Sedatives and Hypnotics

Question 1

What do Benzodiazepines do to the EC50 for the GABA-induced Cl- influx

Answer 1

decreases it ie LEFT SHIFT (slide 18 of sedatives)

Question 2

Actions of the benzodiazepines

Answer 2

1) reduction of anxiety
2) sedative and hypnotic actions
3) anticonvulsant
4) muscle relaxant
5) anesthesia

Question 3

Name the short acting benzodiazepines please

Answer 3

Diazepam

Flurazepam

Question 4

Name the intermediate acting benzodiazepines please

Answer 4

Alprazolam
Lorazepam
Temazepam

Question 5

Name the long acting benzodiazepines please

Answer 5

Oxazepam

Triazolam

Question 6

Name the benzodiazepines that are directly conjugated and are not metabolized at P450

Answer 6

oxazepam - short acting
lorazepam - intermediate acting
temezepam - intermediate acting
(TO < LAT < DF)

Question 7

Which benzodiazepines are P450’d to intermediate active metabolites before being conjugated

Answer 7

diazepam
flurazepam
LONG ACTING

Question 8

Treat me: I have skeletal muscle spasms from MS and cerebral palsy ie degenerative disorders

Answer 8

Dizepam - long acting

Question 9

Treat me: seizures

Answer 9

clonazepam

Question 10

Treat me: status epilepticus

Answer 10

diazepam - long acting

lorazeaom - intermediate

Question 11

Treatm me: OH withdrawl

Answer 11

diazepma - long acting

oxazepam - short acting

Question 12

Treat me: sleep disroders

Answer 12

flurazepma - long
temazepam - intermediate
triazolam - short

Question 13

A/se of Benzoa

Answer 13

drowsy, confusion
ataxia
cognitive impairment
PARADOXICALs: anxiety, irritabiliyt, hostility, rage, paranoia, depression, suicidal ideation (dose related)

Question 14

Withdrawal sxs of Benzos

Answer 14

confusion, anxiety, agitation, restlessness, insomnia, tension

Question 15

MOA benzos

Answer 15

increase FREQUENCY of channel opening

Question 16

MOA barbituates

Answer 16

increase DURATION of GABAa opening
inhibit glutamate receptors centrally
inhibit sodium receptors centrally

Question 17

Actions of barbituates ie things to watch out for

Answer 17

respiratory depression - stops hypoxic chemoreceptor response to CO2
induceds p450s

Question 18

Thiopental use

Answer 18

barbituate used IV to induce anesthesia - short duration

Question 19

Phenobarbital use

Answer 19

barbituate long term management of a) tonic clonic seizures b) status epiliepticus and c) Eclampsia

Question 20

N-phenylbarbital and phenobarbital use

Answer 20

kernicterus and hyperbilirubinemia

Question 21

A/se of barbituates

times five million

Answer 21

CNS - drowsy, impaired concentrcation, mental and phys sluggy

paradoxical excitement

hypersensitivity

hang over

increased porphryin synthesis***

increases perception of pain***

dependence

poisoning - resp and CNS depression***

Question 22

Differentiate between the three non-benzo benoz receptor agonists used for treatment of insomnia

Answer 22

ZOLPIDEM - short t 1/2, used if cxtzd by difficulty in sleep initiation (also ramelteon - 5HT1a agonist)
ZALEPLON - short t1/2 and rapid onset
ESZOPICLONE - longer 1/2; decreases sleep latency and improves sleep maintenance

Question 23

What is Buspirone and who cares a bout it?

Answer 23

only anxiolytic (not hypnotic, not anticonvulsant or muscle relaxant)

used for ANXIETY
takes 2-3 weeks to work

5HT1 a receptor agonist

works like antidepressants

Question 24

What is Ramelteon and who cares about it?

Answer 24

MT1 and MT2 melatonin receptor agonist

used @ insomnia with difficulty with sleep onset just like zolpidem (not zoleplon be careful zolpIdem with an i for insomnia)

Question 25

Hydroxyzine as a sed/hyp

Answer 25

antihistamine with antiemetic activity

used for SYMPTOMATIC RELIEF OF ANXIERTY (kind of like clonidine)

Question 26

Propanolol as a sed/hyp

Answer 26

Propanolol for Performance anxiety

Question 27

Clonidine as a sed/hyp

Answer 27

modifiers autonomic expression of anxiety (kind of liek hydroxyzine)

Question 28

Diphenhydramine and doxylamine

Answer 28

mild types of situational insomnia