Buprenorphine is a semi synthetic opioid with agonist and antagonist actions. It is used in a similar manner as Methadone in the treatment of Opioid addiction and is considered a much safer and more effective alternative. It is extremely potent compared to other opioids and is sold under various brand names and in various forms.
Buprenorphine comes in various forms and dosages, from low dose patches for pain relief to high dose sublingual films for maintenance. Here we'll detail the most common preparations of Buprenorphine:
Suboxone is a form of buprenorphine used for opiate replacement therapy. It is a combination of buprenorphine and naloxone, and it comes in four different strengths, 2mg buprenorphine/0.5mg naloxone, 4mg buprenorphine/1mg naloxone, 8mg buprenorphine/2mg naloxone, 12mg buprenorphine/3mg naloxone. It was at one point widely believed that injecting Suboxone was impossible because of the inclusion of Naloxone, however Buprenorphine's μ-receptor binding affinity is much higher than Naloxone's, rendering it essentially inert. suboxone offers a lemon-lime flavor.
Subutex is a form of buprenorphine used for opiate replacement therapy as well, often used during therapy induction. Unlike Suboxone, Subutex contains no Naloxone.
Zubsolv is a new preparation of buprenorphine used for opiate replacement therapy. Zubsolv, like suboxone, contains Naloxone. Zubsolv utilizes Orexo’s proprietary sublingual platform technology, which comprises enhanced trans-mucosal absorption of active pharmaceutical ingredients, mucosal micro-particle adhesion, as well as taste masking, formulated in a rapidly disintegrating sublingual tablet. These improvements allow for a tablet that dissolves faster and increases absorption levels, allowing for lower overall dosages being administered compared to other buprenophine ORT medications. Zubsolv is available currently in two dosages: 5.7mg buprenorphine/1.4mg naloxone and 1.4mg buprenorphine/0.36mg naloxone. Zubsolv offers a menthol flavor.
Temgesic is an analgesic preparation of 0.2mg buprenorphine for sublingual use.
Buprenex is a preparation of buprenorphine for parenteral (injectible) use, 0.3 mg/ml.
Norspan/Butrans are transdermal patches of buprenorphine that are indicated for the management of moderate to severe chronic pain in patients requiring a continuous, around-the-clock opioid analgesic for an extended period of time. Both Norspan and Butrans are available in 5, 10, and 20 µg/h, 7-day patches.
On Buprenorphine, Naloxone, and Alternate Routes of Administration
Buprenorphine and naloxone are both commonly administered via the intravenous route individually, which is nothing unusual. As for the actual active components, buprenorphine has a higher specificity for the μ-opioid receptor than naloxone. In fact, buprenorphine overdose may not be completely treated with naloxone alone. The standard procedure for bupe OD calls for a larger initial dose of naloxone and continued perfusion of the drug as long as there is respiratory depression. So in concomitant administration of the two, especially in the 4:1 ratio found in Sub, the buprenorphine would be the only thing binding to opioid receptors. Coadministration of buprenorphine and naloxone is not dangerous per se and anecdotal reports bear this out. The things that make Suboxone tablets or films harmful to inject are the lactose, flavorings, dyes, and God knows what other fillers. They're sublingual for a reason. This (and the fact that junkies have a tendency to try and shoot anything) are the reasons that the prescribing sheet accompanying Suboxone throws such a fit about IV use. But with proper injection technique and sterility (use wheel filters!) Buprenorphine injection can be rendered safe.
Even without a wheel filter Suboxone can be filtered and clarified by dissolving the tablet or film in cold water rather than room-temperature (or god forbid, hot) water. The cold temperature of the water doesn't allow the fillers and particulate matter in the pills/films to dissolve completely, allowing for them to be filtered out much more easily. If the solution is heated, it may look clearer, but that's because the filler material has been allowed to dissolve into the solution. A good dissolved solution should look extremely cloudy before filtering and clear after filtering, whereas a heated solution will appear clear throughout the process. If you aren't using a wheel filter, using cold water to dissolve your solution and filtering multiple times is highly advised to increase safety. Don't heat it!
