Generic Contrave ( Bupropion + Naltraxone )

Buy Generic Contrave (Bupropion + Naltraxone) without prescription in Canada

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Contrave is a prescription combination medication that contains bupropion hydrochloride and naltrexone hydrochloride in a single extended‑release tablet. It is used to support chronic weight management in adults with obesity or who are overweight and have weight‑related medical problems. It works by targeting two key areas of the brain involved in hunger and cravings: bupropion stimulates pro‑opiomelanocortin (POMC) neurons to reduce appetite, while naltrexone blocks the natural opioid‑mediated 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. 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 and should not be cut, chewed, or crushed. Do not take with high‑fat meals. 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.

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; naltrexone has a half‑life of about 5 hours, and its active metabolite 6‑β‑naltrexol has a half‑life of approximately 13 hours.

Alcohol recommendation: Alcohol consumption should be strictly avoided or limited during treatment with Contrave. Excessive alcohol use or abrupt discontinuation of alcohol in heavy drinkers can substantially increase the risk of seizures. Naltrexone may alter the subjective effects of alcohol, but it does not prevent the impairing effects of alcohol on motor coordination and judgment.

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 usually mild to moderate, resolving within 2 to 4 weeks. Approximately 24% of patients in clinical trials discontinued Contrave because of an adverse event, most commonly nausea, headache, and vomiting.

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General Information about Contrave (Bupropion + Naltrexone)

• 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 (antiobesity preparations, centrally acting)
• Dosage forms and strengths: Extended‑release bilayer tablet: naltrexone hydrochloride 8 mg / bupropion hydrochloride 90 mg. Supplied in bottles of 120 tablets.
• Manufacturers in Canada: Bausch Health, Canada Inc. (Contrave). Originally distributed by Valeant Canada LP.
• Registration status in Canada: Approved by Health Canada (Notice of Compliance: 2018/02/13; first marketed: 2018/02/13). DIN: 02472945. Status: Marketed.
• OTC / Rx classification: Prescription only (Rx). Schedule I drug under the Controlled Drugs and Substances Act. A valid prescription from a licensed Canadian healthcare professional is required.

Mechanism of Action and Pharmacology

The mechanism of action of Contrave for weight management is not fully understood, but it is believed to involve complementary actions on hypothalamic and mesolimbic pathways. Bupropion, a relatively weak inhibitor of dopamine and norepinephrine reuptake, stimulates pro‑opiomelanocortin (POMC) neurons in the arcuate nucleus of the hypothalamus. POMC neurons release alpha‑melanocyte‑stimulating hormone (α‑MSH), which promotes satiety and energy expenditure, and beta‑endorphin, which provides auto‑inhibitory feedback via μ‑opioid receptors. Naltrexone, a potent μ‑opioid receptor antagonist, blocks this auto‑inhibition, amplifying and prolonging the POMC‑mediated anorectic signal. This synergistic interaction produces a robust and durable reduction in appetite and food intake.

Following oral administration, both components are well absorbed. Contrave is formulated as a bilayer extended‑release tablet. Bupropion undergoes extensive first‑pass hepatic metabolism primarily via CYP2B6 to its active metabolite hydroxybupropion. Naltrexone is metabolised to the active metabolite 6‑β‑naltrexol. The elimination half‑life of bupropion is approximately 21 hours; naltrexone has a half‑life of about 5 hours, and 6‑β‑naltrexol about 13 hours. High‑fat meals significantly increase systemic exposure to both drugs and should be avoided. The tablets must not be cut, chewed, or crushed.

Indications

• Chronic Weight Management: 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, despite containing bupropion.
• Not recommended for use in paediatric patients; safety and efficacy have not been established in individuals under 18 years of age.

