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Is nicotine an acid or a base?
weak base
how is nicotine absorbed in acidic media?
ionized --> poorly absorbed across membranes
how is nicotine absorbed in alkaline media?
nonionized --> well absorbed across membranes
what is the metabolite of nicotine?
cotinine
what is the half-life of nicotine vs cotinine?
• nicotine = 2 hr
• cotinine = 16 hr
how is nicotine excreted?
• Occurs through kidneys (pH dependent; increases with acidic pH)
• Through breast milk
Describe the metabolite of nicotine that is usually monitored to determine abstinence:
cotinine has a longer half-life... makes it a reliable marker for assessing recent nicotine exposure
Discuss the basic principles of nicotine addiction
- Tobacco users maintain a minimum serum nicotine concentration in order to: prevent withdrawal symptoms, maintain pleasure/arousal, + modulate mood
- highly addictive drug
- activates the dopamine reward pathway in the brain
- Tobacco Dependence is behavioral (habit) and physiological (addictive)
Describe how certain beverages (and foods) can affect the absorption of nicotine from the oral mucosa and the counseling that should be provided about eating/drinking etc...
- pH inside the mouth is 7.0
Acidic media (limited absorption)
- Cigarettes
Alkaline media (significant absorption)
- Pipes, cigars, spit tobacco, oral nicotine products
- smoke is acidic
List common physical symptoms of nicotine withdrawal and their usual onset/duration for RECENT quitters
symptoms that occur 1 week later:
- Irritability/Frustration /Anger
- Anxiety
- Difficulty concentrating
- Restlessness/Impatience
- Depressed mood/Depression
- Insomnia
- Impaired task performance
- Increased appetite
- Weight gain
- Cravings
symptoms that occur after 1 week and can last to +6 months:
- Increased appetite
- Weight gain
- Cravings
List common physical symptoms of nicotine withdrawal and their usual onset/duration for FORMER TOBACCO USER quitters
symptoms that occur after 1 week and can last to +6 months:
- Increased appetite
- Weight gain
- Cravings
what is the usual time course of nicotine withdrawal symptoms?
Most symptoms manifest within the first 1-2 days, peak within the first week, and subside within 2-4 weeks
Pharmacotherapy of nicotine cessation is not recommended for which populations?
- Pregnant smokers
- Smokeless tobacco users
- Individuals smoking fewer than 10 cigarettes per day
- Adolescents
what are the FDA‐approved medications for nicotine cessation?
Nicotine polacrilex gum
- Nicorette (OTC)
- Generic nicotine gum (OTC)
Nicotine lozenge
- Nicorette (OTC)
- Generic nicotine lozenge (OTC)
Nicotine transdermal patch
- Habitrol (OTC)
- NicoDerm CQ (OTC)
- Generic nicotine patches (OTC)
Nicotine nasal spray
- Nicotrol NS (Rx)
Bupropion SR
- Generic (Rx)
Varenicline
- Chantix (Rx)
What are NRT precautions?
Underlying CV disease:
- Recent MI (within past 2 weeks)
- Arrythmias
- Serious/worsening angina
What are the components of Nicotine Gum (Nicorette and Generics)?
Resin complex, Nicotine, Polacrilin
What are the available strengths and flavors of Nicotine Gum?
2 mg, 4 mg; original, cinnamon, fruit, and mint (various) flavors
What is the formulation of Nicorette Lozenge and Nicorette Mini Lozenge?
Nicotine polacrilex
How does the nicotine lozenge compare to an equivalent gum dose in terms of nicotine delivery?
Delivers ~25% more nicotine
What are the available strengths of the nicotine lozenge?
2 mg, 4 mg
what is nicotine gum + lozenge dosing based on?
the "time to first cigarette" (TTFC) as an indicator of nicotine dependence
when do should you use the 2 mg gum/lozenge?
If first cigarette of the day is smoked more than 30 minutes after waking
when do should you use the 4 mg gum/lozenge?
If first cigarette of the day is smoked within 30 minutes of waking
what is the recommended usage schedule for gum/lozenge?
