CNS Stimulants

Question 1

doxapram (Dopram, Stimulex, Respiram)

pentylenetetrazol

Answer 1

Analeptic & respiratory stimulant

MOA: bind carotid artery chemoreceptors–>signals to medullary respiratory centers–>increase tidal volume and respiratory rate
Decrease Cl- influx–>hyper polarization–>GABAa and glycine antagonists

Use: respiratory stimulant (postanesthetic)

Fast onset and short duration of action

Question 2

caffeine

theophylline

Answer 2

Methylxanthines

MOA: potent bronchodilator; mild CNS, respiratory, and cardiac stimulant
Antagonist of A1 receptor–>reduce adenosine activity–> inhibition of CNS suppresant

Caffeine: short acting
Use: apnea of prematurity

Theophylline: long-acting, found in tea
Use: asthma and COPD

Question 3

amphetamine (Adderal)
methamphetamine (Desoxyn)
dexamphetamine
methylphenidate (Ritalin)

Answer 3

Sympathomimetic amides-psychomotor stimulants

MOA: enhance excitatory transmission
Stimulate pre-synaptic rlease of DA and NE from storage vesicles–> increase synaptic catecholamine levels
Decrease DA, NE, and 5-HT reuptake
Affect mesolimbic reward circuitry

Effects:
CNS: euphoria, wakefulness, alertness
Cardiovascular: raise systolic and diastolic BP, MI, stroke
Respiratory: effect medullary respiratory center, increase depth and RR

Uses: ADHD, performance enhancement-alertness, narcolepsy and sleep disorders, severe obesity

Question 4

cocaine

modafinil

Answer 4

Sympathomimetic amides-psychomotor stimulants

MOA: enhance excitatory transmission
Block DAT, NET, and SERT–>inhibit uptake of DA, NE, and 5-HT
Affect reward circuitry
Modafinil: does not have CNS stimulant properties

Effects:
CNS: euphoria, wakefulness, alertness
Cardiovascular: raise systolic and diastolic BP, MI, stroke
Respiratory: effect medullary respiratory center, increase depth and RR

Uses: cocaine-local anesthetic

Question 5

atomoxetine (Straterra)

Answer 5

Sympathomimetic amides-psychomotor stimulants

MOA: enhance excitatory transmission
Block NET–>inhibit uptake of NE

Effects:
CNS: euphoria, wakefulness, alertness
Cardiovascular: raise systolic and diastolic BP, MI, stroke
Respiratory: effect medullary respiratory center, increase depth and RR

Uses: first non-stimulant for ADHD

Question 6

methylphenidate (Ritalin)
amphetamine (Adderall)
dextroamphetamine (Dexedrine)

Answer 6

Stimulant drugs for ADHD

Short, intermediate, and long-acting

Side effects: decreased appetite, weight loss, insomnia, headache, stomach aches, moodiness, motor tics

Question 7

atomexetine
clonidine
guanfacine
modafinil
antidepressants (TCAs, MAOIs, bupropion)

Answer 7

Non-stimulant drugs for ADHD
Not addictive

Atomoxetine: selective NE re-uptake blockade

Clonidine/guanfacine: alpha-2 agonist–> increase blood flow to prefrontal cortex
Given adjunct to control behavior

Modafinil: NOT FDA approved for children
Activates histamine neurons in tuberomammillary nucleus of hypothalamus–> wake promoter in brain activated–> attention and awakeness
Used for narcolepsy

Side effects: decreased appetite, weight loss, insomnia, headache, stomach aches, moodiness, motor tics