General

Pronunciation:
am-ee-sul-pride

Trade Name(s)

• Barhemsys

Ther. Class.

antiemetics

Pharm. Class.

dopamine antagonists

Indications

• Prevention of postoperative nausea and vomiting (as monotherapy or in combination with another antiemetic in a different pharmacologic class).
• Treatment of postoperative nausea and vomiting in patients who have received antiemetic prophylaxis with an agent of a different pharmacologic class or have not received prophylaxis.

Action

Blocks dopamine-2 and dopamine-3 receptors in chemoreceptor trigger zone of the CNS, which decreases stimulation of the vomiting center.

Therapeutic Effect(s):

Decreased nausea and vomiting following surgical procedures.

Pharmacokinetics

Absorption: IV administration results in complete bioavailability.

Distribution: Extensively distributed to tissues.

Metabolism and Excretion: Undergoes minimal metabolism. Primarily excreted in urine (74%; 58% as unchanged drug), with 23% excreted in feces (20% as unchanged drug).

Half-life: 4–5 hr.

TIME/ACTION PROFILE (plasma concentrations)

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity
• Congenital long QT syndrome.

Use Cautiously in:

• Arrhythmias, conduction disorders, hypokalemia, hypomagnesemia, or HF (↑ risk of QT interval prolongation);
• Concurrent use of QT interval prolonging medications (↑ risk of QT interval prolongation)
• OB:   Safety not established in pregnancy;
• Lactation: Use while breastfeeding only when potential maternal benefit justifies potential risk to infant;
• Pedi:   Safety and effectiveness in children not established.

Adverse Reactions/Side Effects

CV: hypotension (during surgical procedure), QT interval prolongation

Endo: hyperprolactinemia

F and E: hypokalemia

GI: abdominal distention

Local: pain at infusion site

Misc: chills

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

•  Droperidol  and other  QT interval prolonging medications may ↑ risk of QT interval prolongation and torsades de pointes; avoid concurrent use with droperidol.
•  Dopamine agonists, including  levodopa, may ↓ effectiveness; avoid concurrent use.

Route/Dosage

Prevention of Postoperative Nausea and Vomiting

IV (Adults): 5 mg as a single dose administered at the time of anesthesia induction.

Treatment of Postoperative Nausea and Vomiting

IV (Adults): 10 mg as a single dose administered at onset of nausea/vomiting following surgical procedure.

Availability

Solution for injection: 2.5 mg/mL

Assessment

• Assess patient for nausea, vomiting, abdominal distention, and bowel sounds prior to and following administration.
• Monitor ECG in patients with pre-existing arrhythmias/cardiac conduction disorders, electrolyte abnormalities, HF, patients taking other drugs or medical conditions that prolong the QT interval prior to and during therapy.

Implementation

• IV Push:  Do not dilute. Flush line prior and following injection with sterile water for injection, D5W, 0.9% NaCl, or LR. Solution is clear and colorless; do not administer solutions that are discolored or contain particulate matter. Protect from light; administer within 12 hr of removal from carton.
• Rate: Administer over 1–2 min.

Patient/Family Teaching

• Instruct patient to notify health care professional immediately if they perceive a change in heart rate, feel lightheaded, or faint.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Rep:  Advise patient to notify health care professional if pregnancy is planned or suspected. Advise breastfeeding patients to consider interrupting breastfeeding and pumping and discard breast milk for 48 hr after administration to minimize exposure to infant. May cause a reversible increase in milk production. May cause reversible infertility in females.

Evaluation/Desired Outcomes

Decreased nausea and vomiting following surgical procedures.