SAFETY ALERT FOR ORAL BUPRENORPHINE
In January 2022, the Food and Drug Administration (FDA) issued a
Introduction
The first opioid medication, morphine, was created in 1803. Since then, many different opioids have come onto the market. Some are also added to products made for more specific uses, such as treating a cough.
Currently in the United States many opioid-only and opioid combination drugs are used to treat acute and chronic pain when other medications, such as ibuprofen or acetaminophen, aren’t strong enough. Certain types are also used in the treatment of opioid use disorders.
Opioid products come in many forms. They differ in how you take them as well as how long they take to start working and how long they keep working. Most of these forms can be taken without assistance. Others, such injectable forms, have to be given by a healthcare professional.
Immediate-release products start to work quickly after you take them, but they’re effective for shorter periods. Extended-release products release the drugs over longer periods. Products are generally considered immediate-release unless they’re labeled otherwise.
Immediate-release opioids are used to treat acute and chronic pain. Extended-release opioids are typically only used to treat chronic pain when immediate-release opioids are no longer enough.
If your doctor prescribes extended-release opioids to you, they may also give you immediate-release opioids to treat breakthrough pain, particularly for cancer pain or pain during end-of-life care.
These products contain only opioids:
Buprenorphine
This drug is a long-acting opioid. Generic buprenorphine comes in a sublingual tablet, transdermal patch, and injectable solution. The generic and brand-name injectable solutions are only given by a healthcare provider.
Examples of brand-name buprenorphine products include:
- Belbuca, a buccal film
- Probuphine, an intradermal implant
- Butrans, a transdermal patch
- Buprenex, an injectable solution
Some forms are used for chronic pain that requires around-the-clock treatment. Other forms of buprenorphine are available to treat opioid dependence.
Butorphanol
Butorphanol is only available as a generic drug. It comes in a nasal spray. It’s an immediate-release product and typically used for acute pain. Butorphanol is also available in an injectable solution that must be given by a healthcare provider.
Codeine sulfate
Codeine sulfate is only available as a generic drug. It comes in an immediate-release oral tablet. Codeine sulfate isn’t commonly used for pain. When it is, it’s typically used for mild to moderate acute pain.
Fentanyl
Generic fentanyl comes in oral lozenges, extended-release transdermal patches, and an injectable solution that’s only given by a healthcare provider. Brand-name fentanyl products include:
- Fentora, a buccal tablet
- Actiq, an oral lozenge
- Lazanda, a nasal spray
- Abstral, a sublingual tablet
- Subsys, a sublingual spray
- Duragesic, an extended-release transdermal patch
The transdermal patch is used for chronic pain in people who need around-the-clock treatment and who already regularly use opioid pain medications.
The other products are used for breakthrough pain in people who already receive around-the-clock opioids for cancer pain.
Hydrocodone bitartrate
Hydrocodone bitartrate, as a single ingredient, is available as the following brand-name products:
- Zohydro ER, an extended-release oral capsule
- Hysingla ER, an extended-release oral tablet
- Vantrela ER, an extended-release oral tablet
It’s used for chronic pain in people who need around-the-clock treatment. However, it’s not commonly used.
Hydromorphone
Generic hydromorphone comes in an oral solution, oral tablet, extended-release oral tablet, and rectal suppository. It’s also available in an injectable solution given by a healthcare provider.
Brand-name hydromorphone products include:
- Dilaudid, an oral solution or oral tablet
- Exalgo, an extended-release oral tablet
The extended-release products are used for chronic pain in people who need around-the-clock treatment. The immediate-release products are used for both acute and chronic pain.
Levorphanol tartrate
Levorphanol is only available as a generic drug. It comes in an oral tablet. It’s typically used for moderate to severe acute pain.
Meperidine hydrochloride
This drug is typically used for moderate to severe acute pain. It’s available as a generic drug and as the brand-name drug Demerol. Generic versions are available in an oral solution or oral tablet. Both are also available in an injectable solution that’s given by a healthcare provider.
Methadone hydrochloride
Methadone hydrochloride is available as a generic drug and the brand-name drug Dolophine. It’s used for chronic pain in people who need around-the-clock treatment.
The generic version is available in an oral tablet, oral solution, and oral suspension. It’s also available in an injectable solution given by a healthcare provider. Dolophine is only available in an oral tablet.
Morphine sulfate
Generic morphine sulfate is available in an extended-release oral capsule, oral solution, oral tablet, extended-release oral tablet, rectal suppository, and solution for injection.
