CNS

STIMULANTS
Drugs that have a predominantly stimulant effect on the CNS may be broadly divide into :

• Respiratory stimulants: DOXAPRAM

NIKETHAMIDE

• Psychomotor stimulants: AMPHETAMINE

COCAINE
METHYLXANTHINES

• Convulsants: LEPTAZOL
STRYCHNINE
RESPIRATORY STIMULANTS
• Called as analeptics
• These drugs stimulate respiration and sometimes used to treat respiratory failures.
• Though may bring about temporary improvement in respiration, mortality is not reduced.
• Have low safety margin and may produce convulsions.

DOXAPRAM:
Appears to act mainly on the brainstem and spinal cord
Increases activity of respirator and vasomotor centers
ADVERSE EFFECTS: Nausea, cough, restlessness, hypertension, tachycardia, arrhythmias
and convulsions.

USES:

DOXAPRAM: occasionally used IV as an analeptic in acute respiratory failure.

Apnea in premature infants not responding to theophylline

NIKETHAMIDE: not used because risk of convulsions

PSYCHOMOTOR STIMULANTS: Amphetamine and dextroamphetamine are

sympathomimetic drugs
COCAINE: is CNS stimulants
produce euphoria
is drug abuse
local anesthetic

METHYLXANTHINES:
Caffeine, theophylline and theobromine are naturally xanthine alkaloids.
The beverages- coffee contains caffeine,
tea contains theophylline and caffeine
cocoa has caffeine and theobromine
caffeine and theophylline are CNS stimulants
Increase in mental alertness
Reduction in fatigue
Produce a sense of well being
Improve motor activity and performance with a clearer flow of thought

Caffeine stimulants the respiratory center.

Higher doses produce irritability, nervousness, restlessness, insomnia, excitement and
headache.

High doses can result in convulsions.

CVS
Methylxanthines: increases force of contraction of the myocardium
increases the heart rate
increases the cardiac output
but, they also produce peripheral vasodilatation which tends to decrease BP
(changes in BP and therefore is not consistent)

Caffeine causes vasoconstriction of cerebral blood vessels

KIDNEYS:
The xanthines have diuretic effect and thereby increases urine output.

SMOOTH MUSCLE: Xanthines cause relaxation of smooth muscle especially bronchial

smooth muscle.
SKELETEAL MUSCLE: Xanthines enhance the power of muscle contration
increase the capacity to do muscular work by both a
central stimulant effect and the peripheral actions.

GI TRACT: Xanthines increases the secretion of acid and pepsin in the smooth and gastric
irritants.

ADVERSE EFFECTS: nervousness, insomnia, tremors, tachycardia, hypotension, arrhythmias,

headache, gastritis, nausea, vomiting, epigastric pain and diuresis.
High dose produce convulsisons.
Tolerance develops after sometimes
Habituation to caffeine is common.
USES:
Headache: because of effect of caffeine on cerebral bold vessels
combined with ergotamine for the relief of migraine headache
caffeine is also combined with aspirin/paracetamol for the treatment of headache.

Bronchial asthma: Theophylline used in treatment of bronchial asthma

NOOTROPICS: drugs to improve memory and cognition(cognition enhancers)

PIRECETAM:
described as ‘nootropic agent’ thought to protect cerebral cortex from hypoxia and improve
learning and memory.
In
PIRACETAM:
described as ‘nootropic agent’ thought to protect cerebral cortex from hypoxia and improve
learning and memory.
In higher doses it also inhibits platelet aggregration

ADVERSE EFFECTS: insomnia, weight-gain, nervousness, depression, gastrointestinal

disturbances.

Has been tried in dementia, myoclonus, stroke and cerebrovascular accidents, alcoholism.
Behavioral disorders and learning problems in children and in vertigo.

Beneficial effects in all these is not proved.