CNS Stimulant

CNS STIMULANT
A.SABARIYA BANU
PHARM.D 2nd Year
CNS STIMULANT
• These are the drugs which increase the
muscular (motor) and the mental (sensory)
activities.
• Their effects vary from the increase in the
alertness and wakefulness (as with caffeine).
• To the production of convulsion (as with
strychnine) or death due to over stimulation.
MOA of CNS stimulant
A. Block neurotransmitters reuptake (Most reuptake
B. inhibitors affect either NE or 5-HT(Serotonin):
Cocaine
C. Promote neurotransmitters release:
Amphetamine
D. Block Metabolism MAO inhibitors (monoamine
oxidase):ex. Phenelzine
E. antagonize the effect of inhibitory
neurotransmitter: Picrotoxin & Strychnine
STRYCHΝΙΝΕ
• Strychnine was previously used as
• 1.Purgative
• 2.Appetite suppressant
• 3.Aphrodisiac
• 4.Constituent of nerve tonics.
• Today, this potent alkaloid is mainly used as a
rodenticide, and for killing stray dogs (Nux
vomica seeds are therefore sometimes referred
as "dog buttons")
Mechanism of Action
• Strychnine is a neurotoxin act as a antagonist
of glycine, which is a inhibitory
neurotransmitter.
• Strychnine competitively and reversibly inhibit
neurotransmitter glycine at postsynaptic
neuronal sites in the spinal cord.
ANALEPTICS (Respiratory stimulants)
• These are drugs which stimulate respiration and can have
resuscitative value in coma or fainting.They do stimulate
respiration in subconvulsive doses, but the patient may get
convulsions while still in coma.
• Mechanical support to respiration and other measures to
improve circulation are more effective and safe.
• The role of analeptics in therapeutics is very limited.
• Situations in which they may be employed are:As an expedient
measure in hypnotic drug poisoning until mechanical
ventilation is instituted.
• Suffocation on drowning, acute respiratory insufficiency.Apnoea
in premature infant.Failure to ventilate spontaneously after
general anesthesia.However, the overall utility of analeptics is
dubious.
Doxapram
• It acts by promoting excitation of central
neurones.
• At low doses it is more selective for the
respiratory centre than other analeptics.
• Respiration is stimulated through carotid and
aortic body chemoreceptors as well.
• Falling BP rises. Continuous i.v. infusion of
doxapram may abolish episodes of apnoea in
premature infant not responding to theophylline.
Mechanism of action
Doxapram stimulates chemoreceptor
in the carotid bodies of the carotid arteries
which in turn, stimulates the respiratory centre

in the brain stem.
USES
• A. Doxapramstimulate the respiratory rate in
patients with respiratory failure.
• B. It may be useful for treating respiratory

depression in patients who have taken
excessive doses of drugs such as buprenorphin
• C. also used for recovery after anesthesia

Psychomotor Stimulants
• Marked effect on mental functions &

Behavior:
• Produce Excitement, Euphoria
• Reduce Sensation of Fatigue
• Increase motor Activity
Amphetamines
• These are central sympathomimetics. Compared to
amphetamine, higher central: peripheral activity ratio is
exhibited by dextroamphetamine and
methamphetamine.
• They stimulate mental rather than motor activity;

convulsive doses are much higher. It is a potent CNS
stimulants that is used in treatment of ADHD, narcolepsy
and obesity DEXTROAMPHETAMINE is major member of
this compound. It is non catecholamine
MECHANISM OF ACTION
Amphetamines
Cocaine
• Caffeine Out of the three naturally occurring
methylxanthines, only caffeine is used as a CNS
stimulant.
• Cocaine increase, mental alertness & produce a feeling
of wellbeing & euphoria that is similar to that caused
by amphetamine like amphetamine cocaine can
produce hallucinations, delusion & paranoia cocaine
increases motor activity & at high doses causes
tremors, convulsion & followed by respiratory &
vesomotor depression.
• USES:
Cocaine has a local anesthetic action for the therapeutic
use of cocaine, cocaine is applied topically as a local
anesthetic for eye, ear & nose & throat surgery
Adverse effects
• Toxic effects of caffeine are extensions of its
pharmacological actions.
• Caffeine poisoning is rare, and it is less toxic than
theophylline.
• Gastric irritation, nausea and vomiting may occur as
side effects.
• Excitatory and motor effects such as nervousness,
insomnia, agitation, muscular twitching, rigidity, rise
in body temperature, delirium and convulsions are
produced at toxic doses.
USES
• 1) In analgesic mixture: caffeine benefits headache
probably by allaying fatigue and boredom. It has no
analgesic action of its own.
• 2) Migraine: Caffeine is used in combination with
ergotamine for treatment of migraine attack. It
appears to benefit by augmenting constriction of
cranial vessels and by enhancing absorption of
ergotamine from the g.i.t.
• 3) Apnoea in premature infants: as alternative to
theophylline
THANK YOU

CNS Stimulant

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CNS STIMULANT

in the carotid bodies of the carotid arteries

which in turn, stimulates the respiratory centre

• B. It may be useful for treating respiratory

• C. also used for recovery after anesthesia

• Marked effect on mental functions &

• They stimulate mental rather than motor activity;

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