Smoking, Asthma, COPD Flashcards
True/False: Smoking is bad for you.
True
Name 3 First line options for smoking cessation.
- Nicotine gum
- Nicotine Lozenge
- Transdermal Nicotine Patch
Pregnancy Category of Nicotine Gum?
Category D
ADRs of Nicotine Gum? (Nicorette)
Mouth soreness
hiccups
dyspepsia
aching jaw
What route of absorption does Nicotine Gum use? (Nicorette)
Buccal Absorption
MOA of Nicorette?
Resin complex: nicotine, polacrilin
Sugar free chewing gum base
Contains buffering agents to enhance buccal absorption of nicotine
MOA of Nicotine Lozenge?
Nicotine polacrilex formulation: delivers 25% more than gum
Sugar free
Contains buffering agents to enhance buccal absorption of nicotine
MOA of Nicotein Transdermal Patch? (Nicoderm CQ)
Nicotine = well absorbed across skin
Delivery to systemic circulation avoids hepatic first-pass metabolism
Plasma nicotine levels are lower and fluctuate less than
Can you Swim or Cut Nicotine patch?
Yes Swim
NO Cut
ADR of Nicotine Lozenge?
Nausea, hiccups, cough, heartburn, headache
ADR of Nicotine Patch?
1st hour: Mild itching, burning, tingling
Others: vivid dreams/sleep disturbances, HA, local skin rxns. (rotate patch site, use steroid cream.)
MOA of Nicotine Inhaler?
Delivers 4 mg nicotine vapor over 80 puffs, absorbed across buccal mucosa
(Try not to inhale)
How long must you wait to eat or drink after Nicotine Inhaler (Pfizer)
15 minutes
ADR of Nicotine Inhaler?
Mild irritation of the mouth or throat (40%) Cough (32%) Headache Rhinitis (23%) Dyspepsia (indigestion)
MOA of Varenicline (Chantix)
Non-nicotine cessation aid, partial nicotinic receptor agonist.
Binds with high affinity and selectivity at a4b2 neuronal nicotinic acetylcholine receptors: stimulates low-level agonist activity, competitively inhibits binding of nicotine
Clinical effects: Symptoms of nicotine withdrawal, blocks dopaminergic stimulation responsible for reinforcement & reward associated with smoking
When should pt begin Varenicline (Chantix)
Patients should begin therapy 1 week PRIOR to their quit date. The dose is gradually increased to minimize treatment-related nausea and insomnia.
Major Warnings with Varenicline (Chantix)
Neuropsych symptoms/Suicidality
Cardiovascular events
Other ADRs with Varenicline (Chantix)
Common: N/V, sleep disturbances [insomnia, abnormal dreams], constipation, FARTS!
Uncommon: hypersensitivity, serious skin rxn, accidental injury
What must patient do with every dose of Varenicline (Chantix)
Drink a full Glass of Water!
MOA of Bupropion [Wellbutrin, Zyban]?
Unclear
Blocks DA and NE reuptake
(Use with other Nicotine Replacement Therapies)
CI with Bupropion (Wellbutrin)
SEIZURES, h/o eating disorders, use of MAO-I
ADRs of Bupropion (Wellbutrin, Zyban)?
Dry mouth, insomnia, weight loss or may delay weight gain
Pregnancy Category of Clonidine?
Category C… for Clonidine
What special consideration do you have to consider when taking a patient off Clonidine?
Must taper dosing due to rebound hypertension
ADRs of Clonidine?
Dry mouth (40%)
Drowsiness (33%)
Dizziness (16%)
Sedation, constipation (10%)
Pregnancy category of Nortriptyline?
Category D
3 Warnings when with Nortriptyline?
Counsel pts not to drive
Risk of arrhythmias and impaired contractility
Avoid with MAOI
ADRs of Nortriptyline?
Sedation, dry mouth (64 – 78%) Blurred vision (16%) Urinary retention Lightheadedness (49%) Tremor (23%)
When should you start a patient on Nortriptyline for smoking cessation?
Start 10 – 28 days prior to quit date to reach steady state
What Class of drugs do Albuterol, Levoalbuterol, Pirbuterol belong?
