BuPROPion-naltrexone

Bupropion is an antidepressant medicine that can also decrease appetite. Naltrexone is usually given to block the effects of narcotics or alcohol in people with addiction problems. Naltrexone may also curb hunger and food cravings.

Bupropion and naltrexone is a combination medicine used to help manage weight in obese or overweight adults with weight-related medical problems. This medicine is used together with diet and exercise.

Bupropion and naltrexone is for use only to help you manage your weight. This medicine will not treat any weight-related medical condition, such as high blood pressure, diabetes, or high cholesterol.

Although bupropion is an antidepressant and is sometimes used to help people quit smoking, Contrave is not approved to treat depression or other psychiatric conditions, or to help you quit smoking.

Bupropion and naltrexone may also be used for purposes not listed in this medication guide.

You should not use this medicine if you have uncontrolled high blood pressure, seizures, an eating disorder, kidney failure, if you are pregnant or breast-feeding, or if you have recently stopped using seizure medicine. Do not take this medicine if you also take narcotic medicine or other forms of bupropion (such as Wellbutrin or Zyban), or if you are going through withdrawal from alcohol or drug addiction.

Do not use bupropion and naltrexone if you have used an MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, tranylcypromine, and others.

Do not use bupropion and naltrexone if you are pregnant.

Some young people have thoughts about suicide when first taking bupropion. Your doctor will need to check your progress at regular visits while you are using this medicine. Your family or other caregivers should also be alert to changes in your mood or symptoms.

You should not use this medicine if you are allergic to bupropion or naltrexone, or if you have:

• untreated or uncontrolled high blood pressure;
• an eating disorder (anorexia or bulimia);
• a history of seizures;
• kidney failure (end-stage kidney disease);
• if you are pregnant or breast-feeding;
• if you have recently stopped using seizure medicine suddenly;
• if you have taken any narcotic (opioid) medicine within the past 10 days;
• if you are going through withdrawal from alcohol or drug addiction; or
• if you also take bupropion (Wellbutrin, Aplenzin, Budeprion, Forfivo, Zyban, and others).

Do not use bupropion and naltrexone if you have used an MAO inhibitor in the past 14 days. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, tranylcypromine, and others.

To make sure bupropion and naltrexone is safe for you, tell your doctor if you have:

• past or present depression, mental illness, suicidal thoughts, bipolar disorder (or a family history of bipolar disorder, depression, or suicide);
• a history of addiction to drugs or alcohol;
• narrow-angle glaucoma;
• diabetes, or a history of low blood sugar;
• heart disease, high blood pressure, history of stroke or blood clot;
• liver or kidney disease;
• a history of head injury;
• a history of tumor or infection in your brain or spinal cord;
• if you normally drink a lot of alcohol; or
• if you have taken buprenorphine or methadone in the past 14 days.

Some young people have thoughts about suicide when first taking bupropion. Your doctor will need to check your progress at regular visits while you are using this medicine. Your family or other caregivers should also be alert to changes in your mood or symptoms.

This medicine can harm an unborn baby or cause birth defects. Do not use bupropion and naltrexone if you are pregnant. Use effective birth control while taking this medicine and tell your doctor right away if you become pregnant.

Bupropion and naltrexone can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.

This medicine is not approved for use by anyone younger than 18 years old.

Do not use narcotic medication, methadone, heroin, or other street drugs while you are taking bupropion and naltrexone. Doing so could result in dangerous effects, including coma and death.

Drinking alcohol with bupropion may increase your risk of seizures. If you drink alcohol regularly, talk with your doctor before changing the amount you drink. Bupropion can also cause seizures in a regular drinker who suddenly stops drinking at the start of treatment with bupropion and naltrexone.

Follow your doctor's instructions about any restrictions on food, beverages, or activity. Do not take other weight-loss products or diet pills unless your doctor has told you to.

Naltrexone will block the effects of any narcotic medicines you take (such as prescription medicine for pain, cough, or diarrhea). Harmful side effects could also occur.

Many drugs can interact with bupropion and naltrexone, and some drugs should not be used together. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide. Tell your doctor about all medicines you use, and those you start or stop using during your treatment with bupropion and naltrexone. Give a list of all your medicines to any healthcare provider who treats you.

