aprepitant (Rx)

Brand and Other Names:Emend, fosaprepitant
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule (aprepitant)

  • 40mg
  • 80mg
  • 125mg

powder for injection (fosaprepitant)

  • 150mg

oral suspension

  • 125mg/pouch (once pouch is mixed with 4.6 mL drinking water, resulting suspension yields 25mg/mL)
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Chemotherapy-Induced Nausea & Vomiting

Indicated for prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin; also indicated for nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC)

Use in combination with other antiemetics

IV

  • HEC
    • Day 1: 150 mg IV infused over 20-30 minutes ~30 minutes before chemotherapy plus dexamethasone 12 mg PO and a 5-HT3 antagonist
    • Day 2: Dexamethasone 8 mg PO in AM
    • Days 3 and 4: Dexamethasone 8 mg PO BID (morning and evening)
    • Note: A 50% dosage reduction of dexamethasone on Days 1 and 2 is recommended to account for a drug interaction with aprepitant
  • MEC
    • Day 1: 150 mg IV infused over 20-30 minutes ~30 minutes before chemotherapy plus dexamethasone 12 mg PO and a 5-HT3 antagonist

Oral

  • Day 1: 125 mg PO 1 hr prior to chemotherapy plus dexamethasone 12 mg PO (30 minutes before chemotherapy) and a 5-HT3 antagonist
  • Days 2-3: 80 mg PO 1 hr prior to chemotherapy plus dexamethasone 8 mg PO qAM
  • Day 4: Dexamethasone 8 mg PO in AM

Postoperative Nausea & Vomiting

Indicated for prevention of PONV

40 mg PO within 3 hr prior to anesthesia induction

Dosage Forms & Strengths

capsule (aprepitant)

  • 80mg
  • 125mg

oral suspension

  • 125mg/pouch (once pouch is mixed with 4.6 mL drinking water, resulting suspension yields 25mg/mL)

Chemotherapy-Induced Nausea & Vomiting

Indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin, and for moderately emetogenic cancer chemotherapy (MEC)

Capsule: Aged <12 years and weight <30 kg: Safety and efficacy not established

Oral suspension: Aged <6 months: Safety and efficacy not established

Capsule for aged ≥12 years or <12 years and weight ≥30 kg

  • Day 1: 125 mg PO 1 hr prior to chemotherapy plus dexamethasone 12 mg PO (30 minutes before chemotherapy) and a 5-HT3 antagonist
  • Days 2 and 3: 80 mg PO 1 hr prior to chemotherapy plus dexamethasone 8 mg PO qAM
  • Day 4: Dexamethasone 8 mg PO in AM

Oral suspension for aged ≥6 months to <12 years

  • Day 1: 3 mg/kg PO 1 hr prior to chemotherapy Days 2 and 3: 2 mg/kg PO 1 hr prior to chemotherapy
  • Administer with concomitant dexamethasone and 5-HT3 antagonist (eg, ondansetron)

Dosing Considerations

Children must be able to swallow capsule whole

Has not been studied for treatment of established nausea and vomiting

Chronic continuous administration is not recommended because it has not been studied, and because the drug interaction profile may change during chronic continuous use

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Interactions

Interaction Checker

and aprepitant

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            CINV: generally similar to standard treatments

            PONV: generally similar to ondansetron

            >10% (only seen in CINV)

            Headache

            Asthenia/fatigue

            Anorexia

            Constipation

            Diarrhea

            Nausea

            Alopecia

            Hiccups

            1-10% (selected)

            Dizziness

            Insomnia

            Bradycardia

            Hypotension

            Pharyngolargeal pain

            Mucosal inflammation

            Stomatitis

            Dyspepsia

            Anemia

            Neutropenia

            Hot flash

            Pruritus

            Dehydration

            Fever

            Postmarketing Reports

            Rash, urticaria, rarely Stevens-Johnson syndrome/toxic epidermal necrolysis; ifosfamide-induced neurotoxicity reported after aprepitant and ifosfamide coadministration

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            Warnings

            Contraindications

            Hypersensitivity

            Concomitant pimozide, terfenadine (discontinued), astemizole (discontinued), cisapride

