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Flashcards in 3. Sedation II Deck (34):
1

Site of action of benzos

-GABA A receptor

2

Role of the GABA A receptor

-Inhibitory receptor
-Allows for influx of Cl

3

Clinical effects of benzos/uses

-Anxiety reduction
-Sedation (pre-appointment)
-Hypnosis (sleep production)
-Anterograde amnesia

4

What is anterograde amnesia

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

5

Effects of benzos on the respiratory system

*respiratory depression (at high doses)

6

Benzos have an additive effect with what other drugs

-Other CNS depressants (alcohol, narcotics, other sedatives/hypnotics)
-Hypotensive agents (Ca channel blockers)

7

Location of GABA A receptors

cerebral cortex and limbic system

8

CYP3A inducers are

-Rifampin
-Phenytoin
-Carbamazepine

9

Absolute contraindications for benzos are

-Allergy
-Narrow angle glucoma
-Pregnant patients (teratogenic agent --> congenital craniofacial anomalies)

10

Percautions in benzo use

-Extremes in age (really young and old- diphenhydramien as alternative)
-Suicide potential
-Abuse potential
-Respiratory impairment

11

Two commonly used benzos are

midazolam and diazepam

12

What is the advantages of midazolam over diazepam

midazolam= no active metabolites
-Shorter half life (fast on and fast off)

13

Benzo reversal agent is

flumazenil

14

MOA of flumazenil

Competitive antagonist against benzo binding site on GABA A

15

Chloral hydrate is reduced to what intermediate by what enzyme

trichloroethanol by alcohol dehydrogenase in the liver

16

What happens the the metabolite trichloroethanol

conjugated with glucuronic acid and excreted renally

17

Drug interactions with chloral hydrate

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

18

Absolute contraindication for chloral hydrate

-Allergy
-Porphyria
-Severe hepatic impairment
-Severe renal function
-Severe cardiac disease

19

Relative contraindications for chloral hydrate

-Pregnant/nursing
-Esophagitis
-Gastritis
-Peptic ulcers
-Drug/EtOH dependence

20

MOA of antihistamines

reversible competitive inhibition at the H1 receptor with histamine

21

Benefits of anti-histamines

-Anxiety reduction
-Sedation
-Antiemetic
-Anti-cholinergic

22

Drug interactions with Diphenhydramine

CNS depressants (like alcohol)

23

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

Hydroxizine

24

Drug interactions for hydroxyzine

Same as diphenhydramine (CNS depressants)

25

Contraindications for hydroxyzine

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

26

What class of drug is Zolpidem

Imidazopyridine

27

MOA of Zolpidem

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

28

Advantage of Zolpidem

less amnestic effect than benzos (mental impairment)
-Rapid onset and short duration

29

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

decreased CV and lung function (depression)

30

Administration of flumazenil is (IV/IM)

IV only

31

Major advantage of antihistimines for sedation

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

32

What sedative causes gastric irritation

chloral hydrate

33

What sedatives have an anticholinergic effect

anti-histamines

34

Generic name for Zolpiden is

ambien