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Buprenorphine Sublingual Tablets Generic Name & Formulations
Legal Class
CIII
General Description
Buprenorphine (as HCl) 2mg, 8mg; sublingual tabs.
Pharmacological Class
Opioid (partial agonist-antagonist).
See Also
How Supplied
Films—30; SL tabs—contact supplier
Manufacturer
Generic Availability
YES
Mechanism of Action
Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.
Buprenorphine Sublingual Tablets Indications
Indications
Treatment of opioid dependence, as part of a complete treatment plan to include counseling and psychosocial support.
Buprenorphine Sublingual Tablets Dosage and Administration
Adult
Dissolve under tongue; do not swallow tabs. Avoid food or drinks until tab dissolves. Rinse teeth/gums with water after tab dissolves, and swallow. Start when clear signs of withdrawal occur; individualize based on type and degree of opioid dependence. Supervised induction: 8mg once on Day 1 and 16mg once on Day 2. Dependent on heroin or short-acting opioids: initiate induction at least 4hrs after last opioid use. Dependent on methadone or long-acting opioids: initiate induction at least 24hrs after last opioid use. Maintenance phase: use buprenorphine/naloxone sublingual films at the same buprenorphine dose as Day 2; if intolerant to naloxone, may adjust buprenorphine by 2mg or 4mg increments/decrements to hold treatment level; (target dose): 16mg once daily; (usual range): 4–24mg once daily. Hepatic impairment (severe): reduce dose by ½ and monitor; (moderate): caution and monitor. Concomitant use or discontinuation of CYP3A4 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling).
Children
Not established.
Administration
Dissolve under tongue; do not chew or swallow. Gently rinse teeth and gums with water and swallow after tab dissolves. Wait at least 1hr before brushing teeth.
Nursing Considerations
Dissolve under tongue; do not chew or swallow. The use of buprenorphine HCl sublingual tablets for unsupervised administration should be limited to those patients who cannot tolerate buprenorphine and naloxone sublingual film, for example those patients who have been shown to be hypersensitive to naloxone.
Buprenorphine Sublingual Tablets Contraindications
Not Applicable
Buprenorphine Sublingual Tablets Boxed Warnings
Not Applicable
Buprenorphine Sublingual Tablets Warnings/Precautions
Warnings/Precautions
Potential risk for opioid overdose; strongly consider prescribing naloxone when initiating and renewing therapy. Consider prescribing naloxone if the patient has household members (eg, children) or other close contacts at risk of accidental ingestion or overdose. Abuse potential (monitor). Risk of significant respiratory depression; monitor. Compromised respiratory function (eg, COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, pre-existing respiratory depression). Sleep-related breathing disorders (including central sleep apnea (CSA), sleep-related hypoxemia); consider dose reduction if CSA develops. Unintentional pediatric exposure. Adrenal insufficiency. Obtain LFTs at baseline then monitor periodically; evaluate if hepatic event is suspected. Opioid-naïve. Elevated CSF pressure (eg, head injury, intracranial lesions). Biliary tract dysfunction. Acute abdomen. CNS depression. Moderate and severe hepatic impairment. Risk of QT prolongation (esp. in those with hypokalemia, bradycardia, recent conversion from atrial fibrillation, CHF, digitalis therapy, baseline QT prolongation, subclinical long-QT syndrome, severe hypomagnesemia). Advise patients to obtain regular dental checkups during treatment. Drug abusers. Reevaluate periodically. Avoid abrupt cessation. Elderly. Labor & delivery: may need additional analgesia. Pregnancy/postpartum: may need dose adjustments; monitor closely for withdrawal. Potential neonatal opioid withdrawal syndrome during prolonged use. Nursing mothers: monitor infants.
REMS
Buprenorphine Sublingual Tablets Pharmacokinetics
Distribution
Plasma protein bound: ~96% (buprenorphine); ~45% (naloxone).
Elimination
Fecal (69%), renal (30%). Half-life: 31–35 hours.
Buprenorphine Sublingual Tablets Interactions
Interactions
Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); manage concomitant use as clinically appropriate and closely monitor; strongly consider prescribing naloxone if concomitant use is warranted. During or within 14 days of MAOIs: not recommended. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT3 antagonists, mirtazapine, trazodone, tramadol, cyclobenzaprine, metaxalone, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Concomitant NNRTIs (eg, efavirenz, nevirapine, etravirine, delavirdine) or PIs (eg, atazanavir with/without ritonavir): monitor and reduce buprenorphine/naloxone dose, if needed. Potentiated by CYP3A4 inhibitors (eg, macrolides, azole antifungals, protease inhibitors). Antagonized by CYP3A4 inducers (eg, rifampin, carbamazepine, phenytoin). May antagonize diuretics; monitor. Paralytic ileus may occur with anticholinergics.
Buprenorphine Sublingual Tablets Adverse Reactions
Adverse Reactions
Oral hypoesthesia, glossodynia, oral mucosal erythema, headache, nausea, vomiting, hyperhidrosis, constipation, withdrawal signs/symptoms, insomnia, pain, peripheral edema; respiratory depression, orthostatic hypotension, hepatitis, hypersensitivity reactions, dental adverse events (eg, tooth fracture, tooth loss).
Buprenorphine Sublingual Tablets Clinical Trials
See Literature
Buprenorphine Sublingual Tablets Note
Notes
Formerly known under the brand name Subutex.
Buprenorphine Sublingual Tablets Patient Counseling
See Literature
