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Pregnancy Category: C
Pharmacologic: opioid agonists antagonists
ClassificationTherapeutic: opioid addiction agents
Pharmacologic: opioid agonists antagonists
Maintenance treatment of opioid dependence as part of a comprehensive program including counseling and psychological support.
Buprenorphine—Binds to opiate receptors in the CNS.
Sublingual naloxone— has no pharmacological effect; it is present in the formulation to discourage injection of the product by opioid-dependent patients.
Suppression of withdrawal symptoms during detoxification and maintenance from opioids.
Absorption: Buprenorphine— Well absorbed following SL administration; naloxone—Negligible absorption follows SL administration.
Distribution: Buprenorphine—Crosses the placenta; enters breast milk. CNS concentration is 15–25% of plasma.
Protein Binding: Buprenorphine—96%.
Metabolism and Excretion: Buprenorphine—Mostly metabolized by the liver mostly via the CYP3A4 enzyme system; one metabolite is active; 70% excreted in feces; 27% excreted in urine.
Half-life: Buprenorphine—33 hr; Naloxone—60–90 min (up to 3 hr in neonates).
|SL buprenorphine||unknown||1.5–1.7 hr||24 hr|
Contraindicated in: Hypersensitivity to buprenorphine or naloxone; Lactation: Buprenorphine enters breast milk; avoid breast-feeding.
Use Cautiously in: Compromised respiratory function including COPD, cor pulmonale, diminished respiratory reserve, hypoxia, hypercapnia or respiratory depression of other causes; Geriatric: Elderly or debilitated patients may be more sensitive to drug effects.; Obstetric: Buprenorphine crosses the placenta; use during pregnancy only if potential benefit justifies potential risk; Pediatric: Children <16 yr (safety not established).
Adverse Reactions/Side Effects
Central nervous system
- headache (most frequent)
- insomnia (most frequent)
- orthostatic hypotension
- respiratory depression (life-threatening)
- constipation (most frequent)
- nausea (most frequent)
- oral hypoesthesia (most frequent)
- oral mucosal erythema (most frequent)
- vomiting (most frequent)
- hyperhydrosis (most frequent)
Fluid and Electrolyte
- peripheral edema
- allergic reactions including anaphylaxis (life-threatening)
- physical dependence
- psychological dependence
- withdrawal phenomenon
Drug-Drug interactionUse with extreme caution in patients receiving MAO inhibitors (↑ CNS and respiratory depression and hypotension—↓ buprenorphine dose by 50%; may need to ↓ MAO inhibitor dose.Inhibitors of the CYP3A4 enzyme system including itraconazole, ketoconazole, erythromycin, ritonavir, indinavir, saquinavir, atazanavir, or fosamprenavir may ↑ blood levels and effects; may need to ↓ buprenorphine dose.Blood levels/effects may be ↓ and withdrawal may be initiated by inducers of the CYP3A4 enzyme system including carbamazepine, phenobarbital, phenytoin or rifampicin ; dose alterations may be necessary.↑ risk of CNS depression with other CNS depressants including alcohol, antihistamines, benzodiazepines, phenothiazines, sedative/hypnotics, and some antidepressants ; dose adjustments may necessary.Concomitant use of kava-kava, valerian, chamomile, or hops can ↑ CNS depression.
Route/DosageA Zubsolv 1.4/0.36 tablet is equivalent in terms of buprenorphine content to a Suboxone 2/0.5 sublingual tablet. A Zubsolv 5.7/1.4 tablet is equivalent in terms of buprenorphine content to a Suboxone 8/2 sublingual tablet
Sublingual (Adults) Suboxone—Taken once daily. Progressively ↑/adjusted in increments of buprenorphine 2 mg/naloxone 0.5 mg or buprenorphine 4 mg/naloxone 1 mg. Titrate to keep patient engaged in treatment while suppressing opioid withdrawal; usual target dose is buprenorphine 16 mg/naloxone 4 mg once daily; Zubsolv—Taken once daily. Progressively ↑/adjusted in increments of buprenorphine 1.4 mg/naloxone 0.36 mg or buprenorphine 2.8 mg/naloxone 0.72 mg. Titrate to keep patient engaged in treatment while suppressing opioid withdrawal; usual target dose is buprenorphine 11.4 mg/naloxone 2.8 mg once daily.
