Sedative-Hypnotic Drugs - 汕头大学医学院.ppt

Sedative-Hypnotic Drugs Department of Pharmacology Zhang Yanmei Normal sleep consists of distinct stages,based on three physiologic measures: the electroencephalogram, the electromyogram, and the electronystagmogram. Non-rapid eye movement(NREM) sleep: 70%-75% Stage 1,2 Stage 3,4:slow wave sleep, SWS Rapid eye movement(REM) sleep BASIC PHARMACOLOGY OF SEDATIVE-HYPNOTICS An effective sedative (anxiolytic) agent should reduce anxiety and exert a calming effect with little or no effect on motor or mental functions. A hypnotic drug should produce drowsiness and encourage the onset and maintenance of a state of sleep that as far as possible resembles the natural sleep state. BASIC PHARMACOLOGY OF SEDATIVE-HYPNOTICS Hypnotic effects involve more pronounced depression of the central nervous system than sedation, and this can be achieved with most sedative drugs simply by increasing the dose. Graded dose-dependent depression of central nervous system function is a characteristic of sedative-hypnotics. CHEMICAL CLASSIFICATION Benzodiazepines: not to lead general anesthesia, raraly death. Barbiturates: the older sedative-hypnotics, general depression of central nervous system. With such drugs, an increase in dose above that needed for hypnosis may lead to a state of general anesthesia. At still higher doses, it may depress respiratory and vasomotor centers in the medulla, leading to coma and death. Other classes of drugs: chloral hydrate, buspirone, et al. Ⅰ.Benzodiazepines The first benzodiazepine, chlordiazepoxide, was synthesised by accident in 1961. Ⅰ.Benzodiazepines Derivative of 1,4- benzodiazepines. About 20 are available for clinical use. They are basically similar in their pharmacological actions, though some degree of selectivity has been reported. It is possible that selectivity with respect to two types of benzodiazepine receptor may account for these differences. From a clinical point of view, difference in pharmacokinetic behaviour are more imp