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92 Cards in this Set

  • Front
  • Back
What is asthma?
Chronic inflammatory disease
What are the s/s of asthma?
1. recurrent, episodic bouts of coughing
2. wheezing
3. shortness of breath
What is the pathophysiology behind asthma?
1. narrowing of the trachea and bronchioles
2. contraction of airway smooth muscles, mucosal thickening from edema and cellular infiltration
What happens when mast cells are activated?
Mast cells secrete inflammatory cells and inflammatory mediators
What do inflammatory cells cause?
Inflammation
What do inflammatory mediators cause?
Bronchoconstriction
If asthma is untreated, what are the consequences?
Airway remodeling (chronic effect) -- irreversible
Which drug types function as bronchodilators?
1. Beta-adrenergic receptor agonists
2. Methylxanthines
3. Anticholinergic agents
Which drug types function as anti-inflammatory agents?
1. Corticosteroids
2. Leukotriene modifiers
What is the MOA for beta-adrenergic receptor agonists?
Act on beta receptors in the lungs, causing an increase in cAMP. cAMP --> increased relaxation in lungs => BRONCHODILATION
Which beta receptor is responsible for chronotropy in the heart?
Beta 1
Which beta receptor is responsible for inotropy in the heart?
Beta 2
What are the therapeutic effects of beta agonists?
1. Bronchodilation
2. Inhibit the release of bronchoconstricting mediators
3. Increase mucus clearance
What are some examples of non-selective beta agonists?
epinephrine, terbutaline, isoproterenol, metaproterenol
What are some examples of selective beta agonists?
albuterol, levalbuterol, salmeterol, etc.
(-terol endings)
How quickly do short-acting beta agonists (SABA) work?
5 minutes
What are some examples of SABAs?
epinephrine, terbutaline, albuterol, levalbuterol
How quickly do long-acting beta agonists (LABA) work?
30 minutes
What are some examples of LABAs?
salmeterol, formeterol
How does the duration of action compare between LABAs and SABAs?
LABAs work 2-3x longer than SABAs
Which medications are available as MDIs?
albuterol, levalbuterol
Which medications are available as DPIs?
salmeterol, formoterol
Which medication can be administered orally?
albuterol -- increased risk of side effects
Which medications can be administered subQ?
epinephrine, terbutaline -- increased risk of side effects (tachycardia especially)
What is the relationship between albuterol and electrolyte effects?
Albuterol causes potassium to shift intracellularly, resulting in low serum potassium levels. When albuterol use is ceased, potassium shifts back to the extracellular space.
What is the cause of tremors with beta agonists?
Direct stimulation of beta 2 receptors in skeletal muscle
What causes tachycardia with beta agonist med use?
Direct stimulation of beta 1 and beta 2 receptors on heart
How does tolerance develop with beta agonist med use?
Over time there is a down-regulation of beta 2 receptors in the lung and decreased binding affinity for the remaining receptors
What are some significant drug-drug interactions with beta agonists?
1. Adrenergic meds -- additive side effects
2. Beta blockers -- therapeutic effects of beta 2 agonists may be lost
What are the clinical uses for beta agonists?
1. Acute attacks
2. Maintenance therapy
3. Prophylaxis (before exercise or allergen exposure)
What are the indications for LABA therapy?
LABA therapy must be paired with corticosteroids for long-term asthma control
Under what circumstances should LABAs not be used?
Asthma controlled with low or medium doses of inhaled corticosteroids
What is the MOA of methylxanthines?
Inhibit PDE, the enzyme responsible for cAMP breakdown --> relaxation of airway smooth muscles = BRONCHODILATION
Besides bronchodilation, what do methylxanthines promote?
Increased mucus clearance
What are the methylxanthines?
theophylline, aminophylline
What is important about dosing of theophylline?
Oral dosage forms are not interchangeable on a mg-to-mg basis
In what circumstances is theophylline used?
Rarely used or initiated; one of the last options for tx
With which population is aminophylline okay to use?
Pediatric patients
Why is clinical use limited for methylxanthines?
They have a narrow therapeutic index, requiring serum concentration monitoring
Are methylxanthines effective for acute relief of asthma symptoms?
No, but their use reduces the need for SABAs
What is the metabolism/excretion pattern for methylxanthines?
Metabolism: 90% hepatic (CYP 1A2, CYP 3A4)
Excretion: 10% renal
What are the significant CNS side effects of methylxanthines?
1. Increased alertness
2. Seizures
What cardiac side effects are associated with methylxanthines?
Arrythmias
How does the effectiveness of methylxanthines compare to LABAs?
Methylxanthines are less effective as add-on therapy
What is the MOA of anticholinergic agents?
Compete with ACh at the muscarinic receptor causing decreased vagal tone to the airway => BRONCHODILATION
What are the names of anticholinergic agents?
ipratroprium, tiotroprium
Which of the anticholinergic agents works for 24 hours?
tiotroprium
In what formulation is ipratroprium available?
MDI, solution for nebulization
In what formulation is tiotroprium available?
DPI only
What are the possible side effects of anticholinergic agents?
Blurred vision, headache, flushed skin, tachycardia, urinary retention
What are the clinical uses for anticholinergic agents?
