What Is Buprenorphine?
Buprenorphine is a semi-synthetic drug made in laboratories that is used to treat chronic and severe pain and to help recovering opiate/opioid users avoid withdrawal symptoms. Buprenorphine is made from thebaine, an alkaloid derived from opium poppies. Because it is derived from opium poppies, buprenorphine is an opioid drug.
How Is Buprenorphine Used?
Buprenorphine is available in brand names SUBUTEX®, BUTRANS® and BUPRENEX®. Additionally, buprenorphine preparations with drug naloxone are available in brand names SUBOXONE® and ZUBSOLY®. Buprenorphine is also available in sublingual tablets (taken by placing under the tongue and allowed to dissolve slowly). Sublingual films (which work like sublingual tablets) and extended-release transdermal patches are also available. Buprenorphine hydrochloride is used for deep injection in the muscles (intramuscular) and for transfusion in the veins (intravenous).
Buprenorphine has medicinal value in relieving moderate to severe pain, much like its sister drug, morphine. In this way, buprenorphine is a painkiller and doctors prescribe it to patients suffering from persistent pain caused by surgery, cancer and neuropathy. What are some other effects of buprenorphine? However, buprenorphine is also valued therapeutically because it can be used as opiate substitution therapy for former drug addicts. Buprenorphine delays symptoms of opioid/opiate withdrawal and addresses cravings for stronger narcotics like morphine or heroin.
Some people use buprenorphine as a recreational drug. Like other opioids, buprenorphine can elicit euphoria described as “high” that causes some people to abuse the drug. Some users describe having pleasant feelings, elevated mood and drifting consciousness on using buprenorphine. Still, buprenorphine can cause adverse effects, some of which are life-threatening.
Signs of overdose or indications that you should stop buprenorphine use include:
- feelings of faintness
- respiratory depression or cessation of breathing
Is Buprenorphine Addictive?
Yes, buprenorphine can be addictive. But its addiction liability is considered low. Like other opioid drugs, buprenorphine does have potential to become habit forming (a.k.a. buprenorphine dependence) and also has potential for abuse. These are the main reasons why buprenorphine use and availability is highly restricted. The main signs of problems with buprenorphine abuse include:
- compulsive or obsessive thinking about buprenorphine
- craving more buprenorphine when doses are lowered or stopped
- loss of control of buprenorphine use
- using buprenorphine despite negative consequences to home, work, or health
Can you inject Suboxone?
Yes. But the effects of injecting depend on the opioid tolerance of the person injecting buprenorphine. We review injecting Suboxone here, and invite your questions, comments, or feedback about treatments for Suboxone addiction at the end. In fact, we try to respond to all questions about signs or symptoms of Suboxone addiction with a personal and prompt response.
Why Inject Suboxone?
One common reason for injecting buprenorphine relates to the low oral bioavailability of the drug. Only 25-30% of sublingual buprenorphine reaches the blood circulation, compared to 100% of injected buprenorphine.
Some people who inject buprenorphine claim that they are trying to stretch the action of illicit buprenorphine 4-fold, so that 8 mg prevents cravings and withdrawal for 4 days rather than one. Because of the shortage of buprenorphine-certified physicians in many areas, many addicts ‘treat’ themselves with buprenorphine purchased on the street at inflated prices.
Suboxone Injection And Buprenorphine Tolerance
The brain does not distinguish between buprenorphine that has been injected and buprenorphine taken sublingually. The brain is subject to a more rapid rise in blood level of buprenorphine when the drug is injected. But the effects of injected buprenorphine vary with tolerance.
Buprenorphine has a long half-life (i.e. stays in the body longer than most medications). If a person injects usual clinical doses of buprenorphine daily, tolerance will develop to the medication after a week or two. At that point, injecting buprenorphine will not result in any significant subjective effects, just as sublingual doses do not have significant effects in patients tolerant to buprenorphine.
However, a person who is used to taking large amounts of illicit opioids (greater than 80 mg of oxycodone, for example) will usually experience sudden and severe withdrawal symptoms after injecting buprenorphine. The effects are similar, but more rapid, than the effects of sublingual buprenorphine in the same person.
Little Incentive To Inject Suboxone
The pharmacology of buprenorphine removes much of the incentive to inject the medication. For regular opioid users, injection of buprenorphine precipitates withdrawal. People who inject buprenorphine regularly are essentially ‘on buprenorphine’, and have little subjective effect from the medication. People who get ‘high’ from injecting buprenorphine are those who have a low opioid tolerance, who use buprenorphine infrequently (i.e. every few days or less often).
Does Suboxone cause weight gain or loss?
Suboxone is an opioid man-made synthetic drugs used in the treatment of opiate addiction and occasionally prescribed for pain relief (more on Suboxone for pain). However, any effects of buprenorphine on weight gain/loss are consistent with the effects of all opioid pain pills. So how does Suboxone affect weight? We review here. Then, we answer your general questions about Suboxone, Suboxone injections, or its use at the end.
Suboxone And Weight Gain
Opioids are not directly related to weight gain, but the people who abuse opioids, or abuse buprenorphine, often have other aspects of an unhealthy lifestyle, such as lack of exercise and poor food choices.
Suboxone And Weight Loss
Weight loss is common during active opioid dependence. Opioid intoxication often causes nausea and anorexia. Opioid withdrawal is almost always associated with loss of appetite and weight loss. Additionally, active opioid addiction causes weight loss, but is NOT a healthy way to stay thin!
Normalizing Weight On Suboxone
After stabilization on buprenorphine, some people gain weight from the return to a normal appetite. They find that they are the same as people without opioid dependence in needing exercise and dietary changes in order to avoid weight gain.
How does buprenorphine block opiates?
How Buprenorphine Blocks Opiates
In biochemistry and pharmacology, a ligand is a substance (usually a small molecule), that forms a complex with a bio molecule to serve a biological purpose. Ligands bind to central nervous system nerve receptors through reversible mechanisms based on chemical principles. Positive charges on ligands are attracted to negative charges on receptors, and vice-versa.*
Envision the keyhole on your car, to understand how ligands like buprenorphine work at receptors. Your key is the ligand, and the keyhole is the receptor on the membrane of a nerve cell. Here are three (3) scenarios:
1. Agonists – If your key is an ‘agonist’ similar to oxycodone or methadone, you can insert it into the lock and turn it fully to unlock all of the doors.
2. Partial agonists – A ‘buprenorphine key’ may enter the keyhole but only turn part of the way, enough to unlock only one door. That buprenorphine key then prevents a full agonist key from unlocking the rest of the doors.
3. Antagonists – On the other hand, if an antagonist key would be inserted, it doesn’t turn to unlock any doors. Rather, an antagonist (like naltrexone) prevents any other keys from acting at the receptor.
Buprenorphine As A Ligand
Ligands compete for binding at receptors. Some ligands match up so closely that they effectively out-compete other drugs for actions at the receptor. Some ligands do not match up as well, so their effects require higher concentrations at the receptor in order to compete with other ligands.