Posts Tagged ‘buprenorphine’

Teva to release generic formulation of Subutex

Friday, May 21st, 2010

Teva Pharmaceuticals will produce a new generic formulation of the popular ORT drug, Subutex®.  In October 2009, the first generic formulation of Subutex® was released by Roxane Laboratories.  The full drug application can be viewed at DailyMed, a government site.

http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=18031

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Added generic Subutex

Wednesday, February 24th, 2010

On October 8th, 2009, Roxane Laboratories announced the approval of an AB-rated generic medication for the popular opioid replacement therapy drug, Subutex®. The active ingredient in Subutex® is buprenorphine HCl. The more popular Suboxone, a similar medication by Reckitt Benckiser Pharmaceuticals, still has no generic equivalent.

2 mg Buprenorphine HCl
8 mg Buprenorphine HCl

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Suboxone FAQ / Subutex FAQ

Monday, December 21st, 2009
DISCLAIMER: The information detailed in this article is not medical advice, nor written by medical professionals. Before making any medical decisions, it is imperative to confer with a licensed medical professional. If you have comments, suggestions, or find an error, please feel free to leave feedback using the comments section at the bottom of this page.

TABLE OF CONTENTS

  1. What is Suboxone/Subutex?
  2. How long do I have to wait before taking Suboxone or Subutex?
  3. How is Suboxone taken?
  4. What are some possible side effects of Suboxone and Subutex?
  5. What is precipitated withdrawal?
  6. What are the different stages of Suboxone treatment?
  7. Which is a better treatment for opioid addiction, Suboxone or methadone?
  8. Can a patient on methadone safely switch to Suboxone?
  9. How do I find a doctor that can prescribe Suboxone?
  10. What is the maximum number of patients a doctor may have at any one time?
  11. Is Suboxone addictive?
  12. How long after stopping Suboxone does one have to wait before narcotic painkillers become effective?
  13. Sources
  14. Comments

Terms to Know

  • affinity — the strength with which a drug binds to its receptor
  • intrinsic activity — the degree to which a drug activates its receptors
  • rate of dissociation — measure of disengagement or uncoupling of the drug from the receptor

What is Suboxone/Subutex?

Suboxone®, manufactured by Reckitt Benckiser, is the first opioid substitution treatment available without the hassle involved with going to a methadone clinic everyday or even weekly. The two active ingredients in Suboxone® are buprenorphine hydrochloride, and naloxone hydrochloride dihydrate. Subutex® has only buprenorphine as an active ingredient. Suboxone® and Subutex® are available in the following formulations:

BUPRENORPHINE
NALOXONE
IMPRINT
COLOR / SHAPE
PICTURE
Suboxone®
2 mg
0.5 mg
N2
Orange / Hexagonal
8 mg
2 mg
N8
Orange / Hexagonal
Subutex®
2 mg
B2
White / Oval
8 mg
B8
White / Oval

In a study involving 220 patients, 16-32 mg of Suboxone proved to be just as effective as high-dose methadone, and more effective than low dose methadone as treatment for opioid dependency. Typical starting dosages range from 8 mg to 32 mg per day; however, some patients believe that it is better to start as low as 2 mg. Buprenorphine is only a partial agonist at the opioid receptors, thereby lowering abuse potential. While a small amount of euphoria may be experienced in some patients, buprenorphine will never provide the same degree of intensity as a full opioid agonist (e.g. heroin, oxycodone, morphine). Because buprenorphine possess the quality of being a partial agonist, it shows a ceiling effect. This means there is a point at which buprenorphine will not increase in effectiveness, despite taking more.

How long do I have to wait before taking Suboxone or Subutex?

If Suboxone is procured legally through a doctor, the prescribing physician will almost always ask that the patient be in mild-to-moderate withdrawal during induction. For short-acting opioids, like heroin and oxycodone, withdrawal takes anywhere from 24-36 hours to kick in. When switching from a longer-acting opioid like methadone, the situation becomes a bit more complicated. The typical scenario goes something like this: (1) taper down to 30 mg methadone per day, (2) wait three days before being inducted. Transferring from methadone to Suboxone is something that has to be discussed with a doctor because it is very easy to precipiate withdrawal if the transfer is not done correctly.

“Why does the patient have to be in withdrawal when he/she comes in?”