1. Maintenance therapy for patients with COPD
2. Combination therapy with SABA for acute attack
What is the MOA of corticosteroids?
1. Cause a reduction in the markers of airway inflammation
2. Decrease vascular congestion and cellular infiltration
3. Improve beta 2 receptor agonists sensitivity to the beta 2 receptor in acute setting
In what forms are corticosteroids available for use?
Inhaled, parenteral
How quickly do corticosteroids work?
Inhaled: ~2 weeks
Parenteral: 6-8 hours
How is the dosing for corticosteroids determined?
Individually, based on the severity of the patient's asthma
What special consideration should be paid to the cessation of corticosteroids?
Patient should be weaned over period of 1-2 weeks when discontinuation is desired
What patient teaching is necessary for inhaled corticosteroids?
Rinse mouth after inhalation to prevent fungal infection
What are the immediate adverse effects of corticosteroid use?
Hyperglycemia; psychiatric disturbances (e.g., delirium)
What are the long-term adverse effects of corticosteroid use?
1. Osteoporosis/fracture
2. HTN
3. Thinning of the skin/impaired wound healing
4. Adrenal axis suppression
5. Myopathy
6. Immunosuppression
7. Glaucoma
What are significant drug-drug interactions with corticosteroid use?
Inhaled corticosteroids + potent CYP 3A4 inhibitors:
clinically significant Cushing's syndrome and adrenal insufficiency
What are the clinical uses of corticosteroids?
1. Acute exacerbations -- blunt late phase asthma; first dose IV then oral therapy
2. Prevention of attacks -- inhalation preferred with dosing based on severity
What is the action of leukotrienes?
Potent constrictors of bronchial smooth muscles
What is the MOA of leukotriene modifiers?
1. Exert anti-inflammatory effects by either preventing leukotriene formation
OR
2. Act as a receptor antagonist
Which leukotriene modifier prevents leukotriene formation?
zileuton (Zyflo)
Which leukotriene modifier acts as a receptor antagonist?
zafirlukast, montelukast
What are the adverse effects of leukotriene modifiers?
1. Hepatotoxicity (zileuton)
2. Headache
3. GI upset
Which leukotriene modifiers have drug-drug interactions?
zafirlukast and zileuton (warfarin and theophylline)
What are the clinical uses of leukotriene modifiers?
1. Maintenance therapy (alternative to corticosteroids)
2. Prophylaxis for exercise or allergen-induced asthma
3. Aspirin-induced asthma
What is the final class of medications used to treat asthma?
Monoclonal antibody -- omalizumab (Xolair)
What is the MOA of omalizumab?
Inhibits IgE binding receptors on mast cells
What adverse effects are a/w omalizumab?
Injection site reactions: bruising, redness, burning, pain
What is the clinical use for omalizumab?
Helpful in moderate to severe persistent allergy-related asthma.

Very expensive and rarely prescribed (all other therapies exhausted first)
What is COPD?
Syndrome of chronic limitation of expiratory airflow obstruction (includes emphysema and chronic bronchitis)
What is the greatest risk factor for COPD?
Smoking
Can medications for COPD reverse damage?
No -- medications can slow the decline in lung function and treat symptoms, but damage is irreversible
How is stable COPD managed long-term?
1. Supplemental O2
2. Regular tx with one or more bronchodilators (esp. anticholinergics)
3. Inhaled corticosteroids
How is stable COPD managed when there is an acute exacerbation?
1. SABA
2. Antibiotics in patients with increased secretions
What are the indications for corticosteroid therapy for COPD?
Regular tx should only be prescribed to patients who remain sympomatic or have recurrent exacerbations
What is the risk a/w inhaled corticosteroid-only therapy for COPD?
Increased rate of pneumonia
What is the best management therapy for COPD?
Corticosteroid + LABA
How does nicotine act on the brain?
Stimulates dopamine release, causing excitation
What is the goal of nicotine replacement therapy (NRT)?
Aims to control nictoine levels in teh bloodstream so that withdrawal does not occur?
What are the benefits of nicotine gum, lozenges, and inhaler?
Patients can titrate therapy to manage withdrawal symptoms
What is the benefit of nicotine patch?
Better compliance
What is the disadvantage of nicotine patch?
Patient cannot titrate to manage symptoms
In which patients are nicotine inhalers contraindicated?
Patients with an underlying bronchospastic condition (e.g., patients using asthma inhaler)
In which patient populations should NRT be used with caution?
1. Immediate (past 2 wks) post-myocardial infarction
2. Serious arrhythmias
3. Serious or worsening angina
How does Bupriopion work (MOA)?
Blocks the reuptake of dopamine
What are the benefits of bupriopion?
1. Can be used in combo with NRT
2. First choice for depressed smokers (bupriopion is an antidepressant)
3. Well-tolerated in patients with CV disease
4. May delay weight gain
5. Can begin med 1-2 wks before quit date
With which patients should caution be used when prescribing bupriopion?
Seizure disorder
What is the MOA for varenicline (Chantix)?
1. Acts as partial agonist at nicotine receptors
2. Prevents full agonist activity of nicotine at the receptors
What is a major warning for prescribing Chantix?
Serious neuropsychiatric symptoms have occurred -- changes in behavior, agitation, depressed mood, suicidal ideation, and vivid dreams