Pharm - Sedatives and Hypnotics

Question 1

list the benzodiazepine antagonist

Answer 1

flumazenil

Question 2

-pam suffix indicates what type of drug

Answer 2

benzodiazepines

Question 3

-barbital indicate what type of drug

Answer 3

bartbiturates

Question 4

compare sedatives to hypnotic drugs

Answer 4

sedatives: decrease CNS activity, moderates excitement, calms pt

hypnotic drug: produces drowsiness, facilitates onset and maintenance of sleep
- more pronounced depression of the CNS

Question 5

MOA benzodiazepines

Answer 5

binds to GABA-A receptor and enhances GABA’s effects

–> chloride influx –> hyperpolarization –> fewer number of action potentials –> CNS depression

Question 6

describe the advantages of benzos

Answer 6

1) high therapeutic index
2) antagonist available for OD
3) low risk of drug-drug interactions
4) minimal effect on CV or autonomic system

Question 7

describe the disadvantages of benzos

Answer 7

1) risk of dependence
2) depression of CNS function
3) amnestic effects
4) bad when combined with alcohol

Question 8

describe the half life, active metabolite status, and rate of onset for Diazepam

Answer 8

half life: >100 hours
active metabolites: yes
rate of onset: very fast

Question 9

describe the half life, active metabolite status, and rate of onset for Alprazolam

Answer 9

half life: 12-15 hrs
active metabolites: insignificant
rate of onset: fast

Question 10

list the short to intermediate acting benzos

Answer 10

1) alprazolam
2) oxazepam
3) temazepam
4) midazolam
5) traizolam

Question 11

list the intermediate to long acting benzos

Answer 11

1) diazepam
2) lorazepam
3) clonazepam

Question 12

indications for Alprazolam

Answer 12

• anxiety disorder

- panic disorder

Question 13

contraindications for Alprazolam

Answer 13

• pts w/ acute narrow angle glaucoma

- w/ ketoconazole and itraconazole

Question 14

indications for midazolam

Answer 14

preoperative sedation/anxiolysis/amnesia

Question 15

black box warning for midazolam

Answer 15

respiratory depression

Question 16

indications for diazepam

Answer 16

• management of anxiety disorders and for short term relief of sx of anxiety
• also used in acute alcohol withdrawal

Question 17

how does milk to moderate cirrhosis affect use of diazepam

Answer 17

the average half-life is increased from 2-5 fold

Question 18

contraindications for diazepam

Answer 18

1) peds pts under 6 months
2) myasthenia gravis
3) respiratory insufficiency
4) severe hepatic 3 insufficiency
5) sleep apnea
6) acute narrow angle glaucoma

Question 19

warnings for diazepam

Answer 19

not recommended in tx of psychotic pts and don’t use w/ alcohol

Question 20

indications oxazapam

Answer 20

anxiety, anxiety w/ depression, and acute alcohol withdrawal

Question 21

indications triazolam

Answer 21

short term tx of insomnia (7-10 days)

Question 22

indications chlordiazepoxide

Answer 22

1) management of anxiety disorders or for short term relief of anxiety
2) alcohol withdrawal
4) preoperative apprehension and anxiety

Question 23

indications flurazepam

Answer 23

long acting hypnotic agent useful for tx of insomnia

Question 24

indications lorazepam

Answer 24

seizure disorders like epilepsy

- can also be used before surgery to relieve anxiety

Question 25

indications buspirone

Answer 25

tx of generalized anxiety disorder | ***takes more than a week to become establihsed

Question 26

indications flumazenil

Answer 26

complete or partial reversal of sedative effects of benzos | - management of ODs

Question 27

MOA flumazenil

Answer 27

competitively inhibits activity at benzo recognition site on GABA receptor

Question 28

black box warning flumazenil

Answer 28

seizures most frequently in pts who have been on benzos for long time

Question 29

MOA barbituates

Answer 29

binds to GABA-A receptor and increases duration of GABA gated channel openings --> chloride influx --> hyperpolarization --> decreased number of action potentials --> CNS depression

Question 30

compare the typical indications for ultra short acting, short acting, and long acting barbiturates

Answer 30

ultra short: anesthesia short: insomnia long: seizures

Question 31

indications thiopental

Answer 31

1) sole anesthetic agent for brief procedures 2) induction of anesthesia prior to other anesthetic agents 3) supplements regional anesthesia 4) hypnosis during balanced anesthesia w/ other agents 5) control convulsive states during or following anesthesia 6) increase intracranial pressure in neurosurgical pts

Question 32

indications secobarbital

Answer 32

hypnotic for the short term tx of insomnia (loses effectiveness after 2 weeks)

Question 33

contraindications secobarbital

Answer 33

marked impairment of liver, respiratory dz

Question 34

indications phenobarbital

Answer 34

sedative or hypnotic

Question 35

contraindications phenobarbital

Answer 35

pts with history of manifest or latent porphyria

Question 36

MOA ramelteon

Answer 36

full agonist at MT1 and MT2 melatonin receptors

Question 37

metabolism of ramelteon

Answer 37

metabolized by CYP1A2

Question 38

adverse effects ramelteon

Answer 38

dizziness, somnolence, fatigue, endocrine changes

Question 39

indications ramelteon

Answer 39

insomnia characterized by difficulty with sleep onset

Question 40

MOA zaleplon

Answer 40

interacts with GABA-benzodiazapine receptor complex (but is not a benzo)

Question 41

indications zaleplon

Answer 41

short term tx of insomnia

Question 42

indications zolpidem

Answer 42

short term tx of insomnia characterized by difficulties with sleep initiation

Question 43

indications eszopiclone

Answer 43

insomnia

Question 44

indications meprobamate

Answer 44

anxiety disorders or for short term relief of sx of anxiety

Question 45

MOA meprobamate

Answer 45

slowing activity in brain to allow for relaxation

Question 46

indications chloral hydrate

Answer 46

short term use as sedative or sleep med