Black Box Warning

Not approved for treatment of major depressive disorder or psychiatric disorders

Antidepressants like bupropion increase the risk of suicidal thoughts and behavior in children, adolescents, and young adults in short-term trials but were not seen in patients ≥24 years and a lower risk was seen in patients ≥65 years; patients of all ages should be monitored closely for suicidal thoughts and behaviors

Serious neuropsychiatric reactions reported in patients taking bupropion for smoking cessation that occurred during therapy or while discontinuing therapy; patients should be monitored for neuropsychiatric reactions

Contraindications

Uncontrolled hypertension

Seizure disorder or a history of seizures

Use of other bupropion-containing products

Bulimia or anorexia nervosa, which may increase risk of seizures

Long-term opioid or opiate agonists use or acute opiate withdrawal

Patients undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs

Within 14 days of monoamine oxidase inhibitor therapy

Hypersensitivity

Pregnancy

Cautions

Monitor patients for suicidal ideation or behavior and for unusual changes in behavior (see black box warning)

Discontinue therapy and do not restart if seizure occurs while on therapy; use caution when prescribing to patients with predisposing risk factors for seizures

Not for administration to patients receiving long-term opioids, owing to naltrexone component (opioid antagonist); discontinue therapy if long-term opiate therapy required

Following therapy, patients may be more sensitive to opioids, even at lower doses

A patient should not attempt to overcome naltrexone opioid blockade by administering large amounts of exogenous opioids; may lead to fatal overdose

Opioid-dependent patients, including those being treated for alcohol dependence, should be opioid-free (including tramadol) before therapy is initiated; opioid-free interval of a minimum of 7-10 days is recommended for patients previously dependent on short-acting opioids; patients transitioning from buprenorphine or methadone may need as long as 2 weeks

Blood pressure and pulse should be measured prior to starting therapy and should be monitored at regular intervals, particularly among patients with controlled hypertension prior to treatment

Discontinue therapy if symptoms or signs of acute hepatitis occur

Screen patients for a history of bipolar disorder and the presence of risk factors for bipolar disorder; therapy was not studied in patients receiving antidepressant medications patients with a history of bipolar disorder or recent hospitalization foor psychiatric illness were excluded from clinical trials

Angle-closure attack may occur in patients with anatomically narrow angles that do not have a patent iridectomy

Measure blood glucose levels prior to and during therapy; patients who develop hypoglycemia after initiating Contrave therapy should adjust antidiabetic drug regimen

Use caution in patients with history of tumor or infection of the brain or spine

Initiation of therapy in patients receiving linezolid or intravenous (IV) methylene blue

Use caution in hepatic impairment

May precipitate a manic, mixed, or hypomanic episode; risk higher in patients with bipolar disorders or have risk factors for bipolar disorder, including family history of bipolar disorder, suicide, or depression; not FDA approved for bipolar depression

Some patients who stopped smoking reported to have experienced symptoms of nicotine withdrawal, including depressed mood; depression, rarely including suicidal ideation, reported in smokers undergoing a smoking cessation attempt without medication; however, some of these adverse events occurred in patients taking bupropion who continued to smoke

Neuropsychiatric adverse events reported in patients without and with pre-existing psychiatric disease; some patients experienced worsening of their psychiatric illnesses; observe patients for occurrence of neuropsychiatric adverse events; patient should stop therapy and contact healthcare provider immediately if agitation, depressed mood, or changes in behavior or thinking that are not typical for patient are observed, or if patient develops suicidal ideation or suicidal behavior; symptoms may persist after discontinuation of therapy; in some cases; monitoring and supportive care should be provided until symptoms resolve

Pregnancy category: X

Lactation: Not recommended

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

Oral Administration

Take by mouth in the morning and evening

Do not crush, chew, or cut tablets

Doses >32 mg/360 mg per day not recommended

Do not administer with high-fat meal as it may result in significant increase in bupropion and naltrexone exposure

Therapy may cause elevation in blood pressure or heart rate, especially during initial 3 months of therapy; patients with hypertension should be monitored closely