Generic Contrave (Bupropion + Naltraxone)

Introduction

Contrave is a prescription medication that combines two active agents, bupropion hydrochloride and naltrexone hydrochloride, in a fixed-dose tablet (8 mg/90 mg). It is classified as a centrally acting weight-management drug and is approved in the United States, European Union and several other jurisdictions for chronic obesity treatment in adults with a body-mass index (BMI) ≥ 30 kg/m², or BMI ≥ 27 kg/m² when accompanied by at least one weight-related comorbidity such as hypertension, type 2 diabetes, or dyslipidemia. The product is manufactured by GlaxoSmithKline (GSK) and is marketed under the brand name Contrave; related combination products are also sold under names such as Qsymia.

The medication is taken as a once-daily oral pill and is intended to be used together with a reduced-calorie diet and increased physical activity. Although its primary indication is weight management, the individual components have separate therapeutic roles (bupropion as an antidepressant and smoking-cessation aid; naltrexone as an opioid antagonist), which leads to occasional off-label exploration of the combination for other conditions.

What is Contrave?

• Classification: Fixed-dose combination anti-obesity agent (bupropion + naltrexone).
• Active ingredients: 8 mg bupropion hydrochloride and 90 mg naltrexone hydrochloride per tablet.
• Manufacturer: GlaxoSmithKline (GSK).
• Development history: The concept originated from pre-clinical studies showing that simultaneous antagonism of hypothalamic melanocortin pathways (via naltrexone) and enhancement of catecholamine signaling (via bupropion) could reduce appetite and increase energy expenditure. After Phase III trials demonstrated a statistically significant weight-loss benefit versus placebo, the combination received regulatory approval in 2014 (FDA) and later in the EU (EMA).

Contrave is not a generic; it is the proprietary formulation containing the specific 8/90 mg ratio that was studied in the pivotal trials.

How Contrave Works

1. Bupropion component - Bupropion blocks the reuptake of dopamine and norepinephrine, increasing their synaptic concentrations. In the hypothalamus, elevated dopamine stimulates pro-opiomelanocortin (POMC) neurons, which produce α-melanocyte-stimulating hormone (α-MSH). Activation of the melanocortin-4 receptor (MC4R) downstream leads to reduced appetite and increased thermogenesis.

2. Naltrexone component - Naltrexone is an opioid-receptor antagonist that blunts the autoinhibitory feedback loop on POMC neurons mediated by endogenous β-endorphin. By preventing this feedback, naltrexone sustains the POMC-driven appetite-suppressing signal initiated by bupropion.

The synergistic action results in a net decrease in caloric intake and modest elevation of resting energy expenditure. Clinical pharmacokinetics show a steady-state plasma concentration reached after 5-7 days of daily dosing; the half-life of bupropion is ~21 hours, while naltrexone’s half-life is ~ hours, but its active metabolite (6-β-hydroxynaltrexone) extends the pharmacodynamic effect.

Conditions Treated with Contrave

• Chronic obesity (BMI ≥ 30 kg/m²)

  • Why effective: The dual neurotransmitter modulation targets central appetite regulation, producing an average 5-10 % reduction in body weight after one year when combined with lifestyle changes, as shown in the COR-I and COR-II pivotal trials.

• Obesity with comorbidities (BMI ≥ 27 kg/m² plus hypertension, type 2 diabetes, or dyslipidemia)

  • Why effective: Weight loss of ≥ 5 % improves insulin sensitivity, blood pressure, and lipid profiles, thereby addressing the associated metabolic risk factors.

No other indications have received formal approval from the U.S. Food and Drug Administration (FDA), the European Medicines Agency (EMA), or Health Canada.

Off-Label and Investigational Uses of Contrave

Important: Offlabel applications have not undergone the rigorous safety and efficacy evaluation required for official approval. Any consideration of such uses must be made under direct supervision of a qualified healthcare professional.

Is Contrave the Right Medication for You?

