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| {{DrugProjectFormSinglePage
| | #REDIRECT [[Aprepitant]] |
| |authorTag={{AP}}
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| |genericName=Aprepitant
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| |aOrAn=an
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| |drugClass=[[antiemetic]], [[neurokinin-1 receptor antagonist]]
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| |indicationType=prophylaxis
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| |indication=in combination with other antiemetic agents for the:
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| *acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin
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| *of [[nausea]] and [[vomiting]] associated with initial and repeat courses of moderately emetogenic cancer [[chemotherapy]] (MEC)
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| Also, indicated for the prevention of postoperative nausea and vomiting (PONV)
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| |adverseReactions=[[alopecia]], [[anorexia]], [[asthenia]]/[[fatigue]], [[constipation]], [[diarrhea]], [[headache]], [[hiccups]], [[nausea]], [[hypotension]], [[pruritus]], [[pyrexia]]
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| |blackBoxWarningTitle=<b><span style="color:#FF0000;">TITLE</span></b>
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| |blackBoxWarningBody=<i><span style="color:#FF0000;">Condition Name:</span></i> (Content)
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| |fdaLIADAdult======Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)=====
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| Capsules of EMEND (aprepitant) are given for 3 days as part of a regimen that includes a corticosteroid and a 5-HT3 antagonist. The recommended dose of EMEND is 125 mg orally 1 hour prior to chemotherapy treatment (Day 1) and 80 mg orally once daily in the morning on Days 2 and 3.
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| *EMEND may be taken with or without food.
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| *EMEND (fosaprepitant dimeglumine) for Injection (115 mg) is a prodrug of aprepitant and may be substituted for oral EMEND (125 mg), 30 minutes prior to chemotherapy, on Day 1 only of the CINV regimen as an intravenous infusion administered over 15 minutes.
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| In clinical studies with EMEND, the following regimen was used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:
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| [[file:Aprepitant Dosage1.png|none|300px]]
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| In a clinical study with EMEND, the following regimen was used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
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| [[file:Aprepitant Dosage2.png|none|300px]]
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| =====Prevention of Postoperative Nausea and Vomiting (PONV)=====
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| The recommended oral dosage of EMEND is 40 mg within 3 hours prior to induction of anesthesia. EMEND may be taken with or without food.
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| |offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Aprepitant (patient information) in adult patients.
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| |offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Aprepitant (patient information) in adult patients.
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| |offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Aprepitant (patient information) in pediatric patients.
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| |offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Aprepitant (patient information) in pediatric patients.
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| |contraindications=EMEND is contraindicated in patients who are [[hypersensitive]] to any component of the product. EMEND is a dose-dependent inhibitor of [[cytochrome P450]] isoenzyme 3A4 ([[CYP3A4]]). EMEND should not be used concurrently with [[pimozide]], [[terfenadine]], [[astemizole]], or [[cisapride]]. Inhibition of [[CYP3A4]] by [[aprepitant]] could result in elevated plasma concentrations of these drugs, potentially causing serious or life-threatening reactions.
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| |warnings======CYP3A4 Interactions=====
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| EMEND (aprepitant), a dose-dependent inhibitor of [[CYP3A4]], should be used with caution in patients receiving concomitant medications that are primarily metabolized through [[CYP3A4]]. Moderate inhibition of [[CYP3A4]] by aprepitant, 125 mg/80 mg regimen, could result in elevated plasma concentrations of these concomitant medications.
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| Weak inhibition of [[CYP3A4]] by a single 40 mg dose of aprepitant is not expected to alter the plasma concentrations of concomitant medications that are primarily metabolized through [[CYP3A4]] to a clinically significant degree.
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| When aprepitant is used concomitantly with another [[CYP3A4]] inhibitor, aprepitant plasma concentrations could be elevated. When EMEND is used concomitantly with medications that induce [[CYP3A4]] activity aprepitant plasma concentrations could be reduced and this may result in decreased efficacy of EMEND.
