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Contrave

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Contrave (Naltrexone, Bupropion) is a combination medication used to support long-term weight management in adults. It addresses the neurological aspects of food cravings and appetite control. By targeting specific areas of the brain, it helps individuals adhere to a reduced-calorie diet and increased physical activity.


Ingredients
Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Naltrexone, Bupropion
Reference Brand
Mysimba
Product Form
Prolonged-release tablet
Regulatory Classification
Rx
Primary Category
Weight Management
Product Category
Anti-obesity preparations
Pharmacological Class
Opioid antagonist and aminoketone antidepressant combination
Manufacturer Description
A weight management aid that works on the brain to help reduce food cravings and control appetite.
Mechanism of Action
This drug combines two medicines that target the reward system and hunger centres in the brain to reduce appetite and food cravings, helping people stick to a reduced-calorie diet.
Route of Administration
Oral
Onset Time
Variable; weight loss usually seen within weeks
Duration
12-24 hours per dose
Contraindications
Uncontrolled high blood pressure, Seizure disorders, Eating disorders (Bulimia/Anorexia), Opioid withdrawal
Severe Adverse Events
Seizures, Suicidal thoughts, Severe allergic reactions, Glaucoma
Common Side Effects
Nausea, Dry mouth, Headache
Uncommon Side Effects
Constipation, Dizziness, Insomnia, Anxiety
Drug Interactions
Opioids, Alcohol, MAO inhibitors, Theophylline, Steroids
Pregnancy Safety Warnings
Contraindicated in pregnancy.
Age Restrictions
Only for adults aged 18 and over.
Storage Guidelines
Store below 25°C.
Related Products
Orlistat, Liraglutide (Saxenda), Semaglutide (Wegovy)

Contrave FAQ

Is Contrave approved for weight loss in the United Kingdom?

Contrave is not licensed by the MHRA for any indication in the UK. While the FDA has approved it for chronic weight management, UK clinicians must rely on alternative, licensed therapies for obesity.

How does Contrave differ from other weight-loss drugs such as liraglutide or orlistat?

Contrave combines an opioid antagonist (naltrexone) with a norepinephrine-dopamine reuptake inhibitor (bupropion) to target both appetite and reward pathways. Liraglutide is a GLP-1 receptor agonist that primarily slows gastric emptying and reduces appetite, whereas orlistat works locally in the gut to inhibit fat absorption.

Can I take Contrave if I have a history of depression?

Bupropion is an antidepressant, but individuals with active major depressive disorder or bipolar disorder should be evaluated carefully. Mood changes, including agitation or suicidal thoughts, have been reported, so close psychiatric monitoring is advised.

What should I know about alcohol consumption while on Contrave?

Alcohol can increase the risk of liver toxicity and may heighten blood-pressure elevations. Moderate alcohol intake (up to one standard drink per day) is generally acceptable, but excessive consumption should be avoided.

How is the Contrave tablet identified?

The tablet is usually imprinted with “8/90” on one side and “CONTRAVE” on the other. Specific imprint details may vary by manufacturer, so checking the packaging or pharmacy label is recommended.

Will Contrave show up on a drug test for employment or sport?

Standard workplace drug screens do not test for naltrexone or bupropion. However, specialized testing for these compounds exists and could be requested in certain contexts (e.g., clinical trials).

Does Contrave affect blood sugar levels?

Bupropion has a modest impact on glucose metabolism and may slightly improve glycaemic control in some patients. Nonetheless, regular monitoring of blood glucose is prudent, especially for individuals with type 2 diabetes.

Can I travel internationally with Contrave prescribed privately in the UK?

When travelling, carry a copy of the private prescription and the original pharmacy label. Some countries may restrict importation of unlicensed medicines, so verify local regulations before departure.

Is there a risk of withdrawal if I stop taking Contrave suddenly?

Abrupt discontinuation can lead to transient mood changes, irritability, or a return of appetite. A gradual taper, reducing one tablet per week, is usually recommended to minimise these effects.

How long before I might notice weight loss after starting Contrave?

Clinical studies show an average weight loss of 5 % of baseline body weight after approximately 12-16 weeks of continuous therapy, provided the medication is combined with a reduced-calorie diet and regular physical activity.

What is Contrave?

Contrave is a prescription-only pill that combines two active ingredients-naltrexone (8 mg) and bupropion (90 mg) per tablet. The combination is intended to support weight management by acting on both appetite-control and reward pathways in the brain. In the United Kingdom, Contrave has not been licensed by the Medicines and Healthcare products Regulatory Agency (MHRA), so it is not available on the NHS or through UK pharmacies. The individual components are each approved for other indications: naltrexone for alcohol dependence and bupropion for major depressive disorder.

