Buprenorphine

Although it has pain-reducing properties, buprenorphine is more commonly prescribed to help people free themselves from addiction to narcotics.

Overview

When it is used as prescribed and intended, buprenorphine can be very helpful as a tool in medication-assisted treatment (MAT). It is safe and effective under those circumstances, and is always used as part of an overall program of treatment which includes counseling and behavioral therapy, to reduce or help a patient quit an addiction completely.

Unlike some other treatments for addiction which require a very formalized and structured clinical setting, buprenorphine is a medication which can treat dependency on narcotics in the relaxed environment of a physician's office. The advantage of this is that it greatly increases access to the drug itself, and it makes administration to patients much easier.

As detailed in the Drug Addiction Treatment Act of 2000, US doctors who are qualified can now legally provide buprenorphine in a variety of settings to patients, such as a correctional facility, a community hospital, a health department, and even an office environment. Having this kind of availability and accessibility makes it far easier to treat a greater number of patients who are in serious need of treatment for their opioid dependency.

Buprenorphine has some extremely useful properties which make it uniquely effective in the treatment of opioid addiction, starting with the fact that it reduces the symptoms normally present in a person who is physically dependent on opioids, for example going through withdrawal, and experiencing powerful cravings. Although it is itself a narcotic, it is much weaker than the really powerful narcotics, and that makes it much safer to use in an MAT program, with much less danger of overdose or misuse.

Another very useful property of buprenorphine is that when used by a patient, its euphoric effects increase up to a certain point, and when that threshold is reached, there is no further escalation of euphoric experience. Because it has this built-in ceiling, the dangers of abuse are far less, and actually make it ideal for use in treating addiction to methadone, heroin, or other powerfully addictive drugs. Since it has relatively long-lasting effects, patients can often skip a day or two when being treated with buprenorphine, since for some, the positive effects last that long.

Buprenorphine is sometimes used in tandem with naloxone, to lower the potential for misuse of the drug even further. When these two drugs are ingested as tablets, naloxone blocks the effects of opioid withdrawal, and buprenorphine’s euphoric effects dominate; however when the tablets are crushed and injected, naloxone dominates and opioid withdrawal symptoms become more prevalent and more severe.

Condition Treated

  • Withdrawal from narcotics (such as heroin)

Type of Medicine

  • Opioid (narcotic) medication

Side Effects

Like virtually all drugs, in addition to the benefits it provides, buprenorphine may also cause some side effects to be manifested in patients, and some of these can be extremely dangerous if not treated immediately. Because buprenorphine is a narcotic itself, albeit a much weaker one than heroin, for example, it can still be abused and misused, and that means all the same potential for drug abuse exists with buprenorphine usage.

For that reason, any side effects which are observed in persons under a program of treatment with buprenorphine should be discussed immediately with a doctor, and for some side effects, immediate medical attention is required. As an example, any patient exhibiting signs of an allergic reaction such as swelling of the lips, tongue, throat, or face, pronounced difficulty breathing, or rashes and hives, should seek emergency medical assistance at the earliest possible opportunity.

Because it is a narcotic medication, buprenorphine has the potential to seriously depress your respiratory system and cause dangerously slow breathing. At its most extreme, this can cause death, because insufficient oxygen is distributed throughout the body by the inhibited respiratory system.

The following class of side effects, while not considered life-threatening, are serious nonetheless and should be reported immediately to your doctor so that you can follow recovery instructions:

  • unusual confusion or disorientation, sometimes accompanied by erratic behavior
  • a feeling of faintness, as though you are about to lose consciousness
  • shallowness of breathing
  • nausea or stomach pain
  • loss of appetite
  • dark-colored urine
  • dark-colored stools
  • a yellowish tinge around the eyes or on the skin.
  • Persistent cravings
  • Muscle cramps or pains
  • Unusual irritability in someone who is not normally irritable

There are another group of side effects which may appear in some patients which are less serious in nature, but which should still be discussed with your doctor at the next scheduled visit. These include the following:

  • Headaches
  • unusual sweating
  • problems with sleeping
  • unexplained pains throughout the body
  • persistent nausea or vomiting
  • constipation which is not normal for the patient

Dosage

The normal induction dosage for an adult who has an opiate dependence would be 8 mg taken sublingually on the first day, followed by a dosage of 16 mg taken sublingually on day two. Thereafter, a maintenance dosage can be established from between 4 and 24 mg per day, with increments upward or downward between 2 and 4 mg as needed to suppress all symptoms of opioid withdrawal.

