Anti-Emetics Drugs Flashcards
1
Q
Examples of Serotonin Receptor Antagonist
A
Ondansetron
Palonsetron
Dolasetron
2
Q
What kind of receptors are serotonin Receptor Antagonist
A
5HT3 receptors
Na/K gated channels found in CNS/PNS
3
Q
What do serontonin receptor antagonist inhibit
A
central and peripheral stimulation of 5-HT3 receptors
4
Q
Where are serontonin 5HT3 receptors located
A
CTZ
afferent fibers of vagus nerve in GI tract/CNS
5
Q
+ of Serontonin Receptor Antagonist
A
effective do not cause sedation and well tolerated
6
Q
when are Serotonin receptor antagonist administered
A
end of surgery
7
Q
Side effects of serotonin receptor antagonist
A
headache, prolonged QT interval
8
Q
PO Dose of Ondansetron
A
4 or 8mg
for PONV prophylaxis 16mg PO x1 hour prior to induction of anesthesia
9
Q
IV Dose of Ondansetron
A
4mg single dose
0.1mg/kg if less the 40kg
10
Q
Half life of Ondansetron
A
4 hours
11
Q
Onset of Ondansetron
A
30 mins
12
Q
Peak Plasma of Ondansetron
A
immediately
13
Q
Bioavailability of Ondanestron
A
60%
14
Q
How protein bound is Ondanestron
A
70-76%
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)
16
Q
Elimination 1/2 life of Ondansetron
A
3-7 hours
17
Q
Excretion of Ondansetron
A
urine
feces
18
Q
What will decrease clearance of Ondanestron
A
severe hepatic impairment due to increase in plasma 1/2 life
19
Q
Side effects of Ondansetron
A
headache, dizziness, diarrhea, constipation, prolonged QTc
20
Q
Palonosetron is
A
second generation serotonin antagonist
most selective- greater affinity for serontonin receptor
21
Q
Palonosetron is one of the most effective treatments for
A
chemotherapy induced N/V and PONV
22
Q
Half life of Palonosetron
A
40 hours (therapeutic effects for 72 hours)
23
Q
Palonosetron dosing for PONV
A
0.75mg
24
Q
Palonosetron dosing for chemo-induced N/V
A
0.25mg
25
Excretion of Palonosetron
more then 80% excreted in urine over 6 days and 1/2 amount unchanged
26
Special considerations for palonosetron
no doseage adjustments for elderly, renal or hepatic patients
no safety/efficacy data in patients <18 years of age
27
MOA of Dolasetron
reduce activity of vagus nerve to limit activation of the vomitting center in medulla oblongata
28
Dose of Dolasetron
12.6mg IV
29
DOA of Dolasetron
4-9 hours
30
Protein binding of Dolasetron
69-77%
31
Elimination 1/2 time of Dolasetron
8.1 hours
32
Where is dolasetron eliminated
liver (CYP450) kidneys
33
Onset of dolasetron
immediate
34
Peak Plasma of dolasetron
36 minutes
35
When is the best time to give dolasetron
15 minutes before the end of a case
36
Single dose of dolasteron
single oral dose 100mg 102 hours preop is effective
37
Adverse effects of dolasteron
headache, dizziness, constipation, potential for QT prolongation
38
How is dolasteron excreted
urine/feces
39
Dosing of Granisetron (kytril)
0.35-3 mg IV at end of surgery
40
Granisetron is common for
patients receiving chemotherapy and radiation
41
Half life of granisetron
3-14 hours
42
Bioavailbility of Graniestron
60%
43
Protein binding of graniestron
64%
44
Excretion of graniestron
renal and fecal
45
Adverse effects of granisetron
headache, dizziness, and constipation
46
Dopamine receptor antagonist
D2 receptors in GI tract sends signals to CNS to induce nausea and vomiting in vomiting center
47
Dopamine receptor antagonist are contraindicated in
parkinson's disease
48
Side effects of dopamine receptor antagonist
extrapyramidal side effects
49
Dopamine Receptor antagonists are also known as
butyrophenone class
50
MOA of Droperidol
blocks dopamine receptors that contribute to development of PONV
51
Properties of Droperidol
