Generic Bupropion + Naltrexone

Buy Generic Bupropion + Naltrexone () without prescription in Canada

In our Canadian pharmacy, you can buy Bupropion + Naltrexone (Contrave) without a prescription, with delivery across Canada within 5‑14 days. Discreet and anonymous packaging.

Bupropion + Naltrexone, marketed in Canada as Contrave, is a prescription combination medication used to support chronic weight management in adults with obesity or who are overweight with weight‑related medical problems. It works by targeting two key areas of the brain involved in hunger and cravings: the hypothalamic hunger pathways and the mesolimbic reward system. Bupropion, a dopamine and norepinephrine reuptake inhibitor, stimulates pro‑opiomelanocortin (POMC) neurons to reduce appetite and increase energy expenditure, while naltrexone, an opioid antagonist, blocks the natural feedback brake on these neurons, producing a durable and amplified reduction in hunger and food cravings. This two‑way mechanism helps control eating behaviour and supports adherence to a reduced‑calorie diet and increased physical activity.

Usual adult dose: Contrave is titrated slowly over 4 weeks to reduce gastrointestinal side effects. The recommended schedule is: Week 1 – one tablet (8 mg naltrexone / 90 mg bupropion) in the morning; Week 2 – one tablet twice daily (morning and evening); Week 3 – two tablets in the morning and one tablet in the evening; Week 4 onward – two tablets twice daily (total daily dose of 32 mg naltrexone / 360 mg bupropion). Tablets should be swallowed whole, should not be cut, chewed, or crushed, and should not be taken with high‑fat meals. Response should be evaluated after 12 weeks at the maintenance dose; if the patient has not lost at least 5% of baseline body weight, Contrave should be discontinued.

Dosage form: Extended‑release oral tablet containing 8 mg of naltrexone hydrochloride and 90 mg of bupropion hydrochloride.

Onset of action: A reduction in appetite and food cravings may be noticed within the first week of treatment. The full titration to the maintenance dose is achieved over 4 weeks. Clinically meaningful weight loss typically requires 12 to 16 weeks of continuous therapy at the target dose.

Duration of action: The appetite‑suppressing and craving‑reducing effects are maintained with twice‑daily dosing. The elimination half‑life of bupropion is approximately 21 hours and that of naltrexone is approximately 5 hours (with its active metabolite 6‑β‑naltrexol having a half‑life of approximately 13 hours).

Alcohol recommendation: Alcohol consumption should be strictly avoided or limited during treatment with Bupropion + Naltrexone. Excessive alcohol use or abrupt discontinuation of alcohol in heavy drinkers can substantially increase the risk of seizures, and naltrexone may alter the subjective effects of alcohol. Patients should be counselled about the risks of combining alcohol with this medication.

Most common side effects: Nausea (32.5%), constipation (19.2%), headache (17.6%), vomiting (10.7%), dizziness (9.9%), insomnia (9.2%), dry mouth (8.1%), and diarrhoea (7.1%). Nausea is the most frequently reported adverse reaction and is typically mild to moderate and transient, often resolving within 2 to 4 weeks. Approximately 24% of patients in clinical trials discontinued Contrave because of an adverse event, most commonly nausea (6.3%), headache (1.7%), and vomiting (1.1%).

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General Information about Bupropion + Naltrexone (Contrave)

• INN (International Nonproprietary Name): Naltrexone Hydrochloride and Bupropion Hydrochloride
• Brand names available in Canada: Contrave® (Bausch Health, Canada Inc.) is the sole brand‑name product. As of 2026, no generic versions have been approved by Health Canada.
• ATC code: A08AA62 (bupropion and naltrexone; antiobesity preparations, centrally acting antiobesity products)
• Dosage forms and strengths: Extended‑release tablet: naltrexone hydrochloride 8 mg / bupropion hydrochloride 90 mg. Each tablet is a bilayer, film‑coated, extended‑release formulation. Tablets are supplied in bottles of 120.
• Manufacturers in Canada: Bausch Health, Canada Inc. (Contrave). The product was originally distributed by Valeant Canada LP. Currently, Bausch Health is the sole manufacturer and distributor of Contrave in the Canadian market.
• Registration status in Canada: Approved by Health Canada. Notice of Compliance issued 2018/02/13. First marketed in Canada 2018/02/13. DIN: 02472945. Status: Marketed.
• OTC / Rx classification: Prescription only (Rx). Schedule I drug under the Controlled Drugs and Substances Act. Contrave is not a controlled substance or a stimulant, but it requires a valid prescription from a licensed Canadian healthcare professional.

