Aponvie
(Aprepitant)Dosage & Administration
The recommended dose is 32 mg administered as a 30 second intravenous injection prior to induction of anesthesia. (
The recommended dose in adults of APONVIE is 32 mg administered as a 30 second intravenous injection prior to induction of anesthesia.
By using PrescriberAI, you agree to the AI Terms of Use.
Aponvie Prescribing Information
APONVIE is indicated for the prevention of postoperative nausea and vomiting (PONV) in adults.
The recommended dose is 32 mg administered as a 30 second intravenous injection prior to induction of anesthesia. (
The recommended dose in adults of APONVIE is 32 mg administered as a 30 second intravenous injection prior to induction of anesthesia.
Injectable emulsion: 32 mg/4.4 mL (7.2 mg/mL) aprepitant as an opaque, off-white to amber emulsion, in a single-dose vial.
There are insufficient data on aprepitant use in pregnant women to identify a drug-associated risk of major birth defects, miscarriage or other adverse maternal or fetal outcomes. Avoid use of APONVIE in pregnant women due to the alcohol content
The background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.
APONVIE contains alcohol. Published studies have demonstrated that alcohol is associated with fetal harm including central nervous system abnormalities, behavioral disorders, and impaired intellectual development. There is no safe level of alcohol exposure in pregnancy; therefore, avoid use of APONVIE in pregnant women.
In embryofetal development studies in rats and rabbits, aprepitant was administered during the period of organogenesis at oral doses up to 1000 mg/kg twice daily (rats) and up to the maximum tolerated dose of 125 mg/kg/day (rabbits). No embryofetal lethality or malformations were observed at any dose level in either species. The exposures (AUC) in pregnant rats at 1000 mg/kg twice daily and in pregnant rabbits at 125 mg/kg/day were approximately 4.8 times the exposure at the recommended human dose of APONVIE. Aprepitant crosses the placenta in rats and rabbits.
APONVIE is contraindicated in patients:
- with a history of hypersensitivity to aprepitant or any component of the product [see. Hypersensitivity reactions have included anaphylaxis]
11 DESCRIPTIONAPONVIE injectable emulsion contains the active ingredient, aprepitant. Aprepitant is a substance P/neurokinin 1 (NK1) receptor antagonist, an antiemetic agent, and chemically described as 5-[[(2
R,3S)-2-[(1R)-1-[3,5bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one.Its empirical formula is C23H21F7N4O3, and its structural formula is:
Aprepitant is a white to off-white crystalline solid, with a molecular weight of 534.43. It is practically insoluble in water. Aprepitant is sparingly soluble in ethanol and isopropyl acetate and slightly soluble in acetonitrile.
APONVIE (aprepitant) injectable emulsion is a sterile, opaque, off-white to amber liquid in a single-dose vial for intravenous use. Each vial contains 32 mg aprepitant in 4.4 mL of emulsion. The emulsion also contains the following inactive ingredients: dehydrated alcohol (125 mg), egg lecithin (636 mg), sodium oleate (21 mg), soybean oil (424 mg), sucrose (238 mg), and water for injection (2968 mg).
Chemical Structure [see.]5.1 Hypersensitivity ReactionsSerious hypersensitivity reactions, including anaphylaxis, during or soon after administration of aprepitant have occurred. Symptoms including dyspnea, eye swelling, flushing, pruritus, and wheezing have been reported
[see Adverse Reactions (6.2)].Monitor patients during and after administration. If hypersensitivity reactions occur, administer appropriate medical therapy. Do not administer APONVIE in patients who experience these symptoms with previous use of aprepitant.
- taking pimozide. Inhibition of CYP3A4 by aprepitant could result in elevated plasma concentrations of pimozide, which is a CYP3A4 substrate, potentially causing serious or life-threatening reactions, such as QT prolongation, a known adverse reaction of pimozide [see.]
7.1 Effect of Aprepitant on the Pharmacokinetics of Other DrugsAprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9
[see Clinical Pharmacology (12.3)].Table 2 includes drug interactions affecting drugs co-administered with APONVIE and instructions for preventing or managing them.
