Aprepitant (Cinvanti, Emend) - Indications, Dosage, Brands

Aprepitant prevents acute and delayed vomiting by inhibiting the substance P/neurokinin 1 (NK ) receptor.

Aprepitant intravenous (Cinvanti) is used to treat the following conditions:

  • Use in prevention of chemotherapy-induced nausea and vomiting:

    • It can be used in prevention of nausea and vomiting associated with highly emesis inducing chemotherapy e.g high-dose cisplatin in adults.

    • It is also used in prevention of nausea and vomiting associated with moderately emetogenic chemotherapy in adults.

    • It is mostly used in combination with other anti emetics.

Aprepitant Oral(Emend) is used to treat the following conditions:

  • Prevention of chemotherapy-induced nausea and vomiting:

    • It is used to prevent acute and delayed nausea and vomiting associated with highly emetogenic chemotherapy.

    • It is used to prevent nausea and vomiting associated with moderately emetogenic chemotherapy.

    • It is mostly used in combination with other anti emetics

    • In patients older than 12 years it is used as capsule form and in patients older than 6 months as oral suspension.

Aprepitant Dose in Adults

Prevention of chemotherapy-induced nausea and vomiting:

  • Prevention of acute and delayed nausea & vomiting associated with highly emetogenic chemotherapy:

    • 130 mg is given I/V over 30 minutes.
    •  It is given prior to chemotherapy on day 1 along with a 5- HT antagonist antiemetic on day 1 only and oral dexamethasone on days 1 to 4.
    • Capsules:

      • 125 mg is given orally 1 hour prior to chemotherapy on the first day.

      • It is then followed by 80 mg OD on days 2 and 3

      •      It is given along with a 5- HT-3 antagonist antiemetic on day 1 only and oral  dexamethasone on days 1 to 4
    • Suspension:

      • It is used in adults who are unable to swallow capsules

      • Dose is 3 mg/kg (maximum: 125 mg/dose)

      • It is given 1 hour prior to chemotherapy on day 1, followed by 2 mg/kg (maximum: 80 mg/dose) once daily on days 2 and 3

      •  It is used along with a 5- HT antagonist antiemetic on day 1 only and oral dexamethasone on days 1 to 4

Prevention of nausea & vomiting associated with moderately-emetogenic chemotherapy:

  • 100 mg intravenous is given over 30 minutes prior to chemotherapy on day 1
  • It is used in combination with oral aprepitant 80 mg on days 2 and 3, a 5-HT-3 antagonist and dexamethasone on day 1 only.
    • Capsules:

      • 125 mg is given 1 hour before chemotherapy on day 1

      • It is followed by 80 mg once daily on days 2 and 3

      • It is used in combination with a 5-HT-3 antagonist antiemetic and dexamethasone on day 1

    • Suspension:
      • It is used in adults who are unable to swallow capsules
      • 3 mg/kg (maximum: 125 mg/dose) can be given 1 hour prior to chemotherapy on day 1.
      • It is followed by 2 mg/kg (maximum: 80 mg/dose) once daily on days 2 and 3
      • It is used in combination with a 5- HT antagonist antiemetic and dexamethasone on day 1

Guideline recommendations:

  • Prevention of nausea & vomiting associated with highly emetogenic chemotherapy (including anthracycline and cyclophosphamide [AC] regimens):

  •  Oral:
    • American Society of Clinical Oncology :
      • 125 mg is given before chemotherapy on day 1
      • It is followed by 80 mg once daily on days 2 and 3.
      • It is used along with a 5-HT antagonist antiemetic on day 1 and dexamethasone on days 1 to 4 or days 1 to 3.
  • Multinational Association of Supportive Care in Cancer and European Society of Medical Oncology :
    • 125 mg is given before chemotherapy on day 1
    • It is followed by 80 mg once daily on days 2 and 3
    • It is used in combination with dexamethasone and a 5-HT-3 antagonist antiemetic on day 1, followed by dexamethasone for 3 to 4 more days

Prevention of postoperative nausea and vomiting:

  • 40 mg dose via oral route can be given within 3 hours prior to anesthesia induction.

