Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharm: Psych > 2.17: Sedatives > Flashcards

2.17: Sedatives Flashcards

You may prefer our related Brainscape-certified flashcards:
Psychology 101 flashcards GRE® Psychology flashcards
1
Q

What are the clinical uses of sedative hypnotics?

A
  1. Insomnia
  2. Anxiety
  3. Alcohol withdrawal
  4. Anticonvulsants
  5. Adjust to anesthesia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is the effect of sedative hypnotics dependant on?

A
  • Dose dependent leading to increased awareness and arousability
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

How do the benzos differ from older sedative hypnotics?

A

Their effect tapers off as doses increase leading to them being less likely to cause coma or death

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

Which sedative hypnotics target GABA-a receptors?

A
  1. Benzos
  2. Non benzo agonists:
  3. Barbiturates
  4. Ethanol
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Characteristics of GABA-a receptors?

A
  • Ionotropic receptors
  • Activation by gaba leads to increased Cl channel opening
  • This causes inhibitory postsynaptic potentials decreasing neuronal firing
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Which receptor do sedative hypnotics target?

A

Only GABA-a

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Characteristics of GABA-b receptors? Where are the found? What are their effects in each location?

A

“Metabotropic G protein linked receptors”

  1. Presynaptic regulating release of:
    a. GABA from GABAergic neurons: “homoreceptors”
    b. Other NTs: “heteroreceptors”
  2. Post synaptic:
    a. Receptor activation produces membrane hyperpolarization
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Common GABA-a receptor subtype composition?

A
  • 2 alpha subunits: determines receptor subtype and ability to be modulated by respected drugs
  • 2 beta subunits
  • 1 gamma subunit
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What can BZ1 subtype GABA-a receptors bind?

A
  1. Benzodiazepines
  2. Imidazopyridines
  3. Pyrrolopyrazines
  4. Flumazenil: agonist
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What can BZ2 subtype GABA-a receptors bind?

A
  1. Benzodiazepines

2. Flumazenil: agonist

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

Which are the BZ1 selective drugs?

A
  1. Imidazopyridines

2. Pyrrolopyrazines

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

Characteristics of the alpha / beta interface?

A
  • 2 sites on each receptor

- GABA binds here

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

Characteristics of the alpha / gamma interface?

A
  • 1 site per receptor
  • GABA is necessary for binding of:
    1. Benzodiazepines
    2. Imidazopyridines
    3. Pyrrolopyrazines
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What drug is a GABA-a agonist?

A

Flumazenil

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

Which categories of drugs modulate GABA-a at site other than BZ1/2?

A
  1. Barbiturates
  2. Ethanol
  3. Neuroactive steroids
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

How do benzos work?

A
  • Bind BZ1/2 sites on GABA-a receptors: 90%
  • Are positive allosteric modulators of GABA-a function
  • GABA must be bound four opening of Cl channel
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

How do non-benzo agonists work?

A
  • Bind BZ1 sites on GABA-a receptors: 60%
  • Are positive allosteric modulators of GABA-a function
  • GABA must be bound four opening of Cl channel
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Which are the Pyrrolopyrazines?

A
  1. Eszopiclone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Which are the Imidazopyridines?

A
  1. Zolpidem

2. Zaleplon

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

What is the mechanism for positive allosteric modulation of BZ1/2?

A
  • Binding of benzo increases receptor affinity for GABA
  • Increases the frequency of Cl channel opening
  • Leads to inhibitory postsynaptic potential and decreased neuron firing
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

How do the inverse agonists work?

A
  • GABAs presence is necessary
  • Negative allosteric modulators of GABA receptor function
  • Decrease Cl channel opening increasing neuron firing
  • Lead to anxiety, seizure, or blockage of benzo effects
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are the Inverse agonists?

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

How does Flumazenil work?

A
  • On its own has no effect
  • Will block effect of drugs with affinity for BZ1/2
  • Will NOT antagonize GABA agonists, barbiturates or alcohol
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Clinical indication for flumazenil?

A
  1. Benzo OD

2. Reverse Benzo sedation after surgical procedure

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Characteristics of barbiturate effects on GABA-a receptors?

A
  • Bind sites distinct from BZ sites
  • No specificity for certain type of GABA-a receptor
  • Increase DURATION of Cl channel opening
  • Presence of GABA is necessary
  • Cause opening of Cl channel in absence of GABA at high dose
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Difference in the impact Benzos and barbiturates have on GABA-a receptor?

A

Benzos: increase frequency of opening
Barbs: increase duration of Cl channel opening

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

What potentiates impact of barbiturates?

A

Ethanol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Characteristics of neuroactive steroid effects on GABA-a receptors?

A
  • Bind sites distinct from BZ sites, also on receptors w/o BZ
  • Facilitate or attenuate GABAergic transmission depending on structure
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Ethanol’s impact on GABA receptors?

A

Effects similar to benzos:

  1. Sedation
  2. Anxiolytic
  3. CNS depression
  4. Potentiation of other GABA drugs
30
Q

What do the benzodiazepines usually end in?

A 
"Am," "Lam," or "Pam"
Exceptions:
1. Chlordiazepoxide
2. Clorazepate
***Their metabolite is: desmethyldiazePAM
31
Q

Common uses of the benzos?