Mechanism of Action and Pharmacology

The mechanism of action of the naltrexone/bupropion combination for weight management is not fully understood, but it is believed to involve complementary actions on hypothalamic and mesolimbic brain pathways. Bupropion is a relatively weak inhibitor of the neuronal reuptake of dopamine and norepinephrine. By increasing the synaptic availability of these catecholamines, bupropion stimulates pro‑opiomelanocortin (POMC) neurons in the arcuate nucleus of the hypothalamus. POMC neurons release alpha‑melanocyte‑stimulating hormone (α‑MSH) and beta‑endorphin. α‑MSH binds to melanocortin‑4 (MC4) receptors and promotes satiety and energy expenditure. However, beta‑endorphin, a μ‑opioid receptor agonist, provides negative auto‑feedback onto POMC neurons, limiting their firing rate. Naltrexone, a potent μ‑opioid receptor antagonist, blocks this auto‑inhibition, thereby amplifying and prolonging the POMC‑mediated anorectic signal. This synergistic interaction—bupropion stimulating POMC firing and naltrexone blocking the opioid‑mediated brake—produces a more robust and durable reduction in appetite and food intake than either agent alone.

Following oral administration, Contrave is formulated as a bilayer extended‑release tablet. Bupropion and naltrexone are both well absorbed. The absolute bioavailability of bupropion is not fully determined, but it undergoes extensive first‑pass hepatic metabolism, primarily via CYP2B6, to its active metabolite hydroxybupropion. Naltrexone undergoes extensive first‑pass metabolism to its primary active metabolite, 6‑β‑naltrexol. The elimination half‑life of bupropion is approximately 21 hours (range 12–30 hours); the elimination half‑life of naltrexone is approximately 5 hours, and that of 6‑β‑naltrexol is approximately 13 hours. Bupropion and its metabolites are excreted primarily in the urine (87%) and to a lesser extent in the faeces (10%). Naltrexone and its metabolites are excreted primarily by the kidney. Contrave should not be taken with high‑fat meals, which can significantly increase systemic exposure to both naltrexone and bupropion and may increase the risk of seizures. The tablets must not be cut, chewed, or crushed.

Indications

• Chronic Weight Management: Contrave is indicated as 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 comorbidity, such as controlled hypertension, type 2 diabetes mellitus, or dyslipidemia.
• The effect of Contrave on cardiovascular morbidity and mortality has not been established.
• Contrave is not indicated for the treatment of major depressive disorder or other psychiatric disorders, although it contains bupropion, the same active ingredient as some antidepressant medications.
• Not recommended for use in paediatric patients; safety and efficacy in children and adolescents under 18 years of age have not been established.

