Contrave

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; severe cutaneous adverse reactions eg, SJS, acute generalised exanthematous pustulosis appear. 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. Controlled HTN, active CAD (eg, ongoing angina or recent history of MI), history of cerebrovascular disease & 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. May unmask Brugada syndrome. 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. 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 adverse reactions 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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