Lecture 11 - Anxiolytics & Hypnotics Flashcards Preview

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Flashcards in Lecture 11 - Anxiolytics & Hypnotics Deck (115)
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1

BZDs with long half-lives

chlordiazepoxide
diazepam
pazepam
clorazepate
flurazepam

2

BZDs with short half-lives

lorazepam and oxazepam (without active metabolites)

alprazolam and triazolam ( with active metabolites)

3

Flumazenil is a ?

BZD antagonist

4

Thiopental is a ?

barbiturate

5

Buspirone is a ?

other anxiolytic

6

Zopiclone is a ?

other hypnotic

7

Anxiolytics provide ?

-calming effects
-relief of anxiety

8

Hypnotics provide ?

-promote drowsiness
-promote onset and maintenance of sleep

9

Describe the chemical classification:
A

BZDs

10

Describe the chemical classification:
B

barbiturates

11

Describe the chemical classification:
C

others

12

What drugs are included in classification A: BZDs?

alprazolam
oxazepam
chlordiazepoxide
diazepam
lorazepam
triazolam

13

Describe the BZD basic foundation

benzene ring fused with a diazepine ring

14

What drugs are included in classification B: Barbiturates?

thiopental
pentobarbital

15

Describe the basic structure of barbiturates

all of the barbiturates are related to the structure of barbituric acid

16

What drugs are included in classification C: others

busprione
zopiclone
ethanol
chloral hydrate
antihistamines
ramelteon

17

What is the action site of pharmacological mechanisms of BZDs?

GABA-A receptor

18

Describe GABA-A receptor

-GABA is the primary inhibitory neurotransmitter in the brain

19

Describe GABA-A subunits

-2 alpha subunits
-2 beta subunits
-1 gamma subunit

20

Alpha subunit has 5 isoforms with alpha 1-5:
Describe them

alpha 1 = hypnotic
alpha 2-5 = sedation, psychomotor effect

21

GABA-A receptor = _____ channel

chloride

22

Describe the activation of GABA-A receptor

activation - chloride influx, hyperpolarizes neurons and decreases neuronal activity

23

How do BZDs work to interact with GABA-A receptors?

-BZDs bind to GABA-A receptors - enhance GABA actions and reduce excitability of neurons

-increases frequency of channel-opening events

-act as CNS depressants

24

Describe affinity of BZDs for GABA-B receptors

low affinity

25

How do barbiturates work to interact with GABA-A receptors?

-barbiturates bind to GABA-A receptors
-increases duration of channel-opening events
-GABA-mimetic at high concentration
-inhibit glutamate AMPA receptor

26

Describe general concept of pharmacokinetics

(what the body does to the drug)

absorption
distribution
metabolism
excretion

see slide 11

27

Define: onset

the time required for drug to be effective after administration

28

What does lipophilicity of drugs affect?

onset of action

29

More lipophilic = ?

more rapid onset of action

30

Define: duration

the amount of time that a measurable drug effect persists