Asthma/ COPD Flashcards
Ashtma vs COPD
Asthma- allergen disease, reduced airway via smooth muscle thickining and bronchocontriction, eosinophils, CD4, symptoms- episodic SOB, cough, chest tightness, often reversible lung function
COPD-inflammation with irritation (cigerrette smoke), reduced airway via cellular damage by external irritants, CD8, symptoms- chronic cough, sputum porduction (excessive mucus production), DOE, often irreversible lung function,
Main featues of asthma
Airway inflammation, airway obstruction, bronchial hyperresponsiveness (easily triggered by stimuli)
Early resonse and late response
Main features of COPD
Bronchitis predominant COPD?
Emphysema predominant COPD?
Airway inflammation, structural changes/ “remodeling” (fibrosis), mucolilary dysfunction
Gasping for breath
Bronchitis predominant COPD- excessive muscus production
Emphysema predominant COPD- trouble breathing
Best way to treat COPD?
Smoking Ceasation- varenicline and bupropion
Only treatment that improves lung function
Inhaled therapy
Preferred route of delivery- Reduce systemic exposure
High concentration lower doses
Need good technique
Metered dose inhaler (MDI)
Advantages- small, compact, portable, easy to use, Can be used with a spacer (improved delivery), no drug preparation
Disadvantages- need proper technique/ coordination with breath (requires a breath hold), Expensive
Dry powder inhaler (DPI)
Advantages- small compact, portable, easy to use, usually cheaper vs MDI, less coordination needed
Disadvantages- patients must prepare the dose, requires fast inhalation (requires a beath hold) moisture sensitive (can’t put in bathroom)
Soft mist inhaler
Advantages- compact, portable, multi dose device , high lung deposition, does not contain propellant
Disadvantages- complicated process for first dose, slow moving mist, cannot use spacer, expensive
Nebulizer
Advantages- minimal technique requied, patient is not required to hold breath
Disadvantages- expensive, requires dose preparation, bulky (not portable), administration times 5-15 min, needd a power source, cleaning needed
Consideration for device selection
Patient related factors- age, physical and cognitive ability, prefernce
Availability of the drug
Convenience- portable, maintenance, cleaning
Cos
Short acting B2 agonist (SABA) MOA and use
MOA- stimulate adenylyl cyclase at beta blockers→ increase cAMP in bronchial smooth muscle→ bronchodilation
DOC for acute asthma attack and exercise induced asthma
onset of action-5 min
duration-3-4 hours
Albuterol
- SABA
- use PRN- ADR- mouth irratation, cough
- ADR at high doses- skeletal muscle tremor, tachycardia/ palpitation, tolerance
- lose selectivity and hit beta 1
- No difference in efficacy as other drugs in class
- Less expnesive then levalbuteral- so albuterol preferred
Levalbuterol
- SABA
- use PRN- ADR- mouth irratation, cough
- ADR at high doses-skeletal muscle tremor, tachycardia/ palpitation, tolerance
- lose selectivity and hit beta 1
- No difference in efficacy as other drugs in class
- More expnesive then albuteral- so albuterol preferred
Long acting B2 agonist (LABA)
MOA- stimulate adenylyl cyclase at beta blockers→ increase cAMP in bronchial smooth muscle→ bronchodilation (Same MOA as SABA)
DOC for asthma when combined with inhaled glucocorticoid
CANNOT BE USED AS MONOTHERAPY FOR ASTHMA
CAN BE USED AS MONOTHERPAY FOR COPD
Good for COPD- drys up mucus secretion
onset of action-30 min
duration-12-24 hours
Salmeterol
- LABA- Long acting dosed twice a day
- use PRN- ADR- mouth irratation, cough
-
ADR at high doses-skeletal muscle tremor, tachycardia/ palpitation, tolerance
- lose selectivity and hit beta 1
Formoterol
- LABA- long acting dose twice a day
- use PRN-ADR- mouth irratation, cough
-
ADR at high doses-skeletal muscle tremor, tachycardia/ palpitation, tolerance
- lose selectivity and hit beta 1
Indacaterol
- LABA- ultra long acting dose once a day
- use PRN-ADR- mouth irratation, cough
-
ADR at high doses-skeletal muscle tremor, tachycardia/ palpitation, tolerance
- lose selectivity and hit beta 1
Olodaterol
- LABA- ultra long acting dose once a day
- use PRN-ADR-mouth irratation, cough
-
ADR at high doses-skeletal muscle tremor, tachycardia/ palpitation, tolerance