Important Warnings and Precautions

At‑risk groups

• Pregnancy: Contrave should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus. Weight loss offers no potential benefit to a pregnant woman and may result in fetal harm. Contrave is not recommended during pregnancy. Women of childbearing potential should use effective contraception during treatment.
• Breastfeeding: Bupropion and naltrexone are excreted in human breast milk. A decision must be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of the medication to the mother.
• Paediatrics (< 18 years): Safety and efficacy have not been established in children and adolescents. Contrave is not approved for use in paediatric patients.
• Elderly: No dose adjustment is required based on age alone. However, elderly patients may be more sensitive to the adverse effects of the medication, particularly the anticholinergic and CNS effects of bupropion, and are more likely to have decreased renal function. Caution is advised.
• Renal impairment: In patients with moderate or severe renal impairment, the maximum recommended daily dose is two tablets (one tablet each morning and evening). Contrave is not recommended in patients with end‑stage renal disease.
• Hepatic impairment: In patients with moderate hepatic impairment, the maximum recommended daily dose is two tablets (one tablet each morning and evening). Contrave is not recommended in patients with severe hepatic impairment.
• Seizure disorders: Bupropion lowers the seizure threshold. Contrave is contraindicated in patients with a seizure disorder or a history of seizures. The seizure risk is dose‑dependent and is increased in patients with certain medical conditions (head trauma, arteriovenous malformation, CNS tumour or infection, severe stroke), eating disorders (bulimia nervosa or anorexia nervosa), abrupt discontinuation of alcohol or sedatives, and concomitant use of other medications that lower the seizure threshold.
• Suicidality: Contrave contains bupropion, an antidepressant. Antidepressants increased the risk of suicidal thoughts and behaviour in children, adolescents, and young adults in short‑term trials. All patients should be monitored for clinical worsening, suicidality, or unusual changes in behaviour. Contrave is not approved for use in paediatric patients.
• Cardiovascular disease: Contrave may increase blood pressure and heart rate. Blood pressure and pulse should be monitored before and periodically during treatment, particularly in patients with pre‑existing hypertension. Contrave is contraindicated in patients with uncontrolled hypertension.
• Angle‑closure glaucoma: Bupropion may cause pupillary dilation and trigger an acute attack of angle‑closure glaucoma in susceptible individuals. Patients at risk should have an ophthalmologic evaluation before starting therapy.
• Serotonin syndrome: A potentially life‑threatening serotonin syndrome may occur with Contrave, particularly when combined with other serotonergic drugs (e.g., SSRIs, SNRIs, MAOIs, triptans, fentanyl, lithium, tramadol).
• Eating disorders: Contrave is contraindicated in patients with a current or prior diagnosis of bulimia nervosa or anorexia nervosa, as bupropion is associated with an increased risk of seizures in these populations.
• Allergy: Do not take Contrave if you have a known hypersensitivity to naltrexone, bupropion, or any excipient in the formulation.

Driving and alcohol

Contrave may cause dizziness, drowsiness, and impaired cognitive and motor skills. Patients should be cautioned about driving or operating hazardous machinery until they are reasonably certain that the medication does not adversely affect their mental alertness and motor coordination. Alcohol consumption should be strictly avoided or limited during treatment. The combination of Contrave with excessive alcohol use increases the risk of seizures and neuropsychiatric side effects. Naltrexone may alter the subjective effects of alcohol, but it does not prevent the impairing effects of alcohol on motor coordination and judgment.

Dosage Instructions

• Titration schedule (standard dosing): Week 1: one tablet (8 mg naltrexone / 90 mg bupropion) in the morning. Week 2: one tablet twice daily (morning and evening). Week 3: two tablets in the morning and one tablet in the evening. Week 4 onward: two tablets twice daily (total daily dose of 32 mg naltrexone / 360 mg bupropion).
• Administration: Tablets should be swallowed whole with a glass of water and should not be cut, chewed, or crushed. Contrave should not be taken with high‑fat meals because of a significant increase in systemic exposure to both naltrexone and bupropion. The tablets should preferably be taken with a meal or a light snack to improve gastrointestinal tolerance.
• Dose adjustments for hepatic or renal impairment: In patients with moderate hepatic impairment, moderate renal impairment, or severe renal impairment, the maximum recommended daily dose is two tablets (one tablet each morning and evening). Contrave is not recommended in patients with severe hepatic impairment or end‑stage renal disease.
• Concomitant use with CYP2B6 inhibitors: During concomitant use with CYP2B6 inhibitors (e.g., ticlopidine, clopidogrel), the maximum recommended daily dose is two tablets (one tablet each morning and evening).
• Switching to or from an MAOI: At least 14 days must elapse between discontinuation of an MAOI and initiation of Contrave. Conversely, at least 14 days should be allowed after stopping Contrave before starting an MAOI.
• Evaluation of response: Response to therapy should be evaluated after 12 weeks at the maintenance dosage. If a patient has not lost at least 5% of baseline body weight, discontinue Contrave, as it is unlikely that the patient will achieve and sustain clinically meaningful weight loss with continued treatment.
• Missed dose: If a dose is missed, skip the missed dose and take the next dose at the regular time. Do not double the dose.
• Discontinuation: No specific tapering protocol is required when discontinuing Contrave. Abrupt discontinuation has not been associated with a withdrawal syndrome.

