bupropion/naltrexone (Rx)

Brand and Other Names:Contrave
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Dosing & Uses

AdultPediatric

Dosing Forms & Strengths

bupropion/naltrexone

extended release tablet

  • 90mg/8mg

Obesity

For use as adjunct to reduced-calorie diet and increased physical activity for long-term weight management in adults with initial body mass index of ≥30 kg/m² (obese) or ≥27 kg/m² (overweight) in presence of at least 1 weight-related comorbidity (eg, hypertension, type 2 diabetes, or dyslipidemia)

1 tablet (90mg/8mg) initially week 1; increase by 1 tablet/day each subsequent week until daily maintenance dose of 2 tablets twice daily (360 mg bupropion/32 mg naltrexone) is achieved at the start of week 4

Dosage Modifications

Coadministration with CYP2B6 inhibitors (eg, ticlopidine or clopidogrel): Not to exceed 1 tablet BID

Hepatic impairment: Not to exceed 1 tablet daily

Renal impairment

  • Mild: Not studied
  • Moderate-to-severe: Not to exceed 1 tablet BID
  • End-stage renal disease: Not recommended

Dosing Considerations

Clinical response should be observed by 4 months of treatment

Discontinue therapy if clinically meaningful weight loss (≥5%) not exhibited after 4 months; other weight management strategies should be considered

Effect on cardiovascular morbidity not established

Safety and efficacy when used in combination with other weight-loss products, including over-the-counter drugs and herbal preparations, not established

Do not administer within 14 days of taking a monoamine oxidase inhibitor for depression

Recommendations to reduce risk of seizure

  • Bupropion component may increase the risk of seizures
  • Do not exceed 360 mg bupropion component (4 tablets daily)
  • Administer daily dose in divided doses (twice daily)
  • Escalate dose gradually
  • Do not take more than 2 tablets at one time
  • Avoid coadministration with high-fat meals
  • If dose is missed, wait until next scheduled dose to resume regular dosing schedule

Safety and efficacy not established

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Interactions

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            Adverse Effects

            >10%

            Nausea (32.5%)

            Constipation (19.2%)

            Headache (17.6%)

            Vomiting (10.7%)

            1-10%

            Dizziness (9.9%)

            Insomnia (9.2%)

            Dry mouth (8.1%)

            Diarrhea (7.1%)

            Anxiety (4.2%)

            Hot flash (4.2%)

            Fatigue (4%)

            Tremor (4%)

            Upper abdominal pain (3.5%)

            Viral gastroenteritis (3.5%)

            Influenza (3.4%)

            Tinnitus (3.3%)

            Urinary tract infection (3.3%)

            Hypertension (3.2%)

            Abdominal pain (2.8%)

            Hyperhidrosis (2.6%)

            Irritability (2.6%)

            Increased blood pressure (2.4%)

            Dysgeusia (2.4%)

            Rash (2.4%)

            Muscle strain (2.2%)

            Palpitations (2.1%)

            Frequency Not Defined

            Tachycardia

            Myocardial infarction

            Vertigo

            Motion sickness

            Lower abdominal pain

            Eructation

            Lip swelling

            Hematochezia

            Hernia

            Feeling jittery

            Thirst

            Feeling hot

            Asthenia

            Cholecystitis

            Pneumonia

            Staphylococcal infection

            Kidney infection

            Increased creatinine clearance

            Increased hepatic enzymes

            Decreased hematocrit

            Dehydration

            Intervertebral disc protrusion

            Jaw pain

            Disturbance in attention

            Lethargy

            Intention tremor

            Balance disorder

            Memory impairment

            Amnesia

            Mental impairment

            Presyncope

            Abnormal dreams

            Nervousness

            Dissociation (feeling spacy)

            Tension

            Agitation

            Mood swings

            Vaginal hemorrhage

            Irregular menstruation

            Erectile dysfunction

            Vulvovaginal dryness

            Alopecia

            Postmarketing Reports

            Loss of consciousness, malaise

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            Warnings

            Black Box Warning

            Not approved for treatment of major depressive disorder or psychiatric disorders

            Antidepressants like bupropion increase the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term trials but were not seen in patients ≥24 years and a lower risk was seen in patients ≥65 years; patients of all ages should be monitored closely for suicidal thoughts and behaviors

            Serious neuropsychiatric reactions reported in patients taking bupropion for smoking cessation that occurred during therapy or while discontinuing therapy; patients should be monitored for neuropsychiatric reactions

