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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