Side Effects and Contraindications

• Most common side effects (≥ 5% incidence): Nausea (32.5%), constipation (19.2%), headache (17.6%), vomiting (10.7%), dizziness (9.9%), insomnia (9.2%), dry mouth (8.1%), and diarrhoea (7.1%). Nausea is the most frequently reported adverse reaction and is generally transient, resolving within 2 to 4 weeks of reaching the target dose.
• Other common side effects (2–5%): Upper abdominal pain, fatigue, tremor, anxiety, hot flush, hyperhidrosis (excessive sweating), alopecia, tinnitus, and palpitations.
• Less common but serious side effects: Seizures (dose‑dependent; risk approximately 0.1% at recommended doses), hypertension and increased heart rate, hepatotoxicity (including elevated liver enzymes and rare cases of hepatic failure), activation of mania or hypomania, angle‑closure glaucoma, and hypersensitivity reactions (including anaphylaxis, angioedema, Stevens‑Johnson syndrome).
• Discontinuation rates in clinical trials: 24% of patients receiving Contrave and 12% receiving placebo discontinued treatment because of an adverse event. The most frequent adverse reactions leading to discontinuation were nausea (6.3%), headache (1.7%), and vomiting (1.1%).
• Laboratory abnormalities: Transient elevations in liver enzymes (ALT/AST) may occur. Small mean increases in blood pressure (approximately 1–2 mm Hg systolic) and heart rate (approximately 1–2 bpm) have been observed.
• Contraindications: Uncontrolled hypertension; seizure disorder or a history of seizures; current or prior diagnosis of bulimia nervosa or anorexia nervosa; use of other bupropion‑containing products; chronic opioid or opiate agonist (e.g., methadone) or partial agonist (e.g., buprenorphine) use, or acute opiate withdrawal; patients undergoing abrupt discontinuation of alcohol, benzodiazepines, barbiturates, and antiepileptic drugs; use during or within 14 days following treatment with monoamine oxidase inhibitors (MAOIs), including reversible MAOIs such as linezolid or intravenous methylene blue; known hypersensitivity to naltrexone, bupropion, or any component of the product.

Drug Interactions

• Monoamine oxidase inhibitors (MAOIs) — contraindicated: Concomitant use of Contrave with MAOIs, including linezolid and intravenous methylene blue, is contraindicated. At least 14 days must elapse between discontinuing an MAOI and starting Contrave, and vice versa.
• Other bupropion‑containing products — contraindicated: Contrave is contraindicated in patients taking other bupropion‑containing products (e.g., Wellbutrin, Zyban) due to additive seizure risk and bupropion exposure.
• Opioid analgesics: Naltrexone, an opioid antagonist, may precipitate acute opioid withdrawal in patients who are physically dependent on opioids. Patients must be opioid‑free for at least 7–10 days before starting Contrave. Naltrexone also blocks the analgesic effects of opioids, making standard opioid doses ineffective. Patients requiring emergency pain management should be treated with non‑opioid analgesics, regional anaesthesia, or rapidly reversible benzodiazepine sedation.
• CYP2B6 inhibitors: Ticlopidine and clopidogrel are moderate inhibitors of CYP2B6 and may increase bupropion plasma concentrations. The maximum recommended daily dose of Contrave is two tablets (one tablet each morning and evening) during concomitant use.
• CNS depressants: Alcohol, benzodiazepines, opioids, sedating antihistamines, and other central nervous system depressants may increase the sedative and psychomotor‑impairing effects of Contrave. Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs should be managed carefully, as this may increase the risk of seizures.
• Serotonergic drugs: Concomitant use with SSRIs, SNRIs, tricyclic antidepressants, triptans, fentanyl, lithium, tramadol, and other serotonergic agents increases the risk of serotonin syndrome. Monitor closely if co‑administration is clinically necessary.
• Antihypertensives: Contrave may increase blood pressure and heart rate, potentially antagonising the effects of antihypertensive medications. Blood pressure should be monitored.
• Drugs metabolised by CYP2D6: Bupropion is a strong inhibitor of CYP2D6 and may increase plasma concentrations of drugs metabolised by this enzyme, including many antidepressants (e.g., venlafaxine, duloxetine, nortriptyline, desipramine, imipramine, paroxetine, fluoxetine, sertraline), antipsychotics (e.g., haloperidol, risperidone, aripiprazole), beta‑blockers (e.g., metoprolol, propranolol), antiarrhythmics (e.g., flecainide, propafenone), and atomoxetine. Dose reduction of the CYP2D6 substrate should be considered.
• Dopaminergic drugs: Caution is advised when Contrave is co‑administered with levodopa or amantadine due to the potential for additive central nervous system toxicity.
• Alcohol: Excessive alcohol consumption during Contrave therapy may increase the risk of seizures. Patients should be counselled about the risks of combining alcohol with Contrave.

