Buprenorphine is a wonderful substance that in the past 5-10years has been introduced as a tool for opiate/opioid addiction therapy. There are just two different formulations that are approved today for opiate addiction therapy and those are Suboxone and Subutex.
This writeup will outline some of the facts about buprenorphine and its formulations. Buprenorphine also has one formulation approved for moderate to sever pain called buprenex.
1. The formulations.
Suboxone
Suboxone is the most commonly prescribed execute of buprenorphine for opiate/opioid addiction therapy. Its two sizes are 2mg bupe/.05 mg of naloxone and 8mg bupe/2mg naloxone. They are both orange hexagonal pills that are taken sublingually or under the tongue.
“In addition to active ingredients, Suboxone (brand) contains lactose, mannitol, cornstarch, povidone k30, citric acid, sodium citrate, FD&C yellow No. 6 color, magnesium stearate, Acesulfane K sweetener and a lemon/lime flavor”
Subutex
Subutex is less commonly prescribed and comes also in the 2 and 8mg forms, however; subutex DOES NOT occupy naloxone. It also is not orange flavored like suboxone.
Buprenex
Buprenex is an injectable form of buprenorphine indicated for moderate to severe pain. It is .3mgs of bupe per 1 ml. It is used for intramuscular injection meaning it is for injection into the muscle. Buprenex is not indicated for opiate addiction therapy.
Temgesic
Temgesic is also indicated for injure but is not approved in the US. It is usually in .2mg doses and is also used sublingually.
2. The truth about buprenorphine (FAQ)
What is buprenorphine?
Buprenorphine is what is called a Partial Opioid Agonist. This means that it has partial agonist effects at the mu opioid receptor sites which translates to it will stimulate the opioid receptor sites enough to reduce withdrawal or even completely stop them but it does not stimulate the receptors enough to get the user high IF they have been dependant on a Full Opioid/opiate Agonist.
What is a Full opioid/opiate agonist?
A chubby agonist is a opiate or opioid that fully stimulates the MU Opioid receptor sites. This translates basically, it gets you high. Some examples of fleshy agonists are methadone, heroin, oxycodone, hydrocodone, morphine, codeine, hydromorphone, oxymorphone, etc. the mu opioid receptors are responsible for pleasure, euphoria, analgesia.
What is the naloxone for in suboxone?
The naloxone really does not do anything when outmoded with suboxone due to a couple of reasons. One that naloxone has a short 1 hour half life and two buprenorphine has a higher binding affinity to the Mu opioid receptors. This means that bupe will just kick naloxone out of the receptors and take its residence. It is a current misconception that the Naloxone in suboxone is what causes the antagonistic effects of suboxone but this is not the case. The fact of the matter is since bupe is a partial agonist it also has antagonistic effects. It is though that the naloxone was added to suboxone to speed up trials and approval by the FDA. It is basically a scare tactic to dissuade IV users from crushing and injecting he tablets.
What is Binding Affinity?
Binding affinity is how strong of an attraction a substance will bind to the opioid receptor sites. Buprenorphine has a particularly high binding affinity for the mu opioid receptors so it will kick full agonists off the receptors and it will also block them because most full agonists have a lower affinity for the mu opioid receptors.
Can you level-headed get high on full agonists like heroin if you are on suboxone or buprenorphine?
No because it has a intention of blocking full agonists from binding to the opioid receptors, however; on a low dose of buprenorphine 2mg and under you can still feel the effects of full agonists but it will not be 100% of the effects and it will retract more to produce a high. If you are on 8mg and above do not waste your time and money trying to get on bupe because it will not do anything except increase your risk of overdose. Even if you don’t feel it you can still OD.
What does it mean that bupe has antagonistic effects?
The antagonistic effects of bupe basically mean it WILL kick other opiates or chunky agonists out of the receptors impartial like a dose of naloxone (narcon) would. If a full agonist is in the users system and they are dependant on full agonists then they will experience precipitated withdrawal syndrome.
Can you over dose on buprenorphine?