It also comes in an
Brand-name morphine sulfate products include:
- Kadian, an extended-release oral capsule
- Arymo ER, an extended-release oral tablet
- MorphaBond, an extended-release oral tablet
- MS Contin, an extended-release oral tablet
- Astramorph PF, a solution for injection
- Duramorph, a solution for injection
- DepoDur, a suspension for injection
The extended-release products are used for chronic pain in people who need around-the-clock treatment. Immediate-release products are used for acute and chronic pain. Injectable products are only given by a healthcare provider.
Oxycodone
Some forms of oxycodone are available as generic drugs. Some are only available as brand-name drugs. Generic oxycodone comes in an oral capsule, oral solution, oral tablet, and extended-release oral tablet.
Brand-name versions include:
- Oxaydo, an oral tablet
- Roxicodone, an oral tablet
- Oxycontin, an extended-release oral tablet
- Xtampza, an extended-release oral capsule
- Roxybond, an oral tablet
The extended-release products are used for chronic pain in people who need around-the-clock treatment. The immediate-release products are used for acute and chronic pain.
Oxymorphone
Generic oxymorphone is available in an oral tablet and extended-release oral tablet. Brand-name oxymorphone is available as:
- Opana, an oral tablet
- Opana ER, an extended-release oral tablet or crush-resistant extended-release oral tablet
The extended-release tablets are used for chronic pain in people who need around-the-clock treatment.
However, in June 2017, the
The immediate-release tablets are still used for acute and chronic pain.
Oxymorphone is also available in a form that’s injected into your body as the brand-name product Opana. It’s only given by a healthcare provider.
Tapentadol
Tapentadol is only available as the brand-name versions Nucynta and Nucynta ER. Nucynta is an oral tablet or oral solution used for both acute and chronic pain. Nucynta ER is an extended-release oral tablet used for chronic pain or severe pain caused by diabetic neuropathy (nerve damage) in people who need around-the-clock treatment.
Tramadol
Generic tramadol comes in an extended-release oral capsule, oral tablet, and extended-release oral tablet. Brand-name tramadol comes as:
- Conzip, an extended-release oral capsule
- EnovaRx, an external cream
The oral tablet is typically used for moderate to moderately severe acute pain. Extended-release products are used for chronic pain in people who need around-the-clock treatment. The external cream is used for musculoskeletal pain.
The following products combine an opioid with other drugs. Similar to the opioid-only products, these drugs come in different forms and have different uses:
Acetaminophen-caffeine-dihydrocodeine
This drug is typically only used for moderate to moderately severe acute pain. Generic acetaminophen-caffeine-dihydrocodeine comes in an oral tablet and an oral capsule. The brand-name product Trezix comes in an oral capsule.
Acetaminophen-codeine
This drug is typically only used for mild to moderate acute pain. Generic acetaminophen-codeine comes in an oral tablet and an oral solution. Brand-name acetaminophen-codeine comes as:
- Capital and Codeine, an oral suspension
- Tylenol with Codeine No. 3, an oral tablet
- Tylenol with Codeine No. 4, an oral tablet
Aspirin-caffeine-dihydrocodeine
Aspirin-caffeine-dihydrocodeine is available as a generic and the brand-name drug Synalgos-DC. It comes in an oral capsule. It’s typically only used for moderate to moderately severe acute pain.
Hydrocodone-acetaminophen
This drug is typically used for moderate to moderately severe acute pain. Generic hydrocodone-acetaminophen comes in an oral tablet and oral solution. Brand-name versions include:
- Anexsia, an oral tablet
- Norco, an oral tablet
- Zyfrel, an oral solution
Hydrocodone-ibuprofen
Hydrocodone-ibuprofen is available as an oral tablet. It comes as a generic and the brand-name drugs Reprexain and Vicoprofen. It’s typically used for acute pain.
Morphine-naltrexone
Morphine-naltrexone is only available as the brand-name drug Embeda. It comes in an extended-release oral capsule. This drug is typically used for chronic pain in people who need around-the-clock treatment.
Oxycodone-acetaminophen
This drug is used for both acute and chronic pain. Generic oxycodone-acetaminophen is available as an oral solution and oral tablet. Brand-name versions include:
- Oxycet, an oral tablet
- Percocet, an oral tablet
- Roxicet, an oral solution
- Xartemis XR, an extended-release oral tablet
Oxycodone-aspirin
Oxycodone-aspirin is available as a generic and the brand-name drug Percodan. It comes as an oral tablet. It’s typically used for moderate to moderately severe acute pain.
Oxycodone-ibuprofen
Oxycodone-ibuprofen is only available as a generic drug. It comes in an oral tablet. It’s typically used for no more than seven days to treat short-term severe pain.
Oxycodone-naltrexone
Oxycodone-naltrexone is only available as the brand-name drug Troxyca ER. It comes in an extended-release oral capsule. It’s typically used for chronic pain in people who need around-the-clock treatment.
Pentazocine-naloxone
This product is only available as a generic drug. It comes in an oral tablet. It’s used for both acute and chronic pain.
Tramadol-acetaminophen
Tramadol-acetaminophen is available as a generic drug and the brand-name drug Ultracet. It comes in an oral tablet. This form is typically used for no longer than five days to treat short-term severe pain.
Some opioids can be used alone or in combination products to treat conditions other than acute and chronic pain. These drugs include:
- codeine
- hydrocodone
- buprenorphine
- methadone
For example, both codeine and hydrocodone are combined with other drugs in products that treat cough.
Buprenorphine (alone or combined with naloxone) and methadone are used in products to treat opioid use disorders.
There are many opioids and opioid combination products. They each have different treatment uses. It’s important to use the right opioid and use it correctly.
You and your doctor will need to consider many factors before selecting the best opioid product or products for your individual treatment. These factors include:
- the severity of your pain
- your pain treatment history
- other conditions you have
- other drugs you take
- your age
- whether you have a history of substance use disorders
- your health insurance coverage
Pain severity
Your doctor will consider how severe your pain is when recommending an opioid treatment. Some opioid medications are stronger than others.
Some combination products, such as codeine-acetaminophen, are only used for pain that’s mild to moderate. Others, such as hydrocodone-acetaminophen, are stronger and used for moderate to moderately severe pain.
Immediate-release opioid-only products are typically used for moderate to severe pain. Extended-release products are only meant to be used for severe pain that needs around-the-clock treatment after other medications haven’t worked.
Pain treatment history
Your doctor will consider if you already receive medication for your pain when recommending further treatment. Some opioid medications, such as fentanyl and methadone, are only appropriate in people who already take opioids and need long-term therapy.
Other conditions
Your kidneys remove some opioid medications from your body. If you have poor kidney function, you might have a higher risk for side effects from these drugs. These opioids include:
- codeine
- morphine
- hydromorphone
- hydrocodone
- oxymorphone
- meperidine
Drug interactions
Some drugs should be avoided or used with caution to avoid interactions with certain opioids. It’s important to let your doctor know about all medications you take so your doctor can select the safest opioid for you. This includes any over-the-counter products, supplements, and herbs.
Age
Not all opioid products are appropriate for all age groups.
Children younger than 12 years shouldn’t use products containing tramadol and codeine.
Additionally, these products shouldn’t be used in people between the ages of 12 and 18 years if they’re obese, have obstructive sleep apnea, or have severe lung disease.
History of substance misuse
It’s important to let your doctor know if you’ve had substance use issues. Some opioid products are formulated to reduce the risk of misuse. These products include:
- Targiniq ER
- Embeda
- Hysingla ER
- MorphaBond
- Xtampza ER
- Troxyca ER
- Arymo ER
- Vantrela ER
- RoxyBond
Insurance coverage
Individual insurance plans don’t cover all opioid products, but most plans cover some immediate-release and extended-release products. Generics generally cost less. Talk to your doctor or pharmacist to help determine which product your insurance will cover.
Many insurance companies limit the amount of opioid product you can obtain each month. Your insurance company may also require a prior approval from your doctor before approving your prescription.
Using opioids, even for short periods, can lead to addiction and overdose. There are a few steps you can take to use opioids safely:
- Tell your doctor about any history of substance misuse so they can carefully monitor you during treatment with opioids.
- Follow the directions on your prescription. Taking too much or taking a dose incorrectly (such as crushing pills before taking them) can lead to more side effects, including difficulty breathing and overdose.
- Talk to your doctor about what substances you should avoid while taking an opioid. Mixing opioids with alcohol, antihistamines (such as diphenhydramine), benzodiazepines (such as Xanax or Valium), muscle relaxants (such as Soma or Flexeril), or sleep aids (such as Ambien or Lunesta) can increase your risk for dangerously slowed breathing.
- Store your medication safely and out of reach of children. If you have any unused opioid pills, take them to a community drug take-back program.
Tolerance and withdrawal
Your body will become tolerant to the effects of opioids the longer you take them. This means that if you take them for longer periods, you may need higher and higher doses to get the same pain relief. It’s important to let your doctor know if this happens to you.
Opioids can also cause withdrawal if you suddenly stop them. It’s important to discuss with your doctor how to safely stop taking opioids. Some people may need to stop by slowly tapering off their use.
There are many opioids available to treat acute and chronic pain as well as more specific conditions. Some products may be more appropriate for you, so talk with your doctor to make sure they know about factors that could influence the treatment they recommend for you.
After starting an opioid product, make sure to see your doctor regularly and talk about any side effects or concerns you have. Because dependence can develop over time, also talk with your doctor about what to do if you feel it happening to you.
If you want to stop your opioid therapy, your doctor can work with you on a plan to safely stop taking them.