Short Acting Beta Agonists (SABA)
MOA of Short Acting Beta Agonists?
Albuterol, Levoalbuterol, Pirbuterol
Bind B2 adrenergic receptors, relax bronchial smooth muscle
What is the 1st line for acute asthma symptom relief and prevention of exercise-induced bronchoconstriction
Short Acting Beta Agonists (SABAs)
Albuterol, Levoalbuterol, Pirbuterol
What is the MOST effective medication class for relieving acute bronchospasm [“rescue inhaler”]
Short Acting Beta Agonists (SABAs)
Albuterol
What is the MAJOR contraindication for SABAs?
Betablockers
ADRs of Short Acting Beta Agonists?
Albuterol, Pirbuterol, Levoalbuterol
Tachycardia
tremor
HA
hypokalemia
Onset of Action for SABA?
3-5 Minutes
When should you reassess pt’s who are only taking SABA?
Increasing use indicates inadequate control: using > 2x/week = reassess tx!
To what class do Ipratropium (Atrovent) and Ipratropium & albuterol (Combivent, Duoneb) belong?
Inhaled Anticholinergics
MOA of Inhaled Anticholinergics?
Ipratropium
Indicated for relief of bronchospasm→ Only relieves cholinergic mediated bronchospasm
Does not modify antigen reaction
Ineffective in EIB
Less cardiac stimulation than SABAS
Indication for use of Inhaled Anticholinergics?
Ipratropium
1st line for bronchospasm with beta blockers
Used off label for asthma→ not proven effective
ADRs of Inhaled Anticholinergics?
dry mouth
increased wheezing?
What class do the following drugs belong?
Prednisone
Methylprednisolone
Prednisolone
Systemic Corticosteroids
MOA of Systemic Corticosteroids?
Prednisone, Methylprenisolone, Prednisolone
Inhibit cytokine production, adhesion, protein activation, inflammatory cell migration and activation - immunosuppressant
Indications for use of Systemic Corticosteroids?
Short term burst [3-10 days] to gain control of inadequately controlled asthma
Long term symptom prevention in severe persistent asthma
Contraindications for Systemic Corticosteroids?
Betablockers
ADRs of systemic corticosteroids?
Short term: hyperglycemia, inc appetite, fluid retention, weight GAIN, mood alteration, HTN, peptic ulcer
Long term: adrenal axis suppression, growth suppression, thinning of skin, osteoporosis, HTN, DM, Cushing’s, impaired immune fxn
(Don’t use Systemic Corticosteroids for longer than you have to)
To what class do the following drugs belong?
Beclomethasone HFA (QVAR) Budesonide (Pulmicort) Flunisolide (Aerobid, Aerospan) Fluticasone (Flovent) Mometasone (Asmanex)
Inhaled Corticosteroids (Glucocorticoids)
What am I drinking?
Pabst Blue Ribbon
MOA of Inhaled Corticosteroids?
Beclomethasone Budesonide Flunisolide Fluticasone Mometasone
Potent anti-inflammatory agents
Increase blood neutrophil counts
Reduce: inflammatory mediators [prostaglandins and leukotrienes], other WBCs and lymphocyte and macrophage fxn
Anti-inflammatory:
- Block late phase reaction to allergen
- Reduce airway hyper-responsiveness
- Inhibit cytokine production, adhesion, protein activation & inflammatory cell migration/activation
- Reverse beta receptor down regulation
- Inhibit microvascular leakage
Are Inhaled Corticosteroids 1st line in adults with Persistent Asthma?
Beclomethasone
Fluticasone
Flunisolide
YES
1st line in adults w/ persistent asthma
- Prevent sx
- Suppress, reverse, & control inflammation [↓ exacerbation FREQUENCY]
- Most potent & consistently effective long term control rx for asthma
- decrease need for oral corticosteroid
- Reduce symptom severity
- Improve asthma control and QOL
- Improve PEF and spirometry
- Decrease airway hyper-responsiveness
- Prevent exacerbations
- Reduce systemic corticosteroids, ED care, hospitalization and mortality
- May help with loss of lung function in adults
ADRs of Inhaled Corticosteroids?
