Our Research Insights
We are committed to providing innovative treatment options for the millions of people struggling with their weight. Losing weight and keeping it off is difficult. Comprehensive weight loss management programs consisting of diet, exercise, behavior modification counseling, and medications have been shown to help people lose weight and keep it off, which may lead to improved overall health and wellness.
The research leading to the development of CONTRAVE focused on two regions in the brain: the hypothalamus and the dopamine reward system. One important role of the hypothalamus is to regulate the body’s appetite (energy intake) and metabolism (energy expenditure). The dopamine reward system interacts with the hypothalamus to regulate and control eating behaviors and cravings.
Weight gain results from an energy imbalance caused by the consumption of more calories than the body is able to burn over an extended period. The cause of this imbalance is complex and is influenced by the convergence of various environmental, behavioral and genetic factors. However, at the crux of gaining weight and the inability to sustain weight loss is the role of the brain and CNS in regulating body weight.
The brain is the master regulator of the body, affecting every fundamental function including decisions about what we eat, when we eat, how much we eat and how much energy we burn. Over time, the brain of a person who is overweight or obese becomes insensitive to the “stop” signals from the body, resulting in continued consumption of food beyond the body’s energy needs. When an overweight person starts to lose weight, the brain senses the reduction in weight and causes the body to fight back by increasing hunger and food the rewarding properties of food, while also slowing down metabolism. Together, these processes combine to increase food intake and decrease energy expenditure, thereby leading to weight regain. Thus, many interventions for weight loss may be successful in the short term, but results are typically difficult to maintain.
Two basic opposing neuronal populations in the hypothalamus work through the melanocortin 4 receptor (MC-4) to maintain the body’s weight at a constant level. Activation of the proopiomelanocortin or POMC neurons reduces appetite and increases energy output. Activation of the neuropeptide Y/Agouti-Related Peptide (NPY/AgRP) neurons increases hunger and conserves energy when energy reserves, stored as fat, are low. Additionally, food consumption triggers signals in reward areas of the brain, which may lead to overconsumption due to these reward signals.
Important Safety Information for Contrave
CONTRAVE can cause serious side effects of suicidal thoughts or actions. One of the ingredients in CONTRAVE is bupropion HCl. Bupropion has caused some people to have suicidal thoughts or actions or unusual changes in behavior, whether or not they are taking medicines used to treat depression. Bupropion may increase suicidal thoughts or actions in some children, teenagers, and young adults within the first few months of treatment. If you already have depression or other mental illnesses, taking bupropion may cause it to get worse, especially within the first few months of treatment.
Stop taking CONTRAVE and call a healthcare provider right away if you, or your family member, have any of the following symptoms, especially if they are new, worse, or worry you: thoughts about suicide or dying; attempts to commit suicide; depression; anxiety; feeling very agitated or restless; panic attacks; trouble sleeping (insomnia); irritability; acting aggressive, being angry or violent; acting on dangerous impulses; an extreme increase in activity and talking (mania); other unusual changes in behavior or mood.
While taking CONTRAVE, you or your family members should pay close attention to any changes, especially sudden changes, in mood, behaviors, thoughts, or feelings and maintain communication with your healthcare provider. CONTRAVE has not been studied in and is not approved for use in children under the age of 18.
