近日，美国FDA批准了日本远藤制药株式会社的阿片类药物丁丙诺啡口颊膜贴剂（Belbuca®，盐酸丁丙诺啡）用于需全天治疗且目前替代疗法对其不充分的慢性疼痛患者。
该产品是首次以颊膜传输系统为基础的丁丙诺啡制剂。患者将Belbuca®内衬贴到脸颊，可更快地将镇痛药物丁丙诺啡直接输送到血液。丁丙诺啡与大多数阿片药物相比有更低的滥用可能性。Belbuca®治疗也能阻止鼻腔吸入或注射给药方式的滥用，因为薄膜贴剂难以压碎或溶解。该产品将在2016年第一季度上市销售，本品有七种剂量规格，每12小时使用75μg到900μg不等。
本品可使医生更好地为患者实施个体化给药方案进行治疗。由于这款药物基本上通过脸颊吸收，而几乎不通过消化道，所以Belbuca®可潜在导致更低的便秘发生。
盐酸丁丙诺啡属阿片受体拮抗剂，主要激动μ受体，对σ受体也有一定的激动作用，而对κ受体则有不同程度的拮抗作用。盐酸丁丙诺啡除具有镇痛作用（镇痛作用较吗啡强25～40倍）外。
包装规格[注：本品仅供研究应用]
BELBUCA   75mcg     buprenorphine    63481-161-60
BELBUCA   150mcg   buprenorphine    63481-207-60
BELBUCA   300mcg   buprenorphine    63481-384-60
BELBUCA   450mcg   buprenorphine    63481-519-60
BELBUCA   600mcg   buprenorphine    63481-685-60
BELBUCA   750mcg   buprenorphine    63481-820-60
BELBUCA   900mcg   buprenorphine    63481-952-60

BELBUCA CIII
Pharmacological Class:
Partial opioid agonist.

Active Ingredient(s):
Buprenorphine 75mcg, 150mcg, 300mcg, 450mcg, 600mcg, 750mcg, 900mcg; buccal films; peppermint flavor.

Company
Endo Pharmaceuticals
Indication(s):
Management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate. Limitations of use: reserve for use in patients for whom alternative treatment options are ineffective, not tolerated, or inadequate to provide sufficient management of pain. Not indicated as an as-needed (prn) analgesic.

Pharmacology:
Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.

Clinical Trials:
The efficacy of Belbuca was evaluated in three 12-week double-blind, placebo-controlled trials in opioid-naive and opioid-experienced patients with moderate-to-severe chronic low back pain using pain scores as the primary efficacy variable.

For more clinical trial data, see full labeling.

Legal Classification:
CIII

Adults:
See full labeling. Apply against inside of cheek; do not chew or swallow. Opioid-naive: initially 75mcg once daily or every 12 hours (if tolerated) for at least 4 days, then increase to 150mcg every 12 hours. Individual titration should proceed in increments of 150mcg every 12 hours no sooner than every 4 days. Max 900mcg every 12 hours; consider alternate analgesic if inadequate. Conversion from other opioids: see full labeling. Use 600mcg, 750mcg, and 900mcg doses only following titration from lower doses of Belbuca. Severe hepatic impairment or oral mucositis: reduce initial and titration doses by ½.

Children:
Not established.

Contraindication(s):
Significant respiratory depression. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment. Known or suspected GI obstruction, including paralytic ileus.

Warnings/Precautions:
Abuse potential (monitor). Life-threatening respiratory depression; monitor within first 24–72 hours of initiating therapy and following dose increases. Accidental exposure may cause fatal overdose (esp. in children). COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor and consider non-opioid analgesics. History of long QT syndrome; avoid. Hypokalemia, hypomagnesemia, unstable cardiac disease (eg, unstable atrial fibrillation, symptomatic bradycardia, unstable CHF, active myocardial ischemia); monitor ECG periodically. Head injury. Increased intracranial pressure, brain tumors; monitor. Impaired consciousness, coma, circulatory shock; avoid. Biliary tract dysfunction. Acute pancreatitis. Seizure disorders. Known or suspected mucositis; monitor for toxicity. Hepatotoxicity: obtain baseline LFTs in at-risk patients and monitor during treatment. Moderate or severe hepatic impairment. Avoid abrupt cessation. Reevaluate periodically. Drug abusers. Elderly. Cachectic. Debilitated. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Labor & delivery, nursing mothers: not recommended.

Interaction(s)
May be potentiated by CYP3A4 inhibitors; if needed, monitor and consider dose adjustments. May be antagonized by CYP3A4 inducers; monitor and consider dose adjustments. Concomitant NNRTIs (eg, efavirenz, nevirapine, etravirine, delavirdine) or PIs (eg, atazanavir, ritonavir); monitor and adjust buprenorphine dose, if needed. Potentiation with alcohol or other CNS depressants (eg, sedatives, anxiolytics, hypnotics, neuroleptics, general anesthetics, other opioids); monitor and reduce doses. Increased respiratory depression with concomitant benzodiazepines, muscle relaxants. Avoid concomitant Class IA or III antiarrhythmics or other drugs that prolong the QT interval. Avoid concomitant butorphanol, nalbuphine, pentazocine. May reduce efficacy of diuretics; monitor. Paralytic ileus may occur with anticholinergics.

Adverse Reaction(s)
Nausea, constipation, headache, vomiting, dizziness, somnolence, fatigue; hypersensitivity.

How Supplied:
Films—60

LAST UPDATED:
1/22/2016