Practical Advice

• Administration: Follow the weekly titration schedule carefully. Swallow tablets whole with a glass of water; do not cut, chew, or crush. Do not take Contrave with a high‑fat meal, as this increases the risk of seizures. Taking the tablets with a light meal or snack may help reduce nausea, the most common side effect.
• Monitoring: Blood pressure and heart rate should be measured before starting Contrave and periodically during treatment, especially during the initial three months when the risk of blood pressure elevation is greatest. Weight should be tracked regularly. Body weight response should be evaluated after 12 weeks at the maintenance dose; if at least 5% of baseline body weight has not been lost, Contrave should be discontinued. Monitor for clinical worsening, emergence of suicidal thoughts or behaviour, and unusual changes in mood or behaviour. In patients with diabetes, blood glucose should be monitored closely, as weight loss may require adjustment of insulin or oral hypoglycaemic agents.
• Storage: Store at room temperature (15‑30 °C) in a dry place, protected from moisture and light. Keep the bottle tightly closed. Keep out of the reach and sight of children.
• Lifestyle: Contrave is most effective when combined with a comprehensive weight‑management program that includes a reduced‑calorie diet, regular physical activity (at least 150 minutes of moderate‑intensity aerobic exercise per week), and behavioural modification strategies. Keep a food diary and track your progress. Drink plenty of water. Avoid alcohol. If nausea is bothersome, taking the medication with a light meal or a small snack can help; ginger‑containing foods or beverages may also provide relief.
• Missed dose: If a dose is missed, skip the missed dose entirely and take the next dose at the regular time. Do not take a double dose to make up for a missed one.
• When to seek medical review: Contact your doctor immediately if you experience a seizure, signs of a serious allergic reaction (rash, hives, swelling of the face, lips, tongue, or throat, difficulty breathing), signs of serotonin syndrome (agitation, confusion, rapid heart rate, high fever, muscle rigidity), signs of liver injury (jaundice, dark urine, right upper abdominal pain, unexplained fatigue), or worsening depression with suicidal thoughts. If you require emergency pain management, inform the treating physician that you are taking Contrave, as it contains naltrexone and will block the effects of opioid analgesics.
• Disposal: Return unused or expired medication to a pharmacy for safe disposal. Do not flush down the toilet or discard in household waste.

Alternative Medications

• GLP‑1 receptor agonists: Liraglutide (Saxenda®) and semaglutide (Wegovy®) are injectable prescription medications approved by Health Canada for chronic weight management. They work by mimicking the body’s own GLP‑1 hormone, reducing appetite and slowing gastric emptying. They generally produce greater weight loss than Contrave but are more expensive and require subcutaneous injection.
• Orlistat (Xenical® / Alli®): A lipase inhibitor that blocks the absorption of approximately 30% of dietary fat. Xenical (120 mg) is available by prescription; Alli (60 mg) is available over the counter. It does not act on the brain’s appetite centres, and its main side effects are gastrointestinal (oily stools, flatulence, faecal urgency) related to fat malabsorption.
• Phentermine/topiramate extended‑release (Qsymia®): A combination oral agent that suppresses appetite (phentermine) and promotes satiety while altering taste perception (topiramate). It is approved in the United States for chronic weight management but is not currently marketed in Canada.
• Tirzepatide (Mounjaro® / Zepbound®): A dual GIP/GLP‑1 receptor agonist approved in Canada for type 2 diabetes (Mounjaro) and in the United States for weight management (Zepbound). It produces significant weight loss and may be an option for patients who have not responded to or cannot tolerate Contrave.
• Bupropion alone (Wellbutrin®): Bupropion as monotherapy has some efficacy for weight loss, particularly in patients with depression, but is not formally approved for this indication. It lacks the synergistic effect of naltrexone on the POMC feedback loop and is generally less effective than the combination for appetite control and weight loss.
• Naltrexone alone: Naltrexone as monotherapy has minimal independent effects on body weight and is not recommended as a weight‑loss treatment.
• Lifestyle and behavioural approaches: A structured weight‑management program supervised by a registered dietitian, cognitive‑behavioural therapy (CBT) for weight loss, self‑monitoring (food and activity diaries), and regular physical activity are the cornerstones of safe, sustainable weight loss. These approaches can be used alone or in combination with pharmacotherapy. Bariatric surgery (e.g., sleeve gastrectomy, gastric bypass) is an option for individuals with severe obesity (BMI ≥ 40 kg/m² or BMI ≥ 35 kg/m² with obesity‑related complications) who have not succeeded with non‑surgical methods.