Yes you can but it is very unlikely, however; using buprenorphine and other CNS depressants can be and usually is dangerous and risky. There have been reports of overdose and deaths from the exhaust of benzodiazepines and buprenorphine used in combination.
How is a buprenorphine overdose treated if it does happen?
In a situation that a patient taking buprenorphine has overdosed and is unconscious, the primary management should be the reestablishment of adequate ventilation with mechanical assistance of respiration, if required. Overdose in combination with other CNS depressants should be considered because of increased potential for life threatening respiratory depression. Fresh data suggests that an initial bolus dose of 3mg//70 kg, followed by 4mg/70kg/h over 90 minutes infusion, is needed to have persistent reversal of buprenorphine induced respiratory depression. If an infusion is not possible, repeat the bolus dose as needed.
Why did you say that the naloxone does nothing in suboxone but say that it is also musty to treat a buprenorphine overdose?
Naloxone does not completely reverse a buprenorphine overdose. It only helps keep the patient alive. Due to its short half-life and weaker affinity for the mu receptors and buprenorphines’ remarkable longer half life and stronger affinity the buprenorphine will impartial rebind back to the mu receptors if it is kicked off. This is why they have to keep redosing the naloxone. Also naloxone is not active when you take the medication as directed it is only said to be active when injected.
How long is buprenorphines’ half life?
Buprenorphines’ half life is about 18-73 hours with a mean of 36 hours.
What is the deal with the ceiling dose?
Buprenorphine has what is called a ceiling effect. This means that after a certain point is reached there will be no more added effects. Generally once the ceiling is surpassed the antagonistic effects of bupe will start to become more and more pronounced.
Buprenorphines’ ceiling dose is 24-36mgs
Making the switch to buprenorphine?
Due to buprenorphine being a partial agonist it is HIGHLY important to be in ACTUAL WITHDRAWAL before you ever try making the switch. Why? Because bupe is a partial agonist it also has antagonistic effects, so if the user is dependant on fat agonists and makes the switch to bupe while they have a corpulent agonist in their system they will experience what is called Precipitated Withdrawal syndrome. So you must wait 24-48 hours before making the switch. This number applies to shorter acting opiate/opioid full agonists.
Can you switch from methadone to suboxone or buprenorphine?
Yes you can but first you must taper to under 40mgs of methadone and then detox before you make the switch, you will have to wait at least 72 hours to make the switch from methadone due to its execute of building up in the system and its long half life.
EXTREME CAUTION MUST BE USED WHEN SWITCHING FROM METHADONE TO BUPE.
Does suboxone/subutex/buprenorphine work for everyone?
No, it will not work for every single person. Some have to high of a tolerance to corpulent agonists to even get ANY relief from bupe. If your habit is small enough you will have 0 withdrawal symptoms. Some people still experience some w/d symptoms until thy stabilize on the bupe or their bodies get used to it.
Where can you fetch a doctor?
you can find a doctor on this website: www.naabt.org you unprejudiced register your info and email and a few doctors will contact you within a few days. I had 4 doctors contact me in a matter of a day or so.
Does suboxone/subutex/ buprenorphine have side effects?
Of course: Side effects of buprenorphine are similar to those of other opioids and include nausea, vomiting, and constipation. Buprenorphine and buprenorphine/naloxone can precipitate the opioid withdrawal syndrome. Additionally, the withdrawal syndrome can be precipitated in individuals maintained on buprenorphine. Signs and symptoms of opioid withdrawal include:
-Nausea
-vomiting
-dysphoric mood
-Muscle aches/cramps
-Lacrimation
-Rhinorrhea
-Pupillary dilation
-Sweating
-Piloerection
-Diarrhea
-Yawning
-Mild fever
-Insomnia
-Craving
-Distress/irritability
Prescribing Information:
PI is usually attached to the bottle, ask your obliging local Pharmacist for a copy, or check it out online:
http://www.suboxone.com/patients/pi/
The following is directly quoted, with some sections removed/paraphrased in the interest of brevity.
