Key:SNPPWIUOZRMYNY-UHFFFAOYSA-N Y Bupropion, sold under the brand names Wellbutrin and Zyban among others, is a primarily used as an and aid. It is an effective antidepressant on its own, but is also used as an add-on medication in cases of incomplete response to first-line. Bupropion is taken in tablet form and is available only by prescription in most countries. Common side effects include dry mouth, trouble sleeping, agitation, and headaches. Serious side effects include an increased, which caused the drug to be withdrawn from the market for some time and then the recommended dose to be reduced. In comparison to some other antidepressants, it does not cause as much or, and may result in. It is unclear if use during pregnancy is safe.

Bupropion is known to affect several different. It is a (NDRI) and a. It is an, different from most others.

Chemically, bupropion is a that belongs to the of and the more general class of. Bupropion was first made by and patented by Burroughs Wellcome in 1969, which later became part of. It was first approved for medical use in the United States in 1989. It was originally called by the generic name amfebutamone, before being renamed in 2000.

In 2016 it was the third most prescribed antidepressant in the United States. Wellbutrin XL Depression Bupropion is one of the most widely prescribed antidepressants, and the available evidence indicates that it is effective in. A 2018 meta-analysis of the comparative efficacy of 16 antidepressants found strong evidence of efficacy for all antidepressants except bupropion and vilazodone, both of which had few available clinical trials; the little evidence that was available showed that bupropion and vilazodone had only a weak antidepressant effect.

A 2016 meta-analysis of clinical trials found that bupropion therapy for depression is superior to placebo. Most of the trials which compared bupropion to other drugs for depression showed similar effectiveness, but this finding is based in part upon low-quality evidence. A meta-analysis from 2009 found that bupropion is as effective as several other widely prescribed drugs, including and, although trends favoring the efficacy of, and over bupropion have been observed. It also found that is more effective than bupropion.

Bupropion was approved by the (FDA), in 2006, for the prevention of (SAD). In some countries (including, and the ) depression treatment and SAD prevention are off-label uses. A review on the use of extended-release bupropion for the treatment of seasonal affective disorder found that bupropion is effective in preventing the recurrence of the disorder; however, four out of five individuals who take the drug will not benefit from treatment and may be at risk for harm. Bupropion has several features that distinguish it from other antidepressants: for instance, unlike the majority of antidepressants, it does not usually cause sexual dysfunction. Bupropion treatment also is not associated with the or weight gain that may be produced by other antidepressants. In depressed people who experience symptoms of sleepiness and fatigue, bupropion has been found to be more effective than (SSRIs) in alleviating these symptoms.

There appears to be a modest advantage for the SSRIs over bupropion in the treatment of anxious depression. The addition to a prescribed SSRI is a common strategy when people do not respond to the SSRI, even though this is not an officially approved indication. The addition of bupropion to an SSRI (most commonly fluoxetine or sertraline) may result in an improvement in some people who have an incomplete response to the first-line antidepressant. Smoking cessation Bupropion is prescribed as an aid for smoking cessation. Bupropion reduces the severity of cravings and symptoms.

Bupropion is helpful for smoking cessation in smokers with no history of depression; thus, the effectiveness of bupropion is not due to its antidepressant effect. A typical bupropion treatment course lasts up to twelve weeks, with people halting the use of tobacco about ten days into the course.

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Bupropion increases the likelihood of quitting smoking by approximately 1.6 fold. The effectiveness of bupropion is comparable to, but less effective than.

Animal studies indicate that administration of bupropion at less than the recommended therapeutic dose may actually enhance the rewarding properties of nicotine, i.e., low doses augment nicotine self-administration and high doses attenuate it. In Australia and the UK, smoking cessation is the only licensed use of bupropion.

Attention deficit hyperactivity disorder. This section needs to be updated.

Please update this article to reflect recent events or newly available information. (July 2018) Bupropion has been used as a treatment for (ADHD) since at least 2004, with reports of positive results in both minors and adults.

In a double-blind study of children, while aggression and hyperactivity as rated by the children's teachers were significantly improved in comparison to placebo, parents and clinicians could not distinguish between the effects of bupropion and placebo. The 2007 guideline on the ADHD treatment from American Academy of Child and Adolescent Psychiatry notes that the evidence for bupropion is 'far weaker' than for the FDA-approved treatments. Its effect may also be 'considerably less than of the approved agents. Thus it may be prudent for the clinician to recommend a trial of behavior therapy at this point, before moving to these second-line agents.'