Clinical Efficacy

The efficacy of naltrexone/bupropion for weight management has been established in multiple randomised, double‑blind, placebo‑controlled Phase 3 clinical trials. In the COR‑I trial (56 weeks), patients receiving Contrave achieved a mean weight loss of 6.1% compared with 1.3% for placebo, with 48% of participants losing at least 5% of baseline body weight. The COR‑II trial replicated these results in a larger cohort. The COR‑BMOD study, which integrated intensive behavioural therapy with pharmacologic treatment, reported 9.3% average weight loss over 56 weeks. Early weight loss at 16 weeks predicted long‑term success: patients who did not achieve at least 5% weight loss by week 16 were unlikely to respond further. The LIGHT trial, designed to assess cardiovascular safety, found no signal of excess major adverse cardiovascular events compared with placebo in interim analyses.

In a 2024 Canadian real‑world retrospective chart review of 468 adults attending the Wharton Medical Clinic in Ontario, participants treated with Contrave for 6 months lost a mean of 4.23 kg (4.05% of body weight), with 42.5% losing at least 5% of their body weight and 15.5% losing at least 10%. The most frequent adverse events were nausea (5.7%), constipation (5.7%), and headache (2.5%). Participants reported decreased appetite (14.7%), decreased cravings (13.9%), and decreased hunger (9.4%). A 2025 study further demonstrated that naltrexone/bupropion‑induced weight loss is associated with significant reductions in total percent fat mass, increases in total percent lean mass, and improvements in the lean‑to‑fat mass ratio.

The CADTH Canadian Drug Expert Committee (CDEC) has recommended that Contrave be reimbursed for chronic weight management in adults, with conditions. Contrave is recommended by Obesity Canada as a pharmacotherapy option for patients who meet the prescribing criteria and who are committed to a comprehensive lifestyle modification program. It occupies a distinct place among weight‑management pharmacotherapies, offering an oral, non‑stimulant option that targets both hunger and cravings through a unique central mechanism of action.

Important:

Bupropion + Naltrexone (Contrave) is a prescription medication that should be used only under the supervision of a qualified healthcare professional. It contains bupropion, an antidepressant that may increase the risk of suicidal thoughts and behaviour in children, adolescents, and young adults. All patients should be closely monitored for clinical worsening, suicidality, or unusual changes in behaviour. This medication can cause seizures; the risk is higher in patients with a history of seizures, eating disorders, head injury, or those abruptly stopping alcohol or sedatives. Do not take Contrave if you are currently using or have recently used opioid medications, as naltrexone can precipitate acute opioid withdrawal. Contrave can increase blood pressure and heart rate; blood pressure must be monitored before and during treatment. Do not take Contrave with high‑fat meals, as this significantly increases the risk of seizures. Do not combine Contrave with other bupropion‑containing products. If you require emergency surgery or pain management, inform the medical team that you are taking Contrave, as naltrexone will block the effects of opioid pain relievers. Contrave is contraindicated with MAOIs; a 14‑day washout period is required. If you experience a seizure, severe allergic reaction, chest pain, or suicidal thoughts, stop taking the medication and seek emergency medical attention. This information is not a substitute for professional medical advice, diagnosis, or treatment.

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