Do not take CONTRAVE if you:
- Have uncontrolled high blood pressure
- Have or have had seizures
- Use other medicines that contain bupropion such as WELLBUTRIN, WELLBUTRIN SR, WELLBUTRIN XL, and APLENZIN
- Have or have had an eating disorder called anorexia or bulimia
- Are dependent on opioid pain medicines or use medicines to help stop taking opioids such as methadone or buprenorphine, or are in opiate withdrawal
- Drink a lot of alcohol and abruptly stop drinking, as this may increase your chance of having a seizure; or use medicines called sedatives (these make you sleepy), benzodiazepines, or anti-seizure medicines and you stop using them all of a sudden
- Have taken medicines called monoamine oxidase inhibitors (MAOIs), including linezolid, within the last 14 days
- Are allergic to naltrexone HCl or bupropion HCl or any of the ingredients in CONTRAVE
- Are pregnant or planning to become pregnant. Tell your healthcare provider right away if you become pregnant while taking CONTRAVE
Tell your healthcare provider about all of your medical conditions, especially: depression or other mental illnesses; attempted suicide; seizures; head injury; tumor or infection of your brain or spine; low blood sugar or low levels of sodium in your blood; liver or kidney problems; high blood pressure; heart problems or stroke; eating disorder. Also tell your doctor if you drink a lot of alcohol and plan to suddenly stop; abuse prescription medicines or street drugs; are over the age of 65; have any other medical conditions; or are breastfeeding or plan to breastfeed.
Tell your healthcare provider about all the medicines you take including prescription and over-the-counter medicines, vitamins, and herbal supplements. Do not take any other medicines while you are taking CONTRAVE unless your healthcare provider has said it is okay to take them.
Swallow CONTRAVE tablets whole. Do not cut, chew, or crush CONTRAVE tablets. Tell your healthcare provider if you cannot swallow CONTRAVE tablets whole. Do not take CONTRAVE with high-fat meals. It may increase your risk of seizures. Take CONTRAVE exactly as prescribed.
Possible serious side effects of CONTRAVE:
- If you have a seizure, stop taking CONTRAVE, tell your healthcare provider right away, and do not take CONTRAVE again
- If you take opioid medicines, there may be a risk of opioid overdose. You should get emergency medical help right away if you have trouble breathing; become drowsy with slowed breathing; have slow, shallow breathing; or feel faint, dizzy, or confused
- Sudden opioid withdrawal can be severe and may require hospitalization
- Stop taking CONTRAVE and get medical help immediately if you have any of the following signs and symptoms of severe allergic reactions: rash, itching, hives, fever, swollen lymph glands, painful sores in your mouth or around your eyes, swelling of your lips or tongue, chest pain, or trouble breathing
- Increases in blood pressure or heart rate may occur
- CONTRAVE can cause liver damage or hepatitis. Stop taking CONTRAVE if you have any of the following symptoms of liver problems: stomach area pain lasting more than a few days, dark urine, yellowing of the whites of your eyes, or tiredness
- Manic episodes can occur. CONTRAVE can cause some people who were manic or depressed in the past to become manic or depressed again
- CONTRAVE can cause visual problems (angle-closure glaucoma). Signs and symptoms may include: eye pain, changes in vision, swelling or redness in or around the eye. Talk with your doctor to find out if you are at risk and to get treatment to prevent it
- Increased risk of low blood sugar (hypoglycemia) in people with type 2 diabetes mellitus who also take medicines to treat their diabetes (such as insulin or sulfonylureas). You should check your blood sugar before you start and while taking CONTRAVE
The most common side effects of CONTRAVE include nausea, constipation, headache, vomiting, dizziness, trouble sleeping, dry mouth, and diarrhea.
Tell your healthcare provider about any side effect that bothers you or does not go away. These are not all the possible side effects of CONTRAVE.
Use of CONTRAVE
CONTRAVE is a prescription medicine that contains 2 medicines (naltrexone HCl and bupropion HCl) that may help some obese adults*, or overweight adults who also have weight-related medical problems†, lose weight and keep the weight off.
- CONTRAVE should be used with a reduced calorie diet and increased physical activity
- It is not known if CONTRAVE changes your risk of heart problems or stroke or of death due to heart problems or stroke
- It is not known if CONTRAVE is safe and effective when taken with other prescription, over-the-counter, or herbal weight loss products
*Body mass index (BMI) of 30 kg/m2 or greater.
†BMI of 27 kg/m2 or greater with at least one weight-related medical problem such as high blood pressure, high cholesterol, or type 2 diabetes.
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch or call 1-800-FDA-1088.