Aprepitant Dose in Childrens

Prevention of highly and moderately emetogenic chemotherapy-induced nausea and vomiting, prevention:

  • It is used in combination with 5-HT-3 antagonist antiemetic with or without dexamethasone depending upon the age, chemotherapy-related vomiting, and drug-interaction profile.
  • Infants more than 6 months and children aged less than 12 years weighing 6-30 kg:
    • Oral suspension:
      • 3 mg/kg is given 1 hour prior to chemotherapy on day 1
      • It is followed by 2 mg/kg/dose OD daily on days 2 and 3
  • Children aged less than 12 years weighing more than 30 kgs & Children aged more than 12 years, and adolescents:
    • Capsules, Oral suspension:
      • 125 mg is administered 1 hour prior to chemotherapy on day 1
      • It is followed by 80 mg once daily on days 2 and 3.

Preganancy Risk Factor: B

  • Animal reproduction studies did not show any adverse events.
  • The injection formulation contains ethanol.
  • Females who are pregnant should avoid using it.
  • The effectiveness of hormonal contraceptives could be decreased during and for 28 consecutive days after the last aprepitant dosage.
  • You should plan for substitute or other effective contraceptives during fosaprepitant treatment and for at most 30 days after the last dose.

Breast-feeding with Aprepitant:

  • It is not known if breast milk contains aprepitant.
  • According to the manufacturer of the product, when deciding whether to breastfeed during therapy, one should consider the risks to infants, the benefits to breastfeeding to infants, and the benefits to mother.

Aprepitant Dose in Renal Disease:

  • No dosage adjustment is necessary.

Aprepitant Dose in Liver Disease:

  • Mild to moderate impairment (Child-Pugh class A or B):
    • No dosage adjustment necessary.
  • Severe impairment (Child-Pugh class C):
    • Use with caution.
    • Limited data are available (may require additional monitoring for adverse reactions).

Common Side Effects of Aprepitant Include:

  • Central nervous system:
    • Fatigue
  • Hematologic & oncologic:
    • Neutropenia

Less Common Side effects of Aprepitant Include:

  • Cardiovascular:
    • Hypotension
    • Bradycardia
    • Flushing
    • Palpitations
    • Peripheral Edema
    • Syncope
  • Central Nervous System:
    • Headache
    • Dizziness
    • Anxiety
    • Hypoesthesia
    • Hypothermia
    • Malaise
    • Peripheral Neuropathy
    • Abnormal Behavior
    • Agitation
  • Dermatologic:
    • Pruritus
    • Alopecia
    • Hyperhidrosis
    • Skin Rash
    • Urticaria
  • Endocrine & Metabolic:
    • Dehydration
    • Decreased Serum Albumin
    • Decreased Serum Potassium
    • Decreased Serum Sodium
    • Hot Flash
    • Hypokalemia
    • Hypovolemia
    • Increased Serum Glucose
    • Weight Loss
  • Gastrointestinal:
    • Constipation
    • Diarrhea
    • Dyspepsia
    • Abdominal Pain
    • Hiccups
    • Decreased Appetite
    • Dysgeusia
    • Eructation
    • Flatulence
    • Gastritis
    • Gastroesophageal Reflux Disease
    • Nausea
    • Vomiting
    • Xerostomia
  • Genitourinary:
    • Proteinuria
  • Hematologic & Oncologic:
    • Decreased Hemoglobin
    • Decreased White Blood Cell Count
    • Anemia
    • Febrile Neutropenia
    • Hematoma
    • Thrombocytopenia
  • Hepatic:
    • Increased Serum ALT
    • Increased Serum Alkaline Phosphatase
    • Increased Serum AST
    • Increased Serum Bilirubin
  • Infection:
    • Candidiasis
    • Postoperative Infection
  • Local:
    • Induration At Injection Site
    • Inflammation At Injection Site
    • Infusion Site Reaction
  • Neuromuscular & Skeletal:
    • Weakness
    • Musculoskeletal Pain
  • Renal:
    • Increased Blood Urea Nitrogen
  • Respiratory:
    • Cough
    • Dyspnea
    • Hypoxia
    • Oropharyngeal Pain
    • Pharyngitis
    • Respiratory Depression
  • Miscellaneous:
    • Wound Dehiscence

Contraindication to Aprepitant Include:

  • Allergies to aprepitant and any component of the formulation
  • Concurrent use with pimozide or astemizole, and terfenadine.

