Antiemetic Agents

Nausea and Vomiting

  • Most common and most uncomfortable complaints.

  • Vomiting is a complex reflex reaction to various stimuli.

Managing Nausea and Vomiting

Emetics

  • Cause vomiting

  • No longer recommended for at-home poison control

Antiemetics

  • Decrease or prevent nausea and vomiting

  • Centrally acting or locally acting

  • Varying degrees of effectiveness

Groups of Centrally Acting Antiemetics

  1. Phenothiazines

  2. Nonphenothiazines

  3. Anticholinergics/Antihistamines

  4. Serotonin (5-HT3) Receptor Blockers

  5. Substance P/Neurokinin 1 Receptor Antagonists

  6. Miscellaneous Group

Phenothiazines

Actions

Depresses various areas of the central nervous system (CNS)

Indications

Treatment of nausea and vomiting

Adverse Effects

Drowsiness

Nonphenothiazines

Actions

Acts to reduce the responsiveness of the nerve cells in the CTZ to circulating chemicals that induce vomiting

Indications

Prevention of nausea and vomiting

Adverse Effects

Drowsiness

Fatigue

Restlessness

Anticholinergics/Antihistamines

Actions

Anticholinergics that act as antihistamines and block the transmission of impulses to the CTZ

Indications

Prevention and treatment of nausea and vomiting

Adverse Effects

Drowsiness

Confusion

Dry mouth

Serotonin (5-HT3) Receptor Blockers

Actions

Block those receptors associated with nausea and vomiting in the CTZ and locally

Indications

Control of nausea and vomiting

Pharmacokinetics

Rapidly absorbed, metabolized in the liver, and excreted in urine and feces

Caution

Pregnancy and lactation

Substance P/Neurokinin 1 Receptor Antagonists

Actions

Act directly in the CNS to block receptors associated with nausea and vomiting

Indications

In combination with other agents to prevent nausea and vomiting

Pharmacokinetics

Given orally, metabolized in the liver, and excreted in urine and feces

Miscellaneous Antiemetics

Actions

Varies with agent

Indications

Treatment and prevention of nausea and vomiting

Pharmacokinetics

Varies according to agent

Prototype Phenothiazines

  • Prochlorperazine

Prototype Nonphenothiazines

  • Metoclopramide

Prototype Anticholinergics/
Antihistamines

  • Meclizine

Prototype Serotonin (5-HT3) Receptor Blockers

  • Ondansetron

Prototype Substance P/Neurokinin 1 Receptor Antagonists

  • Aprepitant