Anxiolytics & Hypnotics Flashcards Preview

Pharmacology Block 2 > Anxiolytics & Hypnotics > Flashcards

Flashcards in Anxiolytics & Hypnotics Deck (49)
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1

Benzodiazepines

Potentiate the effect of GABA at Cl- ion channels

2

Diazepam

-A BZD that is a pos allosteric modulator of GABA A Rs

3

Propranolol

Helps with performance anxiety

4

GABA shunt

Refers to alpha ketoglutarate from the Krebs Cycle, converted to glutamic acid by GABA-transaminase; then subsequently to GABA by glutamic acid decarboxylase (GAD). GABA is then metabolized to form succinic semialdehyde to succinic acid and returns to the Krebs Cycle.

5

Glutamine loop

Glutamine is formed as GABA is transaminated and converted to glutamine. The glutamine is reconverted to glutamate; then decarboxylated by neuronal GAD to GABA

6

What do BZD not do themselves?

open the GABA Cl- channel

7

The GABA site of the GABA R is distinct from

the BDZ site and encompasses alpha-1 and beta-2 subunits

8

Flumazenil

BZD antag

9

Barbiturates

-Bind to a distinct subunit combination on the GABA receptor
-At high concentrations can open the channel on their own (without GABA).

10

BZD and hepatic induction

Benzodiazepines do not induce hepatic microsomal enzymes

11

Diazepam uses

anxiety, insomnia, pre-op, muscle relaxant

12

Chlordiazepoxide uses

alcohol detox

13

Flurazepam, Temazepam and Triazolam use

insomnia

14

Clonazepam

-Panic
-Anxiety
-Seizure

15

Alprazolam

-Short acting BZD
-Panic
-Anxiety
-First line treatment for panic disorder withSSRI

16

Lorazepam

-Short acting BZD
-Anxiety
-Alcohol related seizure

17

Adverse effects of BDZ

-Sedation
-Tolerance
-Physical dependence
-Self-admin

18

Toxicity of BZD

-Impaired judgment
-Slurred speech
-Incoordination
-Stupor
-Respiratory depression
-Death

19

Non-BDZ

-Anxiolytic
-Buspirone (5-HT1A R partial agonist)

20

First line treatment for all anxiety disorders

SSRI + BZD
--provides early coverage

21

Cognitive behavioral therapy (CBT)

Often used in conjunctive with SSRIs for anxiety

22

When do we see severe respiratory depression

When BZD are combined with other sedatives/CNS depressants (like alcohol)

23

GAD first line treatment

SSRI, usually venlafaxine, paroxetine or escitalopram

24

Panic disorder first line treatment

SSRI + benzodiazepine for immediate action (alprazolam)

25

PTSF (post traumatic stress disorder) first line treatment

SSRI, usually paroxetine or sertraline

26

Which BZD are used for sleep?

Estazolam, flurazepam, quazepam, temazepam, triazolam

27

Which drugs are typically used for sleep?

Eszoiclone, hydroxyzine, zolpidem, zaleplon, ramelteon

28

Describe the adult sleep cycle

Duration of about 90 min; includes NREM and REM sleep

29

Melatonin

produced in the pineal gland at night

30

Hypnotics

Produce drowsiness and promote the onset and maintenance of sleep

31

What are the symptoms of insomnia?

Difficulty falling asleep, frequent wakenings, poor quality of sleep

32

What is sleep deprivation?

Inadequate opportunity for sleep; sleep itself is relatively normal

33

What is insomnia disorder?

Insomnia complaint and significant daytime impairment

34

Short acting BZDs

Alprazolam, triazolam, lorazepam, oxazepam

35

Long acting BZDs

Flurazepam, clorazepate, prazepam

36

Doxepin

-TCA
-low dose mechanism for insomnia is histamine H1

37

Non-BZD GABA A agonists

Eszopiclone, zolpidem, zaleplon

38

Ramelteon

Melatonin agonist for sleep

39

Which drugs are sedating antidepressants

Trazodone, mirtazapine, amyitriptyline

40

Zolpidem advantges

Shorten sleep latency, improve duration, can be used as needed, no negative effect on sleep architecture

41

Zolpidem disadvantages

4-6 hr effect, therefore not for middle of the night awakenings, associated with parasomnias

42

Traditional BZD disadvantages

Rebound insomnia, memory impairments, loss of coordination, abuse potential, not good for those with respiratory conditions

43

Barbiturates and GABA

Increase duration of channel opening, powerful CNS depression; low margin of safety

44

Diphenhydramine

Benadryl; sedating antihistamine

45

Anxiety, insomnia, pre-op, muscle

-Long acting BZD
-insomnia

46

Temazepam

-BDZ
-insomnia

47

Triazolam

-Short acting BZD
-Insomnia

48

Oxazepam

-Short acting BZD
-Alcohol detox

49

Zolpidem

-Non-BZD GABA A agonist
-insomnia