In cases of opioid dependence, ingestion should be by induction only, and should be accompanied by both counseling and behavioral therapy which includes support from social networks. After induction, a combination of naloxone and buprenorphine is generally used, and the only cases where buprenorphine would be used in standalone mode would be for patients who have a very low tolerance for naloxone. To avoid triggering the onset of withdrawal symptoms during induction, program initiation should only be commenced when clear signs of withdrawal are observed in a patient.

When used as a treatment for chronic pain in adults, an initial dosage of .3 mg administered in a slow intravenous drip is indicated, and this initial dosage may be followed up within an hour if circumstances are deemed to warrant it in the opinion of a medical expert. A maintenance dosage for pain would include a .3 mg intravenous delivery, spaced apart at six-hour intervals as needed by the patient. When buprenorphine is administered in this manner as a treatment for chronic pain, great care should be taken during the intravenous delivery, and the patient should be monitored for signs of a reaction.

If buprenorphine is used as a treatment in the conversion from other types of opioids, all other opioids should be immediately discontinued before embarking on a program of treatment with buprenorphine. In cases where patients are converting from a total opioid dosage which did not exceed 30 mg per day of morphine-equivalent medication administered orally, an initial treatment with a 5 µg per-hour patch should be started.

In cases where patients whose total opioid dosage was somewhere between 30 and 80 mg per day, a patch delivering 10 µg per hour is indicated, and in all cases, short-acting analgesics may be used if necessary, until analgesic efficacy has been achieved. For those patients who are converting from a program of more than 80 mg per day of morphine equivalents, there are two approaches: the first involves using a patch which delivers 20 µg per hour, and if this provides inadequate analgesia, a secondary approach using an alternative analgesic should be considered.

Any patients converting from methadone must be closely monitored, because methadone has a very long half-life, and tends to accumulate in plasma. For such patients, titration should be at a dosage that provides sufficient analgesia while also minimizing any adverse reactions, with the minimum titration interval being at least 72 hours.

In all conversion situations, patients should be closely monitored for any kind of respiratory depression, especially within the first three days of treatment. Whenever a patient being treated reports an increase in the level of pain, the source of that pain should be investigated thoroughly before arbitrarily increasing the buprenorphine dosage level.

All patients converted from other opioids should remain on a program of treatment with buprenorphine per doctor's instructions, with no abrupt discontinuance. A gradual downward titration should be the most effective approach in such cases, while the option may be considered for introduction of an opioid with immediate release capability.

Generally speaking, this kind of a treatment program should only be used for patients whose pain is considered severe enough to warrant treatment daily, around-the-clock, and of a long-term nature. This kind of approach is generally only considered where alternative treatments have already been used and found to be an adequate in dealing with a given patient's symptoms.

When used for the treatment of pain in pediatric patients aged 13 or older, the same kind of intravenous delivery approach can be used, with the precise dosage leveled off at whatever is necessary to control the pain being experienced by the patient. The same is true for patients who are 16 years of age and older, as a standard dosage is difficult to predict because pain levels are so different between individuals.

For patients who are 16 years of age and older, and who are being treated for opiate dependence, the intravenous method is not used, and instead, sublingual delivery of the medication is indicated. In general, dosages will need to be customized to the individual as needed to control symptoms of withdrawal, although initial dosages should be less than what is recommended for an adult patient.

Interactions

There are some precautions which should be observed when using buprenorphine with other medications, especially those types of drugs which induce sleepiness, or can cause your respiratory system to slow down. Because buprenorphine itself has some of these same properties, the double effect resulting from combination with drugs having similar properties can be very dangerous for an individual, and potentially life-threatening.

This means that you should discuss it thoroughly with your doctor before taking any kinds of drugs such as sleeping pills, any other narcotic pain medication, muscle relaxers, sedatives or tranquilizers, and any kinds of medications which act to relieve depression, anxiety or seizures.

There are also some over-the-counter medications, vitamins, and even some herbal products which interact with buprenorphine. For this reason, you should make a complete list of all the other medications you are taking, as well as dietary supplements and herbal products, and the dosages which you are taking for each one.

