Opioids

Medically reviewed by Philip J. Gregory, PharmD, MS, FACN on June 29, 2017Written by University of Illinois at Chicago, Drug Information Group

Introduction

The first opioid medication, morphine, was created in 1803. Since then, many different opioids have come onto the market. 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. Additionally, some opioids are added to products made for more specific uses, such as treating cough or opioid dependence.

Forms of opioids

Opioid products come in many different 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 you take yourself, and some, such an injectable forms, have to be given by a healthcare professional.

Immediate-release products start to work quickly after you take them, but they are effective for shorter periods. Extended-release products release the drugs over longer periods. Products are generally immediate-release unless they are specified 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.

List of opioid-only products

The following products contain only opioids:

  • buprenorphine
  • butorphanol
  • codeine sulfate
  • fentanyl
  • hydrocodone bitartrate
  • hydromorphone
  • levorphanol tartrate
  • meperidine hydrochloride
  • methadone hydrochloride
  • morphine sulfate
  • oxycodone
  • oxymorphone
  • tapentadol
  • tramadol

Buprenorphine

This drug is an extended-release product. 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.

Brand-name buprenorphine products include:

  • Belbuca, a buccal film
  • Probuphine, an intradermal implant
  • Butrans, a transdermal patch
  • Buprenex, an injectable solution

These 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, 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 is not commonly used for pain, but 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 is only 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 and is 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. Demerol is available in an oral tablet. Both are also available in an injectable solution given by a healthcare provider.

Methadone hydrochloride

Methadone hydrochloride is available as a generic drug and the brand-name drug Dolophine. This drug is 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 opium tincture, which is an amount of morphine sulfate mixed with alcohol. This form is used to reduce the number and frequency of bowel movements and can treat diarrhea in certain cases.

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. The immediate-release products are used for acute and chronic pain. The injectable products are only given by a healthcare provider.

Oxycodone

Some forms of oxycodone are available as generic drugs. Some are only available as name-brand 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 an 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 Food and Drug Administration requested that manufacturers of extended-release oxymorphone products discontinue these drugs. This was because they found that the benefit of taking this drug no longer outweighs the risk.

The immediate-release tablets are still used for acute and chronic pain.

Oxymorphone is also available in a form that is 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. The extended-release products are used for chronic pain in people who need around-the-clock treatment. The external cream is used for musculoskeletal pain.

List of opioid combination products

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
  • acetaminophen/codeine
  • aspirin/caffeine/dihydrocodeine
  • hydrocodone/acetaminophen
  • hydrocodone/ibuprofen
  • morphine/naltrexone
  • oxycodone/acetaminophen
  • oxycodone/aspirin
  • oxycodone/ibuprofen
  • oxycodone/naltrexone
  • pentazocine/naloxone
  • tramadol/acetaminophen

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 a capsule that you take by mouth. 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 an oral solution. Brand-name version include:

  • Anexsia, an oral tablet
  • Norco, an oral tablet
  • Zyfrel, an oral solution

Hydrocodone/ibuprofen

Hydrocodone/ibuprofen is available in oral tablet. It comes as a generic product 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 in an oral solution and an 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 as the brand-name drug Percodan. It comes in an oral tablet an is 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 that you typically use 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 and is used for both acute and chronic pain.

Tramadol/acetaminophen

Tramadol/acetaminophen is available as a generic drug and as the brand-name drug Ultracet. It comes in an oral tablet. You typically use it for no longer than five days to treat short-term severe pain.

Opioids in products for uses other than pain

Codeine, hydrocodone, buprenorphine, and methadone are opioids that can be used alone or in combination products to treat conditions other than acute and chronic pain. 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 dependence.

Considerations for opioid use

Although there are many opioids and opioid combination products, not every one of these drugs may be appropriate for your treatment. It’s important that you use the right opioid and that you 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 abuse
  • your health insurance coverage

Pain severity

Your doctor will consider how severe your pain is when recommending an opioid treatment for you. 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 have not 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 chronic therapy.

Other conditions

Some opioid medications are removed from your body by your kidneys. If you have poor kidney function, then you might be at a higher risk of side effects from these drugs. These opioids include codeine, morphine, hydromorphone, hydrocodone, oxymorphone, and 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, including over-the-counter products, supplements, and herbs, so your doctor can select the safest opioid for you.

Age

Not all opioid products are appropriate for all age groups. Products that contain tramadol and codeine should not be used in children younger than 12 years. Additionally, these products shouldn’t be used in people between the ages of 12 and 18 years if they are obese, have obstructive sleep apnea, or have severe lung disease.

History of substance abuse

It’s important to let your doctor know if you have had substance abuse issues. Some opioid products are formulated to reduce the risk of abuse. These products include:

  • OxyContin
  • Targiniq ER
  • Embeda
  • Hysingla ER
  • MorphaBond
  • Xtampza ER
  • Troxyca ER
  • Arymo ER
  • Vantrela ER
  • RoxyBond

Insurance coverage

Not all opioid products are covered by individual insurance plans, 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 will be covered by your insurance.

Many insurance companies limit the amount of opioid product that you can obtain each month. Your insurance company may also require a prior approval from your doctor before approving your prescription.

Steps for safe use of opioids

Using opioids, even for short periods, can lead to addiction, abuse, and overdose. There are a few steps that you can take to use opioids more safely:

  • Make sure to tell your doctor about any history of substance abuse so they can carefully monitor you during treatment with opioids.
  • Make sure to follow your doctor’s directions. 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 of 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 effect 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 stop taking opioids safely. Some people may need to stop by slowly tapering off their use.

Talk to your doctor

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 that you have. Because dependence can develop over time, you should 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.

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