Description: Anorexiant; Dopamine/Norepinephrine-Reuptake Inhibitor; Opioid Antagonist
“ALERT: US Boxed Warning
Suicidality and antidepressant drugs:
Contrave is not approved for use in the treatment of a 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 behaviour in children, adolescents, and young adults in short-term trials. These trials did not show an increase in the risk of suicidal thoughts and behaviour 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 behaviours. Advise families and caregivers of the need for close observation and communication with the prescriber. Contrave is not approved for use in pediatric patients.”
CSA NA – FDA Approved – REMS (N) – Can Ship
How Does It 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 acting on areas of the brain involved in the regulation of food intake: the hypothalamus (appetite regulatory centre) and the mesolimbic dopamine circuit (reward system).
Indications For Use
Officially indicated for weight management in adjunct to a reduced-calorie diet and increased physical activity.
- 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
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; a maximum daily dose of 4 tablets daily.
Points To Consider
Potential exists for misuse in inappropriate patient populations (i.e. anorexia nervosa or bulimia)
Pharmacist Tips On Using
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.
Well tolerated, most side effects are transient and mild to moderate in nature. The most common side effects include:
Central Nervous System: Headache (18%), sleep disorder (14%)
Gastrointestinal: Nausea (33%), constipation (19%), vomiting (11%)