Buprenorphine and Naloxone (Buprenex) are combined to create Suboxone.
Buprenorphine is a partially synthetic opioid derived from thebaine, a lesser component of opium and similar chemically to codeine and morphine, buprenorphine is used to help opioid abusers beat their addiction. Subutex and Cizdol are trade names for medications given to heroin and prescription pain killer addicts while buprenorphine-based Temgesic, Buprenex and Norspan are normally prescribed relieve acute chronic pain.
Buprenex is classified as a partial agonist opioid receptor. Buprenorphine has a number of legitimate uses, including being prescribed as a painkiller for individuals with chronic pain and to provide an alternative treatment for individuals that have developed an opioid addiction. Due to the highly addictive qualities of buprenorphine, it is a prescription drug that is often abused by individuals who are prescribed it to treat an opioid addiction, in a similar manner to how methadone is often abused. Buprenorphine’s common brand names are “Buprenex” and “Butrans”.
How Buprenorphine – Naloxone Works to Treat an Opioid Addiction
Unusual pharmacological properties found in buprenorphine helps reduce its potential for abuse by addicts, diminishes severity of cravings and withdrawal symptoms and exerts partial agonist properties on opioid receptors in the brain. Although buprenorphine does produce opioid-like side effects, such as respiratory depression, drowsiness and euphoria, its effects are significantly weaker than those produced by heroin and prescription pain pills. Eventually, buprenorphine’s effects level off until recovering addicts experience the “ceiling effect”. At this stage, they should no longer suffer withdrawals or strong cravings for their opioid of choice.
Opioid Addiction Treatment & Suboxone
Containing both naloxone (Narcan) and buprenorphine, Suboxone treats opioid addiction by reducing the intensity of cravings and withdrawal symptoms. It blocks opioid receptors in the brain and prevents addicts from experiencing the euphoria produced by heroin and other opioids. Suboxone is typically prescribed during the maintenance stage of treatment, after the addict has taken another medication called Subutex (oral buprenorphine) for several weeks.
Only psychiatrists or MDs with special identification numbers assigned by the U.S. Drug Enforcement Agency can prescribe Suboxone.
When treating opioid addiction, buprenorphine effectively works as a stepping stone drug. High levels of the drug are prescribed, resulting in an addiction to buprenorphine, which is also an opioid. However, because it is only partially antagonist, this drug does not produce a threat of respiratory distress, like normal opioids. Weaning from buprenorphine is generally safer and easier to control than weaning away from illegal opioids.
Suboxone, a combination of buprenorphine / naloxone drug is the most commonly prescribed drug for opiate addiction withdrawal treatment, in part because it is specifically designed to combat abuse of buprenorphine. The buprenorphine portion of the drug works exactly as described above when used to treat opiate addiction. However, the naloxone portion of the drug exists only to deter abuse.
Naloxone does not provide any beneficial medical effects in this combination drug. In fact, if taken properly (orally), it does absolutely nothing because it isn’t absorbed into the body. When injected, though, it is absorbed and that absorption results side effects that are nearly identical to buprenorphine withdrawal effects. These side effects can help limit the most common form of abuse in ways that buprenorphine alone simply can’t.
Administration of Suboxone
Both medications are prescribed as sublingual (under the tongue) tablets or in film form. Lower than normal doses of buprenorphine are given during the first few days, with a gradual increase in dosage occurring over a period of several weeks. Eventually, recovering addicts will switch to Suboxone to complete the final stage of their medication assisted treatment. Doctors may adjust dosing amounts according to patient response.
Treatment with Buprenorphine / Naloxone
Approved by the FDA in 2002, Buprenorphine / Naloxone is now considered an essential component of medication assisted treatment (MAT) for an opioid addiction. Research indicates that when used in combination with behavioral and addiction counseling therapies, buprenorphine supports a “whole patient” method of successfully treating and managing opioid dependence.
Side Effects of Buprenorphine / Naloxone
People taking buprenorphine or Suboxone may experience side effects similar to opioids side effects. These include:
- Nausea and vomiting
- Dry mouth
- Muscle cramping/aching joints/fever
- Gastrointestinal problems
- Insomnia/nighttime restlessness
These side effects should diminish as tolerance builds to the drug.
The Cause Of The Opioid Addiction Epidemic
Opioid addiction is an epidemic health issue in the U.S today. The World Health Organization estimates over 2,000,000 opioid abusers currently struggle with addiction to illegal opioids and prescription medications meant to alleviate pain.The epidemic is so severe that opioid overdose now ranks second behind car fatalities as the most common cause of accidental death.
The increased need for buprenorphine may be attributed to liberalization of laws regulating the ability of physicians to prescribe opioids for treating chronic non-cancer pain. Heroin prices have also dropped over the past 20 years, making heroin a viable alternative to prescription opioids when physicians stop prescribing pain killers to patients who have become addicted to medication.
Buprenorphine For Pain Relief
For individuals that are not opioid tolerant, buprenorphine, in low dosages, works well for relieving chronic pain when taken via a dermal patch. However, it can only provide limited pain relief and does not offer any meaningful benefit for acute pain or for short term pain, like pain which is the result of a recent injury or surgical procedure.
Getting High – Buprenorphine Abuse
Buprenorphine abuse is relatively common in those that were previously addicted to opioids, because it produces roughly the same effects during a high and is less difficult to get. The drug can be obtained by faking chronic pain, purchasing illegally from someone who has chronic pain, or from an opioid withdrawal program.
Prescription patches are particularly easy to abuse because they are portable, discrete, and provide exactly what is needed to curb a physical addiction. Pills, on the other hand, because they are absorbed through the digestive system, do no provide quite the same impact. As a result, abusers often grind the pills up and convert them to an injectable drug.
Finally, while rarely done, because it is highly dangerous, it is also possible to abuse implanted buprenorphine. Normally, implanted buprenorphine is designed to provide a constant and controlled stream of the drug for about six months. If the implant is carefully manipulated, the level of the drug being released can be increased. If done right, this results in a near constant high. If done wrong, it results in an overdose and possibly death.
Withdrawal of Buprenorphine / Naloxone
Buprenorphine is both physically and psychologically addictive. Any gap in use of the drug, including due to intentional withdrawal for the purposes of treatment results in the following side effects:
- Fluctuations in appetite
- Flu-like symptoms including headaches, nausea, cold flashes, general body pain, and sweating
- Difficulty sleeping or staying awake, often resulting in constant restlessness
- Fluid leakage, from both the nasal cavity and eyes
- Dilation of the pupils
- Changes in mood
In a controlled setting, like a rehabilitation clinic, these symptoms can be safely controlled. In an uncontrolled setting, they can result in dangerous dehydration, recklessness with heavy machinery like cars, and loss of motor controls, all of which could cause significant, even fatal, harm.