【藥品性質提示】 根據 2019 AGS Beers Criteria，本藥品為【潛在不適當用藥 (PIM)】，不建議用於有骨折風險之老年人(除非用於急性止痛)。 #高警訊藥品

類鴉片止痛 Pain management; Surgical anesthesia supplement

Opioid Analgesic
Agonist of kappa opiate receptors and partial antagonist of mu opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression

吸收
肌肉注射給予延長釋放劑型150 mg NALDEBAIN之後，被吸收之nalbuphine sebacate即迅速水解為nalbuphine，達到血中最高濃度的時間（Tmax）為64.0±9.3小時。血中最高濃度（Cmax）為15.4±6.4 ng/mL。
分佈
給予150 mg NALDEBAIN予健康受試者，所求得的平均擬似分佈體積（mean apparent volume of distribution）大約為10,628±4403 L。 體外試驗顯示，nalbuphine sebacate在人類血漿中的血漿蛋白結合率約為90%。 Nalbuphine 在血液中分佈在紅血球的量略多於血漿，KRBC/PL 為1.24；nalbuphine sebacate KRBC/PL 為1.20。 Nalbuphine 透過胎盤的轉移比率相當高且迅速，母體與胎兒的比率改變可從1：0.37 至 1：1.6。
代謝
Nalbuphine sebacate在體內被酯解解代謝，經由生體轉換試驗證明，在人類血液中，nalbuphine sebacate可在30分鐘內被轉換為nalbuphine。 Nalbuphine在肝臟進行代謝作用，在體內經由細胞色素P450（Cytochrome P450s )及phase II enzyme UGTs( uridinyl diphosphate glucuronosyltransferases )代謝，形成葡萄糖醛酸代謝物。
排泄
腎臟為nalbuphine主要排泄途徑。肌肉注射給予延長釋放劑型150 mg NALDEBAIN之後，藥品被吸收後即迅速水解為nalbuphine，本品的半衰期為83.2±46.4小時。平均清除率為100±11 L/h。少於4% 的 nalbuphine在尿液中回收。

1. Significant respiratory depression; Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment
2. Known or suspected gastrointestinal obstruction, including paralytic ileus
3. Hypersensitivity to nalbuphine or to any component of the product

Fetal risk cannot be ruled out

Infant risk cannot be ruled out

Sedation, Dizziness, headache, Cold and clammy skin, Nausea and vomiting, xerostomia

Pain management: IM, IV, SubQ
1. Usual dose: 10 mg every 3 to 6 hours as needed (based on a 70 kg patient); may titrate dose to appropriate effect.
2. Maximum dose in nonopioid-tolerant patients: 20 mg/dose; 160 mg/day.
Surgical anesthesia supplement: IV
1. Induction: 0.3 to 3 mg/kg over 10 to 15 minutes
2. Maintenance: 0.25 to 0.5 mg/kg as required

Safety and effectiveness have not been established in patients younger than 18 years of age

There are no specific dosage adjustments provided in the manufacturer's labeling; however, a reduced dose is recommended. Use with caution.

There are no specific dosage adjustments provided in the manufacturer's labeling; however, a reduced dose is recommended. Use with caution.