DDInter1397 DDInter252
Paroxetine is a selective serotonin reuptake inhibitor (SSRI) drug commonly known as Paxil. It has a variety of uses, including the treatment of anxiety disorders, major depression, posttraumatic stress disorder, and symptoms of menopause, among others. It was approved by the FDA in the early 1990s and marketed by SmithKline Beecham.[L7712,L7715] A unique feature of this drug is that it is highly potent and selective in its inhibition of serotonin reuptake and has little effect on other neurotransmitters. Because of its potent inhibition of serotonin reuptake, paroxetine is more likely to cause withdrawal effects upon cessation. Paroxetine is well tolerated in most patients with a similar adverse effect profile to other members of its drug class. The controlled release formulation was designed to decrease the likelihood of nausea that is sometimes associated with paroxetine.[L7700,L7742]
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.
Paroxetine {u} (Compound) binds {v} (Gene) CYP2C8
CYP2C8 {u} (Gene) is bound by {v} (Compound) Bupropion
Paroxetine {u} (Compound) palliates {v} (Disease) panic disorder
panic disorder {u} (Disease) is palliated by {v} (Compound) Bupropion
Paroxetine {u} (Compound) downregulates {v} (Gene) DLD
DLD {u} (Gene) is downregulated by {v} (Compound) Bupropion
Paroxetine {u} (Compound) causes {v} (Side Effect) Dental caries
Dental caries {u} (Side Effect) is caused by {v} (Compound) Bupropion
Paroxetine {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
Paroxetine {u} (Compound) binds {v} (Gene) CYP2B6
CYP2B6 {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
Paroxetine {u} (Compound) binds {v} (Gene) SLC6A3
SLC6A3 {u} (Gene) is associated with {v} (Disease) attention deficit hyperactivity disorder
attention deficit hyperactivity disorder {u} (Disease) is palliated by {v} (Compound) Bupropion
Paroxetine {u} (Compound) binds {v} (Gene) SLC6A2
SLC6A2 {u} (Gene) is bound by {v} (Compound) Dextromethorphan
Dextromethorphan {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Bupropion
Paroxetine {u} (Compound) palliates {v} (Disease) panic disorder
panic disorder {u} (Disease) is palliated by {v} (Compound) Clonazepam
Clonazepam {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Bupropion
Paroxetine {u} (Compound) downregulates {v} (Gene) DLD
DLD {u} (Gene) regulates {v} (Gene) HDAC6
HDAC6 {u} (Gene) is downregulated by {v} (Compound) Bupropion
Paroxetine (Compound) binds CYP2C8 (Gene) and CYP2C8 (Gene) is bound by Bupropion (Compound)
Paroxetine (Compound) palliates panic disorder (Disease) and panic disorder (Disease) is palliated by Bupropion (Compound)
Paroxetine (Compound) downregulates DLD (Gene) and DLD (Gene) is downregulated by Bupropion (Compound)
Paroxetine (Compound) causes Dental caries (Side Effect) and Dental caries (Side Effect) is caused by Bupropion (Compound)
Paroxetine (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
Paroxetine (Compound) binds CYP2B6 (Gene) and CYP2B6 (Gene) is bound by Prasugrel (Compound) and Prasugrel may cause a minor interaction that can limit clinical effects when taken with Bupropion
Paroxetine (Compound) binds SLC6A3 (Gene) and SLC6A3 (Gene) is associated with attention deficit hyperactivity disorder (Disease) and attention deficit hyperactivity disorder (Disease) is palliated by Bupropion (Compound)
Paroxetine (Compound) binds SLC6A2 (Gene) and SLC6A2 (Gene) is bound by Dextromethorphan (Compound) and Dextromethorphan may cause a moderate interaction that could exacerbate diseases when taken with Bupropion
Paroxetine (Compound) palliates panic disorder (Disease) and panic disorder (Disease) is palliated by Clonazepam (Compound) and Clonazepam may cause a moderate interaction that could exacerbate diseases when taken with Bupropion
Paroxetine (Compound) downregulates DLD (Gene) and DLD (Gene) regulates HDAC6 (Gene) and HDAC6 (Gene) is downregulated by Bupropion (Compound)