Contrave: Difference between revisions

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| pregnancy = Contraindicated in pregnancy (FDA label).{{citation needed}}

| legal = [[USLegal:Prescription only|Rx-only]] in US. '''Contraindicated''' in uncontrolled hypertension, seizure disorder, anorexia/bulimia, chronic opioid use (would precipitate withdrawal), and during/within 14 days of MAOI use. Carries '''Boxed Warning''' for suicidal thoughts and neuropsychiatric reactions (bupropion class effect)<ref name="contrave-label" />

| mechanism = <vote slug="contrave-mech-claim">Bupropion inhibits norepinephrine and dopamine reuptake, activating POMC neurons in the hypothalamus to release α-MSH (suppressing appetite) and β-endorphin (which would normally feed back to inhibit POMC). Naltrexone blocks the β-endorphin autoinhibition, sustaining the appetite-suppressing POMC activity. The combination achieves greater weight loss than either component alone.</vote> Modest absolute weight loss (~5% from baseline at 1 year) versus placebo. ~~Drug-interaction~~ profile includes CYP2D6 inhibition (bupropion), so dose-adjustment for tricyclic antidepressants, β-blockers metabolized by 2D6, and certain ~~antipsychotics~~ is warranted<ref name="contrave-label" />.

| mechanism = <vote slug="contrave-mech-claim">Bupropion inhibits norepinephrine and dopamine reuptake, activating POMC neurons in the hypothalamus to release α-MSH (suppressing appetite) and β-endorphin (which would normally feed back to inhibit POMC). Naltrexone blocks the β-endorphin autoinhibition, sustaining the appetite-suppressing POMC activity. The combination achieves greater weight loss than either component alone.</vote> Modest absolute weight loss (~5% from baseline at 1 year) versus placebo. Interaction profile includes CYP2D6 inhibition (bupropion), so dose-adjustment for tricyclic antidepressants, β-blockers metabolized by 2D6, and certain neuroleptics is warranted<ref name="contrave-label" />.

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== References ==

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