DDInter458 DDInter252
Cyclosporine is a calcineurin inhibitor known for its immunomodulatory properties that prevent organ transplant rejection and treat various inflammatory and autoimmune conditions. It is isolated from the fungus _Beauveria nivea_. Initially manufactured by Sandoz and approved for use by the FDA in 1983, cyclosporine is now available in various products by Novartis (previously known as Sandoz).[L11097,L3734,L11118]
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.
Cyclosporine {u} (Compound) binds {v} (Gene) CYP2C8
CYP2C8 {u} (Gene) is bound by {v} (Compound) Bupropion
Cyclosporine {u} (Compound) upregulates {v} (Gene) COL11A1
COL11A1 {u} (Gene) is upregulated by {v} (Compound) Bupropion
Cyclosporine {u} (Compound) upregulates {v} (Gene) HDAC6
HDAC6 {u} (Gene) is downregulated by {v} (Compound) Bupropion
Cyclosporine {u} (Compound) downregulates {v} (Gene) DLD
DLD {u} (Gene) is downregulated by {v} (Compound) Bupropion
Cyclosporine {u} (Compound) causes {v} (Side Effect) Abdominal pain upper
Abdominal pain upper {u} (Side Effect) is caused by {v} (Compound) Bupropion
Cyclosporine {u} (Compound) binds {v} (Gene) CYP2C8
CYP2C8 {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
Cyclosporine {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
Cyclosporine {u} (Compound) upregulates {v} (Gene) COL11A1
COL11A1 {u} (Gene) is regulated by {v} (Gene) HDAC6
HDAC6 {u} (Gene) is downregulated by {v} (Compound) Bupropion
Cyclosporine {u} (Compound) upregulates {v} (Gene) HDAC6
HDAC6 {u} (Gene) regulates {v} (Gene) NFKBIE
NFKBIE {u} (Gene) is upregulated by {v} (Compound) Bupropion
Cyclosporine {u} (Compound) downregulates {v} (Gene) DLD
DLD {u} (Gene) regulates {v} (Gene) HDAC6
HDAC6 {u} (Gene) is downregulated by {v} (Compound) Bupropion
Cyclosporine (Compound) binds CYP2C8 (Gene) and CYP2C8 (Gene) is bound by Bupropion (Compound)
Cyclosporine (Compound) upregulates COL11A1 (Gene) and COL11A1 (Gene) is upregulated by Bupropion (Compound)
Cyclosporine (Compound) upregulates HDAC6 (Gene) and HDAC6 (Gene) is downregulated by Bupropion (Compound)
Cyclosporine (Compound) downregulates DLD (Gene) and DLD (Gene) is downregulated by Bupropion (Compound)
Cyclosporine (Compound) causes Abdominal pain upper (Side Effect) and Abdominal pain upper (Side Effect) is caused by Bupropion (Compound)
Cyclosporine (Compound) binds CYP2C8 (Gene) and CYP2C8 (Gene) is bound by Cimetidine (Compound) and Cimetidine may cause a minor interaction that can limit clinical effects when taken with Bupropion
Cyclosporine (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
Cyclosporine (Compound) upregulates COL11A1 (Gene) and COL11A1 (Gene) is regulated by HDAC6 (Gene) and HDAC6 (Gene) is downregulated by Bupropion (Compound)
Cyclosporine (Compound) upregulates HDAC6 (Gene) and HDAC6 (Gene) regulates NFKBIE (Gene) and NFKBIE (Gene) is upregulated by Bupropion (Compound)
Cyclosporine (Compound) downregulates DLD (Gene) and DLD (Gene) regulates HDAC6 (Gene) and HDAC6 (Gene) is downregulated by Bupropion (Compound)