CNS Stimulants

broad category of drugs with varied uses
- potential for abuse
- cause excitement and euphoria
- decreased feelings of fatigue
- increase motor activity
methylxanthines
- proposed mechanisms
  - increases Ca2+ influx
  - increase cAMP/cGMP
  - blockade of adenosine receptors
- effects
  - increased cardiac output
  - diuresis
  - decreased gastric pH
- therapy
  - bronchodilation
  - vasodilation
    - coronary arteries
  - potentiates analgesia (NSAIDs)
nicotine
- binds to receptors
  - CNS
  - ANS
  - neuromuscular junction
- MOA
  - dose-dependent effect
  - depolarization → depolarization blockade
    - causes receptors to fire → then block firing)
- actions
  - high dose cause respiratory paralysis and hypotension
  - peripheral effects through ANS stimulation
    - variable
varenicline
- chantix
  - used for smoking cessation
  - partial agonist
cocaine
- inhibits reuptake of monoamines
- can lead to dopamine depletion
  - increase NE and serotonin in the synapse
amphetamine
- MOA
  - increases monoamines at synaptic cleft
    - MAOI
    - direct release of intracellular storees
- actions
  - increase dopamine and NE
  - sympathetic effects
- therapeutic uses
  - ADHD
    - blocks dopamine reuptake
    - blocks NE reuptake
  - narcolepsy
    - similar mechanism
  - appetite suppression
    - phentermine
    - diethylpropion
    - controlled substance
- adverse effects
  - CNS
  - cardiovascular
  - GI
  - do not mix with MAO
- side effects
  - vertigo
  - HTN
  - insomnia
  - confusion
  - potential for addiction
  - nausea
  - diarrhea
Methylphenidate
- similar to amphetamine
- MOA
  - increase dopamine and NE
- adverse effects
  - predominantly GI
  - may induce seizures
- side effects
  - vertigo
  - HTN
  - insomnia
  - confusion
  - potential for addiction
  - nausea
  - diarrhea
Modafinil and Armodafinil
- narcolepsy
- may involve adrenergic and dopaminergic systems
- controlled substance