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Wellbutrin

Wellbutrin
Wellbutrin is used to treat major depressive disorder and seasonal affective disorder.

Brand: Bupropion

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: April 2024
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Wellbutrin 300 mg
120 pills - 300 mg
+ 8 free Viagra 100 mg, 5% discount for future orders
$225.95 $1.88 $73.75 Add to cart
90 pills - 300 mg
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$173.98 $1.93 $50.80 Add to cart
60 pills - 300 mg
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$119.93 $2.00 $29.92 Add to cart
30 pills - 300 mg $67.01 $2.23 $7.92 Add to cart
20 pills - 300 mg $49.95 $2.50 No Add to cart
Wellbutrin 150 mg
120 pills - 150 mg
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$141.99 $1.18 $41.57 Add to cart
90 pills - 150 mg
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$113.95 $1.27 $23.72 Add to cart
60 pills - 150 mg $81.33 $1.36 $10.45 Add to cart
30 pills - 150 mg $45.89 $1.53 No Add to cart

Product description

Drug Name

Wellbutrin (Bupropion)

Pharmacological action

Bupropion is a selective inhibitor of catecholamine reuptake (noradrenaline and dopamine) with little effect on indoleamine (serotonin) reuptake, it does not inhibit monoamine oxidase.


Although the mechanism of action of bupropion, like other antidepressants, is currently unknown, it is assumed that its antidepressant effect is carried out by influencing the noradrenergic and/or dopaminergic mediator system.


Clinical efficacy


The efficacy and tolerability of bupropion in sustained release tablets have been investigated in 7 double-blind studies; of these 7 studies, 3 were conducted in Europe in the dose range of interest (up to 300 mg/day). The next 4 studies were conducted in the United States with a flexible dose range up to 450 mg/day. Evidence of long-term effect support was provided by the 1-year study of exacerbation prevention with bupropion; 816 patients received bupropion in the single-blind phase of this study, of whom 423 were randomized to a follow-up double-blind phase (bupropion, 210; placebo, 213).


Bupropion was effective in patients with mild to moderate depression, as well as in patients with severe depression. In pooled European comparative studies, similar degrees of superiority of the drug over placebo were observed in both patients with mild to moderate depression (-1.8, p=0.032) and patients with severe depression (-2.3, p=0.041).


Pharmacokinetics

Absorption


After oral administration of bupropion in sustained-release tablets in healthy volunteers, the time to reach maximum plasma concentration was approximately 5 hours.


Food intake has no significant effect on absorption of bupropion in sustained release tablets.


The kinetics of bupropion and its metabolites are linear with chronic therapy at doses ranging from 150 to 300 mg/day.


Distribution


Bupropion penetrates tissues well; its apparent volume of distribution is approximately 2,000 L.


Bupropion and hydroxybupropion are moderately bound to plasma proteins (84% and 77%, respectively). The degree of binding to proteins of the trio-hydrobupropion metabolite is about 50% of that of bupropion.


Metabolism


Bupropion undergoes intensive metabolism. Three active metabolites are detected in plasma: hydroxybupropion and aminopyrate isomers - treo-hydrobupropion and erythro-hydrobupropion. This fact may be of clinical significance, since plasma concentrations of the metabolites are high or even exceed plasma concentrations of bupropion. Erythro-hydrobupropion is not quantified in plasma after a single dose of the drug. Active metabolites are further metabolized to inactive metabolites and excreted by the kidneys.


In in vitro studies, it was shown that bupropion is metabolized to its main metabolite hydroxybupropion primarily through the CYP2B6 isoenzyme system, while the cytochrome P450 isoenzyme system is not involved in the formation of trio-hydrobupropion


In vitro, bupropion and hydroxybupropion are relatively weak competitive inhibitors of the CYP2D6 isoenzyme system (Ki - inhibition constant is 21 and 13.3 μmol, respectively). In volunteers who were highly metabolized by the CYP2D6 isoenzyme, the simultaneous administration of bupropion and desipramine resulted in a two- to fivefold increase in Cmax and AUC of desipramine This effect was maintained for at least 7 days after the last dose of bupropion.


Because bupropion is not metabolized by the CYP2D6 isoenzyme, desipramine should not be expected to affect the pharmacokinetics of bupropion. Caution is advised when prescribing bupropion concomitantly with substrate drugs for the CYP2D6 isoenzyme enzyme system.


Studies involving volunteers or patients receiving recommended doses of bupropion for 10-45 days have not shown induction of enzyme systems by bupropion or hydroxybupropion


The Cmax of hydroxybupropion in plasma is approximately 10 times the maximum concentration of the parent substance in equilibrium.


The time to reach Cmax for erythro-hydrobupropion and trio-hydrobupropion is approximately the same as for hydroxybupropion.


In a study in healthy volunteers, concomitant administration of ritonavir at a dose of 100 mg twice daily resulted in a 22% and 21% reduction in AUC and Cmax of bupropion, respectively. The AUC and Cmax of bupropion metabolites were reduced by 0 to 44%. In another study in healthy volunteers, ritonavir at a dose of 600 mg twice daily reduced the AUC and Cmax of bupropion by 66% and 62%, respectively. The AUC and Cmax of bupropion metabolites were reduced by 42% and 78%, respectively.


