Tobacco

Pharmacology
Karina DiLuzio, BS, CTTS, CWC and
Julee Moorlag, RCP, CTTS
2017
 Agenda

• Methodology behind medications used for

tobacco cessation
• Types of medications available, with
contraindications, side effects, dosing
information, and instructions for use
• Data behind why medications are used
• Different approaches with medications
• Alternatives to medications

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 Here’s the Big Secret to Quitting

Discovering how you live life as a non-tobacco

user – what do you do instead?

3
 Some ways to quit…

• Medications
• Quitting groups/classes or individual counseling
• Behaviors to take the physical place of tobacco (chewing gum, playing with a
rubber band, straws, toothpicks etc.)

• Learning methods of coping with stress

• Environmental changes (making your home smoke free, getting rid of all
tobacco related products, changing routines around using tobacco, etc.)

• Alternative methods (aromatherapy, hypnosis etc.)

• “Willpower”
Any combination is appropriate!

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 What’s the BEST way to quit?

EVERYONE QUITS DIFFERENTLY!!!

THERE IS NOT “ONE” RIGHT WAY!

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 There IS a BEST formula….

Medications
+
Counseling
+
Follow Up
=
Highest rates of quitting at 6-12 months

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 Let’s talk Cold Turkey!

• A typical day with cold turkey cravings can feel like

this: Cravings
10 10 10
9 9 9
8
Strength

3
2 2 2
1 1

8:00 9:00 10:00 11:00 12:00 1:00 2:00 3:00 4:00 5:00 6:00 7:00 8:00
AM AM AM AM PM PM PM PM PM PM PM PM PM
Axis Title

Cravings

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 Quitting “Cold Turkey”

•The ideal method from a

medical standpoint
•The least successful method to
quit (3-5% succeed every year )
•Need to help patient
determine whether it is realistic
with their specific needs
•Studies show that “weaning”
prior to “quitting” is also not
very successful.
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 A little humor! 

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 Why medications?

• Medications significantly raise the chances of

success by at least double.
– Study overview reported that use of NRT gum, patch,
nasal spray and inhaler, and Wellbutrin, caused a
success rate range of 1.7% – 4.4% higher than placebo
alone
• The success of medications on quitting are raised
even higher when combined with behavioral
counseling.

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 What are they for?

• The point of medications is to give patients a

vacation from cravings long enough to figure out
what to do instead of use tobacco.
• They might not make them no longer want to use
tobacco, but they should make it much easier to
get through the cravings.

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 They must use the vacation!
• 1st month – take a break from smoking and urges, and begin
thinking of alternative behaviors
• 2nd month –using these behaviors, “tweaking” as necessary
• 3rd month – behaviors become more routine and natural

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 Compare it to standing in the ocean…

• First cravings are usually “doable” – patients are

motivated, strong, supported.
• Over time, dealing with many cravings becomes
exhausting…increasing the chances that a
cigarette will look more and more like relief as
time goes by.
• NRT helps people weather the many smaller
cravings in order to focus on alternate behaviors
for triggers.

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 Medications

Seven first line meds:

• NRT
– Gum
– Lozenge
– Patch
– Nicotrol Inhaler
– Nicotine nasal spray
• Pills
– Wellbutrin or Zyban (Buproprion)
– Chantix (Varenicline)
USPHS Clinical Practice Guideline- 2008

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 NRT (Nicotine Replacement Therapy)

• Using purified, specifically dosed nicotine to

manage cravings.
• Allows tobacco user to avoid harmful chemicals
in tobacco while learning new coping and
replacement behaviors. (1 chemical vs 7000+)
• Because the method of delivery is different from
cigarettes with these methods, when used
correctly they rarely become a replacement
addiction.
N. Engl J Med. 1996 Dec 12;335(24):1792-8.

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 NRT Use

• Myth: Once the nicotine is out of the body,

cravings will cease quickly.
– Nicotine is out of the body in about 24-48 hrs.
however receptors can take weeks to months to go
into dormancy.
• Myth: “It takes X days to break a habit”
– When someone is breaking an addiction, not all the
factors will be “broken” in a few weeks or even a
month’s time – chemical, physical, emotional, social,
coping mechanism, etc.

