Pharmacological Class:
Opioid antagonist + aminoketone.

Active Ingredient(s):
Naltrexone HCl, bupropion HCl 8mg/90mg; extended-release tablets.

Company
Takeda Pharmaceuticals North America, Inc.

Indication(s):
Adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults with an initial BMI of ≥30kg/m2 or ≥27kg/m2 in the presence of at least one weight-related comorbidity (eg, hypertension, type 2 diabetes, or dyslipidemia). Limitations of use: effect on cardiovascular morbidity and mortality has not been established. Safety and efficacy in combination with other weight loss products, including Rx or OTC drugs, and herbal preps, have not been established.

Pharmacology:
Contrave combines naltrexone, an opioid antagonist, and bupropion, a relatively weak inhibitor of the neuronal reuptake of dopamine and norepinephrine.

Legal Classification:
Rx

Adults:
Swallow whole. Avoid high-fat meals. Escalate dose gradually. ≥18 years: Week 1: 1 tab daily in the AM; Week 2: 1 tab daily in the AM and 1 tab daily in the PM; Week 3: 2 tabs in the AM and 1 tab in the PM; Week 4 and thereafter: 2 tabs in the AM and 2 tabs in the PM. Max 32mg/360mg per day. eva luate response after 12 weeks. Discontinue if ≥5% weight loss is not achieved. Concomitant CYP2B6 inhibitors (eg, ticlopidine, clopidogrel), moderate or severe renal impairment: max 2 tabs daily (1 tab each AM & PM). Hepatic impairment: max 1 tab in the AM.

Children:
<18 years: not recommended.

Contraindication(s):
Uncontrolled hypertension. Seizure disorder. Concomitant other bupropion-containing products. Bulimia. Anorexia nervosa. Use of chronic opioid or opiate agonist (eg, methadone), or partial agonists (eg, buprenorphine). Acute opiate withdrawal. Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptics. During or within 14 days of discontinuing MAOIs. Concomitant linezolid or IV methylene blue. Pregnancy (Category X).

Warnings/Precautions:
Increased risk of suicidal thoughts and behavior in children, adolescents, and young adults; monitor for clinical worsening or unusual behavioral changes in all patients. Monitor for neuropsychiatric reactions. Increased risk of seizures with predisposing risk factors (eg, history of head trauma, prior seizure, severe stroke, arteriovenous malformation, CNS tumor or infection, others: see full labeling); discontinue if seizure occurs and do not restart. Diabetes. Hypoglycemia. Cardiac or cerebrovascular disease. Monitor BP, pulse, and blood glucose levels prior to starting and during treatment. Risk of hepatic injury; discontinue if signs/symptoms of acute hepatitis occur. Screen for bipolar disorder. Angle-closure glaucoma. Elderly. ESRD, nursing mothers: not recommended.

Interaction(s)
See Contraindications. Vulnerability to opioid overdose with concurrent opioid analgesics; if chronic therapy needed, discontinue Contrave. To prevent precipitation of withdrawal: discontinue chronic opioids 7–10 days prior to initiation. Reduced benefit with opioid-containing drugs (eg, antitussives, antidiarrheals, analgesics). May be potentiated by CYP2B6 inhibitors (see Adults). Avoid concomitant CYP2B6 inducers (eg, ritonavir, lopinavir, efavirenz). Caution with CYP2D6 substrates (eg, tricyclics, SSRIs, antipsychotics [eg, haloperidol, risperidone, thioridazine], β-blockers [eg, metoprolol], Class 1C antiarrhythmics [eg, propafenone, flecainide]); consider dose reduction (esp. drugs with a narrow therapeutic index). Caution with drugs that lower seizure threshold (eg, antipsychotics, antidepressants, theophylline, steroids). Monitor for CNS toxicity with levodopa, amantadine. Avoid alcohol. May potentiate OCT2 substrates (eg, amantadine, amiloride, cimetidine, dopamine, famotidine, memantine, metformin, pindolol, procainamide, ranitidine, varenicline, oxaliplatin); monitor. Concomitant antidiabetics; adjust dose if hypoglycemia develops. May cause false (+) test results in urine immunoassay for amphetamines.

Adverse Reaction(s)
Nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth, diarrhea; allergic reactions.

How Supplied:
Tabs—120

LAST UPDATED:
12/9/2014