CONTRAVE ER (Bupropion/Naltrexone)

What is this medication?

Bupropion+Naltrexone, Contrave
Anorexiant; Dopamine/Norepinephrine-Reuptake Inhibitor; Opioid Antagonist

Officially indicated for weight management in adjunct to a reduced calorie diet and increased physical activity.

“ALERT: US Boxed Warning

Suicidality and antidepressant drugs:

Contrave is not approved for use in the treatment of major depressive disorder or other psychiatric disorders. Contrave contains bupropion, the same active ingredient as some other antidepressant medications (including, but not limited to, Wellbutrin, Wellbutrin SR, Wellbutrin XL, and Aplenzin). Antidepressants increased the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term trials. These trials did not show an increase in the risk of suicidal thoughts and behavior with antidepressant use in subjects over age 24; there was a reduction in risk with antidepressant use in subjects aged 65 and older. In patients of all ages who are started on Contrave, monitor closely for worsening, and for the emergence of suicidal thoughts and behaviors. Advise families and caregivers of the need for close observation and communication with the prescriber. Contrave is not approved for use in pediatric patients.”

How does this medication work? 

Bupropion appears to enhance norepinephrine and dopamine activity and does not inhibit monoamine oxidase or the reuptake of serotonin like other antidepressants.   Naltrexone is a pure opioid antagonist and acts as a competitive antagonist at opioid receptor sites.  The exact neurochemical effects of naltrexone/bupropion leading to weight loss are not fully understood. Effects may result from action on areas of the brain involved in the regulation of food intake: the hypothalamus (appetite regulatory center) and the mesolimbic dopamine circuit (reward system).

How should I take this medication? 

Weight Management
Oral: Take 1 tablet once daily in the morning for week 1; then take 1 tablet twice daily in the morning and evening for week 2; then take 2 tablets in the morning and 1 tablet in the evening for week 3; then take 2 tablets in the morning and 2 tablets in the evening for week 4 and continue for the remainder of the course.

Usual Dosage: Take 2 tablets twice daily; maximum daily dose of 4 tablets daily.

How Do You Use Bupropion+Naltrexone, Contrave:  The maintenance daily dose of Contrave is 2 tablets twice daily.  Make sure to not take Contrave with a high-fat meal.  Do not cut, crush, or chew the tablets.  

Is Bupropion+Naltrexone, Contrave Safe to Use During Pregnancy:  Any medication used for weight loss is not recommended at conception and during pregnancy.  Hence, Contrave is contraindicated in pregnant women.

How Do You Know When to Stop Bupropion+Naltrexone, Contrave:  If you have not lost at least 5% of your baseline body weight after 12 weeks at the maintenance dosage; it is recommended to discontinue therapy.

What should I watch for while using this medication? 

Use with caution in patients with major depressive disorder and other psychiatric disorders

Can lead to accidental opioid overdose and acute withdrawal

Do not use in patients with uncontrolled hypertension

Use with caution in patients with hepatic and renal disease 

Do not use in patients with a seizure disorder or a history of seizures, current or past diagnosis of bulimia or anorexia nervosa

What if I miss a dose?

If you miss a dose of medication, try to take it as soon as possible. However, if it is almost time for your next dose, take only that scheduled dose. Do not take double or extra doses.

How should I store this medication?

Keep out of the reach of children at all times. Store at room temperature, 59 to 86° F (15 to 30° C). Protect from light. Keep the container tightly closed. Properly dispose of any unused medication after the expiration date.

What are the possible side effects of using this medication?

Well tolerated, most side effects are transient and mild to moderate in nature.  The most common side effects include:

>10%:

Central Nervous System: Headache (18%), sleep disorder (14%)

Gastrointestinal: Nausea (33%), constipation (19%), vomiting (11%)