Naltrexone & Bupropion

Naltrexone and bupropion is a prescription medication used to assist with weight management in adults who are obese or overweight with weight-related medical problems. It must be used along with a healthy diet and exercise plan.

It is a single product containing 2 medications: naltrexone and bupropion. Naltrexone belongs to a group of drugs called opioid antagonists. These are believed to work by decreasing appetite. Bupropion belongs to a group of drugs called antidepressants. These work by increasing the activity of certain chemicals in the reward pathways of the brain. The exact ways in which naltrexone and bupropion help in weight loss are not understood.

This medication comes in extended-release tablet form and is taken 2 times a day, in the morning and in the evening. Do not take naltrexone and bupropion with high-fat meals. Do not take Contrave with high-fat meals. Do not chew, crush, or cut the tablets.

Common side effects of naltrexone and bupropion include nausea, constipation, headache, vomiting, insomnia, dry mouth, and diarrhea.

Naltrexone and bupropion can also cause changes in vision, drowsiness, and dizziness. Do not drive or operate heavy machinery until you know how naltrexone and bupropion affects you.

Naltrexone and bupropion is a prescription medication used to assist with weight management in adults who are obese or overweight with weight-related medical problems. Naltrexone and bupropion 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 (hypertension), type 2 diabetes, or high cholesterol (dyslipidemia). It must be used along with a healthy diet and exercise plan. This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Take this medication exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

The dose your doctor recommends may be based on the following:

• the condition being treated
• other medical conditions you have
• other medications you are taking
• how you respond to this medication

The dose of naltrexone and bupropion should be gradually escalated over 3 weeks until a maintenance dose of 2 8-mg/90-mg tablets twice daily is reached.

WARNING: SUICIDAL THOUGHTS AND BEHAVIORS; AND NEUROPSYCHIATRIC REACTIONS

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.

NEUROPSYCHIATRIC REACTIONS IN PATIENTS TAKING BUPROPION FOR SMOKING CESSATION

Serious neuropsychiatric reactions have occurred in patients taking bupropion for smoking cessation. The majority of these reactions occurred during bupropion treatment, but some occurred in the context of discontinuing treatment. In many cases, a causal relationship to bupropion treatment is not certain, because depressed mood may be a symptom of nicotine withdrawal. However, some of the cases occurred in patients taking bupropion who continued to smoke. Although CONTRAVE is not approved for smoking cessation, observe all patients for neuropsychiatric reactions. Instruct the patient to contact a healthcare provider if such reactions occur.

Serious side effects have been reported with naltrexone and bupropion including the following:

• Mental health changes. You, your family, or your caregiver should call your doctor right away if you experience any of the following symptoms: panic attacks; agitation or restlessness; new or worsening irritability, anxiety, or depression; acting on dangerous impulses; difficulty falling or staying asleep; aggressive, angry, or violent behavior; mania (frenzied, abnormally excited mood); talking or thinking about wanting to hurt yourself or end your life; withdrawing from friends and family; preoccupation with death and dying; giving away prized possessions; or any other unusual changes in behavior or mood. Be sure that your family or caregiver knows which symptoms may be serious so they can call the doctor if you are unable to seek treatment on your own.
• Seizures. Bupropion, a component of naltrexone and bupropion, can cause seizures. Naltrexone and bupropion should be used cautiously in patients with a history of head trauma or prior seizure, stroke, central nervous system dysfunctions or infections, certain metabolic disorders, diabetes, or drug or alcohol use or abuse.
• Increased heart rate and blood pressure. Heart rate and blood pressure should be monitored before starting naltrexone and bupropion and regularly during treatment.
• Vision changes, including secondary angle closure glaucoma. Tell your health care provider if you experience any of the following symptoms:
  • changes in visual acuity
  • eye pain
  • eye redness
• Allergic reaction. Tell your health care provider if you experience any of the following symptoms:
  • skin rash
  • itching
  • hives
  • chest pain
  • swelling of the hands, feet, legs, face, neck, or tongue
  • shortness of breath

Naltrexone and bupropion can also cause changes in vision, drowsiness, and dizziness. Do not drive or operate heavy machinery until you know how naltrexone and bupropion affects you.

Do not take naltrexone and bupropion if you:

• are allergic to naltrexone and bupropion or to any of its ingredients
• have uncontrolled hypertension
• have a seizure disorder or a history of seizures
• use other bupropion-containing products (including, but not limited to, Wellbutrin, Wellbutrin SR, Wellbutrin XL, and Aplenzin)
• have bulimia or anorexia nervosa, which increase the risk for seizure
• use a chronic opioid or opiate agonist (e.g., methadone) or partial agonists (e.g., buprenorphine) use or are experiencing acute opiate withdrawal
• are undergoing an abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and antiepileptic drugs
• have used a monoamine oxidase inhibitors (MAOI) in the last 14 days
• are pregnant

Serious side effects have been reported with naltrexone and bupropion. See the “Naltrexone and bupropion Precautions” section.

Common side effects of naltrexone/bupropion include the following:

• nausea
• constipation
• headache
• vomiting
• dizziness
• insomnia
• dry mouth
• diarrhea
• dizziness

This is not a complete list of naltrexone/bupropion side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

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

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• a monoamine oxidase inhibitor (MAOI) including isocarboxazid (Marplan), phenelzine (Nardil), selegiline (Eldepryl, Emsam, Zelapar), and tranylcypromine (Parnate), or if you have taken one of these medications during the past two weeks
• antidepressants including paroxetine (Paxil), nortiptyline (Pamelor), amitriptyline, and imipramine (Tofranil)
• amantadine (Symmetrel)
• amiloride (Midamor)
• antiarrhythmics including flecainide (Tambacor) and propafenone (Rythmol)
• antipsychotics including haloperidol (Haldol), risperdone (Risperdal), and thioridazine
• antiplatelet agents including ticlopidine (Ticlid) and clopidogrel (Plavix)
• beta-blockers including metoprolol (Lopressor)
• cimetidine (Tagamet)
• dopamine
• efavirenz (Sustiva)
• famotidine (Pepcid)
• levodopa
• lopinavir (in Kaletra)
• memantine (Namenda)
• metformin (Glumetza, Fortamet, Glucophage, Riomet)
• opioid pain relievers including meperidine (Demerol), hydromorphone (Dilaudid), oxycodone (OxyContin, Roxicodone, Oxecta, in Percocet)
• oxaliplatin (Eloxatin)
• pindolol (Visken)
• procainamide (Pronestyl, Procan, Procanbid)
• ranitidine (Zantac)
• ritonavir (Norvir)
• systemic corticosteroids including prednisone (Prednisone Intensol), prednisolone (Orapred, Prelone), and methylprednisolone (Medrol, Depo-Medrol, Solu-Medrol)
• theophylline (Theo-24, Theolair, Uniphyl, Elixophylline, Elixophyllin, Quibron-T)
• varenicline (Chantix)

This is not a complete list of naltrexone and bupropion drug interactions. Ask your doctor or pharmacist for more information.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X - are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Naltrexone and bupropion falls into category X. It has been shown that women taking naltrexone and bupropion during pregnancy may have babies born with problems. There are no situations where the benefits of the medication for the mother outweigh the risks of harm to the baby. These medicines should never be used by pregnant women.

Tell your doctor if you are breastfeeding or plan to breastfeed.

Naltrexone and bupropion has been detected in human breast milk. Because of the possibility for adverse reactions in nursing infants from naltrexone and bupropion, a choice should be made whether to stop nursing or to stop use of this medication. Naltrexone and bupropion is not recommended for nursing mothers.