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PHRM 845 > 4.4 Pathophysiology of anxiety and sleep disorders > Flashcards

4.4 Pathophysiology of anxiety and sleep disorders Flashcards

1
Q

What are the stages of sleep?

A
  • Wakefulness
  • Non-rapid eye movement (NREM) slow wave sleep
  • Rapid eye movement (REM) sleep
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2
Q

What are the stages of NREM sleep?

A
  • Stage 1 (dozing)
  • Stage 2 (unequivocal sleep)
  • Stage 3 (voltage increase, frequency decrease)
  • Stage 4 (delta waves)
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3
Q

What is REM sleep similar to?

A

Similar to being awake in EEG

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4
Q

What are the factors that regulate sleep?

A
  • Age
  • Sleep hx
  • Drug ingestion
  • Circadian rhythms
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5
Q

Out of all the neurotransmitters that are regulators of sleep, which one is the main target for current meds?

A

GABA

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6
Q

What neuromodulators are regulators of sleep?

A
  • GH
  • Prolactin
  • Cortisol
  • Melatonin
  • Endogenous peptides
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7
Q

Describe the GABAa receptor’s structure.

A

Pentameric structure comprised of 5 subunits from several polypeptide classes.

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8
Q

What can the GABAa receptor also be known as (hint: what ion does it transport)?

A

The Cl ion channel complex

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9
Q

What sedative hypnotic targets the orthosteric site of the GABAa receptor/Cl ion channel complex?

A

GABA on the alpha1 and beta2

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10
Q

What sedative hypnotics target the allosteric sites of the GABAa receptor/Cl ion channel complex?

A
  • Benzodiazepine on BZD receptor (alpha1 and gamma2)
  • Barbiturate
  • Ethanol
  • Glucocorticoid
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11
Q

What sedative hypnotic target the channel pore of the GABAa receptor/Cl ion channel complex?

A

Picrotoxin

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12
Q

What does picrotoxin do on the GABAa receptor?

A

GABA channel blockers

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13
Q

What do benzodiazepines do at the BZD receptor?

A
  • Facilitate GABA action
  • Increase frequency of channel opening
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14
Q

What do benzodiazepines require to function at the BZD receptor?

A

Requires intact GABA system (internal safety system)

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15
Q

What non-benzos (z-hypnotics) act on the BZD receptor (BZ1)?

A
  • Zolpidem (ambien)
  • Zaleplon (sonata)
  • Eszopiclone (lunesta)
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16
Q

What specific BZD receptor do non-benzos (z-hypnotics) act on?

A

BZ1 receptors of alpha1

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17
Q

What drug class are inverse BZD agonists?

A

B carbolines

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18
Q

What do barbiturates do on the GABAa receptor?

A
  • Increase the duration of channel opening
  • Direct effects on GABAa (w high doses)
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19
Q

What does alcohol do on the GABAa receptor?

A

Enhances actions of GABA at GABAa receptor

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20
Q

What is the SAR of benzodiazepines at the 1 position?

A

Alkylation = source of active metabolites

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21
Q

What is the SAR of benzodiazepines at the 2 position?

A

NH2 or N(CH3)2 is active; oxo is active (ie valium)

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22
Q

What is the SAR of benzodiazepines at the 3 position?

A

3 position has decreased activity; 3-OH rapid excretion

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23
Q

What is the SAR of benzodiazepines at the 4 position?

A

4 nonoxide is active

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24
Q

What is the SAR of benzodiazepines at the 5 position?

A

Substitution on 5-phenyl has decreased activity

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25
Q

What is the SAR of benzodiazepines at the 7 position?

A

7 position has an electronegative group

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26
Q

Annealating what on benzodiazepines has what effect?

A

Annealating 1-2 bond w “electron rich” ring (triazole or imidazole) yields high affinity and decreased half-life

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27
Q

Which benzodiazepine has a long half life and what is its metabolism?

A

Diazepam

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28
Q

Which benzodiazepines have intermediate and rapid elimination rates?

A
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29
Q

What is the biotransformation pathway of benzodiazepines?

A
30
Q

What is the PK and use of chlordiazepoxide (librium)?

A
  • Slow elim rate, has active metabolites
  • 1st benzo, used as anxiolytic and for alcohol withdrawal
31
Q

What is the PK and use of diazepam (valium)?

A
  • Slow elim rate, has active metabolites
  • Use as anxiolytic, for alcohol withdrawal, and for tx of convulsive disorders (ie seizures)
32
Q

What is the PK and use of flurazepam (dalmane)?

A
  • Slow elim rate, has active metabolites
  • Use as hypnotic
33
Q

What is the PK and use of clorazepate (tranxene)?

A
  • Slow elim rate, has active metabolites
  • Use as anxiolytic, for alcohol withdrawal, tx of convulsive disorders
34
Q

What is the PK and use of quazepam (doral)?

A
  • Slow elim rate, has active metabolites
  • Use as hypnotic
35
Q

What is the PK and use of prazepam?

A
  • Slow elim rate, has active metabolites
  • Use as anxiolytic
36
Q

Which of the slow elim rate benzos is currently unavailable in the US?