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| Chemotherapy agents that are known to be metabolized by [[CYP3A4]] include [[docetaxel]], [[paclitaxel]], [[etoposide]], [[irinotecan]], [[ifosfamide]], [[imatinib]], [[vinorelbine]], [[vinblastine]] and [[vincristine]]. In clinical studies, EMEND (125 mg/80 mg regimen) was administered commonly with [[etoposide]], [[vinorelbine]], or [[paclitaxel]]. The doses of these agents were not adjusted to account for potential drug interactions.
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| In separate pharmacokinetic studies no clinically significant change in [[docetaxel]] or [[vinorelbine]] pharmacokinetics was observed when EMEND (125 mg/80 mg regimen) was co-administered.
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| Due to the small number of patients in clinical studies who received the [[CYP3A4]] substrates [[vinblastine]], [[vincristine]], or [[ifosfamide]], particular caution and careful monitoring are advised in patients receiving these agents or other chemotherapy agents metabolized primarily by [[CYP3A4]] that were not studied.
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| =====Coadministration with Warfarin (a CYP2C9 substrate)=====
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| Coadministration of EMEND with [[warfarin]] may result in a clinically significant decrease in [[International Normalized Ratio]] ([[INR]]) of [[prothrombin time]]. In patients on chronic [[warfarin]] therapy, the [[INR]] should be closely monitored in the 2-week period, particularly at 7 to 10 days, following initiation of the 3-day regimen of EMEND with each chemotherapy cycle, or following administration of a single 40 mg dose of EMEND for the prevention of postoperative [[nausea]] and [[vomiting]].
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| =====Coadministration with Hormonal Contraceptives=====
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| Upon coadministration with EMEND, the efficacy of [[hormonal contraceptives]] during and for 28 days following the last dose of EMEND may be reduced. Alternative or back-up methods of contraception should be used during treatment with EMEND and for 1 month following the last dose of EMEND.
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| =====Patients with Severe Hepatic Impairment=====
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| There are no clinical or pharmacokinetic data in patients with severe hepatic [[impairment]] ([Child-Pugh score]] >9). Therefore, caution should be exercised when EMEND is administered in these patients.
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| =====Chronic Continuous Use=====
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| Chronic continuous use of EMEND for prevention of [[nausea]] and [[vomiting]] is not recommended because it has not been studied; and because the drug interaction profile may change during chronic continuous use.
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| |alcohol=Alcohol-Aprepitant (patient information) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
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| }}
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| {{drug header}}
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| ==Why this medication is prescribed==
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| Aprepitant is used with other medications to prevent upset stomach and vomiting caused by cancer chemotherapy treatment. Aprepitant is in a class of medications called antiemetics. It works by blocking the action of neurokinin, a natural substance in the brain that causes upset stomach and vomiting.
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| ==How this medication should be used==
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| Aprepitant comes as a capsule to swallow with a drink. Aprepitant is usually taken once daily, with or without food, during the first few days of your cancer chemotherapy treatment. You will probably take aprepitant 1 hour before your first dose of chemotherapy, and then each morning for the next 2 days. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take aprepitant exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
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| Aprepitant capsules come in two different strengths. Your doctor may prescribe both of the strengths for you to take at different times. You should be careful to take the right strength at the right time as directed by your doctor.
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| Aprepitant only works to prevent upset stomach and vomiting. If you already have these symptoms, do not take aprepitant. Call your doctor instead.
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| Aprepitant is used only during the first 3 days of cancer chemotherapy treatment cycles. Do not continue taking aprepitant longer than instructed by your doctor.
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| ==Other uses for this medicine==
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| This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.
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| ==Special precautions==
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| '''Before taking aprepitant:'''
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| *tell your doctor and pharmacist if you are allergic to aprepitant or any other medications.
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| *do not take aprepitant if you are taking astemizole (Hismanal), cisapride (Propulsid), pimozide (Orap), or terfenadine (Seldane).
