What Are the Uses of Buprenorphine and Naloxone?

The combination of buprenorphine and naloxone is an alternative to methodone given to treat opioid dependence. This medication helps relieve withdrawal symptoms that occur when an individual stops taking opioid drugs. It is a sublingual orange tablet or film placed under the tongue, typically taken once daily. In most cases, patients begin treatment with buprenorphine alone taken in the presence of the health care provider before switching to the combination buprenorphine and naloxone tablet. In the United States, this pairing is marketed under the name Suboxone® and was approved by the Food and Drug Administration in October 2002.

Opioid drugs have therapeutic indications, including analgesic effects, but some individuals use, abuse, and eventually become dependent on them. Such opiates include morphine, heroin, and painkillers like codeine and oxycontin. A dependent individual is unable to stop using opiates and will suffer from a wide range of withdrawal symptoms if the drug is stopped or reduced. Withdrawal symptoms are not life threatening; often begin within 12 hours of the last dose; and range from anxiety to muscle aches, vomiting, and sweating.

Treatment with Suboxone® is generally effective for opiate withdrawal symptoms. It can shorten the detoxification process and may also be given to patients as part of a long-term maintenance regimen. It is designed specifically to decrease an individual’s opiate abuse by injection.

Buprenorphine is an opioid partial agonist, and naloxone is an opioid antagonist. The former is actually an opioid, but at low doses it produces enough of an opiate effect to allow the patient to stop taking whatever stronger opioid he or she is dependent on without suffering many withdrawal symptoms. As a result, buprenorphine can itself cause physical dependence, so patients should not suddenly stop taking Suboxone®.

Naloxone counteracts central nervous system depression. It was added to Suboxone® to discourage detox patients from grinding up their buprenorphine tablets and combining and abusing them with other opiates. This drug is sometimes distributed as part of emergency overdose prevention kits to heroin users because it can counter the effects of opioid overdose.

As some patients do not tolerate naloxone well, treatment typically begins with low doses of buprenorphine alone administered in a health care facility. The health care practitioner will then raise the buprenorphine dose over several days before switching to buprenorphine and naloxone. The buprenorphine and naloxone tablet or film is usually taken once daily and is placed under the tongue until it dissolves, often in two to 10 minutes. The film or tablet may have a citrus or fruit flavor and should not be chewed or swallowed whole.

The most serious potential side effect of buprenorphine and naloxone is breathing difficulties that can be life-threatening. Patients who experience feeling dizzy or confused or slowed breathing should seek medical attention immediately. Taking buprenorphine and naloxone with a sedative, tranquilizer, or antidepressant can cause an overdose. Drinking alcohol while taking buprenorphine and naloxone can result in loss of consciousness and death.

Other potential side effects of Suboxone® include sleepiness and dizziness. Patients may develop liver problems or notice a decrease in blood pressure. Headaches, vomiting, and insomnia have also been reported. Using buprenorphine and naloxone can result in dependence and abuse because buprenorphine is an opioid.

As with any medication, patients should discuss any previous or ongoing health problems with their doctors prior to starting Suboxone®. The patient should reveal all medications, vitamins, and supplements he or she is taking. Individuals with a spinal curve that affects breathing or who are pregnant or may become pregnant should proceed with caution when considering buprenorphine and naloxone.