Weeks 1-6
1 piece q 1-2hr
Weeks 7-9
1 piece q 2-4hr
Weeks 10-12
1 piece q 4-8hr
how should nicotine gum be used?
Chew slowly --> Stop chewing at first sign of peppery taste or tingling sensation --> Park between cheek and gum --> Chew again when peppery taste or tingle fades --> repeat as needed
how should nicotine lozenge be used?
- Place in mouth and allow to dissolve slowly (nicotine release may cause warm, tingling sensation)
- Do not chew or swallow
- Occasionally rotate to different areas of the mouth
- Lozenges will dissolve completely in about 20-30 minutes
Do NOT eat or drink for ____ minutes BEFORE or while using the nicotine gum or lozenge.
15
To improve chances of quitting, how many pieces of gum/lozenge should be used during the first 6 weeks?
at least nine pieces
what foods/beverages may reduce the effectiveness of the nicotine gum/lozenge?
− Coffee
− Juices
− Wine
− Soft drinks
what could chewing the lozenge/using incorrect gum chewing technique result in?
can cause excessive and rapid release of nicotine, resulting in:
- Lightheadedness/dizziness
- Nausea and vomiting
- Hiccups
- Irritation of throat and mouth
what are the adverse effects of nicotine gum and lozenge?
• Mouth and throat irritation
• Hiccups
• Gastrointestinal complaints (dyspepsia, nausea)
describe the Transdermal Nicotine Patch:
• Continuous (24‐hour) nicotine delivery system
• Nicotine is well absorbed across the skin
• Transdermal delivery to systemic circulation avoids hepatic first‐pass metabolism
• Plasma nicotine levels are lower and fluctuate less than with smoking
describe the dosing of transdermal nicotine patches:
• come in 21mg, 14mg, or 7mg
• heavy smokers use up to 21mg whereas light smoker use up to 14mg
• taper dose off (ex: 21mg for a few weeks, then 14mg, then 7mg)
light smokers
≤10 cigarettes/day
heavy smokers
>10 cigarettes/day
how are transdermal nicotine patches used?
• Choose an area of skin on the upper body or upper outer part of the arm
• Make sure skin is clean, dry, hairless, and not irritated
• Apply patch to different area each day
• Do not use same area again for at least 1 week
• Remove protective liner and apply adhesive side of patch to skin
• Peel off remaining protective covering
• Press firmly with palm of hand for 10 seconds
• Make sure patch sticks well to skin, especially around edges
• Wash hands
• Do not leave patch on skin for more than 24 hours
• Adhesive remaining on skin may be removed with rubbing alcohol or acetone
• Dispose of used patch by folding it onto itself, completely covering adhesive area
T or F: you are able to have a nicotine patch on while getting an MRI
false, must be removed
what are common adverse effects of transdermal nicotine patches?
- Irritation at the patch application site (generally within the first hour)
- Sleep disturbances (Abnormal/vivid dreams, Insomnia)
what should you do if after removing a nicotine patch, the skin stays red more than 4 days or if it swells or a rash appears?
contact health care provider—do not apply new patch
what should be assessed after each withdrawal encounter?
assess withdrawal and adjust treatment as needed
Describe the general efficacy of the pharmacologic aids for cessation vs going "cold turkey"
- pharmacologic therapy show higher efficacy rates
- very hard to quit if going "cold turkey"
Identify the “five As” of smoking cessation in the correct order
• ASK about tobacco USE
• ADVISE tobacco users to QUIT
• ASSESS READINESS to make a quit attempt
• ASSIST with the QUIT ATTEMPT
• ARRANGE FOLLOW-UP care
what is the "common cold"?
- acute infectious rhinitis
- self-limiting viral infection of the upper respiratory tract
what causes the common cold?
Rhinovirus and other types of viruses
describe the pathophysiology of the common cold:
- Viruses attach to nasal mucous membranes causing cellular injury
- Cellular defense and plasma protein system is activated
- Chemical mediators of inflammation (PGs, kinins, leukotrienes) are released
- Cholinergic stimulation -- increases mucous gland activity; may cause sneezing
- Inflammation of mucous membranes (esp. the nose, sinuses, and throat)
- Vasodilation and ↑ vascular permeability results in nasal obstruction & discharge
how long does the "typical" common cold last?
