Anxiolytics and Sedatives

Question 1

Which is stronger, benzos or barbituates?

Answer 1

barbituates:

• LOC
• low margin of safety
• more neuronal depression
• resp and cardiac supression

Question 2

Where are receptor sites for benzos and barbs?

Answer 2

Adjacent to GABA sites on neurons of CNS

- when benzo or barb binds to receptor site, GABA receptor site is changed and hold onto GABA more intensely.

Question 3

Lethal dose for barbituates?

Answer 3

LD50

lethal dose for 50% of population

Question 4

barbituate classification

Answer 4

i) long acting
ii) intermediate
iii) short acting
iv) ultra short acting

Question 5

most common barbituate for treating seizures

Answer 5

phenobarbitol

Question 6

ultra short acting barbs

Answer 6

thiopental/pentothal:
used in induction phase of general anesthesia
- also used for lethal injections in US
- truth serum

Question 7

short acting barbs

Answer 7

pentobarbital/nembutal:

• schedule II
• insomnia and pre-op sedation
• used for physician assisted suicide
• 15-30 min

Question 8

intermediate acting barbituates

Answer 8

butalbital/fiorinal:
- C4
- used for HA (migraine)
20-40 minutes - 6 hours

Question 9

long acting barbs

Answer 9

phenobarbital/luminal:

• 1 hour - 12 hours
• tx for seizure disorders
• not appropriate for anxiety (used benzos now)

Question 10

problems with barbituates

Answer 10

• drug tolerance
• psychological and physical dependence
• withdrawal (can be fatal)
• potential for coma and resp failure

Question 11

benzodiazepines

Answer 11

most widely used anxiolytics
binding to GABA adjacent receptors decreases GABA
used for anxiety, muscle relaxation, anticonvulsant, and sedative

Question 12

short acting benzo’s

Answer 12

alprazolam/xanax
estazolam/prosom
used for sleep:
temazepam/restoril
triazolam/halcion

Question 13

least favorite benzo, high addiction potential

Answer 13

alprazolam/xanax

Question 14

most common benzo for procedural sedation

Answer 14

Midazolam/versed

Question 15

Midazolam/versed

Answer 15

benzodiazepine
sedative, anxiolytic, anticonvulsant, muscle relaxant
long term use for seizures not recommended due to abuse potential

Question 16

safest longer duration benzo used for insomnia and anxiety

Answer 16

clonazepam/klonopin

Question 17

uased for acute anxiety or during surgery

Answer 17

lorazepam/ativan

Question 18

diazepam/valium

Answer 18

benzo
enhances GABA
anxiolytic, sedative, muscl relaxant, seizure control
se: drowsiness, impaired mentation

Question 19

zolpidem/ambien

Answer 19

short acting non-benzo
increases GABA
initiates sleep, but doesn’t maintain it
not good for seizurs or muscle relaxation

Question 20

Eszopiclone/lunesta

Answer 20

short acting non-benzo
increases GABA
insomnia
not very effective, no drug tolerance

Question 21

Ramelteon/rozerem

Answer 21

melatonin agonist

structurally idential to melatonin

Question 22

most serious side effect of benzodiazepine withdrawal

Answer 22

suicide

- seizures, ha, shaking, sweating, insomnia, weight loss, depression

Question 23

flumazenil/romazicon

Answer 23

benzo receptor antagonist
rapidly reverses effects of benzos
fatal side effects