Contrave

Generic Name: bupropion hydrochloride and naltrexone hydrochloride

Date of Approval: September 10, 2014

Company: Orexigen Therapeutics

Treatment for: Obesity

FDA Approves Contrave

New weight loss option targets both the physiological and behavioral factors associated with obesity.

The U.S. food and Drug Administration has approved Contrave for chronic weight management in addition to a reduced-calorie diet and physical activity. Contrave is a combination of two FDA-approved drugs in an extended-release formulation:

• naltrexone (ReVia, Vivitrol) used to treat alcohol and opioid dependence
• bupropion (Wellbutrin, Zyban) used to treat depression and seasonal affective disorder, and as an aid to smoking cessation treatment.

Contrave is approved for use in adults with a body mass index (BMI) of 30 or greater (obesity) or adults with a BMI of 27 or greater (overweight) who have at least one weight-related condition such as high blood pressure, type 2 diabetes, or high cholesterol.

Medication Guide

Read this Medication Guide before you start taking this medicine and each time you get a refill. There may be new information. This information does not take the place of talking with your healthcare provider about your medical problems or treatment.

Important information

Contrave can cause serious side effects, including:

• Suicidal thoughts or actions. One of the ingredients is bupropion. 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 this medicine 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
  • new or worse irritability
  • attempts to commit suicide
  • acting aggressive, being angry, or violent
  • new or worse depression
  • acting on dangerous impulses
  • new or worse anxiety
  • an extreme increase in activity and talking (mania)
  • feeling very agitated or restless
  • panic attacks
  • other unusual changes in behavior or mood
  • trouble sleeping (insomnia)

  During treatment, you or your family members should:

  • Pay close attention to any changes, especially sudden changes, in mood, behaviors, thoughts, or feelings. This is very important when you start treatment or when your dose changes.
  • Keep all follow-up visits with your health care provider as scheduled. Call your healthcare provider between visits as needed, especially if you have concerns about symptoms.

Contrave has not been studied in and is not approved for use in children under the age of 18.

What is Contrave?

Contrave is a prescription medicine which contains two medicines (naltrexone and bupropion) that may help some obese or over weight adults, who also have weight related medical problems, lose weight and keep the weight off.

• It should be used with a reduced calorie diet and increased physical activity.
• It is not known if it changes your risk of heart problems or stroke or of death due to heart problems or stroke.
• It is not known if it is safe and effective when taken with other prescription, over-the-counter, or herbal weight loss products.
• It is not known if it is safe and effective in children under 18 years of age.
• It is not approved to treat depression or other mental illnesses, or to help people quit smoking (smoking cessation). One of the ingredients, bupropion, is the same ingredient in some other medicines used to treat depression and to help people quit smoking.

Who should not take Contrave?

Do not take this medicine if you:

• have uncontrolled hypertension
• have or have had seizures
• use other medicines that contain bupropion such as Wellbutrin, Wellbutrin SR, Wellbutrin XL, Aplenzin and Zyban
• have or have had an eating disorder called anorexia (eating very little) or bulimia (eating too much and vomiting to avoid gaining weight)
• 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, or use medicines called sedatives (these make you sleepy), benzodiazepines, or anti-seizure medicines and you stop using them all of a sudden
• are taking medicines called monoamine oxidase inhibitors (MAOIs). Ask your healthcare provider or pharmacist if you are not sure if you take an MAOI, including linezolid. Do not start treatment until you have stopped taking your MAOI for at least 14 days.
• are allergic to naltrexone or bupropion or any of the other ingredients. See theend of this Medication Guide for a complete list of ingredients.
• are pregnant or planning to become pregnant. Tell your healthcare provider right away if you become pregnant while taking Contrave.