  • Formulation: oral tablet (pill)
  • Strength: 8 mg naltrexone / 90 mg bupropion (often abbreviated 8/90 mg)
  • Prescription status: prescription-only medication (UK: unlicensed; US: FDA-approved)

How Contrave Works in the Body

The therapeutic effect of Contrave relies on the complementary actions of its two ingredients:

  • Naltrexone is an opioid-receptor antagonist. By blocking μ-opioid receptors, it reduces the reinforcing effects of food-related reward signals that are mediated through endogenous opioids.
  • Bupropion is a norepinephrine-dopamine reuptake inhibitor (NDRI) and a nicotinic-acetylcholine receptor antagonist. It increases the activity of pro-opiomelanocortin (POMC) neurons in the hypothalamus, enhancing satiety, while also dampening cravings through dopaminergic pathways.

When used together, the drugs are thought to produce a synergistic effect: bupropion stimulates POMC neurons, and naltrexone prevents the auto-inhibitory feedback that would otherwise limit this activation. The net result is reduced appetite, increased feelings of fullness, and a lower drive to seek highly palatable foods. Onset of appetite-modulating effects typically occurs within a few days, with peak pharmacodynamic activity reached after the titration phase is completed (approximately 2 weeks).

Approved Medical Uses

| Region | Regulatory authority | Indication | |--|-|| | United States | FDA | Chronic weight management in adults with a BMI ≥ 30 kg/m², or BMI ≥ 27 kg/m² with at least one weight-related comorbidity (e.g., hypertension, type 2 diabetes). | | United Kingdom | Not approved by MHRA | The combination product is unavailable. Naltrexone alone may be prescribed for alcohol dependence; bupropion alone is approved for major depressive disorder. |

Because Contrave is not licensed in the UK, it cannot be prescribed within the NHS. Any use of the combination would have to occur under a Special Availability Scheme (e.g., via a private prescription) and would be considered off-label.

Evidence-Based Off-Label Uses

Smoking Cessation

Bupropion, when used as a single agent (marketed as Zyban in the United States), is an evidence-based treatment for nicotine dependence. Although the combination with naltrexone has been explored in clinical trials, the data are insufficient to support routine use for smoking cessation. Current UK guidelines continue to recommend varenicline or nicotine-replacement therapy as first-line options.

Disclaimer: Using Contrave for smoking cessation is off-label and should only be considered after a thorough risk-benefit discussion with a qualified healthcare provider.

Alcohol Use Disorder

Naltrexone is approved in the UK for the management of alcohol dependence. Some studies have examined whether adding bupropion enhances outcomes, but results are mixed and not robust enough for formal recommendation.

Disclaimer: The combination has no regulatory approval for alcohol-use disorder; clinicians may consider naltrexone monotherapy where appropriate.

Who Should (and Should Not) Use Contrave?

Absolute Contraindications

  • Known hypersensitivity to naltrexone, bupropion, or any excipients in the tablet.
  • Current seizure disorder or a history of seizures.
  • Uncontrolled hypertension (systolic ≥ 160 mmHg or diastolic ≥ 100 mmHg).
  • Use of monoamine-oxidase inhibitors (MAOIs) within the past 14 days.
  • Pregnancy (Category X) and breast-feeding (risk to infant).
  • Simultaneous use of other NDRI or dopaminergic agents that lower seizure threshold (e.g., certain antipsychotics).

Relative Contraindications / Cautions

  • Cardiovascular disease (e.g., coronary artery disease, arrhythmia).
  • Severe hepatic impairment (Child-Pugh C).
  • Renal impairment (eGFR < 30 mL/min/1.73 m²) - dose adjustment may be required.
  • History of eating disorders (e.g., anorexia nervosa).
  • Current psychiatric conditions such as bipolar disorder or active suicidal ideation; bupropion can increase risk of mood swings.

Special Populations

  • Elderly (≥ 65 years): Start at the lowest dose and monitor blood pressure and mental status closely.
  • Pediatric: Not indicated; safety and efficacy have not been established.
  • Patients on other psychotropic medications: Review for potential pharmacodynamic interactions, especially with other agents that affect dopamine or norepinephrine.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Nausea (often transient, improves with continued dosing)
  • Constipation
  • Headache
  • Insomnia or vivid dreams
  • Dry mouth
  • Dizziness

These events are generally mild to moderate and tend to lessen after the titration period.

