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What Medications are Available for Opioid Dependence?
Buprenorphine/Naloxone Commonly known as Suboxone, Buprenorphine/Naloxone (Bup/Nx) is a prescription opioid medication that is used to treat opioid dependence. At the correct dose, buprenorphine may suppress cravings and withdrawal symptoms and block the effects of other opioids. Buprenorphine is not new. It was first patented in 1969 and has been used in the U.S. to treat pain and in Europe to treat pain and opioid addiction for decades. Buprenorphine is a semi-synthetic opioid and is a partial agonist.
Opioid Agonists are drugs that cause an opioid effect; i.e., heroin, oxycodone, hydrocodone, and methadone. Opioid Antagonists are drugs that block and reverse the effects of agonist drugs. Narcan® is an antagonist and is used to reverse heroin overdoses. Buprenorphine can act as both an agonist and antagonist. It attaches to the opioid receptors but only activates them partially, enough to suppress withdrawal and cravings, but not enough to cause extreme euphoria in opioid-tolerant patients.
When all available receptors are occupied with buprenorphine, no additional opioid effect is produced by taking more. This is called the ‘ceiling effect’. The antagonist property of the medication expels, replaces and blocks other opioids from the opioid receptor sites. Therefore, if the patient decides to misuse opioid drugs after taking buprenorphine, the effects can be blocked, depending on the dosage.
Alternately, if buprenorphine is taken too soon after other opioids, by an opioid-physically dependent patient, the buprenorphine can precipitate withdrawal. The ceiling effect, blocking ability, and the possibility of precipitating withdrawal contributes to buprenorphine having a favorable safety profile and helps lower the risk of overdose and misuse.
In October 2002 the FDA approved the first two prescription Buprenorphine medications for the treatment of opioid addiction; Subutex®* (buprenorphine) and Suboxone®* (buprenorphine/naloxone). Since 2009 the FDA approved generic Bup and Bup/Nx sublingual tablets, the brand-name Bup/Nx sublingual tablet Zubsolv®* and the Bup/Nx buccal film Bunavail™*. Both Suboxone and Subutex tablets were discontinued and replaced with Suboxone Film® – a Bup/Nx sublingual film.
The purpose of the addition of naloxone is to reduce the risk of misuse by injection. If the Bup/Nx combination is injected, the naloxone will help cause immediate withdrawal symptoms in opioid-physically dependent people. However, naloxone is poorly absorbed sublingually. Therefore, when taken as directed, very little naloxone enters the blood. Normally, patients are unaffected by the presence of it, and it is considered clinically insignificant.
*For more information on Bup/Nx go to www.naabt.org
Methadone Maintenance: Methadone has been used for decades to treat people who are addicted to heroin and narcotic pain medicines. When taken as prescribed, it is safe and effective. It allows people to recover from their addiction and to reclaim active and meaningful lives.
Individuals taking methadone to treat opioid addiction must receive the medication under the supervision of a physician. Initially, a person on the “clinic” must attend on a daily basis and receive their dosage of methadone in the presence of nursing staff. After a period of stability (based on progress and proven, consistent compliance with the medication dosage and negative urine drug screens or oral swabs), individuals may be allowed to take methadone at home between program visits. By law, methadone can only be dispensed through an approved opioid treatment program (OTP), which are highly regulated by the state and federal government.
The length of time in methadone treatment varies from person to person. According to the National Institute on Drug Abuse publication, the length of methadone treatment should be a minimum of 12 months. Some individuals may require treatment for years. Even if an individual feels that they are ready to stop methadone treatment, it must be stopped gradually to prevent withdrawal. Such a decision should be supervised by a doctor.
As with all medications used in medication-assisted treatment (MAT) methadone is to be prescribed as part of a comprehensive treatment plan that includes counseling and participation in social support programs.
Naltrexone for opioid AND alcohol use disorders: Naltrexone is a medication approved by the Food and Drug Administration (FDA) to treat opioid and alcohol use disorders. It comes in a pill form or as an injectable. The pill form of naltrexone (ReVia, Depade) can be taken at 50 mg once per day. The injectable extended-release form of the drug (Vivitrol) is administered at 380 mg intramuscular once a month. Naltrexone works by blocking the euphoric and sedative effects of drugs such as heroin and alcohol. It works differently in the body than buprenorphine and methadone, which activate opioid receptors in the body that suppress cravings. If a person relapses and uses the problem drug, naltrexone prevents the feeling of getting high. People using naltrexone should not use any other opioids or illicit drugs; drink alcohol; or take sedatives, tranquilizers, or other drugs.
Naltrexone for opioid use disorders: Naltrexone can be prescribed by any health care provider who is licensed to prescribe medications. It works by binding and blocking the opioid receptors in the brain and reduces cravings. It also decreases reactivity to drug-conditioned cues. To reduce the risk of precipitated withdrawal, individuals are warned to abstain from illegal opioids and opioid medication for a minimum of 7-10 days before starting naltrexone. If switching from methadone to naltrexone, the patient has to be completely withdrawn from the opioids. Individuals on naltrexone may have reduced tolerance to opioids and may be unaware of their potential sensitivity to the same, or lower, doses of opioids that they used to take. If individuals who are treated with naltrexone relapse after a period of abstinence, it is possible that the dosage of opioid that was previously used may have life-threatening consequences, including respiratory arrest and circulatory collapse.
Naltrexone for alcohol use disorders: When used as a treatment for alcohol dependence, naltrexone blocks the euphoric effects and feelings of intoxication. This allows people with alcohol addiction to reduce their drinking behaviors enough to remain motivated to stay in treatment and avoid relapses. Naltrexone is not addictive nor does it react adversely with alcohol. Long-term naltrexone therapy extending beyond three months is considered most effective by researchers, and therapy may also be used indefinitely.