agents for respiratory illness Flashcards
what is asthma
chronic inflammation of airways
contraction of bronchial smooth muscle
acute bronchospasm
increased secretion of mucus
what is the presentation of asthma
SOB
cough
chest tightness
wheezing
what is intermittent asthma
less than two days per week
near normal peak flow or spirometry
no daily medication
quick relief: short-acting B2 agonist
what is mild persistent asthma
more than 2 days per week, not daily
near normal peak flow or spirometry
long term: low dose inhaled corticosteroids
quick: short acting B2 agnoist
what is moderate persistent asthma
daily bronchoconstricitve episodes
60-80% or normal for peak flow or spirometry
long term: low to medium dose corticosteroids and long-acting B2 agonists
quick: short acting B2 agonist
what is severe persistent asthma
continual bronchoconstrictive episodes
less than 60% of normal peak flow or spirometry
high dose inhaled coricosteroids and long acting b2 agonist
quick: short acting B2 agonists
what is well controlled asthma
<2 days/week of symptoms/
< 2x/month nigh-time awakenings
no interference with ADL
short acting b2 agonist use <2 days/week
>80% of peak flow
what is not well controlled asthma
> 2 days/week of symptoms
1-3x/week of night time awakenings
some limitation with ADLs
2 days/week use of short acting b2 agonists
60-80% peak flow
what is very poorly controlled asthma
symptoms throughout the day
nighttime awakenings > 4x/week
extremely limited ADLs
short acting b2 antagonist used several times per day
< 60% peak flow
what determines normal values for peak expiratory flow (PEF)
age and height
what is the target of respiratory drugs
‘conducting zone’
Sympathetic innervation, parasympathetic innervation and mucous secreting and ciliated cells that remove inhaled particles
what is the sympathetic innervation of the respiratory system
sympathetic adrenergic neurons which activate B2 receptors -> bronchial dilation (B2 receptors activated by circulating epinephrine)
what is the the parasympathetic innervation of the respiratory system
parasympathetic cholinergic neurons which activate muscarinic receptors -> bronchial constriction
what is within the conducting zone
trachea
bronchi
bronchioles
what is within the respiraotry zone
respiratory bronchioles
alveolar ducts
alveolar sacs
what is albuterol
short acting beta 2 agonists - bronchodilators
what is the MOA for albuterol
activation of adenylate cyclase and increase in intracellular concentration of cAMP causing bronchodilation, relieves bronchospasm, increase mucous drainage
what is the indication for albuteral
management of acute bronchospasm in asthma and other chronic obstructive airway diseases
what are the adverse effects of albuterol
sympathomimetic effects: tachycardia, hyperglycemia, hypokalemia
tremor (common)
what is metaproterenol (orciprenaline)
moderately selective b2 agonist
inhaled or tablet forms available (only oral in USA)
not recommended for routine use given slow onset of action
known to exist but dont plan to prescribe
what is levalbuterol
another short-acting b2 agonists
inhaled (MDI and nebulizer forms)
deemed inferior to albuterol for management of acute asthma symptoms
what are leukotriene modifiers
zafirlukast and montelukast (leukotriene receptor antagonists)
zileuton (5-lipoxygenase inhibitors)
what are the properties of leukotrienes
chemoattractant for eosinophils and neutrophils
constrict bronchiolar smooth mm
increased endothelial permeability
promote mucus secretion
what are the indications for leukotriene modifiers
prophylaxis and treatment of asthma, allergic rhinitis, exercise-induced broncoconstriction
when are leukotriene modifiers contraindicated
pehnylketonuria
hepatic disease
what is Zafirlukast
first FDA approved leukotriene receptor antagonist in US
2 doses - oral tablets
less effective than inhaled glucocorticoids for management of persistent asthma
preferred in asthma tx in children - not useful for treatment of acute asthma attacks
what is montelukast
phophylaxis and maintenance of asthma and more commonly prescribed in US
can be used to treat chronic urticaria
usually added on after initiation of ICS in adults
what is Zileuton
inhibits 5-liopoxygenase -> inhibits formation of leukotrienes
used for chronic asthma management only
common adverse effect = elevation of liver enzymes
infrequently used, 4x daily dosing
interferes with CYP metabolism
what is the indication for methyxanthines
use for both orally and IV in treatment of asthma, bronchospasm and COPD (rarely); also in infant apnea
alternate treatment for asthma; not first line
what is the MOA for methylxanthines
structurally similar to caffeiene