Table 2: Drug Interactions Affecting Drugs When Co-Administered with APONVIE PimozideClinical ImpactIncreased pimozide exposure. InterventionAPONVIE is contraindicated [see Contraindications (4)].Hormonal ContraceptivesClinical ImpactDecreased hormonal exposure for 28 days after administration of APONVIE [see Warnings and Precautions (5.3), Use in Specific Populations (8.3), and Clinical Pharmacology (12.3)].InterventionEffective alternative or back-up methods of contraception (such as condoms and spermicides) should be used for 1 month following administration of APONVIE. Examplesbirth control pills, transdermal systems, implants, and certain intrauterine systems CYP2C9 SubstratesWarfarinClinical ImpactDecreased warfarin exposure and decreased prothrombin time (INR) [see Warnings and Precautions (5.2)and Clinical Pharmacology (12.3)].InterventionIn patients on chronic warfarin therapy, monitor prothrombin time (INR) in the 2-week period, particularly at 7 to 10 days, following administration of APONVIE. Other Antiemetic Agents5-HT3AntagonistsClinical ImpactNo change in the exposure of the 5-HT3antagonist [see Clinical Pharmacology (12.3)].InterventionNo dosage adjustment needed. Examplesondansetron, granisetron, dolasetron CorticosteroidsClinical ImpactNo clinically significant change in the exposure of dexamethasone or methylprednisolone [see Clinical Pharmacology (12.3)].InterventionNo dosage adjustment needed.
- Hypersensitivity Reactions (including anaphylaxis): May occur during or soon after administration. If symptoms occur, administer appropriate medical therapy. (,
4 CONTRAINDICATIONSAPONVIE is contraindicated in patients:
- with a history of hypersensitivity to aprepitant or any component of the product[see Description (11)]. Hypersensitivity reactions have included anaphylaxis[see Warnings and Precautions (5.1)].
- taking pimozide. Inhibition of CYP3A4 by aprepitant could result in elevated plasma concentrations of pimozide, which is a CYP3A4 substrate, potentially causing serious or life-threatening reactions, such as QT prolongation, a known adverse reaction of pimozide[see Drug Interactions (7.1)].
- Known hypersensitivity to any component of this product.
- Concurrent use with pimozide.
)5.1 Hypersensitivity ReactionsSerious hypersensitivity reactions, including anaphylaxis, during or soon after administration of aprepitant have occurred. Symptoms including dyspnea, eye swelling, flushing, pruritus, and wheezing have been reported
[see Adverse Reactions (6.2)].Monitor patients during and after administration. If hypersensitivity reactions occur, administer appropriate medical therapy. Do not administer APONVIE in patients who experience these symptoms with previous use of aprepitant.
- with a history of hypersensitivity to aprepitant or any component of the product
- CYP3A4 Interactions: Aprepitant is a substrate, weak-to-moderate inhibitor, and inducer of CYP3A4; see full prescribing information. (,
5.2 Clinically Significant CYP3A4 Drug InteractionsAprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4.
- Use of pimozide, a CYP3A4 substrate, with APONVIE is contraindicated[see Contraindications (4)].
- Use of APONVIE with strong CYP3A4 inhibitors (e.g., ketoconazole) may increase plasma concentrations of aprepitant and result in an increased risk of adverse reactions related to APONVIE[see Drug Interactions (7.2)].
- Use of APONVIE with strong CYP3A4 inducers (e.g., rifampin) may result in a reduction in aprepitant plasma concentrations and decreased efficacy of APONVIE[see Drug Interactions (7.2)].
)7.2 Effect of Other Drugs on the Pharmacokinetics of AprepitantAprepitant is a CYP3A4 substrate
[see Clinical Pharmacology (12.3)]. Table 3 includes drug interactions affecting APONVIE when co-administered with other drugs and instructions for preventing them.Table 3: Drug Interactions Affecting APONVIE When Co-Administered with Other Drugs Strong CYP3A4 InhibitorsClinical ImpactSignificantly increased exposure of aprepitant may increase the risk of adverse reactions associated with APONVIE [see Clinical Pharmacology (12.3)].InterventionAvoid concomitant use of APONVIE. Examplesketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, nelfinavir Strong CYP3A4 InducersClinical ImpactSubstantially decreased exposure of aprepitant in patients chronically taking a strong CYP3A4 inducer may decrease the efficacy of APONVIE [see Clinical Pharmacology (12.3)].InterventionAvoid concomitant use of APONVIE. Examplesrifampin, carbamazepine, phenytoin - Use of pimozide, a CYP3A4 substrate, with APONVIE is contraindicated
- Warfarin (a CYP2C9 substrate): Risk of decreased INR of prothrombin time; monitor INR in 2-week period, particularly at 7 to 10 days, following administration of APONVIE. (,
5.3 Decrease in INR with Concomitant WarfarinUse of aprepitant with warfarin, a CYP2C9 substrate, may result in a clinically significant decrease in the International Normalized Ratio (INR) of prothrombin time
[see Clinical Pharmacology (12.3)]. Monitor the INR in patients on chronic warfarin therapy in the 2-week period, particularly at 7 to 10 days, following administration of APONVIE[see Drug Interactions (7.1)].)7.1 Effect of Aprepitant on the Pharmacokinetics of Other DrugsAprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9
[see Clinical Pharmacology (12.3)].Table 2 includes drug interactions affecting drugs co-administered with APONVIE and instructions for preventing or managing them.
