Chapter 37 - Sedative-Hypnotic Drugs Flashcards by Maeryn O

Sedative-hypnotics _________ CNS function

depress

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What are sedative hypnotics used to treat?

anxiety and insomnia

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How are antianxiety and hypnotic effects distinguished?

dosage

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What is the most well known Benzodiazepine?

Diazepam (Valium)

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What is the most prescribed benzodiazepine?

Lorazepam (Ativan)

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Benefits of benzodiazepines over other CNS drugs:

-safer
-lower potential for abuse
-less tolerance and physical dependence
-fewer drug interactions

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What are benzodiazepines used for?

-inducing general anesthesia
-seizure disorders
-muscle spasms
-alcohol withdrawal

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How do Benzodiazepines act?

potentiate action of GABA

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What do Benzodiazepines do to the CNS?

-reduce anxiety
-promote sleep

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How do oral benzodiazepines affect the CV system?

they hardly do

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How do IV benzodiazepines affect the CV system?

-hypotension
-possible cardiac arrest

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How do benzodiazepines affect the respiratory system?

weak depression, even in toxic doses

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Benzodiazepines (are/are not) lipid soluble

are

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Most benzodiazepines undergo hepatic metabolism with active metabolites but which drugs have LESS extensive metabolism but NO METABOLITES…

Lorazepam
Oxazepam
Temazepam
Triazolam

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Most benzodiazepines undergo hepatic metabolism with active metabolites but which drugs have extensive metabolism but NO METABOLITES…

Clonazepam

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Diazepam, clonazepam, and flurazepam are _____ acting and have a half life of 3-100hrs

long

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Triazolam, Lorazepam, and Alprazolam (Xanax) are ______ acting and have a half life of 2-20hrs

short

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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)

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Are benzodiazepines safe during pregnancy?

no - risk category D and X

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What do benzodiazepines interact with?

other CNS depressants

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Does tolerance develop from Benzodiazepines?

to some effects but not others with prolonged use

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What are the symptoms of an oral benzodiazepine overdose?

-drowsiness
-lethargy
-confusion

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What are the symptoms of IV benzodiazepine overdose?

-life-threatening reactions
-hypotension
-respiratory and cardiac arrest

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How is oral benzodiazepine overdose treated?

-gastric lavage
-saline cathartic
-dialysis

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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?

How is lorazepam usually administered?

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

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?

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

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

Chapter 37 - Sedative-Hypnotic Drugs Flashcards

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