Concise Prescribing Info
Naltrexone HCl 8 mg, bupropion HCl 90 mg
Adjunct to a reduced-calorie diet & increased physical activity, for wt management in adult ≥18 yr w/ an initial BMI of ≥30 kg/m2 (obese) or ≥27-<30 kg/m2 (overwt) in the presence of ≥1 wt-related co-morbidities (eg, type 2 DM, dyslipidaemia, or controlled HTN).
Dosage/Direction for Use
Adult Initially, 1 tab in the morning at Wk 1; followed by 1 tab in the morning & evening at Wk 2; then 2 tab in the morning & 1 tab in the evening at Wk 3; & at Wk 4 & onwards, 2 tab in the morning & evening. Max daily dose: 2 tab bd (total dose of 32 mg naltrexone HCl & 360 mg bupropion HCl). Evaluate after 16 wk for continued treatment & re-evaluate annually. Patients w/ moderate or severe renal impairment, & mild hepatic impairment Initially, 1 tab in the morning at Wk 1; then escalate to 1 tab in the morning & evening at Wk 2 onwards. Max daily dose: 2 tab (1 tab in the morning & evening).
Should be taken with food.
Hypersensitivity. Patients w/ uncontrolled HTN; current or history of seizures; known CNS tumour; undergoing acute alcohol or benzodiazepine w/drawal; history of bipolar disorder; current or previous diagnosis of bulimia or anorexia nervosa. Concomitant treatment containing bupropion or naltrexone; currently dependent on chronic opioids or opiate agonists (eg, methadone), or in acute opiate w/drawal. Concomitant administration of MAOIs (at least 14 days should elapse between MAOI discontinuation & treatment initiation w/ naltrexone/bupropion). Severe hepatic impairment; end-stage renal failure.
Special Precautions
Bupropion-associated risk of seizures (dose-related); caution in patients w/ predisposing factors eg, head trauma, excessive alcohol use or cocaine/stimulants addiction, lowered glucose, medicinal products that lower seizure threshold. Risk of BP elevation; must not be given to patients w/ uncontrolled HTN. Caution in patients w/ controlled HTN; active CAD or history of cerebrovascular disease; history of mania. Monitor for any clinical worsening, suicidal behaviour/thoughts & unusual behaviour changes. Discontinue use if chronic opiate therapy is required. Risk of dangerous, possibly fatal, opioid intoxication w/ large amounts of exogenous opioids (when attempting to overcome opioid blockade). Patients may be more sensitive to lower doses of opioids after naltrexone/bupropion discontinuation. Discontinue in case of allergic or anaphylactoid/anaphylactic reactions; if serum sickness or drug-induced liver injury is suspected. Discontinue if patient has not lost at least 5% of initial body wt after 16 wk of treatment. Minimise or avoid alcohol consumption. Not to be taken by patients w/ rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption. May affect ability to drive & use machines. Not recommended in patients w/ moderate hepatic impairment. Not to be used during pregnancy or in women attempting to become pregnant, & during breast-feeding. Not to be used in childn & adolescents <18 yr. Caution in elderly >65 yr. Not recommended in elderly >75 yr.
Adverse Reactions
Headache; nausea, constipation, vomiting. Anxiety, insomnia; dizziness, tremor, dysgeusia, lethargy, somnolence; tinnitus, vertigo; palpitations, increased heart rate; hot flush, HTN, increased BP; dry mouth, abdominal pain, abdominal pain upper; hyperhidrosis, pruritus, alopecia, rash; fatigue, feeling jittery, irritability.
Drug Interactions
Antagonistic effect w/ opioid-containing medicinal products. Bupropion: Enhanced catecholaminergic pathways w/ MAOIs. Reduced exposure w/ CYP2B6 inducers (eg, carbamazepine, phenytoin, ritonavir, efavirenz). Increased bupropion levels & lowered levels of its active metabolite w/ CYP2B6 substrates (eg, cyclophosphamide, ifosfamide) & CYP2B6 inhibitors (eg, orphenadrine, ticlopidine, clopidogrel); medicinal products that inhibit metabolism (eg, valproate). May affect medicinal products metabolised by CYP2D6 including antidepressants (SSRIs & TCAs, eg, desipramine, imipramine, paroxetine), antipsychotics (eg, haloperidol, risperidone & thioridazine), β-blockers (eg, metoprolol) & Type 1C antiarrhythmics (eg, propafenone & flecainide). Higher incidence of AR (eg, nausea, vomiting & neuropsychiatric AR) w/ levodopa or amantadine. Naltrexone: Altered exposure w/ UGT 1A2 & 2B7 inhibitors or inducers.
MIMS Class
Anti-Obesity Agents
ATC Classification
A08AA62 - bupropion and naltrexone ; Belongs to the class of centrally acting antiobesity products. Used in the treatment of obesity.
Contrave 8/90 mg PR tab
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