This document summarizes information about smoking cessation pharmacotherapy. It first discusses how tobacco use is harmful but nicotine is the only pharmacologically active substance. Nicotine acts on nicotinic acetylcholine receptors in the central and peripheral nervous systems. When smoking stops, withdrawal symptoms emerge due to nicotine absence. Nicotine replacement therapy (NRT) delivers nicotine at lower rates to relieve withdrawal symptoms without the same addiction potential as smoking. NRT includes nicotine gum, patches, and other formulations. Non-nicotine therapies like bupropion and varenicline are also discussed. The conclusion recommends a comprehensive pharmacological and behavioral approach for smoking cessation.

1. PPHHAARRMMAACCOOTTHHEERRAAPPYY OOFF SSMMOOKKIINNGG CCEESSSSAATTIIOONN
Sudesh Sharma*, Vikas Soni, Sushil K.Kashaw
DEPARTMENT OF PHARMACEUTICAL SCIENCES, DR. H.S.GOUR UNIVERSITY,SAGAR(M.P.)
●Tobacco use(smoking-Cigarettes/Bidis)
is surely one of the strangest of human
behaviours-
#Necessary neither for the maintenance of
life, nor for the satisfaction of social,cultural
or spiritual need.
#Distasteful???
#Harmful (High risk factor for various
diseases-due to its adherents)
▪Cancer (Particularly of lung and upper
respiratory tract, but also of oesophagus,
pancreas and bladder )
▪Coronary heart disease and other
forms of peripheral vascular disease.
▪Chronic bronchitis
●Nicotine is only pharmacologically active
substance in tobacco smoke, apart from
carcinogenic tars and Carbon mono
oxide(CO).[free nicotine suspended on
minute droplets of tar]
• Nicotine is an agonist at the
Nicotine Acetylcholine
Receptor expressed both in CNS and
Peripheral nervous system.All nACHRs are
pentameric structures that function as ligand-gated
ion channels,present both pre and/or
post synaptically.
·All nACHRs fall into 3 main classes-
MUSCLE TYPE GANGLION TYPE
CNS TYPE
Subunits (α1)2β1δε(Adul
t
(α 3)2(β4)3 (α 4)2(β2)3
and (α7)5
Main
Synaptic
location
Skeletal
neuromuscular
junction.
Autonomic
ganglia.
Many
brain
regions.
Pharmacological actions on CNS
·Pharmacological actions on CNS-
-In BRAIN
(B)AT SPINAL LEVEL
● Stimulates inhibitory Renshaw cells in ventral horn of
spinal cord, which inhibit spinal reflexs →skeletal muscle
relaxation.
Peripheral pharmacological actions
●Stimulates autonomic ganglia and peripheral sensory
receptors (mostly in heart and lungs)→various autonomic
reflex responses → # Tachycardia #Cardiac output ↑
# Arterial pressure ↑
●[Faster– Delivery/Rate of absorption/attainment of
max.concentration of nicotine,Greater- potential for
addiction.]
On stoppage of smoking,Withdrawal Symptoms (main
reasons behind relapses)emerge-including-
●Cravings for tobacco. ●Anxiety ●Nervousness.
●Headache. ●Irritability ●Insomnia
●Depressed mood. ●Tiredness. ●Incresed
appetite.
●Difficulty in concentrating or thinking clearly.
)
●Do not produce the same peak levels of
nicotine in the plasma as seen with
cigarettes/bidis and thus do not cause the
same subjective effects, however suppress the
symptoms of nicotine withdrawal.
DELIVERY
OF
NICOTINE
RATE OF
ABSORP.
Time to
max. Conc.
In plasma
Potential
for
addiction
1.Smoking FAST MORE LESS MORE
2.NRTfor
SLOWER LESS MORE LESS
mulation
(A) IN BRAIN
1 CHEWING
GUM
5.PHARMACOTHERAPY
Only NRT formulation available in India.
NICORETTE®(Johnson & Johnson LTD.)
For light smokers-Available over counter
in 2mg.strength(4& 10gums pack).
For heavy smokers-
Available on Physician’s prescription in
4mg.strength(10gums pack).
2 TRANSDER-MAL
PATCH.
Designed not to be applied for 16-24
hours and are available in diff.
strengths(Not in India.)
To be applied to the hip,trunk or upper
arm.
A different site of application should be
used each day,with several days gap
before the patch is applied to the same
area of skin.
A gradual withdrawal is recommended
by reducing the dose every 2-8 weeks.
1.
(B).NON NICOTINIC THERAPY-.
BUPROPION Weak inhibitor of dopamine and NA reuptake.
 i.e. increases dopamine in nucleus accumbens.
Antidepressant(first choice).
Side effect-Seizures at high doses.
2. NORTRIPTYLINE Antidepressant(Second choice).
3. CLONIDONE α-2 Adrenoceptor agonist.
Promote calming/anxiolysis.
4. VARENICLINE Partial α4β2 subtype nACh receptor agonist.
Elicits moderate and sustained release of
dopamine,countered during cessation
attempts,responsible for relapse.
CHAMPIX®(Pfizer).
5. MECALMYLAM-INE
Nicotine antagonist.
Reduces the reward effect of nicotine.
6. NICVAX Nicotine vaccine-(under clinical trials).
Stimulates the immune system to make
antibodies that bind to nicotine molecules
(Lozenges and Nasal spray are other NRT making them too big to cross BBB.
formulations.)
6.CONCLUSION 7.REFERENCES
1.”How Tobacco Smoke Cause Disease”-A Report of the Surgeon
General,U.S,Department of Health and Human Services.
2.Training Manual For Doctors,NTCP,MOHFW,Govt. Of India.
Smoking addiction is a complex process involving the interplay of pharmacology , conditioned factors,
personality etc.. Therefore, the ideal treatment for smoking-cessation involves a comprehensive approach that
addresses all major issues of smoking addiction ,both pharmacological & nonpharmacological. According to
WHO guidelines , all patients attempting to quit smoking should be encouraged to use pharmatherapeutic
agents, along with behavioural(5Rs Therapy- Relevance,Risks,Rewards,Roadblocks,Repetition).
4. SMOKING CESSATION
1.INTRODUCTION
3.NICOTINE:TOLERANCE&DEPENDANCE
2.NICOTINE:PHARMACOLOGICAL ACTIONS
(A)NICOTINE REPLACEMENT THERAPY (NRT) , ,