Contrave

Bupropion HCl 90 mg, naltrexone HCl 8 mg

Adjunct to reduced-calorie diet & increased physical activity for chronic wt management in adults w/ initial BMI ≥30 kg/m² (obese) or ≥27 kg/m² (overwt) in presence of at least 1 wt-related comorbid condition eg, HTN, type 2 DM or dyslipidemia.

Initially 1 tab in the morning at Wk 1, then 1 tab in the morning & in the evening at Wk 2, followed by 2 tab in the morning & 1 tab in the evening at Wk 3, then 2 tab in the morning & in the evening at Wk 4. Max: 2 tab bd (total dose: Naltrexone HCl 32 mg, bupropion HCl 360 mg). Moderate or severe renal & mild hepatic impairment Initially 1 tab in the morning for Wk 1 then 1 tab in the morning & in the evening from Wk 2 onwards. Max: 2 tab (1 tab in the morning & in the evening).

Should be taken with food: Swallow whole w/ water. Do not cut/chew/crush.

Hypersensitivity. Uncontrolled HTN; current seizure disorder or history of seizures; known CNS tumour; history of bipolar disorder; current or previous diagnosis of bulimia or anorexia nervosa. Patients undergoing acute alcohol or benzodiazepine w/drawal; currently dependent on chronic opioids or opiate agonists (eg, methadone), or in acute opiate w/drawal. Concomitant treatment w/ bupropion or naltrexone; use w/ MAOIs or w/in 14 days of discontinuation. End-stage renal failure; severe hepatic impairment.

Discontinue use if seizure occurs, serum sickness & serotonin syndrome is suspected & sustained BP or pulse rate increases is experienced; suspected drug-induced liver injury. Allergic or anaphylactoid/anaphylactic reactions. Monitor for any clinical worsening, suicidal behaviour or thoughts & unusual changes in behaviour. Predisposing factors increasing risk of seizure eg, history of head trauma, excessive use of alcohol or cocaine or stimulant addiction, hypoglycaemia, medicinal products lowering seizure threshold; sensitivity to lower doses of opioids after discontinuation. Use w/ caution in controlled HTN, active CAD (eg, ongoing angina or recent history of MI), history of cerebrovascular disease & history of mania. May lead to fatal overdose or life endangering opioid intoxication (eg, resp arrest, circulatory collapse) when attempting to overcome naltrexone opioid blockage by administering large amounts of exogenous opioids. Measure BP & pulse rate prior to therapy. Assess estimated GFR prior to initiation. Not to be taken by patients w/ galactose intolerance, total lactase deficiency or glucose-galactose malabsorption. Avoid alcohol consumption. Not to be administered in patients receiving chronic opiate therapy. Concomitant use w/ SSRIs, SNRIs. May affect ability to drive & use machines. Not recommended in moderate hepatic impairment. Hepatotoxicity; renal impairment. Not to be used in women of childbearing potential, during pregnancy & lactation. Not to be used in childn & adolescents <18 yr. Not recommended in elderly >75 yr. Caution in elderly >65 yr.

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 & upper abdominal pain; hyperhidrosis, pruritus, alopecia, rash; fatigue, feeling jittery, irritability.

Enhanced catecholaminergic pathways w/ MAOIs. Antagonistic effect w/ opioid-containing medicinal products eg, cough & cold remedies, antidiarrhoeal prep & opioid analgesics. Increased AUC & C_max of metoprolol, citalopram. Serotonin syndrome w/ SSRIs or SNRIs. Reduced efficacy of tamoxifen. Affected clinical efficacy w/ CYP2B6 inducers eg, carbamazepine, phenytoin, ritonavir, efavirenz; valproate. Reduced exposure w/ ritonavir, lopinavir. Increased plasma levels w/ CYP2B6 substrates (cyclophosphamide, ifosfamide), CYP2B6 inhibitors (orphenadrine, ticlopidine, clopidogrel). Higher incidence of ARs w/ l-dopa or amantadine. Altered exposure w/ UGT1A2 & 2B7 inhibitors or inducers. Decreased plasma digoxin levels. Increased plasma conc w/ food. Caution w/ CYP2D6-metabolised medicinal products eg, TCAs (eg, desipramine, imipramine, paroxetine), antipsychotics (eg, haloperidol, risperidone, thioridazine), β-blockers (eg, metoprolol), type 1C antiarrhythmics (eg, propafenone, flecainide); insulin &/or oral diabetic medicinal products; antipsychotics, antidepressants, antimalarials, tramadol, theophylline, systemic steroids, quinolones, sedating antihistamines.

Anti-Obesity Agents

A08AA62 - bupropion and naltrexone ; Belongs to the class of centrally acting antiobesity products. Used in the treatment of obesity.

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