Budesonide, Fluticasone, Beclomethasone
Oral candidiasis dysphonia cough reflex cough bronchospasm
The following Drugs belong to which Class?
Salmeterol [Serevent, Advair]
Fluticasone/vilanterol [Breo Ellipta]
Formoterol [Symbicort, Dulera]
Indacaterol [Arcapta]
Long Acting Beta Agonists (LABAs)
MOA of Long Acting Beta Agonists?
Salmeterol, Vilanterol, Formoterol, Indacaterol
Relaxes bronchial smooth muscles - bronchodilation
Indications for use of Long Acting Beta Agonistis?
Salmeterol, Formoterol
Longer duration of action than SABAs [12 hrs]
USE WITH STEROID - do NOT use as monotherapy or for acute sx
Warnings for LABA?
Black box for asthma pts ???
ADRs of LABA?
Salmeterol, Vilanterol, Formoterol, Indacaterol
Tachycardia
tremor
hypokalemia
prolonged QT [usually OD]
What Class do the following drugs belong?
Montelukast [singulair]
Zafirlukast [Accolate]
Leukotriene receptor antagonists [LTRAs]
What Class does the following drug belong?
Zileuton [Zyflo]
5-lipoxygenase inhibitor
MOA of Leukotriene Receptor Antagonists?
Montelukast, Zafirlukast
- alternative tx for mild persistent asthma
- adjunct tx with ICS for moderate asthma [proven reduction in systemic steroid use, no change in need for rescue inhalers]
- modest improvement in lung function as monotherapy
MOA of Zileuton?
5-Lipoxygenase inhibitor
Inhibits leukotriene production
At what age can the following drugs be used?
Montelukast
Zafirlukast
Leukotriene Receptor Antagonists
Montelukast = 1 y/o
Zafirlukast = 7 y/o
Zifirlukast (Leukotriene Receptor Antagonist) and Zileuton (5-lipoxygenase inhibitors) are Both P450 Inhibitors!
The two Zs of Leukotrienes are p450 inhibitors
What class does the following drug belong?
Theophylline [Theo-24, Theolair, Quibron-T]
Methylxanthines
MOA of Methylxanthines? (Theophylline)
Nonselective phosphodiesterase inhibitor
relaxes bronchial smooth muscle
↑ diaphragm contractility/mucociliary clearance
MOA of Omalizumab [Xolair]?
Injection
Anti-IGE
Inhibits binding of IgE to IgE receptors on mast cells and basophils
MOA of Mepolizumab?
IL-5 antagonist
IL-5: major role in growth and activation of eosinophils, blocking IL-5 prevents binding to eosinophils - ↓inflamm response
MOA of Reslizumab?
IL-5 antagonist
The following drugs are used for what Dz? Tiotroprium [Spiriva] Glycopyrrolate [Seebri] Aclidinium [Tudorza] Roflumilast [Daliresp]
COPD
MOA of Tiotroprium (Spiriva)
Long acting anticholinergic
Blocks M3 receptors that lead to bronchial smooth muscle constriction
Allows for bronchodilation, slower than alpha agonist
MOA of Glycopyrrolate and Aclidinium?
newer inhalers
Anticholinergics
Why are Anticholinergics used in pt’s which airway problems?
Release of acetylcholine from parasympathetic nerves activates postjunctional muscarinic receptors present on airway smooth muscle, submucosal glands, and blood vessels to cause bronchoconstriction, mucus secretion, and vasodilatation, respectively. … These changes are due to increased parasympathetic nerve activity.
MOA of Romflumilast?
PDE4 inhibitor
PDE4 metabolizes cAMP
Increases intracellular cAMP in lung cells
No direct bronchodilator activity
Reduces moderate to severe exacerbations in pts with chronic bronchitis and COPD
Romflumilast ADRs?
N/D/Ab pain, decreased appetite, HA, sleep disturbances, weight LOSS
Psych: suicidality, insomnia, anxiety, depression, suicidal thoughts, mood changes
P450 substrate!
