exam 2 Flashcards
(241 cards)
1) B2 adrenergic agonists (sympathomimetics)
2) Antimuscarinics/Anticholinergics
Relax airway smooth muscle (bronchodilators)
asthma RELIEVERS
o 1) Glucocorticoids
o 2) Leukotriene Modifiers
o 3) Cromones
o 4) Biologic Therapies
Decrease underlying inflammation
controllers
Methylxanthines (Theophylline)
Both Relievers and Controllers
MOA
B2 receptor couples to a “Gs” protein activation of adenylyl cyclase increased cAMP increased PKA increased bronchodilation
B2 Adrenergic Agonists (Sympathomimetics)
Major effector tissues: smooth muscle including bronchiolar, liver, skeletal muscle
Major functions: relaxes/dilates smooth muscle + gluconeogenesis + glycogenolysis
B2 Adrenergic Agonists (Sympathomimetics)
- Terbutaline: SC and oral
- Albuterol: oral and nebulizer
Short Acting Beta2 Agonists (SABAs)
- Formoterol* (this has rapid onset for inhaler, can be used as rescue inhaler)
- Salmeterol
- Indacaterol (only used for COPD)
all of these MUST be combined with glucocorticoid
Long Acting Beta2 Agonists (LABAs)
MOA:
Normally: Ach stimulates M3 couple with Gq increases IP3 intracellular calcium calmodulin binding myosin and actin contract bronchoconstriction + increased pulmonary secretions
^^ _________________/__________________ block this!
Anticholinergics/antimuscarinics
Ipratropium (Atrovent)
Also used for rhinorrhea
Short Acting Muscarinic Antagonists (SAMAs)
- Tiotropium (Spiriva): once daily
- Glycopyrrolate: once daily
Long-Acting Muscarinic Antagonists (LAMAs)
B2 agonists > Antimuscarinics: _________
B2 agonists = Antimuscarinics: ______
B2 agonists > Antimuscarinics: ASTHMA
B2 agonists = Antimuscarinics: COPD
MOA
Inflammatory stimuli increase in inflammatory proteins
________________ binds to intracellular receptors goes to cell nucleus decreases expression of genes encoding for inflammatory proteins
Glucocorticoids
Inhalers
Beclomethasone (QVAR)
Budesonide (Pulmicort)
Fluticasone (Flovent)
Oral/IV
Hydrocortisone: short acting (½ life: <12 hours)
Prednisone: intermediate acting (½ life: 12-36 hours)
Methylprednisone: intermediate acting (½ life: >48 hours)
Dexamethasone: long acting (½ life: >48 hours)
all have “SON” in them
glucocorticoids
________________ _____________: existing in the cell membrane
Types
1) CysLT1 Antagonists
* Not as effective as glucocorticoids
2) 5-Lipoxygenase Inhibitor
Leukotriene Modifiers
Mild persistent asthma
Exercise induced bronchospasm/asthma
Allergic rhinitis
May reduce the need for glucocorticoids in select patients
CysLT1 Antagonists
Montelukast (Singulair)
What drug class decreases both COX (prostaglandins) + lipoxygenase (leukotrienes) pathways*
Glucocorticoids
NSAIDS will block COX, which will shunt over to the lipoxygenase/leukotriene pathway (this will cause “aspirin exacerbated respiratory disease”; more bronchoconstriction
MOA
Elevated IgE antibodies and sensitivity to perennial allergens (pollen)
Anti-IgE Therapy: anti-IgE antibody binds to circulating IgE and INHIBITS its interaction with receptors on mast cells and other effector cells
biologic therapies
(OmalizuMAB)
MOA
Increase in cAMP = increase in bronchodilation
Increases cAMP by:
1) Inhibiting phosphodiesterase
AND
2) Blocks adenosine receptor, thereby, INCREASING adenylyl cyclase
AND
Enhances histone deacetylation, decreasing inflammation
Methylxanthines (Theophylline)
Both a Reliever and a Controller
Narrow therapeutic index!
Large variation in ½ life (due to it being metabolized in the liver)
o Very similar to caffeine
o CNS excitation (can cause seizures)
o Weak diuretic
o CV stimulation (chronotropy, inotropy, arrhythmias)
o N/V
theophylline
Inducers = ______________ blood levels of theophylline
DECREASED
Inhibitors = ______________ blood levels of theophylline (toxicity risk)
INCREASED
major triggers of asthma attack (4)
beta adrenergic receptor antagonists
aspirin/NSAIDS
histamine (morphine, demerol, Sch, atracurium)
preservatives
______________ is a reliever + controller of asthma but is 2nd line therapy due to risk of AEs
Theophylline
_______________________ is used in select patients to decrease need or dose of glucocorticoid inhaler
Montelukast (Singular)