If there are high levels of another opioid in the body, Suboxone will, in a sense, compete with the other opioid molecules, and knock them off the receptors. This occurs because buprenorphine has an extremely high binding affinity for the opioid receptors. If this happens, the patient will be thrown into precipitated withdrawal, which is extremely unpleasant, and can last a significant period of time.

“Wait, the opioid molecules that are being replaced are being replaced with another opioid, buprenorphine, so shouldn’t that still quell withdrawal symptoms?”

Buprenorphine is only a partial opioid agonist, therefore, it has less opioid effects than those of a full agonist (e.g. morphine, heroin, oxycodone). If the patient is already in withdrawal when the first dose is taken, he/she will feel better not worse.

How is Suboxone taken?

Sublingual tablets are absorbed through veins under the tongue. Before taking Suboxone, it is a good idea to drink a little water to moisten the mouth, which helps the tablets dissolve easier, and faster. If the doctor prescribes two tablets, put one on the left side under the tongue, and put the other on the right side under the tongue. If more than two are prescribed, Reckitt Benckiser, the makers of Suboxone, recommends waiting until after the first two dissolve to take the rest. It generally takes about 10 minutes for a tablet to dissolve, though it can range anywhere from 5-20 minutes. Some patients have reported holding the “juices” in their mouth for as long as 45 minutes can increase effectiveness. Try not to talk while taking Suboxone, as this can interfere with how well it is absorbed. It is important that Suboxone be taken correctly for it to work, and if a patient does not follow directions he/she may end up feeling sick. The following is a list of ways NOT to take Suboxone:

  • Never swallow the tablet — the reason Suboxone is prescribed as a sublingual tablet is because barely any buprenorphine is absorbed orally. Swallowing the tablet will render Suboxone ineffective.
  • Never suck on the tablet — for the same reason a patient does not swallow the tablet, the patient does not suck on the tablet.
  • Never snort a tablet — although intranasal buprenorphine may work, this method does not work as well as taking the tablet sublingually. Snorting anything is counter-productive to recovery, and only reinforces bad habits. Also, snorting any pill can cause severe damage to the lungs, which most people forget about.
  • Never shoot a tablet — in opioid-dependent individuals, shooting a tablet can cause precipitated withdrawal. Most doctors do not like prescribing Subutex because of the fear that people will try to inject them. The naloxone is present in Suboxone as a deterrent. Shooting any pharmaceutical not specifically prepared for injection can cause serious complications, including death. Don’t do it.

What are some possible side effects of Suboxone and Subutex?

The most common reported side effects of Subutex and Suboxone are:[2]

  • cold or flu-like symptoms
  • headaches
  • sweating
  • sleeping difficulties
  • nausea
  • mood swings

Those side effects do not sound too inviting, do they? I think these are primarily experienced during the induction period, as the body becomes accustomed to buprenorphine, rather than a full agonist. From what I have seen, most people who have become stabilized on Suboxone report very little to no side effects, and those that do report adverse reactions usually only experience trouble sleeping, sweating, and headaches. Other side effects include respiratory depression (as with all opioids), constipation, anxiety, depression, pain, and dizziness. For a full list of side effects, please refer to the prescribing information [PDF] or package insert.

What is precipitated withdrawal?

Precipitated withdrawal can occur when a person who is physically dependent on opioids is administered an opioid antagonist or a partial agonist. In those not physically dependent on opioids, an antagonist typically produces no effects, while a partial agonist would. Depending on the half-life of the antagonist or partial agonist used, the qualitative effects of precipitated withdrawal, when compared with the experience of a typical withdrawal syndrome, are often shorter lived but with a faster onset. It is quite easy to imagine why an antagonist would cause precipitated withdrawal. The antagonist has a very high binding affinity for the opioid receptors, so it displaces any full agonist opioids already present and blocks any molecules from binding for a given period of time (depending on the half-life of the antagonist). Because antagonists block the effects of opioid receptors instead of activating them, there is a drastic reduction in the previous agonist effect, resulting in agonizing withdrawal.

Partial agonists can cause precipitated withdrawal, but the concept is a little more complicated than that of an antagonist causing precipitated withdrawal. If an individual who is physically dependent upon opioids receives a dose of a partial agonist too soon after his or her last dose of a full opioid agonist, precipiated withdrawal occurs. Buprenorphine has a high binding affinity for the mu-opioid receptor, but because of its partial agonist properties, it has low intrinsic activity at that receptor (less opioid-like effects and ceiling effect). If there are full opioid agonist molecules still attached to the opioid receptors at the time of administration, the buprenorphine will displace the full agonist. Though partial agonists do activate opioid receptors, the overall effect is much less than that of a full agonist. This decrease in agonist effect can cause precipitated withdrawal. For this reason, buprenorphine is typically only given when the person physically dependent on opioids is in full-fledged withdrawal.

