Xtampza ER
Xtampza ER
Generic Name
Xtampza ER
Mechanism
- Partial μ‑opioid receptor agonist: activates μ‑receptors to alleviate withdrawal without producing the full euphoric effect of full agonists.
- κ‑ and δ‑receptor antagonist activity: reduces dysphoric mood and anxiety associated with withdrawal.
- Slow oral release: delivers a near‑constant plasma concentration for 24 h, diminishing craving and withdrawal symptoms.
---
Pharmacokinetics
| Parameter | Typical Value | |
| Absorption | Oral | Rapid absorption with a mean Tmax of ~2 h; formulation ensures a 24‑h sustained release. |
| Distribution | Protein binding ~85 % (α‑1‑acid glycoprotein) | |
| Metabolism | Hepatic via CYP3A4 → multiple metabolites (inactive) | |
| Elimination | Renal excretion of unchanged drug & metabolites (≈ 50 %) | |
| Half‑life | Elimination t½ ~ 24–36 h; therapeutic levels maintained with once‑daily dosing | |
| Drug–drug interactions | Strong CYP3A4 inhibitors ↑ buprenorphine levels; strong CYP3A4 inducers ↓ levels |
--
•
Indications
- Maintenance therapy for opioid dependence in adults.
- Treatment of opioid withdrawal in patients requiring long‑acting opioid replacement.
---
Contraindications
- Contraindications
- Known hypersensitivity to buprenorphine or any component.
- Concomitant use of naloxone (for rescue) in a setting where opioid withdrawal may precipitate.
- Warnings/Cautions
- Pre‑existing respiratory depression or use of CNS depressants (benzodiazepines, alcohol).
- Hepatic impairment – careful dose adjustment or monitoring.
- Pregnancy – limited data; use only if benefits outweigh risks.
- Renal impairment – limited data; monitor for accumulation.
---
Dosing
- Starting dose: 8 mg PO once daily.
- Titration: Increase by 8 mg increments every 5–7 days if craving/withdrawal persists.
- Maximum dose: 32 mg PO once daily.
- Administration: Take with or without food; avoid crushing or chewing tablets to maintain extended‑release profile.
- Refill: Patients may require a prescription refill every 4–6 weeks.
Important: Must be administered under direct medical supervision; patients should sign an agreement for ongoing treatment.
---
Adverse Effects
| Common | Serious | |
| Nausea, vomiting | Respiratory depression (rare but fatal) | |
| Constipation | Seizures, hepatotoxicity | |
| Headache | Hypotension, syncope | |
| Dizziness | Severe allergic reactions (anaphylaxis) | |
| Somnolence |
*Patients should be instructed to seek immediate care if they experience breathing difficulties or severe dizziness.*
--
•
Monitoring
- Baseline:
- Liver function tests (ALT, AST, bilirubin).
- Renal function (creatinine, eGFR).
- Screening for hepatitis B/C.
- Follow‑up (every 4–6 weeks):
- Weight, metabolic panel, CBC.
- Screening for relapse (urine drug screen).
- Special monitoring:
- Cardiovascular status in patients with prior cardiac disease.
- Pregnancy test in women of childbearing potential.
---
Clinical Pearls
- Avoid Naloxone Rescue: While naloxone is often included in formulations for opioid overdose, Xtampza ER contains no naloxone, reducing risk of precipitated withdrawal if administered accidentally.
- Slow‑Release Integrity: The tablet is coated with a polymer matrix; chewing or crushing will cause an immediate, potentially life‑threatening spike in buprenorphine.
- Methadone Interaction: Co‑administration with methadone or other opioids can lead to additive respiratory depression; taper methadone first if needed.
- Patient Education: Emphasize the importance of daily adherence; missed doses can precipitate withdrawal symptoms quickly.
- Insurance & Access: Xtampza ER is covered under many VA and Medicare Advantage plans; however, check prior authorization requirements as it remains a specialty medication.
- Legal/Regulatory Note: The drug is Schedule III under the Controlled Substances Act; prescription, refills, and documentation must comply with DEA regulations.
--
• Reference: FDA Approved Drug Label – Xtampza ER (buprenorphine extended‑release) 2024.