Contrave (Naltrexone/Bupropion) is an FDA-approved prescription medication to help adult patients with a Body Mass Index (BMI) higher than 30 kg/m2 or a BMI of 27 kg/m2 and at least one comorbidity, such as type 2 diabetes, high blood pressure or high cholesterol. It works by affectying part of the brain and reducing the appetite, and is believed to enhance weight loss in combination with a healthy diet and regular physical activity.
The drug combination is a trademark of Orexigen Therapeutics, Inc., used under license by Takeda Pharmaceuticals America, Inc., and it includes two compounds, 8mg of Naltrexone HCI and 90 mg of Bupropion. Contrave is available in tablets and should be taken according to the physician’s advices. The producer recommends taking one pill in the morning during the first week, one in the morning and another in the evening during the second week, the addition of another pill in the morning at third week, and four pills divided equally into the morning and evening during the following weeks.
History of Contrave (Naltrexone/Bupropion)
Contrave was approved by the FDA in September 2014, three months after a delay in the approval process provoked by the agency due to uncertainty about the drug combination. The approval was based on the results of four 56-week multicenter, double-blind, placebo-controlled trials, named CONTRAVE Obesity Research (COR-I and COR-II) as well as COR-BMOD and COR-Diabetes. The studies focused on the effects of Contrave accompanied by lifestyle alterations, which were evaluated in 4,536 patients and compared to placebo.
At COR-I, COR-II, COR-BMOD and COR-Diabetes, Orexygen studied the effects of the drug in overweight or obese patients and at least one comorbidity, such as hypertension, dyslipidemia and type 2 diabetes, respectively. Despite the fact that Contrave was only approved in the United States in 2014, Naltrexone is one of the oldest compounds approved in the country to treat obesity.
How Contrave (Naltrexone/Bupropion) Works
Naltrexone is a pure opioid antagonist and synthetic relative of oxymorphone and naloxone, which is combined with Bupropion, an antidepressant and dopamine reuptake inhibitor included the drug call of amino-ketone. The drug combination works by interfering with the pathways of the central nervous system in the hypothalamus, responsible for food intake and body weight. Contrave targets these systems, as Bupropion stimulated the pro-opiomelanocor tin (POMC)-producing neurons and Naltrexone blocks the autoinhibitory feedback related to weight loss.
Other Details About Contrave (Naltrexone/Bupropion)
Contrave should not be taken by patients younger than 18 years old, since its effects are not studied, as well as by patients also taking Wellbutrin, Aplenzin, sedatives, benzodiazepines, anti-seizure medicines or monoamine oxidase inhibitors (MAOIs), with eating disorders, dependent on opioid medicines, with a drinking or previous drinking problem, or by pregnant women. Given the drug’s potential to provoke suicidal thoughts or actions as side effect, patients and loved ones should pay particular attention to mood or behavioral changes.
Most common side effects related to Contrave include nausea, constipation, headache, vomiting, dizziness, difficulties in sleeping, dry mouth and diarrhea. The persistance of the symptoms should be communicated to a physician, the same as other symptoms, such as depression, anxiety, serious agitation of restless feeling, panic attacks, insomnia, irritability, aggressiveness, angry or violent behavior, dangerous impulses, mania or additional behavioral or mood alterations.