Bupropion antidepressant

As was previously mentioned, a hangover-like syndrome is common the next day after use of MDMA. MDMA withdrawal, which is thought to be caused by serotonin depletion, can last for weeks and includes symptoms of depression, anxiety, restlessness, and insomnia (Allen et al. 1993 McGuite et al. 1994). No specific treatments are currently indicated fot this withdtawal syndrome, although the antidepressant bupropion may be helpful (Solhkhah... 

Many neurotransmitters are inactivated by a combination of enzymic and non-enzymic methods. The monoamines - dopamine, noradrenaline and serotonin (5-HT) - are actively transported back from the synaptic cleft into the cytoplasm of the presynaptic neuron. This process utilises specialised proteins called transporters, or carriers. The monoamine binds to the transporter and is then carried across the plasma membrane it is thus transported back into the cellular cytoplasm. A number of psychotropic drugs selectively or non-selectively inhibit this reuptake process. They compete with the monoamines for the available binding sites on the transporter, so slowing the removal of the neurotransmitter from the synaptic cleft. The overall result is prolonged stimulation of the receptor. The tricyclic antidepressant imipramine inhibits the transport of both noradrenaline and 5-HT. While the selective noradrenaline reuptake inhibitor reboxetine and the selective serotonin reuptake inhibitor fluoxetine block the noradrenaline transporter (NAT) and serotonin transporter (SERT), respectively. Cocaine non-selectively blocks both the NAT and dopamine transporter (DAT) whereas the smoking cessation facilitator and antidepressant bupropion is a more selective DAT inhibitor. 

Bupropion is an atypical antidepressant drug that is the only nonnicotine-based prescription medicine approved for smoking cessation by the FDA. Its mechanism of action is presumed to be mediated by its capacity to block neuronal reuptake of dopamine and/or norepinephrine (Fiore et al. 2000). Relative to other antidepressants, bupropion has a relatively high affinity for the dopamine transporter (Baldessarini 2001). There is also evidence that bupropion acts as a functional nicotine antagonist, suggesting another potential mechanism by which bupropion could reduce smoking rates (Slemmer et al. 2000). 

Atypical antidepressants Bupropion Duloxetine Mianserin Mirtazapine Nefazodone Reboxetine Trazodone Venlafaxine... 

Carbamazepine and possibly the antidepressant mirtazapine should not be coadministered with clozapine because these drugs may further increase the risk of agranulocytosis. In addition, the antidepressant bupropion should not be coprescribed with clozapine because it may increase clozapine s seizure risk. 

Care should be taken when prescribing other medications with clozapine. The mood stabilizer carbamazepine (Tegretol) and perhaps the antidepressant mirtazap-ine (Remeron) should not be taken with clozapine because they might further increase the risk of agranulocytosis. Likewise, the antidepressant bupropion (Wellbutrin, Zyban) should not be taken with clozapine because it may add to the seizure risk. 

Beta agonists (terbutaline, albuterol) Theophylline Antidepressants Bupropion Citalopram Escitalopram Duloxetine Fluoxetine Fluvoxamine... 

Suicidality in children and adolescents Although Zyban is not indicated for treatment of depression, it contains the same active ingredient as the antidepressant bupropion medications Wellbutrin, Wellbutrin SR, and Wellbutrin XL Antidepressants increased the risk of suicidal thinking and behavior (suicidality) in short-term studies in children and adolescents with Major Depressive Disorder (MDD) and other psychiatric disorders. Anyone considering the use of bupropion or any other antidepressant in a child or adolescent must balance this risk with the clinical need. Closely observe patients who are started on therapy for clinical worsening, suicidality, or unusual changes in behavior. Advice families and caregivers of the need for close observation and communication with the prescriber. Bupropion is not approved for use in pediatric patients. 

Antidepressants Bupropion is the active ingredient found in Wellbutrin and Wellbutrin SR used to treat depression. Do not use in combination with Wellbutrin, Wellbutrin SR or any other medication that contains bupropion. 

Bupropion belongs to the chemical class of aminoketones. It is an atypical antidepressant that acts as a norepinephrine and dopamine reuptake inhibitor, and nicotinic antagonist. Initially developed and marketed as an antidepressant, bupropion was subsequently found to be effective as a smoking cessation aid. If given to lactating women it can trigger convulsions in the newborn. 

