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
| Parameter | Detail |
| Route | Intramuscular injection (deltoid or gluteal) |
| Dose | 380 mg per injection |
| Absorption | Gradual release from biodegradable microspheres; peak plasma concentration occurs 7–10 days post‑dose |
| Bioavailability | ~50–70 % (systemic) |
| Half‑life | 4–5 days (steady state achieved 3–4 weeks) |
| Metabolism | Hepatic glucuronidation (UGT2B7, UGT1A9) |
| Excretion | Renal (≈30 % unchanged; remainder as glucuronide conjugates) |
| Food Effect | No clinically significant impact |
| Key PK Notes | No 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, swelling | Hepatotoxicity (ALT/AST ↑, jaundice) |
| Headache, dizziness | Severe withdrawal symptoms (if improper induction) |
| Nausea, fatigue, insomnia | Major depressive episodes, suicidal ideation |
| Mood changes, anxiety | Severe hypersensitivity reactions |
| Gastrointestinal upset | Respiratory 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.
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• *This card integrates pharmacologic fundamentals with practical prescribing cues to support evidence‑based practice for healthcare professionals and medical students.*