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Summer pharm 4 > Sedatives > Flashcards

Sedatives Flashcards

1
Q

What NT mediate NREM sleep

A

GABA

Adenosine

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2
Q

What regulates REM sleep

A

Cholinergic cells turn REM on

Noradrenergic cells turn REM off

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3
Q

What facilitates arousal and wakefulness

A

Ascending reticular activating system and posterior hypothalamus
-NE, ACh, histamine, Substance P, corticotropin releasing factor

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4
Q

What is dopamine’s effect on sleep

A

Dopamine is alerting!

Low dopamine promotes sleepiness

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5
Q

What are important sleep wake concepts

A

Young adults have difficulty falling asleep
Middle aged and elderly have trouble staying asleep
Those with insomnia often also have anxiety, depression, or substance abuse disorders- and use nonRx drugs or alcohol to treat (esp. chronic insomnia)

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6
Q

Transient insomnia may be 2/2

A

Separation
Death in family
Job change
College exams

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7
Q

Common etiologies of insomnia are

A

Situational
Medical: CV, respiratory, chronic pain, endocrine, GI, Neuro, pregnancy
Psych
Pharm induced: anticonvulsants, central adrenergic blockers, diuretics, SSRI, steroids, stimulants

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8
Q

Goals of treating insomnia are

A

Correct underlying sleep complaint
Consolidate sleep
Improve daytime fxn
Avoid ADE from select therapies

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9
Q

What stimulus control procedures can you attempt as non-pharm Tx of insomnia

A

Establish regular times to wake up and go to sleep
Sleep only as much as you need to feel rested
Go to bed only when sleepy, no reading or TV in bed
Avoid trying to force sleep
Avoid blue-spectrum light
Avoid daytime naps
Schedule worry time during the day

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10
Q

What are sleep hygiene recommendations

A

Exercise 3-4x week, not close to bedtime
Create comfortable sleep environment (avoid temp extremes, loud noises, and light)
D/c alcohol, nicotine, and caffeine
Avoid large quantity of beverage at night
Do something relaxing you enjoy before bed

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11
Q

What effect do sedatives have

A

Reduce anxiety and exert calming effect; Take lowest dose possible to minimize degree of CNS depression

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12
Q

What effect do hypnotics have

A

Produce drowsiness and encourage onset and maintenance of state of sleep
More pronounced CNS depression than sedatives

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13
Q

What are sedatives and hypnotics used for

A

*Relief of anxiety and insomnia
sedation and amnesia for surgical procedures
Tx epilepsy and seizures
*Control of ethanol or other withdrawal states
Muscle relaxation in some neuromuscular d/o
Diagnostic aids or Tx in psych

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14
Q

What is the good thing about benzos vs barbituates and alcohol

A

Benzos will typically level off at a level of anesthesia as the dose increases
Barbituates and alcohol can send you into a coma

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15
Q

What are the PK of sedatives and hypnotics

A

Absorption/Distribution: Lipid soluble, absorbed from GI tract, good distribution to brain
Metabolism/Excretion: metabolized before elimination by hepatic enzymes.

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16
Q

What are the MC used drugs for insomnia

A

Eszopiclone, Zaleplon, Zolpidem (new, non-benzo GABA agonists; sedatives only)
Estazolam, Flurazepam, Quazepam, Temazepam, Triazolam (benzos; sedative, anxiolytic, muscle relaxer, anti-convulsant)

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17
Q

What is the MOA of benzos

A

Benzo receptor is in the thalamus, limbic structures, and cerebral cortex
Binding their receptor facilitates GABA in creating inhibition

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18
Q

Benzos are used for

A 
acute anxiety 
panic attack 
GAD 
insomnia 
skeletal muscle relaxer
seizure disorder
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19
Q