sympathomimetic -> increase HR, inotropy, BP
relaxes smooth muscle
anti-inflammatory and immunomodulatory effect
what is theophylline
methylxanthine
competitive nonselective PDEi which increases intracellular cAMP, activates PKA, inhibits TNF-alpha, inhibits leukotriene synthesis
(reduce inflammation and innate immunity)
also nonselective adenosine receptor antagonists - cardiac effects
whar are concerns with theophylline
narrow TRUTH IS
toxic side effects: N/D, Heart arrhythmias, CNS excitations, seizures
many drug-drug interactions (fluoroquinolone, erythromycin, some SSRIs)
what needs to be monitored with theophylline
LFTs, PFTs and serum theophylline concentration
what is aminophylline
only available outside the US
compound of theophylline with ethylenediamene
less potent and shorter acting
same MOA as theophylline
what are the inidcations for inhaled corticosteroids
acute and or persistent asthma (mild to severe); COPD
what is the MOA for inhaled corticosteroids
suppress inflammatory and immune response, and reduce edema and secretions by the following mechanisms;
controls the rate of protein synthesis
depresses the migration of polymorphonuclear leukocytes and fibroblasts
reverses capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation
what are the toxic effects of inhaled corticosteroids
cough
cataracts, thrush, hoarseness
HPA suppression
growth suppression
reduction in bone density
what are the inhaled corticosteroids
budesonide (nebulized, MDI or Intranasal)
beclomethasone (nebulized or intransal)
fluticasone (propionate) (inhaled only; sub-type available for intranasal use)
mometasone (inhaled and intranasal)
what are oral corticosteroids
methylprednisolone
prednisolone
prednisone
what are long acting beta agnoists used for
maintenance of asthma and prevention of asthma attacks, exercise-inducted bronchoconstriction prevention and COPD management- not used in acute attack of COPD/asthma
are long acting beta agonists monotherapy or combo therapy
CANNOT BE mono-therapy in asthma treatment
can be used as mono-therapy in COPD
what is the difference from LABA and SABA medications
duration of action
what are LABA drugs
Salmeterol
formoterol (in combo)
what is salmeterol
LABA drug
available in combo with ICS and as mono-therapy (in a dry powder inhaler form)
what is formoterol
only available as nebulized solution or in combo with LABA in the US
faster onset of action than salmeterol as a result of lower lipophilicity
more potent
what are combonidation inhalers
LABA/ICS
SABA/anticholinergic
what are LABA/ICS combination inhalers
advair (salmeterol/fluticasone)
symbicort (formoterol/budesonide)
Dulera (formoterol/mometasone)
what is combivent
(albuterol/ipratropium)
SABA/anticholinergic combination inhaler
what are mast cell stabilizers/modulators used for
to prevent or control certain allergic disorders
block mast cell degranulation, stabilizing the cell and thereby preventing release of histamine and related mediators
what is Cromolyn
mast cell stabilizer
formerly non-steroid medication of choice for asthma tx prior to advent of LTRA
taken 4x/day
not seen to provide additive benefit with co-administered with steroids
infrequently used
what is Omalizumab
recombinanat DNA-dervied humanized IgG1k monoclonal antibody that specifically binds to free human immunoglobulin E (IgE) in the blood and interstitial fluid
beings to membrane-bound for of IgE on surface of mlgE-expressing B lymphocytes
what is omalizumab used for
to control severe allergic forms of asthma that are steroid resistant
what are the AE of Omalizumab
anaphylaxis in 1-2/1000 cases; increase stroke and MI risk significantly (by 60%)
what is COPD
chronic, irreversible obstruction to the airway
progressive
associated with decrease in FEV1.
what are the severities of airflow limitation in COPD
GOLD 1 - mild (>80)
GOLD 2 - moderate (<80)
GOLD 3 - severe (<50)
COLD 4 - very severe (<30)
what are the COPD GOLD guidelines
categorize -> initiate first line therapy - > follow up based on further DYSPNEA or EXACERBATIONS
what are the indications for Ipratropium
COPD management, specifically to block cholinergic (vagal) mediated bronchospasm and mucus production
what is the MOA for ipratropium
anti-muscarinic activity on the bronchial smooth muscle that results in decreased contractility of smooth muscle
what are the toxic effects of ipratropium
local and systemic anticholinergic effects
xerostomia
urinary retention
overall well tolerated
what is tiotropium
more costly alternative to ipratropium, with same indications
“long acting” anti-muscarinic medications, so only needed once daily
available in inhaled powder form
