Drug information of Aprepitant

Mechanism of effect

Selective high-affinity antagonist of human substance P/neurokinin 1 receptors

Pharmacodynamic

Aprepitant, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. 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 chemotherapy-induced nausea and vomiting (CI NV).

Pharmacokinetics

The bioavailability is approximately 60% to 65%. Plasma protein binding is more than 95%. metabolized by CYP3A4 and, to a lesser degree, by CYP1A2 and CYP2C19. Following IV administration of a single 100 mg dose, 57% was excreted in the urine and 45% in the feces.

Drug indications

antiemetic

Dosage

Prevention of Postoperative Nausea and Vomiting Adults PO 40 mg within 3 h prior to induction of anesthesia. Prevention of Chemotherapy–Induced Nausea and Vomiting Adults PO 125 mg 1 h prior to chemotherapy treatment on day 1 and 80 mg/day in the morning on days 2 and 3. Administer in combination with a corticosteroid and 5-HT 3 antagonist

Drug contraindications

hypersensitivity to drug or its components. , Coadministration ofcisapride,pimozide terfenadine

Side effects

nausea , Headache , insomnia , constipation , dizziness , vomiting , fatigue , Angioedema , flushing , Bradycardia , Diarrhea , asthenia , pruritus , Hypertension , hypotension , neutropenia , anemia , dyspepsia , Urinary tract infection , Alopecia , anorexia , gastritis , stomatitis

Interactions

Amlodipine , Alprazolam , Ergotamine-C , Itraconazole , Ifosfamide , Bleomycin , Paroxetine , Contraceptive HD , Contraceptive LD , Quetiapine , Etoposide , Vincristin , Vinorelbine , Ketoconazole , Clarithromycin , Contraceptive , Contraceptive DE , Diltiazem , Phenytoin , Methylprednisolone , Midazolam , Warfarin , Vinblastin , Ethosuximide , Erythromycin , Ipratropium bromide , isosorbide dinitrate , Imatinib , Budesonide , Paclitaxel , Tamsulosin , Trazodone , Tolterodine , Docetaxel , Diazepam , Zolpidem , Salmeterol , Cinacalcet , Flurazepam , Granisetron , Gliclazide , Lapatinib , Lidocaine , Medroxyprogesterone , Mefenamic acid , Mexiletine , Nitrazepam , Nifedipine , Nimodipine , Carbamazepine , Colchicine , Clonazepam , Solifenacin , Rivaroxaban , Disulfiram , Azelastine , Daclatasvir , fentanyl , Rifabutin , Ranolazine , propoxyphene , Axitinib , Ivacaftor , Felodipine , Halofantrine , Terfenadine , Pazopanib , Flibanserin , Avanafil , Entrectinib , Lopinavir and Ritonavir , Cabozantinib , Cariprazine , Temsirolimus , Eliglustat , Gefitinib , Cannabidiol , Avapritinib , tucatinib , Abametapir

Alerts

Monitor patient for antiemetic efficacy.

Points of recommendation

May be taken with or without food Advise patient, family, or caregiver to read the patient information leaflet before starting therapy and with each refill. Advise patient, family, or caregiver that medication is designed to prevent nausea and vomiting caused by chemotherapy. It is not to be used to treat nausea or vomiting once it has started. Review dosing schedule with patient, including concomitant use of other antiemetics. Caution patient that first dose of aprepitant must be taken 1 h before chemotherapy administration to provide greatest protection against nausea and vomiting. Advise patient that medication regimen will greatly reduce likelihood of nausea or vomiting, but that these reactions are still possible. Instruct patient to inform health care provider if medication regimen does not prevent nausea or vomiting. Advise patient to report any of the following symptoms to health care provider: intolerable headache; persistent or intolerable constipation, diarrhea, or nausea; persistent weakness or general body discomfort. Advise patient receiving warfarin therapy that clotting status will need to be monitored closely for 2 wk following use of aprepitant. Advise women taking oral contraceptives to use alternative or backup contraceptive methods while using aprepitant. Advise patient, family, or caregiver that follow-up visits and lab tests will be required to monitor therapy and to keep appointments

Pregnancy level

B

Related drugs

rolapitant , Netupitant