Buprenorphine

 
2.6 (2)
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More about Buprenorphine

What is/are Buprenorphine?

Buprenorphine is a semi-synthetic opioid that is used to treat opioid addiction in higher dosages (>2 mg), to control moderate acute pain in non-opioid-tolerant individuals in lower dosages (~200 µg), and to control moderate chronic pain in dosages ranging from 20–70 µg/hour. It is available in a variety of formulations: Subutex, Suboxone (buprenorphine HCl and naloxone HCl; typically used for opioid addiction), Temgesic (sublingual tablets for moderate to severe pain), Buprenex (solutions for injection often used for acute pain in primary-care settings), Norspan and Butrans (transdermal preparations used for chronic pain).

Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, generally available as Temgesic 0.2 mg sublingual tablets, and as Buprenex in a 0.3 mg/mL injectable formulation. In October 2002, the Food and Drug Administration (FDA) of the United States also approved Suboxone and Subutex, buprenorphine's high-dose sublingual tablet preparations indicated for detoxification and long-term replacement therapy in opioid dependency, and the drug is now used predominantly for this purpose.

In the European Union, Suboxone and Subutex, buprenorphine's high-dose sublingual tablet preparations, were approved for opioid addiction treatment in September 2006. In the Netherlands, buprenorphine is a List II drug of the Opium Law, though special rules and guidelines apply to its prescription and dispensation. In the US, it was rescheduled to Schedule III drug from Schedule V just before FDA approval of Suboxone and Subutex. In recent years, buprenorphine has been introduced in most European countries as a transdermal formulation for the treatment of chronic pain.

Medical uses

Indications

Pain

Depending on the application form, buprenorphine is indicated for the palliation of moderate to severe acute or chronic pain with no neuralgic component (or when the neuralgia is otherwise treated, such as with pregabalin), or for peri-operative analgesia. For the treatment of chronic pain, the transdermal formulations (which were released in the United States in January 2011, but were available in Australia and many European countries years beforehand) are preferred. The intravenous formulation is mainly used in postoperative pain (for example, as patient controlled analgesia [PCA]).

Sublingual buprenorphine (also sometimes taken buccally) for pain is available in the United Kingdom, as well as the Republic of India, in dosages of 200 and 400 µg. It is not available in the United States or in Canada, although Subutex or Suboxone (sublingual buprenorphine for addiction) is sometimes used off-label for this purpose, up to a dosage of 2 mg (the lowest-strength Subutex/Suboxone tablet). Sublingual formulations, such as Addnok, Temgesic, Subutex, and Suboxone, are used either as breakthrough medication for patients on transdermal treatment, or as monotherapy in cases where other treatments are not suitable. Niche pain indications for which sublingual/buccal buprenorphine may be a medication of choice include obstruction of the small bowel; continuous nasogastric suction; oesophageal fistula; malignancy in the head or neck; and other cases where the patient is unable to swallow or this is difficult. Additionally, this form of buprenorphine may be an interesting alternative to sustained-release opioids such as morphine (MS Contin) and oxycodone (Targin).

Advantages of buprenorphine in general in the treatment of chronic pain are, from a clinical perspective, its relatively long half-life, the option of sublingual and transdermal application and the excellent safety profile (ceiling effect for respiratory depression, lack of immunosuppressive effect, low pharmacokinetic interaction potential, no accumulation in renal impairment). Although not enough western literature is available, use of inj. buprenorphine in 'spinal' anaesthesia is rising in countries like India. Up to 150 micrograms of the drug (0.5 mL) of the preservative free solution is added to the local anaesthetic bupivacaine, and a smoother analgesia is obtained with the benefit of the patient remaining pain-free until up to eight to ten hours of the spinal being given.

Furthermore, buprenorphine is somewhat sleep-inducing, and may be of particular help when pain leads to sleeplessness. Other prototypical opioid side-effects may prove beneficial in the management of chronic pain, such as its characteristic euphoria (to alleviate depression due to pain, or in cases where the patient cannot tolerate or is resistant to conventional thymoleptic antidepressants), as well as its anxiolytic effects. Buprenorphine is best used in opioid-naïve patients; its efficacy decreases dramatically with tolerance, and the high doses required in this situation, if combined with other opioids, may lead to opioid discontinuation syndrome.