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 Recommendations for NRT

• Match levels of nicotine patch to levels attained

through tobacco use.
• The use of combined NRT, typically a long acting-
patch and short acting NRT (gum, lozenge, inhaler
or nasal spray) are very helpful for most tobacco
users.
• Mono therapy is appropriate for light smokers
(<10 cigs/day), non daily smokers and in
pregnancy.

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 • Because of delivery system (thru cigarette),
arterial plasma levels of nicotine will be more
intense and in higher concentration levels than
thru NRT.
• Consider NRT a faded copy of the real thing.

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 Dosing

• 1 mg equals roughly 1 cigarette.

• 1 pack per day (ppd) = 20 cigarettes
• All the NRT options have their own bioavailability,
so amount given is not the amount actually
delivered/absorbed.
• Try to match level of medication delivered in a 24
hr period to the amount to which the patient’s
body is accustomed to over the last several
months, unless patient can state it’s been at that
lower level consistently for at least one month.
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 Bioavailability (BV)

• BV refers to the amount of medication

actually available to the body per dose
• Each NRT has a different BV, which
influences the amount of mg prescribed.
• Patch – 75-90%
• Lozenge – 75%
• Gum – 50%
• Inhaler – 20%
• Nasal Spray – 53%
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 NRT vs Cigs in nicotine

NRT Option: Equivalent to:

Inhaler cartridge 2 cigs

Patch 7 mg = 4-6 cigs (1/4 ppd)

14 mg = 10-12 cigs (1/2 ppd)
21 mg = 17-19 cigs (1 ppd)
Gum 2 mg = 1 cig
4 mg = 2 cigs
Lozenge 2 mg = 1.5 cigs
4 mg = 3 cigs
Nasal Spray 1 dose (two sprays, one in each
nostril) = ½ cig

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 How high can we go?

• Try to match levels as best you can, as long as

reported intake level is reliable. Many people
underreport their daily use for many reasons and
the cigarette (best drug delivery device ever!) and
smokeless tobacco produce much higher nicotine
levels and much more rapidly than NRT. If the
patient reports any signs of overdose, decrease
the amount.
• Research done by Mayo to evaluate NRT efficacy
for smokeless tobacco users went as high as 63mg
(in an inpt setting). Ebbert Jo, et al. Nicotine Tob Res. 2007.

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 So, what’s available?

• Clinically, some medications work better than

others with higher cessation rates.
• Work with the patient/client to determine what
appeals to them the most and which fit their
lifestyle and needs the best.

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 The Nicotine Patch
• The patch is used to supply a constant stream of
nicotine into the body for a 24 hour duration. It
provides the most steady blood nicotine levels.
• It takes 1-3 hours to become effective once
applied, and 4-6 hrs to reach peak
concentrations.
• Best used for:
– Those who use tobacco daily, especially moderate to
heavy users or if used during the night.
– Patients who are not conscious/lucid enough to
remember how to use other products correctly or
safely.

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 Patch Instructions
• Does not replace the tactile or oral stimulation provided by
tobacco.
• Can cause insomnia or nightmares in some patients. Placing
(and replacing) the patch in the morning (or furthest away
from sleep) can greatly aid in this. Another consideration is
that many “quitters” have these symptoms so it’s hard to
determine if it’s actually from the patch.
• Takes care of the bulk of cravings. May need additional
help with “breakthrough” cravings.
• Replacing the patch at the same time every day helps
greatly with maintaining the most even levels of nicotine in
the body and therefore aids in craving management.
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 Patch Instructions

• Patches can fall off a person’s skin. If this happens,

wiping the area with rubbing alcohol first can help
the patch adhere much better. Medical tape is also
helpful.
• Try and replace patches after a shower, and not
immediately before.
• The patches must be placed at a different location on
the skin every day. Each location must be given at
least two weeks “rest” before it is used again.
• Must be used every day for best effect.
• Do not cut in half!