PK of benzos is

A

Hepatic metabolism
Active metabolites
CNS depression
2-4 hr half life

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20
Q

Benzo toxicity can lead to

A

Extension of CNS depressant actions
Tolerance
Dependence

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21
Q

Which benzos do NOT have active metabolites

A

Lorazepam
Oxazepam
Zolpidem

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22
Q

ADE of benzos are

A

high dose: daytime sedation, psychomotor incoordination, cognitive deficit, prolonged half life in elderly
Tolerance over time
Anterograde amnesia (no memory after taking dose)
Rebound insomnia after abrupt d/c
-take lowest dose possible to min rebound insomnia and amnesia

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23
Q

How long do most benzos maintain hypnotic efficacy

A

1 month

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24
Q

FDA requires this warning label on benzos AND barbiturates

A

Caution regarding anaphylaxis, facial angioedema, complex sleep behaviors

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25
Q

What substances interact with benzos MC

A 
Alcohol 
Antihistamines 
Antipsychotics 
Opioid analgesics 
TCA
26
Q

OD on benzos can cause

A

Potentially lethal respiratory and CV depression; more likely w/ alcohol, barbs, and carbamates; less common with new agents like zolpidem

27
Q

What can reverse the CNS depressant effects of benzos

A

Flumazenil!

but no benefit on OD of other sedatives or hypnotics

28
Q

How does Flumazenil work

A

Antagonist at benzo receptor site on GABA receptor (aka bring you up!)
IV but short half life

29
Q

Toxicities of flumazenil ae

A

agitation
confusion
possible withdrawal syndrome

30
Q

How do newer hypnotics work (zolpidem, zaleplon, eszopiclone)

A

they exert CNS effects via interaction w/ BZ1 or W1 benzo receptors.
They bind more selectively than benzos and bind only a1 GABA subunit near the benzo site (also facilitate Cl channel opening)
They are not benzos, but flumazenil still works on them
May cause dependence

31
Q

What are the barbiturates

A 
Amobarbital 
Butabarbital
Pentobarbital
Phenobarbital
Secobarbital
Thiopental
32
Q

How do barbiturates work

A

Facilitate and promote inhibitory effect of GABA and glycine- binds to different site than benzos
May also block excitatory glutamic acid and sodium channels
Flumazenil does NOT work on them

33
Q

Barbiturates are used for

A

Anesthesia (thiopental)
Insomnia and sedation (secobarbital)
Seizure d/o (phenobarbital)

34
Q

What is the PK of barbiturates

A

Oral activity
Hepatic metabolism
Induce metabolism of many drugs
4-6o hr half life

35
Q

Toxicities of barbiturates are

A

CNS depressant actions
tolerance
high dependence

36
Q

What effect do baribturates and carbamates have on the liver

A

induce liver enzymes= cause drug interactions
Precipitate acute intermittent porphyria
Chloral hydrate can increase anticoag effect

37
Q

What is the role of antihistamines in sedation

A

They have sedating properties and are usually effective in treating mild insomnia
Diphenhydramine and Doxylamine preferred
But, tolerance can develop, and increasing does does not produce a linear effect.

38
Q

ADE of antihistamines are

A

anticholinergic ADE!

blind, dry, red, hot

39
Q

How do antidepressants work in sedation

A

Amitriptyline, Doxepin, and Nortriptyline are sedating antidepressants that induce sleep continuity
*Low dose doxepin is FDA approved for insomnia
Mirtazapine promotes sleep
Trazodone improves sleep continuity at bedtime

40
Q

ADE of antidepressants are

A

daytime sedation
anticholinergic ADE
Mirtazapine: also weight gain
Trazodone: carryover sedation, a-adrenergic block (orthostais, worse in elderly), priapism

41
Q

Who is Trazodone good for

A

Those prone to substance abuse- does not cause dependence

Those with SSRI and buproprion induced insomnia

42
Q

What is Suvorexant

A

recently approved dual Orexin A and B receptor antagonist

Instead of inducing sleepiness, it turns off the wake signaling! Taken at bedtime

43
Q

What is orexin (hypocretin)

A

Excitatory action on 5-HT, histamine, ACh, and DA
Facilitatory role on GABA and glutamate induced neurotransmission
Has a primary role in sleep and arousal; energy regulation

