What Is Transdermal Buprenorphine?

Transdermal buprenorphine is a narcotic medication administered through a timed-release topical patch. Health care providers prescribe buprenorphine for patients suffering chronic pain that ranges from moderate to severe. Buprenorphine is a semi-synthetic opiate that carries a high potential for addiction as well as side effects that are similar to those associated with other narcotic analgesics. Buprenorphine’s strong binding ability to many different opiate receptors causes difficulty when trying to reverse the effects with opiate antagonist medications that include naloxone.

Laboratories create buprenorphine using an alkaloid from Papaver somniferum, commonly known as the opium poppy. The medication is chemically similar to codeine and morphine but thought to be 20% to 40% more potent than morphine. Studies indicate that transdermal buprenorphine acts as a partial agonist on the delta, mu, and ORL1 receptor sites of the brain.

The medication stimulates these receptors, which are responsible for a number of central nervous system and hormonal responses, including appetite regulation, endorphin release, gastric motility, and mood. These centers also determine drug tolerance and physical dependency. Buprenorphine also acts as an antagonist, blocking the kappa receptor. Besides natural pain control, this receptor regulates fluid elimination via the kidneys and regulates levels of consciousness.

Manufacturers produce transdermal buprenorphine in specially layered patches that provide medication doses in 5, 10, or 20 micrograms per hour. Patients generally apply the patch to clean, hairless skin. The upper back, upper chest, upper outer arms and the sides of the chest are recommended application sites, and a patient can generally wear a patch for up to seven days before replacement. Transdermal buprenorphine is also available as a three-day patch in Europe.

Health care providers commonly prescribe transdermal buprenorphine for the chronic pain associated with cancer, osteoarthritis, and neuropathy. Laboratories also manufacture buprenorphine in solution, for intramuscular or intravenous injection. Besides its analgesic uses, the medication has proven effective as an opiate detoxifying agent. Buprenorphine and naloxone are combined in a sublingual tablet for opiate addiction treatment.

Common side effects of buprenorphine include skin irritation associated with the adhesive on the transdermal patch. Instructions recommend that patients alternate application sites regularly, not repeating application to the same site for at least 21 days. Other common reactions include nausea, vomiting, and dizziness, along with headache. Subjecting the patch, or the area with an applied patch, to heat causes increased medication release and also increases vascular circulation. These combined actions create the potential for buprenorphine overdose.

Patients wearing a buprenorphine patch may also experience constipation, fluid retention, and hypotension. Serious central nervous system responses include respiratory depression, sedation, and alterations in judgment. Buprenorphine enhances the effects of alcohol and over-the-counter or prescription medications that act as central nervous system depressants.