Transcript 抗 癫 痫 药

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
nervous system.
stimulate
the
central
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，
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.
Nikethamide（Coramine）


Clinical application: various kinds of
central 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
Stimulants: 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→→→
Thanks!