The FDA has approved the oral substance P/neurokinin-1 (NK-1) receptor antagonist tradipitant (Nereus – Vanda) for prevention of vomiting induced by motion in adults. Tradipitant is the first drug to be approved for motion sickness in more than 40 years. Other oral substance P/NK-1 receptor antagonists (i.e., aprepitant, rolapitant, and netupitant) have been available for years for prevention of chemotherapy-induced nausea and vomiting.1-3
STANDARD TREATMENT — Pharmacologic options for prevention of motion sickness are limited. Over-the-counter...
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ISSUE
Auvelity (Axsome), an extended-release fixed-dose combination of dextromethorphan and bupropion that was approved by the FDA for treatment of major depressive disorder in 2022,1 has now been approved for treatment of agitation associated with dementia due to Alzheimer's disease (AD). It is the second product to be approved in the US for this indication; the oral second-generation antipsychotic drug brexpiprazole (Rexulti) was approved in 2023.2
PHARMACOLOGY ― Dextromethorphan is an uncompetitive antagonist of the N-methyl D-aspartate (NMDA) receptor (an ionotropic glutamate receptor). Its mechanism of action for treatment of agitation in patients with AD dementia is unclear. Dextromethorphan is rapidly absorbed from the GI tract and undergoes extensive first-pass metabolism, mainly via CYP2D6. Bupropion increases serum concentrations of dextromethorphan by inhibiting CYP2D6.
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