Naltrexone

Naltrexone is used to treat narcotic drug or alcohol addiction.

Product dosage: 50mg
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Synonyms Naltrexone oral Revia Nal trex own

Naltrexone is a potent opioid antagonist medication that represents a critical advancement in the management of substance use disorders. As a non-addictive, evidence-based pharmacotherapy, it works by competitively binding to opioid receptors in the brain, effectively blocking the euphoric and sedative effects of exogenous opioids. Its utility extends to alcohol use disorder, where its mechanism modulates the reinforcing effects of alcohol consumption. This product card provides a comprehensive, expert-level overview of naltrexone, detailing its pharmacological profile, clinical applications, and essential safety information for healthcare professionals.

Features

• Pharmacological Class: Pure opioid receptor antagonist.
• Available Formulations: Oral tablets (50 mg standard) and extended-release intramuscular injectable suspension (380 mg/vial).
• Mechanism of Action: Competitive binding at mu-opioid receptors, preventing agonist effects.
• Bioavailability: Oral: 5–40% (extensive first-pass metabolism); IM: Provides sustained release over approximately 4 weeks.
• Half-life: Oral: 4–13 hours; IM (active metabolite, 6-β-naltrexol): 5–10 days.
• Metabolism: Primarily hepatic, via dihydrodiol dehydrogenase.
• Excretion: Primarily renal.

Benefits

• Blocks Opioid Effects: Prevents the euphoria and high associated with opioid use, thereby reducing cravings and supporting abstinence in opioid-dependent patients.
• Reduces Alcohol Craving and Relapse: Significantly decreases the rewarding effects of alcohol, helping patients maintain sobriety and reduce heavy drinking days.
• Non-Addictive Pharmacotherapy: Lacks the abuse potential and physiological dependence associated with agonist therapies like methadone or buprenorphine.
• Flexible Administration Options: Offers both daily oral dosing for immediate initiation and monthly injections to enhance adherence and provide continuous receptor blockade.
• Supports Comprehensive Treatment: Serves as a pharmacological cornerstone within a broader treatment plan that includes counseling and behavioral therapies.
• Facilitates Long-Term Recovery: By mitigating the risk of relapse through receptor blockade, it provides a stable foundation for sustained recovery.

Common use

Naltrexone is FDA-approved for two primary indications. First, for the treatment of opioid use disorder (OUD) in patients who have undergone complete opioid detoxification. It is used to prevent relapse to opioid use. Second, for the treatment of alcohol use disorder (AUD) to reduce alcohol consumption, prevent relapse to heavy drinking, and support abstinence. It is most effective when used as part of a comprehensive treatment program that includes psychosocial support. Off-label, it is sometimes investigated for other compulsive behaviors and certain autoimmune conditions at very low doses (Low Dose Naltrexone or LDN), though these uses lack robust FDA approval.

Dosage and direction

For Opioid Use Disorder:

• Initiation: Treatment must NOT be initiated until the patient is completely opioid-free. A naloxone challenge test or verification of a negative urine toxicology screen is mandatory to avoid precipitating severe withdrawal. A minimum of 7–10 days after last short-acting opioid use (e.g., heroin) and 10–14 days for long-acting opioids (e.g., methadone) is typically required.
• Oral Tablets: The recommended maintenance dose is 50 mg once daily. Alternative dosing schedules, such as 100 mg every other day or 150 mg every third day, may be used to improve adherence, though daily dosing is standard.
• Extended-Release Injection (Vivitrol®): 380 mg is administered via intramuscular gluteal injection every 4 weeks or once monthly. Must be administered by a healthcare professional.

For Alcohol Use Disorder:

• Initiation: It is advisable to initiate treatment after the patient has achieved abstinence and is no longer experiencing acute alcohol withdrawal symptoms.
• Oral Tablets: The recommended dose is 50 mg once daily.
• Extended-Release Injection (Vivitrol®): 380 mg administered via intramuscular gluteal injection every 4 weeks.

General Direction: Oral tablets can be taken with or without food. Adherence to the prescribed regimen is critical for efficacy, particularly with the oral formulation.

Precautions

• Precipitated Withdrawal: The most critical precaution. Administering naltrexone to an opioid-dependent patient will precipitate acute, and potentially severe, withdrawal syndrome. Meticulous patient screening and verification of opioid-free status are imperative.
• Hepatotoxicity: Although associated with dose-related hepatocellular injury at high doses (≥ 300 mg/day), this is rare at recommended doses. Nonetheless, baseline and periodic monitoring of liver function tests (transaminases) is advised.
• Depression and Suicidality: As with many medications used in addiction treatment, patients should be monitored for the emergence or worsening of depression, suicidal ideation, or suicidal behavior.
• Opioid Tolerance: Patients will have a reduced tolerance to opioids. If they relapse and use opioids at their previous dose after a period of naltrexone blockade, they are at high risk of life-threatening overdose and respiratory depression.
• Injection Site Reactions: The intramuscular injection can cause pain, tenderness, induration, swelling, erythema, bruising, or pruritus. Proper injection technique is necessary to minimize these effects.
• Eosinophilic Pneumonia: There have been rare reports associated with the injectable formulation.