Similarly, the Texas Department of State Health Services guideline recommends considering bupropion or a as a fourth-line treatment after trying two different stimulants. Sexual dysfunction Bupropion is one of few antidepressants that does not cause sexual dysfunction. A range of studies demonstrate that bupropion not only produces fewer sexual side effects than other antidepressants, but can actually help to alleviate sexual dysfunction. According to a survey of psychiatrists, it is the drug of choice for the treatment of SSRI-induced sexual dysfunction, although this is not an indication approved by the. There have also been a few studies suggesting that bupropion can improve sexual function in women who are not depressed, if they have (HSDD). Obesity Bupropion, when used for treating over a period of 6 to 12 months, may result in weight loss of 2.7 kg (5.9 lbs) over placebo. This is not much different from the weight loss produced by several other medications, such as.

It has been studied in combination with. Concerns from bupropion include an increase in blood pressure and heart rate. In September 2014, a was approved by the US FDA for the treatment of obesity. Other uses Several other uses have been researched for bupropion. There has been controversy about whether it is useful to add an antidepressant such as bupropion to a in people with, but recent reviews have concluded that bupropion in this situation does no significant harm and may sometimes give significant benefit. Bupropion has shown no effectiveness in the treatment of cocaine dependence, but there is weak evidence that it may be useful in treating methamphetamine dependence. Based on studies indicating that bupropion lowers the level of the inflammatory mediator, there have been suggestions that it might be useful in treating or other autoimmune conditions, but very little clinical evidence is available.

Bupropion—like other antidepressants, with the exception of (Cymbalta) —is not effective in treating chronic low back pain. It does, however, show some promise in the treatment of. Contraindications The drug label advises that bupropion should not be prescribed to individuals with or other conditions that lower the, such as, active brain tumors, or concurrent alcohol and/or use and/or withdrawal.

It should be avoided in individuals who are also taking (MAOIs). When switching from MAOIs to bupropion, it is important to include a washout period of about two weeks between the medications.

The label recommends that caution should be exercised when treating people with liver damage, severe, and severe, and in children, adolescents and young adults due to the increased risk of. Side effects. See also: are the most important adverse effect of bupropion. A high incidence of seizures was responsible for the temporary withdrawal of the drug from the market between 1986 and 1989. The risk of seizure is strongly dose-dependent, but also dependent on the preparation.

The sustained-release preparation is associated with a seizure incidence of 0.1% at daily dosages of less than 300 mg of bupropion and 0.4% at 300–400 mg. The immediate release preparation is associated with a seizure incidence of 0.4% for dosages below 450 mg; the incidence climbs to 5% for dosages between 450–600 mg per day. For comparison, the incidence of unprovoked seizure in the general population is 0.07 to 0.09%, and the risk of seizure for a variety of other antidepressants is generally between 0.1 and 1.5% at recommended dosage levels.

Clinical depression itself has been reported to increase the occurrence of seizures, and a study examining FDA clinical trial data has suggested that in most cases, low to moderate doses of antidepressants may not actually increase seizure risk at all. However, this study also found that bupropion and were unique among antidepressants in that they were associated with increased incidence of seizures.

The prescribing information notes that, sometimes severe, was observed in some people taking bupropion, both with and without pre-existing hypertension. The frequency of this adverse effect was under 1% and not significantly higher than found with placebo. A review of the available data carried out in 2008 indicated that bupropion is safe to use in people with a variety of serious cardiac conditions. In the UK, more than 7,600 reports of suspected adverse reactions were collected in the first two years after bupropion's approval by the as part of the, which monitored side effects. Approximately 540,000 people were treated with bupropion for smoking cessation during that period.

The MHRA received 60 reports of ' suspected emphasis MHRAs adverse reactions to Zyban which had a fatal outcome'. The agency concluded that 'in the majority of cases the individual's underlying condition may provide an alternative explanation.' This is consistent with a large, 9,300-subject safety study that showed that the mortality of smokers taking bupropion is not higher than the natural mortality of smokers of the same age. Psychiatric Suicidal thoughts and behaviors are rare in clinical trials, and the FDA requires all antidepressants, including bupropion, to carry a stating that antidepressants may increase the risk of suicide in persons younger than 25. This warning is based on a statistical analysis conducted by the FDA which found a 2-fold increase in and behavior in children and adolescents, and 1.5-fold increase in the 18–24 age group. For this analysis the FDA combined the results of 295 trials of 11 antidepressants in order to obtain statistically significant results.

Considered in isolation, bupropion was not statistically different from placebo. Suicidal behavior is less of a concern when bupropion is prescribed for smoking cessation. According to a 2014, while there is an association with suicide it is unclear if bupropion was the cause.

