Advanced Pharmacology: Respiratory
Drugs
Asthma - Answer chronic inflammatory disorder of the airway leading to recurrent but
reversible episodes of airway limitations and hyperresponsiveness, wheezing,
breathlessness, and coughing
Asthma pathophysiology: early - Answer IgE binds to receptors on most cells with
allergen exposure causing degranulation and release of histamine, proteolytic,
enzymes, cytokines, leukotrienes, and prostaglandin resulting in bronchoconstriction,
vasodilation, and airway inflammation
Asthma pathophysiology: late - Answer Activated TH2 lymphocytes release cytokines
that recruit more inflammatory cells (eosinophils, mast cells, IgE producing B cells),
leads to airway hyperresponsiveness, edema, mucous production, fibrosis (scarring),
and airway remodeling
Airway remodeling - Answer chronic inflammation that replaces healthy tissue with scar
tissue. Weakens lung function and growth. IRREVERSIBLE
Asthma triggers - Answer allergens, exercise, cold air, environmental pollutants, or
stress
Chronic inflammatory reactions - Answer lead to airway remodeling and damage
Pulmonary Function Tests - Answer Spirometry, PEF, FVC, FEV1
FEV1 - Answer forced expiratory volume in 1 second (less than 25% of predicted value
indicates disease)
FVC - Answer forced vital capacity- maximum act one can forcibly exhale with full
inspiration
PEF - Answer peak expiratory flow (maximum speed of inspiration)
Spirometry - Answer most common PFT, detects 2 abnormal patterns-obstructive
(asthma) or restrictive
Reduced ratio of FEV1:FVC suggests - Answer obstruction, indicative of asthma
Asthma classifications - Answer Intermittent or persistent-mild, moderate, severe
, Treatment goals - Answer minimal or no symptoms, infrequent episodes, no ED visits,
minimal need for reliever medication (SABA), no limitations on activity (including
exercise), normal PEF, minimal adverse effects
Treatment approach - Answer "stepped therapy", as few meds as possible
SABA - Answer short acting Beta2 antagonist, Albuterol or Xopenex, used for quick
relief
ICS - Answer Inhaled Cortocisteroid- QVAR, Pulmicort, Flovent, Asmanex, used for
maintenence
LABA - Answer Long acting Beta-adrenoceptor agonist. Should not be used without
ICS. Servant, Foradil
Combination Products - Answer Fluticasone/Solmeterol (Advair),
Budesonimide/formoterol (Symbicort)
Persistent asthma med progression - Answer 1) SABA prn 2) low dose ICS, SABA 3)
Med dose ICS, or low dose ICS, LABA and SABA 4) Med Dose ICS, LABA and SABA
5) High dose ICS, LABA, SABA (omidizumab?) 6) High dose ICS, LABA, SABA, oral
corticosteroid (omidizumab?)
Histamine and asthma - Answer Asthmatics' bronchial smooth muscle may be 1000x
more sensitive to histamine induced bronchoconstriction than non asthmatics
Why don't we use histamines with asthma? - Answer although they may block histamine
release, they do no reverse bronchoconstriction. Can be used in allergic reactions
Beta 2 Agonist Adverse Effects: Common - Answer tremor, nervousness, headache,
nausea, tachycardia
Beta 2 Agonist Adverse Effects: Long term use - Answer Tolerance (receptor
desensitization, increases asthma exacerbation, decreases bronchoprotection)
Causes of tolerance of Beta 2 Agonists - Answer receptor down regulation, genetic
polymorphisms or beta receptor, isomer effects (can use levalbuterol or Xopenex- same
chemical compound).
