- History of Suboxone
- Approved Uses of Suboxone
- What is Suboxone Maintenance Treatment?
- Nature of Suboxone
- Side Effects of Suboxone
- Interactions with other Drugs
Buprenorphine, as the main ingrdient of Suboxone, was first marketed in the 1980s in the US, as an opioid pain reliever. For this purpose, it was marketed in its pure form (without naloxone as found in Suboxone) as as Temgesic sublingual tablets, and also an injectible form. In October 2002, the Food and Drug Administration (FDA) of the United States, and Health Canada in 2008 approved Suboxone, buprenorphine's higher-dosesublingual tablet preparations indicated for detoxification and long-term maintenance therapy in opioid dependency.
In addition to the sublingual tablet, Suboxone is now marketed in the US form of a sublingual film. The film is not available in Canada yet.
Suboxone is indicated and approved for the following uses:
1. Long-term maintenance treatment of dependence and addiction to opioids such as oxycodone (oxycontin® or percocet), fentanyl, hydromorphone (dilaudid®), heroin etc. Such treatment can happen usually only in certain approved facilities and/or by specially trained physicians.
2. Detoxification treatment of dependence on opioids such as oxycodone (oxycontin® or percocet), fentanyl, hydromorphone (dilaudid®), heroin etc. Such treatment can happen usually only in certain approved facilities and/or by specially trained physicians.
3. Management of moderate to severe chronic pain when a continuous, stable-level opioid analgesic is needed for an extended period of time. This should be done under the care of a physician who is very familiar with the unique pharmacology of methadone.
Suboxone should not be used in the following circumstances:
1. For any treatment of dependence or addiction to non-opioid drugs. Examples of drugs whose addiction do not respond to suboxone are stimulat class drugs such as cocaine and methamphetamines; sedative class drugs such as diazepam (Valium) and alprazolam (xanax); and THC, LSD, and ecstasy.
2. For patients that have taken another kind of opioid in the last 24 hours, or those who have taken methadone in the last 72 hours.
3. For pain that is mild or, occasional, or not expected to persist for an extended period of time.
4. For acute pain from any injury.
5. For postoperative pain.
Many people use Suboxone with the term "Suboxone Maintenance Treatment" interchangeably. This is not correct. Suboxone is a pharmaceutical agent with several uses including pain control. On the other hand, Suboxone maintenance treatment or SMT is a long-term program for those patients who have addiction/dependence to the opioid class of drugs such as oxycodone (OxyContin® or Percocet®), fentanyl, hydromorphone (Dilaudid®), heroin, morphine, codeine, etc. SMT usually integrates non-pharmacological modes such as counseling, social work, and family therapy.
Suboxone is a combination medication containing 2 active ingredients: buprenorphine and naloxone.
1) Buprenorphine, the major ingredient of Suboxone, is a partial opioid agonist. As an agonist, it binds to the receptors in the brain that are responsible for opioid actions, such as pain relief and euphoria. Buprenorphine has high affinity for these receptors and therefore is not displaced by other agonists such as oxycodone or morphine if taken later. On the other hand, as a partial agonist, it does not produce as much euphoria but it does suppress withdrawal and cravings. In other words, although buprenorphine is still an opioid with effects such as pain relief and euphoria, its maximal effects are less than those of full agonists like heroin and methadone.
At low doses, buprenorphine produces sufficient agonist effects to enable opioid-addicted individuals to discontinue the misuse of opioids without experiencing withdrawal symptoms. The agonist effects of buprenorphine increase linearly with increasing doses of the drug until at moderate doses (8-16 mg per day) they reach a plateau and no longer continue to increase with further increases in dose—the “ceiling effect”. Therefore, no more noticeable effects are seen for doses above 24-32 mg per day. This ceiling effect is seen only in partial agonist. Full agonists such as oxycodone, morphine and methadone have no celing effect, thus exerting stronger effects and side effect with increasing dosage. It is for these reasons that buprenorphine carries a lower risk of abuse, addiction, overdose and side effects compared to full opioid agonists.
