3. Sedation II Flashcards

1
Q

Site of action of benzos

A

-GABA A receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Role of the GABA A receptor

A
  • Inhibitory receptor

- Allows for influx of Cl

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Clinical effects of benzos/uses

A
  • Anxiety reduction
  • Sedation (pre-appointment)
  • Hypnosis (sleep production)
  • Anterograde amnesia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is anterograde amnesia

A

Loss of ability to create new memories after the event that caused amnesia (in this case taking the benzo)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Effects of benzos on the respiratory system

A

*respiratory depression (at high doses)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Benzos have an additive effect with what other drugs

A
  • Other CNS depressants (alcohol, narcotics, other sedatives/hypnotics)
  • Hypotensive agents (Ca channel blockers)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Location of GABA A receptors

A

cerebral cortex and limbic system

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

CYP3A inducers are

A
  • Rifampin
  • Phenytoin
  • Carbamazepine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Absolute contraindications for benzos are

A
  • Allergy
  • Narrow angle glucoma
  • Pregnant patients (teratogenic agent –> congenital craniofacial anomalies)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Percautions in benzo use

A
  • Extremes in age (really young and old- diphenhydramien as alternative)
  • Suicide potential
  • Abuse potential
  • Respiratory impairment
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Two commonly used benzos are

A

midazolam and diazepam

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the advantages of midazolam over diazepam

A

midazolam= no active metabolites

-Shorter half life (fast on and fast off)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Benzo reversal agent is

A

flumazenil

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

MOA of flumazenil

A

Competitive antagonist against benzo binding site on GABA A

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Chloral hydrate is reduced to what intermediate by what enzyme

A

trichloroethanol by alcohol dehydrogenase in the liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What happens the the metabolite trichloroethanol

A

conjugated with glucuronic acid and excreted renally

17
Q

Drug interactions with chloral hydrate

A
  • CNS depressants (potentiation)

- Coumarin/inanedione anticoagulants (displace anticoagulant from protein binding site)

18
Q

Absolute contraindication for chloral hydrate

A
  • Allergy
  • Porphyria
  • Severe hepatic impairment
  • Severe renal function
  • Severe cardiac disease
19
Q

Relative contraindications for chloral hydrate

A
  • Pregnant/nursing
  • Esophagitis
  • Gastritis
  • Peptic ulcers
  • Drug/EtOH dependence
20
Q

MOA of antihistamines

A

reversible competitive inhibition at the H1 receptor with histamine

21
Q

Benefits of anti-histamines

A
  • Anxiety reduction
  • Sedation
  • Antiemetic
  • Anti-cholinergic
22
Q

Drug interactions with Diphenhydramine

A

CNS depressants (like alcohol)

23
Q

Which has a faster onset of action (Diphenhydramine or hydroxazine)

A

Hydroxizine

24
Q

Drug interactions for hydroxyzine

A

Same as diphenhydramine (CNS depressants)

25
Q

Contraindications for hydroxyzine

A
  • Allergy

- Pregnant/nursing moms (fetal abnormalities in rats0 not known if secreted in the breast milk)

26
Q

What class of drug is Zolpidem

A

Imidazopyridine

27
Q

MOA of Zolpidem

A
  • Binds the omega site on GABA A
  • Unrelated to benzo MOA
  • Enhances affinity of GABA for Chloride conductance and hyperpolarization
28
Q

Advantage of Zolpidem

A

less amnestic effect than benzos (mental impairment)

-Rapid onset and short duration

29
Q

Excessive amounts of benzos have what effects on the cardiovascular and pulmonary system

A

decreased CV and lung function (depression)

30
Q

Administration of flumazenil is (IV/IM)

A

IV only

31
Q

Major advantage of antihistimines for sedation

A

anti-emetic (block muscarinic cholinergic receptors in the chemoreceptor trigger zone (CTZ)

32
Q

What sedative causes gastric irritation

A

chloral hydrate

33
Q

What sedatives have an anticholinergic effect

A

anti-histamines

34
Q

Generic name for Zolpiden is

A

ambien