Precipitated withdrawal and blockade effect

Use in persons physically dependent on full-agonist opioids while not already in withdrawal may trigger an extremely intense form of opioid withdrawal – called "precipitated withdrawal" or "precipitated withdrawal syndrome." This does not occur in all persons tolerant to full-agonist opioids, but rather depends on the severity of dependence and time elapsed from their last dose.

Buprenorphine (Subutex) itself binds more strongly to receptors in the brain than do other opioids, making it more difficult for opioids (or opiates) to react when buprenorphine is in the system. The blockade effect also has the result of blocking endogenous endorphins from binding to receptors, which can lead to psychological alterations in mood and mental capacity. This can cause cognitive and memory deficiencies via blockade of the reward system, which is pertinent to memory formation and normal mental function.

Contraindication

Like full agonist opiates, buprenorphine can cause drowsiness, vomiting and respiratory depression. Taking buprenorphine in conjunction with central nervous system (CNS) depressants in people not tolerant to either agent can cause fatal respiratory depression. Sedatives, hypnotics, and tranquilizers can be dangerous if ingested with buprenorphine by a person tolerant to neither opioids nor benzodiazepines. Co-intoxication with ethanol carries the greatest risk for lethal overdose, with the lowest doses of a reported fatality in a 48 kg teenage girl with 5 mg of diazepam and the equivalent of 8 ounces of beer (1 unit of alcohol), plus around 2 mg of buprenorphine. However, this female was tolerant to none of the three drugs she ingested that were the cause of the multiple drug intoxication fatality.

Adverse effects

Common adverse drug reactions associated with the use of buprenorphine are similar to those of other opioids and include: nausea and vomiting, drowsiness, dizziness, headache, memory loss, cognitive and neural inhibition, perspiration, itchiness, dry mouth, miosis, orthostatic hypotension, male ejaculatory difficulty, decreased libido, and urinary retention. Constipation and CNS effects are seen less frequently than with morphine. Hepatic necrosis and hepatitis with jaundice have been reported with the use of buprenorphine, especially after intravenous injection of crushed tablets.

The most severe and serious adverse reaction associated with opioid use in general is respiratory depression, the mechanism behind fatal overdose. Buprenorphine behaves differently than other opioids in this respect, as it shows a ceiling effect for respiratory depression. Moreover, former doubts on the antagonisation of the respiratory effects by naloxone have been disproved: Buprenorphine effects can be antagonised with a continuous infusion of naloxone. Concurrent use of buprenorphine and CNS depressants (such as alcohol or benzodiazepines) is contraindicated as it may lead to fatal respiratory depression. Benzodiazepines, in prescribed doses, are not contraindicated in individuals tolerant to either opioids or benzodiazepines.

People on medium- to long-term maintenance with Suboxone or Subutex do not have a risk of overdose from buprenorphine alone, no matter what dosage is taken or route of administration it is taken by, due to the "ceiling effect" on respiratory depression. Overdoses occurring in maintenance patients are cases of multiple-drug intoxication, usually buprenorphine taken with excessive amounts of ethanol and/or benzodiazepine drugs. As a matter of course, all patients on buprenorphine maintenance are tolerant to opioids, and maintenance doses are always higher than the dose at which the "ceiling effect" on respiratory depression is reached (~3±1 milligrammes, depending on method of analysis).

People switching from other opiates should wait until mild to moderate withdrawal symptoms are encountered. Failure to do so can lead to the rapid onset of intense withdrawal symptoms, known as precipitated withdrawal. For short acting opioids such as codeine, hydrocodone, oxycodone, hydromorphone, pethidine, heroin, and morphine, 12–24 hours from the last dose is generally sufficient. For longer acting opioids such as methadone, 2–3 days from the last dose is needed to prevent precipitated withdrawal.

