Week 12 Notes Flashcards
What do Beta 2 Receptor Agonists bind to in the airway?
Beta-2 smooth muscle cells
They stimulate relaxation causing bronchodilation.
What is the action of Beta 2 Receptor Agonists?
Stimulate smooth muscle cell relaxation causing bronchodilation via cyclic AMP pathway and inhibit release of hypersensitivity mediators
Especially from mast cells.
What are the pharmacokinetics of Beta 2 Receptor Agonists?
Absorbed in bronchi, metabolized in liver, excreted in urine
What are common side effects of Beta 2 Receptor Agonists?
Tachycardia, tremors
What precautions should be taken when using Beta 2 Receptor Agonists?
Patients with arrhythmias, cardiovascular disease, hyperthyroidism
What is the duration of action for Short Acting Beta Agonists (SABA)?
4-6 hours
Name three Short Acting Beta Agonists (SABA).
- Albuterol
- Levalbuterol
- Pirbuterol
What is the duration of action for Long Acting Beta Agonists (LABA)?
12 hours
Name two Long Acting Beta Agonists (LABA).
- Salmeterol
- Fomoterol
What is the duration of action for Ultra Long Acting Beta Agonists (ULABA)?
24 hours
Name two Ultra Long Acting Beta Agonists (ULABA).
- Indacaterol
- Olodaterol
What is the black box warning associated with LABAs and ULABAs?
Only indicated for use in combination with an inhaled corticosteroid; never should be used alone.
What do inhaled anticholinergics block?
Muscarinic cholinergic receptors by antagonizing acetylcholine
What is the action of inhaled anticholinergics?
Decreases formation of cyclic GMP causing decreased contractility of smooth muscle in the lungs
What are the pharmacokinetics of inhaled anticholinergics?
Poorly absorbed from lungs and GI tract; 90% swallowed and excreted in feces
What are common side effects of inhaled anticholinergics?
Dry mouth, cough, headache
What precautions should be taken when using inhaled anticholinergics?
Avoid in patients with urinary retention or BPH and closed-angle glaucoma
What is the duration of action for Short Acting Muscarinic Antagonists (SAMS)?
4-6 hours
Give an example of a Short Acting Muscarinic Antagonist (SAMS).
Ipratropium bromide (Atrovent)
What is the duration of action for Long Acting Muscarinic Antagonists (LAMA)?
12 to 24 hours
Name one Long Acting Muscarinic Antagonist (LAMA).
Tiotropium bromide (Spiriva Handihaler)
What are the pharmacokinetics of methylxanthines like theophylline?
Absorbed very well orally, metabolized in liver
What are common side effects of theophylline?
Headache, irritability, gastric irritation, nausea/vomiting
What must be monitored when using theophylline?
Serum drug levels to prevent toxicity
What is the action of inhaled corticosteroids?
Decrease inflammatory response by inhibiting IgE and mast cell mediated migration of inflammatory cells into bronchial mucosa
What are common side effects of inhaled corticosteroids?
Xerostomia, hoarseness, mouth irritation, dysgeusia, oral candidiasis
What precautions should be taken with inhaled corticosteroids?
HPA suppression, high-dose ICS in children may inhibit growth
Name a contraindication for the use of inhaled corticosteroids.
Status asthmaticus
What are leukotriene modifiers used for?
To address inflammatory mediators produced by eosinophils and mast cells
What is the action of leukotriene receptor agonists like Montelukast?
Inhibits the cysteinyl leukotriene receptor blocking action of LTD4
What is Zileuton’s mechanism of action?
Inhibits 5-lipoxygenase, the enzyme responsible for leukotriene formation
What are common side effects of Montelukast?
Headache, sore throat
What precautions should be taken with leukotriene modifiers?
Associated with neuropsychiatric events; avoid in patients with severe liver disease
What is a contraindication for 5-lipoxygenase pathway inhibitors?
Active liver disease