All You Need to Know About Buprenorphine
Before we go into an in-depth discussion about buprenorphine, let us first take a quick look at the reason why it came to be in the first place – opioid addiction.
We have been fighting drugs in this country for more than 100 years and despite all the effort on the legislative front and from law enforcement, addiction to opioids has reached epidemic proportion. Opioid-related deaths continue to increase, with an opioid drug implicated in 3 out of every 5 overdose deaths.1 A recent survey found that there are currently 5.5 million people addicted to opioids in the US.2
The late 1990s saw the medical community prescribing opioid pain relievers left and right upon assurance from pharmaceutical companies that their patients would not get addicted. This, of course, led to widespread misuse, even of the nonprescription opioids, before it came to light that these drugs indeed can be highly addictive. More than 42,000 deaths in 2016 were opioid overdoses, the highest of any year previously, and 40% of all these deaths were from prescription opioid.1
New measures from the government include such changes as getting more people into treatment and recovery programs, limiting opioid prescriptions and investigating what role pharmaceutical companies play in the grand scheme of things.3
Opioid Treatment Programs (OTP) make use of medications as well as behavioral therapy to treat substance use disorders (SUD). Buprenorphine is one of the three medications commonly used in OTPs along with Methadone and Naltrexone.4
What is Buprenorphine?
Is buprenorphine an opioid? Yes, it is. It is semi-synthetic opioid that comes from thebaine, an alkaloid of the opium poppy (aka Papaver somniferum aka bread seed poppy).
Compared to other opioids, however, buprenorphine is a partial agonist, meaning it can bind to a particular receptor in the brain but will only have partial ability to produce the opioid effect compared to a full agonist. In plain English, this means that while it is indeed an opioid that can cause euphoria, respiratory depression etc. like any other opioid, its maximum effects are less than those produced by its full agonist cousins like heroin and methadone.
When given at low doses, buprenorphine’s agonist effect is enough to help people (who are addicted to opioids) discontinue using those other opioids without suffering from withdrawal symptoms. Increasing the dose will also increase the agonist effects, again just like any other opioid – but unlike these other opioids, buprenorphine is unique in that it has this property called “ceiling effect”. This means that there is a point at which the agonist affects plateau or reach a “ceiling”, regardless of whether the dose continues to increase.
The risks of abuse, addiction, and side effects are therefore lower with buprenorphine compared to full agonists. This drug actually blocks the effects of full agonists and cause withdrawal symptoms to kick in if given to a person currently high on a full agonist. Buprenorphine’s higher affinity to the opioid receptors in the brain is what allows it to displace other opioids, occupy the receptors and block other opioids from binding to it.
What is Buprenorphine Used For?
Buprenorphine is an opioid analgesic, so it is basically a pain reliever and thus used to treat moderate to severe pain. Buprenorphine dosage for pain differs according to the method of administration. It may be administered parenterally with a 0.3mg dose every 6-8 hours. When administered sublingually, a typical 0.4mg dose lasts 8 hours or the equivalent of 10mg of morphine injected intramuscularly every 4hours. Buprenorphine is used also as an epidural for cesarean section and post-operative pain.5
Physicians also use buprenorphine to treat opioid addiction, either in their clinic or as a take-home drug dispensed directly from the clinic. Given in appropriate doses during treatment, buprenorphine can:
- Block the effects of other opioids
- Decrease opioid cravings
- Suppress opioid withdrawal symptoms
- Help patients stay in treatment
- Reduce illicit use of opioids
While the risk of buprenorphine abuse and addiction are lower especially under medical supervision, it is still there. It may have given hope to many opioid addicts, but to others, it is simply dope. Those who use buprenorphine recreationally, or without medical supervision, use it in combination with stronger drugs so they can achieve a greater high.
A Brief History of Buprenorphine
- From 1958-1963 Edinburgh-based McFarlan Smith, the main producer of opium alkaloids in the UK at the time, and Reckitt & Colman (Reckitts), a home products company based in Hull, England went into a joint venture to develop OTC analgesics. Kenneth Bentley, the “Father of the Bentley Compounds” was with McFarlan Smith at the time. John Lewis, Oxford-trained chemist and doctoral student of Nobel-prize-winning organic chemist Sir Robert Robinson was with Reckitts. According to Lewis, it was Bentley who laid down the chemical foundation for the opioid drug development project at Reckitts. Bentley believed that opioids with more complex structures compared to morphine could retain their desirable actions while dropping the adverse side effects. When McFarlan Smith was absorbed into another company, Reckitts came into sole control of the joint project.
- In 1966, Ricketts discovered Buprenorphine. They supplied it to the Addiction Research Center in Lexington in the 1970s.