As for insufflation, buprenorphine has much higher bioavailability through that route, something along the lines of 65% as opposed to 30% for sublingual, whereas naloxone is not water soluble enough to have any appreciable bioavailability when snorted or taken as intended. It's sole purpose in the drug is to deter injection, though, as we have already seen, it cannot displace buprenorphine from the opioid receptors. It's a kind of bluff on the part of pharmaceutical companies, which for the most part has worked quite well considering the common (and incorrect) belief that the injection of Suboxone "won't work" or that it'll induce withdrawals. In any case, naloxone's average half-life is 0.5-1.5 hours whereas bupe's average is 37 hours, so the naloxone would wear off first. Here it must be mentioned that when anyone with an opiate habit attempts to IV buprenorphine itself, let alone naloxone, they will be treated to a case of precipitated withdrawals if the bupe (or naloxone) is taken too soon. Snorting Suboxone is not very dangerous if done properly and some consider it a much better use of a very expensive medication. Just take a little under half of your typical sublingual dose and go from there. For many on this website, insufflation is the preferred ROA. Just remember NOT to swallow the powder or try to get a "drip," you'll just be swallowing it and wasting it, instead try to keep it in your sinuses.
As for genuine dangers regarding Suboxone, be aware that the shit is potent. Someone with little to no tolerance could easily OD on one pill. That's why you commonly see threads like "I snorted half of this orange pill and I've been puking for 24 hours... What gives?" As always, research and respect the drugs you use. Don't be a statistic.
If an individual has zero tolerance, taking more then 2mg (and even still 2mg) may result in excessive puking from being so fucking high. A good dosage for a beginner is 1/5th or 1/6th of an 8mg pill. A ceiling effect is reached at 32mg, meaning a person cannot take more than 32mg as anything over that will not be active, effectively wasting your delicious opi.
Note on IV Suboxone and Naloxone Activity
While a lot of people claim that Suboxone (Buprenorphine & Naloxone in a 4:1 ratio) is safe to IV as the buprenorphine has a higher receptor affinity, this is only a half-truth. The problem is that Bupe has diminished returns once you go over 8mg (meaning that the difference in potency between 8mg - 12mg is a lot smaller than the difference between 4mg - 8mg, and so on) the higher your dose goes the smaller the amount of extra opioid effects it will cause, until you reach the ceiling dose of 32mg.
What this means is that while it might be safe to shoot 4mg of suboxone, as 4mg will overpower the 1/2mg of naloxone, by the time you reach 12 - 16mg, the extra opioid agonism from the higher bupe dose will taper off, while the naloxone increases linearly in potency. Eventually, you reach a stage somewhere between 8mg and 24mg (nobody has been brave enough to determine exactly where) at which the naloxone will become powerful enough to override the bupe. This isn't an issue if you aren't dependent, it just means your bupe will take longer to kick in, but it does mean that if you are dependent on buprenorphine (generally because you're on suboxone maintenance) the naloxone will kick it off the receptors, causing you to go into horrible precipitated withdrawals just as it would for any other opiate. For someone who's been on suboxone for months or years, this means being instantly thrown into 2 - 3 hours of the worst depths of withdrawal. It's just as painful as it sounds, so titrate your dose carefully if you want to inject suboxone and you're buprenorphine dependent.
- This is debatable. Buprenorphine has higher receptor affinity than Naloxone, meaning that the Naloxone will have a difficult time displacing the Buprenorphine that has binded to the opiate receptors regardless of saturation levels. (Higher saturation =/= higher binding affinity.) This renders the Naloxone essentially inert in Suboxone preparations. Most Precipitated Withdrawals occur because a tolerant user takes or uses Buprenorphine too soon after another dose of a different opiate. The naloxone doesn't displace the other opiate, but the Buprenorphine itself, with it's "competitive antagonism" can displace most other opiates easily. This is also why in cases of non-tolerant users overdosing on Buprenorphine, Naloxone alone often isn't used as a antagonist, as it's affinity isn't strong enough to displace the Buprenorphine from the receptors.
Drugs that Cause Possible decrease in Absorption
Any type of anti-fungal medication especially if taken orally. Examples: (Fluconazole, Amorolfine, Ketoconazole.) With Buprenorphines need to be orally dissolved for it to be of any use in the body, While on these medicines it cannot be absorbed properly. Call your prescribing physician if you are somehow made to take this medicine.