A
  1. Anxiety
  2. Sleep disorder
  3. Anticonvulsants
  4. ETHO withdrawal
32
Q

Benzons or barbiturates safer?

A

Benzos

33
Q

When can benzos be dangerous

A
  1. Underlying pulmonary illness

2. Taking other CNS medications

34
Q

Which benzos are lipid soluble?

A

All of them to varying extents

35
Q

Protein binding of benzos?

A

Highly protein bound

36
Q

Metabolism of benzos? What is the exception to this?

A

Most under to the following 2 steps:
Phase I: Microsomal oxidation by CYP 3A4 and 2C19
Phase II: Conjugation
**3 go directly to the second step: “LOT”
1. Lorazepam
2. Oxazepam
3. Temazepam

37
Q

Which benzos preferred in elderly and those with hepatic function?

A

“LOT”

  1. Lorazepam
  2. Oxazepam
  3. Temazepam
    - Bypass phase I metabolism and have short half lives so easier on the liver
38
Q

What is the concept of drug accumulation?

A
  • Drugs with longer half lives, will build up [] in the system as they are taking over time risking toxicity
39
Q

What is the impact of age on drug half life?

A

Drug half live will usually increase with age as liver function decreases

40
Q

Side effects of benzos?

A
  1. Drowsiness
  2. Ataxia
  3. Amnesia: good for surgical procedures
  4. Rage (rare)
41
Q

Which benzo is used as date rape drug?

A

Flunitrazepam / rohypnol

42
Q

Which effects of benzos can you develop tolerance to?

A
  • Can become tolerant to the sedative effects

- Cannot become tolerant to the anxiolytic effects

43
Q

What are symptoms of benzo withdrawal?

A
  1. Anxiety
  2. Insomnia
  3. Confusion / delirium
    * **Only seen in chronic use at high dose
44
Q

What to do when taking patient off benzo?

A
  • Taper dose by
45
Q

How is 1/2 life related to tolerance and dependance?

A

Lower 1/2 life, higher risk of dependence

46
Q

How is of time to onset of effects related to dependence?

A

Quicker time to onset, higher risk of dependence

47
Q

How is potency related to tolerance and dependance?

A

Greater potency, greater risk of addiction

48
Q

How is dose related to dependency?

A

Larger dose needed, greater risk of dependence

49
Q

How is length drug take related to dependency?

A

Greater length, greater risk

50
Q

Which are the BZ1 selective non-benzos drugs?

A
  1. Zolpidem
  2. Zaleplon
  3. Eszopiclone
51
Q

MOA of the BZ1 specific non-benzos?

A
  • Positive modulators of GABA-a receptor function
52
Q

Risk of dependence for BZ1 specific non-benzos?

A
  • Lower than benzos
53
Q

OD of BZ1 specific non-benzos?

A
  • NO dangerous CNS depression UNLESS in taken in combo with other CNS depressants
54
Q

What can be given in OD of BZ1 specific non-benzos?

A

Flumazenil will block effect at BZ1

55
Q

Unique side effects of BZ1 specific non-benzos?

A
  1. Rebound insomnia
  2. Anterograde amnesia
  3. Sleep Driving
  4. Sleep eating
56
Q

Which BZ1 specific non-benzos has longest 1/2 life?

A

Eszopiclone - 6 hrs.

57
Q

Metabolism of BZ1 specific non-benzos?

A

Phase I and II in liver

58
Q

What is a benefit of teh BZ1 specific non-benzos over benzos?

A

Shorter half lives give them give them less morning hangover effect

59
Q

Which BZ1 specific non-benzos has no impact on stages of Sleep?

A

Eszopiclone

***Also has longest half life of the group

60
Q

Which are the barbituates? Are they long or short acting?

A

All end in “AL”

  1. Phenobarbital: Long acting
  2. Methohexital: Short acting
  3. Thiopental: Short acting
61
Q

MOA of the barbituates?

A
  1. Bind at site other than BZ1/2 on GABA-a receptor: likely lipophilic beta sub unit
  2. Not specific for GABA-a subtypes as it is not binding BZs
62
Q

Impact of barbituates at high and low dose?

A

LOW: increased duration of Cl channel opening in presence of GABA
HIGH: directly activate Cl channel, independent of GABA
***Low therapeutic index: lethal dose

63
Q

Indication for short acting barbituates?

A

Induction of anesthesia

64
Q

Indication for long acting barbituates?

A

Treatment of epilepsy

65
Q

Side effects of barbituates?

A
  1. Respiratory depressant: potentiated by alcohol
  2. Dependence
  3. Withdrawal: can be deadly
66
Q

What should not be taken with barbiturates?

A

Alcohol

67
Q

Benzos or barbs have more dangerous CNS effects?

A

Barbiturates

68
Q

Impact of barbituates on the liver?

A

Inducers of P450 which metabolize the drug leading to a larger dose being needed to achieve same impact

69
Q

MOA of Ramelteon?

A
  • Melatonin agonist
  • Selectively binds to MT1/2 melatonin receptors;
  • *Higher affinity than melatonin
  • No affinity for BZ receptors
70
Q

Kinetics of Ramelteon?

A
  • Moderate protein binding
  • Large Vd
  • Extensive first pass metabolism via CYP
  • Short half life
71
Q

Major benefit of Ramelteon?

A

No physical dependance of abuse potential

Pharm: Psych (7 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions