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Anti-Emetics Drugs Flashcards

1
Q

Examples of Serotonin Receptor Antagonist

A

Ondansetron
Palonsetron
Dolasetron

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2
Q

What kind of receptors are serotonin Receptor Antagonist

A

5HT3 receptors

Na/K gated channels found in CNS/PNS

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3
Q

What do serontonin receptor antagonist inhibit

A

central and peripheral stimulation of 5-HT3 receptors

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4
Q

Where are serontonin 5HT3 receptors located

A

CTZ

afferent fibers of vagus nerve in GI tract/CNS

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5
Q

+ of Serontonin Receptor Antagonist

A

effective do not cause sedation and well tolerated

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6
Q

when are Serotonin receptor antagonist administered

A

end of surgery

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7
Q

Side effects of serotonin receptor antagonist

A

headache, prolonged QT interval

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8
Q

PO Dose of Ondansetron

A

4 or 8mg

for PONV prophylaxis 16mg PO x1 hour prior to induction of anesthesia

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9
Q

IV Dose of Ondansetron

A

4mg single dose

0.1mg/kg if less the 40kg

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10
Q

Half life of Ondansetron

A

4 hours

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11
Q

Onset of Ondansetron

A

30 mins

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12
Q

Peak Plasma of Ondansetron

A

immediately

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13
Q

Bioavailability of Ondanestron

A

60%

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14
Q

How protein bound is Ondanestron

A

70-76%

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15
Q

Where is ondanestron metabolized?

A

liver by CYP3A4, CYP1A2, CYPD6
extensive metabolism in liver by hydroxylation and conjugation CYP450
less then 5% metabolized in kidneys (no renal dose adjustment)

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16
Q

Elimination 1/2 life of Ondansetron

A

3-7 hours

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17
Q

Excretion of Ondansetron

A

urine

feces

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18
Q

What will decrease clearance of Ondanestron

A

severe hepatic impairment due to increase in plasma 1/2 life

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19
Q

Side effects of Ondansetron

A

headache, dizziness, diarrhea, constipation, prolonged QTc

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20
Q

Palonosetron is

A

second generation serotonin antagonist

most selective- greater affinity for serontonin receptor

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21
Q

Palonosetron is one of the most effective treatments for

A

chemotherapy induced N/V and PONV

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22
Q

Half life of Palonosetron

A

40 hours (therapeutic effects for 72 hours)

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23
Q

Palonosetron dosing for PONV

A

0.75mg

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24
Q

Palonosetron dosing for chemo-induced N/V

A

0.25mg

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25
Q

Excretion of Palonosetron

A

more then 80% excreted in urine over 6 days and 1/2 amount unchanged

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26
Q

Special considerations for palonosetron

A

no doseage adjustments for elderly, renal or hepatic patients
no safety/efficacy data in patients <18 years of age

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27
Q

MOA of Dolasetron

A

reduce activity of vagus nerve to limit activation of the vomitting center in medulla oblongata

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28
Q

Dose of Dolasetron

A

12.6mg IV

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29
Q

DOA of Dolasetron

A

4-9 hours

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30
Q

Protein binding of Dolasetron

A

69-77%

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31
Q

Elimination 1/2 time of Dolasetron

A

8.1 hours

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32
Q

Where is dolasetron eliminated

A

liver (CYP450) kidneys

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33
Q

Onset of dolasetron

A

immediate

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34
Q

Peak Plasma of dolasetron

A

36 minutes

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35
Q

When is the best time to give dolasetron

A

15 minutes before the end of a case

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36
Q

Single dose of dolasteron

A

single oral dose 100mg 102 hours preop is effective

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37
Q

Adverse effects of dolasteron

A

headache, dizziness, constipation, potential for QT prolongation

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38
Q

How is dolasteron excreted

A

urine/feces

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39
Q

Dosing of Granisetron (kytril)

A

0.35-3 mg IV at end of surgery

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40
Q

Granisetron is common for

A

patients receiving chemotherapy and radiation

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41
Q

Half life of granisetron

A

3-14 hours

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42
Q

Bioavailbility of Graniestron

A

60%

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43
Q

Protein binding of graniestron

A

64%

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44
Q

Excretion of graniestron

A

renal and fecal

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45
Q

Adverse effects of granisetron

A

headache, dizziness, and constipation

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46
Q

Dopamine receptor antagonist

A

D2 receptors in GI tract sends signals to CNS to induce nausea and vomiting in vomiting center

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47
Q

Dopamine receptor antagonist are contraindicated in

A

parkinson’s disease

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48
Q

Side effects of dopamine receptor antagonist

A

extrapyramidal side effects

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49
Q

Dopamine Receptor antagonists are also known as

A

butyrophenone class

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50
Q

MOA of Droperidol

A

blocks dopamine receptors that contribute to development of PONV

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51
Q

Properties of Droperidol

A

anxiolytic, sedative, hypnotic and antiemetic properties

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52
Q

Dose of Droperidol

A

0.625-1.25mg IV (SLOW) or IM

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53
Q

Onset of Droperidol

A

3-10 minutes

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54
Q

Peak of Droperidol

A

30 minutes

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55
Q

DOA of droperidol

A

2-4 hours

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56
Q

Where is droperidol metabolized

A

lver

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57
Q

Excretion of droperidol

A

urine (unchanged) and feces

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58
Q

Unwanted side effect of Droperidol

A

qt prolongation

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59
Q

Dose of Droperidol effective at reducing vomiting

A

10-20mcg/kg

60
Q

What dose of droperidol is superioir to metoclopramide PO in reducing PONV

A

20mcg/kg immediately after induction

61
Q

20 mcg/kg of droperidol causes

A

prolonged sedation

62
Q

High dose of droperidol (50-75mg/kg) causes

A

increased side effects: anxiety, dizziness, drowsiness, hypotension, extrapyramidal side effects

63
Q

Droperidol requires

A

12 Lead EKG of patients 2-3 hours after administration

64
Q

Prochlorperazine class

A

Phenothiazine

Anti-psychotic/antiemetic

65
Q

MOA of prochlorperazine

A

affects multiple receptros

histaminergic, dopaminergic (D2 blockade), muscarinic

66
Q

Prochlorperazine is used for

A

PONV prophylaxis

67
Q

Dose of Prochlorperazine

A

5-10mg IM/IV before induction

68
Q

DOA of Prochlorperazine

69
Q

Protein Binding of Prochlorperazine

70
Q

Peak onset Prochlorperazine

71
Q

Prochlorperazine is primarily metabolized by

A

liver (CYP2D6/CYP3A4)

72
Q

Prochlorperazine elimination half life

A

6-10 hours (IV)

73
Q

Excretion of Prochlorperazine

A

biliary inactive metabolites in urine

74
Q

Side effects of Prochlorperazine

A

extrapyramidal and anticholinergic side effects

sedation, blurred vision, hypotension, dizziness, neuroleptic malignant, syndrome, restlessness and dystonia

75
Q

Benzamide

A

Metoclopramide

76
Q

MOA of Metoclopramide

A

centrally acting dopamine receptor antagonist in CTZ/vomiting center (peripherally acting as cholinomimetic in GI tract (facilitates Ach transmission at muscarinic receptors)

77
Q

Metoclopramide will

A

increase LES tone, speeds gastric emptying time, lowers gastric fluid volume

78
Q

Metoclopramide is effective for

A

gastroparesis, GERD, aspiration pneumonia prophylaxiss

79
Q

Dose of Metoclopramide

A

10 mg IV (range 5-20mg) or 0.1-0.25mg/kg IV q6h

80
Q

Metoclopramide must be administered

A

slowly over 1-2 minutes, if not abdominal cramping

81
Q

studies show that Metoclopramide is

A

ineffective at lower doses, unless used in combination with other anti-emetics

82
Q

Advantage of Metoclopramide

A

lack of sedative properties

83
Q

Onset of Metoclopramide

A

3-4 minutes IV

84
Q

Peak of Metoclopramide

85
Q

DOA of Metoclopramide

86
Q

Metabolism of Metoclopramide

87
Q

Elimination of Metoclopramide

A

renal excretion

elimination 1/2 life: 5-6 hours

88
Q

adverse effects of Metoclopramide

A

extrapyramidal side effects

89
Q

Metoclopramide C/A in

A

parkinson’s disease, seziure, GI obstruction and pheochromocytoma

90
Q

Haloperidol belongs to what drug class

A

butyrophenone

91
Q

Dose of Haloperidol

92
Q

Is haloperidol approved by FDA for anti-emetic

93
Q

When do you administer Haloperidol

A

beginning or end of surgery

94
Q

Amisulpride is

A

a D2 adn D3 receptor antagonist

95
Q

Dose of Amisulpride

96
Q

Side effects of Amisulpride

A

mild increase in prolactin level

97
Q

What drug is not associated with sedation, EP or QTc prolongation

A

amisulpride

98
Q

Dose of perphenazine

99
Q

What is perphenazine

A

atypical antipyschotic and dopamine receptor antagonist

100
Q

Neurokinin 1 receptor antagonist

A

found in nucleus of solitary tract and regulate visceral function
provide antemetic activity by suppressing activity at NTS

101
Q

Aprepitant (Emend)

A

neurokinin 1 receptor antagonist

102
Q

MOA of aprepitant

A

inhibit substance P at central and peripheral receptors

103
Q

Does aprepitant have sedative effects?

104
Q

Long half life of aprepitant

105
Q

Dose of aprepitant

A

40-80mg PO preop

106
Q

Aprepitant is recommended for

A

high risk nonpregnant patients

107
Q

Metabolism of aprepitant

108
Q

Bioavailability of Aprepitant

109
Q

Protein binding of aprepitant

110
Q

Excretion of aprepitant

A

feces and urine

111
Q

adverse effects of aprepitant

A

fatigue, dizziness, hypoesthesia, disorientation, N/D, anorexia, constipation, diarrhea, dyspepsia, heartburn, ab pain, gastritis, perforating duodenal ulcer, hiccups

112
Q

When administer dexamethasone + aprepitant

A

reduce dose by 1/2 to maintain dexamethasone plasma concentrations

113
Q

Histamine-receptor Antagonist

A

dramamine dimenhydrinate

Promethazine

114
Q

MOA of Dimenhydrinate

A

H1 antagonist competes with histamine at H1 receptor sites in GI tract, blood vessels and respiratory tract; blocks CTZ, depresses labyrinthine function and vestibular stimulation

115
Q

Adverse effects of dimenhydrinate

A

drowsiness, urinary retention, dry mouth, blurred vision, extrapyramidal effects, commonly causes sedation

116
Q

Dose of dimenhydrinate

A

50-100mg IV/IM q4h

117
Q

Max dose of Dramamine

A

100mg 4hours

118
Q

onset of dramamine

119
Q

duration of dramamine

120
Q

metabolism of dramamine

121
Q

excretion of dramamine

A

metabolites excreted in urine

122
Q

MOA of phenergan

A

Antihistamine (H1) antagonist and anticholinergic/ muscarinic blocking effects responsible for antiemetic properties

123
Q

Dose of Promethazine

A

12.25mg q4-6h

124
Q

DOA of promethazine

125
Q

Metabolism of Promethazine

A

hepatic (glucuronidation and sulfoxidation)

126
Q

Elimination of Promethazine

A

kidney/biliary

127
Q

Elimination 1/2 life of promethazine

A

10-19 hours

128
Q

bioavailibility and protein binding of promethazine

A

88% and 93%

129
Q

Common side effects of Promethazine

A

confusion, drowsiness, dry mouth, constipation (no for patient >65yrs)
significant sedation

130
Q

MOA of scopolamine

A

muscarinic antagonist
inhibits action of ach at parasympathetic sites in smooth muscle, CNS and secretory glands
block communication between nerves of vestibule and vomit center in brainC

131
Q

Scopolamine structure and solubility

A

tertiary amine

lipid soluble

132
Q

Side effects of scopolamine

A

cerebral depression, sedation and amnesia

CNS side efffcts

133
Q

Anticholinergic posioning

A

agitation delirium dry mouth tachycardia, impaired vision hallucinations unconciousness

134
Q

Treatment for anticholinergic OD

A

physostigimine 0.01-0.03mg/kg IV repeat 15-30 mins

135
Q

Scopolamine C/a in pateint

A

closed angle glaucoma

136
Q

Dose of Scopolamine

A

1.5 mg topical patch behind ear

137
Q

Onset of scopolamine

138
Q

DOA of scopolamine

139
Q

Metabolism of scopolamine

140
Q

elimination of scopolamine

141
Q

excretion of scopolamine

142
Q

Scopolamine should be avoided in

A

patients over 65 years of age

143
Q

Adverse effects of scopolamine

A

dry mouth, increased thirst, dry skin, constipation, drowsiness, dizziness, blurred vision, dilated pupils, light sensitivity

144
Q

Ephedrine Class

A

indirect-acting sympathomimetic agent

145
Q

Dose of Ephedrine

A

10-25mg IV recommended for n/v associated with postual hypotension in PACU

146
Q

MOA of Benzo

A

decreases dopamine’s emetic effect in the CTZ and decreases release of serontonin by binding to GABA receptor complex

Pharmacology (14 decks)

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