Low Doses of Nicotine causese what?
INCREASED
Alertness
Cognitive Function
Cholinergic agonist = ^^ BP / HR / O2 Consumption
stimulate respiratory system
relax skeletal muscle
HIGH doses of Nicotine does what?
Stimulates “REWARD” Center in limbic system
Nicotine -> Brain -> Nicotine receptors stimulated
Ventral Tegmental Area –> Nucleus Accumbens
–> Prefrontal Cortex –> DOPAMINE RELEASE
Physical WITHDRAWAL effects
Sweating / Cold-like Symptoms
Tingling in extremeties
Nausea + Headache
Emotional Withdrawal effects of Nicotine
Anxiety / Irritability
Insomnia / Depression
Confusion / Difficulty concentrating
Non-Pharmacologic Treatment for
Smoking Cessation
Education
Trigger Planning
Motivational Interviewing
THE 5 A’s
Ask / Advise / Assess / Assist / Arrange
Pharmacologic treament for
Smoking Cessation
OTC Nicotine Replacement Therapy = NRT
Path / Gum / Lozenge
RX Medications
Buproprion SR = Zyban
Varenicline Tartrate = Chantix
Nicotine Inhaler
Nicotine Nasal Spray
Exceptions to Smoking Cessation Therapy
Pregnant / Adolescent
Light Smoker / smokeless tobacco users
Combo of meds + counseling is more effective than just 1
Rationale of NRT Therapy
Reduces PHYSICAL withdrawal from nicotine
Patient not exposed to carcinogens / toxic component of cigs
Use of NRT INCREASES QUIT RATES by ~2 Fold
Nicotine Patch Facts
Nicoderm CQ
Delivery to systemic circulation, avoids hepatic FIRST PASS metabolism
ONLY LONG ACTING NRT product
QD dosing
Nicotine Patch DOSING
_> 10 cigs per day** = **Step 1_
(_21mg for 4-6 weeks)_
- *Step 2:**
- *14mg for 6 weeks (2 weeks)**
Step 3:
7mg for 2 weeks
Nicotine Patch Administration
Apply to clean / dry / hairless area of skin
on upper chest / upper arm / hip
Leave on for 16-24 hours
ROTATE admin site
if falls off or loosens, REPLACE w/ new patch
Can be left on while SHOWERING / BATHING
Do not cut patch
Nicotine Patch
Side Effects / Education
Most common = Skin irritation / Redness ~50%
AVOID use in those with dermatologic conditions
psoriasis / eczema / atopic dermatitis
Vivid Dreams / Sleep disturbance
- *Headache / Nausea**
- nausea might be from TOO HIGH DOSE*
Nicotine GUM + LOZENGE
Facts
SHORT ACTING NRT products
4mg or 2mg for both
Lozenge delivers ~25% MORE nicotine vs equivilant gum dose
Various Flavors
Absorption is pH dependent
has buffering agents
Nicotine GUM / LOZENGE
DOSING
4mg if 1st cig smoked within <30 min after waking
2mg if not
Chew *at LEAST >*9 pieces/day for first 6 weeks
DO NOT EXCEED 24 GUM PIECES PER DAY
DO NOT EXCEED 20 LOZENGES PER DAY
or 5 Lozenges in a 6 hour period
Nicotine GUM / LOZENGE
DOSING SCHEDULE
- *Weeks 1-6**
- *1 piece Q1-2h**
- *Weeks 7-9**
- *1 piece Q2-4h**
- Weeks 10-12*
- *1 piece** Q4-8h
DO NOT EXCEED _24 PIECES_ PER DAY
DO NOT EXCEED _20 LOZENGES_ PER DAY
or _5 Lozenges in a 6 hour period_
MAX DOSING
for Nicotine GUM
DO NOT EXCEED
24 GUM PIECES
PER DAY
MAX DOSING for
Nicotine LOZENGES
DO NOT EXCEED
20 LOZENGES PER DAY
or
5 Lozenges in a 6 hour period
Chew and Park Method
for Nicotine Gum Admin
Chew slowly until you notice a PEPPER TASTE OR TINGLE
“PARK” gum into the side of mouth
When taste or tingle FADES,
chew again -> REPEAT
Repeat for 20-30 minutes
Avoid eating / drinking _15 minutes_ before/during chewing gum
Nicotine LOZENGE
Administration
1 lozenge in bowht and allow to slowly dissolve (20-30min)
do not CHEW or SWALLOW
Once in a while use tongue to move lozenge from side to side
Do not use within _15 minutes_ of eating/drinking _ACIDIC_ foods or beverages
Side Effects of
NICOTINE GUM / LOZENGES
Hiccups / Flatulence
Nausea / Heartburn / Dyspepsia
Mouth Soreness / jaw ache from gum
Gum may stick to dental work
avoid in those with _dentures_
Advantages of Nicotine GUM / LOZENGE