Switching from buprenorphine to other opioids is generally safe but requires careful dosing in the first few days. Initially, high doses of the alternate opioid are required to overcome buprenorphine's high receptor affinity. Over the next few days, these doses are reduced as buprenorphine's receptor blockade wears off. This issue is of particular relevance when the drug is used for analgesia: adequate levels of analgesia may be difficult or impossible to obtain without high (and potentially dangerous) levels of the alternate opioid.

Precipitated withdrawal can occur when an antagonist (or partial antagonist, such as buprenorphine) is administered to a patient dependent on full agonist opioids. Due to Buprenorphine's high affinity but low intrinsic activity at the mu receptor, it displaces agonist opioids from the mu receptors, without activating the receptor to an equivalent degree, resulting in a net decrease in agonist effect, thus precipitating a withdrawal syndrome.

It is a common misconception that the Naloxone in Suboxone initiates precipitated withdrawal. This is false. The Naloxone can only initiate precipitated withdrawal if injected into a person tolerant to opioids other than buprenorphine. Taken sublingually the Naloxone has virtually no effect. Even in injection scenarios Buprenorphine has a higher binding affinity for opioid receptors then even Naloxone, resulting in a fairly limited effect of the antagonist in any scenario.

Use in pregnancy

Unfortunately, due to the unique qualities of both methadone and buprenorphine, switching to and using buprenorphine during pregnancy instead of methadone is unlikely to be helpful, since the strain of withdrawal on the body is far more dangerous to the fetus than using a traditional opiate such as methadone. Data suggest that, after the first few weeks of life, no developmental differences are found between children born to mothers that were stable on an opiate during pregnancy versus those that were not taking opiates during pregnancy. Babies born to mothers addicted to opiates show signs of withdrawal if not addressed soon after birth This stands in stark contrast to the pathology seen after using the (otherwise socially acceptable) drug alcohol during pregnancy. It is notable that data regarding buprenorphine's safety during pregnancy is less available than is data on methadone use during pregnancy. There is a considerable body of evidence that proper methadone use during pregnancy is safe, and that there are few (if any) significant lasting effects on the children of mothers who use medically supervised methadone regimens during the gestation period. However, recent research has indicated methadone during pregnancy does indeed have a negative effect on the fetus, and needs to be followed up with further research to determine the full amount of damage done to the developing fetus by the methadone.

Detection in biological fluids

Buprenorphine and norbuprenorphine (the major active metabolite of buprenorphine) may be quantitated in blood or urine to monitor use or abuse, confirm a diagnosis of poisoning, or assist in a medicolegal investigation. There is a significant overlap of drug concentrations in body fluids within the possible spectrum of physiological reactions ranging from asymptomatic to comatose. Therefore it is critical to have knowledge of both the route of administration of the drug and the level of tolerance to opioids of the individual when results are interpreted.

Recreational use

Buprenorphine is also used recreationally, typically by opioid users, often by insufflation. Recreational users of buprenorphine who crush the tablet and snort it report a euphoric rush similar to other opioids in addition to a slight "upper"-like effect. Those already using buprenorphine/Suboxone for opioid addiction therapy find that insufflation is only slightly, if any stronger than taking the pill sublingually, although it may have a quicker onset. Those taking it for addiction therapy also report that obtaining euphoria is virtually impossible after the first few doses, even when doubling or tripling their dosage. Many recreational users also report withdrawal symptoms. Due to the high potency of tablet forms of buprenorphine, only a small amount of the drug need be ingested to achieve the desired effects.

Recreational use of buprenorphine is very common in Scandinavia, especially in Finland and Sweden. In 2007, the authorities in Uppsala county in Sweden confiscated more buprenorphine than cocaine, ecstasy, and heroin. In Finland recreational use of buprenorphine is on the rise; in 2005, Finland's incidence of buprenorphine misuse (most often injected intravenously) surpassed the incidence of recreational usage of amphetamine.

Intravenous administration of dissolved buprenorphine pills and insufflation of pulverized pills are the most common modes of recreational buprenorphine use. This method of recreational use of Subutex is also seen in the Finnish documentary Reindeerspotting. The importer of legal Subutex to Sweden has in November 2012 stopped the sales of Subutex in Sweden due to problems with recreational use and drug induced deaths linked to Subutex.

