Lecture 4: Asthma and COPD Drugs Flashcards
Which 3 major drug classes are used as bronchodilators in the tx of asthma and COPD?
- β2-agonists
- Anti-cholinergic
- Methylxanthines
2 most common AE’s assocaited with β2-agonists?
Muscle tremor and palpitations
What is the only β2 drug available for SQ injection?
Who is it not recommended for?
Terbutaline
not for ppl w/ sulfur allergy
What are the indications for use of Terbutaline?
Tx or prophylaxis of bronchospasm assoc. with asthma, bronchitis and emphysema in pt’s >12 y/o
What is the black-box warning for Terbutaline?
Not recommended as a medication for tocolysis
Which β2-agonist for asthma is not recommended for pt’s with sulfa allergies?
Terbutaline
What are some of the more serious maternal AE’s associated with Terbutaline?
- Cardiac or cardiopulmonary arrhythmias
- Pulmonary edema
- MI
- Hypotension
- Tachycardia
Albuterol may have interactions with what 5 other drug classes?
- β-blockers (duh)
- Digoxin
- Diuretics
- MAO inhibitors
- Tricyclic antidepressants
Which life-threatening AE can occur after tx w/ Albuterol?
Paradoxical bronchospasm
What are 2 indications for the use of the β2-agonist Metaproterenol?
- Bronchodilator for bronchial asthma
- Reversible bronchospasm which may occur in assoc. w/ bronchitis and COPD
Which drug class should not be used concomitantly with Metaproterenol?
Beta-adrenergic aerosol bronchodilators due to additive effects
What are 2 cautions/warnings associated with the use of Metaproterenol?
- Can produce significant cardiovascular effect in some pt’s, as measured by pulse, BP, sx’s and/or ECG changes
- Can produce paradoxical bronchospasm (can be life threatening)
Which β2-agonist may be used with or without concurrent theophylline and/or corticosteroid therapy?
Pirbuterol
What are the indications for the use of the β2-agonist, Levalbuterol?
Tx or prevention of bronchospasm in pt’s > 4 y/o with reversible obstructive airway disease
What are the 4 long-acting β2-agonists?
- Fomoterol
- Salmeterol
- Indacaterol
- Olodaterol
What are the 3 indications for use of the LABA, Fomoterol?
- Add-on for tx of asthma in pt’s ≥5 y/o in combo w/ long-term asthma control med such as an inhaled corticosteroid
- Prevention of exercise-induced bronchospasm (EIB) in pt’s ≥5 y/o
- Maintenance tx of bronchoconstriction in pt’s with COPD
What are cautions/warnings for the use of LABA’s in asthma and COPD?
- ↑ risk of asthma-related death and asthma-related hospitlizations
- MUST be used concomitantly with an inhaled corticosteroid for asthma (fomoterol and salmeterol)
What is the indication for the use of the LABA, Indacaterol?
Used to tx breathing problems caused by COPD, including chronic bronchitis and emphysema
What are the 3 indications for use of the LABA, Salmeterol?
- Add-on for tx of asthma in pt’s ≥4 y/o in combo w/ long-term asthma control med such as an inhaled corticosteroid
- Prevention of exercise-induced bronchospasm (EIB) in pt’s ≥4 y/o
- Maintenance tx of bronchoconstriction in pt’s with COPD
What are the most common AE’s of the LABA, Indacaterol?
- Cough + oropharyngeal pain + nasopharyngitis
- HA and nausea
What is the indication for use of the LABA, Olodaterol?
Used as LONG-term, 1x/daily maintenance bronchodilator in pt’s with COPD, including chronic bronchitis and emphysema
Which anticholinergic drug is indicated for use as a bronchodilator for maintenance tx of bronchospasm associated with COPD, including chronic bronchitis and emphysema?
Ipratropium
Which anticholinergic drug is indicated for long-term, 1x/daily, maintenance tx of bronchospasm associated with COPD, and for reducing COPD exacerbations?
Tiotropium
Caution should be used when co-administering tiotropium or ipratropium with what drug classes, due to additive interactions?
Anticholinergic-containing drugs
What is the indication for use of the anticholinergic drug, Aclidinium?
LONG-term, maintenance tx of bronchospasm associated with COPD, including chronic bronchitis and emphysema
What are 3 major AE’s associated with the anticholingeric, Aclidinium?
- Paradoxical bronchospasm
- Worsening of narrow-angle glaucoma
- Worsening of urinary retention
What is a caution/warning related to the use of the anticholingeric, Aclidinium for COPD?
NOT for acute use or initial tx of bronchospasm
What are the Methylxanthines, Theophylline and Dyphylline used for?
Tx of airways obstruction caused by conditions such as asthma, chronic bronchitis, or emphysema
What are the 2 distinct actions of Theophylline in the airways of pt’s w/ reversible obstruction?
- Smooth m. relaxation (bronchodilation)
- Suppression of airways response to stimuli (non-bronchodilator prophylactic effects)
What are some of the AE’s associated with Theophylline?
- CNS excitation + irritability + insomnia + restlessness + seizure
- HA + diarrhea + N/V + urinary retention
Theophylline should be used with extreme caution in pt’s with what 3 underlying clinical conditions?
- Active peptic ulcer disease
- Seizure disorders
- Cardiac arrhythmias (NOT including bradyarrhythmias)
What is given as the first-line therapy for persistent asthma; if sx’s are not controlled at low doses you may add what?
Inhaled corticosteroids (ICS); can add LABA as next step
What are the 2 indications for the use of the ICS, Beclomethasone?