In 2016 the FDA removed the black box warning about psychiatric problems when used for stopping smoking. In 2009 the FDA issued a health advisory warning that the prescription of bupropion for smoking cessation has been associated with reports about unusual behavior changes, agitation and hostility. Some people, according to the advisory, have become depressed or have had their depression worsen, have had thoughts about suicide or dying, or have attempted suicide. This advisory was based on a review of anti-smoking products that identified 75 reports of 'suicidal adverse events' for bupropion over ten years. Bupropion-induced may develop in select populations, or worsen a pre-existing psychotic syndrome. Symptoms may include, hallucinations, and confusion.

In most cases these symptoms can be reduced or eliminated by reducing the dose, ceasing treatment or adding antipsychotic medication. However, adding a benzodiazepine to treat psychosis, instead of an antipsychotic, may become a valid alternative according to the model of amphetamine-induced psychosis. Psychotic symptoms are associated with factors such as higher doses of bupropion, a history of bipolar disorder or psychosis, concomitant medications, for example, lithium or benzodiazepines, old age, or substance abuse.

In a large-scale study of programs where bupropion was used for smoking cessation or treatment of depression, no withdrawal symptoms were observed. As of 2002 there were two case reports of people experiencing withdrawal symptoms when discontinuing bupropion taken to aid smoking cessation; the prescribing information states that dose tapering is not required when discontinuing treatment for smoking cessation. Overdose Bupropion is considered moderately dangerous in overdose. For significant overdoses, seizures have been reported in about a third of all cases; other serious effects include hallucinations, loss of consciousness,.

When bupropion was one of several kinds of pills taken in an overdose, fever, muscle rigidity, muscle damage, hypertension or hypotension, stupor, coma, and respiratory failure have been reported. While most people recover, some people have died, and before they died suffered multiple uncontrolled seizures and heart attacks. In the majority of childhood exploratory ingestions involving one or two tablets, children show no apparent symptoms. Interactions Since bupropion is metabolized to by the enzyme, drug interactions with CYP2B6 inhibitors are possible: this includes medications like paroxetine, sertraline, fluoxetine,.

The expected result is the increase of bupropion and decrease of hydroxybupropion blood concentration. The reverse effect (decrease of bupropion and increase of hydroxybupropion) can be expected with CYP2B6, such as, and others. Conversely, because bupropion is itself a strong inhibitor of ( = 21 μM), as is its active metabolite, hydroxybupropion (K i = 13.3 μM), it can slow the clearance of other drugs metabolized by this enzyme. As an example, the ratio of (a drug that is mainly metabolized by CYP2D6) to its major increased approximately 35-fold when it was administered to people being treated with 300 mg/day bupropion, indicative of a major drug interaction with a common medicine.

Bupropion lowers the threshold for, and therefore can potentially interact with other medications that also lower it, such as, agents, systemic (e.g., ), and some (e.g., ). The prescribing information recommends minimizing the use of, since in rare cases bupropion reduces alcohol tolerance, and because the excessive use of alcohol may lower the seizure threshold. Also, bupropion should not be taken by individuals undergoing abrupt cessation of alcohol or use. Caution should be observed when combining bupropion with a (MAOI), as it may result in. Of racemic bupropion. The carbonyl reductase enzyme that is responsible for producing erythro-bupropion is unknown as of March 2015.

Bupropion is metabolized in the liver by the isoenzyme. It has several active metabolites: R,R-hydroxybupropion, S,S-hydroxybupropion, threo-hydrobupropion and erythro-hydrobupropion, which are further metabolized to inactive metabolites and eliminated through excretion into the urine. Both bupropion and its primary metabolite hydroxybupropion act in the liver as potent inhibitors of the enzyme, which metabolizes not only bupropion itself but also a variety of other drugs and biologically active substances. This mechanism creates the potential for a variety of drug interactions. The biological activity of bupropion can be attributed to a significant degree to its active metabolites, in particular to S,S-hydroxybupropion. GlaxoSmithKline developed this metabolite as a separate drug called, but discontinued development in 2006 due to 'an unfavourable risk/benefit assessment'.

Bupropion is metabolized to hydroxybupropion by, an of the. Alcohol causes an increase of CYP2B6 in the liver, and persons with a history of alcohol use metabolize bupropion faster. Bupropion is metabolized to threo-hydrobupropion via. The metabolic pathway responsible for the creation of erythro-hydrobupropion remains elusive.

The metabolism of bupropion is highly variable: the effective doses of bupropion received by persons who ingest the same amount of the drug may differ by as much as 5.5 times (with a of 12–30 hours), while the effective doses of may differ by as much as 7.5 times (with a half-life of 15–25 hours). Based on this, some researchers have advocated monitoring of the blood level of bupropion and hydroxybupropion. The half-lives of and are roughly 23–43 hours and 24–50 hours respectively. There have been reported cases of false-positive urine amphetamine tests in persons taking bupropion.