Before taking Contrave

Before starting this medicine, tell your healthcare provider if you:

• have or have had depression or other mental illnesses (such as bipolar disorder)
• have attempted suicide in the past
• have or have had seizures
• have had a head injury
• have had a tumor or infection of your brain or spine (central nervous system)
• have had a problem with low blood sugar (hypoglycemia) or low levels of sodium in your blood (hyponatremia)
• have or have had liver problems
• have high blood pressure
• have or have had a heart attack, heart problems, or have had a stroke
• have kidney problems
• are diabetic taking insulin or other medicines to control your blood sugar
• have or have had an eating disorder
• drink a lot of alcohol
• abuse prescription medicines or street drugs
• are over the age of 65
• have any other medical conditions
• are breastfeeding or plan to breastfeed. This medicine can pass into your breast milk and may harm your baby. You and your healthcare provider should decide if you should continue treatment or breastfeed. You should not do both.
• Tell your healthcare provider about all the medicines you take including prescription and over-the-counter medicines, Vitamins, and herbal supplements. This medicine may affect the way other medicines work and vice versa, and can cause side effects.

Ask your healthcare provider for a list of these medicines if you are not sure.

Know the medicines you take. Keep a list of them to show your healthcare provider or pharmacist when you get a new medicine.

How should I take Contrave?

How to take Contrave

Morning Dose Evening Dose Starting: Week 1 1 tablet None Week 2 1 tablet 1 tablet Week 3 2 tablets 1 tablet Week 4 Onward 2 tablets 2 tablets

• Take the tablets exactly as your healthcare provider tells you to.
• Do not change your dose without talking with your healthcare provider.
• Your healthcare provider will change your dose if needed.
• Your healthcare provider should tell you to stop taking the tablets if you have not lost a certain amount of weight after 16 weeks of treatment.
• Swallow the tablets whole. Do not cut, chew, or crush. Tell your healthcare provider if you cannot swallow the tablets whole.
• Do not take more than 2 tablets in the morning and 2 tablets in the evening.
• Do not take more than 2 tablets at the same time or more than 4 tablets in 1 day.
• Do not take the tablets with high-fat meals. It may increase your risk of seizures.
• If you miss a dose, wait until your next regular time to take it. Do not take more than one dose at a time.
• If you overdose, call your healthcare provider or go to the nearest emergency room right away.

What should I avoid?

• Do not drink a lot of alcohol during treatment.
• If you drink a lot of alcohol, talk with your healthcare provider before suddenly stopping. If you suddenly stop drinking alcohol, you may increase your chance of having a seizure.

Contrave side effects

Serious side effects include:

• See Important information
• Seizures. There is a risk of having a seizure when you take this medicine. The risk of seizure is higher in people who:
  • take higher doses
  • have certain medical conditions
  • take this medicine with certain other medicines

  Do not take any other medicines during treatment unless your healthcare provider has said it is okay to take them.

  If you have a seizure, stop taking Contrave and call your healthcare provider right away.

  You should not take Contrave again if you have a seizure.

• Risk of opioid overdose. One of the ingredients (naltrexone) can increase your chance of having an opioid overdose if you take opioid medicines. You can accidentally overdose in 2 ways:
  • Naltrexone blocks the effects of opioids, such as heroin, methadone or opioid pain medicines. Do not take large amounts of opioids, including opioid-containing medicines, such as heroin or prescription pain pills, to try to overcome the opioid- blocking effects of naltrexone. This can lead to serious injury, coma, or death.
  • After you take naltrexone, its blocking effect slowly decreases and completely goes away over time. If you have used opioid street drugs or opioid-containing medicines in the past, using opioids in amounts that you used before treatment with naltrexone can lead to overdose and death. You may also be more sensitive to the effects of lower amounts of opioids:
    • after you have gone through detoxification
    • when your next dose of Contrave is due
    • if you miss a dose
    • after you stop treatment

  It is important that you tell your family and the people closest to you of this increased sensitivity to opioids and the risk of overdose. You or someone close to you should get emergency medical help right away if you:

