Anti-Smoking Medication: Why It Should Be Avoided.

Bupropion

Buproprion, also known as Zyban and Wellbutrin, is a nicotine-free treatment licensed for smoking cessation. It is claimed that Bupropion helps to reduce nicotine withdrawal and the urge to smoke. Bupropion can be used safely with NRT, the company literature states.

An issue to be aware of, if you are contemplating using Zyban, is the possibility of side effects. The most common side effects are a dry mouth, insomnia, a change in appetite, agitation and headaches. The most common side effects which cause people to discontinue use of bupropion are shakiness and skin rash. Also, bupropion can cause seizures. If you have epilepsy or an existing seizure disorder, you definitely should NOT take this drug. It is also important to carefully follow your doctor’s recommendations about dosage, due to the risk of seizures.

Guidance to Doctors on Zyban
Soon after the introduction of Zyban as a prescription drug, newspapers began reporting deaths in patients prescribed with Zyban. The Guardian reported on 26 April 2001 that the anti-smoking drug was suspected of causing adverse reactions in 35 people who had died in the UK since it was introduced in June 2000. This acknowledgement came at the inquest of Kerry Weston, 21, a British Airways air hostess who was found dead in a hotel room in Nairobi, Kenya, two weeks after she began taking the drug to help her quit her 15-a-day habit.

Following these reports, on 31 May 2001 the Committee on Safety of Medicines (CSM) announced a change to the prescribing regime, and strengthened warnings for doctors prescribing Zyban. The CSM reviewed current evidence and advised a delay in increasing the dosage during the period of treatment, and a strengthening of the warnings given to prescribers that Zyban should only be used for patients at risk for seizures if there were compelling clinical reasons.

Professor Breckenridge, Chair of the CSM said:
”The Committee on Safety of Medicines and the Medicines Control Agency in conjunction with other European Regulatory Authorities … will be keeping the safety of Zyban under close, constant scrutiny.”

Suicide Risk
Two investigators in Finland, Drs. Pirkko Kriikku and Ilkka Ojanperä investigated the relationship between bupropion and suicide in post-mortem investigations (Forensic Science International, 23 June 2016). They reviewed 33,727 post-mortem investigations in Finland over five years (2009-2013) and identified cases in which bupropion was detected. Cases positive for other antidepressant drugs were reviewed for comparison.

The post-mortem examinations included, in all cases, the routine screening and quantification of hundreds of drugs and poisons. Bupropion was detected in 65 cases. While this is only .2% of all deaths, a large proportion of the bupropion-positive deaths resulted from suicide (55%). In fatal poisoning cases found positive for bupropion, the proportion of suicide was even higher (77%).

The research ‘highlights’ were:
• Suicide was the most common manner of death among users of bupropion.
• Suicide was significantly more common among users of bupropion than among users of other antidepressant drugs.
• Individuals positive for bupropion died younger than users of other antidepressants.

There are no known suicides following the use of CBT to stop smoking, definitely a safer option than bupropion.

Varenicline
Also known under the trade names of Chantix or Champix, varenicline is a medicine licensed in the US and UK in 2006. It is claimed that varenicline mimics the effect of nicotine on the body. Varenicline is a nicotinic receptor partial agonist—it stimulates nicotine receptors more weakly than nicotine. Therefore, it can reduce the urge to smoke and relieve withdrawal symptoms. The normal dosage is 1 mg twice daily for 12 weeks. Varenicline has not been tested in those under 18 year’s old or pregnant women and therefore is not recommended for use by these groups.

In 2009 the FDA announced a Black Boxed Warning on the prescribing information for Chantix (varenicline) and Zyban (bupropion). The warning highlighted the risk of serious mental health events including changes in behaviour, depressed mood, hostility, and suicidal thoughts when taking these drugs.
“The risk of serious adverse events while taking these products must be weighed against the significant health benefits of quitting smoking,” said Janet Woodcock, M.D., director, the FDA’s Center for Drug Evaluation and Research. “Smoking is the leading cause of preventable disease, disability, and death in the United States and we know these products are effective aids in helping people quit.”

The FDA also issued a warning that Chantix “may be associated with a small, increased risk of certain cardiovascular adverse events in patients who have cardiovascular disease”.

Side effects of the drug include nausea in approximately 30% of people taking varenicline, headaches, insomnia, and nightmares. More rarely occurring side effects include change in taste, vomiting, abdominal pain, flatulence, and constipation.

Aljazeera America reported that over five years, 544 suicides and 1,869 attempted suicides had been reported to the FDA as “adverse events” in connection with Chantix, according to documents obtained under the Freedom of Information Act. The FDA asked Pfizer to investigate reports of violence by Chantix users and report back by 2017.

