Pharmacological Class:
Opioid (partial agonist-antagonist) + opioid antagonist.
 
Active Ingredient(s):
Buprenorphine (as HCl), naloxone (as HCl dihydrate); 1.4mg/0.36mg, 5.7mg/1.4mg; sublingual tabs; menthol-flavor.
 
Company
Orexo U.S.
 
Indication(s):
 
Maintenance treatment of opioid dependence, as part of a complete treatment plan to include counseling and psychosocial support.
 
Pharmacology:
 
Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. Naloxone is a potent antagonist at mu-opioid receptors and produces opioid withdrawal signs and symptoms, if administered parenterally, in individuals physically dependent on full opioid agonists.
 
Legal Classification:
 
CIII
 
Adults:
 
Dissolve under tongue; do not cut, chew or swallow. Place additional tabs sublingually in different places under the tongue at the same time if needed. ≥16yrs: Initiate after supervised induction with buprenorphine sublingual tabs. Maintenance target dose: 11.4mg/2.8mg once daily; adjust in 1.4mg/0.36mg or 2.8mg/0.72mg increments; usual range 2.8mg/0.72mg–17.1mg/4.2mg once daily. Switching between Zubsolv and other buprenorphine/naloxone products: may need dose adjustments; monitor for over- or under-dosing. Switching between Suboxone SL tabs and Zubsolv: see full labeling.
 
Children:
 
<16yrs: not established.
 
Warnings/Precautions:
 
Compromised respiratory function (eg, COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression). Head injury. Increased intracranial pressure. Monitor hepatic function at baseline then periodically; eva luate if hepatic event is suspected. Myxedema. Hypothyroidism. Adrenal cortical insufficiency. Coma. Toxic psychoses. CNS depression. Acute abdomen. Biliary tract dysfunction. GI or GU obstruction. Acute alcoholism. Delirium tremens. Kyphoscoliosis. Avoid abrupt cessation. Abuse potential. Opioid-naïve. Elderly. Debilitated. Unintentional pediatric exposure. Neonatal withdrawal. Pregnancy (Cat.C). Nursing mothers: not recommended.
 
Interaction(s)
 
Potentiated by CYP3A4 inhibitors (eg, azole antifungals, macrolides, HIV protease inhibitors): monitor and may need dose adjustments. Concomitant CYP3A4 inducers (eg, efavirenz, nevirapine, etravirine, phenobarbital, carbamazepine, phenytoin, rifampicin): monitor for opioid withdrawal. Concomitant NNRTIs (eg, efavirenz, delaviridine) or atazanavir with/without ritonavir: monitor and reduce buprenorphine dose, if needed. Increased CNS depression with concomitant opioid analgesics, general anesthetics, benzodiazepines, phenothiazines, other tranquilizers, sedative/hypnotics, or other CNS depressants (eg, alcohol); caution and consider dose reduction of both agents.
 
Adverse Reaction(s)
 
Headache, nausea, vomiting, hyperhidrosis, constipation, signs/symptoms of withdrawal, insomnia, pain, peripheral edema; respiratory depression, orthostatic hypotension, anaphylactic shock.
 
How Supplied:
 
SL tabs—3x10 (per carton)
 
LAST UPDATED:
 
10/25/2013

2013年7月4日，Orexo公司宣布，美国食品药品管理局(FDA)已批准Zubsolv(丁丙诺啡/纳洛酮)用于阿片类依赖患者的维持治疗。该药物将作为包括咨询和社会心理支持在内的完整治疗计划的一部分。
根据该产品标签，Zubsolv属于阿片受体部分激动剂，剂型为薄荷口味的舌下速溶片，每日用药1次。Orexo公司称，与其他丁丙诺啡/纳洛酮药物相比，Zubsolv生物利用度高、溶解迅速且片型较小。
临床试验和上市后应用情况显示，这种丁丙诺啡/纳洛酮舌下片的常见不良事件包括头痛、恶心、呕吐、多汗、便秘、戒断症状、失眠、疼痛及外周水肿。
根据该产品标签，丁丙诺啡可能被以类似其他阿片类药物的方式被滥用，有必要根据患者的稳定程度开展适当的临床监测。在治疗初期或缺乏合适随访的情况下，不应开具多次取药处方。