Warnings and Precautions

  • Hypersensitivity
    • Reports of hypersensitivity reactions including anaphylactic reactions have been made.
    • Dyspnea and erythema are symptoms.
    • Monitor for hypersensitivity reactions during and after infusion.
    • If you experience a reaction, stop the infusion immediately and take appropriate measures.
    • Do not re-initiate.
  • Hepatic impairment
    • Patients with severe hepatic impairment (Child Pugh class C) should be cautious.

Aprepitant: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use  

Risk Factor C (Monitor therapy).
Abemaciclib Moderate CYP3A4 inhibitors may raise serum levels of Abemaciclib.
AmLODIPine Moderate CYP3A4 inhibitors may raise serum levels of AmLODIPine.
Apixaban Moderate CYP3A4 inhibitors may raise the serum Apixaban concentration.
ARIPiprazole Moderate CYP3A4 inhibitors may cause a higher serum level of ARIPiprazole. Monitoring for increased pharmacologic effects of Aripiprazole is important. Aripiprazole dosage adjustments may be necessary depending on the indication and concomitant therapy. For more information, consult the full interaction monograph.
Benzhydrocodone CYP3A4 Inhibitors Moderate may increase serum concentrations of Benzhydrocodone. Hydrocodone concentrations may increase.
Blonanserin Blonanserin may be increased by CYP3A4 inhibitors (Moderate).
Bosentan Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Bosentan CYP3A4 Moderate Inhibitors may cause an increase in serum Bosentan concentrations. Management: It is not recommended to use a CYP2C9 and a CYP3A9 inhibitor simultaneously. For more information, see monograph.
Brexpiprazole CYP3A4 Moderate Inhibitors may increase the serum level of Brexpiprazole. Management: Brexpiprazole should be taken at 25% if it is combined with a strong or moderate CYP3A4 and a strong or medium CYP2D6 inhibit, or if a moderate CYP3A4 inhibition is used in a CYP2D6 weak metabolizer.
Cannabidiol Moderate CYP3A4 inhibitors may raise the serum concentrations of Cannabidiol.
Cannabis CYP3A4 Moderate Inhibitors may increase the serum cannabis concentration. The serum concentrations of tetrahydrocannabinol or cannabidiol may increase.
Clofazimine High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Codeine CYP3A4 Moderate may lower serum levels of active metabolites of Codeine.
Moderate CYP3A4 Inducers Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
CYP3A4 Substrates: High risk with Inhibitors The serum concentration of CYP3A4 Substrates may be increased by apepitant (high risk when taking inhibitors).
Deferasirox Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Dofetilide Moderate CYP3A4 inhibitors may raise the serum level of Dofetilide.
Dronabinol Moderate CYP3A4 inhibitors may raise Dronabinol's serum concentration.
Estrogen Derivatives Moderate CYP3A4 Inhibitors may raise the serum Estrogen Derivatives concentration.
Halofantrine CYP3A4 Moderate Inhibitors may raise the serum level of Halofantrine. If halofantrine is mixed with moderate CYP3A4 inhibitions, extreme caution should be taken. Separate drug interaction monographs will be available for drugs that are listed as exceptions to the monograph.
HYDROcodone Moderate CYP3A4 inhibitors may raise serum levels of HYDROcodone.
Ifosfamide The serum concentrations of Ifosfamide may be increased by taking Aprepitant. Particularly, the concentrations of toxic metabolites may rise in ifosfamide.
Larotrectinib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Manidipine Moderate CYP3A4 Inhibitors may raise the serum level of Manidipine.
Mirodenafil Moderate CYP3A4 inhibitors may raise serum Mirodenafil concentrations.
Naldemedine Moderate CYP3A4 inhibitors may raise serum levels of Naldemedine.
Nalfurafine Moderate CYP3A4 inhibitors may raise serum levels of Nalfurafine.
NiMODipine Moderate CYP3A4 inhibitors may raise the serum level of NiMODipine.
OxyCODONE CYP3A4 Moderate Inhibitors may increase the toxic/adverse effects of OxyCODONE. CYP3A4 Moderate Inhibitors may increase OxyCODONE serum concentrations. The serum concentrations of Oxymorphone, an active metabolite, may be raised.
Palbociclib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
PARoxetine May lower the serum level of Aprepitant. PARoxetine may be decreased by Aprepitant.
Pimecrolimus Moderate CYP3A4 inhibitors may reduce the metabolism of Pimecrolimus.
Propafenone Moderate CYP3A4 inhibitors may raise the serum level of Propafenone. Management: The drug interactions monographs for drugs listed as an exception to this monograph will be discussed in greater detail.
Rupatadine CYP3A4 Inhibitors Moderate may increase serum Rupatadine concentrations.
Ruxolitinib CYP3A4 Inhibitors Moderate may increase serum Ruxolitinib.
Salmeterol Moderate CYP3A4 inhibitors may raise serum Salmeterol concentrations.
Sarilumab Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
SAXagliptin Moderate CYP3A4 inhibitors may raise serum levels of SAXagliptin.
Sildenafil Moderate CYP3A4 inhibitors may raise the serum Sildenafil concentration.
Silodosin Moderate CYP3A4 inhibitors may raise the serum level of Silodosin.
Siltuximab Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
Tamsulosin Moderate CYP3A4 inhibitors may raise the serum level of Tamsulosin.
Tetrahydrocannabinol Moderate CYP3A4 inhibitors may raise the serum level of Tetrahydrocannabinol.
Ticagrelor Moderate CYP3A4 inhibitors may raise serum levels of Ticagrelor.
Tocilizumab Could lower serum concentrations of CYP3A4 substrates (High Risk with Inducers).
TOLBUTamide The serum concentrations of TOLBUTamide may be decreased by taking Aprepitant.
Trabectedin Moderate CYP3A4 inhibitors may raise serum levels of Trabectedin.
Udenafil CYP3A4 Inhibitors Moderate may increase serum Udenafil concentrations.
Vilazodone CYP3A4 Inhibitors Moderate may raise the serum level of Vilazodone
Vindesine Moderate CYP3A4 inhibitors may cause an increase in serum Vindesine concentrations.
Warfarin Warfarin serum concentration may be decreased by taking Aprepitant
Zuclopenthixol Moderate CYP3A4 inhibitors may raise the serum concentration of Zuclopenthixol.

