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 nervou

s system.Classification: Cerebral cortex stimulation: Caffeine, Theo

phylline… Cerebrum and brain stem stimulation: Nike

thamide, Dimefline and Lobeline. Spinal cord stimulation: Strychnine

Caffeine( 咖啡因 )【 Mechanism of Action 】 Inhibit phosphodiesterase, decrease the degradat

ion of cAMP→cAMP↑…… →physiological effect Central neuromodulator antagonist → effect of ad

enosine →block the inhibiting effect of adenosine on central nervous system→stimulate the central nervous system.

Increasing intracellular free calcium Competitive antagonists of Benzodiazepine recep

tor, 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, increas

es 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, insom

nia Overdose→tachycardia Toxis→muscle tremor

Lobeline ( 洛贝林 ) 【 Pharmacologic properties 】 Stimulate carotid body and aortic chemoreceptor, stim

ulate respiratory center reflectivity. Large doses Lobeline can stimulate medulla oblongata

respiratory center directly. Stimulate sympathetic nerve→increase in the heart rat

e, BP↑ Take effect rapidly, hold time is short (several minutes). Lobeline is often used to improve respiratory depressio

n 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

Nikethamide( 尼可刹米 ) ( Coramine 可拉明 )

【 Pharmacologic properties 】 Increase the stimulation of CNS, especially stimulate med

ulla oblongata respiratory center, carotid body and aortic chemoreceptor, and then, stimulate respiratory center reflectivity, increase the CO2 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.

Nikethamide （ Coramine ） Clinical application: various kinds of cent

ral respiratory depression (neonatal asphyxia, CO2 intoxication ， drug intoxication).

Adverse effects are rare. Overdose→BP↑ ，tachycardia, amyostasia and rigor, cough, vomiting, perspiration. Toxis→convulsion.

Central Stimulants【 Clinical application 】 Application conditions of Respiratory Stimulant

s: trachea is smooth, and respiratory muscle is normal （ no obviously sputamentum retention and bronchospasm ） .

Combination measures: etiological treatment inhaling O2, 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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