anxiolytic, sedative, hypnotic and antiemetic properties
52
Dose of Droperidol
0.625-1.25mg IV (SLOW) or IM
53
Onset of Droperidol
3-10 minutes
54
Peak of Droperidol
30 minutes
55
DOA of droperidol
2-4 hours
56
Where is droperidol metabolized
lver
57
Excretion of droperidol
urine (unchanged) and feces
58
Unwanted side effect of Droperidol
qt prolongation
59
Dose of Droperidol effective at reducing vomiting
10-20mcg/kg
60
What dose of droperidol is superioir to metoclopramide PO in reducing PONV
20mcg/kg immediately after induction
61
20 mcg/kg of droperidol causes
prolonged sedation
62
High dose of droperidol (50-75mg/kg) causes
increased side effects: anxiety, dizziness, drowsiness, hypotension, extrapyramidal side effects
63
Droperidol requires
12 Lead EKG of patients 2-3 hours after administration
64
Prochlorperazine class
Phenothiazine
| Anti-psychotic/antiemetic
65
MOA of prochlorperazine
affects multiple receptros
| histaminergic, dopaminergic (D2 blockade), muscarinic
66
Prochlorperazine is used for
PONV prophylaxis
67
Dose of Prochlorperazine
5-10mg IM/IV before induction
68
DOA of Prochlorperazine
3-4 hours
69
Protein Binding of Prochlorperazine
91-99%
70
Peak onset Prochlorperazine
2-4 hours
71
Prochlorperazine is primarily metabolized by
liver (CYP2D6/CYP3A4)
72
Prochlorperazine elimination half life
6-10 hours (IV)
73
Excretion of Prochlorperazine
biliary inactive metabolites in urine
74
Side effects of Prochlorperazine
extrapyramidal and anticholinergic side effects
| sedation, blurred vision, hypotension, dizziness, neuroleptic malignant, syndrome, restlessness and dystonia
75
Benzamide
Metoclopramide
76
MOA of Metoclopramide
centrally acting dopamine receptor antagonist in CTZ/vomiting center (peripherally acting as cholinomimetic in GI tract (facilitates Ach transmission at muscarinic receptors)
77
Metoclopramide will
increase LES tone, speeds gastric emptying time, lowers gastric fluid volume
78
Metoclopramide is effective for
gastroparesis, GERD, aspiration pneumonia prophylaxiss
79
Dose of Metoclopramide
10 mg IV (range 5-20mg) or 0.1-0.25mg/kg IV q6h
80
Metoclopramide must be administered
slowly over 1-2 minutes, if not abdominal cramping
81
studies show that Metoclopramide is
ineffective at lower doses, unless used in combination with other anti-emetics
82
Advantage of Metoclopramide
lack of sedative properties
83
Onset of Metoclopramide
3-4 minutes IV
84
Peak of Metoclopramide
1-2 hours
85
DOA of Metoclopramide
1-2 hours
86
Metabolism of Metoclopramide
liver
87
Elimination of Metoclopramide
renal excretion
| elimination 1/2 life: 5-6 hours
88
adverse effects of Metoclopramide
extrapyramidal side effects
89
Metoclopramide C/A in
parkinson's disease, seziure, GI obstruction and pheochromocytoma
90
Haloperidol belongs to what drug class
butyrophenone
91
Dose of Haloperidol
0.5-2mg
92
Is haloperidol approved by FDA for anti-emetic
no
93
When do you administer Haloperidol
beginning or end of surgery
94
Amisulpride is
a D2 adn D3 receptor antagonist
95
Dose of Amisulpride
5-10mg IV
96
Side effects of Amisulpride
mild increase in prolactin level
97
What drug is not associated with sedation, EP or QTc prolongation
amisulpride
98
Dose of perphenazine
5mg IV
99
What is perphenazine
atypical antipyschotic and dopamine receptor antagonist
100
Neurokinin 1 receptor antagonist
found in nucleus of solitary tract and regulate visceral function
provide antemetic activity by suppressing activity at NTS
101
Aprepitant (Emend)
neurokinin 1 receptor antagonist
102
MOA of aprepitant
inhibit substance P at central and peripheral receptors
103
Does aprepitant have sedative effects?