Use in animals

In the United States and Canada, use of buprenorphine for pain management in animals has become increasingly common, and is a favored analgesic in feline patients for moderate to severe pain. Although registered only for human use by the Food and Drug Administration, it is legal for veterinarians to prescribe it for off-label use in animals they treat.

In the United Kingdom, buprenorphine is licensed for analgesia and sedation in dogs. A solution for injection is made available for the British veterinary market by Alstoe Animal Health under the trade name Vetergesic.

This article uses material from the Wikipedia article Buprenorphine, which is released under the Creative Commons Attribution-Share-Alike License 3.0.

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This page uses publicly available data from the U.S. National Library of Medicine (NLM), National Institutes of Health, Department of Health and Human Services; NLM is not responsible for the page and product and does not endorse or recommend this or any other product.

Reviews for Buprenorphine

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2 reviews

Overall rating 
 
2.6
Overall satisfaction 
 
2.5  (2)
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4.0  (2)
Lack of side effects 
 
1.3  (2)
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hello to all... this is alex from online pharmacy

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How long have you taken this medicine for?
6 months - 2 years
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adam
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zapato is a member of the Pharmacy Reviewer forum
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My opinion and experiences leading to this medicat

Opiate dependency... I miss the original orange tablets like in your photos, they worked so well and at such a reduced amount. I currently use a new form of the medication which is administered orally but not swallowed (Sublingual). It is better tasting than the old tabs and films we all come to know about. But since the FDA (not sure who is responsible but I assume FDA but I have theories if it wasn't) took the tablets off the market so your only option was the film I didn't feel like I was getting what I was with the tabs at a fraction of the mg's (2 mg with tabs vs 8-12 mg on the new films) and I just don't get why I feel so unique and the old suboxone tabs I was given 8 mg and could get by with 1/4 of one per day but maybe 2x depending on my salivation at the time I took it. The new suboxone is a film like those listerine breathe fresheners and taste bad like the tabs but I cannot make 1/4 film cover my symptoms like with the tabs, I currently am on a knock off / more expensive brand which is placed on my inner cheek and dissolves slowly and Covers my dependence at 4.2 mg and works as well as suboxone films if not better and tastes better than the suboxone film. The suboxone film which was 8 or 12 mg and left me feeling that I had done it wrong and it didnt work. I want to come off the med but it is an opiate and much like methadone I don't look forward to the day I have to be institutionalized to come off it. I don't recommend this medicine for humans (being sublingual I assume it would work great on animals that just won't take pills when in pain... Lol. Or not funny the elderly that can't do fentynol patches or pills in general) Anyways back to the review, so my history in one paragraph.

It started with hydros then anything narcotic and commonly found in medicine cabinets which was very infrequent and detoxing was not up to me, more up to supply... Then suggestion by a buddy was methadone maintenance because they never run out, then 11 months after getting on methadone went to rehab and had my shackles removed, only to find that Iowa had lots of chronic pain and could get 3-4 times what I could in MN. But I ended up being back on methadone due to the amount needed was getting to be ridiculous and I was trying to save face with the people I made the commitment to saying I was not going to use pain meds and after the 6 month discomfort from the first rehab from the methadone shackles. I found heroin occasionally after making some untrustworthy friends at the 1st methadone clinic and didn't like thinking that I could either stay sick or die from a dose (who knows what's actually in a baggie??? It could be super potent or it could be brown sugar) I liked that with the pain meds you could know very easily if you were getting what you were buying. But the 2nd methadone I tried to keep secret but it was short lived (hard to hide opiate/methadone withdrawal even for a day) as you need to be very punctual and not do anything against the clinics rules or they would tell they cannot supply you with it due to you weren't here by 10 am or your urine had other substances in it (just a couple examples...) but ended up on Suboxone tabs and thought I had my life back. As it was 1x month appointment and you could go to any pharmacy to get the meds(almost felt normal again). I only had to keep myself off everything else & do what the doctor advised and after 6 months or so on the tablets or one quarter tablet/day I actually had stockpiled enough to last long enough to justify not taking time off work to spend around $250 for these monthly appointments which was covered 0% by insurance and totally justified by the doctor as it needs to cost me something to ensure my sobriety (psuedo-sobriety), well tell me this then, if the doctor wants me to buy that addiction is an illness, say like diabetes, then why wouldn't health insurance cover some of it? So it was easy to justfy stockpiling and disappearing rather than spending $250 to go back after running low with an excuse the doctor would buy (I quit for few to months, or was back on heroin or something of that nature). But I haven't been able to get off the buphenorphine/Suboxone and have been banned from a handful of doctors for various reasons (my fault 100%), I suppose I have to give them more credit than I did as they did attend school for 8 -12 more years than my B- (K-12) average in school, intelligence level. And with the new films I can't stockpile them which made the treatment affordable for someone with just a high school education. I know if I didn't work, or if I made 3$/hour I could get on welfare and get the health care that indigent people get and the meds would be provided but I am an American with entitlement issues, and I enjoy spending money and don't mind having to work for it, but keeping the jobs over a year or two proved difficult. Being that a year into a job suddenly I thought I was more intelligent than my boss or the punctuality thing gave them just cause for getting my walking papers.