In a study in healthy volunteers, combined administration of the combination drug loinavir 400 mg/ritonavir 100 mg twice daily decreased the AUC and Cmax of bupropion by 57%. AUC and Cmax of hydroxybupropion were decreased by 50% and 31%, respectively.


The Cmax of hydroxybupropion in plasma is reached 7 hours after administration of bupropion in sustained release tablets.


Excretion


After ingestion of 200 mg of carbon isotope C14-labeled bupropion, 87% and 10% of the radioactive dose were detected in the urine and feces, respectively. The bupropion dose fraction excreted unchanged was only 0.5% due to active metabolism of bupropion. Less than 10% of the isotope-labeled dose was detected in the urine as an active metabolite


The clearance of bupropion when taken orally is approximately 200 l/h and the elimination half-life is 20 h.


The T1/2 of hydroxybupropion is approximately 20 h, the AUC in equilibrium is approximately 17 times that of bupropion. The T1/2 of trio-hydrobupronion and erythro-hydropropion are longer (37 and 33 h, respectively), with AUCs 8 and 1.6 times higher than those of bupropion. Time to reach equilibrium state of bupropion and its metabolites is within 8 days.

Contraindications to use

  • Hypersensitivity to bupropion or any other component of the drug;
  • seizure disorders;
  • abrupt withdrawal of alcohol or sedatives (including benzodiazepines);
  • concomitant use of other bupropion-containing medications (the occurrence of seizures is a dose-dependent effect);
  • history of bulimia or anorexia nervosa (seizures are possible);
  • concomitant use with MAO inhibitors. Bupropion therapy should not be started at least 2 weeks after withdrawal of irreversible MAO inhibitors.
  • Under 18 years of age.

Caution should be exercised in patients with impaired liver function, impaired renal function, cardiovascular disease and decreased seizure threshold.

Use in pregnancy and lactation

The safety of bupropion administration in pregnant women has not been established.


Bupropion may be administered during pregnancy to patients only when the expected benefits of its use outweigh the possible risks.


In a retrospective study (n = 7,005 infants), there was no increase in congenital malformations (2.3%) or cardiovascular malformations (1.1%) associated with maternal bupropion use in the first trimester of pregnancy (n = 1213 infants) compared with use of other antidepressants in the first trimester (n = 4743 infants - 2.3% and 1.1%, respectively); when using bupropion not in the first trimester (n = 1,049 infants; 2.2% and 1.0%, respectively).


Because bupropion and its metabolites penetrate into breast milk, it is recommended that breastfeeding be discontinued during bupropion therapy.


Use in patients with liver dysfunction

Caution should be exercised in patients with hepatic impairment

Use in patients with impaired renal function

Caution should be exercised when using in patients with impaired renal function

Administration in children

Contraindicated in children under 18 years of age

Use in elderly patients

Clinical studies have shown no differences in tolerability of bupropion in elderly patients and younger patients. However, the possibility of hypersensitivity in some elderly patients cannot be excluded; therefore, a reduction in the dose or frequency of administration may be required.

Indications for the drug Wellbutrin

  • treatment of depression. If adequate response is achieved, continuation of bupropion therapy to prevent exacerbations and relapses of depressive episodes.

Dosing regimen

Bupropion sustained-release tablets should be swallowed whole, without chewing, breaking, or crushing, as this may increase the risk of adverse reactions, including seizure disorders.


Treatment of depression


Clinical effects appear 14 days after initiation of therapy. As with all antidepressants, antidepressant effects may set in after several weeks of treatment.


The maximum single dose of slow-release bupropion should not exceed 450 mg. The interval between doses of bupropion should be at least 24 hours after the last dose. The dose should be increased by no more than 100 mg per day for three days.


Adults


Start of treatment


The initial dose of bupropion is 150 mg once daily, in the morning.


If adequate therapeutic response is not achieved, it is recommended that the dose be increased to the usual adult target dose of 300 mg/day once daily.


Increase the dose above 300 mg/day


Increasing the dose to a maximum daily dose of 450 mg once daily is possible for patients who do not show clinical improvement after several weeks of therapy at a dose of 300 mg/day.


Maintenance therapy


Acute episodes of depression require continued treatment for 6 months or more after initial therapeutic response is achieved. The efficacy of bupropion (300 mg/day) has been proven with long-term therapy (up to 1 year).


Children and adolescents


The safety and efficacy of bupropion in patients under 18 years of age have not been established.


Treatment of depression in special patient groups


Elderly patients.


Elderly patients are more likely to develop a hypersensitivity reaction, so the dose or frequency of the drug should be reduced.


Patients with impaired renal function


Treatment of such patients should be started with a lower dose of the drug, since bupropion and its metabolites may accumulate to a greater extent than usual in such patients. The dose of bupropion in sustained-release tablets, for such patients, should not exceed 150 mg once daily.


Patients with impaired liver function


Because differences in pharmacokinetics are increased in patients with mild to moderate hepatic dysfunction, they may require longer intervals between doses of the drug.


The dose of bupropion in sustained release tablets in patients with severe cirrhosis should not exceed 150 mg once every 2 days.