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PHRM 845 > 4.5 Pharmacology of anxiolytics and sedative hypnotics > Flashcards

4.5 Pharmacology of anxiolytics and sedative hypnotics Flashcards

1
Q

Where are the GABAb receptor located?

A
  • Brain
  • Limbic system
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2
Q

How does GABAb receptor have inhibitory effects on the pre- and post- synapses?

A
  • Presynaptic: decrease Ca2+ conductance
  • Postsynaptic: Increase K conductance
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3
Q

What drug is a GABAb receptor agonist?

A

Xyrem (sodium oxybate salt of GHB)

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4
Q

What are the two classes of Xyrem and what are their uses?

A
  • C1: illicit use
  • C3: Medical use (liquid)
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5
Q

Who is xyrem available to?

A

Available only to prescribers enrolled in xyrem pt success program

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6
Q

What does the use of xyrem w concomitant stimulant lead to?

A
  • Decrease excessive daytime sleepiness
  • Increase daytime wakefulness
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7
Q

What effect does GHB have on the CNS?

A

Can cause CNS depression

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8
Q

What is the severity of GHB’s CNS depression dependent on?

A

Dose dependent

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9
Q

What is an issue regarding GHB for sleep?

A

Pts often awaken spontaneously and require another dose in middle of night

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10
Q

What are acute SE/AEs of GHB?

A
  • CNS depression: dizziness, drowsiness, coma
  • Loss of consciousness and reflexes
  • Amnesia
  • N/V, headache
  • Seizures
  • Death
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11
Q

What is GHB used as and why?

A

Used only as supportive tx bc there is no antagonist to counteract effects

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12
Q

What drugs are melatonin agonist?

A
  • Ramelteon (rozerem)
  • Tasimelteon (hetlioz)
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13
Q

What is the MOA of ramelteon (rozerem)?

A

High affinity for MT1 and MT2 melatonin receptors

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14
Q

Why is ramelteon’s (rozerem) MOA the way it is?

A
  • MT1 and MT2 melatonin receptors are on suprachiasmatic nucleus (SCN) which serves as “master clock” by regulating circadian rhythms
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15
Q

How is ramelteon (rozerem) metabolized?

A

CYP1A2 substrate

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16
Q

What is ramelteon (rozerem) used for?

A

Tx of insomnia characterized by difficulty w sleep onset

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17
Q

Does ramelteon (rozerem) have abuse potential?

A
  • Non-controlled substance sleep aid
  • No abuse, withdrawal, or dependency
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18
Q

What is a risk for ramelteon (rozerem)?

A

Negligible risk for next day “hangover” effects

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19
Q

What is the MOA of tasimelteon (hetlioz)?

A

High affinity for MT1 and MT2 melatonin receptors (same as ramelteon)

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20
Q

What is tasimelteon (hetlioz) used for?

A

Tx of non 24 hr sleep wake disorder

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21
Q

What is special about tasimelteon (hetlioz)?

A

It is an orphan drug

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22
Q

Where is the oxerin/hypocretin system located?

A

Hypothalamus

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23
Q

What is the MOA of suvorexant (belsomra)?

A
  • High affinity antagonist for OX1 and OX2 orexin receptors
  • Decrease arousal and attention via receptors in locus coeruleus and raphe
  • Produce rewarding stimuli via receptors that modulate mesolimbic projections between VTA and nucleus accumbens
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24
Q

What is suvorexant (belsomra) used for?

A

Tx of insomnia

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25
Q

What is a possible SE with suvorexant (belsomra)?

A

Morning impairment likely/possible (use lowest dose possible)

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26
Q

What did the FDA require for labeling on all sleep disorder drugs?

A

Include:
- Sleep driving
- Cooking and eating food and making phone calls while sleeping

27
Q

What is tryptophan?

A

A 5HT precursor dietary supplement

28
Q

What is an issue w tryptophan?

A
  • Withdrawn from market
  • Caused eosinophilia-myalgia syndrome
29
Q

What is melatonin?

A

A nutraceutical

30
Q

What is melatonin used for?

A

Insomnia, sleep disturbances

31
Q

What is a SE w melatonin?

A

Drowsiness

32
Q

What is lemon balm?

