Vivitrol

Vivitrol

Generic Name

Vivitrol

Mechanism

  • Opioid antagonist: Binds irreversibly to μ‑opioid receptors, blocking the effect of endogenous and exogenous opioids, preventing withdrawal and reducing the rewarding properties of opiates.
  • Alcohol craving modulation: Inhibits the activation of opioid‑dependent neuropeptide Y and endogenous opioid release in the nucleus accumbens, thereby attenuating the reinforcing effects of alcohol.
  • Prolonged receptor occupancy: The microsphere matrix provides a slow, continuous release that maintains therapeutic plasma concentrations for ~30 days.

Pharmacokinetics

ParameterDetail
RouteIntramuscular injection (deltoid or gluteal)
Dose380 mg per injection
AbsorptionGradual release from biodegradable microspheres; peak plasma concentration occurs 7–10 days post‑dose
Bioavailability~50–70 % (systemic)
Half‑life4–5 days (steady state achieved 3–4 weeks)
MetabolismHepatic glucuronidation (UGT2B7, UGT1A9)
ExcretionRenal (≈30 % unchanged; remainder as glucuronide conjugates)
Food EffectNo clinically significant impact
Key PK NotesNo dose adjustment needed for renal insufficiency; reduced clearance in severe hepatic impairment

Indications

  • Opioid use disorder – maintenance therapy after induction onto oral naltrexone or after completion of opioid detoxification.
  • Alcohol use disorder – maintenance therapy for reducing heavy drinking episodes in patients stabilized on psychosocial support.
  • Adjunct to psychotherapy – often combined with Cognitive‑Behavioral Therapy or Motivational Interviewing.

Contraindications

  • Acute or chronic hepatitis, cirrhosis, or liver failure.
  • Known hypersensitivity to naltrexone, ethanol, or any component of the formulation.
  • Ongoing opioid use: May precipitate severe withdrawal; ensure opioid detox (≥24–48 h opioid‑free) before first dose.
  • Use with other opioid antagonists (e.g., naloxone) can induce withdrawal.
  • Severe psychiatric instability: Monitor for depression, anxiety, or suicidal ideation, especially in AUD patients.

Warnings:
• Risk of hepatotoxicity (rare but potentially fatal).
• Possible precipitated withdrawal in patients who have recently used opioids.
• Not approved for acute opioid overdose or for patients who need rapid pain control.

Dosing

  • Initial dose: 380 mg IM after confirming opioid withdrawal (e.g., 8‑score on Clinical Opiate Withdrawal Scale) or, for AUD, after a 24‑hour alcohol‑free period.
  • Maintenance: 380 mg IM every 30 days; can be extended to 60 days if patient remains stable and adherent.
  • Missed dose: If ≤7 days missed, administer next injection. If >7 days missed, re‑induce opioid withdrawal before next dose.
  • Premedication: Not required; consider local anesthetic for injection site discomfort.
  • Co‑administered meds: Avoid concomitant opioid analgesics or medications that induce CYP3A4 (may reduce efficacy).

Adverse Effects

Common (≥5 %)Serious (rare)
Injection‑site pain, erythema, swellingHepatotoxicity (ALT/AST ↑, jaundice)
Headache, dizzinessSevere withdrawal symptoms (if improper induction)
Nausea, fatigue, insomniaMajor depressive episodes, suicidal ideation
Mood changes, anxietySevere hypersensitivity reactions
Gastrointestinal upsetRespiratory depression (rare)

Note: Monitor for signs of liver injury and counsel patients to seek immediate medical attention if jaundice or severe abdominal pain develops.

Monitoring

  • Liver function tests (ALT, AST, bilirubin): baseline; then at 1, 2, 3, 4, 6, and 12 months.
  • Mental status & depression scales (PHQ‑9) during treatment.
  • Opioid withdrawal assessment: use COWS before first injection.
  • Injection site inspection at each visit.
  • Alcohol use monitoring (self‑report, breathalyzer) for AUD patients.
  • Blood pressure & heart rate if patient has cardiovascular comorbidities.

Clinical Pearls

  • Pre‑dose screening is critical: Verify complete opioid withdrawal before the first injection; consider a naloxone test dose if uncertain.
  • Combination therapy outperforms monotherapy: Pair Vivitrol with psychosocial interventions for maximal remission rates.
  • Adherence check: Since missed injections (>7 days) can lead to lapse, reinforce patient education on monthly clinic visits.
  • Avoid concurrent opioids: Even small doses (e.g., tramadol) can precipitate withdrawal; coordinate pain management plans.
  • Use in AUD with caution: Patients with severe liver disease or active depression require closer surveillance; consider alternative agents (e.g., acamprosate).
  • Pregnancy & lactation: Not studied; avoid in pregnant or breastfeeding women unless benefits outweigh risks.
  • Storage: Keep injectable vial at 2–8 °C; after reconstitution, keep refrigerated and use within 30 days.

--
• *This card integrates pharmacologic fundamentals with practical prescribing cues to support evidence‑based practice for healthcare professionals and medical students.*

Medical & AI Content Disclaimers
Medical Disclaimer: Medical definitions are provided for educational purposes and should not replace professional medical advice, diagnosis, or treatment.

AI Content Disclaimer: Some definitions may be AI-generated and may contain inaccuracies. Always verify with authoritative medical references.

Scroll to Top