You need to ask yourself whether the chance to stop smoking using a medicine like Chantix or Champix is worth the risk. A vitally interesting scientific report was published in 2016. This was the largest clinical trial on anti-smoking medication ever conducted.

FDA/Big Pharma Clinical Trial

Many deaths have been reported in the media and elsewhere following smokers’ usage of bupropion and varenicline. However, it is difficult to absolutely prove these deaths were caused by the drugs. It is true that the suicide data from Finland are quite convincing. Sixty-five buproprion-linked suicides in Finland and 2,700 lawsuits in America are difficult to ignore. However, plainly there could be additional factors other than the drug itself that led to the deaths, e.g. drug abuse, alcohol abuse, depression, family issues, unemployment and stress.

To establish cause-and-effect it is necessary to carry out a controlled trial. On the theory that there’s no smoke without fire, the FDA requested a trial to investigate the association between the anti-smoking medications and psychiatric disorders. The study was reported in The Lancet in 2016 by Robert Anthenelli and colleagues. The investigators included several known advocates of anti-smoking medications working in collaboration with company scientists from Pfizer and GlaxoSmithKline, the funders of the study.

Incredible though it might seem, the investigators administered the drugs to 8,144 people, half of whom had a history of psychiatric problems. The study sample included 3549 (44%) men, had an average age of 46·5 years, and 6584 (82%) participants were of white race/ethnicity. The aim was to measure the incidence of moderate and severe adverse events. It is important to note that:

“Participants had to be considered clinically stable for inclusion (i.e., no exacerbations of their condition in the preceding 6 months; on stable treatment for at least 3 months, with no treatment change anticipated during the study), and considered by the investigator not to be at high risk of self-injury or suicidal behaviour.” The 8000+ participants were given either varenicline (1 mg twice daily) or bupropion (150 mg twice daily) or a nicotine patch (21 mg per day) or a placebo for 12 weeks with a 12-week non-treatment follow-up. What did they find?

First the good news: nobody died! Daily visits and close supervision from the researchers made that an impossibility. All three of the anti-smoking medications produced reductions in smoking. Varenicline produced the strongest effect, doubling the abstinence rates for buproprion and NRT patch.

Now the bad news. Considering only the non-psychiatric sample, all three of the medications led to significant increases in psychiatric symptoms. Approximately one in three of the buproprion group showed signs of psychiatric disorder – a statistically higher number than in the placebo group. This result was only possible by chance with a probability of one in ten thousand. The varenicline group and the nicotine patch group also showed significantly higher rates of psychiatric disorders. Of particular significance was the increased incidence of abnormal dreams and insomnia. In addition, a quarter of the varenicline group experienced nausea.

It is impossible to know what aspects of the results of this highly controlled trial would be repeated in the real world. We do know that real world studies never produce the same high abstinence rates obtained in clinical trials. We also do not know the full impact of buproprion and varenicline when combined with recreational use of alcohol and illicit drugs, something that can easily happen is the everyday, real world. However, there are plenty of scary reports in the media. The FDA issued a Drug Safety Communication in 2011 to include potential alcohol interaction, risk of seizures, and studies of side effects on mood, behaviour or thinking.

This was a very good idea, as the results of the large trial had found evidence that the drugs were pushing their own drug trial subjects closer to a psychiatric illness.

In 2015 the FDA announced that a Moderate-level Drug Interaction exists between varenicline and alcohol in which some patients treated with varenicline have experienced decreased tolerance to alcohol, including increased drunkenness, unusual or aggressive behaviour, or they had no memory of things that happened. Varenicline users have been advised to limit their consumption of alcohol until they know whether varenicline affects their tolerance for alcohol. Also they are advised to use caution driving or operating machinery until they know how quitting smoking and/or varenicline may affect them.

If a varenicline user develops nervousness, agitation, hostility, aggressive behaviour, depression, thoughts of suicide, or have other changes in behaviour or thinking that are not typical, the FDA warns that they must immediately stop taking varenicline and contact their doctor.

The only safe way to stop smoking is to eliminate nicotine from your body. Smokers who switch to e-cigarettes must remain addicted to nicotine. There is no convincing evidence that E-cigarettes do actually help smokers to quit. The evidence suggests that medication is unsafe. You can ask yourself whether you wish to rely on a drug that has a high chance of giving you nausea, sleepless nights, bad dreams and maybe worse. My recommendation is to steer clear of anti-smoking medications. A far better solution is to stop smoking with CBT and Mindfulness. CBT and meditation are both more effective and safer than medication.

The only effective way of returning the body-mind to a natural state of homeostasis is to eliminate all forms of nicotine and other foreign agents from the bloodstream.