Pulmonary Drugs Flashcards
Albuterol is a
short acting beta 2 agonist
inhalation of this product leads to relaxation of bronchial and tracheal smooth muscles in management of acute bronchospasm in asthma and other Chronic obstructive airway diseases
albuterol
Albuterol indications
management of acute bronchospasm in asthma and other chronic obstructive airway diseases
what part of the anatomic structures of the respiratory system do these drugs target
the bronchial tree - the conducting zone
The conducting zone of the bronchial tree contain
sympathetic innervation
parasympathetic innervation
mucus secreting goblet and ciliated cells that remove inhaled products
MOA albuterol
activates adenylate cyclase – increasing cAMP –
less intracellular Ca2+ – leading to dilation
Relaxation of the bronchial and tracheal smooth muscle leads to
relieves bronchospasm
reduces airway resistance
facilitates mucous drainage
increases vital capacity
SE of albuterol
tachycardia (most common)
hyperglycemia (not a contraindication in DM)
hypokalemia (low potassium)
tremor (common)
paradoxical bronchospasm (rare)
Alternatives to albuterol
metaproterenol (inhaled and tablet)
levalbuterol (deemed inferior to albuterol)
Leukotriene modifiers are
montelukast
zafirlukast
Leukotriene modifiers job is to
reduces edema, decrease mucous production, bronchoconstriction, allergic rxns
Indications for Leukotriene modifiers
asthma
allergic rhinitis
exercise-induced bronchoconstriction
Contraindications for Leukotriene modifiers
phenylketonuria
hepatic disease
daily drug to prevent sx of acute asthma
Leukotriene modifiers (montelukast, zafirlukast)
chronic urticaria can also be used by this acute asthma daily preventative
montelukast
Leukotriene modifiers are thought to be _______ effective than inhaled glucocorticoids for management of persistent asthma
less
5-lipoxygenase inhibits
formation of leukotrienes
Example of a 5-lipoxygenase inhibitor
Zileuton
Common adverse affect of 5-lipoxygenase inhibitor
elevated of liver enzymes and interferes with CYP metabolism
Methylxanthines indications
oral and IV treatment of asthma, bronchospasm and COPD (rarely)
also infant apnea
MOA of Methylxanthines
structurally similar to caffeine
relaxes smooth muscle and anti-inflammatory and immunomodulatory effect
Methylxanthines name
Theophylline
Theophylline MOA
is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP – activates PKA – inhibits TNF-alpha – inhibits leukotriene synthesis – reducing intracellular Ca2+
Aminophylline is _____ and _____ acting than Theophylline
less potent
shorter acting
Theophylline has a _______
narrow therapeutic window
Theophylline can increase risk of _____ if over that therapeutic window
seizures and arrhythmias
other GI upset
many drug-drug interactions
Theophylline monitoring with
PFTs
LFTs
serum theophylline concentrations
Inhaled corticosteroids indications
acute and/or persistent asthma (mild-severe), COPD
MOA inhaled corticosteroids
suppress inflammation and immune responses and reduce edema and secretions by:
controls rate of protein synthesis
depresses the migration of polymorphonuclear leukocytes and fibroblasts
reverse capillary permeability and lysosomal stabilization at the cellular level to prevent or control inflammation
SE of inhaled corticosteriods
cough
thrush, hoarseness, cataracts
growth suppression
reduction in bone density
Inhaled corticosteroids include
budesonide
beclomethasone
fluticasone
mometasone
intranasal forms are not a treatment for
asthma
oral corticosteroids include
methylprednisolone
prednisone
prednisolone
Long-acting beta agonists (LABA) are used in
maintenance of asthma and prevention of asthma attacks, exercise-induced bronchoconstriction prevention and COPD maintenance
LABA’s are not used in
acute asthma attacks or acute COPD attacks
LABA can not be used as monotherapy in
asthma treatment
LABA can be used in monotherapy in
COPD management
difference of LABA and SABA
LABA lasts approximately 12 hours
SABA lasts 4-6 hours
LABA names
salmeterol
formoterol (in combination)
Formoterol is ______ than Salmeterol
more potent and faster acting
Combination inhalers LABA/ICS include
salmeterol/ fluticasone (ADVAIR)
formoterol/budesonide (SYMBICORT)
formoterol/mometasone (DULERA)
Combination inhalers SABA/anticholinergic include
Combivent (albuterol/ipratropium)
Mast cell stabilizers/ Modulators are medications that
are used to prevent or control certain allergic disorders
block mast cell degranulation, stabilizing the cell and thereby preventing the release of histamines and related mediators
Mast cell stabilizers/ Modulators include
Cromolyn
Cromolyn is
a mast cell stabilizer
Omalizumab is used
to control severe allergic forms of asthma that are steroid resistant
SE of Omalizumab is
anaphylaxis, inscrease stroke and MI risks by 60%
MOA of Omalizumab
monoclonal antibody that specifically binds to free IgE in the blood and interstitial fluid and membrane bound form of IgE on the surface of mlgE-expressing B lymphocytes
COPD is a _____ disease
progressive, irreversible
Ipratropium indication
management of COPD, specifically to block cholinergic mediated bronchospasm and mucus production
COPD is associated with a decrease in ____
FEV1
MOA ipratropium
antimuscarinic activity on the bronchial smooth muscle that results in decreased contractility of smooth muscle
Toxic effects of ipratropium