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 Patch Side effects/Contraindications

• Do not use with those who have delicate or fragile

skin.
• Must not be placed on wounds, rashes, etc. and avoid
tattoos.
• Try not to place on hairy areas without shaving area
first.
• The adhesive can cause an allergic reaction in the
form of irritable, itchy rashes, bumps, and/or swelling
to appear on the skin. If mild, try hydrocortisone
cream. If severe, stop use immediately and speak to a
physician if necessary. Adhesives vary from brand to
brand.
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 Nicotine Gum
• Comes in 2mg (~1 cigarette) and 4mg (~2 cigarette) doses
• Less than 1 ppd users typically find 4 mg doses too “strong”
• Doses can be broken in half if necessary
• Many different flavors (cinnamon, mint, teeth whitening,
etc.)
• Can cause nausea or hiccups (if the 4 mg causes this side
effect, the 2 mg may be used instead)
• Takes 15-20 minutes to take effect
• If possible, do not eat or drink anything besides water for 15
minutes before and during use for best absorption.
• Package will suggest a “first cigarette of the day” guideline.
We favor dosing by cigarettes per day.

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 Nicotine Gum Instructions

• “Chew and park” method

• Crack between teeth until a “tingly” or “peppery”
taste is noticeable.
• Tuck between gum and cheek till taste disappears.
• Chew again till taste comes back, and park again.
• Takes about 30 minutes of this process to obtain all
nicotine from the product.
• Chewing too fast can cause nicotine to be released
too quickly and cause side effects and diminished
craving control
• May use every 1-2 hours at first, slowly tapering
down.
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 The Lozenge
• Comes in 2 mg (~1.5 cigarette) and 4 mg (~3 cigarette) doses
• Less than 1 ppd users typically find the 4mg dosage too
“strong”
• Doses can be broken in half if necessary.
• Many different flavors
• Side effects: Can cause nausea or hiccups (if the 4 mg causes
these side effects, the 2 mg may be used instead)
• Package will suggest a “first cigarette of the day” guideline.
We favor dosing by cigarettes per day.

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 Nicotine Lozenge Instructions

• Suck until it is gone – do NOT chew it

• Takes 15-20 minutes to be effective, 30 to be at
peak levels
• If possible, do not eat or drink anything besides
water for 15 minutes before and during use for
best absorption.
• Great for those with dentures or poor dentition

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 Nicotine Gum/Lozenge
Contraindications
• Do not use with gum for those with dentures or
poor dentition.
• If a patient is NPO (nothing by mouth) there may
be times when these products can or can not be
used.
• Do not use either gum or lozenge with patients
who are experiencing nausea/vomiting, or have GI
upset.

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 Nicotrol Inhaler - (not the “E cigarette!”)
• White, plastic tube with tapered end. Cartridge of
nicotine inserted at other end. Pt puffs – NOT
INHALES - on the inhaler to receive nicotine.
• No lighting necessary; there is no smoke or
“vapor” associated with this product
• Legal to use anywhere tobacco is prohibited.
• Provides oral and hand behavior associated with
smoking.
• Up to 16 cartridges per day
• Prescription only

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 Inhaler Instructions
• DO NOT inhale past the throat – puff like a cigar (into
the cheeks), and not a cigarette (into the lungs)
• About 80 puffs and 20 minutes of active puffing in
each cartridge.
• Taste will be “bold, strong” at first, will fade with each
puff. No taste left means the cartridge is empty.
• Instruct patients to puff until the craving is
manageable, most people find this happens in 10-15
minutes.
• Once the cartridge has been pierced, in 2-3 hours it
does not seem to be effective any longer.
• Prep your patient/client to know that this is meant to
be similar to smoking, but not duplicate it exactly.

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 Inhaler Contraindications

– Can cause coughing and throat irritation, especially

when inhaled rather than puffed.

– Not considered best option for smokeless tobacco

users, as is designed to take the place of smoking.

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 Nasal Spray
• One dose equals one spray in each nostril.
Approx equal to ½ a cigarette.
• Becomes effective in 5-10 minutes. (fastest
absorption of all NRT’s)
• Not widely used.
• Can cause burning sensation in nasal cavity. If
people continue to use it, it becomes better
tolerated after using for several days.
• Prescription only

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 Overdosing on NRT
• Symptoms of overdose on nicotine include:
– Nausea (most common)
– Dizziness
– General malaise, anxious or jittery
– Headache
– Rapid heartbeat
• Nicotine overdose can cause death, however very infrequently.
• Remedy is to discontinue use of the NRT immediately, and
reduce dosage if continued after side effects are gone.
• If symptoms are distressing or life threatening, call physician or
911 immediately.
• Children and pets are especially at risk of overdose
• Nicotine overdose occurs infrequently, even at higher doses. The
symptoms usually occur within 1-2 hours of patch application.