- lose selectivity and hit beta 1
Vilanterol
- LABA- ultra long acting dose once a day
- use PRN-ADR-mouth irratation, cough
-
ADR at high doses-skeletal muscle tremor, tachycardia/ palpitation, tolerance
- lose selectivity and hit beta 1
Ipratropium
Muscarinic antagonist- short acting
MOA- competitively block effecrs o Ach in airway→ prevent vasocontriction medicated by vagal discharge
Bronchodilation effects longer then B2 agonist
ADR- minimally absorbed, well tolerated, (HOT, DRY, FAST, CRAZY)
- dry mouth, eyes
- bitter, metallic taste
- constipation
- urinary retention
- NO TREMER OR ARRHYTHMIAS ( good for older COPD patients)
Tiotropium
Muscarinic antagonist- long acting
MOA- competitively block effecrs o Ach in airway→ prevent vasocontriction medicated by vagal discharge
Bronchodilation effects longer then B2 agonist
ADR- minimally absorbed, well tolerated,(HOT, DRY, FAST, CRAZY)
- dry mouth, eyes
- bitter, metallic taste
- constipation
- urinary retention
- NO TREMER OR ARRHYTHMIAS ( good for older COPD patients)
Aclidinium
Muscarinic antagonist- long acting
MOA- competitively block effecrs o Ach in airway→ prevent vasocontriction medicated by vagal discharge
Bronchodilation effects longer then B2 agonist
ADR- minimally absorbed, well tolerated,(HOT, DRY, FAST, CRAZY)
- dry mouth, eyes
- bitter, metallic taste
- constipation
- urinary retention
- NO TREMER OR ARRHYTHMIAS ( good for older COPD patients)
Umeclidinum
Muscarinic antagonist- long acting
MOA- competitively block effecrs o Ach in airway→ prevent vasocontriction medicated by vagal discharge
Bronchodilation effects longer then B2 agonist
ADR- minimally absorbed, well tolerated,(HOT, DRY, FAST, CRAZY)
- dry mouth, eyes
- bitter, metallic taste
- constipation
- urinary retention
- NO TREMER OR ARRHYTHMIAS ( good for older COPD patients)
Glycopyrolate
Muscarinic antagonist- long acting
MOA- competitively block effecrs o Ach in airway→ prevent vasocontriction medicated by vagal discharge
Bronchodilation effects longer then B2 agonist
ADR- minimally absorbed, well tolerated, (HOT, DRY, FAST, CRAZY)
- dry mouth, eyes
- bitter, metallic taste
- constipation
- urinary retention
- NO TREMER OR ARRHYTHMIAS ( good for older COPD patients)
Theophylline
Methylxanthine derivatives
MOA- non-selectively inhibits phosphodiesterase (PDE)→ increasaes cAMP→ bronchodilation blocks adenosine recpotors→ bronchodilation
Considered high concentration to be effective
narrow theraputic index
Younger people- will clear drug quicker (higher dose)
Older people- will clear it slower (lower dose)
CYP 1A2 metabolism- tabacco smoke inducer of CYP 1A2
- Smokers need higer dose
- when they quit smoking need lower dose otherwise toxic effects
ADR- theophyline over 40
- GI distress (enhanced grastic acid secretion)
- Tremor
- Insomnia
- in overdose- severe nausea, vomitting, hypotension, agitation, arrthymias, cardiac arrest, seizures
Roflumilast
- MOA- selectively inhibits PDE-4 (found in the lung)→ increase cAMP→ Bronchodilation
- USED FOR SEVERE ASTHMA/ COPD
- Should be given with at least one other long acting broncodilator for COPD (LABA)
- Partially metabolized by CYP 3A4
- DDI- with rifampin, phenobarbital, phenytoin, carbamazepine
-
ADR
- N/V/D, abdominal pain, HA, dyspepsia
- Psychiatric events- scren for psych events prior to use, d/c therapy if mood changes
- weight loss
Corticosteroids
MOA- Bind to glucocorticoid receptor to
- inhibit inflammatory cell migration and activation
- inhibit cytokines and mediator release
- upregulates b2 recepotris
- inhibits IgE synthesis
DOC FOR ASTHMA IN COMBINATION WITH LABA
TAPER OFF
4-6 weeks for effect
used if on SABA but still chronic SOB
Beclomethasone
Inhaled corticosteroid
ADR- Thrush (oral candidiasis)- consel patient to rinse mouth after each use, dystonia, sore throat, cough
Budesonide
Inhaled corticosteroid
Safe in pregnancy
ADR- Thrush (oral candidiasis)- consel patient to rinse mouth after each use, dystonia, sore throat, cough
Fluticasone propionate
Inhaled corticosteroid
ADR- Thrush (oral candidiasis)- consel patient to rinse mouth after each use, dystonia, sore throat, cough
Fluticasone furoate
Inhaled corticosteroid
ADR- Thrush (oral candidiasis)- consel patient to rinse mouth after each use, dystonia, sore throat, cough