Risk Factor D (Alternative therapy)

  
Acalabrutinib Moderate CYP3A4 inhibitors may raise serum levels of Acalabrutinib. Management: With concurrent use of a moderate CYP3A4 inhibitor, reduce the acalabrutinib dosage to 100 mg daily. Monitoring patient closely for acalabrutinib response as well as evidence of adverse reactions with concurrent use.
Avanafil Moderate CYP3A4 inhibitors may cause a higher serum level of Avanafil. Administration: Avanafil adults are allowed to take 50 mg of the drug in a 24-hour period if taken with a moderate CYP3A4 inhibitor. This combination should be closely monitored for signs of adverse reactions in patients who take it.
Brigatinib Moderate CYP3A4 inhibitors may cause an increase in serum Brigatinib concentration. When possible, avoid concurrent use of brigatinib and moderate CYP3A4 inhibitors. Reduce the dosage of brigatinib to approximately 40% if you cannot avoid a combination like this: 180 mg to 120 mg, 120 mg to 90mg, 90 mg to 90mg, 90 mg to 60mg, etc.
Bromocriptine CYP3A4 inhibitors (Moderate), may raise the serum level of Bromocriptine. Management: Bromocriptine should not be taken in excess of 1.6 mg per day if you are using a moderate CYP3A4 inhibitor. This is the Cycloset brand's recommendation, however other bromocriptine brands do not recommend such a limit.
Budesonide (Topical). CYP3A4 Inhibitors Moderate may increase serum Budesonide (Topical) concentrations. This combination should be avoided according to US prescribing information. Canadian product labels do not recommend strict avoidance. Monitor for excessive glucocorticoid effect as Budesonide may be elevated if combined.
Cilostazol Moderate CYP3A4 inhibitors may cause an increase in the serum level of Cilostazol. Adult patients receiving moderate inhibitors of CYP3A should consider reducing their cilostazol dosage to 50mg twice daily.
Colchicine CYP3A4 Moderate Inhibitors may cause an increase in serum Colchicine concentrations. Management: Use a moderate CYP3A4 inhibitor to reduce the dose of colchicine. Increase monitoring for colchicine-related toxicity. For more information, please refer to the full monograph. Patients with impaired renal or hepatic function should be treated extra cautiously.
Systemic Corticosteroids The serum concentrations of Corticosteroids may be increased by Aprepitant (Systemic). For single doses of 40 mg of aprepitant, no dose adjustment is necessary. Reduce oral dexamethasone and methylprednisolone dosages by 50% for other regimens, and reduce IV methylprednisolone dosages by 25%. This adjustment is made to antiemetic regimens that contain dexamethasone.
Dabrafenib High risk of Inducers causing a decrease in serum CYP3A4 substrates. Management: If possible, seek alternatives to the CYP3A4 substrate. Concomitant therapy should be avoided if possible. Monitor the clinical effects of the substrate carefully (especially therapeutic effects).
Dapoxetine CYP3A4 Inhibitors Moderate may increase serum levels of Dapoxetine. Use a moderate inhibitor of CYP3A to reduce the dose of dapoxetine.
Deflazacort CYP3A4 Moderate Inhibitors may raise serum levels of active metabolites of Deflazacort. When deflazacort is used in combination with a strong, moderate or weak CYP3A4 inhibitor, one-third of the recommended dose should be administered.
DOXOrubicin Conventional CYP3A4 inhibitors (Moderate), may increase serum levels of DOXOrubicin. (Conventional). Treatment: If possible, seek alternatives to moderate CYP3A4 inhibitors for patients who have been treated with doxorubicin. These combinations should be avoided according to one U.S. manufacturer, Pfizer Inc.
