Aprepitant
Generic Details
Generic Name
Aprepitant
Other Names
- Emend
Drug Class
- Neurokinin-1 receptor antagonist
Chemical Formula
C23H21F7N4O3
Molecular Weight
534.42 g/mol
Mechanism of Action
- Blocks Substance P/neurokinin 1 receptors in the brain
Indications
- Prevention of chemotherapy-induced nausea and vomiting
- Treatment of postoperative nausea and vomiting
Common Dosage Forms
- Capsules
Typical Dosage
- 125 mg on day 1, followed by 80 mg on days 2 and 3
Pediatric Dosage
- Not established
Geriatric Dosage
- Adjust dosing based on renal function
Side Effects
- Fatigue
- Dizziness
- Constipation
- Diarrhea
- Loss of appetite
- Hiccups
Contraindications
- Hypersensitivity to aprepitant or any component of the formulation
Pregnancy Category
- Category B
Lactation Safety
- Compatible, caution advised
Drug Interactions
- Warfarin
- Dexamethasone
- Ondansetron
- Phenytoin
- Carbamazepine
- Rifampin
Overdose Symptoms
- No specific overdose symptoms reported
Antidote for Overdose
- Symptomatic and supportive treatment
Storage Conditions
- Store at room temperature (20-25°C)
Pharmacokinetics
- Absorption: Well absorbed after oral administration
- Distribution: Highly protein-bound, distributed extensively
- Metabolism: Metabolized in the liver via CYP3A4 pathway
- Excretion: Excreted in feces (approx. 59%) and urine (approx. 46%)
Precautions
- Use with caution in patients with hepatic impairment
- May cause dizziness, advise against driving or operating machinery
Warnings
- Risk of QT prolongation, especially when used with other QT-prolonging drugs
Others
- Take with food to enhance absorption