Wellbutrin and Lexapro can be taken together
|Drug class||Antidpressants, agents used to treat nicotine addiction|
|Mechanism of action|| Selective norepinephrine |
and dopamine reuptake inhibitors
|Bioavailability||> 87 %|
|Protein binding||84 %|
|Volume of Distribution||~ 2000 l|
|Plasma half-life||24 hours|
|LD50(Rat)||980 mg / kg (oral)|
|Finished medicinal products|
|Wellbutrin®, Budeprion®, Elontril®, Zyban®|
Bupropion (before 2000 Amfebutamone) is a selective norepinephrine and dopamine (slightly also serotonin) reuptake inhibitor (NDRI) from the group of atypical antidepressants.
Approval as an antidepressant
Bupropion had been approved as an antidepressant in the USA since 1984, but was withdrawn in 1986 because of repeated reports of seizures, some of which were fatal. However, after subsequent additional studies, it was found that seizures are a rare and dose-dependent side effect even with this drug. As a result, approval in the USA was granted again in 1989.
In Germany, approval as an antidepressant in a retarded preparation form was granted on April 2, 2007, although the calculated particularly low probability of seizures with this preparation form was not uncontroversial in Germany. Bupropion was used off-label as an antidepressant even before it was officially approved.
Chemically, bupropion belongs to the phenylalkylamines (phenethylamines), more precisely to their subgroup of the amphetamines. Another subgroup of the phenylalkylamines are the catecholamines, which include, for example, the neurotransmitters dopamine, noradrenaline and adrenaline; bupropion is therefore also closely related to these.
Bupropion is approved for the treatment of depression. The overall data situation for use as an antidepressant is unsatisfactory: 2 of 4 studies relevant for approval cannot show any benefit. The only published study is criticized because it only includes patients who had already responded to pretreatment with bupropion, examined a sustained-release preparation that was not sold in Germany, and had about a third of the original participants who dropped out of the study. Suicidal behavior occurs slightly more frequently with bupropion than with placebo, but this difference cannot be statistically proven beyond doubt.
The substance is approved for smoking cessation. A meta-analysis of 31 studies showed that the proportion of patients receiving bupropion treatment who did not smoke for at least six months after treatment was 19%, almost twice as high as that of 10.3% receiving placebo -Treatment. In direct comparison, bupropion is just as effective as nicotine patches. Nicotine patches added to bupropion did not improve the rate of abstinence. There is evidence that bupropion is inferior to varenicline. The therapy is only promising for carriers of a certain gene variant in the cytochrome P450 system, which is widespread in people of European descent. About 45% of all people of European origin have the genotype CYP2B6 * 6. However, it is far less common in people of other origins. 33% of the carriers of this gene variant were able to quit smoking with bupropion (in the test subjects who received a placebo it was only 14%). However, carriers of another gene variant (genotype CYP2B6 * 1) did not benefit from bupropion. , .
Bupropion can be used against ADHD, although the substance has not been approved in Germany and has not been tested for effectiveness and safety in patients under 18 years of age. Bupropion can cause decreased appetite and weight loss, but is not approved for this purpose. In a 48-week, manufacturer-funded study, patients treated with bupropion lost slightly more weight (up to 5.1%) than those who took a dummy drug (placebo). That would roughly correspond to the effect of others Slimming. Whether the body weight increases again after stopping - as is known from similar substances such as sibutramine (Jojo effect), has not yet been clarified.
MAO inhibitors also act on catecholaminergic metabolic pathways and must therefore not be used at the same time. There is evidence of rare neuropsychiatric side effects associated with simultaneous alcohol consumption. The risk of seizures increases with concomitant use of drugs that lower the seizure threshold, such as certain antipsychotics, antidepressants, antimalarials, tramadol, theophylline, systemic steroids, quinolones, and sedating antihistamines.
