naltrexone (Rx)

Brand and Other Names:ReVia, Vivitrol, more...Depade
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 50mg

microspheres for IM injection

  • 380mg

Opioid Dependence

Prevention of relapse after opioid detoxification; to be used only after patient has been opioid-free for 7-10 days and after negative naloxone challenge (no symptom withdrawal after naloxone administration)

PO: 25 mg initially, then observation for 1 hr, then 50 mg once daily starting on day 2; flexible dosing regimens can be employed to accommodate patient convenience or ensure compliance

IM: 380 mg in gluteal muscle every 4 weeks for maintenance of abstinence

Alcohol Dependence

Treatment in patients who have been able to abstain from alcohol in outpatient settings before treatment initiation

PO: 50 mg once daily for ≤12 weeks

IM: 380 mg in gluteal muscle every 4 weeks for maintenance of abstinence

Hepatitis (Orphan)

Orphan designation for treatment of autoimmune hepatitis

Sponsor

  • TaiwanJ Pharmaceuticals Co., Ltd, Room 204 A, Bldg 53; 195 Chung Hsing Rd., Sec 4; Chutung, Hsinchu, Taiwan

Postherpetic Neuralgia (Orphan)

Orphan designation for treatment of postherpetic neuralgia

Sponsor

  • Allodynic Therapeutics, LLC; 1785 NE 123rd Street; North Miami, FL 33181-2537

Safety and efficacy not established

Crohn Disease (Orphan)

Treatment in pediatric patients

Orphan indication sponsor

  • Jill P Smith, MD, Pennsylvania State University, 500 University Drive, Hershey, PA 17033
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Interactions

Interaction Checker

and naltrexone

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Injection site reaction (69%; includes bruising, induration, nodules, pain, pruritus, swelling, tenderness)

            Nausea (33%)

            Headache (25%)

            Decreased appetite (14%)

            Insomnia (14%)

            Vomiting (14%)

            Diarrhea (13%)

            Dizziness (13%)

            Upper respiratory tract infection (URTI) (13%)

            Anxiety (12%)

            Arthralgia (12%)

            Increased creatine phosphokinase (11%)

            Pharyngitis (11%)

            1-10%

            Depression (8%)

            Muscle cramps (8%)

            Back pain (6%)

            Rash (6%)

            Dry mouth (5%)

            Somnolence (4%)

            Increased aspartate aminotransferase (AST) (2%)

            <1%

            Alopecia

            Dyspnea

            Edema

            Hepatocellular injury

            Increased systolic and diastolic blood pressures

            Liver function abnormalities

            Labored breathing

            Nonspecific electrocardiographic (ECG) changes

            Opiate withdrawal (mild to severe signs and symptoms, including drug craving, confusion, drowsiness, visual hallucinations, abdominal pain, vomiting, diarrhea)

            Palpitation

            Phlebitis

            Tachycardia

            Postmarketing Reports

            Hypersensitivity reactions, including anaphylaxis

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            Warnings

            Contraindications

            Patients who are on opioid analgesics, are opioid-dependent (eg, opioid agonists [methadone], opioid partial agonists [buprenorphine]), are in acute opioid withdrawal, have positive urine test for opioids, or fail to pass naloxone challenge

            Hypersensitivity

            Cautions

            Depression, suicide, and suicidality cited in postmarketing reports; causal relation not demonstrated

            Vulnerability to opioid overdose: Patients should be alerted that they may be more sensitive to opioids, even at lower doses, after discontinuance of naltrexone

            Opioid withdrawal precipitated abruptly by administration of opioid antagonist to opioid-dependent patient may result in withdrawal syndrome severe enough to necessitate hospitalization (see Contraindications)

            Risk of hepatotoxicity with increasing doses; dose related hepatocellular injury; discontinue therapy if signs/symptoms of acute hepatitis develop

            Injection may cause severe injection-site reactions (eg, cellulitis, necrosis, hematoma); may be followed by pain, tenderness, induration, swelling, erythema, bruising, or pruritus; however, in some cases injection site reactions may be very severe andmay last for several weeks following administration

            Injectable microspheres are for IM use only; inadvertent SC/IV administration may increase risk of severe injection-site reactions

            Cases of eosinophilic pneumonia reported; consider in patients with symptoms of progressive hypoxia and dyspnea

            Use caution in patients with hepatic failure or with bleeding disorder including thrombocytopenia and hemophilia, or patients taking anticoagulant therapy; beeding hematoma may occur from IM administration

            Use caution in renal impairment or hepatic impairment

            Patients should be opioid free for a minimum of 7-10 days before initiating therapy; a naltrexone challenge test recommended to confirm opioid-free status

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            Pregnancy & Lactation

            Pregnancy

            The available data from published case series with use in pregnant women are insufficient to identify a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes

            Untreated opioid addiction in pregnancy is associated with adverse obstetrical outcomes such as low birth weight, preterm birth, and fetal death; in addition, untreated opioid addiction often results in continued or relapsing illicit opioid use

            Published studies have demonstrated that alcohol is associated with fetal harm including growth restriction, facial abnormalities, central nervous system abnormalities, behavioral disorders, and impaired intellectual development

            Lactation

            The drug and metabolites, are present in human milk; there are no data on effects on breastfed infant or on milk production

            Developmental health benefits of breastfeeding should be considered along with mother’s clinical need for naltrexone and any potential adverse effects on breastfed infant from drug or mother’s underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Opioid competitive receptor antagonist; shows highest affinity for mu receptors; congener of oxymorphone

            Absorption

            96% absorbed from gastrointestinal tract, but because of first-pass metabolism, only 5-40% reaches systemic circulation

            Bioavailability: 5-40%

            Onset: 15-30 min

            Duration: 24 hr

            Peak plasma time: PO tablet, 1 hr; PO solution, 0.6 hr

            Peak plasma concentration (50-mg dose): Naltrexone, 10.6-13.7 ng/mL; 6-β-naltrexol, 109-139 ng/mL

            Distribution

            Protein bound: 21-28%

            Vd: 1350 L

            Metabolism

            Metabolized in liver

            Metabolites: 6-β-naltrexol (major), 2-hydroxy-3-methoxy-6-β-naltrexol (HMN), 2-hydroxy-3-metho-xynaltrexone, noroxymorphone, 3-methoxy-6-β-naltrexol

            Elimination

            Half-life: PO, 4 hr; 6-β-naltrexol, 13 hr; IM and 6-β-naltrexol and IM: 5-10 days

            Excretion: Urine (mainly)

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            Administration

            IM Administration

            Administer IM as gluteal injection, alternating buttocks for each subsequent injection

            Drug must be prepared and administered by a healthcare provider

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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.