• PO, IV: Prevention of:
  • Acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic chemotherapy,
  • Nausea and vomiting associated with initial and repeat courses of moderately emetogenic chemotherapy.
• PO: Prevention of postoperative nausea and vomiting.

Contraindicated in:

• Hypersensitivity
• Concurrent use with pimozide (risk of life-threatening adverse cardiovascular reactions)
• Lactation: May cause unwanted effects in nursing infants.

Use Cautiously in:

• Concurrent use with any CYP3A4 substrates
• Concurrent use with strong or moderate CYP3A4 inhibitors
• Concurrent use with strong CYP3A4 inducers
• OB: Use only if clearly needed
• Pedi: Children <6 mo (IV) and <6 mo (PO) (safety and effectiveness not established).

CV: dizziness, fatigue, weakness.

Derm: STEVENS-JOHNSON SYNDROME.

GI: diarrhea.

Neuro: headache.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS), hiccups, infusion reactions (fosaprepitant IV only).

Drug-Drug:

• May ↑ levels of CYP3A4 substrates, including docetaxel, paclitaxel, etoposide, irinotecan, ifosfamide, imatinib, vinorelbine, vinblastine, vincristine, midazolam, triazolam, and alprazolam; concurrent use should be undertaken with caution.
• Moderate or strong CYP3A4 inhibitors, including ketoconazole, itraconazole, nefazodone, clarithromycin, ritonavir, nelfinavir, and diltiazem) may ↑ levels and risk of adverse reactions.
• Strong CYP3A4 inducers, including rifampin, carbamazepine, and phenytoin may ↓ levels and effects.
• ↑levels and effects of dexamethasone (regimen reflects a 50% dose ↓); a similar effect occurs with methylprednisolone (↓ IV dose by 25%, ↓ PO dose by 50% when used concurrently).
• May ↓ the effects of warfarin (carefully monitor INR for 2 wk), oral contraceptives (use alternate method), and phenytoin.

(Generic available)

• Capsules: 40 mg; 80 mg; 125 mg;
• Emulsion for injection (aprepitant): 7.2 mg/mL;
• Lyophilized powder for injection (fosaprepitant): 150 mg/vial;
• Powder for oral suspension (requires reconstitution): 125 mg/pouch;

Prevention of Nausea and Vomiting Associated with Highly Emetogenic Chemotherapy

• PO (Adults): Capsules or suspension — 125 mg given 1 hr prior to chemotherapy (Day 1) (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 80 mg once daily for 2 days (Days 2 and 3) (with dexamethasone 8 mg once daily for 3 days [Days 2–4]).
• IV (Adults): Fosaprepitant — 150 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT₃ antagonist prior to chemotherapy). Continue dexamethasone on Days 2–4 (8 mg PO on Day 2, 8 mg twice daily on Days 3 and 4); Aprepitant — 130 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT₃ antagonist prior to chemotherapy). Continue dexamethasone on Days 2–4 (8 mg PO on Day 2, 8 mg twice daily on Days 3 and 4).
• PO (Children 12 yr): Capsules — 125 mg given 1 hr prior to chemotherapy (Day 1) (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 80 mg once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 3 days [Days 2–4]).
• PO (Children 6 mo–<12 yr and >6 kg): Suspension — 3 mg/kg (max dose = 125 mg) given 1 hr prior to chemotherapy (Day 1) (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 3 days [Days 2–4]).
• IV (Children 12–17 yr and 6 kg): Single–day chemotherapy regimen — 150 mg given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multi–day chemotherapy regimen — 115 mg given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 80 mg PO once daily (capsules) for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].
• IV (Children 2–<12 yr and 6 kg): Single–day chemotherapy regimen — 4 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multi–day chemotherapy regimen — 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) (oral suspension) PO once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].
• IV (Children 6 mo-<2 yr and 6 kg): Single–day chemotherapy regimen — 5 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multi–day chemotherapy regimen — 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) (oral suspension) PO once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].

Prevention of Nausea and Vomiting Associated with Moderately Emetogenic Chemotherapy

• PO (Adults): Capsules or suspension — 125 mg given 1 hr prior to chemotherapy (Day 1) (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT₃ antagonist), then 80 mg once daily for 2 days (Days 2 and 3).
• IV (Adults): Fosaprepitant — 150 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT₃ antagonist prior to chemotherapy); Aprepitant — 100 mg given 30 min prior to chemotherapy on Day 1 (with dexamethasone 12 mg PO given 30 min prior to chemotherapy and a 5-HT₃ antagonist prior to chemotherapy). Continue aprepitant 80 mg PO on Days 2 and 3.
• PO (Children 12 yr): Capsules — 125 mg given 1 hr prior to chemotherapy (Day 1) (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist), then 80 mg once daily for 2 days (Days 2 and 3).
• PO (Children 6 mo–<12 yr and >6 kg): Suspension — 3 mg/kg (max dose = 125 mg) given 1 hr prior to chemotherapy (Day 1) (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 3 days [Days 2–4]).
• IV (Children 12–17 yr and 6 kg): Single–day chemotherapy regimen — 150 mg given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multi–day chemotherapy regimen — 115 mg given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 80 mg PO once daily (capsules) for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].
• IV (Children 2–<12 yr and 6 kg): Single–day chemotherapy regimen — 4 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multi–day chemotherapy regimen — 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) (oral suspension) PO once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].
• IV (Children 6 mo-<2 yr and 6 kg): Single–day chemotherapy regimen — 5 mg/kg (max dose = 150 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy). Continue dexamethasone on Day 2; Multi–day chemotherapy regimen — 3 mg/kg (max dose = 115 mg) given 30 min prior to chemotherapy on Day 1 (with PO dexamethasone at 50% of recommended dose given 30 min prior to chemotherapy and a 5-HT₃ antagonist given prior to chemotherapy), then 2 mg/kg (max dose = 80 mg) (oral suspension) PO once daily for 2 days (Days 2 and 3) (with PO dexamethasone at 50% of recommended dose once daily for 2 days [Days 2 and 3].

