RHS06 - Respiratory Pharmacology Flashcards
List the classes and subclasses of drugs used in management of asthma.
- Bronchodilators
- ß2 agonists
- Anticholinergics
- Methylxanthines
- Anti-inflammatory Drugs
- Corticosteroids
- Release Inhibitors
- Immunomodulators
- Leukotriene-modifying agents
List the inhaled ß2 agonists we need to know
- Inhaled short-acting ß2 Agonists (SABAs) - albuterol, terbutaline, pirbuterol
- Inhaled long-acting ß2 agonists (LABAs) - salmeterol and formoterol
What is the MOA for inhaled ß2 agonists?
Activation of the typical adenylyl cyclase pathway with PKA phosphorylating and inactivating myosin light chain kinase, leading to muscle relaxation and bronchodilation
What is the DOC for relief of acute asthma symptoms?
SABAs
What is the DOC for prevention of exercise induced bronchospasm?
SABAs
What are the uses for LABAs?
LABAs are typically combined with inhaled corticosteroids (ICS) for long-term control in moderate and severe persistent asthma.
They should not used as monotherapy for long-term control since they have no anti-inflammatory action. They are not used in the treatment of acute symptoms
What are the AEs of SABAs and LABAs?
- Mild tachycardia, tremor, and hypokalemia
- LABAs can increase risk of serious asthma-related events (hospitalization, intubation, and death)
List the anticholinergics used to treat asthma that we need to know
- Inhaled short acting muscarinic antagonists (SAMAs)
- Ipratropium
- Inhaled long acting muscarinic antagonists (LAMAs)
- Tiotropium
What are the uses of SAMAs and LAMAs?
They are less effective than SABAs and LABAs so they are really only used when SABAs or LABAs cannot be used or in conjuction with SABAs and LABAs to provide an added benefit. They may also be safer to use in patients with CV disease
- Ipratropium is the DOC for ß-blocker induced bronchospasm
- Tiotropium is sometimes added to ICS for long-term control of severe persistent asthma
What are the AEs for SAMAs and LAMAs?
- Since these drugs are quaternary ammoniums, they have almost no systemic side effects
- Minor xerostomia may occur
List the methylxanthines we need to know, their MOAs, uses, and AEs.
Theophylline
- MOA - increases [cAMP] by inhibiting phosphodiesterase
- Uses - alternative therapy for patients with persistent asthma
- AEs - headache, nausea, vomiting, abdominal discomfort, restlessness, and, at high concentrations, cardiac arrhythmias and seizures
List the steroids used for treating asthma that we need to know.
- ICS - beclomethasone, budesonide, flunisolide, fluticasone
- System Corticosteroids - prednisolone and dexamethasone
What is the MOA of corticosteroids?
- Inhibit PLA2 activity and inhibit txn of COX-2, resulting in reduced formation of leukotrienes and prostaglandins
- They also somehow prevent/reverse ß2 receptor desensitization
What are the asthma related uses for corticosteroids?
- ICS - DOC for long-term control of persistent asthma
- Oral prednisolone may be added to ICS
- Sometimes, for moderate to severe acute asthma attacks, a short course of systemic corticosteroids is given to speed recovery and prevent recurrence.
What are the AEs for ICSs and systemic corticosteroids?
- ICSs really only have local AEs like oropharyngeal candidiasis (fungal infection), dysphonia (difficulty speaking), reflex cough, and bronchospasm. Long term use may cause osteoporosis and cataracts.
- Long term use of systemic corticosteroids may cause hypercortisolism and Cushing’s syndrome.
List the anti-inflammatory release inhibitors used to treat asthma. What is their MOA?
- Cromolyn and Nedocromil
- Act by inhibiting mast cell degranulation
What are the uses of cromolyn and nedocromil?
- Only used as alternative medications for patients with mild persistent asthma
- Also used to prevent antigen and exercise induced bronchospasm
What are the AEs of cromolyn and nedecromil?
- Throat irritation
- Cough
- Mouth dryness
- Rarely, chest tightness and wheezing
List the immunomodulators used to treat asthma and give their MOAs. What are their uses and AEs?
Omalizumab
- MOA - omalizumab is a monoclonal antibody that binds IgE, preventing it from binding to mast cells. This prevents the mast cells from degranulating
- Uses - management of severe persistent asthma in patients with evidence of allergy
- AE - may cause anaphylaxis
List the leukotriene modifying agents (LTMAs) used to treat asthma and give their MOAs.
Montelukast and Zafirlukast
- MOA - leukotriene receptor antagonist (LTRAs)
Zileuton
- MOA - 5-lipoxygenase inhibitor
What are the uses and AEs of LTMAs?
- Alternative therapy
- Prevention of exercise induced bronchospasm
- Management of NSAID-exacerbated respiratory disease (NERD)
- AEs
- Montelukast can cause insomnia, anxiety, depression, and suicidal thoughts
- Zileuton can cause hepatotoxicity
List the asthma severity classifications
Write out the asthma management guidelines table.
List the drugs used in the management of COPD. What are their MOAs?
- Bronchodilators
- ß2 agonists - same ones for asthma
- Anticholinergics - same ones for asthma
- Corticosteroids - same ones for asthma
- Mucolytic agents - N-acetylcysteine (breaks disulfide linkages in mucus and lowers viscosity)
List the drugs used in treatment of allergic rhinitis. Which ones are first-line drugs?
- Glucocorticoid nasal sprays - FIRST LINE
- Oral antihistamines
- First Generation - diphenhydramine (benadryl), and chlorpheniramine
- Second Generation - loratadine, fexofenadine, cetirizine
- Cromolyn sodium
- Montelukast
- Nasal decongestants (α agonists) - pheylephrine and pseudoephedrine
What are the AEs of the glucocorticoid nasal sprays?
- Local irritation of mucosa
- Nosebleed
- Nasal septal perforation
- Nasopharyngeal candidiasis
List the major differences between firs and second generation antihistamines. Which generation is preferred for treating allergic rhinitis.
What are the MOAs and AEs of the nasal decongestants?
They’re α agonists which cause vasoconstriction, leading to decongestions
If they’re used for longer than 3 days, rebound nasal congestion can occur
What are the drugs used to treat cough. What are their MOAs and AEs?
Codeine and Dextromethorphan
- Suppress cough reflex via a direct action on the cough center in the medulla
- AEs are constipation
- Codeine will also cause drowsiness
- Codeine has a fairly high abuse potential so dextromethorphan is preferred.