Copyright © Françoise
Herrmann
Just three days till May 31 – The UN
World No Smoking Day! And just enough time for your physician to perhaps
decide on prescribing bupropion hydrochloride in sustained release (SR) form,
commercially marketed as Zyban® by GalxoSmithKline as an effective aid to
smoking cessation.
This pharmacotherapy for smoking cessation differs from nicotine and nicotine-replacement
therapies in that it is an active ingredient completely un-related to nicotine. It is the third
and most recent approach to smoking cessation. As a reminder the other combination
lines of treatment are behavioral and nicotine-replacement-type therapies, such
as transdermal patches, gum and lozenges.
The active ingredient bupropion hydrochloride was initially marketed in
the United States as an antidepressant under the brand name Wellbutrin®,
manufactured by GlaxoSmithKline. The structure of the active ingredient bupropion
hcl is similar to diethylpropion, an appetite suppressant. Clinical testing of
the drug demonstrated its effectiveness as a cessation drug as it doubles the
success rate of the cessation, and is as effective as nicotine replacement therapies
in conjunction with behavioral therapies (Roddy, 2004). It is unclear how
bupropion hlc actually supports cessation although the effects of the drug on
brain activity are known. It is hypothesized that inhibition of the reduction
of dopamine and noradrelanine levels occurring with nicotine withdrawal is
probably responsible. (Roddy, 2004).
Bupropion hlc is a highly patented compound. The search term “bupropion”
returned 453 hits at the EPO!
The discovery of the compound is patented in US3819706 titled Meta chloro substituted alpha-butyl-amino propiophenone,
as well as many of its various
formulations, for example US2011020446 titled Method and formulations for making pharmaceutical
compositions containing bupropion.
The various
properties of the compound (including smoking cessation) are
patented:
- as an anti-depressant, for example, US2009304786 titled Stable dosage forms of an antidepressant
- as appetite suppressant, for example, US2011144145 titled Methods of treating visceral fat conditions or US 2011098289 titled Method for treating obesity
- as treatment for sexual dysfunction, for example WO2012028834 titled Use of bupropion in the treatment of sexual dysfunction
- as an aid to smoking cessation: for example US2003064092 titled Pharmaceutical composition containing two active ingredients for smoking cessation or US2004225020 titled Methods and compositions for aiding smoking cessation and for treating pain and other disorders using optically pure (-)-bupropion
And the mode of delivery of the compound
(in SR- Sustained release form) and its manufacture are patented, for
example in US2010008987 titled Modified release pharmaceutical composition of
bupropion hydrochloride, considering all the severe side effects that occur
at peak plasma levels.
There are however warnings associated with the use of this therapy, as it
is linked to neuropsychiatric reactions, suicidal thoughts and behaviors, particularly
with younger populations. (GSK – Zyban)
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So, with just a couple days left before the big Q day, Carpe Diem!
Roddy, E. (2004) Buproprion and other non-nicotine pharmacotherapies. BMJ
Feb. 20, 2004, 328(7438):509-511.
GlaxoSmithKline – Zyban -
Highlights of prescribing information
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