• Ideal candidates

  • Adults aged ≥ 18 years with BMI 30 kg/m², or BMI ≥ 27 kg/m² plus at least one obesity-related comorbidity.
  • Individuals who have been unable to achieve meaningful weight loss through diet and exercise alone.
  • Patients who can adhere to a daily dosing schedule and are motivated to maintain lifestyle modifications.

• Clinical scenarios where Contrave is often recommended

  • When a patient has and prefers a non-surgical, pharmacologic adjunct.
  • When the patient also has a history of depression or nicotine dependence, as the bupropion component may provide secondary mood or cessation benefits.

• Contra-indications

  • Current use of monoamine-oxidase inhibitors (MAOIs) or a history of MAOI use within the past 14 days.
  • Uncontrolled hypertension (SBP ≥ 160 mm Hg or DBP ≥ 100 mm Hg).
  • History of seizure disorder, eating disorders (e.g anorexia nervosa, bulimia), or abrupt discontinuation of alcohol, benzodiazepines, or opioids.
  • Pregnant or breastfeeding individuals (lack of sufficient safety data).
  • Severe hepatic impairment (Child-Pugh class C).

Patients with any of these contraindications should discuss alternative weight-management strategies with their provider.

Risks, Side Effects, and Interactions

Common

• Nausea (up to 30 % of users)
• Constipation
• Headache
• Dry mouth
• Dizziness
• Insomnia

These events are usually mild to moderate and often improve after the first two weeks of therapy.

Rare

• Elevated liver enzymes (ALT/AST)
• Taste disturbances (dysgeusia)
• Mood changes (e.g., irritability)

Routine laboratory monitoring is in patients with pre-existing liver disease.

Serious

• Seizures - Bupropion lowers the seizure threshold, especially at doses > 450 mg/day; the fixed-dose combination mitigates this risk but does not eliminate it.
• Hypertensive crisis - May occur if the medication is taken with monoamine-oxidase inhibitors or in patients with uncontrolled hypertension.
• Suicidal thoughts - As with other antidepressants, an increase in suicidal ideation has been observed, particularly in young adults.
• Severe allergic reactions - Rash, angioedema, or anaphylaxis require immediate medical attention.

Interactions

• MAO inhibitors - Concomitant use is contraindicated; a washout period of at least 14 days is required.
• CYP2B6 substrates (e.g., efavirenz, cyclophosphamide) - Bupropion can inhibit CYP2B6, potentially raising plasma levels of these drugs.
• Alcohol - Acute alcohol intake may increase the risk of seizures and should be avoided, especially during dose titration.
• Other weight-loss agents (e.g., phentermine, orlistat) - Combined use can amplify cardiovascular side-effects and is not recommended.

Patients should provide a complete medication list, including over-the-counter products and supplements, before initiating Contrave.

Use: Dosing, Missed Dose, Overdose

• Standard dosing regimen
  1. Week 1-3 (titration phase): 1 tablet daily (morning).
  2. Week 4-6: 2 tablets daily (morning and evening).
  3. Week 7 onward (maintenance): 3 tablets daily (morning, midday, evening).

The titration schedule reduces gastrointestinal intolerance and allows the body to adjust to the central nervous system effects.

• Missed dose

  • If a dose is missed and it is less than 12 hours until the next scheduled dose, skip the missed tablet and continue with the regular dosing schedule.
  • Do not double-dose to compensate for a missed tablet, as this raises the risk of hypertension, seizures, and insomnia.

• Suspected overdose

  • Signs may include severe nausea, vomiting, agitation, tremor, or seizures.
  • Seek emergency medical care immediately; provide information on the amount ingested and the time of ingestion.
  • Supportive care, activated charcoal, and seizure control are the mainstays of treatment in a hospital setting.

• Administration considerations

  • Take tablets with a full glass of water; they can be taken with or without food, but consistent timing helps maintain stable blood levels.
  • Limit alcohol consumption, as it can potentiate central nervous system side-effects and seizure risk.
  • Operating heavy machinery or driving may be impaired during the first weeks; patients should assess their alertness before engaging in such activities.

FAQ

• How should I store Contrave tablets?

