ABSTRACT
Propranolol is a well-known powerful betareceptor-blocking agent. Its quaternary dimethyl derivative, designated as pranolium was firstly prepared by Lucchesi. Compared to propranolol it possesses no betareceptor-blocking activity and no local anaesthetic properties but shows the same antiarrhythmic action as the starting material. The synthesis of pranolium and its optical isomers starting from the corresponding propranolol derivatives is described. Their pharmacological activities have been tested. No significant differences regarding the pharmacological action could be observed.
Subject(s)
Anti-Arrhythmia Agents/chemical synthesis , Propranolol/analogs & derivatives , Aconitine , Animals , Chemical Phenomena , Chemistry , Coronary Disease/chemically induced , Coronary Disease/prevention & control , Female , Glycogen/metabolism , Guinea Pigs , Heart/drug effects , In Vitro Techniques , Isomerism , Isoproterenol/pharmacology , Magnetic Resonance Spectroscopy , Male , Mass Spectrometry , Propranolol/analysis , Propranolol/chemical synthesis , Propranolol/pharmacology , Rats , Rats, Inbred Strains , Spectrophotometry, Infrared , Spectrophotometry, UltravioletABSTRACT
The useful development and application of controlled-release dosage forms is an important possibility to improve the pharmacotherapy of many diseases. However, according to the present social conditions of reproduction the introduction of a new drug has to be directed not only to a high therapeutic benefit but also to an increased social efficiency i.e., to an improvement of cost-benefit-relation. In the present study, therefore, the effect of using controlled-release dosage forms on the development of social efficiency is discussed. Basing on a comprehensive estimation of the therapeutic efficiency (therapeutic advantages and disadvantages) of controlled-release dosage forms the criteria of cost and benefit being of importance for a complex evaluation of efficiency are described.
