naltrexone (ReVia, Trexan, Vivitrol, Vivitrex)
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Introduction
Tradenames: ReVia, Trexan, Vivitrol. Vivitrex.
Indications
- alcohol dependence in conjunction with behavior modification
- treatment of alcoholism
- adjunct to the maintenance of an opioid-free state in detoxified individuals (prevention of opiate abuse)
- constipation due to opiates
Contraindications
- patients on scheduled or PRN opiates
- opiate withdrawal
- hepatitis or liver failure (cirrhosis)[8]
- patient must be abstinent from alcohol (GRS11)[4]
- may be started despite patient continuing to drink (NCBI)[9]
Dosage
- 50 mg PO QD
- doses up to 150 mg QD have been used
- Vivatrol 380 mg IM monthly[5][6] for alcohol dependence
- do NOT give until the patient is opioid-free for 7-10 days
Tabs: 50 mg.
Pharmacokinetics
- well absorbed orally
- extensive 1st pass metabolism
- 5-40% of oral dose reaches systemic circulation
- onset of action is 30 minutes
- duration is dose-dependent
- metabolized by liver
- eliminated in urine
elimination via liver
elimination via kidney
Monitor
liver function tests[4] ID card/medical alert bracelet for proper pain management in case of emergency[6]
Adverse effects
- common (> 10%)
- less common (1-10%)
- uncommon (< 1%)
- other
- tremor
- diarrhea
- fatigue
- hepatotoxicity
- myalgias
- pain, swelling, tenderness, induration, bruising, pruritus, or redness at the injection site that does not improve or worsens within 2 weeks[7]
Mechanism of action
- competitive mu opioid receptor, kappa opioid receptor & sigma opioid receptor antagonist
- it is though that alcohol stimulates release of endogenous opioids
More general terms
More specific terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Jump up to: 4.0 4.1 4.2 Geriatrics Review Syllabus, American Geriatrics Society, 5th edition, 2002-2004
Geriatric Review Syllabus, 11th edition (GRS11) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2022 - ↑ Jump up to: 5.0 5.1 Journal Watch 25(10):83, 2005 Garbutt JC, Kranzler HR, O'Malley SS, Gastfriend DR, Pettinati HM, Silverman BL, Loewy JW, Ehrich EW; Vivitrex Study Group. Efficacy and tolerability of long-acting injectable naltrexone for alcohol dependence: a randomized controlled trial. JAMA. 2005 Apr 6;293(13):1617-25. Erratum in: JAMA. 2005 Apr 27;293(16):1978. PMID: https://www.ncbi.nlm.nih.gov/pubmed/15811981
- ↑ Jump up to: 6.0 6.1 6.2 Prescriber's Letter 13(5): 2006 New Drug: Vivitrol (Naltrexone Extended-Release Injectable Suspension) Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220607&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Jump up to: 7.0 7.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2008/safety08.htm#naltrexone
FDA MedWatch Vivitrol (naltrexone for extended-release injectable suspension): Medication Guide Required for Patients http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm210755.htm - ↑ Jump up to: 8.0 8.1 Medical Knowledge Self Assessment Program (MKSAP) 14, American College of Physicians, Philadelphia 2006
- ↑ Jump up to: 9.0 9.1 NCBI Bookshelf Incorporating Alcohol Pharmacotherapies Into Medical Practice. Chapter 4 - Oral Naltrexone https://www.ncbi.nlm.nih.gov/books/NBK64042/#:~:text=Patients%20may%20experience%20fewer%20medication,if%20they%20are%20actively%20drinking.
- ↑ Lee JD, Friedmann PD, Kinlock TW et al. Extended-release naltrexone to prevent opioid relapse in Criminal Justice Offenders. N Engl J Med 2016 Mar 31; 374:1232 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27028913 <Internet> http://www.nejm.org/doi/10.1056/NEJMoa1505409