pharm - sedatives, anti-anxiety, & stimulant drugs

what are sedative-hypnotic drugs?

drugs that depress central nervous system function; primarily used to treat anxiety & insomnia

what are drugs that are used to treat anxiety disorders called?

anti-anxiety agents, anxiolytics, or tranquilizers

what are drugs that promote sleep called?

hypnotics

what are 2 sedative-hypnotic drugs?

benzodiazepines & benzodiazepine-like drugs

what is a prototype of BZDs?

alprazolam (xanax)

what is the mechanism of action for alprazolam?

benzodiazepines enhance GABA's effect; neurons become less excitable, leading to calming effects

what are the clinical uses of alprazolam?

anxiety, insomnia, muscle spasms, seizures, & alcohol withdrawal

what are the adverse effects of benzodiazepines?

CNS depression, anterograde amnesia, sleep driving, paradoxical effects, respiratory depression, & abuse

what is the main drug interaction with alprazolam?

combined with another CNS depressant (opioids, alcohol) can cause profound respiratory depression, coma, & death

what are signs of acute toxicity from BZDs, with an oral overdose?

drowsiness, lethargy, & confusion

what are signs of acute toxicity from BZDs, with an IV overdose?

profound hypotension, respiratory arrest, & cardiac arrest

what is the reversal drug of BZD toxicity?

flumazenil

what is flumazenil?

competitive benzodiazepine receptor antagonist; reverses the sedative effects of benzodiazepines but may not reverse respiratory depression

what is another prototype of BZDs?

zolpidem (ambien)

what is the mechanism of action for zolpidem?

chemically different (not true benzodiazepines) but bind to the same receptor site; selectively bind to a subunit on the GABA receptor which results in the sedative-hypnotic effects but little anxiolytic or muscle-relaxant action

what is the clinical use of zolpidem?

insomnia (short-term treatment)

what are the adverse effects of zolpidem?

daytime drowsiness, dizziness, complex sleep behaviors (sleep-waking/sleep-driving), & behavioral changes (agitation, aggressiveness)

what is a prototype of melatonin agonists?

ramelteon (rozerem)

what is the mechanism of action for ramelteon?

activation of melatonin receptors

what is the clinical use of ramelteon?

chronic insomnia; effective for patients having difficulty with sleep onset but not with sleep maintenance; rapid onset of about 30 minutes

what are the adverse effects of ramelteon?

no risk of dependence or withdrawal, minimal cognitive or motor impairment, & not a controlled substance

what are 2 other drugs used for the treatment of insomnia?

trazodone & doxepin

what is trazodone?

an atypical antidepressant with strong sedative action, can decrease sleep latency/prolong sleep duration, & does not cause tolerance or physical dependence

what is doxepin?

a trycyclic antidepressant with strong sedative actions & used to treat patients who have trouble staying asleep

what are 5 types of anxiety disorders?

generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder (social phobia), & post-traumatic stress disorder

what are 2 first-line anti-anxiety drugs?

selective serotonin reuptake inhibitors (SSRIs) & serotonin-norepinephrine reuptake inhibitors (SNRIs)

what are SSRIs?

therapeutic dose same or higher than depression treatment; "start low, go slow" principle

what are SNRIs?

comparable efficacy to SSRIs

what is serotonin syndrome?

autonomic instability (fast heart rate, high blood pressure, fever, sweating, diarrhea), brain/mood (agitation, confusion, restlessness), & muscles/nerves overactive (tremor, twitching, overactive reflexes, muscle jerking)

what is a non-benzodiazepine anti-anxiety drug within the azaprione class?

buspirone (buspar)

what is the mechanism of action for buspirone?

partial agonist at serotonin receptors & also has some affinity for dopamine (D2) receptors

what are the clinical uses of buspirone?

generalized anxiety disorder (GAD); not effect for acute anxiety or panic attacks (onset of action is typically 2 to 4 weeks)

what are the adverse effects of buspirone?

dizziness, nausea, headache, nervousness, & sedation

what are the drug/food interactions with busprione?

grapefruit juice

what is attention-deficit/hyperactivity disorder (ADHD)?

one of the most common neurodevelopmental disorders, often beginning in childhood but frequently persisting into adolescence & adulthood

what are the core symptoms of ADHD?

inattention, hyperactivity, & impulsivity

what is the pathophysiology behind ADHD?

involves dysregulation of dopamine & norepinephrine in brain pathways that control attention, behavior, & executive functioning

what are the 2 CNS stimulants?

amphetamines & methylphenidate

what is a non-stimulant?

alpha 2-adrenergic agonist

what is a prototype of CNS stimulants?

amphetamine (adderall)

what is the mechanism of action for amphetamine?

cause release of norepinephrine & dopamine; inhibits reuptake of both transmitters

what are the clinical uses of amphetamine?

ADHD (improves attention/focus, decreases hyperactivity/impulsivity) & narcolepsy (increase wakefulness/alertness)

what are the adverse effects of amphetamines?

insomnia, restlessness, decreased appetite, weight loss, increased heart rate, increased blood pressure, emotional lability, psychosis, & risk of abuse/misuse

what is tolerance like with amphetamines?

with regular use, tolerance develops to elevation of mood, suppression of appetite, & stimulation of the heart & blood vessels

what is physical dependence like with amphetamines?

abstinence syndrome with abrupt withdrawal

what is abuse like with amphetamines?

high potential for abuse due to euphoria

what is a prototype of methylphenidate/dexmethylphenidate?

ritalin

what is the mechanism of action for ritalin?

similar to amphetamine; key difference is that amphetamine induces four times as much dopamine release as methylphenidate, while methylphenidate is a more potent dopamine transporter inhibitor

what is the clinical use of ritalin?

first line treatment for ADHD in children & adolescencts

what are the adverse effects of ritalin

similar to amphetamines

what is a prototype of nonstimulants?

atomoxetine (strattera)

what is the mechanism of action for atomoxetine?

selective inhibitor of norepinephrine reuptake

what is the clinical use of atomoxetine?

ADHD

what are the adverse effects of atomoxetine?

gastrointestinal reactions, reduced appetite, dizziness, somnolence, mood swings, trouble sleeping, suicidal thoughts in children/adolescents, & hepatotoxicity

what is a prototype of alpha-2 adrenergic agonists?

clonidine

what is the mechanism of action for clonidine?

activates alpha-2 adrenergic receptors in the brain

what is the clinical use of clondinine?

ADHD in children & adolescents

what are the adverse effects of clonidine?

somnolence, fatigue, & hypotension; avoid abrupt discontinuation to avoid rebound hypertension

what is another prototype of alpha-2 adrenergic agonists?

modafinil (provigil)

what is the mechanism of action for modafinil?

binds to the dopamine transporter & inhibits dopamine reuptake; seem to influence areas of the brain involved in maintaining the normal sleep-wakefulness cycle

what are the clinical uses of modafinil?

narcolepsy, shift-work sleep disorder (SWSD), & obstructive sleep apnea/hypopnea syndrome

what are the adverse effects of modafinil?

headache, nausea, nervousness, diarrhea, & rhinitis

what is a drug interaction with modafinil?

oral contraceptives