Buprenorphine and Methadone

Methadone is a very useful tool to help patients manage overwhelming intractable pain. Once their pain is under control, they are more likely going to be able to implement other tools to manage pain, which could eventually lead to reduction or withdrawal of opioids.

You may be concerned about addiction and you should be. Opioids are addictive drugs and carry significant risks. Methadone and buprenorphine/Naloxone are safer opioid alternatives, Buprenorphine-naloxone safer than Methadone. Buprenorphine.Nalone requires withdrawal from other opioids before starting, but there is an option for microdosing. See below.

Some people require opioids like methadone for the rest of their lives. That is called dependence. You depend on the drug for a good quality of life. It may be a small price to pay.

Here is an outline of Methadone Use for Pain.

Buprenorphine is an opioid that can help people manage substance problems, like an opioid addiction. It is being used off-label to help people in pain. Some people develop tolerance to certain opioids and require increasing doses to manage their pain. I recommend decreasing the opioids for a week at least, even quitting for a short period while the nerve regenerates to accept a lower dose again.

Managing pain appropriately will help prevent unnecessary harm, including under-treated pain, suicides and people turning to street drugs.

Buprenorphine is being investigated for use for chronic pain but is not indicated yet for that. Methadone has already achieved indications for chronic pain and is especially useful for neuropathic pain.

Neuropathic pain may not always be obvious on clinical examination. Widespread pain can often involve inflammation of smaller neurons and lead to neuropathic type pain.

When pain is severe, or even moderately severe, opioids are an important pain management tool.

Clinical Guidelines for Physicians BC

I am quoting J Ochsner, from 2018, Spring; 18(1) 23-29, Suboxone: Rationale, Science, Misconceptions. 

Buprenorphine is a long-acting, high-affinity partial agonist at the mu-opioid receptor. As a long-acting agonist, buprenorphine prevents withdrawal and craving and stabilizes opioid receptors. As a high-affinity agonist, buprenorphine blocks other opioids from binding, preventing abuse of other opioids. As a partial agonist, it has a smaller effect with a ceiling, a low overdose risk, and no intoxication in the opioid dependent. Buprenorphine is available in many formulations*. The most common formulation is buprenorphine and naloxone (Suboxone) in a 4:1 ratio. As an opioid antagonist with high first-pass hepatic metabolism, naloxone has no effect on sublingual use of buprenorphine but blocks intravenous or intranasal abuse of buprenorphine. In contrast, naltrexone is another opioid antagonist with greater oral bioavailability that blocks all opioids regardless of delivery method and is also US Foods and Drug Administration (FDA) approved for treatment of opioid use disorder. Buprenorphine without naloxone is used for pain management and can be prescribed for opioid use disorder in sublingual film or tablet form. Except in the case of severe hepatic impairment or pregnancy, prescription of isolated buprenorphine is discouraged given the potential for intravenous abuse.

Addiction vs Dependence

Sometimes patients feel as if their doctors think they are addicts. Almost always this is not the case. Doctors are concerned about opioids as they can produce tolerance and dependence. If you have chronic pain you may be dependent on your medication for pain relief which is not the same as addiction.

Opioids are very easy to misuse, so be sure to read the instructions.

Opioid use Disorder

Excerpt taken from the Suboxone medication information pamphlet from the company

If you feel you may have an opioid use disorder, remember it is a chronic relapsing condition affection the brain and treatment is available.

Psychological dependence

  • The drug is central to your thoughts and often used compulsively +- cravings.

Physical dependence

The body suffers from withdrawal symptoms if the drug is reduced or stopped abruptly

Storage

Store in a safe place locked away – keep away from children and never give the drug to anyone else.

What does it do?

Buprenorphine is an opioid that reduces cravings and symptoms of withdrawal

Naloxone is added to Suboxone to stop people injecting other opioids. It blocks the effects of other opioids like methadone, heroin, morphine and can give withdrawal side effects of these drugs

Route of use

Use it correctly – allow to dissolve under the tongue – and it will work correctly.

Put it under the tongue and let it dissolve – takes 2-10 minutes.

Your doctor will ask you to wait for withdrawal symptoms from your previous opioids before starting Suboxone. This is to avoid intense withdrawal.

If you miss a dose, take it as soon as possible but do not take a double dose in one day.

If you miss more than one dose – contact your pharmacist.

If you land up in an emergency room, let the doctors know you are on Suboxone.

Do not break, crush or chew the tablet.

Signs of overdosage

Slow or weak breathing, dizziness, confusion or extreme drowsiness.

Contact a health professional immediately if this happens

Interactions

Read the pharmacist pamphlet carefully. Do not use with alcohol or benzodiazepines or monoamine oxidase inhibitors

Microdosing

Micro-dosing is a valuable tool for easing into induction of B-N, mitigating the moderate to severe opioid withdrawal for standard induction. As of Dec

Microdosing Strategy. This from 2020 – Depending on the opioid formulation, the opioid can usually be stopped when a dose of 4-1mg to 12-4mg of Buprenorphine has been reached. Patients could be prescribed as needed additional B-N doses of 2-0.5mg to combat minor WD symptoms.

Clonidine, dimenhydrinate, ibuprofen, acetaminophen, and loperamide might be helpful to manage withdrawal.

CMAJ also has a strategy: https://www.cmaj.ca/content/192/3/E73.

Great article on buprenorphine https://www.wired.com/2005/04/bupe/

Here is another article – As in anything in medicine – always do your own research. I’ve included this article as there are some really valid points. But – in Canada – buprenorphine is treated as any other opioid – prescribing it requires opioid prescription pad and specific rules – so not all is true with regard Canada – but there are important points in the article about the affinity the drug has for receptors which make general anesthesia a real challenge – read the article and do more of your own research – https://edsinfo.wordpress.com/2018/08/02/what-makes-buprenorphine-risky-for-pain-patients/