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what are the clinical applications and indications of prescribing CNS stimulants?
fatigue, narcolepsy, ADHD, obesity
the manifestations of stimulant action in increasing order are...
1. increased __________
2. increased _______________ and ____________
3. __________________
alertness, nervousness, anxiety, convulsions/seizures
CNS stimulation is caused by two mechanisms:
the ______________ of an excitatory neurotransmission
the _________________ of an inhibitory neurotransmission
enhancement, depression
caffeine has the greatest stimulant effect of the __________________ (class)
methylxanthines
how does methylxanthine (caffeine) impact headache?
may enhance (and quicken) the analgesic effect of acetaminophen, aspirin or ibuprofen (particularly in the case of migraine headache) (fioricet)
what is the MOA of caffeine?
blocks adenosine receptors on neurons
what are some of the adverse effects of caffeine?
cardiovascular (tachycardia, palpitations, increased BP), CNS (insomnia, restlessness, nervousness, tremors, tinnitus), GI (nausea, diarrhea, gastritis)
what symptoms can chronic caffeine drinkers experience if they abstain from consumption?
headache, fatigue, impaired concentration
what is the half-life of nicotine?
30 minutes
which medications does nicotine cause faster breakdown of?
beta-blockers, benzodiazepines, and opioids
cocaine is apart of which drug schedule class?
CII
what is the MOA of cocaine, centrally and locally?
centrally: inhibits reuptake of dopamine and NE
locally (anesthetic): blocks Na+ channels
what are the main adverse effects of cocaine use?
cardiovascular (tachycardia, HTN, arrhythmias, MI), CNS (excitement, anxiety, agitation, paranoid psychosis), pulmonary (cheyne-stokes, pulmonary edema)
what is the MOA of amphetamine and its derivatives?
increases release of NE and dopamine and blocks their reuptake
name the 4 amphetamine and amphetamine derivatives.
amphetamine, dextroamphetamine, lisdexamphetamine, amphetamine/dextroamphetamine salts
what drug schedule class do amphetamines belong to?
CII
what is the MOA of methylphenidate and dexmethylphenidate?
inhibit dopamine reuptake
what drug schedule class do methylphenidate and dexmethylphenidate belong to?
CII
why are methylphenidate and dexmethylphenidate better than amphetamines?
cause less irritability, anxiety and anorexia
what are the main indications for prescribing amphetamine, amphetamine derivatives & methylphenidate?
narcolepsy, ADHD (children >6 years old)
what are some of the cardiovascular adverse effects of amphetamine, amphetamine derivatives & methylphenidate?
HTN, tachyarrhythmias, stroke, angina, MI
what are some of the CNS adverse effects for amphetamine, amphetamine derivatives & methylphenidate?
increased risk for seizures, jitteriness, dizziness, psychotic symptoms
what are some of the metabolic adverse effects for amphetamine, amphetamine derivatives & methylphenidate, specifically in children?
slowed growth & weight loss
what are some contraindications to prescribing amphetamine, amphetamine derivatives, and methylphenidate?
cardiovascular disease, HTN, hyperthyroidism, glaucoma, anxiety, history of drug abuse, use within 14 days of MAOIs
what is a non-stimulate and non-controlled treatment for ADHD in children, adolescents, and adults?
atomoxetine
what is the MOA of atomoxetine?
selective NE reuptake inhibitor
in what circumstance is atomoxetine used to treat ADHD in children and adolescents?
substance abuse problem, family member with a substance abuse problem, tics, or severe side effects with stimulants
is atomoxetine less or more likely to cause cardiovascular side effects when compared to the other ADHD stimulants?
less likely, still possible
what is the black box warning for atomoxetine?
increased risk of suicidal thinking in children and adolescents
when should the use of atomoxetine be immediately discontinued?
patients with jaundice or laboratory evidence of liver injury
what are some of the adverse effects of atomoxetine?
weight loss, vomiting, nausea, headache, dizziness
what are the contraindications to prescribing atomoxetine?
hypersensitivity to atomoxetine, use within 14 days of MAOIs, glaucoma, pheochromocytoma, severe CV disorders
what are the 4 third line medications/classes for treating ADHD (in adults)?
bupropion, venlafaxine, TCAs, central alpha agonists
what medications are non-amphetamine wakefulness-promoting agents and are considered first line for naroclepsy?
modafinil and armodafinil
what drug schedule class to modafinal and armodafinil belong to?
CIV
what are the labeled uses for modafinal and armodafinil?
narcolepsy, OSA, shift work sleep disorder
which medication - modafinil or armodafinil - has a longer half life?
armodafinil (has extended effects)
what are the 2 important DDIs of modafinil/armodafinil?
increases breakdown of OCP, inhibits metabolism of warfarin
what can modafinil/armodafinil be used to treat off-label?
ADHD
can modafinil/armodafinil be used in children?
no
what are some of the adverse effects of modafinil/armodafinil?
headache, nausea, nervousness, rhinitis, anxiety, insomnia
what is the MOA for solriamfetol?
inhibits dopamine and NE reuptake
what schedule drug class is solriamfetol?
CIV
what are some of the adverse effects of solriamfetol?
headache, nausea, insomnia, anxiety
what is the MOA for sodium oxybate?
GABA agonist
what schedule class does sodium oxybate belong to?
CIII
what are some of the adverse effects of sodium oxybate?
nausea, dizziness, anxiety, weight loss (also weird dosing schedule)
what is the only non-controlled medication approved for narcolepsy?
pitolisant
what is the MOA of pitolisant?
blocks histamine-3 receptors in some areas of the brain, increases histamine release in other parts of the brain
what are some of the adverse effects of pitolisant?
headache, irritability, anxiety, QT prolongation