Asthma/COPD Review Flashcards
What are the class of drugs useful for asthma that are considered bronchodilators?
Sympathomimetics, especially β2-selective agonists, muscarinic antagonists, methylxanthines, and leukotriene receptor blockers.
What are the drugs useful in the treatment of asthma that are considered anti-inflammatory classes drugs?
include corticosteroids, mast cell stabilizers, and an anti-IgE antibody.
Do leukotriene antagonists act as bronchodilators or as anti-inflammatory drugs?
they act as both
Is asthma considered a reversible condition or irreversible?
reversible
COPD is considere a reversible or irreversible condition?
irreversible
Out of bronchodilators or anti-inflammatory agents, which are considered relievers and which are considered controllers?
Anti-inflammatory agents are considered controllers
Bronchodilators are considered relievers
What is the purpose of using prophylactic therapy in the treatment of asthma? (How do they typically act?)
acts by preventing mast cell degranulation and prevents future attacks.
Bronchodilators are used in maintenance therapy and are needed to abort acute or long term attacks?
needed to abort acute attacks
Anti-inflammatory agents are called controllers as they provide long or short term stabilization of symptoms?
long term
Leukotriene antagonist, when used for the treatment of asthma and/or COPD have effects on bronchoconstriction and inflammation but are used only for long or short term treatment?
neither; prophylaxis
What is the general reasoning behind using bronchodilators in the treatment of asthma?
relax airway smooth muscles
What symptoms can bronchodilators not help that may affect the respiratory system?
mucosal edema
cellular infiltration
mucus formation
Name the B2 agonist drugs to treat asthma.
Classify SABA and LABA
SABA: albuterol, levalbuterol, terbutaline, metaproterenol
LABA: Salmeterol, formoterol
Name the sympathomimetic drugs used to treat asthma.
Classify as a, B agonists and selective B agonists
A, B agonists: epinephrine, ephedrine
B agonists: isoproterenol
Name the methylxanthines used to treat asthma.
Aminophylline, theophylline
Name the muscarinic antagonists used to treat asthma.
iptratropium, tiotropium
Which class of drugs, bronchodilators or anti-inflammatory drugs, are used to reduce bronchial responsiveness?
anti-inflammatory drugs
Which drugs are the prototype glucocorticoids used to treat asthma?
Beclomethasone
Budesonide
Dexamethasone
fluticasone
mometasone
What are the Leukotriene antagonist drugs used in the treatment of asthma?
montelukast
zafirlukast
zileuton
What are the anti-IgE antibodies used to treat asthma?
Omalizumab
What is the name of a interleukin-5 antagonist monoclonal antibody (IgG1 kappa) used to treat asthma?
Mepolizumab
What are drugs used to treat mast cell degranulation?
Cromolyn sodium
Nedocromil sodium
T/F. Cromolyn sodium and Nedocromil sodium are used for acute asthma attacks?
False
Used only for prophylaxis
Give an example of inhaled steroids and long-acting bronchodilators that are becoming more widespread-combination preparations and are used to treat asthma.
fluticasone/salmeterol (Advair) andbudesonide/formoterol (Symbicort)
Be able to explain and draw out this picture without looking.
Bronchodilation is promoted by cAMP which can be increased by:
β2-adrenergic agonists that increase its synthesis by adenylyl cyclase
Phosphodiesterase (PDE) inhibitors that slow its degradation
Bronchoconstriction can be inhibited by: muscarinic or adenosine antagonists
What class of drugs are considered the drugs of choice for acute asthmatic attacks?
B2-adrenergic agonists
Salmetorol and formoterol are longer acting drugs that can act over a period of how long?
12 hours
To prevent mortality of longer acting B2 adrenergic drugs what should they be used in combination with?
They should be used in combination with coritcosteroids
What are common adverse effects of B2 agonist drugs?
skeletal muscle tremor,
tachycardia
hypokalemia
nervousness
occasional weakness
T/F. Loss of responsiveness (tolerance, tachyphylaxis) is an unwanted effect of excessive use of the short-acting sympathomimetics
True
What is the benefit of using Levalbuterol over other B2- adrenergic receptor agonists?
Inhalant which is claimed to have fewer central nervous system (CNS) and cardiac adverse effects
What is the MOA of methylxanthines?
It produces bronchodilation by inhibiting the enzyme cyclic nucleotide phosphodiesterase. Increased levels of cAMP results, which explains the cardiac stimulation and smooth muscle relaxation produced by these drugs.
It blocks adenosine receptors. Adenosine acts as a local mediator contracting smooth muscles, so the blockage of receptors produces opposite response.
