Exam #02 - Anxiolytics/Sedatives-Hypnotics Flashcards Preview

Pharmacology 2 > Exam #02 - Anxiolytics/Sedatives-Hypnotics > Flashcards

Flashcards in Exam #02 - Anxiolytics/Sedatives-Hypnotics Deck (25):
1

Which of the following drugs are more specific (in the treatment) to anxiety with fewer AE's?

A. Diazepam
B. Selegiline
C. Phenytoin
D. Phenobarbital
E. None of the above

(A)

Diazepam is a BZD which is more selective and has fewer AE, especially compared to Phenobarbital which is a barbiturate

Phenytoin is an anti-epileptic drug, Selegiline is a MOA-B inhibitor used in the Tx of PD

2

Which of the following statements is/are false?

A.Normal anxiety normally resolves w/o medication
B.Newer anxiolytics are more selective with less AE's
C. Benzodiazepines margin of safety is greater than barbiturates
D. Benzodiazepines increase the duration of GABAa receptor Cl- channel openings
E. Benzodiazepines may have anxiolytic effects on 5-HT systems

(D)

MOA
Benzodiazepines bind to the GABAa receptor complex (allosteric modulator), increasing the FREQUENCY of GABAa receptor Cl- channel opening enhancing Cl- influx

3

All of the following are examples of 'clinical' anxiety except?

A. panic attacks
B. phobias
C. OCD
D. PTSD
E. stress

(E) stress

4

True or False - 10% of the general population have clinically significant anxiety?

True

5

Clinical anxiety is the result of a biochemical change?

A. Yes
B. No
C. Not enough info

(C) not enough info

It is not understood whether an endogenous change causes something like OCD, phobia, or panic attacks OR OCD, phobia or panic attacks cause the endogenous change

6

Which of the following are treatment options for clinical anxiety?

A. psychotherapeutic
B. cognitive
C. behavioral
D. pharmacologic
E. All of the above

(E) all of the above

7

Pharmacologic treatment of clinical anxiety:

A. Typically used for acute attacks
B. treated chronically for 4-8 weeks
C. stopped and switched to alternate therapy if unsuccessful after 4-8 weeks
D. B & C are correct
E. None of the above

(D)

pharmacologic treatment of clinical anxiety is NOT typically used for acute attacks.

They ARE used chronically for ONLY 4-8 weeks and if they don't have the desired effect, they are stopped and patient is treated with a different treatment option like behavioral or psychotherapeutic

8

Why did benzodiazepines replace barbiturates in the 1960's? (3 reasons)

1. more selective
2. less AE's
3. less dependence potential

9

Which of the following regarding benzodiazepines is/are true?

A. BZD bind to their own BZD site on GABAa complex
B. BZD has NO effect of its own on GABAa receptor complex
C. BZD overdose antidote is flumazenil
D. BZD antagonist inhibits GABA
E. A, B, & C are correct

(E)

BZD bind to their own specific receptor site on GABAa receptor complex. When BZD bind there, they allosterically modulate the GABAa receptor complex allowing GABA, the inhibitory NT, to bind more effectively, thereby increasing chloride ion influx and decreasing neuronal excitability

A. BZD bind to their own BZD site on GABAa complex

B. BZD has NO effect of its own on GABAa receptor complex - meaning it needs GABA in order for its effects to occur (effects being an increase amount of Cl- influx)

C. BZD overdose antidote is flumazenil (antagonist) - Flumazenil blocks the BZD receptor site, NOT the GABA receptor site

D. BZD antagonist inhibits GABA -FALSE - BZD antagonist has NO effect on GABA. BZD antagonist binds to GABAa receptor complex at a completely different site than GABA

10

True or False - BZD's have a high TI?

True

Compared with barbiturates, BZD's do not have the degree of AE's such as:

CNS depression, decreased psychomotor function, daytime sedation, drug interactions, respiratory depression, effects on REM sleep, liver enzyme induction

11

Which of the following statements is/are false?

