About
Fosaprepitant is a prodrug of aprepitant, a selective high-affinity antagonist of human substance P neurokinin 1 (NK1) receptors. It is indicated for the prevention of chemotherapy-induced nausea and vomiting (CINV), both acute and delayed, associated with highly emetogenic chemotherapy (HEC) and moderately emetogenic chemotherapy (MEC). As a prodrug, fosaprepitant is rapidly converted to aprepitant in vivo, which then crosses the blood-brain barrier and occupies NK1 receptors in the brain, blocking the emetic signals.
Its mechanism of action targets the central nervous system pathways involved in emesis, providing significant antiemetic protection. It is typically administered intravenously as part of a multi-drug regimen, often combined with a corticosteroid and a 5-HT3 antagonist, to achieve optimal control of CINV. This combination approach is crucial for managing the complex pathophysiology of chemotherapy-induced emesis.
Uses
- Prevention of acute chemotherapy-induced nausea and vomiting.
- Prevention of delayed chemotherapy-induced nausea and vomiting.
- Used with highly emetogenic chemotherapy.
- Used with moderately emetogenic chemotherapy.
Directions For Use
Administered intravenously by a healthcare professional. Follow prescribed dosage and infusion rate.
Benefits
- Highly effective in preventing CINV.
- Targets NK1 receptors in the brain.
- Covers both acute and delayed CINV.
- Improves patient comfort during chemotherapy.
- Reduces need for rescue antiemetics.
- Part of standard antiemetic regimens.
Side Effects
- Fatigue
- Headache
- Dizziness
- Hiccups
- Constipation
- Diarrhea
- Anorexia
- Injection site reactions
- Neutropenia
- Dyspepsia
- Bradycardia
- Hypotension
Safety Measures
- Alcohol - No specific interaction, but alcohol can exacerbate nausea and vomiting, counteracting the drug's effect.
- Pregnancy - Use only if clearly needed and potential benefits outweigh risks; consult a physician.
- Breastfeeding - Not recommended; it is unknown if it passes into breast milk.
- Liver - Use with caution in patients with severe hepatic impairment; monitor closely.
- Kidney - No dose adjustment needed for renal impairment.
- Lung - No specific precautions for lung conditions.
Disclaimer
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