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bupropion
GENERIC NAME: bupropion
BRAND NAME:
Wellbutrin, Wellbutrin SR, Wellbutrin XL,
Zyban
DRUG CLASS AND MECHANISM:
Bupropion is an antidepressant medication that
affects chemicals within the brain that nerves use to
send messages to each other. These chemical messengers
are called neurotransmitters. The neurotransmitters that
are released by nerves are taken up again by the nerves
that release them for reuse. (This is referred to as
reuptake.) Many experts believe that depression is
caused by an imbalance among the amounts of
neurotransmitters that are released. Bupropion is
unrelated to other antidepressants. It works by
inhibiting the reuptake of dopamine, serotonin, and
norepinephrine, an action which results in more
dopamine, serotonin, and norepinephrine to transmit
messages to other nerves. Bupropion is unique in that
its major effect is on dopamine, an effect which is not
shared by the selective serotonin reuptake inhibitors or
SSRIs (e.g. paroxetine, Paxil; fluoxetine, Prozac;
sertraline, Zoloft) or the tricyclic antidepressants or
TCAs (e.g. amitriptyline, Elavil; imipramine, Tofranil;
desipramine,
Norpramin).
PRESCRIPTION:
Yes
GENERIC AVAILABLE:
Yes
PREPARATIONS: Wellbutrin, round
tablets: 75 mg (orange), 100mg (red). Zyban, round
tablets: 100 mg (blue), 150 mg (purple). Wellbutrin SR,
round tablets: 100 mg (blue), 150 mg (purple).
Wellbutrin XL, tablets: 150 and 300
mg.
STORAGE: Tablets should be kept at
room temperature, 15- 25°C
(59-77°F).
PRESCRIBED FOR: Wellbutrin,
Wellbutrin SR, and Wellbutrin XL are used for the
management of major depression and seasonal affective
disorder (depression that occurs primarily during the
fall and winter). Zyban has been approved as an aid to
patients who want to quit
smoking.
DOSING: Bupropion usually is given
in two or three daily doses. When used for smoking
cessation, bupropion usually is started as 150 mg once
daily for three days, and then the dose is increased if
the patient tolerates the starting dose. Smoking is
discontinued two weeks after starting bupropion therapy.
Wellbutrin SR is given as two daily doses. Wellbutrin XL
is given as one dose
daily.
DRUG INTERACTIONS: Although no
systematic studies have been done to assess the
potential of bupropion to interact with other drugs,
bupropion should be used cautiously in patients
receiving drugs that reduce the threshold for seizures.
Such drugs include prochlorperazine (Compazine),
chlorpromazine (Thorazine), and other antipsychotic
medications of the phenothiazine class. Additionally,
persons who are withdrawing from benzodiazepines (e.g.
diazepam, Valium; alprazolam, Xanax) are at increased
risk for seizures.
PREGNANCY: Although there are no
adequate studies of bupropion in pregnant women, studies
in pregnant animals using doses much higher than those
used in humans, have demonstrated that bupropion is
safe. Bupropion, therefore, can be used in pregnancy if
the physician feels that it is
necessary.
NURSING MOTHERS: It is not known
if bupropion is secreted in breast
milk.
SIDE EFFECTS: The most commonly
noted side effects associated with bupropion are
agitation, dry mouth, insomnia, headache, nausea,
constipation, and tremor. In some people, the agitation
or insomnia is most marked shortly after starting
therapy. Some patients may experience weight loss.
Uncommonly, patients may experience manic episodes or
hallucinations. Four of every 1000 persons who receive
bupropion in doses less than 450 mg/day experience
seizures. When doses exceed 450 mg/day, the risk
increases ten-fold. Other risk factors for seizures
include past injury to the head and medications which
can lower the threshold for seizures. (See drug
interactions.)
"If
antidepressants are discontinued abruptly, symptoms may
occur such as dizziness, headache, nausea, changes in
mood, or changes in the sense of smell, taste, etc.
(Such symptoms even may occur when even a few doses of
antidepressant are missed.) Therefore, it is recommended
that the dose of antidepressant be reduced gradually
when therapy is discontinued."
It
has been suggested that bupropion and SSRIs may cause
depression to worsen and even lead to suicide in a small
number of patients. These potential side effects are
difficult to evaluate in depressed patients because
depression can progress with or without treatment, and
suicide is itself a consequence of depression. Moreover,
the evidence supporting these potential side effects is
weak. Therefore, no conclusions can yet be drawn about
the relationship between bupropion and SSRIs and
worsening depression and suicide. Until better
information is available, patients receiving bupropion
or SSRIs should be monitored for worsening depression
and suicidal
tendencies. |