APREPITANT

Other

Brand names: APREPITANT

Oral

Mechanism of Action

12.1 MECHANISM OF ACTION Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK 1 ) receptors. Aprepitant has little or no affinity for serotonin (5-HT 3 ), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with aprepitant have shown that it crosses the blood brain barrier and occupies brain NK 1 receptors. Animal and human studies show that aprepitant augments the antiemetic activity of the 5-HT 3 -receptor antagonist ondansetron and the corticosteroid dexamethasone and inhibits both the acute and delayed phases of cisplatin-induced emesis.

Indications

1 INDICATIONS AND USAGE Aprepitant is a substance P/neurokinin 1 (NK1) receptor antagonist. Aprepitant capsules are indicated • in combination with other antiemetic agents

Contraindications

• potentially causing serious or life-threatening reactions
• such as QT prolongation
• a known adverse reaction of pimozide [see Warnings and Precautions ( 5.1 )] . • Known hypersensitivity to any component of this drug. ( 4 ) • Concurrent use with pimozide. ( 4 )

FDA Warnings

5 WARNINGS AND PRECAUTIONS • CYP3A4 Interactions : Aprepitant is a substrate, weak-to-moderate inhibitor and inducer of CYP3A4; See Full Prescribing Information for recommendations regarding contraindications, risk of adverse reactions, and dosage adjustments of aprepitant and concomitant drugs
2 ) • Warfarin (a CYP2C9 substrate) : Risk of decreased INR of prothrombin time; monitor INR in 2-week period, particularly at 7 to 10 days, following initiation of aprepitant
Use of pimozide with aprepitant is contraindicated due to the risk of significantly increased plasma concentrations of pimozide, potentially resulting in prolongation of the QT interval, a known adverse reaction of pimozide [see Contraindications ( 4 )]
, ketoconazole, diltiazem) may increase plasma conentrations of aprepitant and result in an increased risk of adverse reactions related to aprepitant

Known Side Effects

10 documented side effects by frequency

Nausea

>10%

Fatigue

1-10%

Fever

1-10%

Diarrhea

1-10%

Shortness of Breath

1-10%

Vomiting

1-10%

Hair Loss

1-10%

Rash

1-10%

Decreased Appetite

1-10%

Itching

1-10%

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Formulations

Dosage Forms

Tablet

Route

Oral