~1 week
if the scratchy/sore throat caused by the common cold is severe enough, what could be used for treatment?
oral analgesics
if the runny nose caused by the common cold is severe enough, what could be used for treatment?
first generation antihistamines
how should nasal congestion/stuffiness caused by the common cold be treated?
decongestants
how should systemic complaints caused by the common cold be treated?
oral analgesics
what are symptoms of the common cold?
Scratchy throat / Sore throat
• most noticeable on day 1, resolves quickly
• May or May Not need treatment
Sneezing
• Minimal; not a concern
Runny nose
• usually BRIEF at the start of the illness
• Clear & runny secretions at first, then become thicker and harder to drain
• May or May Not need treatment
Nasal CONGESTION "stuffy head"
• Nearly 100% of pts have nasal involvement
• the most bothersome symptom people seek help for
Cough
• Infrequent
• Often not bothersome until nasal symptoms subside
Systemic complaints: fever, chills, HA, myalgia
- Usually absent, of minimal severity if present
- May or May Not need treatment
what are the general recommendations for the common cold?
- drink fluids
- oral analgesic/antipyretics, treat systemic or scratchy/sore throat complaints only IF present and ONLY if bothersome (acetaminophen, NSAIDs)
is histamine the cause of the common cold?
no
why don't second generation antihistamines relieve a runny nose from a common cold?
- no anticholinergic activity
- not effective
can first generation antihistamines relieve a runny nose from the common cold?
they MIGHT, the MOA has anticholinergic activity
- some effectiveness in adults
- ineffective in children
no way to predict if a patient will respond or not
what are the adverse effects of first generation antihistamines?
- drowsiness/sedation
- drying effect (may increase duration of nasal congestion)
what are the precautions regarding first generation antihistamines?
- narrow angle glaucoma
- urinary retention... may worsen symptoms of BPH
what are the available ingredients in first generation antihistamines?
1. Doxylamine succinate (found in Nyquil® and other combo "nighttime" products) (Not available as a single ingredient except in OTC sleep aid products)
2. Chlorpheniramine maleate
3. Others - also used in some cough/cold products
• Brompheniramine (most associated with the brand name Dimetapp)
• Diphenhydramine (often labeled "nighttime" use)
OTC drug review studies showed ______________ that certain antihistamines show some effectiveness for reducing the runny nose and sneezing due to the common cold.
limited evidence
what is the age limit for 1st generation antihistamines?
6yo
what is the most common ingredient for runny nose in all cough/cold meds?
Chlorpheniramine maleate
which med is the least sedating out of all the sedating?
Chlorpheniramine maleate
what symptoms do almost all patients with the common cold experience?
congestion/stuffy head
What is the MOA of nasal decongestants?
- Sympathomimetic activity
- Alpha receptor stimulation constricts blood vessels in the nasal mucosa
what are the FDA approved uses for nasal decongestants?
• Temporarily relief of sinus congestion and pressure
• Nasal congestion due to the common cold, hay fever or other upper respiratory allergies
what dosage forms do nasal decongestants come in?
1. Oral
2. Topical - nasal sprays and vapor inhalers
what is the ORAL nasal decongestant?
Pseudoephedrine (Sudafed, generics)
how does pseudoephedrine have cardiac effects?
- due to beta receptor stimulation (tachycardia, palpitations...)
- Is NOT considered safe in patients with most CV disease
can pseudoephedrine cross the BBB?
yes, acts as a CNS stimulant... may cause insomnia/restlessness
what are dosage forms of pseudoephedrine?
- Immediate release (30mg tablets, 15mg/5ml liquid)
- Sustained release (120mg SR tabs dosed q12hrs) or (240mg ER tabs dosed q24hrs)
how is immediate release pseudoephedrine dosed?