Extra High On Buprenorphine?
CYP3A4 is the primary enzyme involved in the creation of NOR-BUP[A Higher more potent version of Buprenorphine] Found in St John Wort. PLEASE READ FOLLOWING!
Buprenorphine has one major dealkylated metabolite: Norbuprenorphine. Here is some information on its agonist properties, and binding affinities:
NorBUP exhibited high affinities for Âµ-, delta -, and kappa -opioid receptors with Ki values in the nanomolar or subnanomolar range, comparable to those of BUP. NorBUP and BUP had low affinities for the ORL1 receptor with Ki values in the micromolar range. In the [35S]GTPgamma S binding assay, norBUP displayed characteristics distinct from BUP. At the delta -receptor, norBUP was a potent full agonist, yet BUP had no agonist activity and antagonized actions of norBUP and DPDPE. At Âµ- and kappa -receptors, both norBUP and BUP were potent partial agonists, with norBUP having moderate efficacy and BUP having low efficacy. At the ORL1 receptor, norBUP was a full agonist with low potency, while BUP was a potent partial agonist. In the writhing test, BUP and norBUP both suppressed writhing in an efficacious and dose-dependent manner, giving A50 values of 0.067 and 0.21 mg/kg, s.c., respectively. These results highlight the similarities and differences between BUP and norBUP, each of which may influence the unique pharmacological profile of BUP.
Norbuprenophine is a more potent agonist in most areas, and has a higher affinity in most areas. Though it is allegedly not good at crossing the BBB(Blood Brain Barrier) , This is different for everyone and it could be dangerous to someone inexperienced. As the risk for respiratory depression without a "high" feeling is very likely.
Buprenorphine is metabolized into Norbuprenorphine almost entirely by the P450 cytochrome. This being the case, a P450 Inducer should increase the ratio of Nor-buprenorphine to Buprenorphine. Unfortunately there are not many easily obtained P450 inducers on the market...except for one: St. Johns Wort.
SJW is actually a fairly potent P450 inducer, and it specifically involves the enzymes most important of the P450's in the creation of NOR-BUP.
The ratios of the treatment to baseline values for CYP3A4 using cortisol as the probe were 1.5 [95% confidence interval (CI) 1.3, 1.9] for males, and 1.9 (1.1, 3.0) for females. The corresponding ratios using dextromethorphan as the probe for CYP2D6 were 0.9 (95% CI 0.5, 2.1) for males and 1.9 (1.3, 3.2) for females. For CYP1A2, a significant increase in the metabolic ratios was found only for females (ratio of values 1.2; 95% CI 1.1, 1.4). No influence of SJW on CYP2D6, NAT2, and XO activities was observed.
CYP3A4 is the primary enzyme involved in the creation of NOR-BUP. The others it induces are also involved in its metabolism; furthering its effect on Nor-bup "synthesis".
Its is a risk but as any user knows its all a risk. Either lose perfectly good Bupe, Or risk Respiratory Depression.
Again, please we ask no one try this out. Is it really worth it? Take something else if you want a "High", or stick to taking your medication to keep you away from the "bad" drugs.
Common Questions about Suboxone
Q: "I took suboxone _____ hours ago and was wondering if it was a waste of pills to take another opiate." A: If you take suboxone daily in whole doses (whole tablets) then expect ~36 hours before taking another. But, if you don't do suboxone chronically 12 hours is fine.
Q: "I took said 'Opiate' 4 hours ago, is it safe to take suboxone/Nalaxone?"
A: NO. This will cause precipitated withdrawls and you will think about calling the ambulance. Its an intense withdrawal because the Nalaxone kicks the opiates off the receptors. Depending on the half life of the said 'Opiate', to be safe 24 hours. For Methadone- 36-72 hours. = Higher Half-Life. Lortab 20mg - 8 Hours.. Depending on your size and tolerance and titration of opiates in your body. Your risk, your choice. Too early you will be in the hospital. I have had it happen twice, taking more suboxone does not help. Take a few Benzo's/clonodine and ride it out for a few hours in the shower floor.