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naltrexone (ReVia, Trexan, Vivitrol, Vivitrex)

Tradenames: ReVia, Trexan, Vivitrol. Vivitrex. Indication: - 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: 1) patients on scheduled or PRN opiates 2) opiate withdrawal 3) hepatitis or liver failure (cirrhosis) [8] 4) patient must be abstinent from alcohol (GRS11) [4] 5) may be started despite patient continuing to drink (NCBI) [9] Dosage: 1) 50 mg PO QD 2) doses up to 150 mg QD have been used 3) Vivatrol 380 mg IM monthly [5,6] for alcohol dependence 4) do NOT give until the patient is opioid-free for 7-10 days Tabs: 50 mg. Pharmacokinetics: 1) well absorbed orally 2) extensive 1st pass metabolism 3) 5-40% of oral dose reaches systemic circulation 4) onset of action is 30 minutes 5) duration is dose-dependent 6) metabolized by liver 7) eliminated in urine Monitor: liver function tests [4] ID card/medical alert bracelet for proper pain management in case of emergency [6] Adverse effects: 1) common (> 10%) - abdominal cramping, insomnia, nervousness, headache, arthralgias, nausea/vomiting 2) less common (1-10%) - rash, polydipsia, dizziness, anorexia, sneezing 3) uncommon (< 1%) - insomnia, irritability, anxiety, thrombocytopenia, agranulocytosis, hemolytic anemia, blurred vision narcotic withdrawal 4) 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: 1) competitive mu opioid receptor, kappa opioid receptor & sigma opioid receptor antagonist 2) it is though that alcohol stimulates release of endogenous opioids

Specific

methylnaltrexone (Relistor)

General

opioid receptor antagonist or narcotic antagonist

Properties

INHIBITS: opiate MISC-INFO: elimination route LIVER KIDNEY pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. 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
  5. 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: 15811981
  6. Prescriber's Letter 13(5): 2006 New Drug: Vivitrol (Naltrexone Extended-Release Injectable Suspension) Detail-Document#: 220607 (subscription needed) http://www.prescribersletter.com
  7. 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
  8. Medical Knowledge Self Assessment Program (MKSAP) 14, American College of Physicians, Philadelphia 2006
  9. 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.
  10. 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 PMID: 27028913 http://www.nejm.org/doi/10.1056/NEJMoa1505409

Component-of

bupropion/naltrexone (Contrave)