This information will also come in very handy if you ever have to make an unplanned trip to an emergency room, or to some healthcare clinic or facility for treatment. Unless your primary care doctor is in attendance, a physician at one of these facilities cannot safely prescribe a program of treatment for you, whatever your condition may be at the time, without knowing all the medications you are currently taking, and whether any prescribed medications might interact with them.

Warnings

There are several warnings and precautions which should be observed by patients who are being treated in a program which includes buprenorphine. General warnings include discussing with your doctor any history of low blood pressure you may have, as well as liver disease, problems with your gallbladder, or kidney disease. You should also avoid being exposed to high temperatures or heat conditions when you are using buprenorphine patches.

If you're allergic to buprenorphine or any of the ingredients used to manufacture it, the drug should not be used for treatment. Similarly, if any of the symptoms of an allergic reaction should develop during usage, you should immediately report this to your doctor and should discontinue further usage until otherwise directed.

It is also worth keeping in mind that buprenorphine is itself a narcotic, and therefore subject to all the same potential for abuse and misuse as addictive drugs. While its effects are not considered to be anywhere near as potent as the most powerfully addictive drugs like morphine, heroin, or methadone, buprenorphine still produces a euphoric effect in the user, which makes it potentially appealing as a recreational drug.

In addition to these general warnings, some other specific medical conditions in your past or present medical profile could make it dangerous for you to use buprenorphine. Some of these warnings are as follows:

  • allergic reactions to foods, preservatives, or certain dyes
  • liver disease, liver failure, or hepatitis
  • any history of stroke or seizures
  • problems with urination
  • pancreatic disease or gallbladder disease
  • persistent low blood pressure
  • a history of drug or alcohol dependence
  • a history of respiratory issues such as chronic obstructive pulmonary disease, asthma, or any other lung disease
  • any type of heart disease, irregular heartbeat or a very slow heartbeat
  • head injuries, brain tumors, or any undue pressure on the brain itself
  • kidney disease.

There are some very important warnings which should be observed by women who are pregnant or plan to become pregnant, and may be considering treatment with buprenorphine. It's important to note that any untreated opioid addiction has the potential to cause serious implications with an unborn infant, for instance abnormal birth weight, premature birth, and even death of the fetus.

However, treating an opioid addiction with another opioid-like buprenorphine also carries a certain amount of risk, because the opioids will cross the placenta into the fetus and can produce respiratory depression. For this reason, patients on a program of treatment with buprenorphine are generally advised to discontinue use of the drug prior to labor, and to instead substitute a fast-acting analgesic for the short term.

Along these same lines, there are some warnings which should be noted for women who are breastfeeding or plan to breastfeed after pregnancy. Buprenorphine has the potential to decrease milk production and inhibit lactation, and for these reasons, most physicians will counsel against breastfeeding when buprenorphine has been used as a treatment prior to pregnancy or during pregnancy. If a mother chooses to breastfeed even after having used buprenorphine during pregnancy, the fetus should be closely monitored for an extended period of time, so as to detect any potential negative impacts.

Storage

Patients using buprenorphine should keep it in a location which is cool, dry, and away from any direct light sources. It should not be frozen, because it is not known what impact this may have on the drug, and because during thawing, condensation will form on the tablets and make them crumbly, and more difficult to swallow. For the same reason, buprenorphine should be kept away from humidity, to lessen the likelihood of harmful condensation.

This drug is still effective long beyond any expiration date printed on the label, but if your supply extends well past the expiration date, that probably means you’ve been missing dosages along the way, and should consult your doctor about how to proceed.

Buprenorphine should be kept well out of the reach of pets and children, in a tightly sealed or locked container. An overdose of this drug can be fatal to anyone, especially children whose tolerance will be generally much lower, and will make them more vulnerable to negative impacts.

Summary

Buprenorphine is a narcotic analgesic, used to help patients manage symptoms of withdrawal from a more potent narcotic such as methadone or heroin. Because it is itself a narcotic, great care must be taken in using this drug, and any side effects encountered during use should be immediately discussed with a doctor.

It can be a very effective agent for use in helping addicts recover, especially when used as part of a holistic program that includes regular counseling and psychosocial support. Since its euphoric effects are considered to be much milder than the more potent narcotics, buprenorphine does not have the same status as those other drugs, and its ‘ceiling effect’, i.e. euphoric threshold, makes it ideal for use in treating drug addiction.

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Last Reviewed:
December 25, 2017
Last Updated:
December 22, 2017