buprenorphine

Pharmacologic class

semisynthetic opioid, narcotic analgesic

Buprenex (low-dose injectable solution, 0.3 mg/ml)
Subutex, Subozone (sublingual tablets, 0.4, 2 and 8 mg)
Temgesic (sublingual tablets, 0.2 and 0.4 mg, low-dose injectable solution, 0.3 mg/ml)

opiate addiction with severe withdrawal symptoms
moderate to severe pain

mu opioid partial agonist
kappa opioid antagonist
delta opioid agonist

use of benzodiazepines (possible interactions include breathing difficulties, coma and death)

recommended not to be used with MAO inhibitors
use with caution in respiratory compromise, and impaired liver or renal function

Used with other central nervous system depressants such as anesthetic agents, antihistamines, phenothiazines, barbiturates and tranquilizers, may increase CNS and respiratory depression

CNS: sedation, confusion, lethargy, agitation
CV: bradycardia
respiratory: decreased respiration rate
GI: constipation
GU: urinary retention
skin: itching

Buprenorphine is derived from the morphine alkaloid thebaine. It is most commonly used in the treatment of opiate addiction.
Buprenorphine has a rather significant abuse potential, although it causes significantly less euphoria than heroin or methadone. However, in a recent study it was found that using a combination naloxone-buprenorphine pill significantly reduces the abuse potential, as naloxone prevents euphoria by blocking the opioid receptor sites.
Buprenorphine is currently not approved and consequently not legally available in the US for the treatment of opiate addiction, except when used as an investigational new drug.
Several NIDA-funded studies have found that buprenorphine is a safe and effective treatment for opiate addiction. Particularly, it was found that buprenorphine is more effective than the current standard opiate substitution drug, methadone.
Buprenorphine is currently in schedule V in the US, but DEA is proposing a rescheduling to schedule III.
In Finland, Pentti Karvonen, a doctor who imported Subutex and Temgesic tablets from France and prescribed them to addicts as part of a substitution treatment program was sentenced to jail for five years. During the trial, the leader of the Finnish National Public Health Institute's drug laboratory testified that buprenorphine has an abuse potential comparable to that of heroin. (Note that heroin is Schedule I.)
Methadone treatment is problematic, since methadone is addictive. Buprenorphine, while effectively helping alleviate withdrawal symptoms, has a much lower addiction potential and is therefore much better in treatment that aims to end a person's opiate addiction once and for all.
From 1994 to 1998 in France, buprenorphine was implicated in 1.4 times more deaths than methadone. However, since the number of buprenorphine users was 14 times greater, it was found that buprenorphine is a much safer drug.
Buprenorphine tablets are to be placed under the tongue and allowed to dissolve. Chewing or swallowing them will make them ineffective. Buprenorphine is sometimes injected, particularly when used as a substitute for street heroin. Reports state that some addicts prefer injected buprenorphine to low-quality street heroin. Dosages range from 4 to 32 milligrams per day for heroin dependence.

August 8th, 2002

I accidentally came across some Buprenorphine(Temgesic) advertised as an anti-depressant. I noticed that it took very little to be effective, about .02mg. I also noticed that I also stopped having a craving for alcohol or pot. I now know that Buprenorphine is an opiate, but its main effect seems to be as an anti-depressant.

It is rarely prescribed for this purpose, but studies have been done showing the efficacy of this use. In over a year I have not had to increase the dosage of .02-.04 mg, but it is very habit forming if not addictive. My problem is that I have to get it online from India or Pakistan or the Philippines. The order has always come, but I wonder about the time when I will not be able to obtain it. To me this is a wonder drug as it makes you feel very normal and gives you energy and incentive along with stopping other cravings. Insufflation is the best way to take this as the dosage is so small and is cut with saccharin, so that there is no pain or damage to the nasal cavity. Opiate addicts can ween themselves by taking this drug and it is very effective, but the average addict must take between 2-32mg to be effective. Maybe someday they will see that this drug can be used in place of many dugs that are much more damaging.

Information regarding buprenorphine (suboxone, subutex) for narcotic dependence

Buprenorphine (suboxone) is FDA approved in the US only for narcotic dependent patients and requires special training and a second DEA number to prescribe. In Europe it is also used for chronic pain and is a moderate pain medicine with partial agonist action at the narcotic receptors.

Narcotic dependence can include patients who are using heroin, using prescription medicines illegally or obtaining them through lying, or patients with chronic pain, present or resolving, who have also gotten hooked on narcotics and are overusing or abusing them.

Buprenorphine is tricky to START patients on because it is a partial agonist but sticks to the receptor like glue. So it can kick out any other narcotic including methadone, heroin, oxycontin, all of them out of the receptor. So to START it, the person has to be in withdrawal and that is called an induction. This is why it requires the special training and DEA number. If a patient is not in withdrawal, and is taking a much higher dose of heroin, oxycontin, methadone or other narcotics, they can get immediately massively sick.

Once a patient is on the buprenorphine, it works well for addiction. If they are on the combined buprenorphine/nalaxone, they can't abuse it because the nalaxone stops them from injecting it iv. It doesn't work swallowed. It has to be absorbed slowly under the tongue. It is a partial agonist so it gives moderate pain relief, but it blocks all of the other narcotics, so it is great for addiction and has a very long half life. Some people can take it only three times a week. It doesn't make people somnolent, and the chance of overdose and death are very small. The chance is much higher if you add in benzodiazepines or alcohol.

The DEA said that to use it for addiction I have to prescribe with my second DEA number, which starts with an X. To use it for chronic pain, that is off label and not FDA approved in the US, though it is used for both chronic pain and addiction in Europe. It is much safer than methadone. To use it for chronic pain, the DEA said use the regular DEA number and put "chronic pain" on the script and chart why it's being used. The DEA said that providers can use it off label as long as they use the DEA numbers correctly. Ethically, I think that it is way safer to keep a chronic pain patient that is doing well on suboxone/nalaxone on that than to switch them to long or short acting other narcotics. For the first year after training, a provider can have a maximum of thirty patients maintained on suboxone.

The suboxone/nalaxone used to be much more expensive than the suboxone alone. Suboxone alone can be abused by using it injected. A cheaper suboxone/naltraxone film, rather than tablet, just came out and the pharmacies have it.

I am working with the UW Pain Clinic through the Roam-Echo program, which means that we have an on-line conference every two weeks, with a team including an addiction specialist, chronic pain specialist and psychiatry. The UW Pain Clinic will not accept patients on benzodiazepines in the suboxone program; they must wean first. That and alcohol are causes for consideration of removal from the program because of the risk of overdose and death. Other suboxone provider clinics may have different rules, much as the methadone clinics have different boundaries about alcohol and drugs than the chronic pain clinics.

There is more information at the Substance Abuse and Mental Health Services Administration (SAMSHA) and buprenorphine prescribers can be found on a voluntary list on the SAMHSA site. There are also listings of inpatient treatment centers that can continue buprenorphine and sites for dual diagnosis patients, meaning those with mental health and drug addiction problems.