Naltrexone and Bupropion (Oral)

Naltrexone and bupropion is a combination medication administered to obese or overweight patients to aid in weight loss. It does not treat weight related health complications like hypertension, high cholesterol, or diabetes.

Overview

Naltrexone and bupropion is a prescription drug that contains two medicines (naltrexone and bupropion). It is used to help some overweight or obese adults with weight related medical complications lose weight and maintain good health. This medication should be used with a low-calorie diet plan, and appropriate physical exercises. However, naltrexone and bupropion should not be used to treat depression or any form of mental illness, or by those who want to quit smoking.

Naltrexone is an opioid antagonist while bupropion is an inhibitor of the neuronal reuptake of norepinephrine and dopamine. Both naltrexone and bupropion have effects on the two brain areas that regulate food consumption: the hypothalamus (area that regulates appetite) and the mesolimbic dopamine circuit (the area that regulates the amount of food you eat).

While taking naltrexone and bupropion, you and your family members should:

  • Pay very close attention to any changes, especially sudden changes in behavior, mood, thoughts, and feelings. This is important when you start taking the medication or when you change your dose.
  • Honor all follow-up appointments with your healthcare provider so your response to treatment can be assessed. These appointments are also important for looking out for the drug's side effects.

This medication is only available with the doctor's prescription and comes as tablets that should be swallowed whole.

Conditions Treated

  • Overweight

Type Of Medicine

  • Opiate antagonist

Naltrexone and bupropion side effects

Along with the desired effects, some medications tend to cause unwanted effects. Some of these side effects tend to go away as the body adjusts to treatment. However, some side effects may be so severe as to require medical attention.

Check with your healthcare provider as soon as possible if you experience any of the following naltrexone and bupropion side effects.

  • Confusions and hallucinations
  • Blurred vision
  • Dizziness
  • Paranoid feeling
  • Headache
  • Lack of appetite
  • Irritability
  • Loss of interest or pleasure
  • Irregular heartbeat
  • Trouble sleeping
  • Pounding in the ears
  • Unusual tiredness and body weakness
  • Trouble concentrating
  • Bladder pain
  • Burning, painful urination
  • Bloody or cloudy urine
  • Lower side or back pain
  • Trembling and shakiness in the limbs
  • Frequent urge to urinate
  • Sharp chest pain and discomfort
  • Sweating
  • Nausea and vomiting
  • Pain or discomfort in the arms, back, neck, and jaws
  • Sudden change in behavior
  • Suicidal thoughts
  • Aggressive and angry
  • Peeling, blistering, or loosening of the skin
  • Increased episodes of anxiety
  • Frequent coughs
  • Chills
  • Dark urine
  • Clay colored stool
  • Combativeness, delusions of persecution, suspicions, or mistrust
  • Moving with difficulty
  • Diarrhea
  • Dry mouth
  • Swallowing difficulty
  • Paranoia
  • Fever
  • Hyperventilation
  • Itching, hives, or rashes
  • Muscle or joint pains
  • Large, hive-like swellings on the eyelids, face, hands, feet, genitals, tongue, and throat
  • Puffiness or swelling of the eyelids and lips
  • Muscle stiffness
  • Restlessness
  • Red, irritating eyes
  • Severe mood and mental changes
  • Sores, ulcers, or white spots around the lips
  • Sore throat
  • Swelling of the feet and lower legs
  • Stomach pain and tenderness
  • Yellowing of the eyes and skin
  • Unusual behavior
  • Tightness of the chest

Some naltrexone and bupropion side effects may occur that do not require medical attention. These side effects are mild and will often go away as the body adjusts to the drug. Also, your healthcare professional should be able to advise you on how to prevent or reduce the severity of these side effects. However, you may check with your healthcare provider if any of the following side effects persist or become bothersome:

  • Difficulty having a bowel movement
  • Loss or change of taste
  • Feeling of warmth
  • Persistent ringing or buzzing noise in the ears
  • Hearing loss
  • Redness of the face, arms, upper chest and neck
  • Increased sweating
  • Abdominal pains
  • Digestion problems
  • Feeling of constant movement of self and/or surroundings
  • Thinning of hair or hair loss
  • Severe nausea and vomiting
  • Sensation of spinning

Naltrexone and bupropion dosage

Naltrexone and bupropion comes as a tablet that is taken orally. It is should be taken with or without food once per day. Schedule your dosage at around the same time everyday to help you remember. Carefully read and follow the directions on your prescription label, and ask your pharmacist or healthcare provider to explain what you do not understand. It is important that you take naltrexone and bupropion exactly as directed. Never take more or less of it or take it more often than has been prescribed.