Corticosteroids MOA - Answer Enter cellular membranes, bind to glucocorticoid
receptors, activate receptor complexes (travel to nucleus where they act as gene
transcription factors to increase the production of anti-inflammatory mediators and
decrease production of pro inflammatory mediators OR travel within the cytoplasm
where they bind to and increase the activity of 2 rapidly acting pro inflammatory
transcription factors- nuclear factor KB and activating protein 1)
Drugs
Asthma - Answer chronic inflammatory disorder of the airway leading to recurrent but
reversible episodes of airway limitations and hyperresponsiveness, wheezing,
breathlessness, and coughing
Asthma pathophysiology: early - Answer IgE binds to receptors on most cells with
allergen exposure causing degranulation and release of histamine, proteolytic,
enzymes, cytokines, leukotrienes, and prostaglandin resulting in bronchoconstriction,
vasodilation, and airway inflammation
Asthma pathophysiology: late - Answer Activated TH2 lymphocytes release cytokines
that recruit more inflammatory cells (eosinophils, mast cells, IgE producing B cells),
leads to airway hyperresponsiveness, edema, mucous production, fibrosis (scarring),
and airway remodeling
Airway remodeling - Answer chronic inflammation that replaces healthy tissue with scar
tissue. Weakens lung function and growth. IRREVERSIBLE
Asthma triggers - Answer allergens, exercise, cold air, environmental pollutants, or
stress
Chronic inflammatory reactions - Answer lead to airway remodeling and damage
Pulmonary Function Tests - Answer Spirometry, PEF, FVC, FEV1
FEV1 - Answer forced expiratory volume in 1 second (less than 25% of predicted value
indicates disease)
FVC - Answer forced vital capacity- maximum act one can forcibly exhale with full
inspiration
PEF - Answer peak expiratory flow (maximum speed of inspiration)
Spirometry - Answer most common PFT, detects 2 abnormal patterns-obstructive
(asthma) or restrictive
Reduced ratio of FEV1:FVC suggests - Answer obstruction, indicative of asthma
Asthma classifications - Answer Intermittent or persistent-mild, moderate, severe
, Treatment goals - Answer minimal or no symptoms, infrequent episodes, no ED visits,
minimal need for reliever medication (SABA), no limitations on activity (including
exercise), normal PEF, minimal adverse effects
Treatment approach - Answer "stepped therapy", as few meds as possible
SABA - Answer short acting Beta2 antagonist, Albuterol or Xopenex, used for quick
relief
ICS - Answer Inhaled Cortocisteroid- QVAR, Pulmicort, Flovent, Asmanex, used for
maintenence
LABA - Answer Long acting Beta-adrenoceptor agonist. Should not be used without
ICS. Servant, Foradil
Combination Products - Answer Fluticasone/Solmeterol (Advair),
Budesonimide/formoterol (Symbicort)
Persistent asthma med progression - Answer 1) SABA prn 2) low dose ICS, SABA 3)
Med dose ICS, or low dose ICS, LABA and SABA 4) Med Dose ICS, LABA and SABA
5) High dose ICS, LABA, SABA (omidizumab?) 6) High dose ICS, LABA, SABA, oral
corticosteroid (omidizumab?)
Histamine and asthma - Answer Asthmatics' bronchial smooth muscle may be 1000x
more sensitive to histamine induced bronchoconstriction than non asthmatics
Why don't we use histamines with asthma? - Answer although they may block histamine
release, they do no reverse bronchoconstriction. Can be used in allergic reactions
Beta 2 Agonist Adverse Effects: Common - Answer tremor, nervousness, headache,
nausea, tachycardia
Beta 2 Agonist Adverse Effects: Long term use - Answer Tolerance (receptor
desensitization, increases asthma exacerbation, decreases bronchoprotection)
Causes of tolerance of Beta 2 Agonists - Answer receptor down regulation, genetic
polymorphisms or beta receptor, isomer effects (can use levalbuterol or Xopenex- same
chemical compound).
Corticosteroids MOA - Answer Enter cellular membranes, bind to glucocorticoid
receptors, activate receptor complexes (travel to nucleus where they act as gene
transcription factors to increase the production of anti-inflammatory mediators and
decrease production of pro inflammatory mediators OR travel within the cytoplasm
where they bind to and increase the activity of 2 rapidly acting pro inflammatory
transcription factors- nuclear factor KB and activating protein 1)