- By 1975, Lexington researchers were studying the drug as a potential medication for addiction treatment because of its agonist and antagonist properties. ARC’s Donald Jasinski suggested that buprenorphine effectively blocked morphine because it has the combined characteristics of methadone and those of a pure opiate antagonist. He singled-out buprenorphine for its unique pharmacology in humans – for producing very little physical dependence even with long-term use. Jasinski declared that the 50-year project that hoped to potentially use narcotics therapeutically for pain relief and addiction treatment without resulting to physical dependence has given birth to buprenorphine, citing that the drug offers the advantage of both methadone and naltrexone without their disadvantages.6
- In 1990, the Medications Development Division (MDD) was established by NIDA to work closely with the pharmaceutical industry, the academe, and government agencies like the FDA to develop and evaluate medications for addiction treatment such that they could survive the FDA approval process.
- In 1993, the MDD approached Reckitts and formalized its interest in developing buprenorphine as a treatment for addiction. The interest was for both buprenorphine by itself and buprenorphine + naloxone.
- In 2000 the Drug Addiction Treatment Act of 2000 enabled qualified doctors to treat dependence to opioids by prescribing or dispensing narcotics, including buprenorphine. This Act, however, limits those who can be given buprenorphine to 30 patients per practice. The bigger facilities that have many practicing doctors can only still treat 30 opioid-addicted patients at a time.
- In 2002, the FDA approved Suboxone® (Buprenorphine and Naloxone) tablets and Subutex® for opiate dependence treatment.
- In 2005 the 30-patient limitation per medical group practice under DATA 2000 was lifted, allowing individual doctors to each have 30 patients. This 30-patient limit was increased to 100 by Bill H.R. 6344 the following year.
- In 2009, the FDA approved a generic version of Subutex®. This brand was discontinued in 2011.
- In 2012, Suboxone® tablets were discontinued and replaced by Suboxone® Film.
- In 2013, the FDA approved generics for Suboxone® and approved Zubsolv sublingual tablets.
- In 2014 Bunavail buccal film became available.
- In 2016, The Department of Health and Human Services raised this 100-patient limit further to 275 for qualified physicians. In the same year, the Comprehensive Addiction and Recovery Act of 2016 made Physician Assistants and Nurse Practitioners eligible to prescribe buprenorphine to treat opioid use disorder by amending the Controlled Substance Act. This year, Probuphine® subcutaneous implant was approved by the FDA. It provides a 6-month steady dose of buprenorphine.
Trade Names for Buprenorphine
- Buprenorphine only
- Buprenorphine + Naloxone
Street Names for Buprenorphine
It is important to know how buprenorphine is referred to on the streets. A friend or family member may be into it.
Buprenorphine Side Effects
Being an opioid itself, the side effects from buprenorphine use are similar to those of other opioids:8
- Difficulty sleeping
- Muscle aches
How Long Does Buprenorphine Stay in the Urine?9
Drug detection time varies depending on factors like a person’s metabolism and overall physical condition, age, physical activities prior to urine collection, food and beverage intake, dosage of the drug and frequency of use, time interval between last use and urine collection, urine pH etc. Buprenorphine is not a standard test like the SAMHSA 5 (Cannabinoids, Cocaine, Amphetamines, Opiates, PCP) but it is available in some advanced urine drug test kits when required, say for employment testing. Typically, buprenorphine may be detected in urine for up to 6 days.
Forms and Methods of Use
Signs & Symptoms of Buprenorphine Addiction
It isn’t always easy to spot the signs of buprenorphine addiction and it often progresses to a major health concern for the patient before even close family members realize the problem. Knowing what signs to watch out for will enable the same family members to help their loved ones before they fall any deeper into the habit. Combining buprenorphine with other drugs, as many recreational users do, is very dangerous and can be fatal.
- Doctor shopping
- Making fake/false prescriptions
- Intense cravings for the drug
- Buying illegally
- Preoccupation/obsession with getting and taking the drug
- More frequent dosing
- Prolonging use of the drug despite negative effects
Buprenorphine Addiction Treatment
It is ironic that this drug which is used to treat opioid addiction can itself result in an addiction on top of what it’s supposed to be treating. The reality is that buprenorphine is an opioid, with much the same effects like the rest of its family, albeit milder. The withdrawal symptoms may or may not manifest depending on how it is used. These include headaches, agitation, nausea and sweating and can be quite severe when the drug is misused.
Perhaps the best option for buprenorphine addiction treatment is thru an in-patient program, where the patient will be closely monitored to help them better overcome their physical dependence to the drug on the way to complete detox. They will also have easier access to therapies that can address whatever deeper emotional issues may be driving their addiction.
If in-patient treatment is not an option, outpatient treatment can help taper one’s use of buprenorphine at the very least. The patient will also have access to counseling sessions.
Talk therapies are part of the behavioral modification approach to drug treatment. They help patients whether inpatient or outpatient, delve deeper into the emotional root of their addiction.
Whichever treatment option a patient chooses, the importance of clinical drug testing should be emphasized. It is a critical tool that can measure their response to the treatment.
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