local and systemic anticholinergic effects
xerostomia
urinary retention
(overall well tolerated)
A ‘long acting’ antimuscarinic medication is
Tiotropium
Tiotropium is a ______ alternative to ______ with the same indications
costly
ipratropium
Gold 1 - mild COPD = FEV1 of
greater than or equal to 80%
Gold 2 - moderate COPD = FEV1 of
50% - 79%
Gold 3 - severe COPD = FEV1 of
30% - 49%
Gold 4 - very severe COPD = FEV1
less than 30%
During COPD exacerbation we usually give (name of SAMA)
Ipratropium (inhaled, neb)
Daily LAMA for COPD management
Tiotropium
SAMA and LAMA can be used in
COPD and severe persistent asthma
Antitussives (suppress cough)
Centrally acting - dextromethorphan and opiates (codeine, hydrocodone)
Locally acting - benzonatate
MOA dextromethorphan (DM)
crosses the BBB and activates the sigma opioid receptors on the cough center in the medulla – suppressing the cough reflex
Dextromethorphan indications
short term relief of cough
Dextromethorphan does not affect
ciliary activity (Bronchial tree)
Dextromethorphan adverse reactions
mild and infrequent dizziness and drowsiness
high doses can cause hallucinogenic states
Dextromethorphan contraindications
avoid in chronic cough, hepatic disease, operating machinery
Codeine MOA
suppress the cough reflex centrally, dries bronchial secretions
often co-administered with guaifenesin
Codeine indications
short term relief of cough
Codeine interactions
converts to morphine in the liver via CYP450
other use of opiates with this can lead to sedation and resp depression
Codeine contraindications
resp depression, head injury, seizures, hepatic failure
Codeine adverse reactions
tolerance
resp depression
sedation
N/V
potential for abuse
pruritus
Benzonatate MOA
anesthetizes the stretch receptors of vagal afferent fibers in the lungs, reducing the urge to cough after deep inhalation
Benzonatate interactions
can be additive to other local anestetics
Benzonatate indications
mostly for relief of chronic cough
sometimes used for acute cough
Benzonatate adverse reactions
well tolerated - GI upset, local anesthesia from chewing
overdose - cardiac arrhythmia, seizure, bronchospasm
Benzonatate contraindications
avoid in allergy to ester anesthetics
Guaifenesin (expectorant) MOA
Loosens secretions to allow for more productive cough
increases volume and reduces viscosity of phlegm in trachea/ bronchi - cilia can then more easily propel/ mobilize secretions upwards
Guaifenesin indications
Treatment of acute cough
Guaifenesin contraindications
should not be used for chronic cough
avoid in pediatrics - can lead to seizures
Guaifenesin adverse reactions
excessive can result in nephrolithiasis
Histamine MOA
Produced by mast cells and basophils
Released by an immunologic trigger or following a mechanical or chemical stimulus
Histamine 4 different receptors
H1 - smooth muscle cells, endothelium and brain
H2 - gastric mucosa mast cells, immune cells and brain
Histamine general effects
local vasodilation
transudation of fluid through endothelial cells
stimulates nerve endings, producing pain and itching
Histamine organ specific effects
lung - bronchoconstriction
GI tract - contraction of smooth muscle, potent secretagogue for gastric acid secretion, pepsin, and intrinsic factor
brain - neurotransmitter
Antihistamines first generation includes
Diphenhydramine and hydroxyzine
Avoid first generation antihistamines in
elderly; may cause delirium, dizziness, urinary retention
first generation antihistamines act ______ and are ______
quick
sedating
Hydroxyzine can be used as an
anxiolytic agent
Second generation antihistamines include
Cetirizine, loratadine, fexofenadine
Second generation are _____ hour _____ formulation
24hr
non-drowsy
Second generation antihistamine - certrizine
crosses the BBB a little
little drowsiness but better for itching, hives
Decongestants include
pseudoephedrine
phenylephrine
Pseudoephedrine MOA
decongestant - a and b2 adrenergic receptor agonist - reduces tissue hyperemia and edema
reduces nasal congestion and opens blocked eustachian tubes
pseudoephedrine indications
acute nasal congestion, sinusitis, otitis media
pseudoephedrine adverse reactions
increases HR and contractility
pseudoephedrine contraindications
pts with heart disease, severe HTN, uncontrolled DM
Phenylephrine MOA
binds primarily to a1 receptors causing vasoconstriction - used as a nasal decongestant
Phenylephrine is ______ effective than ___________ for treatment of rhinitis sx
less
pseudoephedrine
Phenylephrine adverse reactions
increases systolic and diastolic pressure - reflex bradycardia
ACE inhibitors can increase clearance of _______ making less effective
Phenylephrine
Topical decongestants include
Oxymetazoline
Fluticasone
Oxymetazoline indications
treating acute rhinitis (from the common cold)
Long duration of Oxymetazoline can lead to
rebound congestion
Fluticasone MOA
glucocorticoid receptor agonist - causes vasoconstriction and inhibitory effects of cells and mediators of inflammation
(mometasone and budesonide also)
Fluticasone indications
treatment and prevention of allergic rhinitis, treatment of chronic nasal polyps
Fluticasone is not indicated for
treatment of acute upper respiratory infections
Inhaled antihistamines include
azelastine and olopatadine
Inhaled antihistamines indications
allergic rhinitis in adults and children
Inhaled antihistamines side effects
nosebleeds, HA, somnolence, poor taste