Pharmaology - Asthma Flashcards
Class: Albuterol
short-acting beta-2 agonist (4-6 hours)
bronchodilator
inhaled
Class: Terbutaline
short-acting beta-2 agonist (4-6 hours)
bronchodilator
inhaled, can also be subQ
Class: Metoproterenol
short-acting beta-2 agonist (4-6 hours)
bronchodilator
Class: Pirbutol
short-acting beta-2 agonist (4-6 hours)
bronchodilator
What is a major effect of beta 2 agonists?
Reduction in cholinergic transmission
***increase in intracellular cAMP –> bronchodilation
Use: Albuterol Metoproterenol Pirbutol Terbutaline
Acute exacerbations;
Exercise-induced or mild asthma
Class: Salmeterol
bronchodilator
long-acting beta-2 agonist (partial agonist)
Class: Formoterol
bronchodilator
long-acting beta-2 agonist (full agonist)
Class: Indicaterol/Vilanterol
bronchodilator
long-acting beta-2 agonist
What long-acting beta-2 agonists are only indicated for use in COPD?
Indicaterol
Vilanterol
Long-acting beta-2 agonists are always used in combination with what in the treatment of asthma?
Corticosteroids
T/F: Beta-2 agonists are less effective in treating COPD
True
Side effects: Beta-2 agonists
Tremor (beta-2 receptors in muscles);
Tachycardia;
Prolongation of QTc - dose dependent –> can lead to fatal v-tach;
Hypokalemia;
V/Q mismatch –> hypoxia;
tolerance with chronic use (short-acting);
overuse associated with respiratory mornidity (long-acting)
Class: Ipratroprium
Antimuscarinic - bronchodilator
Class: Tiotroprium
Antimuscarinic - bronchodilator
**longest half life at M3 receptor
Class: Atropine
Antimuscarinic - bronchodilator
**most systemic side effects
Class: Acidlinium
Antimuscarinic - bronchodilator
newer formulation of tiotroprium, shorter *circulation half-life
less side effects (systemic, CNS)
What antimuscarinic is long-acting for use in COPD?
Tiotroprium
What antimuscarinic is short-acting for use in COPD?
Ipratroprium
What is a secondary effect of tiotroprium as an antimuscarinic in the treatment of COPD?
Anti-inflammatory effects - reduces neutrophil migration;
reduces airway remodeling;
decreased mucus production
Side effects: Antimuscarinic agents (COPD)
urinary retention;
acute angle glaucoma;
dry mouth
T/F: Better M3 selectivity confers better side effect profile in antimuscarinic agents (ie triotroprium) used for COPD.
True
Why are methylxanthines used in the treatment of COPD if they are only weak bronchodilators?
They reverse diaphragmatic fatigue and have anti-inflammatory effects, restores sensitivity to corticosteroids
Examples: Theophylline, Theobromine, Caffeine, Roflumilast
**narrow therapeutic window - not really used anymore, as well as MULTIPLE drug interactions bc of cytochrome P450
Roflumilast is unique among the methylxanthines (treatment of COPD) in that:
It produces the most anti-inflammatory effect;
Selective PDE4 inhibitor
Corticosteroids increase the responsiveness of the lungs to beta-2 agonists.
True
Class: Budesonide
Inhaled corticosteroid
Class: Fluticasone
Inhaled corticosteroid
Class: Beclamethasone
Inhaled corticosteroid
Oral thrush is a side effect of what drugs?
Inhaled corticosteroids
ie Budesonide
Fluticasone
Beclamethasone
What is the first-line therapy for persistent asthma?
Inhaled corticosteroids
ie Budesonide
Fluticasone
Beclamethasone
use before adding in long-acting beta-2 agonists
How is Ciclesonide different from other inhaled corticosteroids such as fluticasone?
Ciclesonide is a prodrug that is only activated in the airway by an esterase, which results in less systemic absorption and side effects
Class: Ciclesonide
Inhaled corticosteroid
Prodrug**
Class: Omalizumab
IgE inhibitor
mAB
Use: Omalizumab
Asthma patients who are refractory to other medications ie corticosteroids