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 Long Term Use

• Most patients want to stop NRT too soon.

• Long term use of NRT (6 months and more) is not
to be discouraged as long as it is maintaining or
decreasing in amount; much better option than
tobacco when relapse prevention is crucial.
• Most people wean themselves off. Encourage
patients to have a small “back up” stash of
nicotine gum, lozenge, spray or inhaler to prevent
relapse during stressful events. Unless relapse is
sustained, patches should not be used because of
receptor activity.
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 When do we not use NRT?

• Co-morbidities such as:

– Buerger’s Disease (allergy to smoking),
– Sometimes spine/ortho surgeries –some surgeons
believe that nicotine use delays wound healing
(quitforsurgery.com)
– Transplant patients who are on the waiting list
• Generally, patients need to be free of nicotine for at least six
months before they are allowed on the waiting list. The
guidelines for this do vary at different Transplant centers.
– Patient’s wishes

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 Chantix (Varenicline)
• Chantix works by “plugging up” the nicotine receptors.
Nicotine can no longer cause chemical release. (antagonist)
• Chantix also causes the nicotine receptors to release a
constant low level of dopamine, epinephrine, etc. This aids in
craving management. (agonist)
• Many feel “ill” or “it makes cigarettes taste disgusting!” when
they smoke while on Chantix. Advise patients/clients not to
count on this as a deterrent, as it doesn’t happen with
everyone.
• Chantix has highest success rates, however using more than
one NRT has shown to be as effective.

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 Chantix Dosage

• Days 1-3 take 0.5 mg pill once daily

• Days 4-7 take 0.5 mg pill twice daily
• On day 8 take 1.0 mg pill twice daily for minimum
of twelve weeks.

(pills can be cut in 2 if restarting without the starter

pack)

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 Alternative Chantix Options

• Some off label use of Chantix – either increasing

dose past standard dosing slowly until efficacy
reached or adding NRT to use alongside
• A half dose of Chantix has been shown to be
nearly as effective as a full dose
• If a patient is able to completely cease tobacco
use on Day 8 and beyond, they will not need to
continue dosage past 3 months. If they slip
towards the end of the 90 days, an additional 3
months of Chantix is recommended.
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 Chantix Side Effects
• 30% have nausea (for first 2 wks is most common)
• Can be managed better when taken with a
meal and full glass of water (or a banana?!)
• Titrating more slowly or maintaining a lower
dose can help control the nausea
• 15% “Vivid dreams” – very “real”. Most of the
dreams are very neutral. However, some report
great dreams, and others have nightmares.
– Taking the pill with their evening meal instead of
at bedtime can cause dreams to be more
tolerable.

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 Chantix Side Effects
•Behavioral change (not found in studies; this side effect
found from patient reports)
•Black Box Warning for mental health diagnoses has been
removed (EAGLE study)

•Instruct patients/clients what to look for:

•irritability, stressed communication with others,
moody, etc can easily be from tobacco cessation
•Other feelings, such as “maybe it would be better if I
weren’t here anymore” are much more concerning.

•Either way, if feelings are distressing, contact your doctor

and stop taking Chantix immediately.

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 Chantix Contraindications

• Chantix is processed via the kidneys. Pts with

renal impairment may take Chantix but with
different dosing levels.
– Guidelines available on Pfizer website under Provider
information.
– If creatinine level is >2, do not use Chantix

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 Dosing for people not ready to quit

• For people wanting to quit in about a month:

– Start taking Chantix. Quit tobacco by day 35. The
later they quit, the more likely they will need an
additional 3 months of Chantix.
• For people wanting to quit within three months:
– Start taking Chantix. Reduce tobacco use by half by
end of 1st month. Reduce tobacco use by half again
by end of 2nd month. Quit completely by end of 3rd
month. Continue taking Chantix for an additional
three months.

