There is more than one medication that can be used for Opioid Substitution Therapy (OST). It is important to get the one that is right for you. For the most up to date information please refer to the CPSO website and the drug manufacturer.
What are the main medications?
One is a Liquid Opioid Full Agonist called Methadone.
We’ll call this Full Agonist (FA) for short.
This is most commonly found in liquid form pre-mixed and is dispensed at the pharmacy. It comes in flavored or unflavored versions. It is commonly mixed with juice.
The other is a Sublingual Opioid Partial Agonist called Suboxone.
This is a strip of film that is placed under your tongue. It dissolves and the medication enters your blood stream. The film is dry and contains no liquid.
We’ll call this Partial Agonist (PA) for short.
Why choose one over the other?
Here is a list of some of the factors that may indicate which medication may work for you.
Full Agonist (FA)
- You have been using opioids for a very long time.
- You are using very high doses of opioids.
- You are taking very strong (full agonist) opioid pain medications.
- You have no plans to travel across provinces or internationally.
- You are on a low or fixed income. It costs less and benefits may cover it.
- You are unwilling to go through withdrawal when starting treatment.
Partial Agonist (PA)
- You have been using opioids for a short period of time.
- You are a young person with good prospects of a quick recovery.
- You are taking lower doses of opioids.
- You are employed and can afford to pay for medication out of pocket.
- You frequently travel internationally or across provinces.
- You are currently in withdrawal.
- You are willing to go into withdrawal when starting treatment.
- You are at higher risk of respiratory failure due to your health or use of other medications or alcohol.
- Your employment prevents you from making regular visits to the pharmacy.
Can any doctor prescribe these medications?
No. A doctor needs a special license and exemption in order to prescribe the FA medication. The doctor needs specific training and knowledge to prescribe the PA medication.
Which medication is right for me?
Selection should be decided in consultation with your doctor. What works for other people may not work for you.
If one medication does not work out for me can I just switch?
It depends. If you are switching from the PA medication to the FA medication, that is a transition that can be managed by your physician. The process should be relatively comfortable.
However, the opposite can be more difficult (FA to PA medication). This has to do with the fact that you would be switching from a much stronger FA medication to a PA medication.
You will have to go into withdrawal in order to do this and the medication may cause precipitated withdrawal. In other words you will have to feel “sick” in order to make the switch.
For more information about FA medication scroll down.
FA Medication Information
How soon can I get my medication?
As soon as you have completed your initial appointment with the doctor.
How much will they give me?
You’ll get 10mg to 30mg for the first three days. Anyone who is at high risk for possible toxic effects will get 10mg to 20mg.
What is the “normal dose” for a patient?
It varies for everyone and you should not base your expectations on the doses other people are getting.
What are the stages of treatment that I’ll go through?
There are three basic stages to the treatment. They are: 1) the early stabilization phase; 2) the late stabilization phase; and 3) the maintenance phase.
The longer you stay in the program the better things will get for you. At the beginning just concentrate on making it through the first two weeks.
We call the first two weeks, the “early stabilization phase.”
What happens in the first two weeks?
You’ll get your first dose at 10mg to 30mg per day for the first three days. If you’re a high-risk patient you’ll start at 10mg to 20mg. Your doses may be increased by 5mg to 15 mg every three to four days.
During this time you are at risk of overdose and death if you use other drugs or alcohol. Your body is getting adjusted to metabolizing the medication and you may feel some withdrawal symptoms.
Just how important is it for me to stay clean for the first two weeks?
Most deaths occur in the first two weeks of treatment due to polydrug use (use of many drugs) and taking illegal opioid medication.
This underscores how important it is to avoid drug and alcohol use during the first two weeks of treatment.
Okay I made it through the first two weeks. Now what?
You’ve entered what we call the late stabilization phase. At this point you’ll probably be taking between 50mg and 80mg.
You’ll be getting partial relief of withdrawal symptoms. Your body is still only partially tolerant to the medication in your system.
Your dose might get adjusted every three to four days in the 5mg to 15mg range.
Six weeks in and I’m doing fine. What now?
You’re in the maintenance phase. At this point your body is largely tolerant to your medication. You should also experience no withdrawal symptoms at all most of the time.
What if I miss a dose just as I’m getting started?
If you miss three or more consecutive doses you have to re-start at the initial dose of 10mg to 30mg.
