Neuro 4: Sedatives & Hypnotics

Front 1

What stage of sleep do you spend the most time in?

Back 1

Stage 2 of NREM

Front 2

What stages of sleep may sleepwalking and dreams begin?

Back 2

3 and 4 of NREM

Front 3

Where do vivid dreams and nightmares occur?

Back 3

REM

Front 4

Which receptor for benzodiazepines utilized for sedation?

Back 4

BZ1

Front 5

Which receptor for benzodiazepines is used for anti-seizure and muscle relaxation?

Back 5

BZ2

Front 6

What blocks the effects of benzodiazepines?

Back 6

Flumazenil

Front 7

If what acts in the bimodal receptor will benzodiazapines cause seizures and anxiety?

Back 7

beta Carboline

Front 8

What do benzodiazapines do for sleep?

Back 8

< time to fall asleep, > stage 2, and < REM and stage 4 (overall time is asleep is still >)

Front 9

What drug is often used to augment anesthetics during colonoscopy and angiography?

Back 9

Midazolam and Fentanyl

Front 10

What drugs are used as anticonvulsants for status epilecticus?

Back 10

Diazepam or Lorazepam

Front 11

What drug is useful to produce a full night's sleep and is thus long-acting?

Back 11

Flurazepam

Front 12

What benzo is poorly absorbed so onset may be slow but has an intermediate duration?

Back 12

Temezepam

Front 13

What benzo is the choice for patients having difficulty falling to sleep but not staying asleep?

Back 13

Triazolam

Front 14

Which benzo has little retrograde amnesia, but has no benefit over flurazepam?

Back 14

Quazepam

Front 15

What sort of dose response range do benzos used for sleep have?

Back 15

Narrower

Front 16

What does the dose response curve look like for benzos you would use to treat anxiety?

Back 16

Long

Front 17

How many subunits of the GABA receptor complex make up a Cl-channel?

Back 17

5

Front 18

Most bezos act at the ___ and ___ receptors on the _____ component of the GABA complex.

Back 18

BZ1 and BZ2 on the gamma component

Front 19

What is the mechanism of action of benzodiazepines?

Back 19

Increase the FREQUENCY of Cl- channel openings and cause hyperpolarization (versus Barbs which affect the DURATION of Cl- channel openings)

Front 20

What would prevent benzodiazepines actoin?

Back 20

Inhibition of GABA synthesis

Front 21

What would enhance the action of benzos?

Back 21

Prevention of GABA degradation

Front 22

Why is the uptake of benzos rapid?

Back 22

Lipophyllic

Front 23

Where does most of the biotransformation of benzos occur?

Back 23

in the liver

Front 24

Where might you see cross tolerance of benzos?

Back 24

Barbituates, alcohol

Front 25

What two things negatively interact with benzos?

Back 25

Alcohol (<resp and coma) and Valprioc acid (psychotic episodes)

Front 26

What would you use in the case of a benzo OD?

Back 26

Flumazenil

Front 27

What receptor does Zolpidem act on?

Back 27

BZ1 (but it is a non-benzo!)

Front 28

Does Zolpidem have any anticonvulsant or muscle relaxant properties?

Back 28

NO

Front 29

What is a negative issue with Zolpidem?

Back 29

Amnesia

Front 30

What non-benzo sedative is similar to Zolpidem but less potent and shorter acting?

Back 30

Zaleplon

Front 31

What receptor does Eszopiclone act on?

Back 31

At or near the BZ receptor

Front 32

What negative effect is NOT associated with Zaleplon that is associated with Zolpidem?

Back 32

Retrograde amnesia

Front 33

What non-benzo is a melatonin receptor agonist?

Back 33

Ramelteon

Front 34

What does Ramelteon do for sleep?

Back 34

Improves sleep onset, but not sleep maintenence

Front 35

Ramelteon should be used cautiously in patients with what?

Back 35

liver dysfunction

Front 36

What non-benzo is associated with endocrine changes?

Back 36

Ramelteon

Front 37

What non-tricyclic non-SSRI antidepressant may cause priapism in males?

Back 37

Trazodone

Front 38

What is the mechanism of Barbiturates?

Back 38

> the duration of Cl- channel openings resulting in hyperpolarization

Front 39

What effects will barbs have on benzos?

Back 39

Enhance benzodiazepine binding and may directly act on the GABA receptor

Front 40

What is an ultra short acting barb?

Back 40

Thiopental

Front 41

Where do barbs diffuse?

Back 41

Across all membranes

Front 42

What is the significance of redistribution?

Back 42

Termination of drug action and consequences of a second administration

Front 43

What is a less lipid soluble barb with a longer time to achieve high concentrations?

Back 43

Phenobarbital

Front 44

Is a second dose of thiopental ultra short like the first?

Back 44

NO, due to lack of redistribution

Front 45

What barbs have significant amounts excreted unchanged?

Back 45

Barbital and Phenobarbital (Longer acting)

Front 46

What drug is often used for induction of anesthesia?

Back 46

Thiopental

Front 47

What effects do barbs have on the cardiovascular system?

Back 47

<BP and HR

Front 48

What effect would barbs have on a pregnancy?

Back 48

< contractions during labor and results in a depressed neonate

Front 49

Why are barbs not useful fore preoperative sedation where pain is involved?

Back 49

They > pain sensitivity

Front 50

What group of drugs > breakdown of coumarin, digitoxin, oral contraceptives, testosterone, anti-depressants?

Back 50

Barbs

Front 51

Barbs drive the formation of what negative feedback mech in normal people?

Back 51

Porphyrins (DO NOT GIVE to people who have acute intermittent porphyria)

Front 52

How do you tx a barb OD?

Back 52

give Bicarb to alkinize the plasma and urine (THER IS NO BARB RECEPTOR ANTAGONIST)

Front 53

How would withdrawal symptoms of barb present?

Back 53

seizures

Front 54

How would you tx barb dependence?

Back 54

Estimate magnitude of habit and give phenobarb and taper off later

Front 55

What do barbs NOT show tolerance to?

Back 55

Respiratory effects

Front 56

What DO barbs show tolerance to?

Back 56

intoxicating effects

Front 57

What drug is unique in the fact that it is almost totally excreted via the lungs in patients with liver and kidney failure?

Back 57

Paraldehyde

Front 58

What can you use as an emergent OTC sedative?

Back 58

Diphenydramine (antihistamine)