Bupropion and naltrexone

Do not use this medicine if you are pregnant. Weight loss during pregnancy can harm an unborn baby, even if you are overweight. Tell your doctor right away if you become pregnant during treatment.

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;

• opioid addiction or withdrawal (or if you take methadone or buprenorphine);

• if you take other forms of bupropion (Wellbutrin, Aplenzin, Budeprion, Forfivo, Zyban, and others); or

• if you have suddenly stopped using alcohol, seizure medication, or a sedative such as Xanax, Valium, Fiorinal, Klonopin, and others).

Do not use an MAO inhibitor within 14 days before or 14 days after you take bupropion and naltrexone. A dangerous drug interaction could occur. MAO inhibitors include isocarboxazid, linezolid, phenelzine, rasagiline, selegiline, and tranylcypromine.

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

• depression, bipolar disorder, or mental illness;

• suicidal thoughts or actions;

• a head injury;

• a tumor or infection in your brain or spinal cord;

• diabetes or low blood sugar;

• low sodium levels;

• liver or kidney disease;

• heart disease, high blood pressure, heart attack, or stroke; or

• drug addiction, or if you normally drink a lot of alcohol.

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

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.

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.

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.

Initial dose:
-Week 1: One tablet (8 mg naltrexone/90 mg bupropion) orally once in the morning; then
-Week 2: One tablet orally twice a day (once in the morning and once in the evening); then
-Week 3: Two tablets orally in the morning and one tablet orally in the evening
Maintenance dose: Week 4 and onward: Two tablets orally twice a day (morning and evening)
Maximum dose: Two tablets orally twice a day

Comments:
-Discontinue therapy if a patient has not lost at least 5% of baseline body weight after 12 weeks at the maintenance dose.
-The effect of this drug on cardiovascular morbidity and mortality has not been established.
-The safety and effectiveness of this drug in combination with other products intended for weight loss, including prescription drugs, over-the-counter drugs, and herbal preparations, have not been established.

Use:
An adjunct to a reduced-calorie diet and increased physical activity for chronic weight management in adults with an initial body mass index (BMI) of:
-30 kg/m2 or greater (obese) or
-27 kg/m2 or greater (overweight) in the presence of at least one weight-related comorbid condition (e.g., hypertension, type 2 diabetes mellitus, or dyslipidemia)

-Maximum dose: One tablet orally once a day in the morning

-Mild renal impairment: Data not available
-Moderate to severe renal impairment: Maximum maintenance dose: One tablet orally twice a day (once in the morning and once in the evening)
-End-stage renal disease: Not recommended

US BOXED WARNING:
-SUICIDAL THOUGHTS AND BEHAVIORS: This drug contains bupropion, which is the active ingredient in some antidepressant medications. Antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults in short-term trials. Monitor patients for worsening and emergence of suicidal thoughts and behaviors. This drug is not approved for use in pediatric patients or in the treatment of major depressive disorder or other psychiatric disorders.
-NEUROPSYCHIATRIC REACTIONS: Serious neuropsychiatric events have occurred in patients taking bupropion for smoking cessation. In many cases, a causal relationship to bupropion treatment is not certain. Although this drug is not approved for smoking cessation, observe patients for neuropsychiatric reactions.

Safety and efficacy have not been established in patients younger than 18 years.

Consult WARNINGS section for additional precautions.

Not recommended

Use is contraindicated. US FDA pregnancy category: X

There are no adequate and well-controlled data in human pregnancy. However, data from the international bupropion Pregnancy Registry (675 first trimester exposures) and a retrospective cohort study using the United Healthcare database (1,213 first trimester exposures) did not show an increased risk for malformations overall. Animal studies have revealed evidence of increased early fetal loss, decreased fetal weights, increased pseudopregnancy, decreased pregnancy rates, and slightly increased fetal malformations and skeletal variations when naltrexone and bupropion were administered separately in doses ranging from 15 to 60 times the maximum recommended human dose (MRHD) of the naltrexone component of this drug, and 2 to 5 times the MRHD of the bupropion component of this drug. US FDA pregnancy category X: Studies in animals or humans have demonstrated fetal abnormalities and/or there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience, and the risks involved in use of the drug in pregnant women clearly outweigh potential benefits.