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29 Cards in this Set
- Front
- Back
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What are the 3 main strategies to treating asthma?
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Bronchodilators
Anti-Inflammatory Avoidance of triggers |
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Exercise induced asthma is treated with bronchodilators. How do you induce bronchodilation? (4)
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Beta 2 agonists
Leukotriene Receptor Antagonists Anticholinergics PDE Inhibitors |
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What is the main bronchodilator used in COPD?
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Anticholinergics - Ipatropium Bromide
These are also used when asthmatics are unresponsive or contraindicated to beta agonists. |
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What receptor do anticholinergics used to treat asthma/copd target?
What is the action of this receptor? |
Muscarinic 3 receptor
ASM contraction and mucus secretion |
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Atropine was used, but no longer is. What two agents are used now?
What are the side effects associated with these agents? |
Ipatropium Bromide
Tiotropium Dry mouth, GI upset |
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Ipatropium Bromide and Tiotropium have a very low degree of systemic absorption and therefore have fewer side effects than atropine. This is why they are used over atropine today.
Ipatropium Bromide and Tiotropium interrupt the neural tone to the lungs that causes bronchoconstriction. They are mainly used in COPD |
In chronic asthma, Ipatropium Bromide is indicated for acute attacks as rescue therapy in those who cannot tolerate Beta 2 agonists.
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The main 3 bronchodilators are anticholinergics, beta 2 agonists, and methylxanthines. Name the 4 newer beta 2 selective agonists.
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Albuterol
Pirbuterol Bitolterol Terbutaline |
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What side effects are seen with these agents if taken at high doses or orally?
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Cardiac effects (heart)
Tremor (skeletal muscle) |
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What is important to know about giving albuterol?
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It is a racemic mixture of two enantiomers R and S. R binds tighter to the Beta 2 receptor.
Patients sensitive to Beta 1 effects need to be switched to the pure R enantiomer. |
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What G protein are short acting adrenergic agonists like albuterol coupled to? What is the ultimate effect that causes the smooth muscle relaxtion?
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Gs
Decreased MLCK and activation of MLP phosphorylase. |
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Describe the onset of action of short acting beta agonists
They are good candidates for this They are bad candidates for this |
Rapid onset 15-30 min
Peak effect 30-60 min Duration 4-6 hours Acute attacks For prevention of attacks unless used prophylactically before known triggers. |
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Name the 2 long acting agonists.
What are their limitations? |
Salmeterol
Formoterol Do not treat inflammation They have a longer onset of action and cannot be used in acute situations. Higher mortality among asthmatics taking LABA's. They are however good candidates for prevention of bronchoconstriction |
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Do not use LABA's as monotherapy! What do you want to use with it?
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Corticosteroids
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COPD is associated with chronic breathlessness, while asthma is associated with acute attacks. Describe the role of beta agonists in COPD.
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Short acting agents are less beneficial than long acting agents.
Many patients have concomitant CAD and anticholinergics are preferred. |
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What is preferred treatment in COPD patients?
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Combination therapy of a beta agonist and an anticholinergic.
The short acting agents are less beneficial because COPD is a chronic disease. |
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Bronchodilation can be accomplished by 2 ways. What are they?
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Increase cAMP production (beta agonists)
Decrease cAMP degradation (Inhibition of PDE) |
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Which cells are inhibited by PKA?
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Mast cells - contain beta receptors that when stimulated, their activity is inhibited.
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Name the 2 methylxanthines.
What is their action? |
Theophylline and Aminophylline
They inhibit PDE 3 and 4 to induce bronchodilation They effect is weak however in asthma They also have effects on the immune system/inflammation by inhibiting T-lymphocyte proliferation and cytokine production. They are used in COPD because of this anti-inflammatory effect. |
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How does theophylline act?
What are 3 positive effects of this agent? |
Through adenosine receptor antagonism
Increased ventilation during hypoxia Increase endurance of diaphragmatic muscles Decreased mediator release from mast cells |
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Describe the adverse effects of Theophylline.
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PDE Inhibition causes cardiac arrhythmia's, nausea, vomiting
Adenosine Receptor Antagonism causes tachycardia, gastric acid secretion and diuresis. |
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Very high doses of theophylline can cause seizures! It has a narrow therapeutic index and has many drug drug interactions. Monitor the plasma levels carefully!
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Beta agonists increase cAMP
Methylxanthines increase cAMP Anticholinergics prevent acetylcholine induced release of Ca which inhibits contraction. |
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What are the 3 main classes of anti-inflammatory drug?
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Corticosteroids
Cromolyns Leukotriene Pathway modifying agents Anti IgE Antibodies |
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Corticosteroids are used to control persistent asthma and a major preventive treatment. They prevent acute exacerbations of asthma.
What is beneficial about corticosteroids? |
They inhibit several different pathways to inflammation including COX synthesis of prostaglandins, LOX synthesis of leukotrienes, histamine and other pathways.
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What is the drawback of corticosteroids?
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They have a lot of side effects. A big issue is managing side effects in chronic asthma patients. High doses cannot be administered all the time
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Corticosteroids up-regulate these
They down-regulate these |
Beta receptors - make you more sensitive to beta agonists and anti-inflammatory proteins
Inflammatory proteins |
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What are the cellular effects of corticosteroids?
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They cause apoptosis of inflammatory cells such as eosinophils and T lymphocytes
No effect on mast cells (mediators are preformed), but they are inhibited over time as the entire inflammatory response is muted. |
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GC's decrease the number of inflammatory cells in the airways, reduce vascular permeability and reduce contractile function in the lungs over time controlling asthma
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The adverse effects of GC's include osteopenia/osteoporosis in adults, stunted growth in children when dose is high enough to enter through the GI into circulation. Oral candidiasis can occur also and should be taken with oral mouthwash.
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What 3 things do you need to monitor for in short term use of GC's?
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Markers of HPA axis (cortisol)
Measures of bone metabolism (osteocalcin) Collagen synthesis |
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What 5 things do you need to monitor for in long term GC use?
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Adrenal insuffciency
Osteoporosis Retardation of bone growth Obesity Psychosis |