  • have trouble breathing
  • become very drowsy with slowed breathing
  • have slow, shallow breathing (little chest movement with breathing)
  • feel faint, very dizzy, confused, or have unusual symptoms
• Sudden opioid withdrawal. People who take Contrave must not use any type of opioid (must be opioid-free) including street drugs, prescription pain medicines (including tramadol), cough, cold, or diarrhea medicines that contain opioids, or opioid dependence treatments, buprenorphine or methadone, for at least 7 to 10 days before starting Contrave. Using opioids in the 7 to 10 days before you start may cause you to suddenly have symptoms of opioid withdrawal when you take it. Sudden opioid withdrawal can be severe, and you may need to go to the hospital. Tell your healthcare provider about all the medications you are taking before a medical procedure or surgery.
• Severe allergic reactions. Some people have had a severe allergic reaction to bupropion, one of the active ingredients. Stop taking this medicine and call your healthcare provider or go to the nearest hospital emergency room right away if you have any of the following signs and symptoms of an allergic reaction:
  • rash
  • painful sores in your mouth or around your eyes
  • itching
  • hives
  • swelling of your lips or tongue
  • fever
  • chest pain
  • swollen lymph glands
  • trouble breathing
• Increases in blood pressure or heart rate. Some people may get high blood pressure or have a higher heart rate when taking this medicine. Your healthcare provider should check your blood pressure and heart rate before you start taking, and while you take Contrave.
• Liver damage or hepatitis. One of the ingredients, naltrexone can cause liver damage or hepatitis. Stop taking this medicine and tell your healthcare provider 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
  • tiredness
  Your healthcare provider may need to stop treatment if you get signs or symptoms of a serious liver problem.
• Manic episodes. One of the ingredients, bupropion can cause some people who were manic or depressed in the past to become manic or depressed again.
• Visual problems (angle-closure glaucoma). One of the ingredients, bupropion, can cause some people to have visual problems (angle-closure glaucoma). Signs and symptoms of angle-closure glaucoma may include:
  • eye pain
  • changes in vision
  • swelling or redness in or around the eye
  Talk with your healthcare provider to find out if you are at risk for angle-closure glaucoma and to get treatment to prevent it if you are at risk.
• Increased risk of low blood sugar (hypoglycemia) in people with type 2 diabetes mellitus who also take medicines to treat their diabetes. Weight loss can cause low blood sugar in people with type 2 diabetes mellitus who also take medicines used to treat type 2 diabetes mellitus (such as insulin or sulfonylureas). You should check your blood sugar before you start taking this medicine and during treatment.

The most common side effects include:

• nausea
• dizziness
• constipation
• trouble sleeping
• headache
• dry mouth
• vomiting
• 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. For more information, ask your healthcare provider or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Storage

Store tablets at room temperature between 59°F to 86°F (15°C to 30°C).

Keep all medicines out of the reach of children.

General information

Medicines are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use this medicine for a condition for which it was not prescribed. Do not give it to other people, even if they have the same symptoms or condition that you have. It may harm them.

If you take a urine drug screening test, Contrave may make the test result positive for amphetamines. If you tell the person giving you the drug screening test that you are taking Contrave, they can do a more specific drug screening test that should not have this problem.

This Medication Guide summarizes the most important information. If you would like more information, talk with your healthcare provider. You can ask your pharmacist or healthcare provider for information that is written for health professionals.

Ingredients

Active ingredients: naltrexone hydrochloride and bupropion hydrochloride

Inactive ingredients: microcrystalline cellulose, hydroxypropyl cellulose, lactose anhydrous, L-cysteine hydrochloride, crospovidone, magnesium stearate, hypromellose, edetate disodium, lactose monohydrate, colloidal silicon dioxide, Opadry II Blue and FD&C Blue #2 aluminum lake

I took this drug for a month of my supervised diet requirement made me dizzy, flat and not eat at all. I am not trying to starve myself and create even worse eating habits. I am currently on belviq until my surgery in March so, I'll see how that goes.

This medication made me sick. Migraine, nausea, and an overall strange feeling. I didn’t like being on this at all.

I have a few questions.

Are you dependent on weight loss medication long term?

What is the rate of regain after patients go off the medication?

Do Dr's give patients supervised weight loss with nutrition consults and behavior changes along with a prescription?

What is the long term success rate?