Table 2: Drug Interactions Affecting Drugs When Co-Administered with APONVIE PimozideClinical ImpactIncreased pimozide exposure. InterventionAPONVIE is contraindicated [see Contraindications (4)].Hormonal ContraceptivesClinical ImpactDecreased hormonal exposure for 28 days after administration of APONVIE [see Warnings and Precautions (5.3), Use in Specific Populations (8.3), and Clinical Pharmacology (12.3)].InterventionEffective alternative or back-up methods of contraception (such as condoms and spermicides) should be used for 1 month following administration of APONVIE. Examplesbirth control pills, transdermal systems, implants, and certain intrauterine systems CYP2C9 SubstratesWarfarinClinical ImpactDecreased warfarin exposure and decreased prothrombin time (INR) [see Warnings and Precautions (5.2)and Clinical Pharmacology (12.3)].InterventionIn patients on chronic warfarin therapy, monitor prothrombin time (INR) in the 2-week period, particularly at 7 to 10 days, following administration of APONVIE. Other Antiemetic Agents5-HT3AntagonistsClinical ImpactNo change in the exposure of the 5-HT3antagonist [see Clinical Pharmacology (12.3)].InterventionNo dosage adjustment needed. Examplesondansetron, granisetron, dolasetron CorticosteroidsClinical ImpactNo clinically significant change in the exposure of dexamethasone or methylprednisolone [see Clinical Pharmacology (12.3)].InterventionNo dosage adjustment needed. - Hormonal Contraceptives: Efficacy of contraceptives may be reduced for 28 days following administration of aprepitant. Use effective alternative or back-up methods of non-hormonal contraception. (,
5.4 Risk of Reduced Efficacy of Hormonal ContraceptivesThe efficacy of hormonal contraceptives may be reduced for 28 days following administration of APONVIE
[see Clinical Pharmacology (12.3)]. Advise patients to use effective alternative or back-up methods of non-hormonal contraception for 1 month following administration of APONVIE[see Drug Interactions (7.1)and Use in Specific Populations (8.3)].,7.1 Effect of Aprepitant on the Pharmacokinetics of Other DrugsAprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9
[see Clinical Pharmacology (12.3)].Table 2 includes drug interactions affecting drugs co-administered with APONVIE and instructions for preventing or managing them.
Table 2: Drug Interactions Affecting Drugs When Co-Administered with APONVIE PimozideClinical ImpactIncreased pimozide exposure. InterventionAPONVIE is contraindicated [see Contraindications (4)].Hormonal ContraceptivesClinical ImpactDecreased hormonal exposure for 28 days after administration of APONVIE [see Warnings and Precautions (5.3), Use in Specific Populations (8.3), and Clinical Pharmacology (12.3)].InterventionEffective alternative or back-up methods of contraception (such as condoms and spermicides) should be used for 1 month following administration of APONVIE. Examplesbirth control pills, transdermal systems, implants, and certain intrauterine systems CYP2C9 SubstratesWarfarinClinical ImpactDecreased warfarin exposure and decreased prothrombin time (INR) [see Warnings and Precautions (5.2)and Clinical Pharmacology (12.3)].InterventionIn patients on chronic warfarin therapy, monitor prothrombin time (INR) in the 2-week period, particularly at 7 to 10 days, following administration of APONVIE. Other Antiemetic Agents5-HT3AntagonistsClinical ImpactNo change in the exposure of the 5-HT3antagonist [see Clinical Pharmacology (12.3)].InterventionNo dosage adjustment needed. Examplesondansetron, granisetron, dolasetron CorticosteroidsClinical ImpactNo clinically significant change in the exposure of dexamethasone or methylprednisolone [see Clinical Pharmacology (12.3)].InterventionNo dosage adjustment needed. )8.3 Females and Males of Reproductive PotentialContraceptionUpon administration of APONVIE, the efficacy of hormonal contraceptives may be reduced. Advise females of reproductive potential using hormonal contraceptives to use an effective alternative or back-up non-hormonal contraceptive (such as condoms or spermicides) for 1 month following administration of APONVIE
[see Warnings and Precautions (5.4), Drug Interactions (7.1), and Clinical Pharmacology (12.3)].