- Maintenance tx and prophylactic for asthma in pt’s ≥5 y/o
- Tx of asthma in pt’s who require ORAL corticosteroid therapy to reduce or eliminate the need for systemic corticosteroids
Which 2 ICS’s require special care if used in pt’s who are transferred from systemically active drugs to less systemically active drugs due to potential for death by adrenal insufficiency?
- Beclomethasone
- Triamcinolone
What is the indication for use of the ICS, Budesonide?
Maintenance or prophylactic tx of asthma in adults and pediatric pt’s ≥ 6 y/o
Which CYP is responsible for the metabolism of corticosteroid?
CYP3A4
Which pt’s should the ICS, Budesonide not be used in?
- For primarytx ofstatus asthmaticusor otheracute episodesofasthmanecessitatingintensive measures
- Pts with severe hypersenitivity to milk proteins
What is the indication for use of the ICS, Ciclesonide?
Maintenance or prophylactic tx of asthma in adult and adolescents ≥12 y/o
When is the ICS, Ciclesonide not indicated for use and should be avoided in the presence of what infection?
- Not indicated for the relief of acute bronchospasm
- Not recommended in presence of Candida albicans infection of the mouth and pharynx, tuberculosis, fungal, bacterial, or parasitic infections
What are the 2 indication for use of the ICS, Flunisolide?
- Maintenance and prophylactic tx of asthma in adults and pt’s ≥6 y/o
- Asthma pt’s requiring oral corticosteroid therapy, where adding flunisolide may ↓ or eliminate the need for other oral corticosteroids
Use of the ICS, Flunisolide is contraindicated for use in which pt’s?
Primary tx of status asthmaticus or other acute episodes of asthma where intensive measures are required
The use of strong CYP3A4 inhibitors (i.e., ritonavir, ketoconazole) should not be used in conjuction with what ICS?
Fluticasone
Which ICS for asthma is associated with potential Candida infection of the mouth and required pt to rinse his/her mouth with water after inhaling the drug?
Fluticasone
Which 2 ICS used for asthma are contraindicated in pt’s with status asthmaticus or other acute episodes of asthma where intensive measures are required + pt’s with a known hypersensitivity to milk proteins?
- Budesonide
- Mometasone
What are the 2 indications for the use of the ICS, Triamcinolone?
- Maintenance and prophylactic tx of asthma
- Asthmatic pt’s who require systemic corticosteroid administration, where adding this agent may reduce or eliminate the need for the systemic corticosteroid
Which ICS has AE’s including oral candidiasis, dysmenorrhea, MSK/back pain, and dyspepsia?
Mometasone
Which ICS has AE’s including oral monilia, toothace, weight gain, bursitis, myalgia, rash, and voice alteration?
Triamcinolone
Which antimuscarinic used in asthma/COPD provides temporary blockade of the receptor?
Atropine
What are the 3 combos of ICS + LABA available as inhalers?
- Fluticasone + Salmeterol
- Mometasone + Formoterol
- Budesonide + Formoterol
When are oral corticosteroids used for asthma and in conjunction with what other drug class?
With short-acting β-agonists for moderate-severe asthma flare-ups
What is the oral corticosteroid which may be used for moderate to severe asthma flare ups in combo with a short acting beta-agonist?
Prednisone
What are 6 of the common AE’s associated with Prednisone?
- Fluid retention
- Alteration in glucose tolerance
- ↑ in BP
- Behavioral and mood changes
- ↑ appetite —> weight gain
What should patients of Prednisone be monitored for?
- Cushing’s syndrome due to HPA-axis suppression
- Hyperglycemia w/ chronic use (doses must be tapered gradually)
What are the 3 leukotriene antagonists used for asthma?
- Montelukast
- Zafirlukast
- Zileuton
What is the MOA of Montelukast?
Binds w/ high affinity and selectivity to the CysLT1 receptor; INHIBITING the physiologic actions of LTD4
Montelukast is primarily prescribed for what?
Treat allergies and prevent asthma attacks
Which leukotriene receptor antagonist used for asthma is associated with hepatotoxicity as an AE?
Zafirlukast
What is Zafirlukast prescribed for?
Prophylaxis and chronic tx of asthma in pts ≥5 y/o
Patients on which other drug need to be monitored clinically if taking Zafirlukast for asthma?
Warfarin –> need to monitor PTT
What is the MOA of Zileuton?
Inhibitor of 5-lipoxygenase and thus inhibits leukotriene (LTB4, LTC4, LTD4, and LTE4) formation
3 most common AE’s associated with Zileuton?
- Sinusitis
- Nausea
- Pharyngolaryngeal pain
What is the indication for the use of Zileuton?
Prophylaxis and chronic tx of asthma in pt’s ≥12 y/o
Zileuton is not indicated for use in pt’s with what underlying disease/abnormalities?
- Active liver disease
or
- Persistent hepatic function enzymes ≥3x upper limit of normal
What are the 2 indications for the use of Omalizumab?
- Moderate to severe persistent asthma in pt’s ≥6 y/o w/ (+) skin test for perennial aeroallergen and sx’s inadequately controlled w/ ICS
- Chronic idiopathic urticaria in pt’s ≥12 y/o who remain symptomatic despite H1 antihistamine tx
What is the MOA of Omalizumab?
- Binds to free IgE and blocks binding to FCεRI
- Causes ↓ release of mediators from mast cells, basophils, and eosinophils
What is a black box warning for Omalizumab?
Administer only in a healthcare setting prepared to manage anaphylaxis that can be life threatening
What are some of the most common AE’s associated with Omalizumab?
- Arthraliga + pain (general) + fracture
- Pruritus + dermatitis
- Earache
- Fatigue + dizziness
Which pt’s may benefit from triple therapy with ICS + LABA + LAMA?
Pt’s w/ features of both asthma + COPD
