Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is REM sleep similar to?

A

Similar to being awake in EEG

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the factors that regulate sleep?

A
  • Age
  • Sleep hx
  • Drug ingestion
  • Circadian rhythms
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

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

A

GABA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What neuromodulators are regulators of sleep?

A
  • GH
  • Prolactin
  • Cortisol
  • Melatonin
  • Endogenous peptides
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Describe the GABAa receptor’s structure.

A

Pentameric structure comprised of 5 subunits from several polypeptide classes.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

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

A

The Cl ion channel complex

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

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

A

GABA on the alpha1 and beta2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

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

A

Picrotoxin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What does picrotoxin do on the GABAa receptor?

A

GABA channel blockers

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What do benzodiazepines do at the BZD receptor?

A
  • Facilitate GABA action
  • Increase frequency of channel opening
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What do benzodiazepines require to function at the BZD receptor?

A

Requires intact GABA system (internal safety system)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

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

A
  • Zolpidem (ambien)
  • Zaleplon (sonata)
  • Eszopiclone (lunesta)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

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

A

BZ1 receptors of alpha1

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What drug class are inverse BZD agonists?

A

B carbolines

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What do barbiturates do on the GABAa receptor?

A
  • Increase the duration of channel opening
  • Direct effects on GABAa (w high doses)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What does alcohol do on the GABAa receptor?

A

Enhances actions of GABA at GABAa receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What is the SAR of benzodiazepines at the 1 position?

A

Alkylation = source of active metabolites

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What is the SAR of benzodiazepines at the 3 position?

A

3 position has decreased activity; 3-OH rapid excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is the SAR of benzodiazepines at the 4 position?

A

4 nonoxide is active

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What is the SAR of benzodiazepines at the 5 position?

A

Substitution on 5-phenyl has decreased activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What is the SAR of benzodiazepines at the 7 position?
7 position has an electronegative group
26
Annealating what on benzodiazepines has what effect?
Annealating 1-2 bond w "electron rich" ring (triazole or imidazole) yields high affinity and decreased half-life
27
Which benzodiazepine has a long half life and what is its metabolism?
Diazepam
28
Which benzodiazepines have intermediate and rapid elimination rates?
29
What is the biotransformation pathway of benzodiazepines?
30
What is the PK and use of chlordiazepoxide (librium)?
- Slow elim rate, has active metabolites - 1st benzo, used as anxiolytic and for alcohol withdrawal
31
What is the PK and use of diazepam (valium)?
- Slow elim rate, has active metabolites - Use as anxiolytic, for alcohol withdrawal, and for tx of convulsive disorders (ie seizures)
32
What is the PK and use of flurazepam (dalmane)?
- Slow elim rate, has active metabolites - Use as hypnotic
33
What is the PK and use of clorazepate (tranxene)?
- Slow elim rate, has active metabolites - Use as anxiolytic, for alcohol withdrawal, tx of convulsive disorders
34
What is the PK and use of quazepam (doral)?
- Slow elim rate, has active metabolites - Use as hypnotic
35
What is the PK and use of prazepam?
- Slow elim rate, has active metabolites - Use as anxiolytic
36
Which of the slow elim rate benzos is currently unavailable in the US?
Prazepam
37
What is the PK and use of alprazolam (xanax)?
- Intermediate elim rate - Use as anxiolytic and anesthetic
38
What can occur w alprazolam (xanax)?
Withdrawal sxs can present if abrupt d/c occurs
39
What is the PK and use of lorazepam (ativan)?
- Intermediate elim rate - Use as anxiolytic and as hypnotic
40
What is the PK and use of clonazepam (klonopin)?
- Intermediate elim rate - Use as anticonvulsant
41
What can occur w prolonged clonazepam (klonopin) use?
Tolerance may develop
42
What is the PK and use of oxazepam (serax)?
- Intermediate elim rate - Use as anxiolytic and for alcohol withdrawal
43
What is the PK and use of temazepam (restoril)?
- Intermediate elim rate - Use as short term hypnotic
44
What is the PK and use of midazolam (versed)?
- Rapid elim rate - Use as rapid anesthesia
45
What is the PK and use of triazolam (halcion)?
- Rapid elim rate - Used as short term hypnotic
46
Which of the rapid elim rate benzos is not available anymore?
Triazolam (halcion), due to d/c
47
What is an issue with slow elim rate benzos?
Can cause drowsiness and sedation
48
In what pts are slow elim rate benzos useful in?
Useful in pts who "wake up"
49
What are issues w intermediate elim rate benzos?
- Rapid tolerance - Rebound insomnia
50
In what pts are intermediate elim rate benzos useful in?
- Preferable in pts w hepatic problems - Preferable in elderly pts
51
What are general considerations of benzos?
- 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
How does the pharmacological properties of benzos affect sleep physiology?
- 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
What are problems that could be caused from the pharmacological properties of benzos?
- CV and respiratory depression (major issue when combined w other agents) - Anterograde amnesia - Unable to recall events that occurred
54
What are SEs of benzos dependent on?
Dose dependent
55
What are the SEs of benzos?
- Sedation: confusion, ataxia, daytime sedation w longer acting agents - Weakness, headache, vertigo, nausea, paradoxical effects
56
What is the abuse potential w benzos?
- Possibly abuse potential, low vs barbiturates
57
Which drug is a BZD antagonist and what is its function?
Flumazenil (romazicon) - Tx of z-hypnotic overdose
58
What is the initial dose of flumazenil?
- 0.2 mg IV over 30 seconds - If desired consciousness is not obtained, increase to 0.3 mg IV over 30 secs
59
What is the max cumulative dose of flumazenil?
3 mg (usual range 1-3 mg)
60
What are SEs of flumazenil?
- Induces convulsions, panic attacks (in pts who developed dependence) - Agitation, confusion - N/V - Headache
61
What is the use of zolpidem (ambien)?
Short term tx of insomnia - W difficulty of sleep onset - Ambien CR for sleep maintenance
62
What is the use of zaleplon (sonata)?
- Short term tx of insomnia (7-10 days) - Rapid acting, rapidly elim - LIttle tolerance or dependence
63
What is the use of eszopiclone (lunesta)?
- Active enantiomer of zopiclone (50x greater affinity) - Tx of insomnia, approved for long term use
64
How are z-hypnotics metabolized?
3A4 to some extent
65
What are SEs of z-hypnotics?
- Daytime drowsiness, dizziness, ataxia, N/V - Cause less negative effects on sleep patterns - FDA warning: sleep- driving, eating, sex
66
Which barbiturates are long acting?
- Phenobarbital (luminal) - Mephobarbital (mebaral)
67
What are long acting barbiturates used as?
Anticonvulsants
68
Which barbiturates are short to intermediate acting?
- Amobarbital (amytal) - Butabarbital (butisol sodium) - Pentobarbital (nembutal) - Secobarbital (seconal) - Apropbarbital (alurate)
69
What are short to intermediate acting barbiturates used as?
Sedative hypnotics
70
Which barbiturates are ultra short acting?
- Thiopental (pentothal) - Methohexital (brevital sodium) - Thiamylal (surital)
71
What are ultra short acting barbiturates used as?
IV anesthetics

PHRM 845 (48 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions