Opioid Use Disorder: These Treatments Are Available, Now
Medically reviewed by L. Anderson, PharmD. Last updated on Dec 14, 2018.
The Opioid Epidemic: A Public Health Crisis
The opioid addiction epidemic is rampant in the U.S. and it's hard to ignore the news. You may have a personal experience, too: either yourself, family, friends, or even co-workers. The headlines are nonstop, the statistics are shocking, and the outcomes are tragic. Consider these numbers:
- Every day, more than 200 Americans die from an opioid overdose. That equates to one person dying about every 7 minutes.
- It's not just street heroin or other illicit drugs that's the problem. In fact, in 2015, over 33,000 Americans died from an opioid overdose that also included prescription pain killers like hydrocodone and oxycodone, and illegally manufactured or diverted drugs sold on the streets, like fentanyl and carfentanil, both powerful and dangerous synthetic opioids.
- Fentanyl is 50 times stronger than heroin; carfentanil, used to tranquilize large animals, is 5,000 times stronger. As reported in 2018, fentanyl is now the top opioid involved in overdose deaths. It is often cut into heroin bought on the streets.
- China is a main source of fentanyl and other synthetic opioids in the US, as reported by the DEA.
Prescription misuse is widespread, too.
- One quarter of those who receive a prescription for an opioid pain medication will misuse it in some way, 8% to 12% develop an opioid use disorder, and up to 6% may transition to the use of heroin, often because it's cheaper than painkillers bought on the street.
- About 80% of people who use heroin first misused a prescription opioid they probably received legally via a prescription from their doctor.
Which Drugs Are Opiates?
Opiates, sometimes called narcotics, are either prescribed medications most often used to control pain, or bought from a dealer, such as heroin. These drugs can be abused, whether they are legally obtained with a prescription from the doctor, or illegally on the streets.
Knowing which drugs might have addiction potential is important. Examples of prescription opioid analgesics include:
- Oxycodone (Oxycontin, Roxicodone), Xtampza ER)
- Hydrocodone (Hysingla ER, Zohydro ER)
- Acetaminophen/Hydrocodone (Lortab, Lorcet, Vicodin)
- Tramadol (Ultram, ConZip)
- Acetaminophen/Codeine (Tylenol with Codeine)
- Fentanyl (Duragesic, Actiq, Sublimaze)
- Morphine (Arymo ER, MS Contin, Kadian, MorphaBond ER)
- Hydromorphone (Dilaudid, Exalgo)
- Methadone (Dolophine, Methadose)
- Oxymorphone (Opana, Opana ER, Numorphan)
- Tapentadol (Nucynta, Nucynta ER)
Today, dealers on the street may try to sell pain medications claiming they are legitimate prescription drugs. Do not trust them. Many deaths have occurred due to drugs made in illicit labs using dangerous, highly potent opioids like fentanyl or toxic chemicals, to "cut" pharmaceuticals. Illicit drug use has never been more dangerous. But it's not just illegal drugs that have caused the problem.
Learn More: Understanding Opioid (Narcotic) Pain Medications
What is Opioid Use Disorder?
Opioid use disorder (OUD) is a biological disease characterized by a problematic pattern of continued opioid misuse. According to the Diagnostic and Statistical Manual of Mental Disorders (DSM-5), an opioid use disorder is defined as the repeated ocurrence of 2 or more of these 11 problems within a 12-month period. OUD can involve prescription opioids or heroin.
Exhibiting 6 or more of the following items indicates severe opiate dependence:
- Opioid withdrawal symptoms (sweating, shaking, headache, drug craving, nausea, vomiting, stomach cramps, diarrhea, agitation).
- Failing job, school or home responsibilities due to recurrent opioid use.
- Unsuccessful efforts to cut down or control opioid use.
- Opioid use in longer or in larger amounts than anticipated.
- Excessive time spent getting or using the opioid, or recovering from its effects.
- Opioid tolerance.
- Use in physically dangerous situations.
- Craving or strong desire to use opioids.
- Social or interpersonal problems caused by opioid effects.
- Occupational, recreational, or social activities are given up due to opioid use.
- Continued opioid use despite knowledge of the addiction problem.
Dependence is not the same as addiction. Addiction means that a person uses opioids to get high instead of to control pain. Dependence occurs after you have used opioids regularly for a long period of time and your body gets used to how much medicine you take.
MAT: Treatments for Opioid Use Disorder
Patients with Opioid Use Disorder (OUD) can benefit from Medication Assisted Therapy (MAT) for long-term maintenance to prevent relapse after a medically supervised withdrawal (detoxification).
Medication Assisted Therapy (MAT) is a multi-pronged approach that combines approved medications with counseling and support to treat patients with OUD. MAT can help you remain free of drug dependence on opiates (often called narcotics) by blocking the euphoria (high) that is experienced. Methadone, buprenorphine, buprenorphine-naloxone, and naltrexone are all approved for this use.
The first step in treatment is knowing you have a problem and seeking help with detoxification. But it's a known fact: relapse -- the continued use of opioids after opioid withdrawal -- is a common, and dangerous, event. Relapse can occur in up to 90% of patients within the first 1 to 2 months unless treated with medications for maintenance, like MAT.
There is an added safety factor with MAT, too: those who lose their tolerance to opioids (for example, after having gone through a withdrawal program or just quitting on their own) are at risk of fatal overdoses if they return to opioid use, so medical supervision can save lives.
Benefits of Medication Assisted Therapy (MAT)
- Easier Transition Away from Opioid Use: Patients adhering to MAT have reduced opioid withdrawal symptoms and the desire to use opioids, without causing the cycle of highs and lows associated with opioid misuse or abuse.
- It's Safer: Statistics note that patients receiving medication assisted therapy for their opioid use disorder cut their risk of death from all causes in half. These patients have a greater chance of remaining in treatment, as well.
- It's Evidence-Based: Using MAT to help maintain abstinence from heroin or prescription opioids, quite often over at least one year or longer, is a proven method to treat addiction. Some patients may need a lifetime of treatment.
- Social and Group Support: MAT can be more effective when combined with prescribed counseling. After detox, behavioral treatments can help you learn how to avoid opioids, manage cravings, and mend relationships.
Medications Used for Opioid Use Disorder
Medications used for opioid use disorder (OUD) come in many different dose forms: oral solutions and tablets, dissolvable oral films, subdermal (under-the-skin) implants, and long-acting injections.
Generic and brand names include:
- Methadone (Dolophine, Methadose, Methadone Intensol)
- Buprenorphine (Probuphine, Sublocade)
- Buprenorphine-naloxone (Bunavail, Suboxone, Zubsolv)
- Naltrexone (Vivitrol)
First-line maintenance after opioid withdrawal is often started with buprenorphine or methadone. In the U.S., methadone is a schedule II, highly regulated drug, and treatment usually involves going to a registered clinic for your daily dose. Licensed outpatient setting must also provide counseling. Methadone is also available from licensed inpatient hospitals, and any licensed provider can prescribe methadone for up to 72 hours in a supervised setting when deemed necessary and by following federal guidelines (21 CRF1306.07(b)).
Buprenorphine, a schedule III medication, can be given in a doctor's office by certified and trained physicians, which may be more convenient in general.
Naltrexone is not a scheduled drug as it is an antagonist and blocks euphoric actions only (it can cause no "high"). Naltrexone might be an option for you if you are a highly motivated patient with milder symptoms of OUD and you can be reliably followed for medication compliance. However, clinical studies have shown greater effectiveness with methadone or buprenorphine treatment for OUD.
Methadone: The Test of Time
Methadone has been used for over 40 years for opioid use disorder. How does methadone work to ease opioid cravings?
- Methadone is a synthetic mu opioid agonist, which means it acts on the same brain receptors as other opioids, like heroin, morphine or codeine. However, methadone acts more slowly, and has a longer half-life of 8 to 59 hours (a half-life is the amount of time for half of a dose to be eliminated from the body).
- Brand names include: Dolophine, Methadose, Methadone Intensol
- Some people criticize that using an opioid agonist for treatment is just replacing one opioid with another. However, in someone who is opioid tolerant, methadone does not cause the euphoria (the "high") seen with shorter acting drugs, when used appropriately. This is one reason why it is so effective in opioid use disorder.
- Because of the long action (half-life), methadone can accumulate in your body. Your doctor should avoid frequent or rapid dose changes. Rapid dose changes may put you at risk for slowed breathing (respiratory depression), which can be fatal.
- Methadone can prevent withdrawal symptoms for 24 hours, reduce cravings, and lower euphoria if other opioids are used.
Methadone is also approved for the treatment of pain, but should only be prescribed by a healthcare provider familiar with the use of potent opioids for the management of chronic pain.
Methadone maintenance is the first-line treatment for OUD in pregnant women.
Methadone: The Right Dose
Methadone dosing for opioid use disorder (OUD) is not the same as dosing for pain and can be complicated. Dosing is always individualized based on your level of opioid tolerance and the withdrawal symptoms you might be experiencing. Dosing in clinics is usually given as a liquid taken by mouth, diluted with juice or colored water, often with direct observation by personnel.
- If you have not taken opioids for several days you may no longer be opioid-tolerant. Your doctor should use a lower first dose if your tolerance is expected to be low at treatment entry. However, your doctor will dose you adequately over the longer-term to suppress your cravings and block the euphoria of other opioids.
- Dose changes will be frequent over the first few days as your doctor adjusts your dose of methadone. When adjusting methadone doses, it's important to keep in mind that methadone levels will accumulate over the first several days of dosing; deaths have occurred in early treatment due to the cumulative effects.
- Dose increases should proceed slowly based upon on your level of cravings, withdrawal symptoms, and side effects.
- Drug interactions with the cytochrome P450 enzymes (responsible for metabolism and excretion of drugs in your body) are possible with methadone and may affect your required dose; tell your doctor and pharmacist about all of your medications.
- After detoxification and slow upwards titration, clinical stability is typically achieved at doses between 80 to 120 mg/day for maintenance treatment. Doses are usually given once per day.
- It is important that you do not quickly stop methadone. Dose reductions - generally 10% or less of your dose every 10 to 14 days - should also be slow and directed by your doctor.
Learn More: Dosing specifics on methadone detoxification and maintenance.
Methadone: Side Effects and Precautions
Methadone is a strong, schedule II opioid medication and important precautions and side effect warnings should be emphasized:
- Serious and fatal respiratory depression (slowed breathing) can occur; this effect can occur later than the peak effects of methadone due to accumulation of methadone in your body.
- QTc interval prolongation and torsades de pointes (serious heart rhythm disorders) are a possibility. Patients with risk factors for cardiac arrhythmias (heart rhythm changes) should be closely monitored; an electrocardiography (ECG or EKG), a recording your heart electrical activity, may be needed. Inform your provider if you have structural heart disease, history of heart rhythm disorders (arrhythmia), or fainting. Drug interactions can also contribute to prolonging the QT interval.
- Use during pregnancy can cause a withdrawal syndrome in newborn babies (neonatal abstinence syndrome) which can be life-threatening if left untreated.
- Do not drink alcohol while on methadone treatment as it can contribute to the sedative effects of methadone, slowed breathing, and even death.
Other side effects include: drowsiness, sweating, nausea, vomiting, headache, erectile dysfunction, constipation, peripheral edema, and seizures.
- Drug interactions are numerous, including CYP enzymes (in the liver): Review methadone drug interactions of all newly prescribed or discontinued medications with a pharmacist or other healthcare provider. Be sure to check over-the-counter, vitamin, and herbal medications, too.
- Use of methadone products for detoxification and maintenance of opioid withdrawal should be administered in accordance with the federal and state treatment standards, including limitations on unsupervised administration. Your doctor will explain these specifics.
Buprenorphine: An Option to Methadone
Buprenorphine was first FDA-approved in 2002. It is a partial mu-opioid agonist, which means it activates opioid receptors, but with a smaller effect. It also has kappa-opioid receptor antagonist properties. Buorenorphine is a schedule III controlled substance. Dosing for buprenorphine is important to help maintain treatment success and lower rates of treatment drop outs.
Buprenorphine is available as a sublingual (under the tongue) tablet or film, as a buccal film, and as a long-acting implant. It is most commonly taken sublingually, in combination with naloxone, for opioid use disorder (OUD) maintenance.
Brand names for single buprenorphine include:
- Probuphine (buprenorphine), a long-acting implant in place for 6 months.
- Sublocade (buprenorphine), a long-acting injection (depot) formulation, given every 26 days.
- Subutex (buprenorphine) sublingual tablet brand has been discontinued, but generic versions are available.
Naloxone is a full opioid antagonist that blocks opioid receptors in the brain has no euphoric ("high") effects. Naloxone is used in certain buprenorphine products to deter misuse by crushing, dissolving, or injecting the oral formulations. Intravenous naloxone injections would precipitate opiate withdrawal. It has little to no activity when given sublingually.
- Cassipa (buprenorphine and naloxone) is a sublingual film used under the tongue.
- Bunavail (buprenorphine and naloxone) is a buccal film placed against the inside of your cheek.
- Zubsolv (buprenorphine and naloxone) is a sublingual tablet brand.
- Generic buprenorphine and naloxone sublingual tablets or buccals films are also FDA approved.
A Cochrane Review from Mattick and colleagues found that methadone and buprenorphine were equally effective at reducing opioid use and retention in treatment if used in fixed medium or high doses, but fixed doses are not commonly used in clincical practice.
- Compared to methadone, buprenorphine retains fewer people in treatment with flexible, lower doses compared to fixed doses.
- Therefore, methadone is superior to buprenorphine in retaining people in treatment, but methadone and buprenorphine equally suppress illicit opioid use.
Buprenorphine: Side Effects and Precautions
Because buprenorphine is a partial mu-opioid agonist, it can lead to withdrawal in patients who have not stopped using other opioids for long enough. You may need to be in an early state of withdrawal before starting buprenorphine, but once you begin, the buprenorphine will quickly block the withdrawal symptoms by binding to the opioid receptors. Your provider will direct dosing specific for your circumstances.
Most patients will stabilize on a dose of 8 to 16 mg/day of buprenorphine. However, buprenorphine with naloxone is the preferred drug for maintenance treatment, and doses can vary. Only your doctor should adjust your dose. Buprenorphine should be avoided if you have more severe liver disease. The ratio of oral buprenorphine to naloxone is 4:1 with different dose sizes.
Side effects with buprenorphine include:
- Difficulty sleeping
- Stomach upset
- Respiratory depression (slowed breathing)
Overdose with buprenorphine is a risk with intravenous abuse or combined used of benzodiazepines (e.g., Valium, Ativan, Xanax) or alcohol.
- Overdose can lead to respiratory depression (slowed breathing) and possible death.
- Check for buprenorphine drug interactions here.
- As with methadone, buprenorphone should be discontinued slowly under medical supervision.
Probuphine: A Long-Acting Implant
In June 2016 the FDA approved the Probuphine (buprenorphine) subdermal implant, from Braeburn Pharmaceuticals, an added weapon in the treatment of opiate addiction. Diversion and misuse of oral buprenorphine can be problematic, and long-acting implants provide an effective alternative to oral formulations. In addition, patients may benefit from not having to remember to take a daily dose.
Probuphine is the first buprenorphine subdermal implant for the maintenance treatment of opioid dependence:
- Probuphine consists of four, one-inch-long rods that are implanted under the skin to provide a constant, low-level dose of buprenorphine for six months.
- A minor, in-office surgical procedure is used to place the implants.
- It is only used in patients already stabilized on other forms of buprenorphine.
- Probuphine implants are not for use as a pain medication.
In clinical studies, 63% of Probuphine-treated patients had no evidence of illicit opioid use throughout the six months of treatment – similar to the 64% of those who responded to sublingual (under the tongue) buprenorphine alone.
Sublocade: A Long-Acting Injection
Sublocade is injected by a health care professional under the skin (subcutaneously) as a solution, and the delivery system forms a solid deposit (or depot) containing buprenorphine. After initial formation of the depot, buprenorphine is released by the breakdown (biodegradation) of the depot.
A partial opioid agonist formulation, Sublocade is used in patients already on a stable dose of transmucosal buprenorphine for a minimum of 7 days. A long-acting formulation, Sublocade may reduce the burden of taking daily medication for patients in recovery, as well as hinder diversion or abuse of oral buprenorphine.
In research studies, Sublocade-treated patients had more weeks without positive urine tests or self-reports of opioid use compared to the placebo group. Sublocade provided sustained therapeutic plasma levels of buprenorphine over the one-month dosing interval.
Naltrexone and A Long-Acting Option With Vivitrol
Naltrexone is a full opioid antagonist approved for opioid use disorder (OUD) to help prevent relapse. It blocks the effects of opioids (narcotics) and narcotic pain relief medications, including the pain relief and feelings of euphoria ("high"), that can lead to opioid abuse. The 50-mg oral tablets have an effect that lasts 24 to 36 hours.
The Revia brand of buprenorphine, an oral tablet formulation, has been discontinued and is no longer marketed; however, the generic form is still available. Poor adherence has limited the use of oral naltrexone for OUD.
Naltrexone is also available in the US under the brand name Vivitrol which was FDA-approved in 2010. Vivitrol is an extended-release injection used to prevent relapse and may be beneficial for patients who have trouble sticking to the oral treatment regimen. Vivitrol, an intramuscular injection, can help block cravings for one month. It is also used to treat alcoholism.
Learn More: Naltrexone Dosing Specifics
Naltrexone: Side Effects and Warnings
Naltrexone can precipitate withdrawal symptoms if you still use narcotics and should not be used prior to completion of a medically-supervised opioid withdrawal, usually at least 7 to 10 days. Naltrexone may be considered a third-line agent to use in OUD; your doctor may consider it a good option if you are highly motivated and can be monitored closely. It may be appropriate for patients who cannot use opioids for maintenance treatment.
Side effects are infrequent with naltrexone. More common side effects reported with Vivitrol include:
- Stomach cramping
- Headache, dizziness
- Injection site reaction like pain or tenderness
- Anxiety, nervousness
- Trouble sleeping
- Muscle pian
- Nausea or vomiting
Do not to take large amounts of opioid medicines to overcome the Vivitrol block. This can lead to serious injury, coma, or death. Tell your doctor if you take any opioid-containing medicines for pain, cough, or diarrhea.
Naloxone: An Emergency Treatment
Naloxone, also commonly known as Narcan, rapidly reverses the effects of an opioid (narcotic) overdose and is the standard treatment. It is not addictive or considered an opioid itself. A naloxone injection may be administered in a medical emergency.
Naloxone has been available in injection form to reverse the effects of an opioid overdose for more than 40 years. Prior naloxone treatments required administration via a syringe and needle and were most commonly used by trained medical personnel.
- Today, newer naloxone approvals come as nasal sprays called Narcan Nasal and auto-injectors called Evzio to make these life-saving drugs more user-friendly.
- In fact, all states have now passed legislation designed to improve lay-person naloxone access. In all U.S. states, naloxone can be accessed at the pharmacy either through a standing prescription order, pharmacist prescribing or can be dispensed without a prescription, according to the National Alliance of State Pharmacy Associations (NASPA).
If you use opioids, or live in the same household as someone who does, there should be immediate access to naloxone for overdose emergencies. Speak to your pharmacist, doctor, or other healthcare provider about how you can have quick access to naloxone. Learn how naloxone works and how to use it in the event of an overdose emergency. It truly does save lives.
Learn More: Know Your Naloxone: Save a Life
Lucemyra: First Non-Opioid for Opioid Withdrawal Symptoms
In May 2018 the U.S. Food and Drug Administration (FDA) approved Lucemyra (lofexidine hydrochloride) to reduce the severity of opiate withdrawal symptoms and allow a more abrupt discontinuation in adults. It is NOT a treatment for opioid use disorder (OUD) but is approved to help manage OUD. Withdrawal symptoms typically peak the first 5 to 7 days following the last use of an opioid.
- Lucemyra is an oral, selective alpha 2-adrenergic receptor agonist that helps to block the release of norepinephrine, a chemical neurotransmitter in the brain thought to contribute to opiate withdrawal symptoms.
- While Lucemyra may lessen symptoms of withdrawal (such as yawning, pounding heartbeats, anxiety, nausea, stomach cramps, watery eyes, feeling cold, stomach pain, and sleep problems), it may not completely reverse them and can only be used for 14 days.
- Opioid withdrawal can occur both in patients who use prescribed opioids appropriately and in OUD.
Lucemyra is manufactured by US WorldMeds.
What's the US Doing to Address the Opioid Epidemic?
The U.S. Department of Health and Human Services’ Five-Point Strategy to Combat the Opioid Crisis is a specific federal response to address this crisis.
The Five-Point Strategy is:
- Improving access to treatment and recovery services.
- Promoting use of overdose-reversing drugs, such as naloxone.
- Strengthening our understanding of the epidemic through better public health surveillance.
- Providing support for cutting-edge research on pain and addiction.
- Advancing better practices for pain management.
In addition, the National Institutes of Health (NIH) is exploring formal partnerships with pharmaceutical companies and academic research centers to develop:
- Safe, effective, non-addictive strategies to manage chronic pain.
- New, innovative medications and technologies to treat opioid use disorders.
- Improved overdose prevention and reversal interventions to save lives and support recovery.
What Can You Do About the Opioid Epidemic?
If you think you are addicted to opioids, or know someone who is, speak to a healthcare provider and know that there are steps that can be taken. The first step is taking charge of the situation to get help. It's not easy, but if you follow these recommendations you will be on your way:
- Commit to quitting the use of opioids: if you are ready to take the steps to control your behavior, the path will be easier.
- Get help from a trusted healthcare professional. Your doctor may be able to prescribe medicine that will help to lessen the cravings for the opioid drug, and lead you through a treatment plan.
- Get support through addiction counseling and talk with others. Organizations in the US are committed to helping people who have problematic opioid use. They have experience in helping people get their lives and relationships back on track and putting opioid use in their past. Ask your family, friends and partners for support, too.
Finished: Opioid Use Disorder: These Treatments Are Available, Now
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