Sedatives/Hypnotics

Question 0

chlordiazepoxide

Answer 0

chlordiazepoxide: Librium
Anxiety, alcohol withdrawal, pre-anaesthetic

long acting benzo
(active metabolites)

Question 1

alprazolam

Answer 1

alazopram: Xanax
anxiety

intermediate acting benzo
(active metabolites)

Question 2

clonazepam

Answer 2

clonazepam: Klonopin
SEIZURES, mania, movement disorders

intermediate acting benzo & centrally acting spasmolytic

Question 3

diazepam

Answer 3

diazepam: Valium
anxiety, STATUS EPILEPTICUS,muscle relaxant, pre-anaesthetic

long acting benzo & centrally acting spasmolytic
(active metabolites)

Question 4

estazolam

Answer 4

estazolam: Prosom
insomnia

intermediate acting benzo

Question 5

flurazepam

Answer 5

flurazepam: Dalmane
insomnia

intermediate acting benzo
(active metabolites)

Question 6

lorazepam

Answer 6

lorazepam: Ativan
anxiety, STATUS EPILEPTICUS, pre-anaesthetic

intermediate acting benzo

Question 7

midazolam

Answer 7

midazolam: Versed
pre-anaesthetic, intraoperative medication

short acting benzo

Question 8

quazepam

Answer 8

quazepam: Doral
insomnia

long acting benzo
(active metabolites)

Question 9

temazepam

Answer 9

temazepam: Restoril
insomnia

intermediate acting benzo

Question 10

triazolam

Answer 10

triazolam: Halcion
insomnia

short acting benzo
(active metabolites)

Question 11

flunitrazepam

Answer 11

flunitrazepam: Rohypnol
date rape drug

long acting benzo

Question 12

How do benzodiazepines work?

Answer 12

increase GABA(a) receptor-mediated inhibition
(increase Cl- conduction -> hyperpolarize neuron -> CNS depression)

Question 13

Adverse effects of benzodiazepines

Answer 13

• altered sleep
• CNS depression: impaired mental/motor function, ataxia…
• withdrawal sx: anxiety, nausea, seizures
• tolerance
• abuse

Question 14

How are benzodiazepines metabolized?

Answer 14

hepatic: CYP3A4 glucuronidation –> urinary excretion

some are active metabolites

Question 15

zolpidem

Answer 15

zolpidem: Ambien
increase sleep duration
- withdrawal: anxiety, tremor, agitation, rebound insomnia, seizures

short term (8-10d) non-benzo

Question 16

zaleplon

Answer 16

zaleplon: Sonata
help fall asleep
- risk of addiction in long term use

short term (<10d) non-benzo

Question 17

eszopiclone

Answer 17

eszopiclone: Lunesta
increase sleep duration
- potential for tolerance, dependence, abuse

long term (up to 6mo) non-benzo

Question 18

Advantages of non-benzodiazepines over benzodiazepines

Answer 18

• less rebound insomnia/withdrawal symptoms

- lower potential for tolerance, dependence, abuse

Question 19

How do non-benzodiazepines (z-drugs) work?

Answer 19

bind BZ1 receptors of GABA receptor-Cl channel complex

Question 20

flumazenil

Answer 20

flumazenil: Romazicon
reverse action of benzodiazepines (competitive antagonist)

also cause:

• agitation, confusion, dizziness, nausea
• withdrawal sx, seizures in benzo overdose/dependence

Question 21

ramelteon

Answer 21

ramelteon: Rozeram
melatonin agonist (MT1/MT2)
no CNS depression
CYP1A2

Question 22

Advantages of Melatonin agonist

Answer 22

• no CNS depression
• no motor/cognitive impairment
• little withdrawal sx/rebound insomnia
• can be used long term
• not controlled, no abuse potential

Question 23

Adverse effects of Melatonin agonist

Answer 23

• increased serum prolactin

- decreased testosterone

Question 24

buspirone

Answer 24

partial agonist at serotonin receptor : anxiolytic less abuse potential than benzos no CNS depression

Question 25

doxylamine

Answer 25

doxylamine: Unisom (and others) | OTC sleep aid

Question 26

diphendydramine

Answer 26

diphenhydramine: Benadryl (and others) | OTC sleep aid

Question 27

How does alcohol affect sleep?

Answer 27

hypnotic: - initial CNS depression - later rebound excitation (disrupts sleep)

Question 28

GHB

Answer 28

gamma-hydroxybutyrate/sodium oxybate: metabolite and precursor for GABA : cataplexy, narcolepsy - addictive, abuse risk: hallucinogenic, euphoric

Question 29

What do spasmolytics do and what conditions can they treat?

Answer 29

muslce relaxants: tx for spasms - MS - ALS - spinal cord transection - cerebral palsy - stroke - local muscle trauma

Question 30

Centrally acting spasmolytics

Answer 30

- diazepam/clonazepam - baclofen - tizanidine

Question 31

baclofen

Answer 31

baclofen: Lioresal centrally acting spasmolytic, less sedation than benzos GABA(b) receptor agonist

Question 32

tizanidine

Answer 32

tizanidine: Zanaflex centrally acting spasmolytic alpha-2 adrenergic agonist (pre-/post-synaptic inhibition of motor neurons)

Question 33

dantrolene

Answer 33

dantrolene: Dantrium direct acting spasmolytic causes muscle weakness (not for ALS) can treat malignant hyperthermia