anti-emetics Flashcards

1
Q

aprepitat category

A

NK1 receptor antagonist

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2
Q

dose of aprepitat

A

40 mg 3 hours prior to induction

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3
Q

peak of aprepitat

A

3 hours

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4
Q

brand name aprepitat

A

emend

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5
Q

MOA aprepitat

A

as an anti-emetic
G protein coupled receptors found in BOTH
central and peripheral NS
also in GI tract
HIGH concentrations of these receipts in regions responsible for N/V

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6
Q

regions of the brain responsible for the vomiting reflex

A

brainstem nuclei
nucleus tractus solataries
area postrema

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7
Q

metabolism aprepitat

A

hepatic

crosses BBB

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8
Q

major A/E of aprepitat

A
fatigue
nausea
constipation
weakness
hiccups
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9
Q

contraindications of other medications with aprepitat

A

Do not combine w/ pimozide,
terfenadine,
astemizole,
or cisapride.

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10
Q

how does aprepitat affect warfarin?

A

Concurrent Warfin use decreases INR

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11
Q

what drugs improve aprepitat’s efficacy?

A

Greater efficacy for preventing vomiting than any other single intervention
*Combine w/ other anti-emetics

(5HT3 antagonist - ondansetron

or dexamethasone - steriod

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12
Q

category of diphenhydromine

A

H1 receptor antagonist

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13
Q

activity of diphenhydromine

A

anticholinergic
antimuscarinic
weak antidopaminergic

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14
Q

dose of diphenhydromine PONV

A

12.5 mg

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15
Q

dose of diphenhydromine allergic RXN

A

10-50 mg

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16
Q

max dose of diphenhydromine

A

400 mg/day

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17
Q

onset diphenhydromine IV

A

IV 2-3 minutes

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18
Q

onset diphenhydromine PO

A

15-30 minutes

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19
Q

peak diphenhydromine IV

A

30-60 minutes

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20
Q

peak diphenhydromine PO

A

2.5 hours

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21
Q

DOA diphenhydromine

A

3-6 hours

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22
Q

uses of diphenhydromine

A

PONV

allergic rxn

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23
Q

metabolism diphenhydromine

A

hepatic

SIGNIFICANT first pass

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24
Q

elimination diphenhydromine

A

urine

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25
Q

major A/E diphenhydromine

A
Drowsiness,
 dry mouth, 
blurred vision, 
urinary retention 
extrapyramidal symptoms, 
sedation, 
increased IOP
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26
Q

contraindications of diphenhydromine

A

Acute asthma,
neonates or premature infants, breast-feeding,
use as local anesthetic

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27
Q

category of dolasetron

A

Serotonin (5ht3) receptor antagonist

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28
Q

brand name dolasetron

A

anzemet

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29
Q

dose of dolasetron

A

IV 12.5 mg PONV

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30
Q

peak dolasetron

A

40 minutes

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31
Q

MOA dolasetron

A

Inhibit central and peripheral stimulation of 5ht3 receptors

32
Q

metabolism dolasetron

A

Hepatic(plasma t ½ twice as long as ondanestron)

33
Q

elimination dolasetron

A

urine

34
Q

major adverse effects dolasetron

A

QTc prolongation, headache, diarrhea, serotonin syndrome (agitation, tachycardia, muscle twitching/

35
Q

what is dolasetron not effective for?

A

chemo related N/V

36
Q

category of droperidol

A

Dopamine receptor antagonist

other receptors antagonized include GABA, NE, and 5HT3

37
Q

name all the receptors antagonized by droperidol

A

Dopamine- main

GABA, NE, 5Ht3

38
Q

dose of droperidol

A

0.625- 1.25 mg IV

39
Q

onset droperidol

A

3-10 minutes

40
Q

peak droperidol

A

30 minutes

41
Q

DOA droperidol

A

2-4 hours

42
Q

uses of droperidol

A

Anti-emetic and antipsychotic.

