DDInter535 DDInter252
Diazoxide is a non-diuretic benzothiadiazine derivative that activates ATP-sensitive potassium channels.[A255647,L44612] It is chemically related to thiazide diuretics but does not inhibit carbonic anhydrase and does not have chloriuretic or natriuretic activity. Diazoxide is commonly used in the treatment of hyperinsulinaemic hypoglycemia due to its ability to inhibit insulin release. Diazoxide also exhibits hypotensive activity and reduces arteriolar smooth muscle and vascular resistance. When administered intravenously, diazoxide can be used to treat hypertensive emergencies; however, this specific form of diazoxide is no longer available in the US. Diazoxide is usually well tolerated, and some of its more common side effects include fluid retention and electrolyte disturbances. In September 2015, the FDA issued a safety alert regarding post-marketing reports of pulmonary hypertension occurring in infants and neonates.[A255
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.
Diazoxide {u} (Compound) downregulates {v} (Gene) USP22
USP22 {u} (Gene) is downregulated by {v} (Compound) Bupropion
Diazoxide {u} (Compound) causes {v} (Side Effect) Chest pain
Chest pain {u} (Side Effect) is caused by {v} (Compound) Bupropion
Diazoxide {u} (Compound) resembles {v} (Compound) Chlorothiazide
Chlorothiazide {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Bupropion
Diazoxide {u} (Compound) downregulates {v} (Gene) USP22
USP22 {u} (Gene) is regulated by {v} (Gene) GPER1
GPER1 {u} (Gene) is upregulated by {v} (Compound) Bupropion
Diazoxide {u} (Compound) downregulates {v} (Gene) MTHFD2
MTHFD2 {u} (Gene) regulates {v} (Gene) GPER1
GPER1 {u} (Gene) is upregulated by {v} (Compound) Bupropion
Diazoxide {u} (Compound) causes {v} (Side Effect) Chest pain
Chest pain {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
Diazoxide {u} (Compound) causes {v} (Side Effect) Anorexia
Anorexia {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
Diazoxide {u} (Compound) causes {v} (Side Effect) Haemorrhage
Haemorrhage {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
Diazoxide {u} (Compound) causes {v} (Side Effect) Feeling hot
Feeling hot {u} (Side Effect) is caused by {v} (Compound) Propafenone
Propafenone {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Bupropion
Diazoxide {u} (Compound) binds {v} (Gene) KCNJ11
KCNJ11 {u} (Gene) is bound by {v} (Compound) Minoxidil
Minoxidil {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Bupropion
Diazoxide (Compound) downregulates USP22 (Gene) and USP22 (Gene) is downregulated by Bupropion (Compound)
Diazoxide (Compound) causes Chest pain (Side Effect) and Chest pain (Side Effect) is caused by Bupropion (Compound)
Diazoxide (Compound) resembles Chlorothiazide (Compound) and Chlorothiazide may cause a moderate interaction that could exacerbate diseases when taken with Bupropion
Diazoxide (Compound) downregulates USP22 (Gene) and USP22 (Gene) is regulated by GPER1 (Gene) and GPER1 (Gene) is upregulated by Bupropion (Compound)
Diazoxide (Compound) downregulates MTHFD2 (Gene) and MTHFD2 (Gene) regulates GPER1 (Gene) and GPER1 (Gene) is upregulated by Bupropion (Compound)
Diazoxide (Compound) causes Chest pain (Side Effect) and Chest pain (Side Effect) is caused by Tolterodine (Compound) and Tolterodine may cause a minor interaction that can limit clinical effects when taken with Bupropion
Diazoxide (Compound) causes Anorexia (Side Effect) and Anorexia (Side Effect) is caused by Doxazosin (Compound) and Doxazosin may cause a moderate interaction that could exacerbate diseases when taken with Bupropion
Diazoxide (Compound) causes Haemorrhage (Side Effect) and Haemorrhage (Side Effect) is caused by Prasugrel (Compound) and Prasugrel may cause a minor interaction that can limit clinical effects when taken with Bupropion
Diazoxide (Compound) causes Feeling hot (Side Effect) and Feeling hot (Side Effect) is caused by Propafenone (Compound) and Propafenone may cause a moderate interaction that could exacerbate diseases when taken with Bupropion
Diazoxide (Compound) binds KCNJ11 (Gene) and KCNJ11 (Gene) is bound by Minoxidil (Compound) and Minoxidil may cause a moderate interaction that could exacerbate diseases when taken with Bupropion