Metoclopramide
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| ID | DRUG-METOCLOPRAMIDE |
|---|---|
| Тип | Препарат |
| Синоніми | CerucalMaxolonReglanМетоклопрамід |
| Статус | переглянуто 2026-04-27 | очікує клінічного підпису |
| Хвороби | Не вказано |
| Джерела | SRC-ESMO-DLBCL-2024 SRC-NCCN-BCELL-2025 |
Дані про препарат
| Клас | Dopamine D2 receptor antagonist (central + peripheral); 5-HT4 agonist; weak 5-HT3 antagonist (at high dose); prokinetic |
|---|---|
| Механізм дії | Substituted benzamide that antagonizes dopamine D2 receptors centrally in the chemoreceptor trigger zone (area postrema) and peripherally in the upper GI tract, reducing nausea and accelerating gastric emptying. Also a 5-HT4 receptor agonist (potentiating release of acetylcholine in the enteric plexus → enhanced peristalsis) and at high doses (≥1 mg/kg) a weak 5-HT3 antagonist. The prokinetic action distinguishes it from pure D2 antagonists and is therapeutically useful for chemotherapy-induced gastroparesis, opioid-induced delayed gastric emptying, and post-treatment dyspepsia. Approved by FDA in 1979 for nausea/vomiting and gastroparesis; widely used as breakthrough antiemetic in CINV regimens. Use restricted in 2009 (FDA boxed warning) and 2013 (EMA) due to tardive dyskinesia risk with prolonged or high-dose use. |
| Типове дозування | Breakthrough CINV (adult): 10-20 mg PO/IV/IM every 4-6 hours as needed, max 30 mg/day or 0.5 mg/kg/day for routine use; total duration limited to ≤5 days per EMA / FDA restrictions to minimize tardive dyskinesia risk. High-dose CINV (historical, pre-5-HT3- antagonist era): 1-2 mg/kg IV q2h × 3-5 doses with diphenhydramine premed for EPS — now rarely used outside salvage. Renal impairment: reduce dose ~50% if CrCl <60 mL/min (renal excretion). Hepatic: caution. Pediatric: 0.1 mg/kg PO/IV q6h, max 0.5 mg/kg/day, ≤5 days. Elderly (>65 yrs): start 5 mg with extended interval (q8h); higher tardive dyskinesia risk. |
| Зареєстровано в Україні | True |
| Відшкодовується НСЗУ | True |
| Остання перевірка для України | 2026-04-27 |
Застереження
- Tardive dyskinesia — irreversible movement disorder risk increases with cumulative exposure and treatment duration; LIMIT to ≤12 weeks chronic / ≤5 days acute use (CINV); higher risk in elderly, women, diabetics
Нотатки
Cheap, widely available, fast-acting breakthrough antiemetic for CINV unresponsive to first-line 5-HT3 antagonists. Largely supplanted by 5-HT3 antagonists for primary CINV prophylaxis since the 1990s but retains a niche for: breakthrough nausea, opioid-induced nausea, chemotherapy-induced gastroparesis, and post-radiation nausea. CRITICAL: total duration limited to ≤5 days for acute use and ≤12 weeks for any indication (FDA 2009 boxed warning, EMA 2013) due to irreversible tardive dyskinesia risk. Risk highest in elderly, women, and diabetics. Acute EPS (oculogyric crisis, dystonia) responds to diphenhydramine 50 mg IV or benztropine 1-2 mg IV. AVOID combination with metoclopramide + olanzapine (additive EPS / TD risk). Ukraine: cheap, ubiquitous, NSZU-covered.
Де використовується
У YAML-корпусі не знайдено зворотних посилань.