What are the different stages of Suboxone treatment?

Suboxone treatment should never be used by itself. It is not a cure, but rather a treatment. When used concurrently with some sort of therapy, the success rate is much higher. Suboxone treatment really beings with a phone call called the pretreatment screening; this consists of a brief interview to qualify the person, and a date may be set for intake and induction. Intake is the gathering of medical records to measure suitability for office-based treatment. If the physician feels it is necessary, he or she may perform a physical exam. At this point, the advantages and disadvantages of treatment are discussed, and any questions the patient has are answered. The next step after intake is induction. The goal of induction is to find a dose of Suboxone at which the patient feels comfortable, and withdrawal is suppressed.[3]

Once the patient becomes accustomed to their daily dose of Suboxone, he/she enters the stage of stabilization. At this point, the patient is not feeling any withdrawal symptoms or side effects, has no uncontrollable cravings for opioids, and is not using any additional opioids. During the maintenance phase, which can last anywhere from a few weeks to a few years, the patient is monitored less often, withdrawal symptoms are prevented, cravings are still suppressed, and the need to self-administer opioids is lowered greatly. The next stage is a medically-supervised withdrawal where the patient is slowly tapered off of Suboxone. Only mild withdrawal is felt if the drug is tapered correctly. Either way, the patient should be prepared to have some symptoms of withdrawal, which may include fatigue, reduced appetite, insomnia, and irritability.[3]

Which is a better treatment for opioid addiction, Suboxone or methadone?

Each person differs in what he/she requires as far as treatment in concerned because varying factors such as body chemistry, size of habit, duration of addiction, finances, etc. To help addicts find the right treatment plan, TPC! has put together a side-by-side comparison of Suboxone and methadone. Remember, Suboxone or methadone by themselves should not be considered complete treatment plans, but instead part of a comprehensive plan which leaves no aspect of opioid addiction untended. A link is provided below:

Suboxone vs. Methadone

Can a patient on methadone safely switch to Suboxone?

It is possible for a patient on methadone to switch to Suboxone; however, the difference between the two drugs may cause the former methadone-treated patient to feel unsatisfied, though there have been many successful cases noted. Methadone, being a full-opioid agonist, is more similar to heroin and oxycodone than buprenorphine. Buprenorphine is a partial-opioid agonist, which means it does not provide the same intense release of painkilling chemicals that full agonists provide. As a full agonist, methadone is also more likely to give a patient euphoria.

Because of methadone’s long half-life, it is required that the patient being inducted into Suboxone treatment be at least 72 hours without methadone. If Suboxone is taken prematurely it could cause precipitated withdrawal, a very unpleasant experience. It is important that the patient also be down to 20-30 mg of methadone before making the switch to buprenorphine. A switch should not be attempted with anyone taking over 30 mg of methadone. It is probable that the patient will experience discomfort during the first 3-5 days while his or her body becomes accustomed to buprenorphine, though it is typically fairly mild.

How do I find a doctor that can prescribe Suboxone?

Not all doctors can prescribe Suboxone because it requires special certification. If a doctor wants to be able to prescribe Suboxone, he/she must (1) send a letter of intent to the Substance Abuse and Mental Health Administration, (2) be qualified, and (3) take a special course to learn about Suboxone. Many patients believe their doctors are largely uneducated on the subject. Although every doctor must meet certain criteria, many doctors do not seem to understand addiction or how Suboxone can be used effectively. The qualifications, as taken from SUBOXONE.COM, are listed below:

According to DATA 2000, licensed physicians (MDs or DOs) are considered qualified to prescribe SUBOXONE, if at least 1 of the following criteria has been met:

  • Holds an addiction psychiatry subspecialty board certification from the American Board of Medical Specialties
  • Holds an addiction medicine certification from the American Society of Addiction Medicine (ASAM)
  • Holds an addiction medicine subspecialty board certification from the American Osteopathic Association (AOA)
  • Completion of not less than 8 hours of authorized training on the treatment or management of opioid-dependent patients
  • Organizations currently authorized to provide training: American Academy of Addiction Psychiatry, American Medical Association, AOA (through the American Osteopathic Academy of Addiction Medicine), American Psychiatric Association, and ASAM
  • Participation as an investigator in 1 or more clinical trials leading to the approval of SUBOXONE
  • Training or other such experience as determined by the physician’s state medical licensing board
  • Training or other such experience as determined by the United States Secretary of Health and Human Services

