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Neuro 2 > Drugs for Insomnia > Flashcards

Drugs for Insomnia Flashcards

1
Q

Cell groups from the PPT and LDT that activate the thalamus use what neurotransmitter?

A

Ach

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2
Q

What is the role of orexin?

A

controls transition from sleep to awake states

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3
Q

What is the function of GABA in wakefulness?

A

GABA functions as a negative regulator of these ascending pathways and also functions as an inhibitor of the neuronal activity in the cortex.

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4
Q

What are the goals for treatment of insomnia?

A

improve nighttime and daytime symptoms

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5
Q

What are the only FDA approved drug classes for insomnia?

A

Benzodiazepines
Benzodiazepine receptor agonists
Melatonin receptor agonist

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6
Q

What is the MOA of benzodiazepines and benzodiazepine receptor agonists in the treatment of insomnia?

A

Endogenous GABA opens the channel and these drugs structurally reconfigure the open pore

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7
Q

What is the MOA of antidepressants in the off-label treatment of insomnia?

A

sedation due to anti-histaminergic effect centered in the tuberomammillary nucleus

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8
Q

What is the MOA of OTC 1st generation antihistamines in the treatment of insomnia?

A

sedation due to anti-histaminergic effect centered in the tuberomammillary nucleus

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9
Q

List the benzodiazepines used in the treatment of insomnia.

A 
Estazolam 
Flurazepam
Quazepam
Temazepam
Triazolam
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10
Q

Which benzodiazepine is known for its short half-life?

A

estazolam

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11
Q

True or false: all benzodiazepines bind to the GABA receptor at DISTINCT sites.

A

TRUE

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12
Q

Which alpha-subunits do benzodiazepines bind to on the GABA receptor?

A

BZ-1
BZ-2
BZ-3

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13
Q

What is the role of BZ-1 alpha subunit?

A

sedation

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14
Q

What is the role of BZ-2 alpha subunit?

A

anxiolysis

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15
Q

What is the role of BZ-3 alpha subunit?

A

myorelaxation and anticonvulsant

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16
Q

List the benzodiazepine receptor agonists used in the treatment of insomnia.

A

Zolpidem
Zaleplon
Eczopiclone

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17
Q

Which alpha subunits do benzodiazepine receptor agonists bind to?

A

BZ-1

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18
Q

What is interesting about the pharmacokinetic parameters of benzodiazepines and benzodiazepine receptor agonists?

A

Allosteric modulators, so left-shift in the dose response curve to endogenous GABA. Have a “ceiling effect”.

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19
Q

True or false: elimination half-life of benzodiazepines have a close relation to the time course of pharmacological effect.

A

FALSE: Formation of active metabolites makes it where the elimination half-life of a parent drug may have little relation to the time course of pharmacological effect

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20
Q

Which drugs are offered with a “quick release, slow release” co-formulation?

A

benzodiazepine receptor agonists

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21
Q

Which drug for insomnia has a rapid action with sublingual and oral spray?

A

zolpidem

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22
Q

Which drug for insomnia has sex-related differences in metabolism? (women slower than men)

A

zolpidem (REDUCE DOSE OF ZOLPIDEM in WOMEN due to increased risk of next-day impairment)

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23
Q

What is ramelteon?

A

melatonin receptor agonist

24
Q

What receptors does ramelteon bind to?

A

MT1 and MT2 (GPCRs)

25
Q

What does binding of ramelteon to MT1 do?

A

Binding to MT1 attenuates suprachiasmatic nucleus activity and induces sleep

26
Q

What does binding of ramelteon to MT2 do?

A

MT2 binding maintains circadian rhythm.

27
Q

How is ramelteon metabolized?

A

CYPS in the liver

28
Q

List the antidepressants used to treat insomnia.

A

Doxepin
Mirtazapine
Trazodone

29
Q

MOA: M block, NE reuptake block, 5-HT reuptake block. Primarily antihistamine at low doses

A

Doxepin

30
Q

MOA: 5-HT reuptake block

A

trazodone

31
Q

MOA: Significant alpha-2 antagonism reinforcing NE and 5-HT release

A

mirtazapine

32
Q

List the 1st generation antihistamines used in the treatment of insomnia.

A

Diphenhydramine

Doxylamine

33
Q

MOA of 1st generation antihistamines in treatment of insomnia.

A

H1 antagonism and anticholinergic effects

34
Q

What is Suvorexant?

A

it was an orexin receptor antagonist (that gave problems with next-day sedation so it was rejected by the FDA)

35
Q

What are the major FDA concerns with drugs to treat insomnia?

A
  • Persistent CNS-debilitating effects the day after consuming the drug
  • Unrecognized physical activity at night
  • Suicidal Ideation
  • Narcolepsy-associated events
36
Q

List the benzodiazepine that is NOT CYP metabolized.

A

Temazepam

37
Q

List the benzodiazepines that are CYP3A4 metabolized.

A

Estazolam
Flurazepam
Triazolam

38
Q

List the benzodiazepine that is CYP 2B6>3A4.

A

Quazepam

39
Q

What drug should be used with caution in Asians due to some CYP ethnic variabilities?

A

Zaleplon

40
Q

What is the most widely prescribed hypnotic in USA and the only drug approved for middle-of the night awakening?

A

Zolpidem

41
Q

What drug class is absolutely contraindicated in pregnancy (CAT X)?

A

Benzodiazepines

42
Q

What benzodiazepines do you have to worry about accumulation with?

A

Flurazepam

Quazepam

43
Q

Which benzodiazepine undergoes rapid inactivation?

A

Triazolam

44
Q

What drugs should be used with caution in hepatic disease, COPD, depression, driving, and closed angle glaucoma?

A

Benzodiazepines

Benzodiazepine receptor agonists

45
Q

What drug types do Benzodiazepines and Benzodiazepine receptor agonists have reactions with?

A

CNS drugs

CYP-metabolized drugs

46
Q

TOXICITY: sedation, cognitive impairment, rebound insomnia (especially with short/intermediate-acting dugs) and can lead to physical dependence and withdrawal (with severe ventilatory impairment*)

A

Benzodiazepines

Benzodiazepine receptor agonists

47
Q

What is the CYP specificity of Ramelteon

A

metabolized by 1A2>2C9 and 3A4

48
Q

TOXICITY: SEDATION major; suicidal ideation; psychotic episodes

A

Antidepressants

49
Q

TOXICITY: Few AEs (HA, somnolence, nausea, insomnia, and nasopharyngitis and URTI with long-term use)

A

ramelteon

50
Q

True or false: remelteon is not a scheduled drug, so there is NO abuse potential or respiratory depression.

A

TRUE

51
Q

What are some side effects seen with 1st generation antihistamines?

A

Sedation and xerostomia, blurred vision, urinary retention, increased intraocular pressure.

52
Q

What is the only way in which benzodiazepines can be lethal?

A

Only lethal when consumed with quantities of alcohol

53
Q

Which drug class should be used with caution in the elderly and those with narrow-angle glaucoma?

A

1st generation antihistamines

54
Q

Which drug class should be used with caution in those with pre-existing suicidal thoughts or psychotic disorders?

A

antidepressants

55
Q

In which drug class does rapid tolerance develop?

A

1st generation antihistamines

56
Q

Which drug is used to reverse the effect of BNZ and BzRAs?

A

Flumazenil (GABA inhibitor)

57
Q

What are the potential side effects of flumazenil?

A

seizures and symptoms of withdrawal as well as dysphoria, agitation, and possible increased adverse effects due to the abrupt awakening

Neuro 2 (11 decks)

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