Buprenorphine hydrochloride:
-weakly acidic
-limited solubility in water (17mg/mL)
-molecular fomula: C29H41NO4HCI
Naloxone hydrochloride:
-soluble in water, dilute acids, and strong alkali
-molecular fomula: C19H21NO4HCI.2H2O
In addition to active ingredients, Suboxone (brand) contains lactose, mannitol, cornstarch, povidone k30, citric acid, sodium citrate, FD&C yellow No. 6 color, magnesium stearate, Acesulfane K sweetener and a lemon/lime flavor
Physiologic and subjective effects following acute sublingual administration of SUBOXONE and SUBUTEX tablets were similar at equivalent dose levels of buprenorphine. Naloxone, in the SUBUTEX formulation, had no clinically significant effect when administered by the sublingual route…SUBOXONE, when administered sublingualy even to an opioid-dependent population, was recognized as an opiod agonist, wheras when administered intra-muscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone.
In methadone, heroin, and morphine dependent subjects, intravenous administration of buprenorphine/naloxone precipitated opioid withdrawal and was …unpleasent.
…the most intense withdrawal effects were produced by 2:1 and 4:1 ratios, less intense by an 8:1 ratio. SUBOXONE tablets bear…at a 4:1 ratio.
*SO remember kids, When taking SUBOXONE, keep in mind the different properties of Buprenorphine and Naloxone….one route of administration might cause exiguous effects interms of opioid antagonist action ect, but OTHERS WILL CAUSE DISCOMFORT, but every individual will be different, some may be thrown into precipitated w/d some may gather they are euphoric. Once again read the product insert for more information.
Before using suboxone or other buprenorphine preparations anyway besides directed please read the above. The injection of suboxone has been shown to cause certain adverse reactions including but not itsy-bitsy to hepatic necrosis. Hepatic necrosis can occur even when taken as directed by certain individuals who are subceptable. Your doctor can accelerate tests to make sure your liver is functioning properly. Accidental injections into a artery have result in severe adverse reactions and amputation may be required.(added by: ilovechronic)
http://en.wikipedia.org/wiki/Intravenous_drug_use_(recreational)#Disadvantages
Buprenorphine undergoes both N-dealkylation to norbuprenorphine and glucoronidation. The N-dealkylation pathway is mediated by cytochrome p-450 3A4 isozyme. Norbuprenorphine, an active metabolite can further undergo glucoronidation.
Naloxone undegoes direct glucoronidation to naloxone 3-glucuronide as well as N-dealkylation, and reduction of the 6-oxo group.
(OF PARTICULAR INTEREST)…
CYP 3A4 INHIBITORS AND INDUCERS….
A pharmacokinetic interaction study of ketoconazole (400MG/A DAY) a potent inhibitor of CYP 3A4, in 12 patients stabilized on SUBOXONE [8mg (n=1) or 12mg (n=5) or 16mg (n=6)] RESULTED IN INCREASES IN BUPRENORPHINE MEAN CMAX VALUES….AND MEAN AUC VALUES..
Again the preceding information was edited for brevity. The full PI sheet should be consulted for further information.
Please use suboxone,buprenorphine, and all other bupe formulations AS DIRECTED. Suboxone and Buprenorphine are valuable tools for maintainance and tapering off of opioids and opiates. The information about injection of subxone is only supplied for harm reduciton and educational purposes, we DO NOT condone the abuse or misuse of buprenorphine and all of its formulations and preparations.
More information can be found here:
Suboxone megathread(includes pics of the pills)
http://www.bluelight.ru/vb/showthread.php? t=395580&highlight=suboxone+megathread
http://www.wikipedia.org/wiki/Buprenorphine
www.drugs.com/pro/buprenorphine-injection.html
VERY USEFUL, THIS IS THE PRODUCT INSERT/INFORMATION FOR PHARMACISTS:
www.fda.gov/Cder/foi/label/2002/20732pharmacist.pdf
Product insert:
http://www.suboxone.com/patients/pi/
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