Aponvie Generic Name & Formulations
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.
Prevention of postoperative nausea and vomiting (PONV).
Limitations of Use
Not for treating established nausea and vomiting.
Aponvie Dosage and Administration
Give prior to induction of anesthesia. 32mg IV over 30secs. Flush with normal saline prior to and after administration.
Aponvie Boxed Warnings
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.
Following administration of a single IV 32 mg dose to healthy subjects, mean (CV%) area under the plasma concentration-time curve (AUC0-∞) was 7.8 (27.4%) mcg·hr/mL and mean plasma concentration at 5 mins postdose was 2.1 (19%) mcg/mL.
Plasma protein bound: >99%. Mean volume of distribution: ~72 L.
Half-life: 12 hours. Mean plasma clearance: 4.4 L/h.
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
Constipation, fatigue, headache.
Aponvie Clinical Trials
Aponvie Patient Counseling