byoo-pre-NOR-feen/na-LOX-one
Therapeutic Classification:
Pharmacologic Classification: opioid agonists antagonists, opioid antagonists
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/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).
CV: QT interval prolongation, orthostatic hypotension.
Derm: ↑sweating.
Endo: ADRENAL INSUFFICIENCY.
F and E: peripheral edema.
GI: constipation, nausea, oral hypoesthesia, oral mucosal erythema, vomiting, glossodynia, hepatitis.
Neuro: headache, insomnia.
Resp: RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA).
Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS) , physical dependence, psychological dependence, tolerance, withdrawal phenomenon.
A Zubsolv 1.4/0.36 tablet is equivalent in terms of buprenorphine content to a Suboxone 2/0.5 tablet. A Zubsolv 5.7/1.4 tablet is equivalent in terms of buprenorphine content to a Suboxone 8/2 tablet.
Induction
- SL (Adults): Suboxone film: Initiate therapy on Day 1 with buprenorphine 2 mg/naloxone 0.5 mg or buprenorphine 4 mg/naloxone 1 mg; then titrate up in increments of buprenorphine 2–4 mg every 2 hr until achieve dose of buprenorphine 8 mg/naloxone 2 mg based on control of acute withdrawal symptoms. On Day 2, a single daily dose of up to buprenorphine 16 mg/naloxone 4 mg is recommended. Zubsolv: Induction: Initiate therapy on Day 1 with buprenorphine 1.4 mg/naloxone 0.36 mg; then follow with up to buprenorphine 4.2 mg/naloxone 1.08 mg given as 1–2 tablets of buprenorphine 1.4 mg/naloxone 0.36 mg every 1.5–2 hr on Day 1 (not to exceed 3 tablets). On Day 2, a single daily dose of up to buprenorphine 11.4 mg/naloxone 2.9 mg is recommended.
Maintenance
- Buccal, SL (Adults): Suboxone film: Dose taken once daily. Progressively ↑/adjust 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;.
- SL (Adults): Tablets (generic): Dose taken once daily. Progressively ↑/adjust 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 tablets: Dose taken once daily. Progressively ↑/adjust 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.
Bunavail, Suboxone, Zubsolv