I’ve been maintaining for over six weeks and I missed a dose. Do I have to start over?
No. If you miss one or two days you can keep going on your regular dose as long as you are not currently using other drugs.
If you miss three days your remaining prescription will be cancelled. You will probably have to restart at 50% of your normal dose.
If you miss four days you have to start over from the beginning. Since you are not totally new to the medication your dose can be increased quickly in 10mg increments towards your normal maintenance dose.
What are “carries” and how do I get them?
After a while you’ll be able to get doses to take home so you’re not going to the pharmacy every day.
For the first two months you won’t get any carries. After two months you may be granted carries if you have been giving negative urine samples, your dose is stable, you are emotionally stable, have a safe place to live, have a stable support system, and have been keeping up with your program requirements.
Carries must be stored in a locked box and should be refrigerated. If you are living on the street or in a hostel or shelter that does not have proper storage facilities you will be denied carries.
You can get one carry per month after the first two months in treatment. After that you can get one additional carry per month up to a maximum of six doses per week if you remain clean.
If any of the criteria that qualify you for carries changes your carries may be revoked at any time. If you relapse the carries may be removed or reduced at the doctor’s discretion.
If you sell or give away your doses or if you try to cheat on a urine test your carries will be completely lost. Selling or giving away your medication is illegal.
It may be possible to grant more carries if the patient has a disability that makes it difficult or impossible for them to get to the pharmacy.
This will be done at the doctor’s discretion and will be changed in response to changes in the patient’s disability.
If you need to travel for the purposes of work or vacation your doctor may increase your carries accordingly.
Suboxone (Buprenorphine and Naloxone) Sublingual Film
What is a sublingual film?
Sublingual means that the medication in the film is absorbed into the bloodstream through blood vessels under your tongue. The film is placed in the mouth under the tongue and it dissolves.
What is the first pharmaceutical ingredient in the sublingual film?
It is an opioid commonly administered for opioid dependence. It is a partial agonist. Many opioids are full agonists like pain medications.
What is the difference between a partial and full agonist?
If you have become addicted to powerful pain medications you may require a full agonist OST medication. A partial agonist may not control your withdrawal effects and cravings.
If you have become addicted to more moderate levels of opioids, a partial agonist may do a good job of controlling withdrawal effects and cravings.
What is the second pharmaceutical ingredient?
It is an opioid antagonist.
What does an opioid antagonist do?
It’s an opioid drug that reverses the effect of other opioids and causes you to go into withdrawal.
Why is the opioid partial agonist combined with an opioid antagonist? How can this combination work? If one is supposed to counteract the other don’t they cancel each other out?
This is done in order to prevent the abuse of the medication. Manufacturers are building in safety features in order to discourage people from abusing their medication.
When taken as directed, by letting the film dissolve under the tongue, the opioid partial agonist is absorbed into the blood stream.
The opioid antagonist is not absorbed into the blood stream. It has no effect on the opioids in your body.
When the remains of the dissolved film are swallowed the opioid antagonist is not absorbed into the blood stream via the stomach or intestines. It has no effect on the opioids in your body.
The opioid antagonist only enters your bloodstream if it is taken by other methods such as snorting, smoking, or injecting the medication.
Do not attempt to inject or otherwise abuse the sublingual film. Injection may cause life-threatening infections as well as other health related problems. It may cause serious withdrawal symptoms depending on the presence of opioids in your system.
What varieties of this medication are available?
In Canada the sublingual film is the most commonly available form. The opioid does exist in the singular form but is used more commonly in other countries.
Are the side effects of sublingual film worse than what I’m on now?
The opioid in the sublingual film is the same category as other opioids. The side effects should be similar. You may find a reduction in side effects due to your constant stable dose.
Side effects may include but are not limited to the following: Sweating, constipation, dry mouth, weight gain, irregular heartbeat, depressed respiration, and drowsiness. For a complete list of all possible side effects contact a doctor or pharmacist.
The sublingual film seems to be newer. How long has it been around?
It was originally launched in 2003 in tablet form. A film was developed as it dissolves more quickly than tablets and has less after taste. The film is also abuse resistant as it is more difficult to crush into a powdered form.
What does the sublingual film do when I take it?
When you are opioid dependent the discontinuation of opioid use leads to withdrawal symptoms. The opioid partial agonist suppresses withdrawal symptoms and reduces cravings.
Am I substituting one drug for another?