A

Prazepam

37
Q

What is the PK and use of alprazolam (xanax)?

A
  • Intermediate elim rate
  • Use as anxiolytic and anesthetic
38
Q

What can occur w alprazolam (xanax)?

A

Withdrawal sxs can present if abrupt d/c occurs

39
Q

What is the PK and use of lorazepam (ativan)?

A
  • Intermediate elim rate
  • Use as anxiolytic and as hypnotic
40
Q

What is the PK and use of clonazepam (klonopin)?

A
  • Intermediate elim rate
  • Use as anticonvulsant
41
Q

What can occur w prolonged clonazepam (klonopin) use?

A

Tolerance may develop

42
Q

What is the PK and use of oxazepam (serax)?

A
  • Intermediate elim rate
  • Use as anxiolytic and for alcohol withdrawal
43
Q

What is the PK and use of temazepam (restoril)?

A
  • Intermediate elim rate
  • Use as short term hypnotic
44
Q

What is the PK and use of midazolam (versed)?

A
  • Rapid elim rate
  • Use as rapid anesthesia
45
Q

What is the PK and use of triazolam (halcion)?

A
  • Rapid elim rate
  • Used as short term hypnotic
46
Q

Which of the rapid elim rate benzos is not available anymore?

A

Triazolam (halcion), due to d/c

47
Q

What is an issue with slow elim rate benzos?

A

Can cause drowsiness and sedation

48
Q

In what pts are slow elim rate benzos useful in?

A

Useful in pts who “wake up”

49
Q

What are issues w intermediate elim rate benzos?

A
  • Rapid tolerance
  • Rebound insomnia
50
Q

In what pts are intermediate elim rate benzos useful in?

A
  • Preferable in pts w hepatic problems
  • Preferable in elderly pts
51
Q

What are general considerations of benzos?

A
  • Readily absorbed (can be delayed by food)
  • Increased lipid solubility will increase speed of delivery to brain
  • Redistribution to highly perfused tissue may decrease duration of action
  • Crosses placenta and detected in breast milk
52
Q

How does the pharmacological properties of benzos affect sleep physiology?

A
  • Reduce sleep latency
  • Increase total sleep time
  • Increase stage 2
  • Decrease REM
  • Decrease stage 3 and 4
  • Tolerance and rebound to delta and REM
53
Q

What are problems that could be caused from the pharmacological properties of benzos?

A
  • CV and respiratory depression (major issue when combined w other agents)
  • Anterograde amnesia
  • Unable to recall events that occurred
54
Q

What are SEs of benzos dependent on?

A

Dose dependent

55
Q

What are the SEs of benzos?

A
  • Sedation: confusion, ataxia, daytime sedation w longer acting agents
  • Weakness, headache, vertigo, nausea, paradoxical effects
56
Q

What is the abuse potential w benzos?

A
  • Possibly abuse potential, low vs barbiturates
57
Q

Which drug is a BZD antagonist and what is its function?

A

Flumazenil (romazicon)
- Tx of z-hypnotic overdose

58
Q

What is the initial dose of flumazenil?

A
  • 0.2 mg IV over 30 seconds
  • If desired consciousness is not obtained, increase to 0.3 mg IV over 30 secs
59
Q

What is the max cumulative dose of flumazenil?

A

3 mg (usual range 1-3 mg)

60
Q

What are SEs of flumazenil?

A
  • Induces convulsions, panic attacks (in pts who developed dependence)
  • Agitation, confusion
  • N/V
  • Headache
61
Q

What is the use of zolpidem (ambien)?

A

Short term tx of insomnia
- W difficulty of sleep onset
- Ambien CR for sleep maintenance

62
Q

What is the use of zaleplon (sonata)?

A
  • Short term tx of insomnia (7-10 days)
  • Rapid acting, rapidly elim
  • LIttle tolerance or dependence
63
Q

What is the use of eszopiclone (lunesta)?

A
  • Active enantiomer of zopiclone (50x greater affinity)
  • Tx of insomnia, approved for long term use
64
Q

How are z-hypnotics metabolized?

A

3A4 to some extent

65
Q

What are SEs of z-hypnotics?

A
  • Daytime drowsiness, dizziness, ataxia, N/V
  • Cause less negative effects on sleep patterns
  • FDA warning: sleep- driving, eating, sex
66
Q

Which barbiturates are long acting?

A
  • Phenobarbital (luminal)
  • Mephobarbital (mebaral)
67
Q

What are long acting barbiturates used as?

A

Anticonvulsants

68
Q

Which barbiturates are short to intermediate acting?

A
  • Amobarbital (amytal)
  • Butabarbital (butisol sodium)
  • Pentobarbital (nembutal)
  • Secobarbital (seconal)
  • Apropbarbital (alurate)
69
Q

What are short to intermediate acting barbiturates used as?

A

Sedative hypnotics

70
Q

Which barbiturates are ultra short acting?

A
  • Thiopental (pentothal)
  • Methohexital (brevital sodium)
  • Thiamylal (surital)
71
Q

What are ultra short acting barbiturates used as?

A

IV anesthetics

PHRM 845 (48 decks)

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