Anxiolytics/Hypnotics and Psychostimulants Flashcards
Indications for anxiolytics and hypnotics?
anxiety disorders, muscle spasm, seizures, sleep disorders, alcohol withdrawal, anesthesia
Benzodiazepine mechanism?
potentiating effects of GABA
What benzos are long acting (half life >20 hrs)?
Diazepam (Valium), Clonazepam (Klonopin)
What benzos are intermediate acting (half life 6-20 hrs)?
Alprazolam (Xanax), Lorazepam (Ativan), Oxazepam (Serax), Temazepam (Restoril)
What benzos are short acting (half life <6 hrs)?
Triazolam (Halcion), Midazolam (Versed)
Which benzo has rapid onset?
Diazepam (Valium)
What is Diazepam (Valium) used for?
used during detoxification from alcohol or sedative-hypnotic anxiolytics and for seizures
less commonly prescribed to treat anxiety than previously
What is Clonazepam (Klonopin) used for?
anxiety, panic attacks
When should Clonazepam (Klonopin) be avoided?
avoid with renal dysfunction (longer half life acids once a day dosing)
Alprazolam (Xanax) is used for?
anxiety, panic attacks
What does one need to worry about with alprazolam (Xanax)?
short onset of action–>euphoria and high abuse potential
What is lorazepam (Ativan) used for?
panic attacks
alcohol and sedative-hypnotics-anxiolytic detoxification
agitation
What benzos are not metabolized by the liver (and thus can be used in chronic alcoholics or liver disease patients)?
LOT
Lorazepam (Ativan)
Oxazepam (Serax)
Temazepam (Restoril)
What is Oxazepam (Serax) used for?
alcohol and sedative-hypnotic-anxiolytic detoxification
What is temazepam (Restoril) used for?
decreasingly used for insomnia treatment due to dependence
What is Triazolam (Halcion) used for?
insomnia
primarily used in medical and surgical settings
What is midazolam (Versed) used for?
primarily used in medical and surgical settings
What are the major side effects of benzos?
drowsiness, impaired intellectual func, reduced motor coordination (careful in elderly), anterograde amnesia
Benzo toxicity can cause…
respiratory depression (especially when combined with alcohol!!)
Benzo toxicity is treated by…
flumazenil
Benzo withdrawal can cause…
seizures! death!
List non-benzo hypnotics
- Zolpidem (Ambien)/Zaleplon (Sonata)/eszopiclone (Lunesta)
- Diphenhydramine (Benadryl)
- Chloral hydrate (Noctec, Somnote)
- Ramelteon (Rozerem)
Zolpidem (Ambien)/Zaleplon (Sonata)/eszopiclone (Lunesta) mechanism?
Bind to benzo receptor 1 (selective receptor binding)–>sedation
Zolpidem (Ambien)/Zaleplon (Sonata)/eszopiclone (Lunesta) are used to treat what?
short term treatment of insomnia
Put in order of half life: Zolpidem (Ambien)/Zaleplon (Sonata)/eszopiclone (Lunesta) mechanism?
Zaleplon (Sonata)–>Zolpidem (Ambien)–>Eszopiclone (Lunesta)
Zolpidem (Ambien)/Zaleplon (Sonata)/eszopiclone (Lunesta) specific side effects?
anterograde amnesia, hallucinations, sleepwalking, GI side effects
less risk for tolerance/dependence than benzos with prolonged use (but can occur)
Diphenhydramine (Benadryl) specific side effects?
associated with antihistamine
sedation, dry mouth, constipation, urinary retention, blurry vision
Chloral hydrate (Noctec, Somnote) not commonly prescribed because…
- tolerance and dependence issues
- lethal in overdose (hepatic and liver failure)
Ramelteon (Rozerem) mechanism?
selective melatonin MT1 and MT2 agonist
Ramelteon (Rozerem) major benefit?
No tolerance or dependence
List Non-benzo anxiolytics
Buspirone (BuSpar)
Hydroxyzine (Atarax)
Barbituates (butalbitol, phenobarbitol, amobarbitol, pentobarbitol)
Propranolol
Buspirone (BuSpar) mechanism?
5HT-1A receptor (partial agonist)
… similar to trazodone
What are the pros and cons of buspirone?
- slower onset of action than benzos (1-2 weeks)
- not considered as effective–>often used in combo with other agents like SSRIs for treatment of anxiety
- does not potentiate CNS depression of alcohol (thus, useful in alcoholics)
- low potential for abuse/addiction
Hydroxyzine (Atarax) mechanism? Side effects?
antihistamine
–>sedation, dry mouth, constipation, urinary retention, blurry vision
Hydroxyzine (Atarax) most useful for what patients?
Anxiety patients that need quick-acting, short-term medication but cannot take benzos
Propranolol mechanism?
beta blocker
Propranolol is most useful for what patients?
treating autonomic effects of panic attacks or performance anxiety (palpitations, seating, tachycardia)
can also treat akathisia (from typical antipsychotics)
What patients should you be careful using propranolol with?
Caution in people with:
- DM and hyperthyroidism (can mask hypoglycemia)
- PVD and Raynaud’s (can exacerbate)
- MG may be worsened
- Other drugs with bradycardic effects
Contraindicated in patients with:
- Reversible airways diseases (asthma or COPD)
- Bradycardia, Sick sinus syndrome, AV block
- Shock
- Severe hypotension
- Cocaine toxicity
List psychostimulants
Dextroamphetamine and amphetamines (Dexedrine, Adderall)
Methylphenidate (Ritalin, Concerta)
Atomoxetine (Strattera)
Modafinil (Provigil)
Psychostimulants are used primarily for what disorders?
ADHD and refractory depression
Which of the psychostimulants are schedule II?
Adderall and methylphenidate (Ritalin, Concerta)
What should one monitor when taking dextroamphetamine and amphetamines?
bp, weight loss, insomnia
What should one monitor when taking methylphenidate (Ritalin, Concerta)?
leukopenia, anemia, inc LFTs
bo, weight loss, insomnia
Atomoxetine (Strattera) mechanism?
presynaptic NE transporter inhibitor
What are the benefits and cons to Atomoxetine (Strattera)?
less appetite suppression and insomnia
rare liver toxicity, possible inc SI in children/adolescents
Which psychostimulant is used in treating narcolepsy?
Modafinil (Provigil)
