Sedative/Hypnotics

Question 1

Sedative vs Hypnosis

Answer 1

Sedative- calming effect; relief of anxiety

Hypnotic- encourage sleep ; more pronounced w higher dose

Question 2

Explain GABA-R Activity

Answer 2

GABA-A: primary- induces sedative hypntoic state; Cl- channel

Opens channel; lets Cl- come into cell= hyperpolarization= harder to excite cell (can work on pre & post synaptic cells)

Question 3

Where does the amnesic effect come from?

Answer 3

Blocking of glutamate

Question 4

Benzos: MOA

Answer 4

MOA: Enhance GABA= depresses all levels of CNS

Diazepam, Midazolam

Question 5

Diazepam use ?

Answer 5

Use: Anxiety (presurgery), muscle spasms, ETOH withdrawal

Question 6

Clonazepam Use?

Answer 6

Use: Panic D/o, Sz

Question 7

Lorazepam use ?

Answer 7

Use: Anxiety, Sz (SE)

Question 8

Barbituates: Use, Dose Index

Answer 8

Use: RARE d/t easy OD; anticonvulsants, anesthesia

Dose index: VERY NARROW therapeutic range

(tolerance, dependence, abuse)

Question 9

Barbiturates Classification

Answer 9

Question 10

Barbiturates Adverse effects

Answer 10

Drowsiness
Memory issues; judgement
Abuse

Question 11

Common anesthesia meds

Answer 11

Barbituates- Thiopental &
Methohexital= can induce sz if sensitive to it

Benzodiazpenes

Question 12

Flumazenil

Answer 12

Reversal for benzodiazepines

Question 13

General Anesthetics Types

Answer 13

1) Inhaled
2) Injected

Question 14

Inhalation Anesthetics

Answer 14

Ex: Isoflurane, deslfurane..

Question 15

Injectable anesthetics ex

Answer 15

Ex: Pentothalm

Question 16

Propofol: Use, Pharmacokinetics

Answer 16

Route: Injectable anesthetic

Use: Day care surgery

ADME: Highly lipid soluble, T1/2= 2-8 min

E:kidney excretion

Question 17

Propofol MOA

Answer 17

Incs GABA-A
INC Glycine
Supresses 5HT, nicotinic

(does not work at glutamate= not amnesic)

Question 18

Propofol Uses

Answer 18

1) Anesthesia
2) Antiemetic
3) Anti-convulsive
4) Antipruritic

Question 19

Propofol adverse effects

Answer 19

1) Thrombophlebitis
2) Allergy
3) Hypotension
4) Propofol Syndrome
5) PE

Question 20

Propofol Infusion Syndrome

Answer 20

Metabolic acidosis
Rhabdo
CV collapse

Question 21

Who can’t take propofol?

Answer 21

Egg or soy allergy (tanya)

(oil & water emulsion= needs to be mixed w egg/soy)

Question 22

Explain the alcohol dehydrogenase pathway (non-chronic drinkers)

Answer 22

1) Ethanol–> Alcohol dehydrogenase + NAD+ = Acetaldehyde (hangover s/s) & NADH

2) Acetaldehyde–> aldehyde dehydrogenase+ NAD+ = Acetate & NADH

3) Producing excess NADH= beer belly

Question 23

Explain Pharmacokinetics fo Ethanol & how it varies on dose

Answer 23

M: Liver

Normal Con: 1st order Kinetics ( 1standard drink /hr)

High Concentration= 0 Order Kinetics

Question 24

Explain microsomal ethanol oxidizing systems (MEOS)

Answer 24

Chronic ETOH

1) Ethanol–> Ethanol oxidizing system (MEOS) + NADHP= Acetaldehyde & NADP

2) Acetaldehyde–> NAD+ & Aldehyde dehydrogenase= Acetate

3) Not producing excess NADH= dec in energy

Question 25

Formeipozole: MOA, Use?

Answer 25

MOA: Inhibits alcohol dehydrogenase Use: Antifreeze OD

Question 26

How does disulfiram work?

Answer 26

Inhibits aldehyde dehydrogenase leading to inc acetaldehyde = nasty feeling (N/V) hangover s/s after immediately drinking

Question 27

Why do chronic alcoholics lose weight?

Answer 27

Normal Drinkers: NADH made = gain weight Chronic= dec NADH, less energy & weight loss

Question 28

Ethanol: MOA

Answer 28

1) Enhances GABA 2) Inhibits glutamate= why you black out

Question 29

Diff between ETOH dependence & tolerance & addiction

Answer 29

Tolerance= Need higher concentrations to get same initial effect Dependence= physical withdrawal s/s if stop drinking Addiction= behavior; seek our drug despite negative consequences

Question 30

Wernicke Korsakoff syndrome

Answer 30

Paralysis of external eye muscles, ataxia, confusion, psychosis, coma, death Caused by: Thiamine deficiency from chronic ETOH

Question 31

ETOH Withdrawal Syndrome- Mild S/s

Answer 31

Begins 6-8 hrs after consumption stops; lasts 1-2 days S/s: Tachycardia, hypertension, tremor, anxiety, insomnia, diaphoresis

Question 32

ETOH Withdrawal TX? How does this med effect opioids?

Answer 32

Naltrexone- Long acting opioid antagonist may cause acute withdrawal syndrome in pt who are on opioids

Question 33

Acmprostate

Answer 33

Adjunct therapy- suppresses need/desire for ETOH Used for ETOH withdrawal

Question 34

Disulfiram

Answer 34

Inhibits aldehyde dehydrogenase= acetaldehyde accumulation - Causes severe discomfort in patient that drinks (won't cause discomfort unless person drinks w it)

Question 35

Ultra Short Acting Barbiturate: Ex? Use?

Answer 35

Ultra-short acting: Thiopental (inducing anesthesia)

Question 36

Short Acting Barbiturate: Use, Ex?

Answer 36

Short acting: Pentobarbital (sedation)

Question 37

Intermediate Acting Barb: Ex, Use?

Answer 37

Intermediate acting: Amobarbital (anxiety)

Question 38

Long Acting Barb: Ex:? Use?

Answer 38

Long acting: Phenobarbital (seizures)

Question 39

Sedative Hypnotic Goal for Sleep Cycle

Answer 39

1) Decreased time to fall asleep 2) Increased stage 2 NREM (non-rapid eye movement) sleep

Question 39

ETOH Sleep Effects

Answer 39

ETOH induced sleep 1) Rapid induction to Stage 4 2) Longer time in stage 4 3) Enters REM in second half of evening; vivid dreams

Question 40

UNDESIRABLE Sleep change with sedative hypnotic

Answer 40

Decreased REM (rapid eye movement) sleep Decreased stage 4 NREM slow-wave sleep

Question 41

Neurotoxicity from ETOH

Answer 41

1) Generalize symmetric peripheral nerve injury (distal paraesthesia) 2) Neurological D/o- gait issues, dementia 3) Wernicke Korsakoff Syndrome

Question 42

ETOH Withdrawl S/s- Severe

Answer 42

Lasts: 1-5 days S/s: seizures, fever, hallucinations

Question 43

Delirium tremens ETOH withdrawal

Answer 43

Delirium, extreme agitation, autonomic system instability

Question 44

What med is used to tx anxiety that doesn't cause sedation?

Answer 44

Buspirone – 5-HT1A Receptor Agonist

Question 45

Sleep D/o Tx

Answer 45

Nonpharm= diet, no caffeine Pharm= Zolpidem (Ambien) or Escopiclone (Lunesta) only after sleep study & for short period ; antihistamines