What is Buprenorphine?
At the correct dose, Buprenorphine may suppress cravings and withdrawal symptoms and block the effects of other opioids. Buprenorphine (´bu•pre•´nôr•fen) is not new. It was first patented in 1969 and has been used in the U.S. to treat pain and in Europe to treat pain and opioid addiction for decades. Buprenorphine is a semi-synthetic opioid and is a partial agonist.
- Opioid Agonists are drugs that cause an opioid effect; i.e., heroin, oxycodone, hydrocodone, and methadone.
- Opioid Antagonists are drugs that block and reverse the effects of agonist drugs. Narcan® is an antagonist and is used to reverse heroin overdoses.
Buprenorphine can act as both an agonist and antagonist. It attaches to the opioid receptors but only activates them partially, enough to suppress withdrawal and cravings, but not enough to cause extreme euphoria in opioid-tolerant patients.
When all available receptors are occupied with Buprenorphine, no additional opioid effect is produced by taking more.
This is called the ‘ceiling effect’. The ceiling effect, blocking ability, and possibility of precipitating withdrawal contribute to Buprenorphine having a favorable safety profile and helps lower the risk of overdose and misuse.
Oral medications, injections, and long-term implants:
In October 2002 the FDA approved the first two prescription Buprenorphine medications for the treatment of opioid addiction; Subutex®* (buprenorphine) and Suboxone®* (buprenorphine/naloxone).
Both Suboxone and Subutex tablets were discontinued and replaced with Suboxone Film®.
Dosage Forms and Strengths
SUBOXONE sublingual film is supplied as an orange rectangular film with a white printed logo in four dosage strengths:
- Buprenorphine 2 mg/naloxone 0.5 mg,
- Buprenorphine 4 mg/naloxone 1 mg,
- Buprenorphine 8 mg/naloxone 2 mg and
- Buprenorphine 12 mg/naloxone 3 mg
The first once-monthly injection for moderate to severe opioid use disorder designed to deliver a sustained release of buprenorphine. One dose every month, one buprenorphine treatment every month.
PROBUPHINE is an implant that contains the medicine buprenorphine.PROBUPHINE is used to treat certain adults who are addicted to (dependent on) opioid drugs (either prescription or illegal). It is indicated for the maintenance treatment of opioid dependence in patients who have achieved and sustained prolonged clinical stability on low-to-moderate doses (doses no more than 8 mg per day) of a buprenorphine-containing product.
Probuphine is the first and only product on the market for maintenance treatment of opioid addiction that provides non-fluctuating blood levels of buprenorphine around the clock for a period of six months following a single treatment procedure.