APONVIE Dosage & Rx Info | Uses, Side Effects

Aponvie Generic Name & Formulations

Legal Class

General Description

Aprepitant 32mg/4.4mL (7.2mg/mL); emulsion for IV inj; contains egg lecithin, ethanol, soybean oil, sucrose.

Pharmacological Class

Substance P/NK₁ receptor antagonist.

How Supplied

Single-dose vials—10

Manufacturer

Heron Therapeutics

Generic Availability

Mechanism of Action

Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK₁) receptors. Aprepitant has little or no affinity for serotonin (5-HT₃), dopamine, and corticosteroid receptors, the targets of existing therapies for postoperative nausea and vomiting (PONV). Aprepitant has been shown in animal models to inhibit emesis via central actions.

Aponvie Indications

Indications

Prevention of postoperative nausea and vomiting (PONV).

Limitations of Use

Not for treating established nausea and vomiting.

Aponvie Dosage and Administration

Adult

Give prior to induction of anesthesia. 32mg IV over 30secs. Flush with normal saline prior to and after administration.

Children

Not established.

Aponvie Contraindications

Contraindications

Concomitant pimozide.

Aponvie Boxed Warnings

Not Applicable

Aponvie Warnings/Precautions

Warnings/Precautions

Monitor for hypersensitivity reactions; discontinue and treat appropriately if occur; do not reinitiate if symptoms developed with previous use. Severe hepatic impairment. Pregnancy: avoid. Advise females of reproductive potential using hormonal contraceptives to use an effective alternative or back-up non-hormonal contraception for 1 month after administration. Nursing mothers.

Aponvie Pharmacokinetics

Absorption

Following administration of a single IV 32 mg dose to healthy subjects, mean (CV%) area under the plasma concentration-time curve (AUC_0-∞) was 7.8 (27.4%) mcg·hr/mL and mean plasma concentration at 5 mins postdose was 2.1 (19%) mcg/mL.

Distribution

Plasma protein bound: >99%. Mean volume of distribution: ~72 L.

Metabolism

Hepatic (primarily CYP3A4), (minor CYP1A2, CYP2C19).

Elimination

Half-life: 12 hours. Mean plasma clearance: 4.4 L/h.

Aponvie Interactions

Interactions

See Contraindications. Avoid concomitant strong CYP3A4 inhibitors (eg, ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir) or strong CYP3A4 inducers (eg, carbamazepine, phenytoin, rifampin). May antagonize warfarin (closely monitor INR for 2 weeks after starting each cycle), other CYP2C9 substrates, oral contraceptives (use alternative or backup methods [eg, condoms, spermicides]).

Aponvie Adverse Reactions

Adverse Reactions

Constipation, fatigue, headache.

Aponvie Clinical Trials

See Literature

Aponvie Note