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Wellbutrin XL, SR Medication
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Basic information
- Generic name: bupropion hydrochloride extended
release
- Brand/Trade names: Wellbutrin XL, Wellbutrin SR, Zyban
- Dosages:
75 mg, 100 mg immediate release tablets
150 mg, 300 mg extended release tablets
150 mg, 200 mg sustained release tablets
- Pharmacologic category: Aminoketone antidepressant,
Norepinephrine and Dopamine Reuptake Inhibitor
- FDA approved: August 29, 2003
- Manufacturer: GlaxoSmithKline
- Habit forming? No
- Pregnancy risk factor: C
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You can buy Bupropion SR without a Prescription
| Dosage |
Quantity |
Price |
Pharmacy |
Order |
| 150 mg |
30 tablets |
$19 |
4RX.com |
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| 150 mg |
60 tablets |
$36 |
4RX.com |
|
| 150 mg |
120 tablets |
$66 |
4RX.com |
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| 150 mg |
240 tablets |
$119 |
4RX.com |
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| 150 mg |
500 tablets |
$240 |
4RX.com |
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Medical uses
Wellbutrin XL (extended-release) is used to relieve mental depression.
This medication effectively treats depression with a low risk
of sexual side effects and a low risk of weight gain.
This antidepressant
is often prescribed for depression when selective serotonin
reuptake inhibitors (SSRIs) or tricyclic antidepressants (TCAs)
are not able to be used or are not effective.
Dosing: The starting dose is 150 mg per day, which your doctor
may increase to the usual adult dose of 300 mg per day. The maximum
dosage for this drug is 450 mg per day. Always make sure that
you take Wellbutrin XL as prescribed by your doctor. |
Wellbutrin + SSRI combination
Although not an approved indication, the combination of bupropion
and either an SSRI or an SNRI is generally well tolerated and
can boost antidepressant response. Augmenting antidepressants
with bupropion has become a common strategy in the treatment of
resistant depression. The results of clinical study have shown
that Wellbutrin SR added to the SSRI or venlafaxine (Effexor) in
patients failed to response to an SSRI or venlafaxine can increase
the number of responders [5].
The drug appears to significantly affect dopaminergic neurotransmission
and may help with fatigue and sexual dysfunction induced by SSRIs
of SNRIs (Effexor). A study by Papakostas and associates examined
the impact of bupropion vs SSRIs on sleepiness and fatigue in
patients with deprssion. The investigators pooled data from 6
double-blind, randomized clinical trials and found greater improvements
in fatigue scores among both bupropion-treated and SSRI-treated
groups than placebo-treated patients, and greater improvements
in fatigue scores among bupropion-treated than SSRI-treated patients
[6].
Wellbutrin may reverse SSRI-induced sexual dysfunction due to
its dopaminergic effect. In addition to the SSRI produces
produces an increase in desire to engage in sexual activity and
frequency of engaging in sexual activity [7]. |
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Pharmacological characteristics
- Metabolism: Extensively metabolized by hydroxylation
or oxidation in the liver. CYP2B6 is involved in formation of
hydroxybupropion (50% as potent as bupropion). The other 2 main
metabolites are threohydrobupropion and erythrohydrobupropion,
which are 20% as potent as bupropion.
- Elimination half-life: about 21 hr (bupropion), about
20 hr (hydroxybupropion), about 37 hr (threohydrobupropion),
and about 33 hr (erythrohydrobupropion).
- Excretion: 87% excreted in urine, 10% in feces, and
0.5% as unchanged drug;
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Benefits
- once a day dosage regimen
- low risk of sexual dysfunction [2]: does not lower libido, produce impotence or impair orgasms
- low risk of weight gain
- decreased appetite and weight loss (however, may be a harmful
effect for anorectic persons)
- low potential for triggering mania in the bipolar disorder
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Concerns
- frequently cause agitation, anxiety, and insomnia (treatment
with a sedative/hypnotic agent or discontinuation of therapy
may be required; gradual escalation of dose may minimize symptoms)
- risk of seizures
- risk of hypertension
- high potential for drug interactions
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Difference between Wellbutrin XL and Wellbutrin
SR
Wellbutrin XL contains the same active ingredient as Wellbutrin
SR (bupropion sr), but XL is formulated in an extended-release,
once-daily tablet. This means that with XL formulation, you can
take one tablet in the morning, continue with your daily activities,
and not worry about remembering to take a second dose. |
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Unlabeled uses
- attention-deficit/hyperactivity disorder (ADHD)
- depression associated with bipolar disorder
- neuropathic pain
- enhancement of weight loss
- augmenting a partial response to SSRIs
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Mechanism of action
The mechanism of bupropion's activity is not fully understood.
It is a relatively weak inhibitor of the neuronal uptake
of norepinephrine and dopamine, and does not inhibit monoamine
oxidase or the reuptake of serotonin. Metabolite inhibits the
reuptake of norepinephrine. The primary mechanism of action is
thought to be dopaminergic and/or noradrenergic. |
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Reviews, Discussion Boards &
Forums
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References
- 1. U.S. Food and Drug Administration. Wellbutrin XL
U.S. Prescribing Information. Available at (PDF format): Prescribing
Information
- 2. Coleman CC, King BR, Bolden-Watson C, Book MJ, Segraves
RT, Richard N, Ascher J, Batey S, Jamerson B, Metz A A placebo-controlled
comparison of the effects on sexual functioning of bupropion
sustained release and fluoxetine. Clin Ther. 2001 Jul;23(7):1040-58.
PubMed
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Interesting facts
- Bupropion was first synthesized by Burroughs Research in 1966,
and patented by Burroughs-Wellcome (later Glaxo-Wellcome) in 1974.
It was approved by the FDA in 1989 and marketed under the name Wellbutrin
as an antidepressant.
- Wellbutrin XL is the first and only once-daily norepinephrine
and dopamine reuptake inhibitor (NDRI) for the treatment of depression
in adults.
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