Prevention of Postoperative Nausea and Vomiting

• PO (Adults): 40 mg given within 3 hr prior to induction of anesthesia.

Emend

• Acts as a selective antagonist at substance P/neurokinin 1 (NK₁) receptors in the brain.

• Decreased nausea and vomiting associated with chemotherapy.
• Augments the antiemetic effects of dexamethasone and 5-HT₃ antagonists.

Therapeutic Classification: antiemetics

Pharmacologic Classification: neurokinin antagonists

Absorption: 60–65% absorbed following oral administration. Following IV administration, fosaprepitant is rapidly converted to aprepitant, the active component. IV administration results in complete bioavailability.

Distribution: Crosses the blood brain barrier; remainder of distribution unknown.

Protein Binding: 95–99%.

Metabolism/Excretion: Mostly metabolized by the liver (CYP3A4 enzyme system); not renally excreted.

Half-life: Aprepitant — 9–13 hr.

(antiemetic effect)

*Blood level.

• Instruct patient to take aprepitant as directed. Direct patient to read the Patient Package Insert before starting therapy and each time Rx renewed in case of changes.
• Instruct patient to notify health care professional if nausea and vomiting occur prior to administration.
• Advise patient to notify health care professional immediately if symptoms of hypersensitivity reaction (hives, rash, itching, redness of the face/skin, difficulty in breathing or swallowing) occur.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
• Advise patient and family to use general measures to decrease nausea (begin with sips of liquids and small, non-greasy meals; provide oral hygiene; remove noxious stimuli from environment).
• Rep: Caution patient that aprepitant and fosaprepitant may decrease effectiveness of oral contraceptives. Advise patient to use alternate nonhormonal methods of contraception during and for 1 mo following treatment. Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.

fos-a-PREP-i-tant

NDC Code^*

• 0591- Actavis Pharma, Inc.
  • 0591-4385- Fosaprepitant
    • 0591-4385-79- 1 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION in 1 CARTON (0591-4385-79)

• 43598- Dr. Reddy's Laboratories Inc.,
  • 43598-859- Fosaprepitant
    • 43598-859-11- 1 VIAL in 1 CARTON (43598-859-11) > 1 mL in 1 VIAL

• 60505- Apotex Corp
  • 60505-6105- Fosaprepitant
    • 60505-6105-1- 1 VIAL, SINGLE-DOSE in 1 CARTON (60505-6105-1) > 5 mL in 1 VIAL, SINGLE-DOSE

• 63323- Fresenius Kabi USA, LLC
  • 63323-972- Fosaprepitant
    • 63323-972-10- 1 VIAL, SINGLE-DOSE in 1 CARTON (63323-972-10) > 10 mL in 1 VIAL, SINGLE-DOSE

• 67457- Mylan Institutional LLC
  • 67457-889- fosaprepitant
    • 67457-889-10- 1 VIAL, SINGLE-DOSE in 1 CARTON (67457-889-10) > 5 mL in 1 VIAL, SINGLE-DOSE

• 68001- BluePoint Laboratories
  • 68001-421- Fosaprepitant
    • 68001-421-22- 1 VIAL, SINGLE-DOSE in 1 CARTON (68001-421-22) > 5 mL in 1 VIAL, SINGLE-DOSE

• 69097- Cipla USA Inc.
  • 69097-830- fosaprepitant
    • 69097-830-37- 1 VIAL, SINGLE-DOSE in 1 CARTON (69097-830-37) > 5 mL in 1 VIAL, SINGLE-DOSE

• 69539- MSN LABORATORIES PRIVATE LIMITED
  • 69539-034- Fosaprepitant
    • 69539-034-01- 1 VIAL, SINGLE-DOSE in 1 CARTON (69539-034-01) > 5 mL in 1 VIAL, SINGLE-DOSE

• 71288- Meitheal Pharmaceuticals Inc.
  • 71288-418- FOSAPREPITANT
    • 71288-418-10- 1 VIAL, SINGLE-DOSE in 1 CARTON (71288-418-10) > 5 mL in 1 VIAL, SINGLE-DOSE

• 71839- BE Pharmaceuticals Inc.
  • 71839-104- fosaprepitant
    • 71839-104-01- 1 VIAL, SINGLE-DOSE in 1 CARTON (71839-104-01) > 5 mL in 1 VIAL, SINGLE-DOSE

• 72205- Novadoz Pharmaceuticals LLC
  • 72205-026- Fosaprepitant
    • 72205-026-01- 1 VIAL, SINGLE-DOSE in 1 CARTON (72205-026-01) > 5 mL in 1 VIAL, SINGLE-DOSE