Your healthcare provider may recommend that you start naltrexone and bupropion on a low dosage before gradually increasing the dose every two weeks.

What you should avoid when taking naltrexone and bupropion

It is important that you follow your doctor's instructions about any food, beverage, and activity restrictions while on this medication. Do not take any other weight loss product or diet pill without the approval of your healthcare provider.

Avoid narcotic medications such as heroin, methadone, and other street drugs while on naltrexone and bupropion. Using hard drugs while on this medication can result in dangerous effects such as coma and even death.

Alcohol consumption while on bupropion may increase your risk of seizure attacks. If you are an alcoholic, talk to your healthcare provider before adjusting the amount you drink. Bupropion may also trigger a seizure in a regular drinker who stops drinking abruptly.

Usual Adult Dose for Weight Loss:

Starting dose

  • First week: One tablet (8 mg naltrexone/90 mg bupropion) taken by mouth once per day, preferably in the morning

Maintenance dose (Week 4 and onward): Two tablets taken by mouth twice a day (morning and evening). This is the maximum recommended naltrexone and bupropion dose.

Important note:

  • Discontinue therapy if a patient has not lost at least 5% of baseline body weight after 12 weeks at the maintenance dose.

Missing a dose

Take the missed dose as soon as you remember. However, you may skip the missed dose if it is almost time for your next scheduled dose. Do not make up for the missed dose by double dosing. You should never take more than four tablets within 24 hours (one day).

Naltrexone and bupropion overdose

In case of naltrexone and bupropion overdose, contact the local poison control center at 1-800-222-1222. Call the emergency if the overdose victim is unconscious. Symptoms of naltrexone and bupropion overdose include:

  • Dizziness and fainting
  • Slow heart rate
  • Profuse sweating
  • Shaking
  • Confusions
  • Headache
  • Nervousness, irritability, and sudden change of mood and behavior
  • Pale skin
  • General body weakness
  • Numbness and tingling around the mouth
  • Sudden hunger
  • Seizures
  • Jerky or clumsy movement
  • Breathing difficulty
  • Vomiting
  • Fatigue

Naltrexone and bupropion interactions

Drug interactions may affect how the medication works or increase your risk, and severity, of the side effects. Some products that may interact with naltrexone and bupropion include:

  • Narcotic based medications such as hydrocodone and codeine
  • Cough medications such as dextromethorphan
  • Disulfiram
  • Diarrhea medications like diphenoxylate
  • Tamoxifen
  • Pimozide

Taking MAO inhibitors with naltrexone and bupropion may trigger a serious (possibly fatal) drug interaction. Therefore, avoid MAO inhibitors like linezolid, isocarboxazid, methyl blue, phenelzine, moclobemide, procarbazine, safinamide, rasagiline, tranylcypromine, and selegiline while on naltrexone and bupropion. Most MAO inhibitors should never be taken two weeks before and two weeks after naltrexone and bupropion.

Naltrexone and bupropion may interfere with certain laboratory tests such as a urine test for amphetamine, a brain scan for Parkinson's disease, and narcotic drug tests. Be sure to inform your healthcare provider that you are on this medication when going for any laboratory test.

Naltrexone and bupropion warnings

Bupropion, one of the ingredients in naltrexone and bupropion, may increase the risk of suicidal thinking, especially in children, adolescents, and young adults. As such, patients on this medication should be closely monitored for suicidal tendencies and behaviors that might cause self-harm. Naltrexone and bupropion is not approved for treating children under 18 years old.

Discontinue naltrexone and bupropion immediately and contact your healthcare provider if you experience any of the following symptoms: thoughts about self-harm or suicide or dying, severe depression, feeling restless and agitated, anxiety, panic attacks, insomnia, aggression, irritability, anger or violent behavior, acting on dangerous impulses, and any other unusual change in behavior or mood.

Do not take naltrexone and bupropion if you have uncontrolled hypertension, a history of seizures, or use other medications that contain bupropion such as APLENZIN, WELLBUTRIN, or ZYBAN. Also, you should never take this medication if you have an eating disorder, are dependent on opioid medications or are on medications that help stop the use of opioids such as buprenorphine or methadone. Also, you should never use this medication if you are on opiate withdrawal, drink a lot of alcohol and abruptly stop drinking, or are allergic to any of the ingredients of naltrexone and bupropion.

Do not use this medication if you are pregnant or are planning to be pregnant. Severe weight loss during pregnancy can cause harm to your unborn baby even if you are overweight. Inform your healthcare provider right away if you conceive while on this treatment.

