DDInter624 DDInter252
Efavirenz (brand names Sustiva® and Stocrin®) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and is used as part of highly active antiretroviral therapy (HAART) for the treatment of a human immunodeficiency virus (HIV) type 1. For HIV infection that has not previously been treated, efavirenz and lamivudine in combination with zidovudine or tenofovir is the preferred NNRTI-based regimen. Efavirenz is also used in combination with other antiretroviral agents as part of an expanded postexposure prophylaxis regimen to prevent HIV transmission for those exposed to materials associated with a high risk for HIV transmission.
Bupropion (also known as the brand name product Wellbutrin®) is a norepinephrine/dopamine-reuptake inhibitor (NDRI) used most commonly for the management of Major Depressive Disorder (MDD), Seasonal Affective Disorder (SAD), and as an aid for smoking cessation. Bupropion exerts its pharmacological effects by weakly inhibiting the enzymes involved in the uptake of the neurotransmitters norepinephrine and dopamine from the synaptic cleft, therefore prolonging their duration of action within the neuronal synapse and the downstream effects of these neurotransmitters. More specifically, bupropion binds to the norepinephrine transporter (NET) and the dopamine transporter (DAT).[A6399,A178810] Bupropion was originally classified as an "atypical" antidepressant because it does not exert the same effects as the classical antidepressants such as Monoamine Oxidase Inhibitors (MAOIs), Tricyclic Antidepressants (TCAs), or Selective Serotonin Reuptake Inhibitors (SSRIs). While it has comparable effectiveness to typical first-line options for the treatment of depression such as SSRIs,[A178798,A178804] bupropion is a unique option for the treatment of MDD as it lacks any clinically relevant serotonergic effects, typical of other mood medications, or any effects on histamine or adrenaline receptors.[A6399,A178840] Lack of activity at these receptors results in a more tolerable side effect profile; bupropion is less likely to cause sexual side effects, sedation, or weight gain as compared to SSRIs or TCAs, for example.[A178804,A178807] When used as an aid to smoking cessation, bupropion is thought to confer its anti-craving and anti-withdrawal effects by inhibiting dopamine reuptake, which is thought to be involved in the reward pathways associated with nicotine, and through the antagonism of the nicotinic acetylcholinergic receptor.[A178825,A1966,A16508] A Cochrane Review of meta-analyses of available treatment modalities for smoking cessation found that abstinence rates approximately doubled when bupropion was used as compared to placebo, and was found to have similar rates of smoking cessation as [nicotine] replacement therapy (NRT). Bupropion is sometimes used as an add-on agent to first-line treatments of depression such as selective serotonin reuptake inhibitor (SSRI) medications when there is a treatment-failure or only partial response. Bupropion is also used off-label for the management of Attention/Deficit-Hyperactivity Disorder (ADHD) in adults with comorbid bipolar depression to avoid mood destabilization caused by typical stimulant medications used for the treatment of ADHD. When used in combination with [naltrexone] in the marketed product ContraveⓇ for chronic weight management, the two components are thought to have effects on areas of the brain involved in the regulation of food intake. This includes the hypothalamus, which is involved in appetite regulation, and the mesolimbic dopamine circuit, which is involved in reward pathways. Studies have shown that the combined activity of bupropion and [naltrexone] increase the firing rate of hypothalamic pro-opiomelanocortin (POMC) neurons and blockade of opioid receptor-mediated POMC auto-inhibition, which are associated with a reduction in food intake and increased energy expenditure.[L6562,A179038,A179050] The combination of naltrexone and bupropion was shown to result in a statistically significant weight loss, with a mean change in body weight of -6.3% compared to -1.3% for placebo.
Efavirenz {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Bupropion
Efavirenz {u} (Compound) downregulates {v} (Gene) OXA1L
OXA1L {u} (Gene) is downregulated by {v} (Compound) Bupropion
Efavirenz {u} (Compound) causes {v} (Side Effect) Dyspepsia
Dyspepsia {u} (Side Effect) is caused by {v} (Compound) Bupropion
Efavirenz {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Prasugrel
Prasugrel {u} may cause a minor interaction that can limit clinical effects when taken with {v} Bupropion
Efavirenz {u} (Compound) binds {v} (Gene) CYP2D6
CYP2D6 {u} (Gene) is bound by {v} (Compound) Cimetidine
Cimetidine {u} may cause a minor interaction that can limit clinical effects when taken with {v} Bupropion
Efavirenz {u} (Compound) downregulates {v} (Gene) OXA1L
OXA1L {u} (Gene) is regulated by {v} (Gene) KIT
KIT {u} (Gene) is upregulated by {v} (Compound) Bupropion
Efavirenz {u} (Compound) causes {v} (Side Effect) Dyspepsia
Dyspepsia {u} (Side Effect) is caused by {v} (Compound) Tolterodine
Tolterodine {u} may cause a minor interaction that can limit clinical effects when taken with {v} Bupropion
Efavirenz {u} (Compound) causes {v} (Side Effect) Apathy
Apathy {u} (Side Effect) is caused by {v} (Compound) Doxazosin
Doxazosin {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Bupropion
Efavirenz {u} (Compound) causes {v} (Side Effect) Mediastinal disorder
Mediastinal disorder {u} (Side Effect) is caused by {v} (Compound) Prasugrel
Prasugrel {u} may cause a minor interaction that can limit clinical effects when taken with {v} Bupropion
Efavirenz {u} (Compound) causes {v} (Side Effect) Flank pain
Flank pain {u} (Side Effect) is caused by {v} (Compound) Nilotinib
Nilotinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Bupropion
Efavirenz (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Bupropion (Compound)
Efavirenz (Compound) downregulates OXA1L (Gene) and OXA1L (Gene) is downregulated by Bupropion (Compound)
Efavirenz (Compound) causes Dyspepsia (Side Effect) and Dyspepsia (Side Effect) is caused by Bupropion (Compound)
Efavirenz (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Prasugrel (Compound) and Prasugrel may cause a minor interaction that can limit clinical effects when taken with Bupropion
Efavirenz (Compound) binds CYP2D6 (Gene) and CYP2D6 (Gene) is bound by Cimetidine (Compound) and Cimetidine may cause a minor interaction that can limit clinical effects when taken with Bupropion
Efavirenz (Compound) downregulates OXA1L (Gene) and OXA1L (Gene) is regulated by KIT (Gene) and KIT (Gene) is upregulated by Bupropion (Compound)
Efavirenz (Compound) causes Dyspepsia (Side Effect) and Dyspepsia (Side Effect) is caused by Tolterodine (Compound) and Tolterodine may cause a minor interaction that can limit clinical effects when taken with Bupropion
Efavirenz (Compound) causes Apathy (Side Effect) and Apathy (Side Effect) is caused by Doxazosin (Compound) and Doxazosin may cause a moderate interaction that could exacerbate diseases when taken with Bupropion
Efavirenz (Compound) causes Mediastinal disorder (Side Effect) and Mediastinal disorder (Side Effect) is caused by Prasugrel (Compound) and Prasugrel may cause a minor interaction that can limit clinical effects when taken with Bupropion
Efavirenz (Compound) causes Flank pain (Side Effect) and Flank pain (Side Effect) is caused by Nilotinib (Compound) and Nilotinib may cause a moderate interaction that could exacerbate diseases when taken with Bupropion