CNS Stimulants and Related Drugs – Chapter 13
Structurally Related Central Nervous System Stimulants
Chemical Category CNS Stimulants & Related Drugs
Amphetamines and related Dextroamphetamine,
stimulants methamphetamine, benzphetamine,
methylpenidate, dexmthylphenidate
Serotonin agonists Almotriptan, electriptan, frovatriptan,
naratriptan, rizatriptam, sumatriptan,
zolmitripan
Sympathomimetics Phentermine
Xanthines Caffeine, theophylline, aminophylline
Miscellaneous Modafinil, armodafinil, orlistat (lipase
inhibitor), doxapram (analeptic)
Central Nervous System Stimulants: Site of Action
Primary Site of Action CNS Stimulants
Cerebrovascular system, 5-HT Serotonin agonists
(1D/1B) receptors
Cerebral Cortex Amphetamines, phenidates, modafinil,
armodafinil
Hypothalamic and limbic regions Anorexiants
Medulla and brainstem Analeptic
CNS Stimulants & Related Drugs: Therapeutic Categories
Category Drugs
Anti-ADHD dextroamphetamine, lisdexamfetamine, methamphetamine,
methylphenidate, atomoxetine (norepinephrine reuptake
inhibitor)
Antinarcolep dextroamphetamine, methamphetamine, methylphenidate,
tic modafinil, armodafinil
Anorexiant methamphetamine, phentermine, phendimetrazine,
diethylpropion, benzphetamine, orlistat (lipase inhibitor),
loracaserin
Antimigraine almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan,
sumatriptan, zolmitriptan (serotonin agonists);
dihydroergotamine mesylate, ergot-amine tartrate with
caffeine (ergot alkaloids)
Analeptic caffeine, doxapram, aminophylline, theophylline, modafinil,
armodafinil (antinarcoleptic)
, CNS Stimulants and Related Drugs – Chapter 13
Drugs for Attention-Deficit/Hyperactivity Disorder and
Narcolepsy
Amphetamines and Related Stimulants
Amphetamines
o Dextroamphetamine (Immediate Release): ADHD & Narcolepsy
PO: 30-60min – 3hr – 12hr – 10hr
Dextroamphetamine sulfate (Dexedrine); Dextroamphetamine
sulfate, dextroamphetamine saccharate, amphetamine
sulfate, and amphetamine aspartate (Adderall, Adderall XR)
o Atomoxetine – Strattera: ADHD in children older than 6yrs and
adults
PO: 60min – 1-2hr – 5-24hr – 24-120hr
Not a controlled substance because it lacks addictive
properties; erectile dysfunction is a common side effect
Suicidal tendencies in adolescents and children
o Methylphenidate – Ritalin: narcolepsy and ADHD
PO: 30-60min – 6-8hr – 103hr – 4-6hr
Extended-release dosage forms include Ritalin SR, Concerta,
and Metadate CD
Child: 5mg before breakfast and lunch. Adult: 20mg after
lunch
o Modafinil – Provigil: daytime sleepiness associated with narcolepsy
PO: 1-2months – 2-4hr – 8-15hr – unknown
Schedule IV drug; related drug is armodanfinil (Nuvigil)
Antimigraine Drugs
Serotonin Receptor Agonists – are used to treat migraine headache. Produce
relief from moderate to severe migraines within 2 hours in 70% to 80% of
patients. Work by stimulating 5-HT(1) receptors in the brain and are
sometimes referred to as SSRAs to triptans.
Sumatriptan – Imitrex
o PO: 0.5-1hr – 2.5hr – 2.5hr – 4h
Ergot Alkaloids – Ergotamine
o Nasal spray (Migranal)
o Ergotamine tartrate w/ caffeine (Cafergot) – tablet form
o Adverse Effects: dizziness, numbness, and nasal irritation.
Structurally Related Central Nervous System Stimulants
Chemical Category CNS Stimulants & Related Drugs
Amphetamines and related Dextroamphetamine,
stimulants methamphetamine, benzphetamine,
methylpenidate, dexmthylphenidate
Serotonin agonists Almotriptan, electriptan, frovatriptan,
naratriptan, rizatriptam, sumatriptan,
zolmitripan
Sympathomimetics Phentermine
Xanthines Caffeine, theophylline, aminophylline
Miscellaneous Modafinil, armodafinil, orlistat (lipase
inhibitor), doxapram (analeptic)
Central Nervous System Stimulants: Site of Action
Primary Site of Action CNS Stimulants
Cerebrovascular system, 5-HT Serotonin agonists
(1D/1B) receptors
Cerebral Cortex Amphetamines, phenidates, modafinil,
armodafinil
Hypothalamic and limbic regions Anorexiants
Medulla and brainstem Analeptic
CNS Stimulants & Related Drugs: Therapeutic Categories
Category Drugs
Anti-ADHD dextroamphetamine, lisdexamfetamine, methamphetamine,
methylphenidate, atomoxetine (norepinephrine reuptake
inhibitor)
Antinarcolep dextroamphetamine, methamphetamine, methylphenidate,
tic modafinil, armodafinil
Anorexiant methamphetamine, phentermine, phendimetrazine,
diethylpropion, benzphetamine, orlistat (lipase inhibitor),
loracaserin
Antimigraine almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan,
sumatriptan, zolmitriptan (serotonin agonists);
dihydroergotamine mesylate, ergot-amine tartrate with
caffeine (ergot alkaloids)
Analeptic caffeine, doxapram, aminophylline, theophylline, modafinil,
armodafinil (antinarcoleptic)
, CNS Stimulants and Related Drugs – Chapter 13
Drugs for Attention-Deficit/Hyperactivity Disorder and
Narcolepsy
Amphetamines and Related Stimulants
Amphetamines
o Dextroamphetamine (Immediate Release): ADHD & Narcolepsy
PO: 30-60min – 3hr – 12hr – 10hr
Dextroamphetamine sulfate (Dexedrine); Dextroamphetamine
sulfate, dextroamphetamine saccharate, amphetamine
sulfate, and amphetamine aspartate (Adderall, Adderall XR)
o Atomoxetine – Strattera: ADHD in children older than 6yrs and
adults
PO: 60min – 1-2hr – 5-24hr – 24-120hr
Not a controlled substance because it lacks addictive
properties; erectile dysfunction is a common side effect
Suicidal tendencies in adolescents and children
o Methylphenidate – Ritalin: narcolepsy and ADHD
PO: 30-60min – 6-8hr – 103hr – 4-6hr
Extended-release dosage forms include Ritalin SR, Concerta,
and Metadate CD
Child: 5mg before breakfast and lunch. Adult: 20mg after
lunch
o Modafinil – Provigil: daytime sleepiness associated with narcolepsy
PO: 1-2months – 2-4hr – 8-15hr – unknown
Schedule IV drug; related drug is armodanfinil (Nuvigil)
Antimigraine Drugs
Serotonin Receptor Agonists – are used to treat migraine headache. Produce
relief from moderate to severe migraines within 2 hours in 70% to 80% of
patients. Work by stimulating 5-HT(1) receptors in the brain and are
sometimes referred to as SSRAs to triptans.
Sumatriptan – Imitrex
o PO: 0.5-1hr – 2.5hr – 2.5hr – 4h
Ergot Alkaloids – Ergotamine
o Nasal spray (Migranal)
o Ergotamine tartrate w/ caffeine (Cafergot) – tablet form
o Adverse Effects: dizziness, numbness, and nasal irritation.
