L2 Anxiolytics

Question 1

What is the therapeutic rationale for anxiety disorders?

Answer 1

sedative, hypnotic and anxiolytic actions of antidepressants are closely-related - the same drug can have more than one action depending on dose:

• low dose -> anxiolytic and sedative effects
• higher doses -> hypnotic
• even higher doses -> can cause anesthesia, used for surgery

Question 2

Benzodiazepines: Diazepam

Answer 2

• used as anxiolytics/sedatives
• used as hypnotics
• used as pre-anesthetics
• may also have anti-convulsant effects

Question 3

Benzodiazepines: Lorazepam

Answer 3

• used as anxiolytics/sedatives

Question 4

Benzodiazepines: Triazolam

Answer 4

• used as hypnotics

Question 5

Benzodiazepines: Temazepam

Answer 5

• used as hypnotics

Question 6

Benzodiazepines: Midazolam

Answer 6

• used as pre-anesthetics

Question 7

Examples of benzodiazepines

Answer 7

diazepam, lorazepam, triazolam, temazepam, midazolam

Question 8

Examples of non-benzodiazepines

Answer 8

barbiturates eg phenobarbital, buspirone, zolpidem, propranolol

Question 9

GABA

Answer 9

inhibitory transmitter in brain regions (limbic system, reticular activating system, motor cortex)

Question 10

Limbic system

Answer 10

alters mood

Question 11

Reticular activating system

Answer 11

cause drowsiness

Question 12

Motor cortex

Answer 12

relax muscles

Question 13

MOA of benzodiazepines

Answer 13

potentiate GABA actions by increasing frequency of GABA-induced channel opening

Question 14

What drug can be used to treat acute toxicity/overdose of benzodiazepines?

Answer 14

Flumazenil, a benzodiazepine antagonist

Question 15

Why is it important to withdraw benzodiazepines gradually?

Answer 15

dependence can develop: withdrawal effects include disturbed sleep, rebound anxiety, tremor and convulsions

Question 16

What are some common side effects of benzodiazepines?

Answer 16

drowsiness, confusion, amnesia, impaired muscle co-ordination

Question 17

Which drug has similar MOA as benzodiazepines and bind to same receptor site? Is it used as anxiolytics too?

Answer 17

Zolpidem, not as effective as anxiolyticcs, primarily used to treat insomnia (hypnotic)

Question 18

Which drug has similar MOA but distinct binding site from benzodiazepines?

Answer 18

Barbiturates

Question 19

Are barbiturates or benzodiazepines preferred for use as sedative-hypnotic?

Answer 19

Benzodiazepines - largely replaced use of barbiturates (which has a higher tendency to develop tolerance and dependence)

Question 20

Most of barbiturates use is limited to:

Answer 20

ultra-short duration for anesthesia

Question 21

Which is the drug that has a structure similar to GABA? Does it act like GABA?

Answer 21

pregabalin, does not act like GABA - only increases synaptic release of GABA!

Question 22

Which anxiolytic drugs work on serotonin receptors?

Answer 22

• buspirone: 5HT1a receptor partial agonist (+dopamine)

- hydroxyzine: 5HT2 receptors antagonism

Question 23

Which anxiolytic drug is an antihistamine?

Answer 23

hyroxyzine: first gen antihistamine with serotonergic and a-adrenergic receptor

Question 24

Which of the anxiotlytic drug is a BB? What is its contraindications?

Answer 24

Propanolol - patients with asthma and heart conditions

Question 25

Long acting benzodiazepines (1-3days)

Answer 25

chlorazepate, chlordiazepoxide, diazepam, flurazepam, quazepam

Question 26

intermediate-acting benzodiazepines (10-20hrs)

Answer 26

alprazolam, estazolam, lorazepam, temazepam

Question 27

short-acting benzodiazepines (3-8hr)

Answer 27

oxazepam, triazolam

Question 28

long-acting barbiturates (1-2days)

Answer 28

• anticonvulsant

- eg. phenobarbital

Question 29

short acting barbiturates (3-8hrs)

Answer 29

• sedative and hypnotic

- eg. pentobarbital and amobarbital

Question 30

ultrashort barbiturates (20 mins)

Answer 30

• iv induction of anesthesia

- eg. thiopental