Buprenorphine is a type of drug called an opioid and works by activating opioid receptors in your body to provide an analgesic effect. It is usually used to relieve pain, but it can also sometimes be used to help people who are dependent on opioids such as heroin.
Brand Names and Doses
Buprenorphine is the generic name, which is the name of the actual drug component inside your medication.
Brand names of buprenorphine used for pain relief include Temgesic and Norspan. Temgisic is available as a sublingual tablet to place under your tongue and as an injection and is best for acute pain. Norspan is available as a patch to put on your body, which takes longer to work but is able to provide ongoing and continuous pain relief so it is better for chronic pain relief.
There are several different doses of the Norpan patch. For most people, it is best to begin with the lowest dose (releases 5mcg per hour) and gradually increase the dose until the pain is relieved. It's best to wait for 3 days before increasing the dose to allow the body time to notice the effect of the dose change.
Brand names of buprenorphine used for opioid dependence are subutex and suboxone. Both are available as a subligual tablet and suboxone is also available as a sublingual film. Both of these medications are taken but putting the tablet or film under the tongue so that it can be absorbed into the blood stream.
What type of drug is it?
Buprenorphine is a type of drug called an opioid. This is a drug class that helps us to group drugs that work in a similar way together. Other opioid medications include:
- Dextropropoxyphene (Propoxyphene)
Unlike other types of opioids, buprenorphine it is a partial agonist of the opioid receptors. This means that it attaches to the opioid receptors in the same way as other opioids, but it may be less effective. As a result, it is used less often for relieving pain. However, this actually makes it more useful for other purposes, such as for helping people with an opioid dependency.
What is Buprenorphine used for?
Buprenorphine can be used for two very different purposes:
- To relieve moderate - severe pain
- To assist people with a dependence on opioids
However, buprenorphine is more commonly used for opioid dependence than to relieve pain. This is because it is a partial opioid agonist and it is often less effective to relieve pain than other types of pain. On the other hand, this characteristic makes it beneficial for people who are dependent on opioids because it can block the effect of other opioid drugs.
How does it work?
Everyone naturally has endogenous opioids inside their body, which can bind to special receptors, called opioid receptors, to activate several effects in the body. When an endogenous opioid attaches to the right receptor, it has several effects on the body:
- Provides analgesia to relieve pain
- Slows down breathing
- Makes you feel tired
- Makes it more difficult to defecate.
Buprenorphine manipulates this natural process by activating the same receptors that the endogenous opioids do. They mimic the effect of natural opioids in your body.
Additionally, buprenorphine can also decrease the transmission of pain impulses in the body. They do this by interrupting the pain messages in the spinal cord and interfering with the messages coming from the brain in the central nervous system (CNS). This is another way it can relieve pain in the body.
There are several general side effects of opioid medications such as buprenorphine that can affect some people. Common side effects of opioids may include:
- Dry mouth
- Infrequent urination
The Norspan patch that contains buprenorphine can lead to some side effects related to the skin, such as a rash, itchiness or an allergic skin reaction.
You can find out more information about some of the specific side effects by clicking on them below.
It's common for people to notice some nausea when they first start taking an opioid drug. This usually only lasts a short time and gets better after a few days. However, if the nausea is severe, you may want to talk to your doctor about taking an anti-nausea drug for a few days.
A side effect that occurs to almost everyone who takes an opioid drug, especially for chronic pain, is constipation. Unfortunately, this doesn't get better with time and you usually need to do something to help with digestion in your body.
There are several things that you can do such as:
- Drink lots of water
- Eat foods that are easy to digest
- Keep active
- Take laxatives (usually two types: a stimulant and a stool softener)
If you are experiencing constipation, have a chat to your doctor or pharmacist about the best options for you.
In high doses, opioid medications can cause respiratory depression, which is breathing below what is required for the gas exchange with the blood to occur in the lungs. This means that you don't breathe enough for the oxygen in the air to make it into the lungs and blood.
As a result, your body doesn't have enough oxygen for normal functioning. In severe cases, this can lead to coma or death.
How can you tell if someone taking opioids has respiratory depression?
Usually by the time you notice changes in breathing it's too late. Instead, focus on how awake the person is. They should be easy to rouse and be able to stay awake. If they're not easy to rouse, a lower opioid dose is probably needed.
Over time, your body can get used to taking opioid medications and begin to depend the medications. This means that if you stop taking the drug, you may notice withdrawal symptoms such as:
This happens most often when people take opioid medications for a long time, such as if you are taking it for chronic pain.
There are several people who may need special attention if they are taking buprenorphine due to other medications or health conditions they have. For example, people who have the following conditions often need a lower dose than usual:
- Endocrine disease
- Adrenocortical insufficiency
- Myasthenia gravis
- Central nervos system (CNS) depression
- Frequent use of alcohol
Additionally, people with epilepsy are more likely to have a seizure while taking buprenorphine, so this should be considered.
Buprenorphine has a long half life of 10-24 hours, which means that it takes your body up to a day to reduce the concentration of the drug in your body to half. There will still be some traces of the drug in your blood stream 2-3 days after taking the last dose. In practice, this is a good thing to provide relief of chronic pain on an ongoing basis, but means you need to be careful if you need to change to a different opioid medication - you should stop buprenorphine a few days before starting the next one.
If you wish to stop taking buprenoprhine, it is important to talk to your doctor. Over time, your body "gets used" to taking the drug and you may experience withdrawal effects if you suddenly stop. Instead, you may need help in slowly decreasing the dose to allow your body time to adjust.
People who are elderly often require a lower dose of opioids than other adults.
This is because their body takes longer to process the drug, so the concentration in the bloodstream builds up more quickly. As a result, elderly people are more likely to experience side effects, such as cognitive impairment, sedation and respiratory depression. They may also be at risk for having a fall.
If you take buprenorphine at the same time as another drug the way they work can sometimes interact and change their effect on your body.
Firstly, buprenorphine is not usually used with other opioid drugs because it blocks the effect of the other opioid to reduce the pain relief, as well as causing some withdrawal effects.
Both atazanavir and tipranavir can increase the concentration of buprenorphine in your body because your body is less effective at clearing them out when you take them together. This can increase the side effects of buprenorphine. They are sometimes used together, but your doctor will probably suggest a lower dose of buprenorphine because of the interaction.
All drugs that cause your breathing to slow down can increase the risk of a serious side effect of buprenorphine: respiratory depression. Many drugs to lower blood pressure, such as beta blockers, can have this effect. Often they can be used together, but it's important that your doctor knows about the combination and checks that the dose is right for your body.
Some drugs that are used in the treatment of depression called selective seretonin reuptake inhibitors (SSRIs) can cause a condition called seretonin toxicity. The risk of this is higher if buprenorphine is taken at the same time, so you need to be on the lookout for early signs.
Pregnancy and Breastfeeding
Buprenorphine is not usually recommended for pregnant women because your baby is more likely to have respiratory depression, which can be fatal, and they may experience withdrawal effects when they are born and no longer get the dose from your blood stream. Instead, it is usually best for pregnant women to take other medications to relieve pain while they are pregnant, such as paracetamol.
Buprenorphine may be used for some women with opioid dependence while they are pregnant. This is not known to be safe, but the withdrawal symptoms in the baby appear to be less that the alternative, methadone.
For women who are breastfeeding, occasional doses with opioid are thought to be safe. However, their may be some risk to your baby if they are used every day for an extended period of time.