Might satisfy ORAL cravings
- might* delay weight gain
- 4-mg*
Patients can titrate therapy to manage withdrawal symptoms
Nicotine INHALER
Counseling / Considerations
Menthol Flavor / Helps with hand+mouth satisfaction
caution with those w/ _reactive airway disease_
absorption is pH dependent
Cough / Rhinitis / Dyspepsia / Headache
Mild irritation of MOUTH or THROAT
relatively mild and frequency declines with use
Nicotine INHALER
Administration
- Place 1 cartridge into inhaler
- Push Top / bottom of mouthpiece back together
- Puff on inhaler in short breaths
- during inhilation nicotine is vaporized
- absorbed across OROPHARYNGEAL MUCOSA
- Nicotine is used up after about 20 minutes of puffing
- __do not use within _15 minutes_ of eating/drinking
Nicotine INHALER
DOSING
Start with >6 Cartridges/day
during the first 3-6 weeks of therapy
Increase prn to a MAX of 16 cartridges/ day
Recommended duration is 3 months
Patients STRUGGLE to use enough cartridges
Nicotine NASAL SPRAY
Counseling / Considerations
Nicotrol NS (10mg/ml)
Rapid Absorption = Quick onset
tilt head back to administer
High potential for abuse
avoid in those with _Allergic Rhinitis_
DO NOT Sniff / Swallow / Inhale
through nose as dose is being administered
Hot Peppery feeling in back of throat / nose
- *Sneezing / Coughing / Runny Nose / Watery Eyes**
- side effects limit its use*
Nicotine NASAL SPRAY
DOSING
Nicotrol NS (10mg/mL)
Use at LEAST > 8 doses/day
for the first 6-8 weeks for optimal results
1 dose = 0.5mg (1spray) in EACH nostril
May be beneficial to _taper over 4-6 weeks_
Nicotine NASAL SPRAY
Dosing Schedule / Max Doses
1-2 doses/hour
1 dose = 0.5mg (1 spray) in EACH nostril
MAX 5 doses/hour
MAX 40 doses/day
3 MONTHS OF THERAPY RECOMMENDE
Varenicline
MoA / Effects
Chantix
Binds with HIGH affinity & selectively
@ a2b2 neuronal nicotinic acetylcholine receptors
Stimulates low-level agonist activity
Competitively inhibits binding of nicotine
- Reduce symptoms of nicotine WITHDRAWAL*
- blocks dopaminergic stimulation* responsible for
- *reinforcement / reward** associated w/ smoking
Varenicline
DOSING
Patients should BEGIN THERAPY 1 week PRIOR to quit date
Increase dose GRADUALLY to minimize treatment-related
nausea / insomnia
Days 1 -3 : 0.5mg QD
Days 4-7: 0.5mg BID
Days 8 to end: 1mg BID
has RENAL dosing
Varenicline
RENAL DOSING
CrCl <30 ml/min:
0.5mg QD –> MAX 0.5mg BID
- *Hemodialysis Dosing:
0. 5mg QD**
Varenicline = Chantix
SIDE EFFECTS
Nausea / Headache / Dry Mouth
Insomnia + Abnormal Dreams
Constipation
Suicide / Aggresiveness / Mood Changes
Bupropion
MoA / Effects
- *ZYBAN**
- *Atypical antidepressant** thought to affect levels of:
- *Dopamine + Norepinephrine**
Beneficial for Patients concerned with WEIGHT GAIN
helpful in patients with underlying depression, may increase anxiety
Reduce Craving for Cigarettes
Reduce SYMPTOMS of nicotine WITHDRAWAL
Bupropion SR = Zyban
DOSING
150mg QD for 3 days
then, 150mg BID
Seperate doses by at least 8 hours
avoid taking second dose @ bedtime
May continue to smoke for first 1-2 weeks,
then select to quit by 2nd week
Bupropion = Zyban
SPECIAL DOSING
CONTAINDICATED WITH SEIZURES
Hepatic Impairment : 150mg Every OTHER Day
Elderly or Renal Impairment: 150mg QD
Side effects with BID dosing –> 150mg QD
Combination Pharmacotherapy
LONG-ACTING Formulation + Short Acting Formulation
LONG ACTING:
Bupropion SR / Nicotine Patch / Chantix
Produces relatively CONSTANT levels of nicotine
Short Acting:
NRT Gum + Lozenge / Nicotine Nasal Spray + Inhaler
Allows for ACUTE dose titration
S/Sx of nicotine OVERDOSE
N/V/D
Headache / Ab-pain+cramps
Cold Sweats / Breathing difficulties
AGITATION / RAPID HR
Ringing in the ears