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Cassandra's Pharmacology > Module 4 Chapter 29 Sedative/hypnotics > Flashcards

Module 4 Chapter 29 Sedative/hypnotics Flashcards

1
Q

sedative hypnotics are used primarily for 2 common disorders

A

anxiety and insomnia

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2
Q

agents given to promote sleep

A

hypnotics

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3
Q

what type of dose of sedative hypnotics to relieve anxiety

A

low dose

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4
Q

what type of dose of sedative hypnotics to promote sleep

A

high doses

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5
Q

drugs that are in the Benzodiazepine class

A 
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)
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6
Q

side effects of Benzodiazepines

A 
reduce anxiety
promote sleep
induce muscle relaxation
confusion
anterograde amnesia
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7
Q

Cardiovascular system with Benzodiazepines

A

when taken orally -> almost no heart affects

when taken IV -> profound Hypotension and cardiac arrest

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8
Q

Benzodiazepines and resp system

A

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

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9
Q

How do Benzodiazepines work

A

intensify effects of GABA

high lipid solubility -> readily cross BBB

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10
Q

What benzodiazepines undergo very little metabolic alteration and are preferred in pt with hepatic impairment

A

Oxazepam
temazepam (Restoril)
lorazepam (Ativan)

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11
Q

Benzodiazepines are drugs of first choice for

and also approved for

A

acute anxiety

insomnia
seizure disorders

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12
Q

what 4 benzodiazepines are approved for seizure disorders

A

diazepam
clonazepam
lorazepam
clorazepate

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13
Q

what benzodiazepine may be administered to ease withdrawal from alcohol

A

diazepam

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14
Q

what benzodiazepine for muscle spasm and spasticity

A

Diazepam

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15
Q

anterograde amnesia in Benzodiazepines is esp troublesome with

A

triazolam (Halcion)

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16
Q

Sleep problem with Benzodiazepines

A

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

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17
Q

Paradoxical effects with benzodiazepines

A 
insomnia
excitation
euphoria
anxiety
rage

should be d/c

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18
Q

what type of benzodiazepines can cause resp depression

A

IV

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19
Q

abuse potential of benzodiazepines

what schedule?

A

low risk

schedule IV

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20
Q

Benzo in pregnancy

A

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

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21
Q

Benzodiazepines and breastfeeding

A

NO

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22
Q

long vs short duration of action of benzo with physical dependence

A

short duration of therapy will have more intense symptoms of withdrawal (ie-Xanax)

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23
Q

prescribing a benzo that needs to help fall asleep

A

Triazolam

remember “tri to fall asleep) also tri to remember (retrograde amnesia

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24
Q

benzo and needs to prevent waking up later at night

A

estazolam would have a slower onset

remember “sta” asleep

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25
Q

what are the benzodiazepine-like drugs and what are they approved for

A

Zolpidem (Ambien)
zaleplon
eszopiclone

insomnia
(act on GABA)

(trying to get your zzzzzzs)

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26
Q

Benzodiazepine-like drugs are schedule

A

IV with low abuse potential

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27
Q

which Zolpidem (ambien) formulation would help you fall asleep and which one would help you stay asleep

A

All formulations will help you fall asleep

Ambien CR - help you stay asleep

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28
Q

when therapy is d/c for Zolpidem (ambien), is there rebound insomnia when d/c

A

no

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29
Q

side effect of Zolpidem (ambien)

A

daytime drowsiness
dizziness

sleep driving

small risk for angioedema and anaphylaxis

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30
Q

Zolpidem (ambien) is a schedule

A

IV

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31
Q

CNS and Zolpidem (ambien)

A

do not combine with other CNS depressants

32
Q

Zaleplon (Sonata) is used for what part of sleep

A

fall asleep

33
Q

side effects of Zaleplon (Sonata)

A 
headache
nausea
drowsiness
dizziness
myalgia
abd pain
sleep driving
mild rebound insomnia the first night after drug withdrawal
34
Q

Zaleplon (Sonata) is a schedule

A

IV

35
Q

Eszopiclone (Lunesta) is approved for treating

A

insomnia

reduces nighttime awakenings

36
Q

adverse effect of Eszopiclone (Lunesta)

