Opioids Medications: Naltrexone/Vivitrol, Buprenorphine, Sublocade, and Methadone.

 

1- What are the most important things to know before starting Naltrexone/Vivitrol?

Naltrexone is an “antagonist.” It binds to the mu-opioid receptor and blocks opioids such as heroin to get onto the receptor preventing the opioid to work.

Naltrexone is a daily pill medication while Vivitrol is Naltrexone in a slow-release injection form that lasts 30 days. Vivitrol tends to produce better results because it isn’t a daily medication. Side effects to consider:  Most common GI system side effects (Nausea, abdominal pain, etc), CNS, Central nervous system (Feeling tired, restless, insomnia). The Vivitrol injection can cause swelling and pain at the injection site. There is a black box warning regarding possible liver injury so most prescribers request baseline liver function labs although the data showing liver toxicity may be less than once thought. When starting this medication a patient must wait about 1 week after ingesting/injecting any opioid, otherwise, the medication may lead to terrible side effects from precipitated withdrawal. In my experience, this medication is well tolerated and people state it helps with cravings. The data shows Vivitrol doubles sobriety rates. 

2- What are the most important things to know before starting Buprenorphine (e.g Suboxone)?

Buprenorphine is a “partial agonist.” It binds to the mu-opioid receptor.  It has a ceiling effect so taking a higher dose shouldn’t cause more symptoms including respiratory depression. There is a daily pill version (such as Suboxone) and an Injectable one a monthly version (Sublocade). The medication has similar side effects to all opioids such as itch, constipation, dry mouth, and urinary reception, but it has a ceiling effect so it should be safer.  It does have a black box warning to not mix with respiratory depressants such as benzodiazepine/alcohol because increased respiratory depression may be fatal. The medicine does show a doubling of the sobriety rate and decreasing cravings. The data shows Suboxone doubles sobriety rates. 

I want patients to realize before starting the commitment that is expected when starting Suboxone. There is debate on how long the commitment should be (2-5 years to a lifetime). You can’t just stop Suboxone quickly without getting withdrawal symptoms. 

3- What are the most important things to know before starting Sublocade? 

Sublocade is the injectable version of Suboxone i.e. the buprenorphine product discussed earlier. Because it is the same compound as above (question 2) it has the same side effects. It has the advantage of being a monthly injection so one doesn’t need to worry about taking it daily. Prescribers like it because they don’t need to worry about patients not taking their Suboxone.  It does have the disadvantage of not being able to control the dose, and if you have a side effect on the higher dose there isn’t really much control over how much medication you’re being given.  Furthermore, since it’s an injection it can cause pain at the injection site. 

4- What are the most important things to know before starting Methadone?

Methadone is an “agonist” binding to the opioid receptor and does its effect. Because it acts as an agonist,  It is more “dangerous” when compared to Naltrexone and/or Buprenorphine.  Methadone has a black-box warning for Respiratory Depression.  Do not take Benzodiazepines or alcohol at the same time as  Methadone since it is a lethal combination. Furthermore, Methadone may cause an irregular heartbeat by prolonging QT. All this means is before starting you should have an EKG. It also has all the other normal side effects of an opioid such as dry mouth, constipation, and urinary retention. 

I want patients to realize before starting I like Suboxone. If you start methadone and stop suddenly it will lead to withdrawal symptoms. Furthermore, the drug is highly regulated by the federal government, and each state and each center may have its own rules regarding what must be done for a prescription. 

5- Which one do you choose?

There are different opinions regarding which medication is best. It depends on the person. I like recommending the medications in a stepwise approach. I like starting with Naltrexone. If that doesn’t work I then consider prescribing Buprenorphine, and if that doesn’t work I encourage the patient to consider Methadone. There are several reasons I like prescribing it this way, however, one major reason is that the Buprenorphine and Methadone are a bigger commitment.  If one suddenly stops, it would induce withdrawal. 

Which medications work best may depend on where someone is in their sobriety. Perhaps with someone with a lifelong difficulty, more potent methadone is a good option.  Furthermore, if the pain is an issue suboxone or methadone may be better than naltrexone. There is no right answer. 

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