Given every 4-6 hours up to maximum of 4 doses /24hrs as follows:
• ≥12yrs 60mg per dose (max 240mg daily)
• 6-11yrs 30mg per dose (max 120mg daily)
• 4-5yrs 15mg per dose (max 60mg daily)
for immediate release pseudoephedrine, "do not use" labeling for children under...
4yo
what age is sustained release pseudoephedrine approved for?
patients ≥ 12yrs
when should you avoid taking pseudoephedrine?
4-6hr before bedtime due to CNS stimulation
describe the bioavailability/half-life of phenylephrine HCL (Sudafed-PE®, generics):
• Low oral bioavailability (38%) due to extensive 1st pass effect and erratic absorption
• Short half-life...only 2.5 hours! (has a shorter duration of action)
is phenylephrine HCL considered safe in CV patients?
CV effects are unpredictable; are usually dose related; is NOT considered safe in CV patients
does pseudoephedrine or phenylephrine HCL cause less CNS stimulation?
phenylephrine HCL... may cause less insomnia/restlessness
how is phenylephrine HCL dosed?
Immediate release (10mg tabs, 2.5mg/5ml)
Given q 4 hours up to 6 doses per day
• ≥12yrs 10mg per dose (max 60mg daily)
• 6-11yrs 5mg per dose (max 30mg daily)
• 4-5yrs 2.5mg per dose (max 15mg daily)
what are the issues with phenylephrine?
Controversy over EFFICACY
what are the precautions with pseudoephedrine/phenylephrine?
1. Urinary retention / May worsen symptoms of BPH
2. Heart disease
- Do not use
- examples: MI, heart failure, TIA, stroke, CABG, stents, arrhythmias
3. Hypertension - sometimes will use pseudoephedrine, NEVER phenylephrine... ask the pharmacist
what are the contraindications (do not use) with pseudoephedrine/phenylephrine?
- Pts receiving antidepressant drugs MAO Inhibitors (or within 14 days of therapy).... may cause hypertensive crisis which can be fatal!
• Nardil® (phenelzine)
• Parnate® (tranylcypromine)
• Marplan® (isocarboxazid)
can pseudoephedrine/phenylephrine be used in pregnancy?
• Do NOT use in pregnancy except under the advice of a physician
• No Self-Care
• Concern - the effect of systemic vasoconstriction in the developing fetus is not known
can pseudoephedrine/phenylephrine be used while breastfeeding?
• Phenylephrine is NOT compatible
• PSEUDOEPHEDRINE - is rated as COMPATIBLE by the American Academy of Pediatrics
what effect does pseudoephedrine have on breast mil?
known to decrease milk production
what is the MOA of TOPICAL nasal decongestants?
sympathomimetic vasoconstrictor; act locally on the nasal mucosa; acts very rapidly
what is the age limit for LIQUID NASAL SPRAYS?
• Check your labels! Approved for patients ≥ 6yrs or patients ≥ 12yrs
• Parents should be discouraged from using these products in young children
what are the ingredients in liquid nasal sprays?
1. oxymetazoline
2. phenylephrine
how is oxymetazoline dosed?
- Administered q 10-12hrs
- Max of 2 doses in 24hrs
what is the approved age of use of oxymetazoline?
≥12yo
oxymetazoline
Afrin®
how is phenylephrine dosed?
Administered q 4hrs
what is the approved age of use of phenylephrine?
≥ 6yo or ≥ 12yo
phenylephrine (liquid nasal spray)
NeoSynephrine®
what are the warnings surrounding liquid nasal sprays?
• heart disease
• high blood pressure
• difficulty urination due to enlargement of the prostate gland
what may liquid nasal sprays cause?
"Rebound Congestion" (aka: rhinitis medicamentosa)
what is rebound congestion?
nasal congestion when the drug wears off...
when does rebound congestion occur?
topical decongestants are used for longer than 3-5 days
FDA requires labeling to limit use of topical decongestants to no longer than _____ days
3
when may liquid nasal sprays be appropriate to consider recommending?
for patients who can't use PSE
what ages are approved medicated vapor inhaler use?
≥6yo