NK1 receptor antagonists
What are NK1 receptor antagonists?
Neurokinin-1 (NK1) receptor antagonists are used for prevention of acute and delayed nausea and vomiting. The NK1 receptor antagonist competitively binds to the NK1 receptor, which blocks the binding of substance P and prevents the emetic signal being transmitted. NK1 receptor antagonists can be used in conjunction with 5-HT3-receptor antagonists and corticosteroids to augment their antiemetic activity.
Neurokinin-1 Receptor Antagonists
Two formulations are available, aprepitant (oral) and fosaprepitant (parenteral), and several others (e.g., casopitant, vestipitant, netupitant) are undergoing evaluation.
| Drug Name | Avg. Rating | Reviews |
|---|---|---|
| aprepitant systemic (Pro) Brand names: Aponvie, Cinvanti, Emend | 8.0 | 18 reviews |
| rolapitant systemic (Pro) Brand name: Varubi | 10 | 1 review |
| fosaprepitant systemic (Pro) Brand names: Emend for Injection, Focinvez | 1 review |
The other analgesics, such as acetaminophen or ibuprofen, typically found in narcotic analgesic combinations mainly work by inhibiting enzymes called cyclo-oxygenase (COX) enzymes that produce prostaglandins. Prostaglandins promote inflammation, pain and fever.
Antagonist drugs interfere in the natural operation of receptor proteins. They are sometimes called blockers; examples include alpha blockers, beta blockers, and calcium channel blockers.
List of NK1 receptor antagonists
Fluticasone nasal
Olopatadine (nasal)
Oxymetazoline nasal
QNASL





