SM 180 Pulmonary Pharmacology Flashcards
Are LABA’s first line for Asthma?
No, LABA’s are second line for Asthma
Which is better, LABA/LAMA or LABA/ICS?
LABA/LAMA works better than LABA/ICS
How do spacers work?
They decrease the velocity of discharged particles and allow the aerosol to expand in the spacer itself, improving delivery to the lung
When are LABA’s used for Asthma?
LABA’s are used for Asthma only if a patient’s symptoms persist despite an ICS
What are LABA’s first line for?
Salmetrol and Formeterol are first line for COPD
What do Beta2 mediate?
Bronchodilation via relaxation of smooth muscle
What are the three pathophysiologic hallmarks of COPD?
Fibrosis of the small airways (bronchiolitis), alveolar wall destruction (emphysema), and mucus hypersecretion
What class of drug is Tiotropium?
LAMA
What is the most common PDE-4 inhibitor?
Rofluminast is the most common PDE-4 inhibitor and is used to reduce exacerbations in patients with class D COPD
When are Leukotriene Antagonists not used?
Montelukast is not used for COPD
What cells underlie the inflammation in COPD?
Mast cells, eosinophils, T-lymphocytes, macrophages, and neutrophils
List the SABA’s?
Albuterol and Levalbuterol
How does smoking cessation alter lung function?
Smoking cessation slows the decline in FEV1 associated with age, regardless of when a person stops, and improves life expectancy/disability
How do ICS levels change in Asthma treatment?
ICS doses increase with progressively worse Asthma
What is a rescue inhaler?
SABA
What are Leukotriene Antagonists?
Leukotriene antagonists like Montelukast block the effects of Leukotrienes and are used for Allergies and Asthma, but not COPD
What are PDE-4 inhibitors indicated for?
Late stage COPD, chronic bronchitis, and as an addon to Triple Therapy in COPD
What are Leukotriene Antagonists indicated for?
Leukotriene antagonists like Montelukast are indicated for Allergies and Asthma, not COPD
What is the first line for treatment of patients with COPD?
LABA’s like Salmeterol and Formeterol (or LAMA’s)
What are the effects of corticosteroids on the respiratory system itself?
Less inflammatory cells in the airway, limit mucus hypersecretion, and decrease capillary leak
Are Muscarinic Receptor Antagonists reversible or irreversible?
SAMA and LAMA are reversible and lead to bronchodilation
List the LABA’s?
Salmeterol and Formoterol
What class of drug is Levalbuterol?
SABA
What class of drug is Ipratropium?
SAMA
What are LABAs?
Long Acting Beta2 Agonists that can last up to 24 hours
Where are b1R found?
The heart, where they increase CO and Renin release
What is the first line treatment for COPD?
LAMAs
What is the major perk of Montelukast?
Minimal drug-drug interactions and favorable side effect profile
Which trial indicates why LABA’s are not first line for Asthma and why?
The SMART trial found that patients who took LABA’s had an increased risk for respiratory related deaths, but that there was no increased risk in LABA+ICS or ICS therapy
What are SAMA’s?
Short Acting Muscarinic Antagonists like Ipratropium
What is the effect of a PDE-4 inhibitor?
Blocks PDE and leads to increases in cAMP, resulting in relaxation of smooth muscle
What are LAMA’s?
Long Acting Muscarinic Antagonists
How do LABAs compare in their utility for COPD and Asthma?
LABA are first line in COPD and added to ICS as a second line in Asthma
Where are b3R found?
Adipose tissue, where they increase lipolysis
If LABA’s increase respiratory risk in Asthma, why are they second line agents?
No increase in risk for LABA’s if taken with ICS, never use LABA monotherapy
What is the first line treatment for Asthma?
Inhaled Corticosteroids
What class of COPD requires a PDE-4 inhibitor?
PDE-4 inhibitors like Rofluminast are indicated in Class D COPD that does not respond to triple therapy
What are spacers?
A form of non-pharmacologic pharmacologic that improves inhaled drug delivery
What is the common adverse effect of ICS?
ICS suppress the immune system and predispose Thrush and Pneumonia
Are LAMAs the first line treatment for COPD?
Yes
What does Zileaton inhibit?
5 Lipoxygenase, but rarely used due to hepatic dysfunction as a side effect
How do b2 agonists work?
They bind the b2 GPCR and increase generation of cAMP and PKA, leading to opening of K channels and bronchodilation
What class of drug is Salmeterol?
LABA
Where is the M3 muscarininc receptor found?