Yes. Your body is now physiologically dependent on opioids. In order to suppress withdrawal symptoms and reduce cravings you body needs opioid medication. The idea is to substitute a legal and long acting medication as a replacement for other opioids you may be taking.
Street drugs can be cut with unknown substances, are costly, and dangerous. OST medication provides a safe substitute that is cost effective, legal when taken as prescribed by a physician, and does not produce any euphoric effects.
Is taking the sublingual film enough to prevent me from taking drugs?
Managing your withdrawal symptoms and cravings are only one part of recovery. Social and lifestyle factors play a huge role in staying clean. Ongoing treatment that includes counseling and cognitive behavioral therapy will increase your ability to stay clean.
What are some side effects I might experience from taking the sublingual film?
Side effects may include the normal side effects associated with opioid use such as constipation and sweating. Other side effects may include numb mouth, redness of the mouth, painful tongue, irregular heartbeat, blurred vision, fainting, dizziness, or sleepiness.
Due to the nature of the medication you could also experience some withdrawal symptoms. These include flu like symptoms such as chills, aches, headache, insomnia, and stuffy nose.
When I start how much will I get?
Films come pre-packaged in pre-determined doses. Your doctor will prescribe the appropriate dose for you to take. During “induction,” which is your first dose, it is common to prescribe 4mg and then to observe the results. If there is no precipitated withdrawal another dose may be administered.
Normal dose adjustments are in the 2mg – 4 mg range. After two to three days it may be possible to go to once a day dosing. It takes up to a week for steady state blood levels to be achieved. A comfortable steady dose may be obtained within two weeks.
What is the normal amount that people get?
Everyone is different but most patients should be able to be stable at 12mg – 16mg. Some people may require a higher dose but amounts over 32 mg are uncommon.
How does the partial agonist work?
When opioids are introduced to your bloodstream they reach the brain and attach to receptors in the brain. Opioid binding at the receptors stimulates the release of a chemical called dopamine into another area of the brain associated with pleasurable sensations.
The increased dopamine activity in the area associated with pleasurable sensations is of the reasons why people abuse opioid medications.
Repeated use of an opioid causes receptors to become tolerant. Tolerance means that higher doses are required in order to get the same pleasurable effect.
With continued opioid use and continued elevated doses, the brain chemistry is altered so that the opioid no longer provides pleasurable sensations. Instead it becomes a necessity for normal functioning. Without the opioid, withdrawal symptoms will result.
Once tolerance has been established if the opioid concentration in the brain drops – the receptors become unoccupied. This leads to an overall decline in opioid-induced activity.
This upsets the brain which then releases another chemical which the patient experiences as the symptoms of opioid withdrawal.
When the partial agonist enters the bloodstream it travels to the brain where it binds to and occupies the receptors. This keeps opioid activity in the brain. As a partial agonist it helps control withdrawal symptoms.
The partial agonist has a high affinity for the receptor. This prevents it from being replaced by other opioids that enter the blood stream and thus, blocks the effects of these other opioids. Once you are on a stable dose most of the receptors will remain occupied and withdrawal symptoms and cravings will be controlled.
Is the sublingual film more expensive than other OST medication?
Yes. The other FA medication is less expensive and is also covered by government benefit programs. The sublingual film is not covered by government programs and may or may not be covered by your drug plan or other workplace drug benefit plans.
Does the sublingual film last longer than other OST medication?
It may last longer than other OST medications so you may have to dose less often.
Why would anyone inject the sublingual film?
Some people are psychologically addicted to injecting with needles. Some people may not understand how the medication works or what it is so they do what they normally do and inject it. Injecting it is dangerous and should never be done.
If I miss a dose will I get sick?
You will begin to feel the normal opioid withdrawal effects.
Is it possible to be allergic to the pharmaceutical ingredients in the sublingual film?
Yes. If you have a history of hypersensitivity or allergy to medications inform your doctor. An allergic reaction may have serious effects on your health. If you are allergic to the contents of the film do not take it.
For more info on PA medication scroll down.
Can I overdose while taking the sublingual film?
Yes. If you are taking OST medication you should not consume other drugs including alcohol, benzodiazepines, or other sedatives that can depress your central nervous system. These can lead to respiratory failure and death. Other street drugs and medications can also cause serious complications and you should inform your physician if there is a risk that you could consume these street drugs and medications.
