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NEURO PHARM > Sleep Rx > Flashcards

Sleep Rx Flashcards

1
Q

There are two ascending arousal pathways. What’s the first?

A

The cholinergic cell groups in the upper pons( the PPT and LDT) activate the thalamus

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2
Q

What’s the 2nd AAS pathway?

A

2nd pathway: monoamine, histaminergic, GABAergic activates cortex to process thalamic inputs

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3
Q

What mediates the very rapid transition between sleep and awake state?

A

Orexin containing neurons in the hypothalamus. These neurons provide a link between the limbic system, energy homeostasis, the brain stem, and other system

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4
Q

How do orexin neurons promote wakefullness?

A

Orexin neurons promote wakefulness through monoaminergic nuclei that are wake-active

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5
Q

Stimulation of dopaminergic centers by orexins modulate what system?

A

The reward systems (VTA)

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6
Q

Stimulation of neuropeptide Y by orexin does what?

A

Increases food intake

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7
Q

How does the suprachiasmatic nucleus send input to orexin neurons?

A

Via the dorsomedial hypothalamus

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8
Q

Goals of insomnia Rx?

A

Improvement in nighttime and daytime Sx

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9
Q

What are some of the FDA concerns regarding the development of insomnia drugs?

A

Daytime somnolence, especially while driving. Unconscious nighttime activity, suicidal ideation, and other narcolepsy assoc events like sleep paralysis, hypnagogic hallucinations, and mild cataplexy

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10
Q

What are some key points regarding the Rx of insomnia?

A

Most drugs are used off label. 75% of the drugs are anti-depressants, only a handful are actually approved for insomnia, and lots of ppl treat themselves with OTC and herbal supplements (1st gen anti histamines and melatonin)

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11
Q

Which drugs are approved for Rx of insomnia?

A

Benzodizepines, BNZ receptor agonists, and melatonin receptor agonists

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12
Q

All of the drugs used to Rx insomnia act through effects on the GABA receptors in the CNS except for?

A

Ramelteon: which acts upon the melatonin receptor

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13
Q

What is thought to be responsible for the sedative, anti convulsant, anxiolytic, and myorelaxant drug properties?

A

Subunit modulation of the GABA-A receptor chloride channel

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14
Q

At normal clinical doses do any of the Rx’s work in place of endogenous GABA in opening the channel?

A

No. It is critical to appreciate that each of these drug classes modifies the response pattern of the GABA receptor to endogenous ligand.

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15
Q

Why have barbiturates been largely replaced by BNZ and BRA’s?

A

Clinical safety

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16
Q

What do BNZ and BRA require to act?

A

GABA-they allosterically modify the receptor response to GABA (shift the dose response curve to the left)

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17
Q

Why are barbiturates lethal at high doses?

A

B/c they fnc like GABA itself

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18
Q

What schedule are the BNZ’s and BRA’s?

A

Schedule IV

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19
Q

ADE’s of BNZs?

A

Sedation, cognitive impairment, and rebound insomnia (esp with short acting drugs)

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20
Q

What are withdrawal Sx of BNZs?

A

Anxiety, irritability, restlessness, obstructive sleep apnea, severe ventilatory impairment. Taper withdrawal

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21
Q

What subunit of the GABA receptor do BNZs bind?

A

alpha

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22
Q

What are the 3 different subgroups of the GABA-A receptor?

A

BZ-1=sedative and amnesic
BZ-2=anxiolysis
BZ-3=myorelaxation and anticonvulsant (supraclinical doses)

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23
Q

Which subgroups do BNZ’s and BRA’s effect?

A

BNZ’s: effect all three

BRA’s: BZ-1

24
Q

BNZ’s duration of action?

A

Complex mech. of elimination, but all lead to conjugation and renal excretion. Some drugs have many steps to reach glucoronidation (diazepam=long t1/2) but others go straight to glucoronidation (lorazepam and estazolam=short t1/2)

25
Q

What are contraindications for benzo’s?

A

liver dz, COPD, depression, driving, other CNS drugs, and glaucoma. Cat. X

26
Q

Estazolam?

A

CYP 3A4, doesn’t accumulate

27
Q

Flurazepam?

A

CYP 3A4, does accumulate

28
Q

Quazepam?

A

CYP 2B6>3A4, does accumulate

29
Q

Temazepam?

A

NO CYPs, doesn’t accumulate

30
Q

Triazolam?

A

CYP 3A4, no accumulation (rapidly inactivated)

31
Q

ADEs of BRA’s?

A

Sedation, cognitive impairment, rebound insomnia (esp short acting drugs)

32
Q

What are the withdrawal Sx of BRA’s?

A

Anxiety, irritability, restlessness, obstructive sleep apnea, severe ventilatory impairment. Taper withdrawal

33
Q

What are the contraindications for the BRAs?

A

All have CYP interactions, Liver dz, COPD, depression, driving, CNS drug interactions. Cat C

34
Q

What are the BRA’s we need to know?

A

Zolpidem, Zaleplon, and Eszopiclone

35
Q

Specifics for zolpidem?

A

Most prescribed hypnotic, sub lingual (only Rx for middle of the night use), and oral spray. Reduced dose for women (morning impairment)

36
Q

Specifics for zaleplon?

A

Ald dehydrogenase, variability in asians

37
Q

What’s Flumazenil?

A

Benzo antagonist. Used for reversal of sedation from benzos and BRAs. IV quick acting. Causes abrupt awakening (with dysphoria, agitation and maybe increased AE’s).

38
Q

What can cause seizures and withdrawal if given to chronic benzo users?

A

Flumazenil

39
Q

Can Flumazenil reverse sedation from any other drugs?

A

Nope

40
Q

Specifics regarding melatonin?

A

Involved in circadian rhythm. Receptors=GPCRs. Widely distributed in the CNS

41
Q

What does the MT-1 receptor do?

A

Attenuates suprachiasmatic nucleus activity

42
Q

What does the MT-2 receptor do?

A

Maintains circadian rhythms

43
Q

What does the MT-3 receptor do?

A

We don’t give a shit b/c it’s not involved in sleep

44
Q

What’s ramelteon?

A

Melatonin receptor agonist. Not a schedule Rx, no morning impairment, abuse or respiratory depression.

45
Q

Does ramelteon have CYP activity?

A

Yes, but no accumulation

46
Q

ADE’s for ramelteon?

A

HA, solmnolence, insomnia, upper RTI/nasopharyngitis. Not many studies done so far though

47
Q

Can antidepressants be used for insomnia?

A

Yes

48
Q

ADEs with antidepressants?

A

Sedation, CYPs, interaction with CNS drugs and EtOH

BBW for suicide, so caution in psychotic pts

49
Q

Which antidepressants do we need to know?

A

Doxepin, mirtazapine, and trazodone

50
Q

Specifics for doxepin?

A

Primarily anti H1 at low dose. Sedation. Muscarinic blocker, SNRI. Only one approved for insomnia

51
Q

Specifics for mirtazapine?

A

Significant a2 antagonism (reinforces 5HT and NE release)

52
Q

Specifics for trazadone?

A

Sedation with little 5HTRI

53
Q

How do 1st gen anti histamine cause sedation?

A

Cross BBB and produce sedation through central H1 action

54
Q

ADEs of anti H1’s?

A

Some anticholinergic effects (like zerostomia, blurred vision, urinary retention, and increased ocular pressure). Rapid tolerance may develop. Caution in old peeps and glaucoma

55
Q

Which anti H1’s should we know?

A

Diphenhydramine and doxylamine

NEURO PHARM (10 decks)

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