Effect of bupropion on other drugs
Bupropion and its metabolic products inhibit the CYP450-2D6 metabolic pathway and lead to an increase in the blood level of all tricyclics except doxepin (very strong: desipramine, nortriptyline, strong: clomipramine) and many SSRIs, the painkiller tramadol, antipsychotics such as risperidone and thioridazine Metoprolol, class 1C antiarrhythmics such as propafenone and flecainide. The citalopram level also rises despite a different metabolic pathway when taken at the same time. The sedative effect of diazepam is reduced. Simultaneous administration with nicotine patches can lead to an increase in blood pressure.
Effect of other drugs on bupropion
Bupropion itself is metabolized to its active metabolite hydroxybupropion via the cytochrome P450-2B6. Drugs that affect this metabolic pathway (such as cyclophosphamide, isofosfamide, orphenadrine, ticlopidine, clopidogrel) shift the ratio of bupropion to hydroxybupropion with an unexplained effect. Caution is advised when used concomitantly with other drugs known to interfere with the metabolic pathways such as carbamazepine, phenytoin and valproic acid. Bupropion should be used with caution with levodopa and amantadine, as side effects are increased.
Combination with other antidepressants
The combination of bupropion with other antidepressants (except citalopram and desipramine), benzodiazepines (except diazepam) and neuroleptics has not been systematically investigated. Combinations of bupropion with different SSRIs were only carried out in the context of studies on the effect of bupropion on sexual dysfunctions triggered by SSRIs.
In combination with other antidepressants, bupropion is said to compensate for some of the side effects of these substances. Unwanted fatigue caused by sedating antidepressants (e.g. mianserin and mirtazapine) can, if necessary, be counteracted by the stimulating effect of bupropion. To relieve symptoms of tiredness, bupropion is taken at the beginning and the tiring antidepressant at the end of the day. Sleep-promoting or sexually depressant antidepressants can counteract sleep disorders or priapism caused by bupropion. Correcting the side effects of other antidepressants is not an approved indication for bupropion.
The idea of improving sexual dysfunction under treatment with other antidepressants by adding bupropion was discarded after several negative clinical studies.
Bupropion is very different in its side effect profile from the commonly used antidepressants, because the side effects are mainly the typical side effects of psychostimulants. The most common side effects are dry mouth and insomnia, although the latter can be reduced by avoiding medication at bedtime. Other side effects may include be: headache, drowsiness, loss of appetite, joint and muscle pain, tremors, fear, difficulty concentrating, confusion. In addition, bupropion (the medical emergency) can trigger priapism or increase blood pressure and heart rate.
Bupropion has a proconvulsive (convulsive) effect. It can cause seizures in people who have no previous history, as well as lowering the seizure threshold of people who are prone to convulsions. Overall, however, seizures are a rare and dose-dependent side effect even with this drug. The frequency is given as 0.1% in the dose range up to 450 mg. Only at doses of 600 mg / day or more does the statistical risk of seizures suddenly increase rapidly.
With prolonged or frequent use, addictive behavior cannot be ruled out. In a study by the Innsbruck University Clinic it was found that around six percent of all test subjects got a "high" feeling from bupropion. However, caffeine in an amount that corresponds to two cups of strong coffee produced significantly stronger “pleasant effects” and “high feelings” than bupropion in the group of smokers tested 
As a phenylalkylamine, bupropion has pharmacologically similar structures to amphetamines. It is possible that patients taking bupropion will get positive results in the amphetamine or methamphetamine group on a urinal drug test.
In contrast to many other antidepressants - especially SSRIs - bupropion has much less or no limiting effects on sexual function. This has been shown in comparative studies, especially in men, since women are far less prone to sexual dysfunction caused by antidepressants. Namely in studies regarding venlafaxine, Paroxetine, Sertraline, Escitalopram and fluoxetine It was found that, unlike the comparator drugs, bupropion is largely free of side effects on sexual function. An improvement in sexual function or a compensation of functional disorders caused by treatment with other antidepressants, however, was neither investigated nor ascertained.