Mometasone
Inhaled corticosteroid
ADR- Thrush (oral candidiasis)- consel patient to rinse mouth after each use, dystonia, sore throat, cough
Flunisolide
Inhaled corticosteroid
ADR- Thrush (oral candidiasis)- consel patient to rinse mouth after each use, dystonia, sore throat, cough
Ciclesonide
Inhaled corticosteroid
ADR- Thrush (oral candidiasis)- consel patient to rinse mouth after each use, dystonia, sore throat, cough
Prednisone
Oral/ IV corticosteroid
ADR- adrenal supression , cushings syndrome, growth retardation, osteroporosis (dose limiting),glucose intolerance, infection risk, mood changes, weight gain, edema
Prednisolone
Oral/ IV corticosteroid
ADR- adrenal supression , cushings syndrome, growth retardation, osteroporosis (dose limiting),glucose intolerance, infection risk, mood changes, weight gain, edema
Methyleprednisolone
Oral/ IV corticosteroid
ADR- adrenal supression , cushings syndrome, growth retardation, osteroporosis (dose limiting),glucose intolerance, infection risk, mood changes, weight gain, edema
Hydrocortisone
Oral/ IV corticosteroid
ADR- adrenal supression , cushings syndrome, growth retardation, osteroporosis (dose limiting), glucose intolerance, infection risk, mood changes, weight gain, edema
Corticosteriod in kids
Potential growth stunting but only in the first year not progressive
Still preferred DOC in children for asthma
Zileuton
Lipoxygenase inhibitors
MOA- inhibits action of 5-lipoxygenas to inhibit the synthesis of leukotrienes
ADR- Insomnia, Headache, somnolence GI upset, Heptoxicity ( if LFT is greater then 3x the ULN, females greater then 65 at greater risk (monitor))
Neuropsychiatric events- abnormal dreams, hostility, agression, suicidality, agitation, hallucination
DO not use in alcoholics, hepititis
Montelukast
MOA- competitively block action of leukotrienes at LTD4 receptor
Can be used for asthma, allergic symptoms, exercise-induced asthma, urticaria (if anti-hisamine failed)
ADR- Neuropsychiatric events- abnormal dreams, hostility, agression, suicidality, agitation, hallucination
Zafirlukast
MOA- competitively block action of leukotrienes at LTD4 receptor
Can be used for asthma, allergic symptoms, exercise-induced asthma, urticaria (if anti-hisamine failed)
ADR- Neuropsychiatric events- abnormal dreams, hostility, agression, suicidality, agitation, hallucination, Hepatoxicity
DDI- with warfarin→ may increase risk of bleeding
Cromolym sodium
- Mast cell stabilizers- multiple daily doses
- MOA- Block influx of Ca→ prevention of mast cell degreanulation→ stabilize mast cells→ prevent release of inflammatory mediator
- Do not excert any firect bronchodilating, antihistaminic oranti-inflammatory effect (only used for mild cases of asthma)
- Not for rescue symptoms
- Clinical improvment in 2-6 weeks
- Well tolerated
- mild throat irratation, cough abnormal taste in mouth
Nedrocromil sodium
Mast cell stabilizers- multiple daily doses
MOA- Block influx of Ca→ prevention of mast cell degreanulation→ stabilize mast cells→ prevent release of inflammatory mediator
Do not excert any firect bronchodilating, antihistaminic oranti-inflammatory effect (only used for mild cases of asthma)
Not for rescue symptoms
Clinical improvment in 2-6 weeks
Well tolerated
mild throat irratation, cough abnormal taste in mouth
Omalizumab
Anti- IgE
MOA- moncolonal IgE antibody→ inhibits bindng of IgE to surface of mast cells & basophils→inhibit inflammatory mediators
Indicated for allergic asthma not relieved with corticosteroid therapy
Dose based on IgE levels and body weight- SQ injection
Must be older the 12
Takes up to 12 weeks to work
ADR-
- Injection site reactions
- anaphylaxsis→ usually 1.5-2 hours post dose (monitor in office)
- Arthralgia, headache
- Pharyngitis and sinitus
- malignancies?
Mepolizumab
IL-5 Antagonist
MOA- humanized interleukin-5, monoclonal antibody antagonist to reduce the amount of circulating eosinophils
Used for severe asthma for patients who continue to have exacerbations despite adequte therapy
SQ injection or IV every 4 weeks by HCP
Must be older then 18 with eosinophilic phenotype
ADR-
- injection site reactions
- headache
- hypersensitivity reactions- monitor after first dose
- malignancies
- muscle and face bpain