Suboxone is a drug manufactured by the British company, Reckitt Benckiser. It contains buprenorphine and naloxone at a ratio of four to one. Suboxone is administered sublingually, which is under the tongue. Buprenorphine is an opioid drug that is most often used to treat addiction to other more addictive opioids like heroin, oxycodone and morphine. At a lower dose, it reduces acute and chronic pain. Naloxone is a drug that is added to Suboxone, because it blocks the effects of opioid injection overdose. Currently the Food and Drug Administration, or FDA, has only approved Suboxone for treating opioid addiction and not for treating acute and chronic pain.
Opioid System
The opioid system in the body regulates pain, reward, addiction and mood. Opioids activate specific proteins, called opioid receptors. There are three different types of opioid receptors and they are distributed throughout the nervous system. Endogenous chemicals, like endorphins, stimulate opioid receptors. Opioids are sometimes found in plants or are made in the laboratory. These compounds, of which morphine is the most notable, also stimulate opioid receptors and cause physiological effects, such as pain reduction, euphoria and addiction.
Dosage
In human trials that demonstrated substantial pain reduction in patients, buprenorphine was administered sublingually in divided daily doses between 4 and 16 mg. The mean duration of treatment was between 8 and 16 months. The website Outcome Resources, states that sublingual tablets start relieving pain in 15 minutes with a duration of activity between six and eight hours. This website also reports that the FDA has approved buprenorphine injection for severe acute pain management. The injected dose is 0.3 mg at six-hour intervals.
Efficacy
Opioid therapy has been used for many years to treat chronic pain associated with cancer and other serious illnesses. A 2005 study in the "American Journal of Therapeutics" reported that 86 percent of patients with chronic pain experienced moderate to substantial relief of pain after treatment with low doses of buprenorphine or buprenorphine in combination with naloxone. In this study, patients that were previously addicted to other opioid drugs exhibited fewer symptoms of dependence. A human study in the journal "Drugs" reported that buprenorphine was as effective as morphine in relieving moderate to severe pain and was longer-acting in patients treated after surgery.
Side Effects
Because stimulation of opioid receptors inhibits the transmission of many signals in the brain opioids depress the activity of the central nervous system, causing sedation. Some opioid receptors in the brain control emotional state and stimulation of these receptors and can lead to euphoria or mood enhancement. Buprenorphine-induced euphoria has only been reported after injection. Opioid receptors are also located in the brain stem and in the gut. Buprenorphine only at high doses can also stimulate these receptors causing respiratory depression and constipation.
Addiction and Withdrawal
Suboxone is primarily used to treat addiction to other opioid pain killers and has been reported in human studies to be much less addictive than other opioid drugs. The National Library of Medicine reports on the website, DailyMed, that the withdrawal symptoms of buprenorphine are milder than seen with other opioids and may be delayed in onset. A review in "Psychopharmacology" reported that buprenorphine has a low addictive and dependence-inducing potential. However, if this drug is injected rather than administered sublingually in people that are dependent on opioids, naloxone will intensify withdrawal symptoms.
References
- "Experimental and Clinical Psychopharacology"; Opioids and the Treatment of Chronic Pain: Controversies, Current Status, and Future Directions; Andrew Rosenblum et al.; October 2008
- DailyMed: Suboxone (Buprenorphine Hydrochloride and Naloxone Hydrochloride) Tablet
- "American Journal of Therapeutics"; Sublingual Buprenorphine Is Effective in the Treatment of Chronic Pain Syndrome; Herbert Malinoff; 2005
- "Psychopharmacology"; Behavioral Pharmacology of Buprenorphine, with a Focus on Preclinical Models of Reward and Addiction; T. Tzschentke; April 2002
- "Drugs"; Buprenorphine: A Review of its Pharmacological Properties and Therapeutic Efficacy; C. Heel et al.; February 1979
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