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 Wellbutrin, Zyban (bupropion)

• Antidepressant which also reduces cravings to use

tobacco
• Not sure precisely how it works to reduce cravings
but does work on nicotinic receptors
• Dosing:
– 150 mg pill once daily for three days
– 150 mg pill twice daily after for twelve weeks
minimum
• Typically takes 2-4 weeks to produce benefit.
• Often helpful in reducing weight gain from
cessation
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 Wellbutrin “Window”

• Anecdotal evidence shows that once patients

begin having reduced cravings, they must stop
smoking immediately.
• If they do not, the craving reduction benefit will
disappear even if they continue taking the
medication

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 Bupropion Side Effects

• Slight risk of seizure

• Insomnia
• Headache
• Dry mouth
• Anxiety/Agitation
• If seizure happens, bupropion to be discontinued
immediately and a physician seen.
• If other side effects are not tolerable, contact
physician.
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 Buproprion Contraindications

• History of seizure
• History of alcoholism, not currently in remission or at
high risk of relapse.
• Alcohol use must be extremely minimal if at all when
using bupropion
• History of head trauma which caused loss of
consciousness
• History of eating disorder
• Shouldn’t be used alongside other SSRI’s, or with
medications that lower seizure threshold. Do not use
with MAO inhibitors.

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 Additional Side Effects

• Feeling “weird”, or “not themselves”

• Fainting
• Feeling “weird, off, odd, really really loopy”. This
happens rarely, but when it does, it seems to
affect the patient dramatically (anecdotal
evidence only).

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 Combining Medications

• Known as “Combination Therapy”, this provides a tailored approach to

patient’s situation.

• Mix and match any of the meds, but most common is to use a long acting
med (patch, Chantix or Zyban) with a short acting med (gum, lozenge,
inhaler or nasal spray).

• NRT and Bupropion can be combined.

• NRT and Chantix can be combined, but typically the NRT can be weaned
off after 3-4 weeks as the receptors should be fully saturated by then.
There are some situations where continuing NRT longer is acceptable.

• Chantix and Wellbutrin can be combined together too, but not meant as
a first line therapy and data suggests it is not more effective than using
one, except in very heavy tobacco users.

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 Examples – what are the best options?

• 1 ½ ppd smoker who wants to use patch and

nicotine gum
– A) 21 mg patch plus up to 10 pieces (2mg) gum per
day
– B) 14mg patch plus up to 10 pieces (4mg) gum per day
– C) 21mg patch plus up to 5 pieces (4mg) gum per day

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 • Patient who smokes 6 cigarettes a day and has
dentures
– A) 7 mg patch
– B) up to 6 pieces (2mg) gum per day
– C) nothing
– D) up to 3 pieces (4mg) gum per day

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 • 3 ppd smoker
– A) Chantix or bupropion
– B) 3 (21mg) patches
– C) 2 (21mg) patches plus up to 10 nicotrol inhaler
cartridges/day

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 • ½ ppd smoker who wants to use the inhaler
– A) Up to 2 inhaler cartridges/day
– B) Up to 10 inhaler cartridges/day
– C) Up to 5 inhaler cartridges/day

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 Let’s take the pressure off

• Standard dosing is 3 months minimum.

Too many patients take themselves off
the meds after only a few weeks, and
relapse later. Why?
– Elevated expectations that they “should
beat this” very quickly
– “I want to do it on my own”
– Dislike of taking medications in general

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 A Cause of Relapse

• Misunderstanding that it’s not just the nicotine

most smokers are addicted to; it’s also the
mechanical behavior, the routine, the “go to”
stress reliever, boredom reliever, etc.

• And by the way, it’s not the nicotine killing

people….it’s what is in the tobacco! Nicotine is
the means of getting someone addicted!

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 Cont’d

– They feel “okay” and feel “cured”, and stop taking

medication before they’ve had a chance to develop
alternative behaviors.
• Then events in life happen and they are
unprepared and relapse easily

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 Let’s give them some time

• Reassure the patient that this doesn’t have to be

beaten immediately. If necessary, take their time
and ease into it. It’s okay to use the meds…give
themselves some wiggle room!
• That’s what the meds are there for!!

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discussion
thank you!

email.address@allina.com