A. Both BZD and barbiturates bind to separate sites on the GABAa receptor complex
B. All CNS neurons and glial cells are GABA sensitive
C. GABA is primarily synthesized from an excitatory NT (glutamate)
D. BZD's are mainly metabolized by liver microsomal enzymes while Zolpidem and Buspirone are excreted renally unchanged

(D)

Barbiturates, BZD's, and miscellaneous anxiolytics are all metabolized in the liver

Miscellaneous anxiolytics (Buspirone, Zaleplon, Zolpidem, Rozerem) are specifically metabolized by Aldehyde Oxidase

12

Which of the following statements regarding the GABAa receptor is/are false?

A. GABAa receptor is pentameric
B. An inverse agonist at the GABAa receptor results in less inhibitory post-synaptic potential
C. GABAa receptor is ionotropic
D. BZD and barbiturate binding sites on the GABAa receptor are separate from GABA receptor and located extracellularly
E. All of the above are true

(D)

BZD and barbiturate binding sites on the GABAa receptor are separate from GABA receptor and located extracellularly

It's true that BZD and barbiturate binding sites are separate sites from the GABA receptor, however ONLY the BZD binding site is located extracellularly while the barbiturate binding site is within the plasma membrane on the GABAa receptor complex

13

Barbiturates increase the __________ of GABAa receptor Cl- channel opening?

A. Frequency
B. Duration
C. None of the above

(B)

Barbiturates increase the DURATION of GABAa receptor Cl- channel openings while BZD increase the FREQUENCY of Cl- channel openings

14

All of the following statements are true except?

A. Most BZD are readily absorbed from the GI tract
B. Metabolism of BZD often leads to active metabolites
C. BZD are lipid soluble
D. Most BZD readily pass into placenta
E. BZD have no abuse potential

(E)

BZD have no abuse potentail - FALSE

15

Why should you use precaution with administering BZD to elderly patients?

BZD are metabolized in the liver and elderly patients often have diminished liver function.

16

True of False - Antergrade amnesia AE is associated more with BZD's while withdrawal symptoms are more associated with barbiturates?

True

Anterograde amnesia - the inability to create new memories

17

Give the trade names for the following drugs for Insomnia. Also, indicate which enzyme each is metabolized by:

Zolpidem
Zaleplon
Eszopiclone
Ramelteon
Doxepin


Zolpidem (Ambien ®) - aldehyde oxidase
Zaleplon (Sonata ®) - aldehyde oxidase
Eszopiclone (Lunesta®) - CYP3A4
Ramelteon (Rozerem ®) - CYP1A2
Doxepin (Silenor ®) - CYP2C19 & CYP2D6

18

Which drug for insomnia is approved for long term use?

Eszopiclone (Lunesta)

19

Which drug for insomnia binds to melatonin receptors?

Ramelteon (Rozerem)

20

Which drug for insomnia is an H1 antagonist?

Doxepin (Silenor)

21

True or False - Lunesta is in a different chemical class than BZD and Z drugs(Zolpidem and Zaleplon)?

True

22

True or False - Ambien and Sonata are in the same chemical class as BZD and bind to BZD receptor having similar MOA?

False - Zolpidem (Ambien) and Zaleplon (Sonata) are in a DIFFERENT chemical class than BZD, however they do bind to BZD receptor and have a similar MOA

23

Which drug for insomnia is effective for up to 1 year?

Ramelteon (Rozerem)

24

All of the following BZD's are prodrugs to the active metabolite Oxazepam, except:

A. Prazepam
B. Alprazolam
C. Diazepam
D. Triazolam
E. Both B & D

(E)

Alprazolam and Triazolam are NOT prodrugs and have no active metabolites

25

All of the following BZD's are prodrugs to the active metabolite Oxazepam, except:

A. Flurazepam
B. Chlordiazepoxide
C. Lorazepam
D. Only A
E. A & C

(E)

Flurazepam and Lorazepam are NOT prodrugs and have no active metabolites