Before taking naltrexone and bupropion, tell your healthcare provider about all the medications you are currently taking, including over the counter medications, vitamin and mineral supplements, as well as herbal medications. Do not combine naltrexone and bupropion with any other medication without the approval of your healthcare provider.

Tell your healthcare provider about all your present and past medical conditions, especially if you have suffered from the following: severe depression or mental illness, head injury, attempted suicide, tumor or infections of the brain and spine, seizures, low blood sugar and sodium levels, high blood pressure, kidney and liver failures, heart attack and heart problems, eating disorder, stroke, alcohol and hard drug abuse, diabetes.

Naltrexone and bupropion does not treat any weight-related medical conditions such as diabetes, high blood pressure, or high cholesterol.

Naltrexone and bupropion is not approved for treating depression or any psychiatric condition. It cannot help you quit smoking.

Naltrexone and bupropion may make you dizzy. Combining it with alcohol and hard drugs like marijuana can worsen this condition. Do not drive, operate industrial machinery, or perform any task that requires you to be alert until you can perform it safely. Talk to your doctor if you are using marijuana or drinking alcohol before taking this medication.

Naltrexone and bupropion can be passed to the nursing baby via breast milk. Consult your healthcare provider before taking this medication if you are breastfeeding.

Naltrexone and bupropion and seizures

As already mentioned, bupropion can trigger seizure attacks. The risk of seizure attacks is dose related. Thus, this medication should be permanently discontinued in patients who suffer seizure attacks while on treatment. The risk of seizure attacks is also related to the patient's health condition, concomitant medications that lowers the seizure threshold, as well as clinical situations. These factors should be considered before prescribing this medication to the patient. This medicine is contraindicated in patients with seizure disorders, current or previous diagnosis of bulimia or anorexia nervosa, or undergoing abrupt discontinuation of alcoholic beverages, barbiturates, benzodiazepines, and antiepileptic medications. Naltrexone and bupropion should be prescribed with caution to patients with predisposing factors that can increase their risk of seizure attacks such as:

  • A history of seizure or prior trauma, arteriovenous malformation, stroke, infection or tumor in the central nervous system, or metabolic disorders such as hyponatremia, hypoglycemia, hypoxia, and severe hepatic impairment.
  • Excessive use of sedatives, alcohol, hard drugs, or withdrawal from sedatives
  • Diabetic patients on insulin treatment or oral diabetic medications that may cause hypoglycemia
  • Concomitant administration of medications that may lower the patient's seizure threshold, such as antipsychotics, systemic steroids, tricyclic antidepressants, and theophylline.

Naltrexone and bupropion and opioid analgesics

This medication should never be administered to patients on chronic opioids due to the naltrexone ingredient component, which is an opioid receptor antagonist. The medication should be terminated if the patient requires chronic opiate therapy while on naltrexone and bupropion treatment. In addition, this medication should not be administered to patients who are sensitive to opioids.

Naltrexone and bupropion and allergic reactions

Anaphylactoid reactions are characterized by symptoms such as urticaria, pruritus, dyspnea, and angioedema. In addition, bupropion has been associated with rare cases of erythema multiforme, anaphylactic shock, and Stevens-Johnson syndrome. This medication should be immediately discontinued if the patient develops allergic reactions such as hives, pruritus, skin rashes, edema, chest pain, or shortness of breath while on treatment.

Naltrexone and bupropion and hepatotoxicity

Long term exposure to naltrexone can cause hepatitis and liver dysfunction. Therefore, patients should look out for symptoms of liver problems while on this medication, such as yellowing of the skin and eyes.

Naltrexone and bupropion and activation of mania

Bupropion is a major ingredient in depression medication. Antidepressant medications can trigger mixed, maniac, or hypomanic episodes, with the risk increasing in patients with bipolar disorder or a history of bipolar disorders. Therefore, before administering this medication, the patient should be screened for a history of bipolar disorder or the presence of risk factors of bipolar disorders.

Risk of hypoglycemia in patients with Type 2 diabetes

Severe and rapid weight loss can increase the risk of hypoglycemia in patients with Type 2 Diabetes who are on insulin and/or secretagogues treatment such as sulfonylureas. Therefore, it is important that the patient's blood sugar level is measured prior to and during naltrexone and bupropion treatment. If a patient develops hypoglycemia while on treatment, appropriate adjustments should be made to the antidiabetic medication the patient is presently taking.