Low doses- alpha adrenergic receptor blocker  increased sedation.

Antiemetic tx for PONV at higher doses

43
Q

metabolism droperidol

A

hepatic

crosses BBB

44
Q

major A/E droperidol

A
QT prolonged, 
hypotension, 
torsade de pointes, 
depression, 
hallucinations, 
neuroleptic malignant syndrome, 
extrapyramidal symptoms
45
Q

contraindications droperidol

A

Pt’s with known/suspected QT prolongation,
Parkinson’s disease,
bradycardia (

46
Q

trade name droperidol

A

Inapsine,

47
Q

warning with droperidol

A

2001 FDA BB warning arrhythmia and death

48
Q

ondansetron category

A

Serotonin (5ht3) receptor antagonist

not other receptors found for droperidol

49
Q

ondansetron dose

A

4 mg IV

50
Q

onset ondansetron

A

30 minutes

51
Q

peak ondansetron

A

1 hour

52
Q

uses of ondansetron

A

Cancer induced N/V (CINV),
postoperative N/V,
radiotherapy induced N/V

53
Q

metabolism of ondansetron

A

Hepatic (crosses BBB, limited accumulation of these drugs in CNS)

54
Q

elimination of ondansetron

A

urine/feces

55
Q

side effects of ondansetron

A
H/A, 
constipation, 
QTc prolongation, 
cardiac arrhythmia, 
drowsiness, 
serotonin syndrome (agitation, tachycardia, muscle twitching/stiffness)
56
Q

ondansetron MOA

A

*5ht3 receptors are ligand gated Na/K channels in the CNS/PNS,

notably CTZ and afferent fibers of vagus nerve in gut and CNS;

5ht3 activation of CTZ and vagal afferents canvomiting reflex

57
Q

Palonosetron category

A

Newest

Serotonin (5ht3) receptor antagonist

58
Q

dose palonsetron

A

0.25 (CINV)-0.075 (PONV) mg

59
Q

A/E of palonsetron

A

QTc prolongation,
bradycardia,
HA,

60
Q

promethazine MOA

A

Phenothiazine derivative

and a potent antihistamine w/ moderate anti-muscarinic (anticholinergic) activity

61
Q

dose of promethazine

A

12.5-25 mg Q4hrs

62
Q

promethazine onset

A

~ 5 mins

63
Q

promethazine DOA

A

4-6 hrs (up to 12 hrs)

64
Q

uses promethazine

A

Effective rescue tx PONV, use for allergic reactions, sedative

65
Q

metabolism promethazine

A

hepatic

66
Q

promethazine adverse side effects

A

Altered cardiac conduction,
anticholinergic effects,
extrapyramidal symptoms,
neuroleptic syndrome

67
Q

conditions that promethazine is contraindicated with

A
Glaucoma, 
myasthenia gravis, 
Parkinson’s disease, 
respiratory disease, 
seizure disorder
68
Q

promethazine severe warning

A

FDA BB warning 2004: do not use in children

69
Q

Metoclopramide MOA

A

Procainamide derivative and a benzamide prokinetic agent

70
Q

metoclopramide dose

A

25-50 mg IV/IM

71
Q

uses of metoclopramide

A

Most commonly used D2 receptor antagonist for antiemetic prophylaxis,

primarily for PONV and chemo associated w/ low emetogenic risk

72
Q

metoclopramide metabolism

A

1st pass hepatic metabolism decreases bioavailability to 75%;

readily passes BBB and placenta

73
Q

side effects of metoclopramide

A
GI obstruction, 
tardive dyskinesia when used beyond 12 wks., 
Sedation, 
hypotension, 
brady/tachycardia
74
Q

contraindications of metoclopramide

A

Avoid after GI surgery

75
Q

MOA

A

Central and peripheral D2 receptor antagonist activity

Also acts on peripheral D2, muscarinic, and 5HT4 receptors prokinetic activity

Enhances GI motility decreases stomach reflux/urge to vomit