44
Q

MC ADE of Suvorexant are

A

Somnolence

Sleep paralysis, cataplexy, other narcolepsy-like Sx

45
Q

What is Ramelteon

A

Melatonin receptor agonist approved for sleep-onset insomnia
Selective MT1 and 2 receptor to help melatonin regulate circadian rhythm and sleep onset
-Forms active metabolite via CYP1A2

46
Q

What are ADE of ramelteon

A

HA, dizziness, and somnolence

47
Q

Who is Ramelteon good for

A

Those with hx of substance abuse- not a controlled substance!
Those w/ COPD and sleep apnea

48
Q

What is Valerian

A

Herb with sedative-hypnotic properties for those w/ insomnia (can drink as tea at bedtime)
MOA may involve increasing GABA, but not fully known
-bad? it smells like gym socks

49
Q

What drugs do you do in different states

A

Anxiety: Alprazolam, Clonazepam
Sleep d/o: Estazolam, Flurazepam, Triazolam, Zolpidem, Zaleplon, Eszopiclone
Induce anesthesia: Thiopental
Component of anesthesia: diazepam, midazolam
Seizure d/o: Clonazepam, phenobarbital
Bipolar: Clonazepam
Muscle spasticity: diazepam
Managing withdrawal (longer acting): Chlordiazepoxide*, diazepam

50
Q

What do you need in order to diagnose anxiety disorder

A

overt anxiety or overt manifestation of a copine mechanism
Not just an adjustment disorder
Somatic Sx (dyspnea, palpitations, paresthesias)
Not 2/2 physical disorder or psych condition or drug abuse

51
Q

What medical illnesses are associated with anxiety

A

Cardiovascular: angina, arrhythmia, CHF, HTN
Endocrine: cushings, DM, hyper/hypothyroid, hypoglycemia
GI: IBS, IBD, PUD
Neuro: migraine, Sz, stroke
Resp: asthma, COPD, PE, PNA
anemia, cancer, SLE

52
Q

What are some drug classes associated with anxiety Sx

A 
anticonvulsants 
antidepressants 
antiHTN
antibiotics 
bronchodilators 
corticosteroids 
dopamine agonists 
herbals 
ecstasy, marijuana 
NSAIDs 
caffeine, cocaine, amphetamines, nicotine
Sympathomimetics
thyroid hormones
53
Q

What is first line for GAD

A 
Duloxetine 
Escitalopram 
Paroxetine 
Sertraline 
Venlafaxine
54
Q

What is first line for panic disorder

A

SSRI

Venlafaxine

55
Q

What is first line for social anxiety disorder

A 
Escitalopram 
Fluvoxamine 
Paroxetine 
Sertraline 
Venlafaxine
56
Q

What is Buspirone

A 
a selective anxiolytic; 
Partial 5HT agonist +/- D2 agonist 
Partial 5HT1a agonist 
Minimal CNS depressant effects; can still drive while on it 
No anticonvulsant or muscle relaxant properties
Safe in pregnancy! 
Minimal dependence with long term use 
Little rebound anxiety
57
Q

PK of Buspirone are

A

Slow onset (1 week)
Forms active metabolite
Interacts with CYP3A4 inducer and inhibitor

58
Q

Who is Buspirone good for

A

Generalized anxety disorder

Less effective for panis disorder

59
Q

ADE of Buspirone are

A

GI distress
tachycardia
paresthesia

60
Q

What drugs treat panic disorder (specifically)

A

SSRI: Citalopram, Escitalopram, Fluoxetine, Fluvoxatine, Paroxetine, Sertraline
SNRI: Venlafaxine
Benzo: Alprazolam, Clonazepam, Diazepam, Lorazepam
TCA: Imipramine
MOI: Phenelzine

61
Q

What type of alprazolam is best for panic disorder

A

Xanax XR! it has a longer half life so you dont get panic Sx when you stop taking it like you do with regular xanax

Summer pharm 4 (14 decks)

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