What happens if I take other opioids in combination with the sublingual film?
Doing this is very dangerous. The effects depend on if you have taken the sublingual film as directed and the quantity and type of other opioids you have taken.
Example 1. You take opioids and then take the sublingual film.
If you have already taken other full agonist opioids and they are still in your system and you take the sublingual film you will feel acute withdrawal symptoms. You will feel “sick.”
The opioid the sublingual film contains is a potent antagonist at the opioid receptors. It will remove the full agonist opioids that are already in your brain and place itself into the receptors in their place. You will bring on precipitated withdrawal.
Example 2. You take the sublingual film and then take more opioids.
If you have already taken the sublingual film and you take other opioids the situation is different. The opioid in the sublingual film has a high affinity for the receptor and this keeps it from being replaced by other opioid full agonists.
It blocks the effects of other opioids. So taking other opioids while on PA medication is pointless and dangerous.
You will not feel the effect of the additional opioids. At the same time you have loaded your body with a dangerous amount of opioids that could cause an overdose and death.
A person might think that they didn’t take enough additional opioids because they felt no effect. They might take even more. This further increases the risk of an overdose.
So if I’m getting into treatment and I have a lot of strong opioids in my system and I take the PA medication and it replaces the other drugs in my brain, will I feel like I’m going through withdrawal?
Yes. The opioid partial agonist has a “low intrinsic activity” which means it does not activate the receptor to the same extent that other full agonist opioids do. In other words it is a “step down” from the full agonist opioids in your system.
As a result when the partial agonist replaces the other opioids you will feel worse than you did before. This is because your receptors are not activated to the same extent that they were previously. This if referred to as “precipitated withdrawal.”
This is why you should not start taking the sublingual film until you are already in withdrawal.
You mean I have to get sick before I start taking the medication?
Yes. This is for your comfort, safety, and maximum effectiveness of the medication. It may sound strange that you have to get “sick” before you take the medication that is supposed to prevent you from getting “sick.” That is how it works.
Is the opioid antagonist (the second ingredient in the sublingual film) causing the precipitated withdrawal?
No. It has virtually no effect when taken sublingually and swallowed. It only comes into effect if the drug is injected directly into the bloodstream with a needle or otherwise used in an abusive manner.
If you are taking your medication as directed by your physician the medication will not cause a withdrawal.
So if the doctor asks when I last “used” when discussing which OST medication to prescribe?
Be honest about the frequency, quantity, and type of opioids you use. Precipitated withdrawal symptoms are difficult to get through.
Getting the right medication for your needs is important for your comfort and safety. Make sure to discuss your options when considering the type of treatment you need.
By being honest you can time your first dose in order to avoid the worst withdrawal symptoms.
Also patients with a very high tolerance may find that a partial agonist may not effectively block their cravings and withdrawal symptoms. Other OST medications may be a better option.
For more info on PA medication scroll down.
What if I have acute or chronic pain?
In some cases non-opioid drugs or procedures may be substituted for pain treatment. This is because the PA occupies receptors and blocks other opioids, thus it will block the effectiveness of other opioids in the treatment of acute and chronic pain.
Does the partial agonist produce a euphoric effect like other opioids?
No. When taken as directed it will mask withdrawal symptoms and cravings.
What are the risks if I take other drugs in combination with this medication?
The main risk is an overdose leading to respiratory failure and death. Only take the medications prescribed by your physician and only as directed by your physician.
I want to try the sublingual film before I join the program. Can I just buy some on the street?
Selling, buying, or giving opioids to another person is illegal and dangerous and carries with it the risk of overdose and other serious health related consequences, including death.
Is it harder to get off of the sublingual film than other opioids?
The withdrawal symptoms are typically milder than what is seen with full agonists.
Withdrawal effects may include the following:
- Muscle Aches
- Abdominal Cramps
- Hot Flashes
- General discomfort
- Drug craving
- Dilated pupils
- Abdominal tenderness
Do I have to quit taking my OST medication eventually?
No. There in no time limit on how long you can be in treatment. That is a choice that is up to you and your physician. This should be determined by discussing the idea with your physician. The process for getting off the medication is called tapering.
This will cause you to feel withdrawal symptoms and you may have cravings. If the taper is done under proper control and supervision the effects should be minimized.
Outside factors like your living situation and community support will play a big role in how well you transition though this stage.
© 2015 Addiction Centre Toronto.