Bupropion (Zyban)

Bupropion chlorhydrate (or Zyban) was initially used in the USA as an antidepressant. Although it proved relatively ineffective at treating depression, it was observed in 1992 that the treatment took away some patients’ desire to smoke. Since then, scientific studies have shown that this product can be effective in aiding smoking cessation, although successful and permanent cessation is also dependent on other factors. In addition, bupropion is a medicine which can cause side effects, so it can only be obtained on prescription and when accompanied by appropriate medical supervision.

How does it work?

Smokers develop a dependence on nicotine, a chemical product contained within tobacco. Nicotine acts on the nervous system, where it bonds with receptors and triggers the release of a chemical messenger, dopamine, which plays a role in the pleasure felt when smoking. The specific ways in which bupropion functions are not entirely clear, but we know that it acts via chemical messages. It is thought that bupropion reduces the displeasure of smoking cessation by inhibiting the recapture of neuromediators and compensating for the dopamine deficit linked to smoking cessation.

Generally speaking, antidepressants can sometimes be useful in promoting smoking cessation for three reasons (Hughes et al., 2007):

  1. Nicotine withdrawal can produce symptoms of depression or even, in the worst cases, major depression. Antidepressants prevent these risks.

  2. The “antidepressant” properties of nicotine are one of the factors that drive people to carry on smoking. Because smokers craving nicotine feel depressed when they are no longer smoking, they start smoking again to make themselves feel better. An antidepressant, however, can replace the effect of the nicotine.

  3. Antidepressants act on the nervous system and on certain receptors which have a proven link to nicotine addiction.

As the first two hypotheses have not been proven, it would seem that bupropion produces particular anti-smoking effects which are independent from its “antidepressant” effect.

Advantages

Bupropion helps people to quit smoking because it:

  1. Reduces the enjoyment of smoking
  2. Reduces withdrawal symptoms
  3. Limits weight gain

Side Effects

The most frequently observed side effect is insomnia, reported in 25% to 35% of cases. Patients have sometimes reported the following: dry mouth, agitation, anxiety, irritability, depression, shakes, headaches, dizziness, increased heart rate, back pain, abdominal pain, sickness, constipation, temporary rash, hives and very occasionally, epileptic fits (risk of 1 in 1000).

As with varenicline (Champix®) and Nicotine Replacement Therapy (NRT), many of the side effects can be attributed to smoking cessation itself.

There are some situations in which using bupropion (Zyban®) goes against medical advice, and this should be respected. For example, the use of this medicine by those who have a known sensitivity to the product, an eating disorder or alcohol dependency is strongly discouraged. In any case, your doctor is the only one who can prescribe you this medicine. Make sure you tell him or her about any other medicines you are taking so that your prescription can be adapted if necessary.

For a detailed list of all the medical contraindications and side effects, visit the Compendiumliens_externe_bleu-sur-blanc.

Pregnancy and Breastfeeding

As with many medicines, we have limited data on the effects of Zyban® on women during pregnancy. Although there is no known toxic effect or malformation of the foetus linked to bupropion, doctors prefer not to prescribe it to female patients during pregnancy because the potential risks are still unknown. If unsure, speak to your gynecologist to discuss the possible options. If you are planning to get pregnant, you should factor in one week after you stop taking Zyban® for its traces to be eliminated from your body. Given that the active ingredients of Zyban® are transmitted through breast milk, you are advised not to breastfeed while taking this medicine.

Summary

  • This medicine is for smokers who have a strong dependence on tobacco and who have made a decision to quit smoking. It requires medical monitoring and supervision as well as an accompanying quit plan.

  • In general, bupropion is particularly useful for smokers who cannot undergo NRT for medical reasons, who have experienced several failures with NRT, or who have a history of depression.

  • Your doctor will judge which drug is the most suited to your needs and expectations. Zyban® (bupropion) is only available on medical prescription.

  • Treatment begins 7 to 14 days before your quit date, giving the substance time to develop its effects.

  • In the first 6 days, one 150 mg tablet is to be taken each morning.

  • From the 7th day onwards, 2 tablets are to be taken daily, 1 first thing in the morning and 1 in the afternoon (at least 8 hours after the first).

  • The treatment lasts 7 to 9 weeks.

  • If you experience substantial or lasting side effects, do not stop taking the medicine without speaking to your doctor. The dose can be reduced to 1 tablet per day, which will considerably reduce the side effects while remaining nearly as effective for smoking cessation.

  • It is possible to combine Zyban® with NRT, but this has not been scientifically proven to increase its effects.

Summary of the dosage

The information below is only intended as a guide. Your doctor must be the one to prescribe you this medicine and give you advice on how to take it.

Day 1 -6 of the treatment

1 x 150 mg Zyban every morning

Day 7 until the end of the treatment (between 7 and 9 weeks)

2 x 150 mg Zyban
(1 in the a.m. and 1 in the p.m.,) at least 8 hours later

Your smoking quit date should fall between day 7 and day 15 of your treatment

 

Price

The cost of the treatment over 7 weeks of treatment (92 tablets) is equal to a daily consumption of around 26 cigarettes, depending on the price of the packet. This medicine can normally only be obtained on medical prescription and by those over 18. In many countries it is not covered by basic medical insurance, but it is sometimes covered by complementary insurance.

Effectiveness

A recent meta-analysis on the effect of antidepressants on tobacco withdrawal symptoms which covered 66 trials, including 49 using bupropion, showed that:

  • When used as the only treatment, ie. without being accompanied by any other medicine, bupropion increases the chances of long-term smoking cessation by more than 1.5 times (36 studies, N = 11,140, relative risk index [RR] 1.69; 95% confidence interval [CI] 1.53 to 1.85).

  • Bupropion is not proven to be more effective than NRT or varenicline.

  • There is not sufficient evidence to state that taking a combination of bupropion and NRT improves the chances of long-term smoking cessation.

The authors conclude that bupropion can aid smoking cessation and that its effectiveness may be comparable to that of NRT. Serious side effects necessitating a discontinuation of the treatment have thankfully rarely been reported.

We stress that this treatment can only be undertaken under medical supervision and that it represents just one part of the cessation process among other important social, behavioral and psychological measures.

References

Cochrane Review (meta-analysis) on the use of antidepressants for smoking cessation

Selected studies

 


Auteur: Grégoire Monney

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