Availability (generic available)
Sublingual filmlime-flavored: buprenorphine 2 mg/naloxone 0.5 mg, buprenorphine 4 mg/naloxone 1 mg, buprenorphine 8 mg/naloxone 2 mg, buprenorphine 12 mg/naloxone 3 mg Cost: 8 mg/2 mg $226.81 / 30
Sublingual tablets: buprenorphine 2 mg/naloxone 0.5 mg, buprenorphine 8 mg/naloxone 2 mg
Sublingual tablets (Zubsolv): buprenorphine 1.4 mg/naloxone 0.36 mg, buprenorphine 5.7 mg/naloxone 1.4 mg
- During initial therapy, assess patient at least weekly during first month and frequently thereafter for compliance, effectiveness of treatment plan, and overall patient progress. Once a stable dose is achieved, monthly assessment may be used. Determine absence of medication toxicity, medical, or behavioral adverse effect; responsible handling of medications by patient; compliance with treatment plan including recovery-oriented activities and psychotherapy or other modalities; abstinence from illicit drug use.
- Lab Test Considerations: Monitor liver function test prior to beginning therapy and periodically during treatment.
Potential Nursing DiagnosesIneffective coping (Indications)
- Buprenorphine/naloxone sublingual film and sublingual tablets are not appropriate as an analgesic.
- Can only be prescribed by clinicians who meet qualifying requirements, and who have notified the Secretary of Health and Human Services of their intent to prescribe this product for the treatment of opioid dependence and have been assigned a unique identification number that must be included on every prescription.
- Induction of therapy begins with patient being in a moderate state of opioid withdrawal and receiving buprenorphine for 2–3 days. Once the induction phase is completed, maintenance begins with buprenorphine/naloxone titration.
- Patients receiving buprenorphine/naloxone sublingual tablets may be switched to sublingual film of same dose. Dose adjustments may be required. A Zubsolv 1.4/0.36 tablet is equivalent in terms of buprenorphine content to a Suboxone 2/0.5 sublingual tablet. A Zubsolv 5.7/1.4 tablet is equivalent in terms of buprenorphine content to a Suboxone 8/2 sublingual tablet
- Sublingual: Film: Place film under tongue. If additional film is required for dose, place on opposite side of tongue from first film, minimizing overlap. Keep film under tongue until dissolved (5–7 min); do not chew, swallow, or move after placement.
- Tablets:Place under tongue until dissolves, about 5 min. Do not cut, chew, or swallow. Do not eat or drink anything until tablet is dissolved.
- Instruct patient to take medication as directed. Take missed doses as soon as remembered unless almost time for next dose; do not double doses. Do not take more often than prescribed and consult health care professional before stopping; dose should be ↓ gradually to prevent withdrawal syndrome. Instruct patient to read Medication Guide before starting therapy and with each Rx refill in case of changes. Advise patient to keep medication in a safe place, out of reach of children and protected from being stolen and do not share with others, even if they have the same symptoms. Explain that buprenorphine/naloxone sublingual film may be fatal to children and individuals not tolerant to opioids. Advise patient that selling or giving medication away is against the law.
- To dispose of unused films, remove from foil pouch and drop each film into toilet and flush.
- Caution patient of the danger of taking non-prescribed benzodiazepines or other CNS depressants, including alcohol, during therapy.
- May cause dizziness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
- Advise patient to make position changes slowly to prevent orthostatic hypotension.
- Advise female patients to notify health care professional if pregnancy is planned or suspected, or if breastfeeding.
- Instruct patient to inform family that, in the event of an emergency, treating health care professionals should be informed that patient is physically dependent on an opioid and being treated with buprenorphine/naloxone sublingual film.
- Maintenance treatment of opioid dependency.
A trademark for a preparation of the drug buprenorphine combined with naloxone.
buprenorphineA formulation of semi-synthetic opioid which may be superior to methadone in reducing heroin and cocaine abuse/dependence.