The M3R is found in the respiratory system, making it a good target for SAMA’s and LAMA’s
What are SABAs?
Short Acting Beta2 Agonists
How do ICS compare in their utility for COPD and Asthma?
ICS are last line in COPD and first line in Asthma
What class of drug is Formoterol?
LABA
How do ICS work?
Inhaled corticosteroids bind the cytoplasmic corticoid receptor and translocate to the nucleus, where they increase transcription of anti-inflammatory genes and decrease expression of inflammatory signals
What are common ICS?
Common inhaled corticosteroids include Budesonide, Mometasone, Fluticasone
What is non-pharmacologic pharmacotherapy?
Addressing barriers to treatment such as inhaler technique and adherence, as well as smoking cessation
How are ICS used in COPD?
ICS are only used as a triple therapy if the LABA/LAMA combination does not work
What is Theophylline?
Theophylline is a nonselective PDE inhibitor with narrow therapeutic windows and risk for fatal arrhythmias and seizures
What should always be done when providing a new inhaler?
Watch the patient demonstrate how to use it so you can verify it works correctly
What ionic derangement can b2 agonists treat?
Because b2 agonists can cause hypokalemia, they can be used to treat hyperkalemia
Which should be used as a first line treatment for COPD?
LAMAs are generally used first, and then LABAs are added on as a second line
What are SABAs used for?
Symptomatic control of immediate symptoms
What receptor do SAMA’s and LAMA’s target?
The M3 Muscarinic receptor, leading to vasodilation
When should LAMAs and LABAs not be prescribed?
If they are already on an anti-cholinergic, since muscarinic receptor antagonists have anti-cholinergic effects
What does the M3R normally bind?
The M3R is a Muscarinic Receptor that binds Acetylcholine
What suffix do Beta agonsists end with?
-erol = Beta Agonist
What is the normal effect of ACh binding to M3R?
ACh binding to M3R leads to Ca influx and bronchoconstriction
What kind of side effects can b2 agonists cause?
Tremors, tachycardia, palpitations, and hypokalemia
What does Montelukast inhibit?
Montelukast inhibits the Cysteinyl Leukotriene-1 Receptor
What are the major side effects of PDE-4 inhibitors?
GI side effects
When are Leukotriene Antagonsts used in the treatment of Asthma?
Montelukast is added onto low dose ICS as a second in Asthma
What characteristics of SABAs allow for their effectiveness in immediate symptom relief?
SABAs are delivered via inhaled aerosol to maximize delivery to the lungs while minimizing systemic delivery and potential side effects
What are a potential adverse effect of Muscarinic Receptor Antagonist?
Unilateral dilated pupils which can be mistaken for a stroke, due to anti-cholinergic effects
When can LABA’s not be a monotherapy?
LABA’s cannot be a monotherapy in the treatment of Asthma, and must be used as a second line agent with ICS
What type of protein are Beta receptors?
GPCR’s which regulate cAMP levels
What does the -tropium suffix indicate?
Muscarinic Receptor Antagonist
What does the Beta Blockade refer to?
Beta Blockade refers to unintentional crossover and inhibition of different Beta-acting drugs; smokers need b1 antagonists for HF but also need b2 agonists for COPD, so concern for crosstalk
Which type of BetaR mediates bronchodilation?
Beta2 Receptors
What constitutes the Anticholinergic Toxidrome?
BMDRH
Blind as a Bat Mad as a Hatter Dry as a Bone Red as a Beat Hot as a Dessert
What class of drug is Albuterol?
SABA
Why do b2 agonists cause side effects?
Binding of a b2 agonist in the systemic circulation can lead to side effects
Does COPD benefit from bronchodilators?
Although COPD is traditionally characterized as “fixed”, patients do get some benefit from bronchodilators
How long do SABAs take to act and how long do they last?
SABA’s take 5-15 minutes to take action and last 4-6 hours
How do Leukotriene Antagonists work?
They prevent the breakdown of Arachidonic acid
How does COPD present?
Wheezing, breathlessness, chest tightness, and coughing
What are LABAs used for?
Long term control of COPD and Asthma on a day to day basis
How do LAMAs compare in their utility for COPD and Asthma?
LAMAs are first line in COPD and added to LABA/ICS in Asthma
Are beta blockers safe in COPD?
Yes; normally, we treat COPD with b2 agonists, but a b1 antagonist used to treat smoking simultaneously does not worsen COPD surprisingly
What causes symptoms in COPD?
Inflammation
Are LAMA’s used in Asthma?
Generally no, and only as a last line salvage therapy in Asthma after ICS and LABA with persistent symptoms