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| *tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, and nutritional supplements you are taking. Be sure to mention any of the following: anticoagulants ('blood thinners') such as warfarin (Coumadin); antifungals such as fluconzaole (Diflucan), itraconzaole (Sporanox), and ketoconazole (Nizoral); benzodiazepines such as alprazolam (Xanax), diazepam (Valium), and triazolam (Halcion); buspirone (BuSpar); calcium channel blockers such as amlodipine (Norvasc), diltiazem (Cardizem, Dilacor, Tiazac,), felodipine (Lexxel, Plendil), nifedipine (Adalat, Procardia), nisoldipine (Sular), and verapamil (Calan, Isoptin, Verelan); chlolesterol-lowering medications (statins) such as atorvastatin (Lipitor), fluvastatin (Lescol); lovastatin (Altocor, Mevacor), and simvastin (Zocor); cancer chemotherapy medications such as docetaxel (Taxotere), etoposide (Toposar, VePesid), ifosfamide (Ifex), imatinib (Gleevec), irinotecan (Camptosar), paclitaxel (Taxol), tamoxifen (Nolvadex), vinblastine, vincristine (Vincasar), and vinorelbine (Navelbine); carbamazepine (Tegretol); celecoxib (Celebrex); chlorpheniramine (Chlor-Trimeton, other cough, cold and sinus medications); cimetidine (Tagamet); clarithromycin (Biaxin); cyclosporine (Neoral, Sandimmune); danazol (Danocrine); delavirdine (Rescriptor); dexamethasone (Decadron); diclofenac (Arthrotec, Voltaren); efavirenz (Sustiva); erythromycin (E.E.S., E-Mycin, Erythrocin); ethosuximide (Zarontin); fluoxetine (Prozac, Sarafem); fluvoxamine (Luvox); glipizide (Glucotrol); haloperidol (Haldol); HIV protease inhibitors such as indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir), and saquinavir (Fortovase, Invirase); ibuprofen (Advil, Motrin); irbesartan (Avapro, Avalide); isoniazid (INH, Nydriazid); losartan (Cozaar, Hyzaar); methadone (Dolophine, Methadose); methylprednisolone (Medrol); metronidazole (Flagyl); naproxen ( Naprosyn); nefazadone (Serzone); oral contraceptives (birth control pills); phenobarbital (Luminal, Solfoton); phenytoin (Dilantin); piroxicam (Feldene); quinidine (Cardioglute, Quinaglute); quinine; rifabutin (Mycobutin); rifampin (Rifadin, Rimactane); tacrolimus (Prograf); sildenafil (Viagra); sulfamethoxazole (Bactrim, Septra, Sulfatrim); tolbutamide (Orinase); torsemide (Demadex); trazodone; troleandomycin (TAO); and zafirlukast (Accolate). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
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| *tell your doctor what herbal products you are taking, especially St. John's Wort.
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| *tell your doctor if you have or have ever had liver disease.
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| *tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking aprepitant, call your doctor.
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| ==Special dietary instructions==
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| Talk to your doctor about drinking grapefruit juice while taking this medicine.
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| ==What to do if you forget a dose==
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| Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
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| ==Side Effects==
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| ===Minor Side Effects===
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| Aprepitant may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
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| *weakness
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| *extreme tiredness
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| *dizziness
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| *diarrhea
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| *constipation
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| *stomach pain
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| *upset stomach
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| *hiccups
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| *loss of appetite
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| ===Severe Side Effects===
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| Some side effects can be serious. The following symptoms are uncommon, but if you experience any of them, call your doctor immediately:
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| *hives
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| *skin rash
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| *difficulty breathing or swallowing
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| *swelling of the face, throat, tongue, lips, eyes, hands, feet, ankles, or lower legs
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| *hoarseness
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| Laboratory animals who were given aprepitant developed tumors. It is not known if aprepitant increases the risk of tumors in humans. Talk to your doctor about the risks of taking aprepitant.
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| Aprepitant may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.
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| If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online [at http://www.fda.gov/MedWatch/report.htm] or by phone [1-800-332-1088].
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| ==Storage conditions needed for this medication==
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| Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.
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| ==In case of emergency/overdose==
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| In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.
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| '''Symptoms of overdose may include:'''
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| *drowsiness
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| *headache
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| ==Other information==
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| Keep all appointments with your doctor.
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| Do not let anyone else take your medication. Ask your pharmacist any questions you have about refilling your prescription.
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| ==Brand names==
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| *Emend®
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| [[Category:Oncology Drugs]]
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| [[Category:Gastrointestinal Drugs]]
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