Anxolytic Agents

Question 1

At low doses these drugs have what type of effect? What are they used to treat?

Answer 1

anxiolytic; decrease anxiety, used to treat anxiety and apprehension

Question 2

At moderate doses these drugs have what type of effect? What are they used to treat?

Answer 2

sedative; decrease activity and moderates excitement

Question 3

At high doses these drugs have what type of effect? What are they used to treat?

Answer 3

hyypnotic; produces drowsiness and facilitates onset and maintenance of sleep

Question 4

When are these drugs used for muscle relaxation?

Answer 4

only if associated with anxiety/CNS (does not work at the neuromuscular junction

Question 5

What are the two types of CNS Depressants?

Answer 5

a. continuous CNS depressants

b. other type (“type b”)

Question 6

How do Continuous CNS depressants work?

Answer 6

they continue to work more and more powerfully at higher doses. They have a well defined therapeutic index.

Question 7

What are examples of continuous CNS depressants?

Answer 7

Barbituates, alcohol, chloral hydrate, GHB, and general anesthetics

BAGAC

Question 8

How do “Type B” drugs work?

Answer 8

plateau and are more useful for sleep aids and axniety

Question 9

What are some examples of “Type B” drugs?

Answer 9

Benzodiazepines (they are especially useful anxiolytics

Question 10

Fun fact about diazepam:

Answer 10

aka valum; has alot better therapeutic index than older benzodiazepines. Phenobartbital has a therapeutic index of 2.0. Aka no thank you, come again

Question 11

Mechanism for benzodiazepine:

Answer 11

Increase the affinity/activity of GABAa receptors for GABA, BUT ALONE DO NOT OPEN THE CHANNEL. This means it is not an agonist.

Question 12

What are GABAa receptors?

Answer 12

They are ligand gated channels=fast inhibitory responses ( they are the primary inhibitory NT in the brain). They permit CL- ions to flow through the membrane, keeping cells potential negative, which makes action potentials less likely.

Question 13

Mechanism for barbituates?

Answer 13

Increase the amount of opening by GABA AND at a high concentration can open in the ABSENCE of GABA. Increases the efficacy and affinity

Question 14

Which are safer?

Answer 14

Benzodiazepines because tey do not increase the efficacy. The have the ability to produce a desired or intended result.

Question 15

Classifications of Anxiolytics:

Answer 15

Barbituates vs. Benzodiazepines

Question 16

Types of Benzodiazepines:

Answer 16

MALT-D: Midazolam (IV only), Alprazolam, Lorazepam, Triazolam, Diazepam

Question 17

Types of Barbituates:

Answer 17

Phenobarbital, Thiopental, Pentobarbital

Question 18

Where are most benzodiazepines metabolized?

Answer 18

Liver

Question 19

What two of these are special and why are they special?

Answer 19

Lorazepam and oxazepam, they are fast acting and are rapidly metabolized. THEY HAVE NO METABOLITES

Question 20

What is another special case?

Answer 20

Triazolam: it has active metabolites but bot triazolam and its metabolite have short half lives.

Question 21

Which of the benzodiazepines are long acting?

Answer 21

Diazepam

Question 22

Therapeutic affects of benzodiazepines:

Answer 22

Anti-anxiety- you dont want short acting
Sedation ( at low level, constant stimulation), Tolerance develops though
Hypnosis- fast acting work best
Anti-convulsants- diazepam for status epilepticus and alcohol withdrawls

Question 23

Benzodiazepines and hypnosis:

Answer 23

Latency of onset is reduced, REM duration is decreased

. Tolerance develops

Question 24

Side effects!!

Answer 24

Respiration- depression at the meduallary center; not as toxic as barbituates.
Euphoria- makes fast acting drugs more likely to be abused
Parodoxical excitement- release of punishment supression behavior
Anterograde amnesia- in ability to remember events occurring wile on drug

Question 25

Interactions with other drugs

Answer 25

1. Additive or even synergistic CNS depression
2. Functional cross tolerance with ehtanol
3. Oral contraception reduces diazepam elimination
4. Asymmetric cross tolerance with Barbituates (metabolized by the same enzymes)

Question 26

Benzodiazepine antagonist:

Answer 26

Flumazenil- short half life, IV only

Question 27

Mechanism for Flumazenil

Answer 27

Binds to same spot as BZD on GABA

Question 28

Thiopental

Answer 28

intravenous anesthetic, ULTRA SHORT ACTING

Question 29

Pentobarbital

Answer 29

Sedatives, highly abused hypnotic

Question 30

Phenobarbital

Answer 30

used in epilepsy

Question 31

Other drugs used to treat anxiety (non sedatives)

Answer 31

Buspirone- very slow acting, used for chronic treatment. Not good for alcoholics
Beta-adrenergic blocker(propanolol)- short term treatment; decrease symp. tone
Alpha-2-agonist (Clonidine)- decrease symp tone, can cause sedation
Tricyclic anti. dep- for panic attacks

Question 32

Zolipidem

Answer 32

other sedative hypnotic, act at BZD binding site. Sedative effects over anoxiolytic effects. Can decrease REM

Question 33

Chloral hydrate

Answer 33

sedative hypnotic in institutions or pediatric clinics. CAN HAVE HEPATIC TOXICITY and decrease REM

Question 34

Antihistamines (hydroxyine, diphenhydramine)

Answer 34

OTC sedatives/hypnotics; may synergize with morphine for analgesia. Have anticholinergic se: dry mouth

CONTRAINDICATED FOR PREGNANT WOMEN

Question 35

These drugs are not analgetic

Answer 35

They do not treat pain