Serious Adverse Events

  • Elevated blood pressure or hypertensive crisis (monitor at each visit).
  • Seizures - risk is dose-related; avoid in patients with seizure predisposition.
  • Psychiatric effects such as agitation, anxiety, or emergent suicidal thoughts.
  • Liver injury - rare but reported, especially in patients with pre-existing hepatic disease.
  • Allergic reactions (rash, angioedema) - discontinue immediately if observed.

Drug Interactions

| Interaction type | Example agents | Clinical implication | ||-|-| | Major | MAO inhibitors, CNS stimulants, other NDRIs, antipsychotics that lower seizure threshold | May precipitate seizures or severe hypertension; avoid concurrent use. | | Moderate | CYP2B6 inhibitors (e.g., ritonavir) or inducers (e.g., rifampin) | May alter bupropion plasma concentrations; dose adjustment may be needed. | | Pharmacodynamic | Opioid analgesics (e.g., morphine) | Naltrexone blocks opioid receptors, potentially reducing analgesic efficacy. |

Food and Lifestyle Interactions

  • Alcohol: Use with caution; excessive intake can increase the risk of liver toxicity and may blunt the appetite-suppressing effect.
  • Caffeine: No direct interaction, but both ingredients can cause insomnia; limit caffeine if sleep disturbances occur.
  • Driving: Dizziness or visual disturbances may impair ability to operate machinery; avoid driving until you know how the medication affects you.

How to Take Contrave

Standard Titration Schedule (FDA-labelled regimen)

  1. Week 1: 1 tablet (8/90 mg) taken in the morning.
  2. Week 2: Increase to 2 tablets daily (1 in the morning, 1 in the evening).
  3. Week 3 onward: Increase to 3 tablets daily (1 in the morning, 2 in the evening). This yields a total daily dose of 16 mg naltrexone / 270 mg bupropion.

Note: The titration is designed to minimise nausea and other gastrointestinal side effects. The final maintenance dose is reached after two weeks of gradual escalation.

  • Administration: Swallow the tablets whole with a full glass of water. They may be taken with or without food, but consistent timing (morning and evening) helps maintain stable plasma levels.
  • Missed dose: Take the missed tablet as soon as you remember unless it is close to the next scheduled dose; do not double-dose.
  • Overdose: Symptoms may include severe nausea, vomiting, tremor, seizures, or rapid heart rate. Seek emergency medical care; activated charcoal may be considered if ingestion is recent.
  • Discontinuation: Do not abruptly stop without consulting a healthcare provider. Gradual tapering (reducing one tablet per week) can mitigate potential withdrawal-like symptoms.

Because Contrave is unlicensed in the UK, any prescribing would be under a private or special-access arrangement and must follow the same titration principles used in the United States.

Monitoring and Follow-Up

  • Baseline assessments before initiating therapy: blood pressure, heart rate, fasting glucose, liver function tests (ALT, AST), and a brief psychiatric screening.
  • Follow-up visits at weeks 2, 4, and then every 3 months to review weight change, blood pressure, mood, and any adverse events.
  • Laboratory monitoring: repeat liver enzymes if the patient has pre-existing liver disease or if symptoms suggest hepatic injury.
  • Weight loss goal: a clinically meaningful reduction is ≥ 5 % of baseline body weight maintained for at least 6 months.

If adverse effects arise (e.g., uncontrolled hypertension, seizure, severe mood changes), the medication should be discontinued promptly.

Storage and Handling

  • Store tablets at room temperature (15 °C - 25 °C), away from excessive heat, moisture, and direct sunlight.
  • Keep the container tightly closed and out of reach of children and pets.
  • Do not use the medication after the expiry date printed on the packaging.
  • Dispose of unused tablets according to local pharmacy take-back programs or the MHRA’s guidelines for safe medication disposal.

Medication-Specific Glossary

POMC (Pro-opiomelanocortin)
A precursor peptide in the hypothalamus that, when activated, promotes satiety and reduces food intake.
Titration
A stepwise increase in medication dose to improve tolerability while achieving therapeutic effect.
Seizure Threshold
The level of neuronal excitability at which a seizure may be triggered; certain drugs lower this threshold.
Pharmacokinetic
The study of how a drug is absorbed, distributed, metabolised, and excreted by the body.
Contraindication
A specific situation or condition in which a drug should not be used because the risk outweighs any potential benefit.

Medical Disclaimer

This article provides educational information about Contrave and is not a substitute for professional medical advice. Treatment decisions, including the use of unlicensed or off-label medications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes only and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Contrave is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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