ch 29 Flashcards
sedative hypnotics are used primarily for 2 common disorders
anxiety and insomnia
agents given to promote sleep
hypnotics
what type of dose of sedative hypnotics to relieve anxiety
low dose
what type of dose of sedative hypnotics to promote sleep
high doses
drugs that are in the Benzodiazepine class
Alprazolam (Xanax) chlordiazepoxide (librium) clorazepate (Tranxene-T) Diazepam (Valium) Lorazepam (Ativan) Oxazepam
Estazolam Flurazepam Midazolam (Versed) Temazepam (Restoril) - insomnia only Triazolam (Halcion) - insomnia only Clonazepam (klonopin)
side effects of Benzodiazepines
reduce anxiety promote sleep induce muscle relaxation confusion anterograde amnesia
Cardiovascular system with Benzodiazepines
when taken orally -> almost no heart affects
when taken IV -> profound Hypotension and cardiac arrest
Benzodiazepines and resp system
weak resp depressants
in therapeutic doses -> little to no resp depression
toxic doses -> moderate resp depression at most
if combined with alcohol, opioids, barbiturates, ect…it can be a problem
with chronic COPD -> may worsen hypoventilation and hypoxemia
in Obstructive sleep apnea -> may exacerbate apneic episodes
How do Benzodiazepines work
intensify effects of GABA
high lipid solubility -> readily cross BBB
What benzodiazepines undergo very little metabolic alteration and are preferred in pt with hepatic impairment
Oxazepam
temazepam (Restoril)
lorazepam (Ativan)
Benzodiazepines are drugs of first choice for
and also approved for
acute anxiety
insomnia
seizure disorders
what 4 benzodiazepines are approved for seizure disorders
diazepam
clonazepam
lorazepam
clorazepate
what benzodiazepine may be administered to ease withdrawal from alcohol
diazepam
what benzodiazepine for muscle spasm and spasticity
Diazepam
anterograde amnesia in Benzodiazepines is esp troublesome with
triazolam (Halcion)
Sleep problem with Benzodiazepines
Sleep driving, preparing and eating meals, making phone calls. can occur even with normal doses
should be withdrawn if sleep driving is reported
must be tapered slowly with this side effect
Paradoxical effects with benzodiazepines
insomnia excitation euphoria anxiety rage
should be d/c
what type of benzodiazepines can cause resp depression
IV
abuse potential of benzodiazepines
what schedule?
low risk
schedule IV
Benzo in pregnancy
use during first trimester of pregnancy is associated with an increased risk for congenital malformations such as cleft lip, inguinal hernia and cardiac abnormalities.
use near time can cause CNS depression in neonate
d/c med if pregnant
Benzodiazepines and breastfeeding
NO
long vs short duration of action of benzo with physical dependence
short duration of therapy will have more intense symptoms of withdrawal (ie-Xanax)
prescribing a benzo that needs to help fall asleep
Triazolam
remember “tri to fall asleep) also tri to remember (retrograde amnesia
benzo and needs to prevent waking up later at night
estazolam would have a slower onset
remember “sta” asleep
what are the benzodiazepine-like drugs and what are they approved for
Zolpidem (Ambien)
zaleplon
eszopiclone
insomnia
(act on GABA)
(trying to get your zzzzzzs)
Benzodiazepine-like drugs are schedule
IV with low abuse potential
which Zolpidem (ambien) formulation would help you fall asleep and which one would help you stay asleep
All formulations will help you fall asleep
Ambien CR - help you stay asleep
when therapy is d/c for Zolpidem (ambien), is there rebound insomnia when d/c
no
side effect of Zolpidem (ambien)
daytime drowsiness
dizziness
sleep driving
small risk for angioedema and anaphylaxis
Zolpidem (ambien) is a schedule
IV
CNS and Zolpidem (ambien)
do not combine with other CNS depressants
Zaleplon (Sonata) is used for what part of sleep
fall asleep
side effects of Zaleplon (Sonata)
headache nausea drowsiness dizziness myalgia abd pain sleep driving mild rebound insomnia the first night after drug withdrawal
Zaleplon (Sonata) is a schedule
IV
Eszopiclone (Lunesta) is approved for treating
insomnia
reduces nighttime awakenings
adverse effect of Eszopiclone (Lunesta)
bitter aftertaste headache somnolence dizziness dry mouth sleep driving
rarely -anaphylaxis or angioedema
Eszopiclone (Lunesta) is a schedule
IV
Ramelteon is a
helps with what part of sleep
melatonin agonist
sleep onset
Ramelteon is a schedule
not regulated
Ramelteon onset
rapid (30 min)
most common side effects of Ramelteon are
somnolence dizziness fatigue sleep driving hallucination agitation mania amenorrhea galactorrhea reduced libido fertility problems
angioedema
