Chapter 59:
Antiemetic Agents
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Nausea and Vomiting
Most common and most uncomfortable complaints.
Vomiting is a complex reflex reaction to various stimuli.
In some cases, it may be desired to induce vomiting.
In many clinical conditions, the reflex reaction of
vomiting is not beneficial.
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Managing Nausea and Vomiting
Emetics
o Cause vomiting
o No longer recommended for at-home poison control
Antiemetics
o Decrease or prevent nausea and vomiting
o Centrally acting or locally acting
o Varying degrees of effectiveness
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Sites of Action of Emetics/Antiemetics
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Use of Drugs Affecting the Female Reproductive
System Antiemetic Agents Across the Lifespan
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Groups of Centrally Acting Antiemetics
Phenothiazines
Nonphenothiazines
Serotonin (5-HT3) Receptor Blockers
Substance P/Neurokinin 1 Receptor Antagonists
Miscellaneous Group
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Phenothiazines #1
Antianxiety drug that blocks the responsiveness of the
CTZ to stimuli, leading to a decrease in nausea and
vomiting
o Prochlorperazine (generic)
o Chlorpromazine (generic)
o Perphenazine (generic)
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Phenothiazines #2
Actions
o Depresses various areas of the central nervous
system (CNS)
Indications
o Treatment of nausea and vomiting
Adverse Effects
o Drowsiness
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Prototype Phenothiazines
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Nonphenothiazines #1
Prevention of nausea and vomiting associated with
emetogenic cancer chemotherapy, prevention of
postoperative nausea and vomiting
o metoclopramide (Reglan)
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Nonphenothiazines #2
Actions
o Acts to reduce the responsiveness of the nerve cells
in the CTZ to circulating chemicals that induce
vomiting
Indications
o Prevention of nausea and vomiting
Adverse Effects
o Drowsiness
o Fatigue
o Restlessness
o Extrapyramidal symptoms
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Prototype Nonphenothiazines
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(5-HT3) Receptor Blockers #1
Blocks those receptors associated with nausea and
vomiting in the CTZ and locally
o Dolestron (Anzemet)
o Granisetron (generic)
o Ondansetron (Zofran)
o Palonosetron (Aloxi).
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(5-HT3) Receptor Blockers #2
Actions
o Block those receptors associated with nausea and
vomiting in the CTZ and locally
Indications
o Control of nausea and vomiting
Pharmacokinetics
o Rapidly absorbed, metabolized in the liver, and
excreted in urine and feces
Caution
o Pregnancy and lactation
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(5-HT3) Receptor Blockers #3
Adverse Effects
o Headache, drowsiness, myalgia, urinary retention,
constipation, pain at the injection site
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Prototype (5-HT3) Receptor Blockers
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Substance P/Neurokinin 1 Receptor Antagonists
Newest class of drugs for treating nausea and vomiting
o (Emend)
o Rolapitant (Varubi)
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Substance P/Neurokinin 1 Receptor Antagonists
#1
Actions
o Act directly in the CNS to block receptors associated
with nausea and vomiting
Indications
o In combination with other agents to prevent nausea
and vomiting
Pharmacokinetics
o Given orally, metabolized in the liver, and excreted in
urine and feces
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Substance P/Neurokinin 1 Receptor Antagonists
#2
Adverse Effects
o Anorexia, fatigue, constipation, diarrhea, liver
enzyme elevation, dehydration
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Prototype Substance P/Neurokinin 1 Receptor
Antagonists
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Question #1
Please answer the following statement as true or false.
Emetic medications are used to induce vomiting and
should be kept in the home in case of an accidental
poisoning.
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Answer to Question #1
False
Rationale: Emetics cause vomiting and are no longer
recommended for at-home poison control.
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Miscellaneous Antiemetics #1
Dronabinol (Marinol), nabilone (Cesamet) cannabis
(marijuana); hydroxyzine (Vistaril) and (Tigan)
Actions- Varies with agent
Indications
o Treatment and prevention of nausea and vomiting
Pharmacokinetics
o Varies according to agent
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Miscellaneous Agents
Contraindications
o Coma
o Severe CNS depression
o Brain damage or injury
o Hypotension or hypertension
o Severe liver dysfunction
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Miscellaneous Antiemetics #2
Caution
o Renal dysfunction
o Active peptic ulcer disease
o Pregnancy
o Lactation
Adverse Effects
o Linked to interference with normal CNS stimulation or
response
Drowsiness
Dizziness
Weakness
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Miscellaneous Antiemetics #3
Adverse Effects (cont.)
o Photosensitivity
o Hypotension, hypertension, and cardiac arrhythmias
Drug-to-Drug Interactions
o Alcohol
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Nursing Considerations for Antiemetics
Assess:
o History and Physical Exam and known allergy
o Renal or hepatic function, CNS injury, pregnancy and
lactation
o Neurological status, cardiopulmonary status, skin,
BS, abdomen, N&V and appropriate lab values
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Question #2
What is an anticholinergic antiemetic recommended for
vestibular (inner ear) problems?
A. Granisetron
B. Meclizine
C. Palonosetron
D. Perphenazine
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Answer to Question #2
B. Meclizine
Rationale: These drugs—buclizine, cyclizine and meclizine
are anticholinergics that act as antihistamines and block
the transmission of impulses to the CTZ. They are
recommended for the nausea and vomiting associated
with motion sickness or vestibular (inner ear) problems.
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