Important Warnings and Precautions

At‑risk groups

• Pregnancy: Contrave should be used during pregnancy only if the potential benefit justifies the potential risk. Weight loss offers no potential benefit to a pregnant woman and may result in fetal harm. It is not recommended during pregnancy. Women of childbearing potential should use effective contraception.
• 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. Contrave is not approved for use in children or adolescents.
• Elderly: No dose adjustment is required based on age alone. However, elderly patients may be more sensitive to adverse effects, 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. Risk factors for seizure include head trauma, 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. 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.
• Serotonin syndrome: A potentially life‑threatening serotonin syndrome may occur, 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 because of the increased seizure risk.
• 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 cautious when driving or operating hazardous machinery until they are reasonably certain the medication does not adversely affect their mental alertness and motor coordination. Alcohol consumption should be strictly avoided or limited. Excessive alcohol use increases the risk of seizures and neuropsychiatric side effects. Naltrexone does not prevent the impairing effects of alcohol on 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 must be swallowed whole with a glass of water. Do not cut, chew, or crush. Contrave should not be taken with high‑fat meals. Taking the tablets with a light meal or snack may improve gastrointestinal tolerance.
• Dose adjustments for hepatic or renal impairment: Maximum two tablets per day (one tablet each morning and evening) in patients with moderate hepatic impairment, moderate renal impairment, or severe renal impairment. Not recommended in 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, and vice versa.
• Evaluation of response: Assess response after 12 weeks at the maintenance dosage. If the patient has not lost at least 5% of baseline body weight, discontinue Contrave.
• Missed dose: 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; 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 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, alopecia, tinnitus, and palpitations.
• Serious side effects: Seizures (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 (anaphylaxis, angioedema, Stevens‑Johnson syndrome).
• Discontinuation rate: 24% of patients on Contrave discontinued treatment due to adverse events (vs. 12% on placebo), most commonly nausea (6.3%), headache (1.7%), and vomiting (1.1%).
• Contraindications: Uncontrolled hypertension; seizure disorder or 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; abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs; concomitant use or within 14 days of treatment with monoamine oxidase inhibitors (MAOIs), including linezolid or intravenous methylene blue; known hypersensitivity to naltrexone, bupropion, or any component of the product.

Drug Interactions

• Monoamine oxidase inhibitors (MAOIs) — contraindicated: Allow at least 14 days between discontinuation of an MAOI and starting Contrave, and vice versa.
• Other bupropion‑containing products — contraindicated: Contrave must not be combined with other bupropion products (e.g., Wellbutrin, Zyban).
• Opioid analgesics: Naltrexone may precipitate acute opioid withdrawal in opioid‑dependent patients. Patients must be opioid‑free for at least 7–10 days before starting Contrave. Naltrexone blocks the analgesic effects of opioids; alternative pain management must be used in emergencies.
• CYP2B6 inhibitors: Ticlopidine, clopidogrel: maximum Contrave dose is two tablets per day.
• CNS depressants: Alcohol, benzodiazepines, opioids, and sedating antihistamines may increase sedation and psychomotor impairment. Abrupt discontinuation of alcohol, benzodiazepines, barbiturates, or antiepileptic drugs increases seizure risk.
• Serotonergic drugs: SSRIs, SNRIs, TCAs, triptans, fentanyl, lithium, tramadol, and others increase the risk of serotonin syndrome. Monitor closely.
• Drugs metabolised by CYP2D6: Bupropion is a strong CYP2D6 inhibitor; dose reduction of CYP2D6 substrates (e.g., many antidepressants, antipsychotics, beta‑blockers, antiarrhythmics) may be necessary.
• Dopaminergic drugs: Caution with levodopa or amantadine due to additive CNS toxicity.
• Alcohol: Avoid or strictly limit; excessive alcohol use increases seizure risk.