anaphylaxis
Ramelteon with fluvoxamine (luvox)
increase levels of Ramelteon so should be avoided
Ramelteon and alcohol
can intensify sedation, avoid
Ramelteon should be avoided in
hepatic impairment
pregnancy
breastfeeding
Suvorexant (Belsomra) is approved for
insomnia with sleep onset and/or sleep maintenance problem
Suvorexant (Belsomra) is a schedule
IV
side effects Suvorexant (Belsomra)
somnolence headache dizziness diarrhea dry mouth cough hallucinations sleep paralysis vivid disturbing perceptions
Suvorexant (Belsomra) used with CYP
inhibitors such as ketoconazole, clarithromycin, ect can increase levels of Suvorexant (Belsomra)
Suvorexant (Belsomra) and digoxin
can increase digoxin levels
Suvorexant (Belsomra) contraindicated in
COPD obstructive sleep apnea narcolepsy breastfeeding pregnancy
ultra short acting Barbiturates are used for
induction of anesthesia
short to intermediate acting barbiturates are used for
sedatives and hypnotics
long acting barbiturates are used for
primarily antiseizure drugs
cardiovascular effects of barbiturates
hypnotic doses -> modest reduction in BP and HR
toxic doses -> profound hypotension and shock
high doses -> depress the myocardium and vascular smooth muscle along with all other electrically excitable tissues
CNS effects of barbiturates progress from ____ to ___ to ____
sedation to sleep to general anestesia
barbiturates and hepatic metabolism
CPY inducer
can accelerate its own metabolism and other drugs by promoting the synthesis of porphyrin which convers to heme which is incorporated into cyp450
tolerance and dependence of barbiturates
dose with continued treatment remains relatively constant whereas the therapeutic dose climbs higher and higher. You can knock out their resp drive
cross tolerance of barbiturates
barbiturates
alcohol
benzodiazepines
general anesthetics
withdrawal from general CNS depressants
weakness restlessness insomnia hyperthermia orthostatic hypotension confusion disorientation
by 3rd day - seizures
psychotic delirium - similar to alcoholic delirium tremens
extreme cases
exhaustion
cardiovascular collapse
death
evolves over 8 days
long acting barbiturate may be used to facilitate withdrawal process —-whats an example
phenobarbital
Barbiturates and insomnia
can promote sleep but bc of the undesired effects, now replaced by benzos and related drugs for treatment of choice for insomnia
Barbiturates are a schedule
III
high abuse potential
transient insomnia is ____ term laststing
short term - 2-3 weeks
if tolerance occurs with barbiturates what should you do
interrupt treatment is preferred rather than increasing dose which will restore responsiveness to treatment
hypnotics are contraindicated for
resp disorders
pregnancy
breastfeeding
drug dependency insomnia
a condition that can lead to the inappropriate prolongation of therapy
continued drug use ->low level dependence develops -> upon cessation of treatment ->mild withdrawal syndrome occurs and disrupt sleep -> failing to recognize the inability to sleep is a manifestation of drug withdrawal -> pt becomes convinced insomnia has returned and resumes drug use -> continued drug use leads to heightened physical dependence -> makes withdraw harder
Trazodone (oleptro)
used for?
physical dependence and tolerance?
adverse effects?
atypical antidepressant with strong sedative action
decrease sleep latency and prolong sleep duration
no tolerance or physical dependence
esp useful for insomnia resulting from use of antidepressants that cause cns stim
adverse effects
daytime grogginess
posural hypotension
Doxepin
old TCA with strong sedative effects
increased total sleep time and maintained the affected for more than 12 weeks due to block receptor of histamine
Doxepin side effects
when used in low doses for sleep maintenance
sedation
nausea
URI
when used in high doses for depression
hypotension
dysrhythmias
anticholinergic
Doxepin is contraindicated in
narrow angle glaucoma
severe urinary retention
Pt was taking a MAOI and now switching to Doxepin, how long do they have to wait
2 weeks
Doxepin is schedule
not regulated
what 2 OTC meds are approved for sleep aids by FDA
Diphenhydramine
Doxylamine (unisom)
anticholinergic effects
hormone that can be purchased used for sleep
Melatonin
normally, melatonin secretion is low during the day and begins to rise around ____ and reaches a peak between ___ and ____ and returns to baseline by ____
9pm
2am- 4am
baseline by morning
short term use of large doses of Melatonin can cause
hangover headache nightmares hypothermia transient depression
