Name of NK1 Receptor Antagonist
- Aprepitant
1.Aprepitant
| Aprepitant |
| Availability : Capsules: 40 mg, 80 mg, 125 mg Powder for injection, lyophilized: 115 mg, 150 mg in single-dose vials |
| Indications and Dosages ØTo prevent acute and delayed nausea and vomiting associated with highly emetogenic chemotherapy, including high-dose cisplatin CAPSULES Adults. 125 mg 1 hr before chemotherapy treatment, followed by 80 mg daily in morning on next 2 days. I.V. INFUSION Adults. 115 mg 30 min before chemotherapy begins (day 1 only). |
| To prevent postoperative nausea and vomiting CAPSULES Adults. 40 mg within 3 hr before induction of anesthesia |
| Administration ● Give with other antiemetics as prescribed. ● For the 115-mg and 150-mg I.V. dose, reconstitute powder with 5 ml normal saline solution in vial and inject in infusion bag containing 110 ml and 145 ml normal saline solution, respectively, to yield a final concentration of 1 mg/ml. Then gently invert I.V. bag two or three times. Don’t mix with other solutions, including lactated Ringer’s and Hartmann’s solutions. |
Mechanism of Action
Crosses the blood–brain barrier to occupy brain NK1 receptors, which prevents nerve transmission of signals that cause nausea and vomiting.
Contraindications
- Hypersensitivity to drug
- Concurrent pimozide, terfenadine, astemizole, or cisapride therapy
- Breastfeeding
Precautions:
- Patients receiving concurrent warfarin or CYP3A4 inhibitors
- Pregnant patients.
Pharmacokinetics
- Metabolism
- Hepatic CYP3A4 (major); CYP1A2, CYP2C19 (minor)
- Enzymes inhibited: CYP3A4
- Enzymes induced: CYP2C9
- Elimination
- Half-life: 9-13 hr
- Total body clearance: 62-90 mL/min
- Excretion (IV admin): 57% urine; 45% feces
Adverse reactions
- CNS: dizziness, neuropathy, headache, insomnia, asthenia, fatigue
- EENT: tinnitus
- GI: nausea, vomiting, constipation, diarrhea, epigastric discomfort, gastritis, heartburn, abdominal pain, anorexia Hematologic: neutropenia
- Other: fever, dehydration, hiccups
Patient monitoring
- Monitor neurologic status. Institute measures to prevent injury as needed.
- Assess nutritional and hydration status.
- Monitor CBC.
Patient teaching
- Tell patient that drug may cause CNS effects. Explain that he’ll be monitored to ensure his safety.
- Advise patient to minimize GI upset by eating small, frequent servings of food and drinking plenty of fluids.
- Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, hearing, strength, balance, and alertness.
- As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.
Nursing Considerations
- Use caution when giving aprepitant to patients with severe hepatic insufficiency because drug’s effects on such patients aren’t known.
- For maximum antiemetic effects, expect to administer aprepitant with dexamethasone and a 5-HT3 antagonist, such as dolasetron, granisetron, or ondansetron.
- Drug is given intravenously only as the first dose 30 minutes before chemotherapy. Later doses are given orally.
- To reconstitute parental aprepitant, inject 5 ml normal saline for injection along vial wall to prevent foaming. Swirl vial gently. Withdraw contents from vial and add to an infusion bag containing 110 ml normal saline solution. Gently invert the bag two or three times. Administer over 15 minutes. Reconstituted solution may be stored at room temperature for 24 hours.
REFERENCES
- Robert Kizior, Keith Hodgson, Saunders Nursing Drug handbook,1st edition 2024, Elsevier Publications. ISBN-9780443116070
- McGraw Hill- Drug Handbook, Seventh Edition, 2013, McGraw Hill Education Publications,9780071799430.
- April Hazard, Cynthia Sanoski, Davi’s Drug Guide for Nurses -Sixteenth Edition 2019, FA Davis Company Publications,9780803669451.
- Jones and Bartlet, Pharmacology for Nurses, Second Edition, 2020, Jones and Bartlet Learning Publications, ISBN 9781284141986.
- Nursebro.com, Search – Nursebro
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