In 2016, three new major metabolites of bupropion, all formed exclusively by, were identified. These include 4'-OH-bupropion, erythro-4'-OH-hydrobupropion and threo-4'-OH-hydrobupropion, and represent 24% of a dose of bupropion excreted in urine. For comparison, bupropion and its three previously known primary metabolites, hydroxybupropion, threohydrobupropion, and erythrohydrobupropion represent 23% of a dose of bupropion excreted in urine. Chemistry Bupropion is a that belongs to the of and the more general class of.

Synthesis It is synthesized in two chemical steps starting from 3'-chloro. The alpha position adjacent to the ketone is first followed by of the resulting alpha-bromoketone with and treated with to give bupropion as the hydrochloride salt in 75–85% overall yield. A profile comparison of 150 mg extended-release bupropion as produced by for and for. Bupropion was invented by Nariman Mehta of Burroughs Wellcome (now ) in 1969, and the US patent for it was granted in 1974. It was approved by the (FDA) as an antidepressant on 30 December 1985, and marketed under the name Wellbutrin. However, a significant incidence of at the originally recommended dosage caused the withdrawal of the drug in 1986. Subsequently, the risk of seizures was found to be highly dose-dependent, and bupropion was re-introduced to the market in 1989 with a lower maximum recommended daily dose.

In 1996, the FDA approved a formulation of bupropion called Wellbutrin SR, intended to be taken twice a day (as compared with three times a day for immediate-release Wellbutrin). In 2003, the FDA approved another sustained-release formulation called Wellbutrin XL, intended for once-daily dosing. Wellbutrin SR and XL are available in form in the United States and Canada. In Canada, generic XR bupropion is distributed by Mylan. In 1997, bupropion was approved by the FDA for use as a smoking cessation aid under the name Zyban.

In 2006, Wellbutrin XL was similarly approved as a treatment for seasonal affective disorder. In France, marketing authorization was granted for Zyban on 3 August 2001, with a maximum daily dose of 300 mg; only sustained-release bupropion is available, and only as a smoking cessation aid. Bupropion was granted a licence for use in adults with major depression in the Netherlands in early 2007, with GlaxoSmithKline expecting subsequent approval in other European countries. On 11 October 2007, two providers of consumer information on nutritional products and supplements, and The People's Pharmacy, released the results of comparative tests of different brands of bupropion. The People's Pharmacy received multiple reports of increased side effects and decreased efficacy of generic bupropion, which prompted it to ask ConsumerLab.com to test the products in question. The tests showed that 'one of a few generic versions of Wellbutrin XL 300 mg, sold as Budeprion XL 300 mg, didn't perform the same as the brand-name pill in the lab.'

The FDA investigated these complaints and concluded that Budeprion XL is equivalent to Wellbutrin XL in regard to bioavailability of bupropion and its main active metabolite hydroxybupropion. The FDA also said that coincidental natural mood variation is the most likely explanation for the apparent worsening of depression after the switch from Wellbutrin XL to Budeprion XL. On 3 October 2012, however, the FDA reversed this opinion, announcing that 'Budeprion XL 300 mg fails to demonstrate therapeutic equivalence to Wellbutrin XL 300 mg.' The FDA did not test the bioequivalence of any of the other generic versions of Wellbutrin XL 300 mg, but requested that the four manufacturers submit data on this question to the FDA by March 2013. As of October 2013 the FDA has made determinations on the formulations from some manufacturers not being bioequivalent.

In April 2008, the FDA approved a formulation of bupropion as a hydrobromide salt instead of a hydrochloride salt, to be sold under the name Aplenzin. In 2012, the U.S.

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Justice Department announced that GlaxoSmithKline had agreed to plead guilty and pay a $3-billion fine, in part for promoting the unapproved use of Wellbutrin for weight loss and sexual dysfunction. Society and culture Names Bupropion is the (INN) and (BAN) while bupropion hydrochloride is the (USAN). Amfebutamone was the former INN.

Recreational use According to the US government classification of psychiatric medications, bupropion is 'non-abusable'. However, in animal studies, and rats could be induced to self-administer bupropion, which is often taken as a sign of addiction potential.

There have been a number of anecdotal and case-study reports of bupropion abuse, but the bulk of evidence indicates that the subjective effects of bupropion via the oral route are markedly different from those of addictive stimulants such as cocaine or amphetamine. That said, bupropion, via non-conventional routes of administration (e.g., injection, insufflation), is reported to be abused in the and, notably in prisons.

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