PDA II Exam II [Dr. Sharma]

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1

What are anxiolytics?

Sedatives

2

What kind of effect do they have?

Calming effect

3

What effect does hypnotics have?

Drowsiness

Encourage the onset and maintenance of a state of sleep

4

What kind of NT is GABA?

Inhibitory

5

Neurons that secrete GABA are called...

GABAnergic

6

How is GABA synthesized?

Via the decarboxylation of Glutamate

7

What enzyme catalyzes the decarboxylation of Glutamate?

GAD (glutamate decarboxylase)

8

GAD (glutamate decarboxylase) activity requires what cofactor?

Pyridoxal Phosphate PLP

9

Pyridoxal Phosphate PLP is generated from what vitamin?

Vitamin B6

10

PLP requires what for activation?

Zinc

11

Deficiency of zinc of defect in PLP can cause....

Seizures

12

What is GABAA modulated by?

GABA

Benzodiazepines

Barbiturates

13

What kind of receptors are GABAA?

Ligated-gated Cl- ion channels

14

What binds to GABAA receptors?

GABA

BZs

Barbiturates

15

What is a GABAB agonist?

Baclofen

16

The major isoform of the GABAA receptor has what subunits?

Two α1 subunits

Two β2 subunits

One γ2 subunit

17

Where are the binding sites for GABA located?

Between α1 and β2

18

Where are the binding sites for BZs located?

Between α1 and γ2

19

Where is the binding site for Barbiturates located?

α1

20

What do α1 subunits mediate?

Sedation

Amnesia

Ataxic

21

What do α2 and α3 subunits mediate?

BZ anxiolytic action

Muscle Relaxation

22

What do α5 subunits mediate?

BZ Memory impairment

23

What effect do BZs have on GABA receptor?

Increases synaptic inhibition

24

What does increasing synaptic inhibition do?

Enhances hyperpolarization

25

How do BZ enhance GABAergic rec without directly activating the GABAA receptor?

Increase the frequency of Cl- channel openings

Enhance Cl- conductance

26

What are GABAA BZ site agonists?

All BZs

27

What are GABAA agonists?

Zolpidem

Zaleplon

Eszopiclone

28

What is the function of GABAA agonists?

Enhance membrane hyperpolarization similar to BZs

29

GABAA agonists does not cause....

Anxiolytic effect

Muscle relaxant effect

Amnesia effect

30

What are BZ antagonists?

Flumazenil

31

What is the function of Flumazenil?

Block BZ action

Block Zolpidem, Zaleplon, Eszopilone action

32

What doesn't Flumazenil block?

Barbiturates

Meprobamate

Ethanol

33

What are the inverse agonists of Flumazenil?

B-carboline

34

What is the function of the inverse agonists of Flumazenil? And what does it cause?

Blocks BZ;

Causes anxiety and seizures

35

Graded dose-dependent depression of the CNS is seen with....

BZs

Barbiturates

Ethanol

Newer agents

36

Older sedatives/ hypnotics such barbiturates have a....

Linear dose relationship

37

What does the linear dose relationship mean?

As the dose increases, CNS depression increases.

38

What is the MOA of barbiturates on GABAA and how does this occur?

Enhances membrane hyperpolarization by increasing the duration that the GABA-gated Cl- channels are opened

39

Compare the selectivity of barbiturates compared to BZs.

Barbiturates are less selective than BZs

40

Describe the absorption properties of BZs and Barbiturates.

Lipophilic

41

Barbiturates and BZs are rapidly absorbed through which route of absorption (ROA)?

Oral

42

BZs are classified based on duration of action. Name the long-acting drugs and its duration.

24-48 hours

Diazepam

Chlordiazepoxide

Flurazepam

Clonazepam

Clorazepate

43

BZs are classified based on duration of action. Name the medium-acting drugs and its duration.

24 hours

Nitrazepam

44

BZs are classified based on duration of action. Name the short-acting drugs and its duration.

12-18 hours

Alprazolam

Lorazepam

Oxazepam

Temazepam

45

BZs are classified based on duration of action. Name the ultrashort-acting drugs and its duration.

6 hours

Triazolam

Midazolam

46

What are the rapidly absorbed BZs?

Diazepam

Clorazepate

47

How does elimination half-life of diazepam affect elderly patients?

In geriatric patients, elimination half-life is prolonged.

48

What side effects are associated with the frequent use of BZs? What drug causes this?

Rebound REM sleep; Triazolam and drugs with short duration of action

49

True/False: Newer drugs affect rebound REM.

False

50

What kind of drug is Clorazepate?

Prodrug

51

How does Clorazepate produces its effect following oral administration?

It converts to its active form (desmethyldiazepam/nordiazepam) by acid hydrolysis in the stomach.

52

What barrier do all sedative-hypnotics cross?

BBB and Placental barrier

53

Drugs with very short half lives for hypnotic effects may lead to....

Withdrawal symptoms between doses

54

What is Flumazenil?

A BZ competitive inhibitor with high affinity

55

What is the use of Flumazenil?

Reversing CNS depression effects of BZ OD

Helps recovery in anesthetic and diagnostic procedures

56

Explain the onset and DOA for Flumazenil.

Rapid onset and short half life

57

What is the half-life of Flumazenil?

0.7-1.3 hours

58

List the adverse effects of Flumazenil.

Agitation

Confusion

Dizziness

Nausea

59

What agents do not act through GABA-BZ mechanisms?

Ramelteon

Buspirone

60

Explain the ROA and DOA of Ramelteon and Buspirone?

Rapidly absorbed orally

Undergoes extensive first-pass metabolism (2-5 hours)

61

What drug reduces the plasma levels of Ramelteon and its active metabolites?

Rifampin

62

What is the function of rifmapin?

CYP450 inducer

63

What receptor(s) does Buspirone not interact with?

BZ sites and GABAA

64

True/False: Buspirone causes more psychomotor impairment than BZs.

False; Buspirone causes less psychomotor impairment than BZs and does not affect driving skills.

65

True/False: Unlike BZs, elderly do not appear to be more sensitive to buspirone

True

66

True/False: Buspirone is used in generalized anxiety states but less effective in panic disorders.

True