Naltrexone/bupropion

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Naltrexone/Bupropion

Chemical structures of Bupropion and Naltrexone

Naltrexone/bupropion is a combination medication used for weight management in adults. It combines two drugs: naltrexone, an opioid antagonist, and bupropion, an atypical antidepressant. This combination is marketed under the brand name Contrave, among others.

Mechanism of Action

Naltrexone and bupropion work together to affect the central nervous system. Naltrexone is primarily used to manage alcohol and opioid dependence by blocking the euphoric effects of these substances. Bupropion, on the other hand, is used to treat depression and aid in smoking cessation. When combined, these drugs influence the hypothalamus and the mesolimbic dopamine circuit, which are involved in regulating appetite and energy balance.

Clinical Use

Naltrexone/bupropion is prescribed as part of a comprehensive weight management program that includes a reduced-calorie diet and increased physical activity. It is indicated for use in adults with an initial body mass index (BMI) of 30 kg/m_ or greater (obese) or 27 kg/m_ or greater (overweight) in the presence of at least one weight-related comorbid condition such as hypertension, type 2 diabetes mellitus, or dyslipidemia.

Side Effects

Common side effects of naltrexone/bupropion include nausea, constipation, headache, vomiting, dizziness, insomnia, dry mouth, and diarrhea. Serious side effects may include seizures, increased blood pressure, and liver damage. Patients are advised to monitor for any unusual changes in mood or behavior, as bupropion can increase the risk of suicidal thoughts and behaviors.

Contraindications

Naltrexone/bupropion is contraindicated in patients with uncontrolled hypertension, seizure disorders, a history of anorexia nervosa or bulimia, and those undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and antiepileptic drugs. It is also contraindicated in patients who are currently dependent on chronic opioids or opiate agonists, or who are in acute opiate withdrawal.

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Contributors: Prab R. Tumpati, MD