In high doses and under certain circumstances, buprenorphine can actually block the effects of full opioid agonists and can precipitate withdrawal symptoms if administered to an opioid-addicted individual while a full agonist like morphine or oxycodone is in the bloodstream.
Like methadone, buprenorphine has a slow and long metabolism, unlike commonly known opioids such as oxycodone (OxyContin® or Percocet®), fentanyl, hydromorphone (Dilaudid®), heroin, morphine, codeine, etc. While such other opioids reach peak action within minutes or seconds (if injected or inhaled), suboxone can take some hours to reach its peak action. Due this slower metabolism, suboxone stays in the body much longer too -often days as opposed to hours. This allows a more even and stable action of the medication as opposed to the rapid onset and offset of a short acting opioid such as morphine or oxycodone. So while buprenorphine exerts its opiate-like effect, it does it in a slower and more controlled way. This effect is one that is desired for an individual addicted to the euphoria or "high" achieved from the rapid-acting opioids. While buprenorphine provides relief from the symptoms of withdrawal such as aches, chills, and cramps and the mental effects of craving for the high, it does not produce a high itself.
Buprenorphine has poor oral absorption and therefore, the medication is not available in an oral form. The tablets must be dissolved and absorbed from the mouth under the tongue.
2) Naloxone is the other active ingredient of Soboxone. It is a full opioid antagonist that can only be absorbed via injection. An antagonist is a medication that reverses the actions of an agonist. Naloxone is not orally or sublingually absorbed. Naloxone will be active only when injected. Due to its antagonist properties, if injected, it will cause immediate and full precipitation of withdrawal from any opioids present in the body. The naloxone is added to Suboxone to decrease its abuse potential and discourage the injection use of Suboxone for purposes of achieving euphoria.
The side effects associated with buprenorphine are similar to those caused by other opioid medications. Most of these side effects are likely to be more pronounced at the beginning of treatment — during the two weeks of treatment.
The most frequently reported side effects include drowsiness and light-headedness, headache, nausea and vomiting, dry mouth, weakness, and constipation. Most patients build tolerance to these side effects as the treatment goes on and the dose is adjusted by the physician. The physician can also investigate and prescribe other medications to alleviate these side effects, if they tend to persist.
Suboxone may cause opioid withdrawal symptoms. This is likely at the start of treatment if there are any other opioids present in the body from recent use. A very serious allergic reaction to this drug is rare. Symptoms of a serious allergic reaction, include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
This is not a complete list of possible side effects. Please consult a pharmacist for a complete list of Suboxone's side effects. If you notice other effects not listed above, contact your doctor or pharmacist.
The following is a list of the most common drug interactions for Suboxone. This is by no means a complete list. Consult a physician or pharmacist for a complete list. Always inform your physician or pharmacist about the complete list of your medications so that you could be alerted to any dangerous interactions.
Concurrent use of Suboxone and such medications can increase the risk of respiratory depression, hypotension, and profound sedation , coma and death. Of particular concern among these drugs are the benzodiazepines. While Suboxone has a higher safety profile when used with benzodiazepines, deaths have been reported when buprenorphine was taken in conjunction with benzodiazepines (especially when injected). Closer monitoring is needed if these medications are used/abused along with Suboxone. There are many drugs within the class of benzodiazepines but the mostly commonly used ones are: diazepam (Valium), lorazepam (Ativan), clonazepam (Klonipin), alprazolam (Xanax), oxazepam (Serax), temazepam (Restoril), chlordiazepoxide (Librium), etc.
Opioid Antagonists, Mixed Agonist/Antagonists, and Full Agonists:
Withdrawal symptoms, sometimes severe and prolonged, can be induced when someone on a full agonist, takes suboxone. Examples of full agonists are methadone, oxycodone (OxyContin® or Percocet®), fentanyl, hydromorphone (Dilaudid®), heroin, morphine, codeine, etc.
Withdrawal symptoms can also be induced when someone on Suboxone, takes a full antogonist, or partial antagonist. Examples of pure antagonists are naloxone (Narcan), naltrexone (Revia or Vivitrol); and an example of mixed or partial agonist is pentazocine (Talwin).