Eletriptan CYP3A4 Inhibitors Moderate may raise the serum level of Eletriptan. Management: Eletriptan should not be taken within 72 hours after a moderate CYP3A4 inhibitor has been administered.
Eliglustat CYP3A4 Moderate Inhibitors may increase serum Eliglustat concentrations. Under certain circumstances, Eliglustat should not be used. For more information, please refer to the full drug interaction monograph.
Encorafenib CYP3A4 Inhibitors Moderate (Moderate), may increase serum Encorafenib concentrations. Management: If possible, avoid concomitant administration of encorafenib. Concomitant administration should be avoided if possible. Reduce the encorafenib dosage to one-half the dose that was used before initiating the CYP3A4 inhibition.
Eplerenone CYP3A4 Moderate Inhibitors may raise the serum level of Eplerenone. Management: Eplerenone dosage recommendations can vary depending on the indication and the international labeling. For more information, please refer to the full drug interaction monograph.
Contraceptive: Estrogen Derivatives The serum Estrogen Derivatives may be decreased by Aprepitant (Contraceptive). Management: It is recommended to use a nonhormone-based contraceptive.
Everolimus CYP3A4 Inhibitors Moderate may increase Everolimus serum concentration. For most indications, Everolimus dose reductions may be required. For specific dose adjustments and monitoring recommendations, please refer to the full monograph.
FentaNYL Moderate CYP3A4 inhibitors may cause an increase in serum FentaNYL concentrations. Monitoring patients closely for several hours after initiating this combination. If necessary, adjust the dose of fentanyl as needed.
GuanFACINE Moderate CYP3A4 inhibitors may cause an increase in GuanFACINE serum concentration. Management: Lower the dose of Guanfacine by 50% before initiating this combination.
Ibrutinib Moderate CYP3A4 inhibitors may cause an increase in serum Ibrutinib concentrations. Management: If you are treating B-cell malignancies, reduce ibrutinib dose to 280 mg daily if you take moderate CYP3A4 inhibitors. If you are treating graft-versus-host disease, keep an eye on patients and adjust the dose if necessary based upon adverse reactions.
Ivacaftor Moderate CYP3A4 inhibitors may cause an increase in serum Ivacaftor concentration. Management: Ivacaftor dose cuts are necessary. Refer to the full monograph for weight- and age-specific recommendations. Use of ivacaftor/lumacaftor in combination with a moderate CYP3A4-inhibitor does not require dose adjustments.
Ivosidenib Moderate CYP3A4 inhibitors may cause an increase in serum Ivosidenib concentration. Use moderate CYP3A4 inhibitors in combination with ivosidenib should be avoided whenever possible. Monitor for increased toxicity of ivosidenib if the two are combined. Separate drug interaction monographs provide more information on drugs that are not listed as exceptions.
Lorlatinib High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates. Management: Do not use lorlatinib concurrently with any CYP3A4 Substrates. Even a slight decrease in serum concentrations could cause therapeutic failure or serious clinical consequences.
Lurasidone CYP3A4 Moderate Inhibitors may raise the serum level of Lurasidone. Management: The US Lurasidone labeling suggests reducing the dose of lurasidone by half using a moderate CYP3A4 inhibitor. Non-US labels recommend starting lurasidone at 20mg/day and limiting it to 40mg/day. It is not recommended to use grapefruit products concurrently.
