Bupropion is a dopamine and norepinephrine reuptake inhibitor.
It is about twice as potent an inhibitor of dopamine reuptake than
of norepinephrine reuptake. As bupropion is rapidly converted in
the body into several metabolites with differing activity, its action
cannot be understood without reference to its metabolism. The occupancy
of dopamine transporter (DAT) by bupropion and its metabolites in
the human brain as measured by positron emission tomography was
6–22% in an independent study and 12–35% according to GlaxoSmithKline
researchers. Based on analogy with serotonin reuptake inhibitors,
higher than 50% inhibition of DAT would be needed for the dopamine
reuptake mechanism to be a major mechanism of the drug's action.
Bupropion does not inhibit monoamine oxidase or serotonin reuptake.
However, it has been shown to indirectly enhance the firing of serotonergic
neurons, via activation of downstream norepinephrine flow. Bupropion
has also been shown to act as a noncompetitive nicotinic antagonist.The
degree of inhibition of receptors correlates well with the decrease
in self-administration of morphine and methamphetamine in rats,
and may be relevant to the effect of bupropion on nicotine addiction.
The drug is supplied as a racemic mixture, and no studies have been
published on the activities of the individual enantiomers.
Use Zyban as directed by your doctor. Check the label on the medicine
for exact dosing instructions.
Take Zyban by mouth with or without food.
Swallow Zyban whole. Do not break, crush, or chew before swallowing.
Several weeks may pass before your symptoms improve. Do not stop
taking Zyban without checking with your doctor.
Take your doses at the same times each day at least 8 hours apart
unless directed otherwise by your doctor. This may help to decrease
the risk of seizures with Zyban.
It takes about 1 week for Zyban to work. You should begin taking
while you are still smoking. However, you and your doctor should
decide on a date that you will stop smoking during the 2nd week
of taking Zyban.
If you have not made progress towards stopping smoking by the 12th
week, contact your doctor.
If you are not able to stop smoking while using Zyban, talk to your
doctor to determine why you were not successful. After the reasons
have been reduced or eliminated, you should try to stop smoking
again.
Continue to take Zyban even if you feel well. Do not miss any doses.
This medication is generally well tolerated. Dry mouth, headache, increased sweating, nausea/vomiting, constipation, anxiety, fatigue and blurred vision may occur. If these effects persist or worsen, notify your doctor. Report promptly: unusual weight loss or gain, palpitations, agitation, trouble sleeping. Unlikely but report promptly: tremor, dizziness, fainting, mood changes, slowed movements, difficulty urinating, decreased sex drive, drowsiness. Very unlikely but report promptly: seizures, mental problems, fever, muscle aches, yellowing of the eyes or skin. In the unlikely event you have an allergic reaction to this drug, seek medical attention immediately. Symptoms may include trouble breathing, rash, itching, swelling, or severe dizziness. If you notice other effects not listed above, contact your doctor or pharmacist.
Pregnancy Category C. In studies conducted in rats and rabbits, bupropion was administered orally at doses up to 450 and 150 mg/kg/day, respectively (approximately 14 and 10 times the maximum recommended human dose [MRHD], respectively, on a mg/m2 basis), during the period of organogenesis. No clear evidence of teratogenic activity was found in either species; however, in rabbits, slightly increased incidences of fetal malformations and skeletal variations were observed at the lowest dose tested (25 mg/kg/day, approximately 2 times the MRHD on a mg/m2 basis) and greater. Decreased fetal weights were seen at 50 mg/kg and greater.
Seek emergency medical attention if an overdose is suspected. Symptoms of a Zyban overdose include seizures, hallucinations, loss of consciousness, weakness, a fast heartbeat, and heart attack.