Do not take naltrexone and bupropion if you:

  • Have a history of seizures
  • Have uncontrolled high blood pressure
  • Use bupropion containing medications such as Wellbutrin TR, Wellbutrin, Zyban, Aplenzin, and Wllbutrin XL.
  • Have a history of anorexia or bulimia
  • Are dependent on opioid pain medicine
  • Drink a lot of alcohol
  • Are taking a group of drugs called monoamine oxidase inhibitors (MAOIs)
  • Are allergic to naltrexone and bupropion
  • Are pregnant or planning to conceive

Before taking naltrexone and bupropion, tell your doctor about all your medical conditions, including if you:

  • Have suffered depression or any form of mental illness including bipolar disorder
  • Have had seizures
  • Have attempted suicide in the past
  • Have had a head injury
  • Have had a tumor or infection in your spine or brain
  • Have low blood sugar and low blood sodium levels
  • Have high blood pressure
  • Have liver and kidney problems
  • Have had a stroke, heart attack, or other heart problems
  • Are diabetic and on insulin treatment
  • Consume a lot of alcohol
  • Abuse hard drugs
  • Are over 65
  • Are breastfeeding or planning to breastfeed

Storage

Naltrexone and bupropion should be stored in a tight container away from moisture and heat. The medication should be stored at 25 degrees C with excursions permitted to 15 degrees C to 30 degrees C (59 degrees F and 86 degrees F). Store the medicine out of reach of children and pets. Keep away from direct sunlight. Do not keep expired or unused medicine. Ask your healthcare provider how to dispose of medications that you no longer use.

Summary

Naltrexone and bupropion is used in combination with a doctor-approved diet, behavior changes, and exercises to help reduce weight. It is prescribed for people with weight problems, such as people who are obese or have weight related medical complications. Shedding off excess pounds and keeping fit can reduce the risk of health complications associated with obesity such as diabetes, heart diseases, high blood pressure, and shorter life expectancy.

Response to naltrexone and bupropion therapy should be assessed after 12 weeks at the maintenance dosage. The therapy should be discontinued if the patient fails to lose at least 5 percent of their baseline body weight, as it is less likely that the patient will achieve and sustain the desired weight loss with continued medication.

Naltrexone belongs to a class of medicines called opiate antagonists while bupropion is an antidepressant that helps restore certain brain chemicals (neurotransmitters). These two medicines work together on separate parts of the brain to lower the user's appetite and the amount of food they eat.

Other forms of naltrexone and bupropion are administered to treat a variety of conditions such as mood/mental disorders, depression, addiction to narcotic medications, smoking cessation, and alcohol and hard drug abuse.

It is important that you read and understand the Medication Guide and ask any questions you might have before starting naltrexone and bupropion therapy. This medication should be taken orally with a low-fat meal as directed by your healthcare provider usually twice per day in the morning and evening.

Some patients may experience sleeping difficulty when starting this medication. Thus, you should not schedule your evening dose too close to your bedtime.

Naltrexone and bupropion tablet should be swallowed whole. Do not chew or crush the medicine as doing so can release all the drug at once, increasing your risk of suffering side effects like seizures.

Naltrexone and bupropion dosage is based on the patient's medical condition, response to therapy, as well as other medications that the patient might be using. The dosage should be slowly increased (usually after every seven days) to minimize the risk of seizures and the side effects such as insomnia, opiate withdrawal symptoms, and high blood pressure. You should never change your dosage without your healthcare provider's knowledge and approval.

To get the most benefit from it, take your medication on a regular basis. Scheduling your dosage at the same time every day can help you remember to take your medicine. Inform your healthcare provider if you have not lost weight after 16 weeks on naltrexone and bupropion treatment.

Important information

Inform your doctor about all the medications you are currently taking. Many medicines can interact with naltrexone and bupropion, affecting its efficiency.

Do not use this medication if you have uncontrolled high blood pressure, history of seizures, opioid addiction, eating disorder, if you are on any form of narcotic medication, if you have suddenly stopped taking alcohol, or if you are pregnant or breastfeeding.

Some people may develop suicidal thoughts while taking this medication. It is therefore important that you look out for any symptoms of mood changes. Be sure to report new or worsening cases to your healthcare provider.

Avoid taking any MAO inhibitor within 14 days before and 14 days after taking naltrexone and bupropion to avoid dangerous drug interactions. MAO inhibitors include linezolid, isocarboxazid, and phenelzine.

Some patients may develop high blood pressure or heart rate problems while on naltrexone and bupropion treatment. This risk may be greater during the first three months of treatment. Because patients with pre-existing high blood pressure conditions may be at a greater risk of developing blood pressure elevations, such patients should be closely monitored during the entire naltrexone and bupropion treatment period.

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