            Cautions

            Not indicated for treatment

            Severe hepatic impairment (Child-Pugh score >9)

            Decreased corticosteroid dose by 25% (IV) or 50% (PO) on days aprepitant is administered

            May reduce efficacy of oral contraceptives - alternatives recommended during and for 1 month after last aprepitant dose

            CYP3A4 inhibitor and CYP2C9 inducer

            IV: Isolated reports of immediate hypersensitivity reactions including flushing, erythema, and dyspnea during infusion of fosaprepitant; discontinuation infusion and do reinitiate

            Injection is incompatible with divalent cation-containing solutions

            Severe and disabling arthralgia reported in patients taking DPP-4 inhibitors; consider as a possible cause for severe joint pain and discontinue drug if appropriate

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            Pregnancy & Lactation

            Pregnancy Category: B

            Lactation: It is not known whether this drug is excreted in milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Substance P/neurokinin 1 (NK1) receptor antagonist

            Absorption

            Bioavailability: 60-65% (PO)

            Peak plasma time

            • 125 mg PO once: 4 hr
            • 80 mg PO twice: 4 hr
            • 40 mg PO once: 3 hr

            Peak plasma concentration

            • 125 mg PO once: 1.6 mcg/mL
            • 80 mg PO twice: 1.4 mcg/mL
            • 40 mg PO once: 0.7 mcg/mL
            • 150 mg IV once: 4.15 mcg/mL

            AUC

            • 125 mg PO once: 19.6 mcg·hr/mL
            • 80 mg PO twice: 21.2 mcg·hr/mL
            • 150 mg IV once: 37.38 mcg·hr/mL

            Distribution

            Protein bound: >95%

            Vd: 70 L

            Metabolism

            Hepatic CYP3A4 (major); CYP1A2, CYP2C19 (minor)

            Fosaprepitant (IV form) rapidly converted to aprepitant in vivo

            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

            Dialyzable: No

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            Administration

            IV Incompatibilities

            Divalent cation-containing solutions (Ca++, Mg++, Zn++ etc), eg, LR

            IV Preparation

            Aseptically inject 5 mL 0.9% NaCl into vial along the vial wall in order to prevent foaming; avoid jetting the 0.9% NaCl into the vial

            Gently swirl to dissolve; do not shake

            Aseptically withdraw entire volume from vial and transfer it into a prepared infusion bag of 145 mL 90.9% NaCl to yield a total volume of 150 mL and a final concentration of 1 mg/mL

            Gently invert bag 2-3 times to mix

            Stable for 24 hr at ambient room temperature (ie, ≤25°C [77°F])

            IV Administration

            Infuse IV over 20-30 min

            Do not mix with other drugs

            Oral Administration

            Take with or without food

            Capsule: Swallow capsule whole

            Oral suspension

            • Dose is prepared by a pharmacist and dispensed to the patient or caregiver in an oral dispenser/oral syringe; once pouch is mixed with 4.6 mL drinking water, the resulting concentration is 25 mg/mL
            • Keep the dispenser in the refrigerator until administered to the patient
            • The dose can be stored at room temperature for up to 3 hr before use
            • When ready to use, take the cap off the dispenser, place the dispenser in the patient’s mouth along the inner cheek on either the right or left side
            • Slowly administer the medicine along the inner cheek
            • Use dose within 72 hr of preparation
            • Discard any doses remaining after 72 hr

            Storage

            Oral suspension

            • Unopened pouch
              • 20-25°C (68-77°F); excursions permitted between 15-30°C (between 59-86°F)
              • Store in the original container
              • Do not open pouch until ready to prepare for use
            • Prepared dose
              • If the dose is not administered immediately after measuring, store filled oral dosing dispenser(s) in the refrigerator (between 36-46°F [2-8°C]) for up to 72 hr prior to use
              • When dispensing dose(s) to the patient or caregiver, instruct them to refrigerate the oral dosing dispenser(s) until they are ready to administer the dose
              • When ready to use, the mixture can be kept at room temperature (68-77°F [20°C-25°C]) for up to 3 hr
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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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