Chapter 37 - Sedative-Hypnotic Drugs Flashcards
Sedative-hypnotics _________ CNS function
depress
What are sedative hypnotics used to treat?
anxiety and insomnia
How are antianxiety and hypnotic effects distinguished?
dosage
What is the most well known Benzodiazepine?
Diazepam (Valium)
What is the most prescribed benzodiazepine?
Lorazepam (Ativan)
Benefits of benzodiazepines over other CNS drugs:
-safer
-lower potential for abuse
-less tolerance and physical dependence
-fewer drug interactions
What are benzodiazepines used for?
-inducing general anesthesia
-seizure disorders
-muscle spasms
-alcohol withdrawal
How do Benzodiazepines act?
potentiate action of GABA
What do Benzodiazepines do to the CNS?
-reduce anxiety
-promote sleep
How do oral benzodiazepines affect the CV system?
they hardly do
How do IV benzodiazepines affect the CV system?
-hypotension
-possible cardiac arrest
How do benzodiazepines affect the respiratory system?
weak depression, even in toxic doses
Benzodiazepines (are/are not) lipid soluble
are
Most benzodiazepines undergo hepatic metabolism with active metabolites but which drugs have LESS extensive metabolism but NO METABOLITES…
Lorazepam
Oxazepam
Temazepam
Triazolam
Most benzodiazepines undergo hepatic metabolism with active metabolites but which drugs have extensive metabolism but NO METABOLITES…
Clonazepam
Diazepam, clonazepam, and flurazepam are _____ acting and have a half life of 3-100hrs
long
Triazolam, Lorazepam, and Alprazolam (Xanax) are ______ acting and have a half life of 2-20hrs
short
What are the adverse effects of Benzodiazepines?
-dizziness
-drowsiness
-confusion
-anterograde amnesia
-sleep depriving
-risk of falls (elderly)
-paradoxical effects (elderly)
-abuse
-withdrawal reaction
-respiratory depression (when injected or combined)
Are benzodiazepines safe during pregnancy?
no - risk category D and X
What do benzodiazepines interact with?
other CNS depressants
Does tolerance develop from Benzodiazepines?
to some effects but not others with prolonged use
What are the symptoms of an oral benzodiazepine overdose?
-drowsiness
-lethargy
-confusion
What are the symptoms of IV benzodiazepine overdose?
-life-threatening reactions
-hypotension
-respiratory and cardiac arrest
How is oral benzodiazepine overdose treated?
-gastric lavage
-saline cathartic
-dialysis
What is the reversal agent for acute benzodiazepine overdose?
flumazenil
What is flumazenil?
-competitive benzo receptor antagonist
What does flumazenil do?
reverse sedative effects but not respiratory depression
When does flumazenil work?
benzo OD and reversing effects after general anesthesia
How is flumazenil administered?
IV over 15s and repeated every min to a max dose of 3mg
Which benzodiazepines are available orally?
all of them
How is diazepam usually administered?
IV
How is lorazepam usually administered?
IM
What sedative class is zolpidem?
benzodiazepine-like drugs
What is Zolpidem?
a hypnotic for short-term management of insomnia
How does Zolpidem act?
interacting with a GABA-BZ receptor complex that bind to BZ1 and some a1 receptors
Does long-term Zolpidem use involve tolerance or increased AE?
generally no
What are the side effects of Zolpidem?
-drowsiness
-dizziness
-headache
-confusion
-euphoria
-muscle aches
How is Zolpidem administered?
sublingually
What is the initial Zolpidem dose for women?
5mg
What is the initial Zolpidem dose for men?
5-10mg
When should Zolpidem be taken?
before bed with 7-8hrs before awakening
Why does Zolpidem have a risk for morning driving impairment?
high blood levels after 10mg use overnight
What sedative class is Zopiclone?
benzodiazepine-like drugs
What is Zopiclone used for?
insomnia
How does Zopiclone act?
binding to the GABA𝚊 A1 subunit in the brain
What is the most common AE of Zopiclone?
bitter aftertaste
What are other side effects of Zopiclone?
-headache
-somnolence
-dizziness
-dry mouth
How is Zopiclone administered?
oral tabs
What is the recommended starting dose for Zopiclone?
3.75mg at bedtime
Zopiclone dose should not exceed ___ mg in old patients
5
What should patients taking Zopiclone be advised about driving?
wait 12 hours after dosing before driving
What is Lemborexant for?
insomnia
How does Lemborexant act?
competitive antagonist at orexin receptors (OX1R and OX2R)
What does the orexin neuropeptide system do?
promote wakefulness
Lemborexant is contraindicated in patients with _____________
narcolepsy
What are side effects of Lemborexant?
-somnolence
-headache
-nightmares
-depression
-suicidal ideation
Does tolerance to Lemborexant develop?
no
Lemborexant should not be taken with…
food or alcohol
Lemborexant is contraindicated in…
pts with liver disease
What are the side effects of melatonin?
-headache
-tachycardia
-pruritis
-nightmares
What are the side effects of L-Tryptophan?
-GI upset
-dry mouth
-dizziness
Chloral hydrate is fatal at doses more than ___ g
4
What are the side effects of chloral hydrate?
-GI
-arrhythmia risk
Chloral hydrate shouldn’t be taken with __________
alcohol
What are negative takeaways of Barbiturates?
-tolerance and dependence
-abuse
-multiple DI’s
-respiratory depressants, fatal
-not used as often (Benzos used more)
Thiopental is an __________-acting barbiturate
ultrashort
Secobarbital is a ______ to ________-acting barbiturate
short to intermediate
Phenobarbital is a _______-acting barbiturate
long
How do barbiturates act?
bind to GABA receptor-chloride channel complex
Barbiturates are lethal if mixed with _________
alcohol
Barbiturates have a _______ onset and _______ duration
rapid; brief
Barbiturates induce hepatic _________
enzymes
What are barbiturates used for?
-seizure disorders
-**mainly induction of anesthesia
-insomnia
What are the adverse effects of Barbiturates?
-respiratory depression
-suicide
-abuse
What are the symptoms of acute barbiturate toxicity?
-respiratory depression
-coma
-pinpoint pupils
How is barbiturate toxicity treated?
-removal of barbiturate (charcoal)
-maintain oxygen supply to brain
How are barbiturates administered?
oral, IV, IM
