MODULE 2 | CNS STIMULANTS Flashcards
two groups of drugs that act primarily to stimulate the CNS
psychomotor stimulants
hallucinogens
cause excitement and euphoria, decrease feelings of fatigue, and increase motor activity
PSYCHOMOTOR STIMULANTS
produce profound changes in thought patterns and mood, with little effect on the brainstem and spinal cord
HALLUCINOGENS
PSYCHOMOTOR STIMULANTS
- inhibition of phosphodiesterase thus increase cAMP
- increase Ca permeability
- blockade of the adenosine receptors - this leads to inhibition of the hyperpolarizing effect of K in the cardiac cells
METHYLXANTHINES
caffeine
PSYCHOMOTOR STIMULANTS | METHYLXANTHINES
inhibition of the enzyme that metabolizes cAMP thus increasing cAMP levels
phosphodiesterase
PSYCHOMOTOR STIMULANTS | METHYLXANTHINES
increase ____ pemeability
Ca
PSYCHOMOTOR STIMULANTS | METHYLXANTHINES
blockade of the ____ receptors – leads to inhibition of the hyperpolarizing effect of K in cardiac cells
adenosine receptors
PSYCHOMOTOR STIMULANTS
- decrease fatigue and increase mental awareness, anxiety, tremors
- has a positive ionotropic and chronotropic effects on the heart
- can induce diuresis
- stimulate secretions of HCL from the gastric mucosa
METHYLXANTHINE
rate of contraction of the ❤️
chronotropic
PSYCHOMOTOR STIMULANTS | METHYLXANTHINES
included in some OTC analgesic preparations, particulary in headache remedies
caffeine
PSYCHOMOTOR STIMULANTS | METHYLXANTHINES
for bronchial asthma – bronchodilator
theophylline
PSYCHOMOTOR STIMULANTS | METHYLXANTHINES | ADVERSE EFFECTS
insomnia, anxiety, agitation
moderate doses
PSYCHOMOTOR STIMULANTS | METHYLXANTHINES | ADVERSE EFFECTS
emesis and convulsion
high doses
PSYCHOMOTOR STIMULANTS
stimulate the CNS by:
* stimulation of catecholamine release
* blocking the reuptake of monoamines
* inhibition of MAO enzymes
all of these mechanisms lead to increase catecholamine concentration exhibiting central and peripheral actions
AMPHETAMINES
PSYCHOMOTOR STIMULANTS | AMPHETAMINES
stimulate motor and physical activity, increase alertness and decrease fatigue
central actions
PSYCHOMOTOR STIMULANTS | AMPHETAMINES
decrease appetite, increase BP, increase heart rate
peripheral actions
common drug for ADHD
AMPHETAMINE
PSYCHOMOTOR STIMULANTS
- used to treat narcolepsy and also used clinically to alleviate behavioral problems and reduce hyperkinesias in children with ADHD
- has high potential for addiction – classified as prohibited drug
AMPHETAMINE
PSYCHOMOTOR STIMULANTS
AE:
* insomnia
* irritability
* weakness
* dizziness
* tremor
* hyperactive reflexes
AMPHETAMINE
PSYCHOMOTOR STIMULANTS | AMPHETAMINES
chronic use may lead to ____
amphetamine psychososis
PSYCHOMOTOR STIMULANTS
- potentiates and prolong CNS and peripheral actions of catecholamines by stimulating their release
- due to intense euphoria produceed by this, this is used as a recreational drug and is highly abused
- clinically, it is used to increase mood and psychomotor activities during the first few weeks of treatment of severely depressed patients
- it is also used as local anesthetic in ENT surgery due to its ability to cause vasoconstrictions
COCAINE
PSYCHOMOTOR STIMULANTS | COCAINE
used as ____ in ENT surgery
local anesthetic
PSYCHOMOTOR STIMULANTS | COCAINE
ester
esa i
PSYCHOMOTOR STIMULANTS | COCAINE
amide
two i
PSYCHOMOTOR STIMULANTS | COCAINE
xylocaine
amide
brand name of lidocaine
psychomotor stimulants can cause ____
vasodilation
psychomotor stimulant that can cause vasoconstriction
COCAINE
PSYCHOMOTOR STIMULANTS
- widely abused drug
- low dose: causes arousal & relaxation
- high dose: respiratory paralysis
- not currently used therapeutically except in smoking cessation
- can increase rate of metabolism of a number of drugs so can cause potential interactions
NICOTINE
PSYCHOMOTOR STIMULANTS | NICOTINE
low dose
arousal & relaxation
PSYCHOMOTOR STIMULANTS | NICOTINE
high dose
respiratory paralysis
Psychmimetic stimulants are also called ____ and are seldom used clinically due to their high abuse potential
HALLUCINOGENS
also called hallucinogens
psychomimetic stimulants
PSYCHOMIMETIC STIMULANTS
- inhibits reuptake of DA, SE, NE
- has anticholinergic activity, but produces hypersalivation
- an analog ok KETAMINE that porduces “dissociative anesthesia” (insensitivty to pain without loss of consciousness) and analgesia
- withdrawn from its use as dissociative anesthetic because of its hallucinogenic property and is now replaced by ketamine
PHENCYCLIDINE (PCP) - ANGEL DUST
PSYCHOMIMETIC STIMULANTS | PHENCYCLIDINE
inhibits reuptake of ____, ____, ____
DA
SE
NE
PSYCHOMIMETIC STIMULANTS | PHENCYCLIDINE
has ____ activity
anticholinergic
PSYCHOMIMETIC STIMULANTS | PHENCYCLIDINE
produces ____
hypersalivation
PSYCHOMIMETIC STIMULANTS | PHENCYCLIDINE
an analog of ____ that produces dissociative anesthesia
KETAMINE
PSYCHOMIMETIC STIMULANTS | PHENCYCLIDINE
has been replaced by
KETAMINE
insensitivity to pain without the loss of consciousness
dissociative anesthesi
PSYCHOMIMETIC STIMULANTS
- interacts with several 5HT receptor subtypes in the brain
- agonist of SE
- low dose: hallucinations with brilliant colors and mood alteration
- high dose: long-lasting psychotic changes
LYSERGIC ACID DIETHYLAMIDE (LSD)
PSYCHOMIMETIC STIMULANTS | LYSERGIC ACID DIETHYLAMIDE
agonist of
SE
PSYCHOMIMETIC STIMULANTS | LYSERGIC ACID DIETHYLAMIDE
LOW DOSE
hallucinations w brilliant colors & mood alteration
PSYCHOMIMETIC STIMULANTS | LYSERGIC ACID DIETHYLAMIDE
high dose
long lasting psychotic changes
PSYCHOMIMETIC STIMULANTS
- main alkaloid in marijuana
- retrograde activity (reverse)
- produces euphoria followed by drowsiness and relaxation
- impairs short term memory and mental activity
- increases appetite, causes xerostomia (dry mouth), visual hallucinations, delusions, and enhancement of sensory activity
- MOA is unkown
TETRAHYDROCANNABINOL (THC)
PSYCHOMIMETIC STIMULANTS | TETRAHYDROCANNABINOL
main alkaloid in
marijuana
PSYCHOMIMETIC STIMULANTS | TETRAHYDROCANNABINOL
produces ____ followed by drowsiness & relaxation
euphoria