Goodnick, P.J. (1991) Pharmacokinetics of second generation antidepressants bupropion. Psychopharmacol Bull 27 513—519. 

Other alternatives to the stimulants that have been studied for treatment of ADHD in children and adults include the tricyclic antidepressants desipramine and nortriptyline the newer antidepressants bupropion, venlafaxine, and atomoxetine the beta-blocker pindolol and the selective monoamine oxidase inhibitor, deprenyl. Across these agents, the number of controlled studies varies from none (nortriptyline) to four (bupropion). Only deprenyl and desipramine have been studied in children with ADHD and tic disorders. 

Various antidepressants bupropion hydrochloride nefazodone hydrochloride trazodone hydrochloride L-tryptophan... 

Cooper B, Hester T, Maxwell R. Behavioral and biochemical effects of the antidepressant bupropion (Wellbutrin) evidence of selective blockade of dopamine uptake in vivo. J Pharmacol Exp Ther 1980 215 127-134. 

Bupropion is rapidly absorbed and has a mean protein binding of 85%. It undergoes extensive hepatic metabolism and has a substantial first-pass effect. It has three active metabolites including hydroxybupropion the latter is being developed as an antidepressant. Bupropion has a biphasic elimination with the first phase lasting about 1 hour and the second phase lasting 14 hours. 

Compound Z (molecular formula C9H9CIO) can be converted to the antidepressant bupropion (Figure 18.3) by a series of... 

Since many borderline patients are at risk for transient psychosis, the antidepressant bupropion (a dopamine agonist) should be used with caution. This drug, which is an effective antidepressant, may precipitate psychosis in prepsychotic individuals. 

We now have at least three major groups of antidepressants cyclic antidepressants, selective serotonin reuptake inhibitors (SSRIs), and MAO inhibitors. Additionally, stimulants (such as Dexedrine, Ritalin), atypical antidepressants (bupropion and venlafaxine) and buspirone have been used to treat depression. 

Figure 8.4. Structures of some of the newer atypical antidepressants bupropion, mirtazepine, nefazodone, and trazodone.

Bupropion is a well-tolerated antidepressant. It is non-sedating and lacks the cardiovascular and anticholinergic side effects of tricyclic antidepressants. Bupropion s most commonly observed adverse effects are insomnia and dry mouth. The drug is also known to be associated with a low rate of seizures however, no seizure incidents were reported in the smoking cessation clinical trials. Other less frequently occurring side effects include nervous system disturbances (mainlytremor) and skin rashes (170,182). 

So far, the P DC-catalyzed formation of (R)-PAC (whole cell biotransformation) is the only process for fhe synfhesis of chiral 2-hydroxyketones via carlioligallon used on an industrial scale. The transformations depicted in Scheme 4.3 might provide access to chiral intermediates used in fhe synthesis of biologically active compounds, like fhe antifungal Ro 09-3355 [24], the antidepressant bupropion [25], and the analgesic naproxen [26]. So far, such chiral building blocks have mostly been synthesized by racemic resolution using e. g. lipases. 

The amine hypothesis of mood postulates that brain amines, particularly norepinephrine (NE) and serotonin (5-HT), are neurotransmitters in pathways that function in the expression of mood. According to the amine hypothesis, a functional decrease in the activity of such amines would result in depression a functional increase of activity would result in mood elevation. Difficulties with this hypothesis include the facts that (1) antidepressant drugs cause changes in amine activity within hours, but weeks may be required for them to achieve clinical effects (2) most antidepressants ultimately cause a down-regulation of amine receptors and (3) at least one antidepressant, bupropion, has minimal effects on brain NE or 5-HT. 

Tricyclics modify peripheral sympathetic effects in two ways through blockade of norepinephrine reuptake at neuroeffector junctions and through alpha adrenoceptor blockade. Sedation and atropine-like side effects are common with tricyclics, especially amitriptyline. In contrast to sedative-hypnotics, tricyclics lower the threshold to seizures. The answer is (B). Selective serotonin reuptake inhibitors cause sexual dysfunction in some patients, with changes in libido, erectile dysfunction, and anorgasmia. Tricyclic antidepressants may also decrease libido or prevent ejaculation. Of the heterocyclic antidepressants bupropion is the least likely to affect sexual performance. The drug is also used in withdrawal from nicotine dependence. The answer is (B). 

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