In addition, physicians must satisfy BOTH of the following criteria:

  • Have the capacity to provide or to refer patients for necessary ancillary services, such as psychosocial therapy
  • Agree to treat no more than 30 patients at any one time in an individual or group practice

Finding the right doctor can be a bit hard sometimes. It is very important that the patient be comfortable, and compatible with the doctor. Some of the doctors listed at the site below will not prescribe Suboxone to anyone, or are part of pain management or a clinic, so it may take some looking before the right one is found. The Buprenorphine Physician and Treatment Program Locator is very easy to use, and has an interactive map of the United States to help anyone looking find a doctor. Also, anyone can put their name on a waiting list if a doctor is at full capacity, so that when a spot frees up, he/she gets an e-mail; however, this is largely unnecessary because the patient limit was recently increased from 30 to 100. It should be fairly easy to find a doctor. Below is a link:

The Buprenorphine Physician and Treatment Program Locator

What is the maximum number of patients a doctor may have at any one time?

In December 2006, DATA 2000 was amended, giving Suboxone-certified doctors the ability to treat up to 100 patients; however, for the first year a doctor can only treat 30 patients at any one time. One year after the original letter of intention to treat patients using buprenorphine was submitted, the physician may submit a second notification of the need and intent to treat up to 100 patients.[4]

Is Suboxone addictive?

Yes. The active ingredient in Suboxone that keeps withdrawal at bay is buprenorphine, a partial opioid agonist. Buprenorphine has an extremely high binding affinity to opioid receptors in the brain, but because it is only a partial agonist, full effects, as produced by full agonists (e.g. oxycodone, heroin), are not present. Many people are grossly misinformed about the addictive nature of buprenorphine, and claim that there is no withdrawal syndrome, which is incorrect; however, because of its long half-life and partial agonist properties, the withdrawal is longer, but milder than that of full agonists. Some people have horror stories of their attempts to get off of Suboxone, but most of them come from people who did not taper properly. The bottom line is Suboxone is addictive, and eventually some withdrawal has to be dealt with. Suboxone will soften the fall, and withdrawal from it is certainly not as bad as withdrawal from oxycodone or heroin.

How long after stopping Suboxone does one have to wait before narcotic painkillers become effective?

Suboxone can block opioids for three days, and for individuals on high doses (>16 mg) it may be longer. An individual taking 24 mg for a few days indicated it took 5-6 days before he felt the full effects of the full agonist, oxycodone. It takes 37 hours for half of the buprenorphine in the body to be eliminated. Because of the long half-life of buprenorphine, the drug builds up in the body each day, which is part of the reason it could take a bit more than a day or two for other opioid anagesics to be effective. In summary, the factors that determine the effectiveness of opioids are dosage, frequency of use, length of time using, and individual body chemistry and metabolism.

After doing a bit of research and talking to drug users who have been in this situation, 72 hours seems to be the general consensus. Some people indicated feeling the effects after just 24-36 hours, and others said they felt a fraction of the full effects. Please understand, after taking Suboxone for a given period of time, tolerance may be significantly lower, so do not overdo it. Also, it is important to remember that even though the effects not be felt after 24 hours, it is very possible to overdose. It is impossible to monitor how the body is handling the mixture of buprenorphine and another opioid when it can barely be felt. Always consult a doctor before switching medications.

Sources

[1] Johnson, R.E., et al. A comparison of levomethadyl acetate, buprenorphine, and methadone for opioid dependence. New England Journal of Medicine 343(18):1290-1297, 2000. [Abstract]

[2] Subutex and Suboxone: Questions and Answers. FDA/Center for Drug Evaluation and Research. October 8, 2002. [link]

[3] SUBOXONE Treatment Walk-through. Subxone.com. Reckitt Benckiser. 2007. Accessed: April 23, 2007 [link]

[4] Buprenorphine-Frequently Asked Questions. Substance Abuse & Mental Health Services Administration. US Dept. of Health and Human Services. 2007. Accessed: April 25, 2007 [link]

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