  • Store at room temperature (15-30 °C / 59-86 °F) away from moisture and direct sunlight. Keep the bottle tightly closed and out of reach of children.

• Can I travel internationally with Contrave?

  • Yes, but carry the medication in its original labeled container, include a copy of the prescription (or a physician’s letter if required), and verify the import regulations of the destination country beforehand.

• What does the Contrave pill look like?

  • The tablet is white, filmcoated, and oval-shaped, embossed with “8/90” on one side to denote the bupropion/naltrexone dosage.

• Are there any inactive ingredients that might cause allergies?

  • Inactive components include microcrystalline cellulose, magnesium stearate, and lactose monohydrate. Patients with lactose intolerance should discuss alternatives with their provider.

• Will Contrave affect routine blood tests?

  • The medication can cause modest elevations in liver enzymes; periodic liver function testing is recommended, especially in patients with pre-existing hepatic conditions.

• Is it safe to use Contrave while on hormonal birth control?

  • No clinically significant pharmacokinetic interaction has been identified; however, weight loss itself may alter levels, so continued contraception monitoring is advisable.

• Can I take Contrave if I have type 2 diabetes?

  • Yes, patients with type 2 diabetes are among the approved comorbidity groups; weight loss can improve glycemic control, but glucose levels should be monitored regularly.

• Does Contrave supplements such as St. John’s Wort?

  • St. John’s Wort induces CYP3A4 and may reduce bupropion concentrations, potentially diminishing efficacy. Discuss all supplements with a healthcare professional.

• How long does it take to see weight-loss results?

  • Clinical data show a mean weight reduction of 5 % body weight after 12 weeks of therapy, with continued loss up to 10 % after one year when combined with diet and exercise.

• What should I do if I experience severe nausea?

  • Take the medication with food, split the dose (morning/evening) if tolerated, and contact a clinician if nausea persists beyond two weeks, as dose adjustment may be required.

Glossary

Bupropion

An antidepressant that inhibits the reuptake of dopamine and norepinephrine, thereby increasing their synaptic availability.

Naltrexone

An opioid-receptor antagonist that blocks the effects of endogenous and exogenous opioids; in Contrave, it prolongs the appetite-suppressing signal from POMC neurons.

POMC neurons

Pro-opiomelanocortin neurons located in the arcuate nucleus of the hypothalamus; activation leads to production of melanocortins that reduce food intakeTherapeutic window

The dosage range in which a drug provides clinical benefit without causing unacceptable adverse effects.

Buying Contrave from Our Online pharmacy

Patients who encounter limited availability, high out-of-pocket costs, or long wait times at traditional pharmacies may consider obtaining Contrave through our online pharmacy. Our service partners with licensed overseas pharmacies that source medication directly from approved manufacturers, ensuring that each package meets stringent quality standards.

• Cost-effectiveness: Prices are set close to the wholesale acquisition cost, resulting in a lower overall expense compared with many domestic retail pharmacies.
• Verified quality: All shipments are tracked and accompanied by authentic batch numbers and tamper-evident packaging, guaranteeing that you receive the exact formulation studied in clinical trials.
• Discreet delivery: Packages are shipped in unmarked, secure envelopes, and the billing statements use neutral language to protect your privacy. Standard international shipping typically arrives within 7 days for express service or 2-3 weeks for regular airmail.
• Convenient access: The pharmacy broker model enables customers in regions where Contrave is not locally marketed to obtain the medication legally and safely, without the need for a local prescriber to hold stock.

Our platform is designed to help patients focus on their health goals rather than logistical hurdles.

Disclaimer

The material presented here about Contrave is intended solely for general informational purposes and does not substitute for professional medical advice. All therapeutic decisions, including those concerning off-label applications, must be made under the direct oversight of a qualified healthcare provider. Readers are presumed to be competent adults capable of evaluating health information responsibly. Our online pharmacy supplies Contrave to individuals who may experience limited access through conventional pharmacies or insurance plans, or who are seeking cost-effective generic alternatives. Always consult a physician before initiating, modifying, or discontinuing any medication.