Olaparib CYP3A4 inhibitors (Moderate), may cause an increase in the serum level of Olaparib. If possible, avoid the use of moderate CYP3A4 inhibitors when treating patients with olaparib. If concurrent use is impossible, the daily dose of olaparib should not exceed 150 mg.
Pitolisant High risk of Inducers causing a decrease in serum concentrations of CYP3A4 substrates Management: Avoid combining pitolisant and a CYP3A4 substrat with a low therapeutic index. Pitolisant should not be combined with other CYP3A4 sub-substances.
Contraceptive Progestins The serum concentration of Progestins may be decreased by aprepitant (Contraceptive). Management: You should use alternative or additional contraceptives during and after treatment with aprepitant or fosaprepitant , as well as for at least one year following the last dose of aprepitant/fosaprepitant.
Ranolazine Ranolazine may be increased by moderate CYP3A4 inhibitors (Moderate). Treatment: In patients who are concurrently taking moderate CYP3A4 inhibitors (e.g., erythromycin or verapamil), limit the adult ranolazine dose to 500 mg twice daily. ().
Sirolimus Moderate CYP3A4 Inhibitors may cause an increase in serum sirolimus concentrations. Management: If sirolimus is combined with a moderate CYP3A4 inhibitor, monitor for an increase in serum sirolimus concentrations. It is possible to reduce sirolimus doses, or lower sirolimus initial doses.
Sonidegib Moderate CYP3A4 inhibitors may cause an increase in serum Sonidegib concentrations. Management: If possible, avoid concomitant sonidegib use and take moderate CYP3A4 inhibitors. If concomitant use is not possible, reduce CYP3A4 inhibition use to no more than 14 days. Monitor for sonidegib toxicity (especially musculoskeletal adverse effects).
St John's Wort High risk of Inducers causing a decrease in serum CYP3A4 Substrates. Management: You may consider a different drug to replace one of the interacting drugs. Some combinations might be contraindicated. Refer to the manufacturer's label.
Stiripentol High risk of Inhibitors causing an increase in serum concentrations of CYP3A4 substrates. Management: Avoid stiripentol use with CYP3A4 Substrates that have a narrow therapeutic Index. This is to avoid adverse effects and toxicities. Monitoring of any CYP3A4 substrate that is used with stiripentol should be closely done.
Suvorexant Suvorexant may be increased by moderate CYP3A4 inhibitors. Patients receiving a moderate CYP3A4 inhibitor should take 5 mg of suvorexant daily. If necessary, the maximum dose of suvorexant can be increased up to 10 mg per day (maximum dosage) for efficacy.
Tezacaftor CYP3A4 inhibitors (Moderate), may increase Tezacaftor serum concentrations. Management: If combined with moderate CYP3A4 inhibitors, tezacaftor/ivacaftor 100 mg/150 mg should be taken in the morning and every other day. 150 mg of Ivacaftor should be taken alone in the morning. It can also be used as an alternate day to tezacaftor/ivacaftor.
Tolvaptan Tolvaptan serum concentration may be increased by moderate CYP3A4 inhibitors. When Jynarque is used in combination with a moderate CYP3A4 inhibitor, it will need to be adjusted. For more information, refer to the labeling or full interaction monograph. Samsca should be avoided when there are moderate CYP3A4 ihibitors.
Venetoclax Moderate CYP3A4 inhibitors may cause an increase in the serum level of Venetoclax. Treatment: Patients who require these combinations should reduce their venetoclax dosage by at least half the amount.
Zopiclone Moderate CYP3A4 inhibitors may raise the serum level of Zopiclone. Management: If combined with a moderate CYP3A4 inhibitor, the starting adult dose should not exceed 3.75mg. If these agents are used together, monitor patients for signs and symptoms.