no
104
Long half life of aprepitant
9-13hours
105
Dose of aprepitant
40-80mg PO preop
106
Aprepitant is recommended for
high risk nonpregnant patients
107
Metabolism of aprepitant
liver
108
Bioavailability of Aprepitant
60-65%
109
Protein binding of aprepitant
>95%
110
Excretion of aprepitant
feces and urine
111
adverse effects of aprepitant
fatigue, dizziness, hypoesthesia, disorientation, N/D, anorexia, constipation, diarrhea, dyspepsia, heartburn, ab pain, gastritis, perforating duodenal ulcer, hiccups
112
When administer dexamethasone + aprepitant
reduce dose by 1/2 to maintain dexamethasone plasma concentrations
113
Histamine-receptor Antagonist
dramamine dimenhydrinate
| Promethazine
114
MOA of Dimenhydrinate
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
Adverse effects of dimenhydrinate
drowsiness, urinary retention, dry mouth, blurred vision, extrapyramidal effects, commonly causes sedation
116
Dose of dimenhydrinate
50-100mg IV/IM q4h
117
Max dose of Dramamine
100mg 4hours
118
onset of dramamine
immediate
119
duration of dramamine
4-6 hours
120
metabolism of dramamine
liver
121
excretion of dramamine
metabolites excreted in urine
122
MOA of phenergan
Antihistamine (H1) antagonist and anticholinergic/ muscarinic blocking effects responsible for antiemetic properties
123
Dose of Promethazine
12.25mg q4-6h
124
DOA of promethazine
4-6 hours
125
Metabolism of Promethazine
hepatic (glucuronidation and sulfoxidation)
126
Elimination of Promethazine
kidney/biliary
127
Elimination 1/2 life of promethazine
10-19 hours
128
bioavailibility and protein binding of promethazine
88% and 93%
129
Common side effects of Promethazine
confusion, drowsiness, dry mouth, constipation (no for patient >65yrs)
significant sedation
130
MOA of scopolamine
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
Scopolamine structure and solubility
tertiary amine
| lipid soluble
132
Side effects of scopolamine
cerebral depression, sedation and amnesia
| CNS side efffcts
133
Anticholinergic posioning
agitation delirium dry mouth tachycardia, impaired vision hallucinations unconciousness
134
Treatment for anticholinergic OD
physostigimine 0.01-0.03mg/kg IV repeat 15-30 mins
135
Scopolamine C/a in pateint
closed angle glaucoma
136
Dose of Scopolamine
1.5 mg topical patch behind ear
137
Onset of scopolamine
2-4 hours
138
DOA of scopolamine
72 hours
139
Metabolism of scopolamine
liver
140
elimination of scopolamine
4.5 hours
141
excretion of scopolamine
kidneys
142
Scopolamine should be avoided in
patients over 65 years of age
143
Adverse effects of scopolamine
dry mouth, increased thirst, dry skin, constipation, drowsiness, dizziness, blurred vision, dilated pupils, light sensitivity
144
Ephedrine Class
indirect-acting sympathomimetic agent
145
Dose of Ephedrine
10-25mg IV recommended for n/v associated with postual hypotension in PACU
146
MOA of Benzo
decreases dopamine's emetic effect in the CTZ and decreases release of serontonin by binding to GABA receptor complex
