Buprenorphine Hydrochloride (11 brand names, 4 dosage forms, 5 routes)
Available dosage forms: TABLET, FILM, IMPLANT, INJECTABLE.
Routes of administration: SUBLINGUAL, BUCCAL, SUBLINGUAL, IMPLANTATION, INJECTION, BUCCAL.
Brand Names
- BELBUCA
- BUNAVAIL
- BUPRENEX
- BUPRENORPHINE HYDROCHLORIDE
- BUPRENORPHINE HYDROCHLORIDE AND NALOXONE HYDROCHLORIDE
- BUPRENORPHINE HYDROCHLORIDE; NALOXONE HYDROCHLORIDE
- CASSIPA
- PROBUPHINE
- SUBOXONE
- SUBUTEX
- ZUBSOLV
Indications and Usage
ZUBSOLV is indicated for treatment of opioid dependence. ZUBSOLV should be used as part of a complete treatment plan that includes counseling and psychosocial support.
Contraindications
ZUBSOLV is contraindicated in patients with a history of hypersensitivity to buprenorphine or naloxone as serious adverse reactions, including anaphylactic shock, have been reported [see Warnings and Precautions (5.9)].
Adverse Reactions
The following serious adverse reactions are described elsewhere in the labeling:• Addiction, Abuse, and Misuse [see Warnings and Precautions (5.1)]• Respiratory and CNS Depression [see Warnings and Precautions (5.2, 5.3)]• Neonatal Opioid Withdrawal Syndrome [see Warnings and Precautions (5.5)]• Adrenal Insufficiency [see Warnings and Precautions (5.6)]• Opioid Withdrawal [see Warnings and Precautions (5.7, 5.10)]• Hepatitis, Hepatic Events [see Warnings and Precautions (5.8)]• Hypersensitivity Reactions [see Warnings and Precautions (5.9)]• Orthostatic Hypotension [see Warnings and Precautions (5.16)]• Elevation of Cerebrospinal Fluid Pressure [see Warnings and Precautions (5.17)]• Elevation of Intracholedochal Pressure [see Warnings and Precautions (5.18)]
Drug Interactions
Table 4 includes clinically significant drug interactions with ZUBSOLV. Table 4. Clinically Significant Drug Interactions with ZUBSOLV Benzodiazepines and other Central Nervous System (CN-S) Depressants Clinical Impact: Due to additive pharmacologic effects, the concomitant use of benzodiazepines and other CNS depressants, including alcohol, increases the risk of respiratory depression, profound sedation, coma, and death. Intervention: Cessation of benzodiazepines or other CNS depressants is preferred in most cases of concomitant use. In some cases, monitoring in a higher level of care for taper may be appropriate. In others, gradually tapering a patient off of a prescribed benzodiazepine or other CNS depressant or decreasing to the lowest effective dose may be appropriate.Before co-prescribing benzodiazepines for anxiety or insomnia, ensure that patients are appropriately diagnosed and consider alternative medications and non-pharmacologic treatments [see Warnings and Precautions (5.2, 5.3)]. If concomitant use is warranted, strongly consider recommending or prescribing an opioid overdose reversal agent, as is recommended for all patients on buprenorphine treatment for opioid use disorder [see Warnings and Precautions (5.2) ]. Examples: Benzodiazepines and other sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, gabapentinoids (gabapentin or pregabalin), other opioids, alcohol. Inhibitors of CYP3A4 Clinical Impact: The concomitant use of buprenorphine and CYP3A4 inhibitors can increase the plasma concentration of buprenorphine, resulting in increased or prolonged opioid effects, particularly when an inhibitor is added after a stable dose of ZUBSOLV is achieved.After stopping a CYP3A4 inhibitor, as the effects of the inhibitor decline, the buprenorphine plasma concentration will decrease [see Clinical Pharmacology (12.3)], potentially resulting in decreased opioid efficacy or a withdrawal syndrome in patients who
Mechanism of Action
ZUBSOLV contains buprenorphine and naloxone. 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.
Overdosage
Clinical Presentation The manifestations of acute buprenorphine overdose include pinpoint pupils, sedation, hypotension, hypoglycemia, respiratory depression, and death. Toxic leukoencephalopathy has been reported after opioid overdose and can present hours, days, or weeks after apparent recovery from the initial intoxication. Treatment of Overdose In the event of overdose, the respiratory and cardiac status of the patient should be monitored carefully. When respiratory or cardiac functions are depressed, primary attention should be given to the re-establishment of adequate respiratory exchange through provision of a patent airway and institution of assisted or controlled ventilation. Oxygen, IV fluids, vasopressors, and other supportive measures should be employed as indicated. In the case of overdose, the primary management should be the re-establishment of adequate ventilation with mechanical assistance of respiration, if required. An opioid overdose reversal agent may be of value for the management of buprenorphine overdose. Higher than normal doses and repeated administration may be necessary. The long duration of action of ZUBSOLV should be taken into consideration when determining the length of treatment and medical surveillance needed to reverse the effects of an overdose. Insufficient duration of monitoring may put patients at risk.