The Buprenorphine Transdermal Patch is designed for managing severe, chronic pain requiring around-the-clock opioid treatment. Its pharmacokinetic profile includes steady-state achievement by day 3, 15% bioavailability, and 96% plasma protein binding. Hepatic metabolism via CYP3A4 and UGT enzymes leads to fecal excretion (70%), with a terminal half-life of ~26 hours. The patch provides stable plasma concentrations over 24 hours, with peak levels at 8 hours post-application. Available in 5–20 mcg/h doses (up to 70 mcg/h internationally), it offers weekly dosing convenience and is ideal for patients with swallowing difficulties or nausea.
Key Points Explained:
1. Absorption & Bioavailability
- Steady-state achievement: Reached by the third day of continuous use.
- Bioavailability: 15%, typical for transdermal delivery due to skin barrier limitations.
- Peak plasma time: 8 hours post-application, reflecting gradual absorption through the skin.
2. Distribution & Protein Binding
- Plasma protein binding: 96%, primarily to albumin and alpha-1-acid glycoprotein, limiting free drug availability.
- Stable brain concentrations: Animal studies confirm consistent CNS levels correlating with plasma stability.
3. Metabolism & Elimination
- Hepatic metabolism: Via CYP3A4 and UGT-isoenzymes, necessitating caution with CYP3A4 inhibitors/inducers (e.g., ketoconazole, rifampin).
- Excretion: Predominantly fecal (70%), with renal clearance playing a minor role.
- Terminal half-life: ~26 hours, supporting prolonged action but requiring monitoring in hepatic impairment.
4. Dosing & Strengths
- Available doses: 5, 7.5, 10, 15, and 20 mcg/h (U.S.); higher strengths (35–70 mcg/h) internationally.
- Duration: 24-hour wear time, with once-weekly dosing enhancing adherence.
5. Clinical Advantages
- Stable plasma levels: Avoids peaks/troughs associated with oral opioids, reducing abuse potential.
- Non-oral route: Ideal for patients with dysphagia, vomiting, or malabsorption.
6. Special Considerations
- Not for acute pain: Reserved for chronic, severe pain unresponsive to other therapies.
- Monitoring: Required for drug interactions (CYP3A4 modulators) and hepatic dysfunction.
This profile underscores the patch’s role in long-term pain management, balancing efficacy with safety through controlled release and metabolic predictability.
Summary Table:
| Property | Details |
|---|---|
| Steady-State Achievement | Reached by day 3 of continuous use. |
| Bioavailability | 15% (typical for transdermal delivery). |
| Peak Plasma Time | 8 hours post-application. |
| Protein Binding | 96% (primarily to albumin and alpha-1-acid glycoprotein). |
| Metabolism | Hepatic (CYP3A4 & UGT enzymes). |
| Excretion | 70% fecal, minor renal clearance. |
| Terminal Half-Life | ~26 hours. |
| Dosing Strengths | 5–20 mcg/h (U.S.), up to 70 mcg/h internationally. |
| Dosing Frequency | Once weekly (24-hour wear time). |
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