Naltrexone

Treatment with naltrexone for extended-release injectable suspension should be part of a comprehensive management program that includes psychosocial support. Naltrexone for extended-release injectable suspension contains naltrexone, an opioid antagonist, and is indicated for the treatment of alcohol dependence in patients who are able to abstain from alcohol in an outpatient setting prior to initiation of treatment with naltrexone for extended-release injectable suspension. Patients should not be actively drinking at the time of initial naltrexone for extended-release injectable suspension administration (1.1) . …

• Naltrexone for extended-release injectable suspension must be prepared and administered by a healthcare provider
• Prior to initiating naltrexone for extended-release injectable suspension, an opioid-free duration of a minimum of 7–10 days is recommended for patients, to avoid precipitation of opioid withdrawal that may be severe enough to require hospitalization
• The recommended dose of naltrexone for extended-release injectable suspension is 380 mg delivered intramuscularly (deep) as a gluteal injection, every 4 weeks or once a month, alternating buttocks for each subsequent injection, using the carton components provided
• Naltrexone for extended-release injectable suspension must ONLY be administered as a deep intramuscular gluteal injection
• See Full Prescribing Information for complete Directions for Use
• Important Dosage and Administration Information Naltrexone for extended-release injectable suspension must be prepared and administered by a healthcare provider
• Naltrexone for extended-release injectable suspension must ONLY be administered as a deep intramuscular gluteal injection
• Parenteral products should be visually inspected for particulate matter and discoloration prior to administration whenever solution and container permit
• A properly mixed suspension will be milky white, will not contain clumps, and will move freely down the wall of the vial [see Dosage and Administration ] . …

Naltrexone for extended-release injectable suspension is an off-white to light tan powder for injectable suspension in a 5 mL single-dose vial. Naltrexone for extended-release injectable suspension contains 380 mg of naltrexone in a microsphere formulation per vial (337 mg of naltrexone per gram of microspheres). …

• The safety and efficacy of naltrexone for extended-release injectable suspension have not been established in the pediatric population
• The pharmacokinetics of naltrexone for extended-release injectable suspension have not been evaluated in a pediatric population

In trials of alcohol-dependent subjects, 2.6% (n=26) of subjects were >65 years of age, and one patient was >75 years of age. Clinical studies of naltrexone for extended-release injectable suspension did not include sufficient numbers of subjects age 65 and over to determine whether they respond differently from younger subjects. No subjects over age 65 were included in studies of opioid-dependent subjects. …

• Advise the patient to read the FDA-Approved patient labeling ( Medication Guide )
• Physicians should include the following issues in discussions with patients for whom they prescribe naltrexone for extended-release injectable suspension
• Naltrexone for Extended-Release Injectable Suspension for Opioid Use Disorder: Advise patients that if they previously used opioids, they may be more sensitive to lower doses of opioids and at risk of accidental overdose should they use opioids when their next dose is due, if they miss a dose, or after naltrexone for extended-release injectable suspension treatment is discontinued. …

• Naltrexone for extended-release injectable suspension is contraindicated in: Patients receiving opioid analgesics [see Warnings and Precautions ]
• Patients with current physiologic opioid dependence [see Warnings and Precautions ]
• Patients in acute opioid withdrawal [see Warnings and Precautions ]
• Any individual who has failed the naloxone challenge test or has a positive urine screen for opioids [see Warnings and Precautions ] . …

Patients taking naltrexone for extended-release injectable suspension may not benefit from opioid-containing medicines. Naltrexone antagonizes the effects of opioid-containing medicines, such as cough and cold remedies, antidiarrheal preparations and opioid analgesics. Naltrexone antagonizes the effects of opioid-containing medicines, such as cough and cold remedies, antidiarrheal preparations, and opioid analgesics (7) .

Vulnerability to Opioid Overdose : Following naltrexone for extended-release injectable suspension treatment, opioid tolerance is reduced from pretreatment baseline and patients are vulnerable to potentially fatal overdose at the end of a dosing interval, after missing a dose, or after discontinuing naltrexone for extended-release injectable suspension treatment. Attempts to overcome blockade may also lead to fatal overdose. Strongly consider recommending or prescribing an opioid reversal agent (e.g., naloxone, nalmefene) for the emergency treatment of opioid overdose (5.1) . …

The following clinically significant adverse reactions are described elsewhere in the labeling: Accidental Opioid Overdose [see Warnings and Precautions ( 5.1 ) ] Injection Site Reactions [see Warnings and Precautions ( 5.2 ) ] Precipitated Opioid Withdrawal [see Warnings and Precautions ( 5.3 ) ] Hepatotoxicity [see Warnings and Precautions ( 5.4 ) ] Depression and Suicidality [see Warnings and Precautions ( 5.5 ) ] Eosinophilic Pneumonia [see Warnings and Precautions ( 5.7 ) ] Hypersensitivity Reactions [see Warnings and Precautions ( 5.8 ) ] The adverse events seen most frequently in association with naltrexone for extended-release injectable suspension therapy for alcohol dependence (i.e …

8.1 Pregnancy Risk Summary The available data from published case series with naltrexone for extended-release injectable suspension use in pregnant women are insufficient to identify a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. There are clinical considerations (see Clinical Considerations ). …

There is limited experience with overdose of naltrexone for extended-release injectable suspension. Single doses up to 784 mg were administered to 5 healthy subjects. There were no serious or severe adverse events. The most common effects were injection site reactions, nausea, abdominal pain, somnolence, and dizziness. There were no significant increases in hepatic enzymes. In the event of an overdose, appropriate supportive treatment should be initiated.

تناولها عندما تتذكر، إلا إذا اقترب موعد الجرعة التالية. عندها تخطَّ الجرعة المنسية. لا تتناول جرعتين معًا أبدًا للتعويض. راجع النشرة، فبعض الأدوية مختلفة.