PDA II Exam II Sharma 1.0

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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/ maintenance 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 this rxn

GAD

8

GAD activity require what cofactor

Pyridoxal Phosphate PLP

9

PLP is generated from what vitamin

B6

10

PLP requires what for activation

Zinc

11

Deficiency of zinc of defect in PLP can cause

Seizures

12

What kind of rec are GABAA rec

Ligated-gated Cl- ion channels

13

What kinds to GABAA rec

GABA

BZs

Barbiturates

14

What is a GABAB agonist

Baclofen

15

The major isoform of the GABAA rec has what subunits

(2) a1

(2) b2

(1) y2

16

Where are the (2) binding site for GABA located

Between a1 and b2

17

Where are the binding sites for BZs located

Between a1 and y2

18

Where is the binding site for Barbiturates located

On a1

19

a1 subunits mediate

Sedation

Amnesia

Ataxic

20

a2 and a3 subunits mediate

BZ anxiolytic action

Muscle Relaxation

21

a5 subunits mediate

BZ Memory impairment

22

What effect do BZs have on GABA rec

Increase synaptic inhibition

23

What does this do

Enhances hyperpolarization

24

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

Increase the frequency of Cl- channel openings

Enhance Cl- conductance

25

What are GABAA BZ site agonists

All BZs

26

What are GABAA agonists

Zolpidem

Zaleplon

Eszopiclone

27

What is their function

Enhance membrane hyperpolarization similar to BZs

28

What do they no do

Cause:

Anxiolytic effect

Muscle relaxant effect

Amnesia effect

29

What are BZ antagonists

Flumazenil

30

What is the function of Flumazenil

Block BZ action

Block Zolpidem, Zaleplon, Eszopilone action

31

What doesn't Flumazenil block

Barbiturates

Meprobamate

Ethanol

32

What are the inverse agonists

B-carboline

33

What is the function of the inverse agonists

Blocks BZ

34

What does it cause

Anxiety

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 this mean

As the dose increases CNS depression increases

38

What is the MOA of barbiturates on GABAA

Enhances membrane hyperpolarization

39

How does this occur

Increasing the duration that the GABA-gated Cl- channels are opened

40

Describe the selectivity of Barbiturates

Less selective than BZs

41

Describe the absorption properties of BZs and Barbs

Lipophilic

42

Barbs and BZs are rapidly absorbed through which ROA

Oral

43

What are the rapidly absorbed BZs

Diazepam

Clorazepate

44

What kind of drug is Clorazepate

Prodrug

45

What is its active form

Desmethyldiazepam

46

What is the significance of Lorazepam

...

47

Explain the distribution properties

Rapid onset

48

What barrier do all sedative-hypnotics cross

BBB and Placental barrier

49

What happens when this occurs

Depression of neonatal vita functions

50

What enzyme aids BZ metabolism

CYP3A4

51

In what phase

Phase 1

52

What is phase 2

Conjugation

53

What are factors that affect biodisposition

In geriatric patients elimination half life is prolonged

54

What is dose dependent anterograde amnesia

Inability to recall events that occurred during the drugs duration of action

55

When does this occur

During sedation

56

What side effects are associated with the frequent use of BZs

Rebound REM sleep

57

What drug causes this

Triazolam and drugs with short duration of action

58

Do newer drugs affect rebound REM

No

59

Rebound insomnia occurs when what drugs at high doses

Zolpidem

Zaleplon

60

Drugs when very short half lives for hypnotic effects may lead to

Withdrawal symptoms between doses

61

What is Flumazenil

A BZ competitive inhibitor with high affinity

62

What is its use

Reversing CNS depression effects of BZ OD

Help recovery in anesthetic and diagnostic procedures

63

Explain the onset and DOA for Flumazenil

Rapid onset and short half life

64

What is its half life

0.7- 1.3 hours

65

What are adverse effects of Flumazenil

Agitation

Confusion

Dizziness

Nausea

66

What are agents that do not act through GABA-BZ mechanisms

Ramelteon

Buspirone

67

What rec do they act on

Melatonin (MT1 and MT2)

68

Explain the ROA and DOA

Rapidly absorbed via oral

Extensive first-pass metabolism (2-5 hours)

69

What biotransformation enzymes are involved

CYP1A2 (main)

CYP2C9

70

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

Rifampin

71

Is Ramelteon a controlled substance

No

72

What rec does Buspirone not interact with

BZ sites and GABAA rec

73

They are partial agonists on which rec

5-TH 1A

74

What are their function

Inhibit the firing rate of 5-TH containing neurons

75

Where does this take place

Dorsal Raphe

76

What are the overall effects

5-TH, NE, DA

5-TH is suppressed

NE and DA are enhanced

77

What is the major petabolite

1-(2-Pyrimidyl)-piperazine (1-PP)

78

Explain the absorption of Buspirone

Rapid via oral

79

How long does it take for it to be eliminated

Half life is 2-4 hours

80

What does rifampin do to Buspirone

Decreases its half life

81

What is the function of rifmapin

CYP450 inducer