Risk Factor X (Avoid Combination)

  
Astemizole Astemizole may be increased by apepitant.
Asunaprevir Moderate CYP3A4 inhibitors may raise serum Asunaprevir concentration.
Bosutinib Moderate CYP3A4 Inhibitors may raise the serum Bosutinib concentration.
Budesonide (Systemic). Budesonide (Systemic) can be increased by CYP3A4 inhibitors (Moderate).
Cisapride The serum Cisapride concentration may be increased by taking Aprepitant.
Cobimetinib CYP3A4 Inhibitors Moderate (Moderate), may raise the serum level of Cobimetinib. Management: Avoid concomitant use cobimetinib. Use moderate CYP3A4 inhibitors. Reduce the daily cobimetinib dosage to 20 mg if concurrent (14-day or less) use is not possible.
Conivaptan High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Strong CYP3A4 Inducers May lower the serum concentrations of Aprepitant.
Moderate CYP3A4 inhibitors May increase serum Aprepitant concentration.
Strong CYP3A4 inhibitors May increase serum Aprepitant concentration.
Domperidone CYP3A4 Inhibitors Moderate may raise the serum level of Domperidone. Management: The drug interactions monographs for drugs listed as an exception to this monograph will discuss the management of these drugs in greater detail.
Flibanserin Flibanserin serum concentration may be increased by CYP3A4 inhibitors (Moderate).
Fosaprepitant Moderate CYP3A4 inhibitors may raise serum Fosaprepitant concentrations.
Fusidic Acid (Systemic). High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Idelalisib High risk of Inhibitors causing an increase in serum CYP3A4 Substrates concentrations
Ivabradine Moderate CYP3A4 inhibitors may raise serum levels of Ivabradine.
Lomitapide Moderate CYP3A4 inhibitors may raise the serum Lomitapide concentration.
Naloxegol Moderate CYP3A4 inhibitors may raise the serum concentrations of Naloxegol.
Neratinib Moderate CYP3A4 inhibitors may raise the serum level of Neratinib.
Pimozide Pimozide may be increased by apixant.
Simeprevir Moderate CYP3A4 inhibitors may raise the serum level of Simeprevir.
Terfenadine Terfenadine may be increased by apepitant.
Ulipristal Moderate CYP3A4 inhibitors may increase serum levels of Ulipristal. Management: This applies only to ulipristal being used for symptoms/signs of uterine fibroids. Patients receiving ulipristal as an emergency contraceptive should be closely monitored for any signs or symptoms of ulipristal toxicities.

Monitor:

  • In patients receiving concurrent warfarin, monitor INR/PT for 2 weeks (particularly at 7 to 10 days) following aprepitant administration.
  • Monitor for signs and symptoms of hypersensitivity reactions.

How to administer Aprepitant:

Intravenous injections:

  • Do not inject for more than 2 minutes (30 minutes) prior to chemotherapy. Before and after administration, flush the infusion line with NS.

Intravenous Infusion

  • Do not infuse for more than 30 minutes (30 minutes) before you start chemotherapy.

Capsules

  • Take it whole.

Preventing nausea and vomiting from chemotherapy

  • You can take it with or without food.
  • One hour before chemotherapy, the first dose of chemotherapy should be administered.
  • If chemotherapy is not administered on days 2, 3 and 4, the next doses should be taken one hour before or in the morning.

Oral suspension

  • A health care provider should prepare the dose and give it to the patient or caregiver in an oral dispensing device.
  • Place the medicine in the mouth of the patient along the inner cheek. Slowly dispense the medicine.

Postoperative nausea and vomiting can be prevented

  • Take the medication within three hours of induction

Mechanism of action of Aprepitant:

  • Aprepitant is a medication that prevents acute or delayed vomiting.
  • It inhibits the substance P/neurokinin-1 (NK) receptor.
  • It increases the antiemetic activities of corticosteroids and 5-HT-3 receptor antagonists to prevent acute and delayed phases in chemotherapy-induced emesis.
  • It crosses the blood-brain barrier.

Protein binding: when administered intravenous is  >99%, and when given Orally is >95%

Metabolism: Extensively hepatic via CYP3A4 (major); CYP1A2 and CYP2C19 (minor); forms 7 metabolites which are weakly active.

Bioavailability: 60% to 65%

Half-life elimination: Terminal: about 9 to 13 hours

The time to peak plasma concentration is 4 - 6 hours in children and 3 - 4 hours in adults. 

Excretion: Primarily via metabolism  

International Brands of Aprepitant: 

  • Emend
  • Emend Tri-Pack
  • Emepitant
  • Nulhastar
  • Prevom

Aprepitant Brands in Pakistan:

Aprepitant [Caps 40 Mg]
Apreon Ferozsons Laboratoies Ltd.

Aprepitant [Caps 80 Mg]
Apreon Ferozsons Laboratoies Ltd.

Aprepitant [Caps 125 Mg]
Apreon Ferozsons Laboratoies Ltd.
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