Anxiolytic- sedative- hypnotic

Question 1

What is an anxiolytic?

Answer 1

relaxes a patient
not concerned with surroundings and
fully functional

Question 2

What is a sedative drug?

Answer 2

Decreases activity and moderates excitement and calms patient
- patient is still awake

Question 3

What is a hypnotic?

Answer 3

produces drowsiness and facilitate the onset of sleep

pt may be easily aroused

Question 4

What is GA?

Answer 4

state in which there is a loss of consciousness

Question 5

What are some examples of barbs?

Answer 5

Thiopental
Phenobarbital
Pentobarbital

Question 6

At what levels can you potential GABAergic inhibition?

Answer 6

Many levels including:

• Spinal cord
• hypothalamus
• hippo
• substantia nigra
• Cerebellar cortex
• cerebral cortex

Question 7

What role does lipid solubility play in uptake of drug by the brain of barbituates?

Answer 7

Phenobarbital- 20 mins onset= less lipid solubility

Thiopental- 30 seconds= high lipid solubility

Question 8

What is the half life of barbs?

Answer 8

4-5 days with multiple dosing cumulative effects

Question 9

What can be administered to excreted phenobarbital overdose?

Answer 9

Sodium bicarbonate which elevated the urinary pH to excrete more of the drug
-works less for lipid soluble drugs

Question 10

How do hypnotics effect sleep?

Answer 10

Decreased time need to fall asleep, REM and 4 NREM slow wave sleep
- however, it increased stage 2 NREM sleep

Question 11

Can you achieve GA from sedative hypnotics?

Answer 11

yes at a high enough dose one can depress the CNS enough

Question 12

How do sedative hypnotics effect the RS and CV?

Answer 12

CV and RR depression due to medullary vasomotor centers involvement
- at toxic doses you have have circulatory collapse due to depressed vascular tone and heart contractibility

Question 13

How are half-lives related to withdrawal?

Answer 13

The longer the half-life the longer the drug is in the system and one can be weened off more slowly.

• thus the longer the half-life the less likely you are to have withdrawal from a drug
• short half-life drugs can lead to withdrawal even between doses

Question 14

What are some of the clinical uses of barbituates?

Answer 14

Hypnosis
Seizure control
Anesthesia induction

Question 15

What are some examples of benzos?

Answer 15

Diazepam
Lorazepam
Triazolam
Alprazolam

Question 16

What is the mechanism of action of benzos?

Answer 16

Enhance the effects of GABA allosterically without directly activation the GABAa receptors
- increased frequency of chloride channel opening events

Question 17

What are the clinical uses of benzos?

Answer 17

anxiety
insomina
seizures 
muscle relaxation 
pre-anesthetic medication

Question 18

Factors affecting bio-disposition of benzos?

Answer 18

Unlike barbs benzos have little impact on hepatic drug metabolizing enzyme activity

Question 19

What is Flumazenil and what is it used for?

Answer 19

It is a benzo binding site antagonist

• USED FOR BENZO OD
• cant be used for Barbs OD

Question 20

What is the MOA of Ambien?

Answer 20

AKA zolpidem

• Non-benzo, benzo receptor agonist
• selectively bind certain subtypes of GABAr

Question 21

What does ambien promote?

Answer 21

Sleep

• no residual effects upon waking
• rapid onset, low tolerance, short half life

Question 22

What is Buspirone?

Answer 22

Selective anxiolytic

• may take up to 1 week
• no hypnotic effects or sedative effects

Question 23

What is the MOA of Buspirone?

Answer 23

Partial agonist of 5HT1a receptor and affinity for D2 DA

Question 24

What is the MOA of Remelteon?

Answer 24

MT1 and MT2 melatonin R agonist at suprachiasmatic nuclei

- help people fall asleep