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Bupropion
Bupropion, formerly called amfebutamone, and sold under the brand name Wellbutrin among others, is an atypical antidepressant that is indicated in the treatment of major depressive disorder, seasonal affective disorder, and to support smoking cessation. It is also popular as an add-on medication in the cases of "incomplete response" to the first-line selective serotonin reuptake inhibitor (SSRI) antidepressant. Bupropion has several features that distinguish it from other antidepressants: it does not usually cause sexual dysfunction, it is not associated with weight gain and sleepiness, and it is more effective than SSRIs at improving symptoms of hypersomnia and fatigue. Bupropion, particularly the immediate-release formulation, carries a higher risk of seizure than many other antidepressants, hence caution is recommended in patients with a history of seizure disorder. The medication is taken by mouth. Common adverse effects of bupropion with the greatest difference fro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydroxybupropion
Hydroxybupropion (code name BW 306U), or 6-hydroxybupropion, is the major active metabolite of the antidepressant and smoking cessation drug bupropion. It is formed from bupropion by the liver enzyme CYP2B6 during first-pass metabolism. With oral bupropion treatment, hydroxybupropion is present in blood plasma, plasma at area under the curve (pharmacokinetics), area under the curve concentrations that are as many as 16 to 20 times greater than those of bupropion itself, demonstrating extensive conversion of bupropion into hydroxybupropion in humans. As such, hydroxybupropion is likely to play a very important role in the effects of oral bupropion, which could accurately be thought of as functioning largely as a prodrug to hydroxybupropion. Hydroxybupropion has two chiral centers and is a racemic mixture, mixture of four possible enantiomers. In humans however, presumably due to steric hindrance, only (2R,3R)-Hydroxybupropion, (2''R'',3''R'')-hydroxybupropion and (2S,3S)-Hydroxybup ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Threohydrobupropion
Threohydrobupropion (developmental code names BW 494, BW A494U) is a substituted amphetamine derivative—specifically a β-hydroxyamphetamine—and a major active metabolite of the antidepressant drug bupropion (Wellbutrin). Bupropion is a norepinephrine–dopamine reuptake inhibitor and nicotinic acetylcholine receptor negative allosteric modulator, with its metabolites contributing substantially to its activities. Chemistry Threohydrobupropion exists as a racemic mixture of two stereoisomers, (1''R'',2''R'')-threohydrobupropion and (1''S'',2''S'')-threohydrobupropion. Other metabolites of bupropion include hydroxybupropion and erythrohydrobupropion. Pharmacology Information on the pharmacological actions of threohydrobupropion is scarce. In any case, it is about 20% as pharmacologically potent as bupropion and in the range of 20 to 50% as potent as bupropion in mouse models of depression. Moreover, threohydrobupropion has been reported to weakly inhibit the reuptake o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Erythrohydrobupropion
Erythrohydrobupropion (developmental codes BW 287, BW 17U) is a substituted amphetamine derivative—specifically a β-hydroxyamphetamine—and a minor active metabolite of the antidepressant drug bupropion (Wellbutrin). Bupropion is a norepinephrine–dopamine reuptake inhibitor and nicotinic acetylcholine receptor negative allosteric modulator, with its metabolites contributing substantially to its activities. Erythrohydrobupropion exists as a racemic mixture of two stereoisomers, (1''R'',2''S'')-erythrohydrobupropion and (1''S'',2''R'')-erythrohydrobupropion. Other metabolites of bupropion include hydroxybupropion and threohydrobupropion. Information on the pharmacological actions of erythrohydrobupropion is scarce. In any case, it is about 20% as pharmacologically potent as bupropion and in the range of 20 to 50% as potent as bupropion in mouse models of depression. It circulates at similar concentrations as bupropion during bupropion therapy. Conversely, two other metabo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Smoking Cessation
Smoking cessation, usually called quitting smoking or stopping smoking, is the process of discontinuing tobacco smoking. Tobacco smoke contains nicotine, which is Addiction, addictive and can cause Substance dependence, dependence. As a result, nicotine withdrawal often makes the process of quitting difficult. Smoking is the Leading causes of preventable death, leading cause of preventable death and a global public health concern. Tobacco use leads most commonly to diseases affecting the heart and lungs, with smoking being a major risk factor for Myocardial infarction, heart attacks, strokes, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF), emphysema, and various types and subtypes of cancers (particularly lung cancer, Oropharyngeal cancer, cancers of the oropharynx, Laryngeal cancer, larynx, and Oral cancer, mouth, Esophageal cancer, esophageal and pancreatic cancer). Smoking cessation significantly reduces the risk of dying from smoking-rel ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidepressant
Antidepressants are a class of medications used to treat major depressive disorder, anxiety disorders, chronic pain, and addiction. Common side effects of antidepressants include Xerostomia, dry mouth, weight gain, dizziness, headaches, akathisia, sexual dysfunction, and emotional blunting. There is an increased risk of Suicidal ideation, suicidal thinking and Suicide, behavior when taken by children, adolescents, and young adults. Antidepressant discontinuation syndrome, Discontinuation syndrome, which resembles recurrent Depression (mood), depression in the case of the Selective serotonin reuptake inhibitor, SSRI class, may occur after stopping the intake of any antidepressant. Research regarding the effectiveness of antidepressants for depression in adults is controversial and has found both benefits and drawbacks. Meanwhile, evidence of benefit in children and adolescents is unclear, even though antidepressant use has considerably increased in children and adolescents in th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Selective Serotonin Reuptake Inhibitor
Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder, anxiety disorders, and other psychological conditions. SSRIs primarily work by blocking serotonin reabsorption (reuptake) via the serotonin transporter, leading to gradual changes in brain signaling and receptor regulation, with some also interacting with sigma-1 receptors, particularly fluvoxamine, which may contribute to cognitive effects. Marketed SSRIs include six main antidepressants— citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, and sertraline—while dapoxetine is indicted for premature ejaculation. Fluoxetine has been approved for veterinary use in treatment of canine separation anxiety. SSRIs are the most widely prescribed antidepressants in many countries. Their effectiveness, especially for mild to moderate depression, remains debated due to mixed research findings and concerns abo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYP2B6
Cytochrome P450 2B6 is an enzyme that in humans is encoded by the ''CYP2B6'' gene. CYP2B6 is a member of the cytochrome P450 group of enzymes. Along with CYP2A6, it is involved with metabolizing nicotine, along with many other substances. Function This gene, CYP2B6, encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and its expression is induced by phenobarbital. The enzyme is known to metabolize some xenobiotics, such as the anti-cancer drugs cyclophosphamide and ifosphamide. Gene Transcript variants for this gene have been described; however, it has not been resolved whether these transcripts are in fact produced by this gene or by a closely related pseudogene Pseudogenes are nonfunctional segments of DNA that resemble functional genes. Pseudo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Seasonal Affective Disorder
Seasonal affective disorder (SAD) is a mood disorder subset in which people who typically have normal mental health throughout most of the year exhibit depressive symptoms at the same time each year. It is commonly, but not always, associated with the reductions or increases in total daily sunlight hours that occur during the winter or summer. Common symptoms include sleeping too much, having little to no energy, and overeating. The condition in the summer can include heightened anxiety.Seasonal affective disorder (SAD): Symptoms MayoClinic.com (September 22, 2011). Retrieved on March 24, 2013. However, there are significant differences in the duration, severity, and symptoms of each individual's experience of SAD. For instance, in a fifth of patients, the disor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine–dopamine Reuptake Inhibitor
A norepinephrine–dopamine reuptake inhibitor (NDRI) is a type of drug that inhibits the reuptake of the monoamine neurotransmitters norepinephrine and dopamine and thereby increases extracellular levels of these neurotransmitters and noradrenergic and dopaminergic neurotransmission. They work by competitively and/or noncompetitively inhibiting the norepinephrine transporter (NET) and dopamine transporter (DAT). NDRIs are used clinically in the treatment of conditions including attention deficit hyperactivity disorder (ADHD), narcolepsy, and depression. Examples of well-known NDRIs include methylphenidate and bupropion. A closely related type of drug is a norepinephrine–dopamine releasing agent (NDRA). List of NDRIs Many NDRIs exist, including the following: Some NDRIs, such as methylphenidate, may not act as simple NDRIs but rather as DAT "inverse agonists" (and possibly also analogously at the NET as well). If this theory is correct, then methylphenidate a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atypical Antidepressant
An atypical antidepressant is any antidepressant medication that acts in a manner that is different from that of most other antidepressants. Atypical antidepressants include: * agomelatine * bupropion * iprindole * opipramol * tianeptine * mianserin * mirtazapine * trazodone * nefazodone The agents vilazodone and vortioxetine are partly atypical. Typical antidepressants include the SSRIs, SNRIs, TCAs, and MAOIs, which act mainly by increasing the levels of the monoamine neurotransmitters serotonin and/or norepinephrine. Among TCAs, trimipramine is an atypical agent in that it appears not to do this. In August 2020, esketamine (JNJ-54135419) was approved by the U.S. Food and Drug Administration (FDA) for the treatment of treatment-resistant depression with the added indication for the short-term treatment of suicidal thoughts. Buprenorphine/samidorphan (ALKS-5461) is an antidepressant with a novel mechanism of action In pharmacology, the term mechanis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Major Depressive Disorder
Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive depression (mood), low mood, low self-esteem, and anhedonia, loss of interest or pleasure in normally enjoyable activities. Introduced by a group of US clinicians in the mid-1970s, the term was adopted by the American Psychiatric Association for this syndrome, symptom cluster under mood disorders in the 1980 version of the ''Diagnostic and Statistical Manual of Mental Disorders'' (DSM-III), and has become widely used since. The disorder causes the second-most years lived with disability, after low back pain, lower back pain. The diagnosis of major depressive disorder is based on the person's reported experiences, behavior reported by family or friends, and a mental status examination. There is no laboratory test for the disorder, but testing may be done to rule out physical conditions that can cause similar symptoms. The most common time o ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dry Mouth
Xerostomia, also known as dry mouth, is a subjective complaint of dryness in the mouth, which may be associated with a change in the composition of saliva, reduced salivary flow, or have no identifiable cause. This symptom is very common and is often seen as a side effect of many types of medication. It is more common in older people (mostly because individuals in this group are more likely to take several medications) and in people who breathe through their mouths. Dehydration, radiotherapy involving the salivary glands, chemotherapy and several diseases can cause reduced salivation (hyposalivation), or a change in saliva consistency and hence a complaint of xerostomia. Sometimes there is no identifiable cause, and there may sometimes be a psychogenic reason for the complaint. Definition Xerostomia is the subjective sensation of dry mouth, which is often (but not always) associated with hypofunction of the salivary glands. The term is derived from the Greek words ξηρός (' ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