A

A sedative herb

33
Q

What is a caution w lemon balm?

A

Use w caution in pts w thyroid problems

34
Q

What is valerian?

A

A sedative herb

35
Q

What is valerian used for?

A

Insomnia

36
Q

What has been noted w valerian use?

A

Hepatotoxicity

37
Q

What is chamomile?

A

A mild sedative herb

38
Q

What are cautions w chamomile?

A
  • Avoid use in pts w a ragweed allergy
  • Use w caution in pts using P450 substrates
39
Q

What is kava kava?

A

A sedative herb

40
Q

What is kava kava used for?

A

Insomnia

41
Q

What is a possible problem w kava kava?

A

Possibly hepatotoxic

42
Q

What is the incidence and severity of sedative hypnotics overdose?

A
  • Incidence: commonly encountered in emergency room
  • Benzos or z-hypnotics in combination w other agents
43
Q

What are causes of sedative hypnotics overdose?

A
  • Suicide and suicide attempts
  • Drug abuse
44
Q

What are s/sxs of sedative hypnotics overdose?

A
  • Depressed respiration
  • Decreased BP and reflexes
  • Hypothermia
45
Q

What are txs for sedative hypnotics overdose?

A
  • Supportive tx: flumazenil for benzos or z-hypnotics
  • Maintain respiration
  • Maintain CV function
46
Q

When should tx for anxiety be considered?

A
  • Interferes w normal life
  • Interferes w another disease
47
Q

What drugs can induce anxiety?

A
  • Cocaine
  • Beta agonists
  • Psychostimulants like caffeine
  • Corticosteroids
48
Q

What diseases can induce anxiety?

A
  • CHF
  • COPD
  • Diagnosis of terminal disease
49
Q

Withdrawal of what meds can induce anxiety?

A
  • Antidepressants
  • Anxiolytics
  • Drugs of abuse
50
Q

What neurotransmitters can cause anxiety?

A

NE and serotonin

51
Q

How does NE cause anxiety?

A
  • Overactive locus coeruleus releases NE -> stimulates autonomic nervous system -> projects to amygdala (fear center)
  • Dysregulated in GAD and other anxiety disorders
52
Q

How is the GABAergic system involved in controlling/causing anxiety?

A
  • Normally counteracts/balances stimulatory effects of excess NE
  • Hypothesis is reduced GABAergic signaling causes anxiety
53
Q

How is serotonin involved in anxiety?

A

May involve amygdala and balance w NE

54
Q

Which serotonin targeting drugs have efficacy in GAD, panic disorder, OCD, social anxiety?

A
  • Drugs that target multiple receptors/SSRIs
  • Partial agonists of 5HT1A receptors effective
55
Q

What are the drug txs for anxiety?

A
  • Benzos (quick acting, effective)
  • Antidepressants (SSRIs, SNRIs, TCAs: take weeks; ketamine nasal spray: new breakthrough, very quick acting)
  • Buspirone (buspar)
  • BBs
56
Q

What is the pharmacological profile of buspirone (buspar)?

A
  • Partial agonist on brain for 5HT1A receptors
  • Moderate affinity for brain dopamine D2 receptors
57
Q

What is buspirone’s (buspar) onset of action compared to benzos?

A

Longer (adaptive response)

58
Q

What is the abuse potential of buspirone (buspar)?

A
  • Low abuse potential
  • Little to no withdrawal
59
Q

What are uses of buspirone (buspar)?

A
  • GAD, social anxiety, comorbid depression
  • Adjunct use w OCD, PTSD
60
Q

What is buspirone (buspar) not good for?

A

Panic disorders (use benzos instead)

61
Q

What are propranolol’s use?

A
  • Social anxiety: decreased peripheral sxs of anxiety
  • PTSD nightmares
62
Q

What are monitoring parameters of propranolol?

A

Monitoring CV:
- HR
- BP

63
Q

What are SEs of propranolol?

A
  • Hallucinations
  • Vivid dreams
  • Lethargy
  • Impotence
64
Q

What meds are misc anxiolytics?

A
  • Hydroxyzine (vistaril): histamine H1 antagonist
  • Clonidine (catapres): alpha2 agonist

PHRM 845 (48 decks)

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