Contraindications

• Patients receiving opioid analgesics or currently dependent on opioids (including those in acute withdrawal).
• Patients with a failed naloxone challenge test or positive urine screen for opioids.
• Patients with acute hepatitis or liver failure.
• Known hypersensitivity to naltrexone or any component of the formulation (e.g., polylactide-co-glycolide (PLG) in the injectable suspension, carboxymethylcellulose sodium).

Possible side effect

Common side effects are often transient and may include:

• Nausea (most common with oral formulation)
• Headache
• Dizziness
• Insomnia
• Anxiety
• Nervousness
• Abdominal pain/cramps
• Joint and muscle pain
• Injectable-specific: Injection site reactions (pain, induration, swelling, erythema, bruising)

Less common but more serious side effects require medical attention:

• Signs of hepatotoxicity (e.g., abdominal pain lasting more than a few days, white bowel movements, dark urine, yellowing of the eyes)
• Severe depression or suicidal thoughts
• Signs of pneumonia (e.g., shortness of breath, wheezing, cough, chest pain)
• Allergic reactions (e.g., rash, hives, swelling, difficulty breathing)

Drug interaction

• Opioid Analgesics: Naltrexone will block the therapeutic effects of opioid pain medications (e.g., morphine, oxycodone, hydrocodone, fentanyl). In a emergency pain situation, management requires significantly higher doses of opioids under close supervision in a controlled medical setting, with awareness of the risk of respiratory depression once the naltrexone blockade is overcome.
• Opioid-Containing Medications: Will also block the effects of opioid agonists found in some antidiarrheal (e.g., loperamide) and cough suppressant medications.
• Thioridazine: Concomitant use has been reported to cause lethargy and somnolence.
• Hepatotoxic Drugs: Caution is advised when co-administering with other medications known to have hepatotoxic potential.

Missed dose

• Oral Tablets: If a dose is missed, it should be taken as soon as possible. However, if it is almost time for the next dose, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed one.
• Extended-Release Injection: The next injection should be administered as soon as possible. A patient who is late for their injection may be vulnerable to opioid or alcohol use, as the receptor blockade may wane.

Overdose

Naltrexone alone in massive overdose has not been associated with serious systemic sequelae or fatalities. The primary concern in overdose is the potential for dose-dependent hepatotoxicity. There is no specific antidote. Management involves discontinuation of the drug, providing symptomatic and supportive care, with close monitoring of liver function. However, a patient attempting to overcome the receptor blockade by consuming large amounts of opioids is at extreme risk of profound respiratory depression, coma, and death.

Storage

• Oral Tablets: Store at room temperature (20°–25°C or 68°–77°F) in a tight, light-resistant container. Keep out of reach of children.
• Extended-Release Injection (Vivitrol®): The kit must be refrigerated (2°–8°C or 36°–46°F) in an upright position. Do not freeze. The product may be kept at room temperature for no more than 7 days prior to administration. Once mixed, the suspension must be administered promptly.

Disclaimer

This information is intended for educational and informational purposes only for healthcare professionals and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of a qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. Full prescribing information, including Boxed Warnings, should be reviewed prior to initiating therapy.

Reviews

• “Naltrexone, particularly in its long-acting injectable form, has been a game-changer in my addiction medicine practice. It removes the daily burden of pill-taking and provides a tangible ‘safety net’ for patients highly motivated for recovery.” – Addiction Psychiatrist, 15 years experience.
• “The key to success with naltrexone is proper patient selection and education. Ensuring complete detoxification first is non-negotiable. For the right patient, it’s an incredibly powerful tool that supports true autonomy in recovery.” – Certified Addiction Registered Nurse, outpatient clinic.
• “As a researcher in the field, the data for naltrexone’s efficacy in reducing heavy drinking days is robust. It’s underutilized in primary care settings for AUD where it could make a significant public health impact.” – PhD, Clinical Pharmacology.
• “The monthly injection model drastically improves adherence compared to daily tablets. While the injection is painful for some, most of my patients find the trade-off for a month of peace of mind to be well worth it.” – Family Medicine Physician, MAT provider.