Injectable Naltrexone for Smoking Cessation

By: Jacqueline Meaney, PharmD Candidate c/o 2015, University at Buffalo: School of Pharmacy and Pharmaceutical Sciences

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Extended release naltrexone (XR-NTX), marketed as once-monthly IM Vivitrol^®, is currently FDA approved for use in treating both alcohol and opiate dependence. Naltrexone is a mu-opioid receptor antagonist that blocks the euphoric effect of heroin and prescription opioids. Naltrexone may be useful as a tool for smoking cessation because previous studies have demonstrated a link between opioids and nicotine. Cigarette smoking continues to be the leading cause of preventable death in the United States, and as such, naltrexone may provide an additional option for patients who want to quit smoking or for patients who need an adjunct to their current smoking cessation regimen.²

Oral naltrexone has been studied for smoking cessation and has yielded mixed results.^2-14 Oral naltrexone was not shown to be effective for nicotine dependence in patients receiving naltrexone for alcohol addicion,¹⁴ and was shown to be no more effective than placebo when used in combination with the nicotine patch.⁵ In contrast, other studies have demonstrated the efficacy of oral naltrexone when used with and without the nicotine patch,¹¹ and an additional study found that oral naltrexone was only effective for nicotine dependence in women.⁸

Compared to treatment with oral naltrexone, treatment with XR-NTX has shown increased rates of adherence, which may result in XR-NTX being effective as a smoking cessation aid.^15,16 In addition, XR-NTX achieves greater cumulative plasma concentrations than oral naltrexone – the AUC of XR-NTX after multiple dose administration is 160 ^ngxh/_mL, while that of oral naltrexone is only 35 ^ngxh/_mL.¹⁷

As a result, oral naltrexone may not provide high enough plasma levels or enough exposure to naltrexone for the drug to be effective as a smoking cessation aid. It is therefore possible that the increase in the AUC of naltrexone when administered as XR-NTX may result in XR-NTX being more effective for smoking cessation.¹⁸

Case studies have shown that patients who were chronic cigarette smokers had decreased cravings for nicotine following initiation of XR-NTX therapy. In addition, some patients stopped smoking entirely when treated with XR-NTX combined with nicotine replacement therapy and smoking cessation classes.¹⁹ Increased exposure to naltrexone and increased compliance to the naltrexone regimen may support the use of XR-NTX for smoking cessation.^{18, 21} XR-NTX has not yet been studied for the treatment of nicotine dependence, which may be a possible use for this medication.

 

SOURCES:

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[pubmed_related keyword1=”naloxone” keyword2=”smoking” keyword3=”cessation”]