Next topic, Equivalence compared to other narcotics (.33 mg tabs is what I think they give for severe pain to people that are not dependent on narcotics or allergic to 95% of the standard pain medications so one 8 mg suboxone is like taking 24 recommended doses of vicodin or percs which can be 2 pills a time so we could double the 24 pill equivalence to 48 pills per day if we are being really technical.  So are we really trading one habit for another? Yes IMHO and if you look at it in the equivalency I have just typed and I hope I am wrong as it is almost more scary thinking to switch to another narcotic would be like 120 mg of oxys per day which was more than i was on at my worst. We maybe not but very close...

So what didn't I mention about the medication? A lot as I am no doctor and I did not sleep at a Holiday Inn last night(I think I am funny too). Rather all my info came experimentation or Wikipedia or online health sites or trying to buy it online. Oh yeah, they put a small amount of the drug police carry now (naloxone) for people that just overdosed from heroin to take all the effects of narcotic pain meds away in an instant. The reason is to keep us from putting it in a hypodermic needle and injecting it like some do with the heroin and more expensive/dangerous narcotics like dilaudid or those patches given to people who are not able to swallow a small pill every 4-6 hours... If I am ever to the point that swallowing a pill is too much to handle I would probably be better off dead and am probably being kept alive to provide jobs for all our medical professionals or to give doctors the opportunities to keep practicing their profession.  I'm sure but given the chance to redo it I would have just stayed off all of them and sweat it out, but time travel is impossible and living on such a high dose of narcotic pain med for so long 24/7 I have been very rough on my body and not really felt it at the times. So I did the brick work or retaining wall work and have very painful hands and knuckles and other injuries that I am sure I toughed out when I should have seeked treatment or a different job. Then add about 20 years since I realized I was never going to Like Mike, (remember those Nike commercials about Air Jordan? Lol) and I am sure I will have issues with pain and now that information is so easily kept and transferred I'm sure any doctor will never prescribe anything with a narcotic in it other than maybe t-3s if I am lucky because of liability issues, and our medical histories not being kept private. If China or North Korea can access top secret government info by computers then I can't believe HIPA will our keep medical info secret for much longer if it's not already overlooked or being ignored. Being at most of recent appointments the doctor is looking at a computer monitor and typing on a ipad.
Best intentions, I know that everything I have complained about came about came from people's best intentions so I will stop writing and start wishing for big $ to fall into my pockets because IMHO the only way to get what you want or need in today's society in America is with $.. Money talks and the rest walks. And if you read this and are offended in any way I am sorry I only found it strange the latest photos were the tablets which have been absent for years and that no reviews had been written about the medication yet and no photos of the films were uploaded either... I would if I had suboxone which the main brand and the original (other option) than methadone maintenance for opiate dependency.

Thank you for reading and feedback is welcome as it applies to the opiate dependency part I have no experience with pain management as of yet. I am just under 40 and look like an old 25, I guess I am chemically preserved...

Zapato

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How long have you taken this medicine for?
More than 2 years
Z
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