抗-癫-痫-药---中国医学科学院北京协和医学院-精品课程建设.pptVIP

中枢兴奋药 Central Stimulants Central Stimulants(中枢兴奋药) Definition: Drugs can stimulate the central nervous system. Classification: Cerebral cortex stimulation:Caffeine, Theophylline?… Cerebrum and brain stem stimulation: Nikethamide, Dimefline and Lobeline. Spinal cord stimulation: Strychnine Caffeine(咖啡因) 【Mechanism of Action】 Inhibit phosphodiesterase, decrease the degradation of cAMP→cAMP↑…… →physiological effect Central neuromodulator antagonist → effect of adenosine →block the inhibiting effect of adenosine on central nervous system→stimulate the central nervous system. Increasing intracellular free calcium Competitive antagonists of Benzodiazepine receptor, decrease the open frequency of Cl－channel→stimulate the central nervous system. Caffeine 【Pharmacologic properties and clinical application】 CNS：In small doses , it causes wakefulness, increases mental alertness, and decreases response times for simple motor task. Cardiovascular effects：Small doses →stimulate vagus nerve→heart rate↓ Large doses→increase the sensitivity of heart rate→arrhythmia Vasoconstriction effects: use with Ergotamine, brain arteriectasis→treatment of migraine, usually compatible with antipyretic analgesic→cold, headache, hypertension headache（APC、Somedon）. Caffeine 【Adverse effect】 Rare. Stimulation, discomfortable, insomnia Overdose→tachycardia Toxis→muscle tremor Lobeline (洛贝林 ) Pharmacologic properties: Stimulate carotid body and aortic chemoreceptor, stimulate respiratory center reflectivity. Large doses Lobeline can stimulate medulla oblongata respiratory center directly. Stimulate sympathetic nerve→increase in the heart rate, BP↑ Take effect rapidly, hold time is short (several minutes). Lobeline is often used to improve respiratory depression which induced by neonatal asphyxia and pedo-infectious diseases, it also can improve respiratory failure which induced by drug intoxication and CO2 intoxication. Adverse effect：increase in the heart rate，overdose→convulsion Nikethamid