A 
bitter aftertaste
headache
somnolence
dizziness
dry mouth
sleep driving

rarely -anaphylaxis or angioedema

37
Q

Eszopiclone (Lunesta) is a schedule

A

IV

38
Q

Ramelteon is a

helps with what part of sleep

A

melatonin agonist

sleep onset

39
Q

Ramelteon is a schedule

A

not regulated

40
Q

Ramelteon onset

A

rapid (30 min)

41
Q

most common side effects of Ramelteon are

A 
somnolence
dizziness
fatigue
sleep driving
hallucination
agitation
mania
amenorrhea
galactorrhea
reduced libido
fertility problems

angioedema
anaphylaxis

42
Q

Ramelteon with fluvoxamine (luvox)

A

increase levels of Ramelteon so should be avoided

43
Q

Ramelteon and alcohol

A

can intensify sedation, avoid

44
Q

Ramelteon should be avoided in

A

hepatic impairment
pregnancy
breastfeeding

45
Q

Suvorexant (Belsomra) is approved for

A

insomnia with sleep onset and/or sleep maintenance problem

46
Q

Suvorexant (Belsomra) is a schedule

A

IV

47
Q

side effects Suvorexant (Belsomra)

A 
somnolence
headache
dizziness
diarrhea
dry mouth
cough
hallucinations
sleep paralysis
vivid disturbing perceptions
48
Q

Suvorexant (Belsomra) used with CYP

A

inhibitors such as ketoconazole, clarithromycin, ect can increase levels of Suvorexant (Belsomra)

49
Q

Suvorexant (Belsomra) and digoxin

A

can increase digoxin levels

50
Q

Suvorexant (Belsomra) contraindicated in

A 
COPD
obstructive sleep apnea
narcolepsy
breastfeeding
pregnancy
51
Q

ultra short acting Barbiturates are used for

A

induction of anesthesia

52
Q

short to intermediate acting barbiturates are used for

A

sedatives and hypnotics

53
Q

long acting barbiturates are used for

A

primarily antiseizure drugs

54
Q

cardiovascular effects of barbiturates

A

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

55
Q

CNS effects of barbiturates progress from ____ to ___ to ____

A

sedation to sleep to general anestesia

56
Q

barbiturates and hepatic metabolism

A

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

57
Q

tolerance and dependence of barbiturates

A

dose with continued treatment remains relatively constant whereas the therapeutic dose climbs higher and higher. You can knock out their resp drive

58
Q

cross tolerance of barbiturates

A

barbiturates
alcohol
benzodiazepines
general anesthetics

59
Q

withdrawal from general CNS depressants

A 
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

60
Q

long acting barbiturate may be used to facilitate withdrawal process —-whats an example

A

phenobarbital

61
Q

Barbiturates and insomnia

A

can promote sleep but bc of the undesired effects, now replaced by benzos and related drugs for treatment of choice for insomnia

62
Q

Barbiturates are a schedule

A

III

high abuse potential

63
Q

transient insomnia is ____ term laststing

A

short term - 2-3 weeks

64
Q

if tolerance occurs with barbiturates what should you do

A

interrupt treatment is preferred rather than increasing dose which will restore responsiveness to treatment

65
Q

hypnotics are contraindicated for

A

resp disorders
pregnancy
breastfeeding

66
Q

drug dependency insomnia

A

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

67
Q

Trazodone (oleptro)

used for?
physical dependence and tolerance?

adverse effects?

A

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

68
Q

Doxepin

A

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

69
Q

Doxepin side effects

A

when used in low doses for sleep maintenance
sedation
nausea
URI

when used in high doses for depression
hypotension
dysrhythmias
anticholinergic

70
Q

Doxepin is contraindicated in

A

narrow angle glaucoma

severe urinary retention

71
Q

Pt was taking a MAOI and now switching to Doxepin, how long do they have to wait

A

2 weeks

72
Q

Doxepin is schedule

A

not regulated

73
Q

what 2 OTC meds are approved for sleep aids by FDA

A

Diphenhydramine
Doxylamine (unisom)

anticholinergic effects

74
Q

hormone that can be purchased used for sleep

A

Melatonin

75
Q

normally, melatonin secretion is low during the day and begins to rise around ____ and reaches a peak between ___ and ____ and returns to baseline by ____

A

9pm
2am- 4am
baseline by morning

76
Q

short term use of large doses of Melatonin can cause

A 
hangover
headache
nightmares
hypothermia
transient depression

Cassandra's Pharmacology (14 decks)

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