- J. Schöpf: Modern antidepressants - switch, combine and augment, Steinkopf Verlag Darmstadt, 2003. ISBN 3-7985-1426-7
- Brigitte Woggon: Treatment with psychotropic drugs, 2nd, completely revised and expanded edition 2005. Verlag Hans Huber, Hogrefe AG, Bern 1998/2005. ISBN 3-456-83538-8
- ↑ ab drug telegram 2007; 38: 45-6.
- ↑ WEIHS, K.L. et al .: Biol. Psychiatry 2002; 51: 753-61
- ↑ http://ctr.gsk.co.uk/Summary/bupropion/IV_suicide_observational.pdf
- ↑ Hughes JR, Stead LF, Lancaster T. Antidepressants for smoking cessation. Cochrane Database of Systematic Reviews 2007, Issue 1. Art. No .: CD000031
- ↑ Cahill K, Stead LF, Lancaster T. Nicotine receptor partial agonists for smoking cessation. Cochrane Database of Systematic Reviews 2007, Issue 1. Art. No .: CD006103. doi: 10.1002 / 14651858.CD006103.pub2
- ↑ Biological Psychiatry (2007); 62: pp. 635-641
- ↑ http://www.aerzteblatt-studieren.de/doc.asp?docId=106337
- ↑ Bupropion ADHD (English)
- ↑ abcdef Technical information Elontril, GSK 02/2007
- ↑ Bloodhound Scientist - Sniffing out the latest research at Nutrition Week 2002 at T-Nation ™
- ↑ Obesity Research 10: 633-641 (2002)
- ↑ Expert Rev Neurother. 2007 Jan; 7 (1): 17-24.
- ↑ abSustained-release bupropion for selective serotonin reuptake inhibitor-induced sexual dysfunction: a randomized, double-blind, placebo-controlled, parallel-group study. (English abstract) at PubMed
- ↑ abA placebo-controlled trial of bupropion SR as an antidote for selective serotonin reuptake inhibitor-induced sexual dysfunction. (English abstract) at PubMed
- ↑ J. Schöpf: "Modern antidepressants - changing, combining and augmenting", Steinkopf Verlag Darmstadt, 2003. ISBN 3-7985-1426-7
- ↑ Brigitte Woggon: "Treatment with Psychopharmaka", 2nd, completely revised and expanded edition 2005. Hans Huber publishing house, Hogrefe AG, Bern 1998/2005. ISBN 3-456-83538-8
- ↑ DeBattista, C. et al. (2005): A placebo-controlled, randomized, double-blind study of adjunctive bupropion sustained release in the treatment of SSRI-induced sexual dysfunction. In: J. Clin. Psychiatry. Vol. 66, No. 7, pp. 844-848. PMID 16013899
- ↑ Wellbutrin (bupropion) (English) at NAMI
- ↑ Zyban - Side Effects (English) at RxList
- ↑ Yellow list: Elontril® product information, April 2007.
- ↑ Addicted to Bupropion? (German abstract) - doi: 10.1159 / 000075550 (English original article)
- ↑A double-blind comparison between bupropion XL and venlafaxine XR: sexual functioning, antidepressant efficacy, and tolerability. (English abstract) at PubMed
- ↑Sexual function during bupropion or paroxetine treatment of major depressive disorder. (English abstract) at PubMed
- ↑A placebo-controlled comparison of the antidepressant efficacy and effects on sexual functioning of sustained-release bupropion and sertraline. (English abstract) at PubMed
- ↑Sexual dysfunction associated with the treatment of depression: a placebo-controlled comparison of bupropion sustained release and sertraline treatment. (English abstract) at PubMed
- ↑Evaluation of sexual functioning in depressed outpatients: a double-blind comparison of sustained-release bupropion and sertraline treatment. (English abstract) at PubMed
- ↑Bupropion extended release compared with escitalopram: effects on sexual functioning and antidepressant efficacy in 2 randomized, double-blind, placebo-controlled studies. (English abstract) at PubMed
- ↑A placebo-controlled comparison of the effects on sexual functioning of bupropion sustained release and fluoxetine. (English abstract) at PubMed
Categories: Phenylethylamine | Antidepressant | Drug
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