Pharmaclogy - Sedatives and Hypnotics Flashcards Preview

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Flashcards in Pharmaclogy - Sedatives and Hypnotics Deck (27):
1

What is a sedative?

Sedative = calming = anxiolytic effect (ideally with little effect on motor or mental functions)

2

What is a hypnotic?

Hypnotic = induce sleep
(more pronounced CNS depression than sedation; can be achieved with most sedative drugs simply by increasing dose)

3

MOA: Sedatives and Hypnotics

bind to some site on
GABA-A Receptor complex and potentiate GABA-mediated inhibition

4

GABA-A receptos is what kind of channel?

Chloride

5

Where do benzodiazepines bind to the GABA-A receptor?

binding site between α1 – γ2 sub-units

6

Where do barbituates bind to the GABA-A receptor?

bind to α or β sub-unit

7

Where does ethanol bind to the GABA-A receptor?

binds to α

8

T/F: Most benzodiazepines bind to both GABA-A receptor subtypes.

True

omega-1 and omega-2

9

What is the "ceiling effect" of benzos?

Increasing doses do not produce respiratory arrest/coma, whereas barbs and alcohol can induce full CNS depression

10

T/F: In high doses, barbituates and alcohol can directly open chloride channels, resulting in full CNS depression (total GABA rush)

True

11

Give the class:
Diazepam
Chlordiazepoxide
Lorazepam
Flurazepam
Alprazolam
Midazolam i.v. or i.m.
Triazolam

Benzodiazepines

12

Most benzos are metabolized how?

most benzos undergo microsomal oxidation (Phase I, via P450 system; particularly CYP3A4 and CYP2C19, with only modest P450 induction), and subsequent conjugation

13

What is the half life of flurazepam?

74 hours

14

Which benzo has the shortest half life?

Midazolam, 1.9 hrs

15

How is Zolpidem different from the more traditional benzodiazepines?

Zolpidem is specific for BDZ1 agonist (omega-1) whereas traditional benzos act on both omega 1 and 2.

This results in sedation w/o muscle relaxation/anticonvulsant activity

16

Use: Flumazenil

Benzo-antagonist
Use to reverse overdoses of benzos

17

What is the half life of phenobarbital?

4-5 days
less lipid soluble therefore slower onset

18

What is a barbituate commonly used to induce anesthesia due to its lipid solubulity and subsequent "fast on fast off" character?

Thiopental
known for its rapid redistribution

19

Does buspirone interact with the GABA-A complex?

No
Relieves anxiety w/o marked sedation

20

Use: alprazolam

Anti-anxiety;
shorter-acting benzo

21

Use: Lorazepam

Anti-anxietyl
Anti-convulsant
shorter-acting benzo

22

Use: Triazolam

Induce sleep;
very short-acting benzo

23

Use: Zolpidem

Induce sleep, a "pseudo-benzo"

24

What benzo is used in anesthesia to produce anterograde amnesia?

Midazolam
very short-acting benzo

25

Use: Diazepam

Anticonvulsant;
muscle relaxer

26

Use: Phenobarbital

Anticonvulsant

27

Name 3 adverse effects of the sedatives-hypnotics classes.

1. drowsiness & "hangover"

2. falls! – especially in the elderly - use caution – it is easy to produce confusion, sedation, unsteadiness with these drugs in the elderly

3. dose-related CNS depression
(additive CNS depression with more than one agent)

4. tolerance = common feature of sedative-hypnotic drug use -cross tolerance
-metabolic tolerance - induce enzymes (notably with barbiturates and alcohol)
-dynamic tolerance - decreased CNS responsiveness (receptor down-regulation)

5. psychologic & physiologic dependence is significant problem;

Note: abrupt withdrawal can be life-threatening, notably with non-benzo seditive-hypnotics (e.g. alcohol and barbiturates)

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