Sedative-Hypnotic

Question 1

Role of GABA

Answer 1

Modulate activity of other neurons through inhibition

Question 2

GABA A receptor

Answer 2

Allows Cl entry causing hyperpolarization and decreases firing of cell
Benzodiazepines and barbiturates work here

Question 3

GABA B receptor

Answer 3

Increased K efflux and decreased Ca entry hyperpolarizes

Baclofen works here

Question 4

Minimum requirement for GABA binding

Answer 4

2 alpha and 2 beta subunits

Question 5

Therapeutic uses for sedative-hypnotic drugs

Answer 5

Anti anxiety, sedation, anti seizure, amnesia, muscle relaxation, hypnosis, anesthesia

Question 6

Benzodiazepine binding

Answer 6

Binds to GABA A receptor at a site distinct from GABA agonist site to enhance action of GABA
Acts as allosteric modulator
Increases the FREQUENCY of Cl ion channel openings

Question 7

Do not take what with benzos

Answer 7

Alcohol

Question 8

Adverse affects of benzos

Answer 8

Daytime drowsiness, motor incoordination, rebound insomnia, anterograde amnesia

Question 9

What is used in a benzo overdose

Answer 9

Flumazenil

Question 10

Anxiolytics used for

Answer 10

Alcohol withdrawal, seizure disorders, status epilepticus, preop sedation, anxiety relief, panic disorder

Question 11

Lorazepam

Answer 11

Can be used for status epilepticus IV

Intermediate acting benzo

Question 12

Midazolam

Answer 12

Short acting benzo

Can be used for preop sedation and anxiety relief

Question 13

Alprazolam

Answer 13

Can be used to manage panic disorder

Short acting benzo

Question 14

Diazepam

Answer 14

Long acting benzo

Question 15

Temazepam

Answer 15

Sedative
6-8 hours action (overnight to sleep)
Avoid sudden withdrawal as it can cause rebound insomnia

Question 16

Z drugs

Answer 16

DOC benzos for short term management of insomnia
Zolpidem, Zaleplon
Very short half life

Question 17

Barbiturates used for

Answer 17

Anticonvulsants, anesthestic induction, drug induced coma for TBI

Question 18

Phetobarbital

Answer 18

Used for induced coma for traumatic brain injury

Question 19

Barbiturates binding

Answer 19

Bind to different site of GABA A receptor

Increase the duration of Cl channel opening

Question 20

Antidote of barbiturate

Answer 20

Nitric oxide

Question 21

Withdrawal of benzos and barbiturates cause

Answer 21

Excitation, insomnia, life threatening seizures

Question 22

Buspirone

Answer 22

Anti anxiety drug–partial agonist at serotonin receptors

Too much serotonin can cause anxiety–Buspirone blocks this

Question 23

Ramelteon

Answer 23

Agonist at melatonin receptors MT1 and MT2

FDA approved for insomnia, particularly with delayed onset of sleep