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