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中枢兴奋药 Central Stimulants 北京协和医学院基础医学院药理学系 叶菜英. Central Stimulants Definition: Drugs that can stimulate the central nervous system. Classification: Cerebral.

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Presentation on theme: "中枢兴奋药 Central Stimulants 北京协和医学院基础医学院药理学系 叶菜英. Central Stimulants Definition: Drugs that can stimulate the central nervous system. Classification: Cerebral."— Presentation transcript:

1 中枢兴奋药 Central Stimulants 北京协和医学院基础医学院药理学系 叶菜英

2 Central Stimulants Definition: Drugs that 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

3 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.

4 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 ).

5 Caffeine 【 Adverse effect 】 Rare. Stimulation, discomfortable, insomnia Overdose→tachycardia Toxis→muscle tremor

6 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 CO 2 intoxication. Adverse effect : increase in the heart rate , overdose→convulsion

7 Nikethamide( 尼可刹米 ) ( Coramine 可拉明 ) 【 Pharmacologic properties 】 Increase the stimulation of CNS, especially stimulate medulla oblongata respiratory center, carotid body and aortic chemoreceptor, and then, stimulate respiratory center reflectivity, increase the CO 2 sensitivity of CNS, accelerating and deepening breathing, improving respiratory function. The stimulate effect of cerebral cortex vasomotor center and spinal cord is weak. Take effect rapidly, hold time is short , a single intravenous bolus can maintain 5 to 10 minutes.

8 Nikethamide ( Coramine ) Clinical application: various kinds of central respiratory depression (neonatal asphyxia, CO 2 intoxication , drug intoxication). Adverse effects are rare. Overdose→BP↑ , tachycardia, amyostasia and rigor, cough, vomiting, perspiration. Toxis→convulsion.

9 Central Stimulants 【 Clinical application 】 Application conditions of Respiratory Stimulants: trachea is smooth, and respiratory muscle is normal ( no obviously sputamentum retention and bronchospasm ). Combination measures: etiological treatment inhaling O 2, artificial respiration. The holding time of central stimulants is short, so it should be used again and again. Prevent convulsion ( Overdose→ convulsion ): several kinds of drug can be used taking turns, control doses strictly→→→

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