (upper curve), but the contractile force of the heart, expressed as dp/dt, was not inhibited, as could be expected from the high inhibitory action in the isolated heart muscle preparation. Instead of a decrease, a certain increase of dp/dt was established, as can be seen from the lower curve.
2nd International Adalat® Symposium: New Therapy of Ischemic Heart Disease by W. Lochner (auth.), Professor Dr. Wilhelm Lochner, Wolfgang Braasch, Günther Kroneberg (eds.)