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Pharmacology of Opioids
Published in Pamela E. Macintyre, Stephan A. Schug, Acute Pain Management, 2021
Pamela E. Macintyre, Stephan A. Schug
Aprepitant results in less vomiting compared with other antiemetics, but its efficacy against nausea is similar to other antiemetics (Zabirowicz & Gan, 2019). It is the first drug of this class to be developed and approved for use and is nonsedating.
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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Aprepitant undergoes extensive metabolism. Following a single IV 100mg dose of [14C]fosaprepitant, a prodrug for aprepitant, aprepitant accounts for approximately 19% of the radioactivity in plasma over 72 hours. 12 metabolites of aprepitant have been identified in human plasma. The metabolism of aprepitant, primarily by CYP3A4 and potentially with minor contribution by CYP1A2 and CYP2C19, occurs largely via oxidation at the morpholine ring and its side chains and the resultant metabolites were only weakly active.
Drug profiles: generic names A–Z
Published in Jerome Z. Litt, Neil H. Shear, Litt's Drug Eruption & Reaction Manual, 2017
Clinically important, potentially hazardous interactions with: acebutolol, alfuzosin, amiodarone, amitriptyline, amprenavir, aprepitant, atazanavir, atenolol, atorvastatin, avanafil, bisoprolol, bosentan, carbamazepine, celiprolol, cilostazol, cobicistat/elvitegravir/emtricitabine/tenofovir alafenamide, cobicistat/elvitegravir/emtricitabine/tenofovir disoproxil, colchicine, copanlisib, corticosteroids, cyclosporine, deflazacort, delavirdine, dronedarone, dutasteride, efavirenz, epirubicin, erythromycin, fingolimod, flibanserin, lurasidone, midostaurin, mifepristone, moricizine, naldemedine, naloxegol, neratinib, nevirapine, nifedipine, olaparib, oxprenolol, posaconazole, ranolazine, silodosin, simvastatin, sonidegib, sulpiride, telaprevir, venetoclax
Peptide receptor radionuclide therapy in neuroendocrine neoplasms and related tumors: from fundamentals to personalization and the newer experimental approaches
Published in Expert Review of Precision Medicine and Drug Development, 2023
These are mainly related to the AA infusion used for renal protection (for details see PROCEDURE section of the chapter). Co-infusion of this AA raises a state of metabolic acidosis and causes symptoms like nausea, vomiting, abdominal discomfort, and headaches. Different centers have reported varying ranges of these effects (vomiting in 10%, significant nausea 25%) as a reporting system and threshold of the reference population. There also occurs a mild degree of electrolyte imbalance especially hyperkalemia and hypernatremia during this period [33]. Caution should be taken if there is severe nausea/vomiting precipitating a state of significant dehydration and thereby could further worsen the electrolyte imbalance. For all patients precautionary measures are taken using a combination of corticosteroid and antiemetic administration before PRRT. Some of these patients require repeat administration of this or consideration of drugs like aprepitant for symptom control. Adequate patient counseling, preparation, and hydration form the backbone of facing these effects.
A pharmacological overview of aprepitant for the prevention of postoperative nausea and vomiting
Published in Expert Review of Clinical Pharmacology, 2023
Andrew Padilla, Ashraf S Habib
The target of aprepitant is the NK-1 receptor which is located throughout the body with an increased density in the central nervous system (CNS), particularly of interest in the area postrema and NTS. When these receptors are bound by substance P, a tachykinin neuropeptide, signals are relayed to the chemoreceptor trigger zone and vomiting center of the brain that may induce vomiting [24]. Aprepitant is a selective, high-affinity NK-1RA that passes through the blood brain barrier and blocks substance P binding to reduce stimulation of vomiting [28]. Positron emission tomography (PET) has demonstrated this binding of NK-1 receptors in healthy human patients [29]. Aprepitant has minimal or no affinity for common antiemetic targets including 5-HT3, dopamine or corticosteroid receptors [17].
Pharmacological management of cannabinoid hyperemesis syndrome: an update of the clinical literature
Published in Expert Opinion on Pharmacotherapy, 2022
Guillermo Burillo-Putze, John R. Richards, Consuelo Rodríguez-Jiménez, Alejandro Sanchez-Agüera
Aprepitant, an NK1 receptor antagonist, has been used in prevention of post-chemotherapy nausea and vomiting. Aprepitant has been studied in children with CVS. By blocking NK1 receptors from substance P, aprepitant mitigates nausea and vomiting. There is one case report in which aprepitant successfully resolved CHS symptoms in a patient who failed to improve after conventional antiemetics and haloperidol [130]. A 2019 guideline recommended all patients with CVS, regardless of concomitant cannabis use, be offered standard therapy for both prophylaxis and treatment of acute episodes, specifically tricyclic antidepressants such as amitriptyline, aprepitant, and topiramate as alternatives [131]. The use of these medications for acute treatment of CHS is uncommon, but these may represent therapeutic alternatives in the future.