Aprepitant
Детермінований перегляд YAML-сутності з джерельної бази. Клінічний авторитет лишається за вказаними source ID та статусом клінічного sign-off.
| ID | DRUG-APREPITANT |
|---|---|
| Тип | Препарат |
| Синоніми | EmendАпрепітант |
| Статус | переглянуто 2026-04-27 | очікує клінічного підпису |
| Хвороби | Не вказано |
| Джерела | SRC-ESMO-DLBCL-2024 SRC-NCCN-BCELL-2025 |
Дані про препарат
| Клас | Substance P / neurokinin-1 (NK1) receptor antagonist |
|---|---|
| Механізм дії | Selective high-affinity antagonist of the human substance P / neurokinin-1 (NK1) receptor in the central nervous system, blocking the late vomiting signal mediated by substance P binding in the nucleus tractus solitarius and area postrema. This complements the early-phase blockade by 5-HT3 antagonists (which control acute CINV) by preventing the delayed phase (24-120 h post-chemotherapy). Standard component of triple-antiemetic prophylaxis (NK1 + 5-HT3 + dexamethasone, ± olanzapine) for highly emetogenic chemotherapy (HEC) such as cisplatin ≥50 mg/m², AC (anthracycline + cyclophosphamide), and BEACOPP. Approved by FDA March 2003 and EMA November 2003. |
| Типове дозування | Oral 3-day regimen for HEC: 125 mg PO 1 hour before chemotherapy on day 1, then 80 mg PO once daily on days 2 and 3. For MEC: same schedule. Always combined with 5-HT3 antagonist (ondansetron 8-16 mg or palonosetron 0.25 mg IV) and dexamethasone (12 mg PO/IV day 1, then 8 mg days 2-4 — note dex DOSE REDUCTION when combined with aprepitant due to CYP3A4 interaction roughly doubling dex AUC). No dose adjustment for renal impairment or mild-moderate hepatic impairment; not studied in severe hepatic impairment (Child-Pugh C). Single-day 165 mg dose available in some regions for selected regimens. Pediatric (≥6 months): weight-based dosing. |
| Зареєстровано в Україні | True |
| Відшкодовується НСЗУ | True |
| Остання перевірка для України | 2026-04-27 |
Нотатки
Foundation NK1 antagonist for CINV prevention in HEC regimens. Three- drug regimen (NK1 + 5-HT3 + dex) shifts complete-response rate from ~50% (5-HT3 + dex alone) to ~80% across days 1-5 in cisplatin-based HEC trials (Hesketh, Warr). Adding olanzapine 10 mg PO d1-4 to make it a four-drug regimen further improves complete response by ~10% absolute (Navari, NEJM 2016). Critical interaction: aprepitant doubles dexamethasone exposure → must halve dex dose when co- prescribed (16 mg → 8 mg on day 1 if using oral dex; IV dex needs similar adjustment). Fosaprepitant 150 mg IV is the IV pro-drug alternative (single dose). For high-risk DLBCL R-CHOP / BEACOPP / ICE / DHAP, aprepitant is standard premed.
Де використовується
У YAML-корпусі не знайдено зворотних посилань.