Practical Advice

• Administration: Follow the weekly titration schedule exactly. Swallow tablets whole with water; do not cut, chew, or crush. Avoid high‑fat meals. Taking tablets with a light meal or snack may help reduce nausea.
• Monitoring: Measure blood pressure and heart rate before starting and periodically during treatment, especially during the first 3 months. Track body weight regularly; evaluate response at 12 weeks. Discontinue if < 5% weight loss. Monitor for suicidal thoughts, mood changes, or unusual behaviour. In patients with diabetes, monitor blood glucose closely.
• Storage: Store at room temperature (15‑30 °C) in a dry place, protected from moisture and light. Keep the bottle tightly closed and out of the reach and sight of children.
• Lifestyle: Combine Contrave with a reduced‑calorie diet, regular physical activity (at least 150 minutes per week), and behavioural strategies. Keep a food diary. Drink plenty of water. Avoid alcohol. If nausea occurs, taking the dose with food or ginger‑containing products may help.
• Missed dose: Skip the missed dose; do not double the next dose.
• When to seek medical review: Immediately report a seizure, severe allergic reaction (rash, swelling of face/throat, difficulty breathing), serotonin syndrome (agitation, confusion, high fever, muscle rigidity), liver injury (jaundice, dark urine, right upper abdominal pain), or suicidal thoughts. If emergency surgery or pain management is required, inform the medical team you are taking Contrave, as naltrexone will block 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 for chronic weight management. They generally produce greater weight loss but are more costly and require injection.
• Orlistat (Xenical® / Alli®): A lipase inhibitor that blocks dietary fat absorption; available by prescription (120 mg) or over‑the‑counter (60 mg). Gastrointestinal side effects are prominent.
• Phentermine/topiramate extended‑release (Qsymia®): An oral combination (not marketed in Canada) that suppresses appetite and promotes satiety.
• Tirzepatide (Mounjaro® / Zepbound®): A dual GIP/GLP‑1 receptor agonist with significant weight‑loss effects; available in Canada for diabetes and under evaluation for weight management.
• Bupropion alone (Wellbutrin®): Has some off‑label efficacy for weight loss but is less effective than the combination with naltrexone.
• Lifestyle and behavioural approaches: Structured diet and exercise programs, cognitive‑behavioural therapy (CBT) for weight loss, and bariatric surgery for individuals with severe obesity are foundational or alternative options.

Clinical Efficacy

The efficacy of naltrexone/bupropion for weight management has been established in multiple randomised, double‑blind, placebo‑controlled Phase 3 trials. In the COR‑I trial (56 weeks), Contrave achieved a mean weight loss of 6.1% vs. 1.3% for placebo; 48% of participants lost ≥ 5% of baseline body weight. COR‑II replicated these results. COR‑BMOD, integrating intensive behavioural therapy, reported 9.3% average weight loss over 56 weeks. Early response predicted long‑term success: patients not achieving ≥ 5% weight loss at week 16 were unlikely to respond further. The LIGHT trial interim analysis found no excess cardiovascular events compared with placebo.

A 2024 Canadian real‑world chart review (Wharton Medical Clinic, Ontario) of 468 adults treated with Contrave for 6 months showed a mean weight loss of 4.23 kg (4.05% of body weight), with 42.5% losing ≥ 5% and 15.5% losing ≥ 10%. The most frequent adverse events were nausea (5.7%), constipation (5.7%), and headache (2.5%). Participants reported decreased appetite, cravings, and hunger. A 2025 study demonstrated that Contrave‑induced weight loss is associated with reductions in total percent fat mass and improvements in lean‑to‑fat mass ratio.

The CADTH Canadian Drug Expert Committee (CDEC) has recommended Contrave for reimbursement in chronic weight management with conditions. Obesity Canada lists it as a pharmacotherapy option for patients meeting prescribing criteria who are committed to lifestyle modification. Contrave provides a unique oral, non‑stimulant option that targets both hunger and cravings.

Important:

Contrave (bupropion + naltrexone) 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 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. Do not take with high‑fat meals. Do not combine with other bupropion‑containing products. If you require emergency surgery or pain management, inform the medical team you are taking Contrave, as naltrexone will block the effects of opioid pain relievers. Contrave is contraindicated with MAOIs; a 14‑day washout is required. If you experience a seizure, severe allergic reaction, chest pain, or suicidal thoughts, stop the medication and seek emergency medical attention. This information is not a substitute for professional medical advice, diagnosis, or treatment.

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