            Contraindications

            Uncontrolled hypertension

            Seizure disorder or a history of seizures

            Use of other bupropion-containing products

            Bulimia or anorexia nervosa, which may increase risk of seizures

            Long-term opioid or opiate agonists use or acute opiate withdrawal

            Patients undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs

            Within 14 days of monoamine oxidase inhibitor therapy

            Hypersensitivity

            Pregnancy

            Cautions

            Monitor patients for suicidal ideation or behavior and for unusual changes in behavior (see black box warning)

            Discontinue therapy and do not restart if seizure occurs while on therapy; use caution when prescribing to patients with predisposing risk factors for seizures

            Not for administration to patients receiving long-term opioids, owing to naltrexone component (opioid antagonist); discontinue therapy if long-term opiate therapy required

            Following therapy, patients may be more sensitive to opioids, even at lower doses

            A patient should not attempt to overcome naltrexone opioid blockade by administering large amounts of exogenous opioids; may lead to fatal overdose

            Opioid-dependent patients, including those being treated for alcohol dependence, should be opioid-free (including tramadol) before therapy is initiated; opioid-free interval of a minimum of 7-10 days is recommended for patients previously dependent on short-acting opioids; patients transitioning from buprenorphine or methadone may need as long as 2 weeks

            Blood pressure and pulse should be measured prior to starting therapy and should be monitored at regular intervals, particularly among patients with controlled hypertension prior to treatment

            Discontinue therapy if symptoms or signs of acute hepatitis occur

            Screen patients for a history of bipolar disorder and the presence of risk factors for bipolar disorder; therapy was not studied in patients receiving antidepressant medications patients with a history of bipolar disorder or recent hospitalization foor psychiatric illness were excluded from clinical trials

            Angle-closure attack may occur in patients with anatomically narrow angles that do not have a patent iridectomy

            Measure blood glucose levels prior to and during therapy; patients who develop hypoglycemia after initiating Contrave therapy should adjust antidiabetic drug regimen

            Use caution in patients with history of tumor or infection of the brain or spine

            Initiation of therapy in patients receiving linezolid or intravenous (IV) methylene blue

            Use caution in hepatic impairment

            May precipitate a manic, mixed, or hypomanic episode; risk higher in patients with bipolar disorders or have risk factors for bipolar disorder, including family history of bipolar disorder, suicide, or depression; not FDA approved for bipolar depression

            Some patients who stopped smoking reported to have experienced symptoms of nicotine withdrawal, including depressed mood; depression, rarely including suicidal ideation, reported in smokers undergoing a smoking cessation attempt without medication; however, some of these adverse events occurred in patients taking bupropion who continued to smoke

            Neuropsychiatric adverse events reported in patients without and with pre-existing psychiatric disease; some patients experienced worsening of their psychiatric illnesses; observe patients for occurrence of neuropsychiatric adverse events; patient should stop therapy and contact healthcare provider immediately if agitation, depressed mood, or changes in behavior or thinking that are not typical for patient are observed, or if patient develops suicidal ideation or suicidal behavior; symptoms may persist after discontinuation of therapy; in some cases; monitoring and supportive care should be provided until symptoms resolve

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            Pregnancy & Lactation

            Pregnancy category: X

            Lactation: Not recommended

            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

            Bupropion: Increases dopamine activity in the brain, which appears to lead to a reduction in appetite and increase in energy expenditure by increasing activity of pro-opiomelanocortin (POMC) neurons

            Naltrexone: Blocks opioid receptors on the POMC neurons, preventing feedback inhibition of these neurons and further increasing POMC activity

            Combination may regulate activity in the dopamine reward system of the brain that helps control food cravings and overeating behaviors

            Absorption

            Naltrexone

            • Peak time: 2 hr

            Bupropion

            • Peak time: 3 hr

            Metabolism

            Naltrexone

            • Hepatic

            Bupropion

            • Hepatic, via CYP2B6

            Distribution

            Naltrexone

            • Protein bound: 21%

            Bupropion

            • Protein bound: 84%

            Elimination

            Naltrexone

            • Excretion: Urine (53-79%)
            • Half-life: 5 hr

            Bupropion

            • Excretion: Urine (87%); feces (10%)
            • Half-life: 21 hr
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            Administration

            Oral Administration

            Take by mouth in the morning and evening

            Do not crush, chew, or cut tablets

            Doses >32 mg/360 mg per day not recommended

            Do not administer with high-fat meal as it may result in significant increase in bupropion and naltrexone exposure

            Therapy may cause elevation in blood pressure or heart rate, especially during initial 3 months of therapy; patients with hypertension should be monitored closely

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            Formulary

            FormularyPatient Discounts

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            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.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the 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.