What is the benefit of using Pentoxifylline to treat asthma?
remedy for intermittent claudication
In asthma, what is the most important therapeutic action of Theophylline?
bronchodilation
What are some other effects of using therapeutic doses of theophylline?
Smooth muscle relaxation.
CNS excitation.
Cardiac stimulation.
What are some toxicities related to using Theophylline?
The common adverse effects of methylxanthines include gastrointestinal distress, tremor, and insomnia.
Severe nausea and vomiting, hypotension, cardiac arrhythmias, and seizures may result from overdosage.
Very large doses have been linked to suicide attempts
What is the benefit of using anticholinergics to treat asthma?
reverse vagally mediated bronchospasm.
Also decrease mucus gland hyper secretion seen in asthma
Why is Ipratropium bromide used instead of atropine to treat asthma?
is free of atropine side effects?
Which has a longer duration of action? Tiotropium or Ipratropium bromide? How long?
Tiotropium (24 hours)
When are systemic (oral)corticosteroids used?
used chronically only when other therapies are unsuccessful.
What are some local aerosol surface-active corticosteroid used in the treatment of asthma? (name the drugs)
(eg, beclomethasone, budesonide, dexamethasone, flunisolide, fluticasone, mometasone ) is relatively safe, and inhaled
When are corticosteroids first-line therapy in the treatment of asthma?
for individuals with moderate to severe asthma
What is the most important intravenous corticosteroid for treatment of status asthmaticus?
prednisolone and hydrocortisone
What is the MOA of corticosteroids?
Corticosteroids reduce the synthesis of arachidonic acid by phospholipase A2 and inhibit the expression of COX-2, the inducible form of cyclooxygenase.
Do corticosteroids relax smooth muscles directly? (explain)
no; act by inhibiting the production of inflammatory cytokines
T/F. Corticosteroids decrease responsiveness of adrenoceptors in the airway.
False; Increase responsiveness of adrenoreceptors
The effect of corticosteroids on airway obstruction is partly due to what factors?
potentiation of the effects of β-receptor agonists
T/F. Inhaled glucocorticoids are now considered appropriate (even for children) in most cases of moderate asthma that are not fully responsive to aerosol agonists.
True
It is believed that corticosteroids that are used early may prevent the severe, progressive inflammatory changes characteristic of what type of asthma?
long-standing asthma
What is the major toxicities associated with use of corticosteroids in treating asthma?
Inhaled preparations may cause oropharyngeal candidiasis or hoarseness from vocal cord irritation .
Cushingoid effects
What is a Leukotriene synthesis inhibitor?
Zileuton
What is a leukotriene receptor antagonists?
Zafirlukast
Montelukast.
MOA of Zafirlukast and Montelukast?
CysT1 receptor antagonist
What is the MOA of Zileuton?
5-LOX inhibitor
Which Leukotrienes are mainly targeted in the treatment of asthma?
LTC4 and LTD4
What asthmatic effects do LTC4 and LTD4 create?
mucosal edema, mucus hypersecretion, increased bronchial reactivity, and bronchoconstriction
MOA of Omalizumab.
Monoclonal antibody that inhibits binding of IgE to mast cells but does not inactivate already bound IgE
Lowers plasma IgE levels and reduces bronchospasm
Who is Omalizumab typically prescribed for?
Cost is high, hence omalizumab is mainly prescribed for patients with with moderate to severe persistent asthma who have a positive skin test or in vitro reactivity to a specific allergen and whose symptoms are inadequately controlled with inhaled corticosteroids.
MOA mast cell stabilizers? Clinical use?
These drugs are thought to act by inhibiting mast cell degranulation and, as such, have no direct bronchodilator action,
inhibit both antigen- and exercise-induced bronchospasm in asthmatic patients.
Clinical use of Ketotifen? ROA?
administered orally and is a prophylactic drug for allergic and bronchial disorders.
MOA of chromones?
mechanism not clearly known.
What was the most important use for cromolyn and nedocromil?
asthma (especially in children)
What routes of administration are cromolyn available in? What is it’s clinical use for typically?
oral formulation used
for food allergy and hay fever.
Are ADR of chromones common?
no; they are mild and rare
What is the treatment plan for patients with status asthmaticus?
Terbutaline
Hydrocortisone
Nebulized Albuterol/terbutaline and ipratropium bromide
antibiotics for chest infections
correct dehydration and acidosis
humidified oxygen
What are the treatment options used to treat acute symptoms of COPD?
inhalation of a short-acting β agonist (eg, albuterol) with or without anticholinergic drug (eg, ipratropium bromide).
What are the treatment options used to treat persistent symptoms of COPD?
regular use of an LABA or a long-acting anticholinergic, or the two together, is indicated.