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75 Cards in this Set

  • Front
  • Back
An exaggerated ____ response often predominates in asthma.
TH2 (T Helper 2)
What is the main effector function of TH2 cells?
Stimulate differentiation of eosinophils

Activate B cells
Chronic Asthma associated with allergies has 3 responses mediated by the immune system. What are they?
Chronic inflammation

Bronchospasm

Airway hyperresponsiveness
What are the most effective drugs for chronic tx of asthma?
Anti-Inflammatory
What is the best way to minimize systemic side effects from steroids when treating asthma?
Inhalation

Less systemic effects since you're targeting the lungs. Also, with inhalation you are using lower dosages
"-one/ -lide / -nide"
Inhaled Corticosteroids
Beclomethasone dipropionate

Fluticasone

Triamcinolone

Flunisolide

Budesonide

Ciclesonide
Inhaled Corticosteroids
Do inhaled corticosteroids cause bronchodilation?
NO!

No direct effect on muscle tension
Inhaled Corticosteroids MOA:
Potentiate β adrenergic agents by:

↑cAMP and upregulating receptor level
What is the most potent and consistently effective long termcontrol medication for asthma?
Inhaled corticosteroids
Advantage of using inhaled corticosteroids?
Higher local drug concentration than an equivalent dose of systemic corticosteroids

**↓ SIDE EFFECTS**
You have started a patient on a long term asthma drug and they complain of an unpleasant taste, oral thrush, difficulty speaking and lots of coughing with worsening asthma after use... what type of drug did you give them?
Inhaled corticosteroid
What are some ways we can prevent/reduce adverse effects with the use of inhaled corticosteroids?
-Spacers or valved holding chambers

-Rinse and spit after inhalation

-Use short acting β2 activator before inhalation --> prevent bronchospasm
"Predniso"
Oral Systemic Corticosteroids
Prednisone

Prednisolone

Methylprednisolone
Oral Systemic Corticosteroids
Why do you want to minimize the dose of oral steroids?
Adverse Effects
When would you use oral systemic corticosteroids for asthma?
-Moderate to severe exacerbations of asthma (3-10 days to control severe cases)

-Used for long-term control ONLY in the MOST SEVERE, difficult to control cases (must minimize the dose)
What can be used/done to block/inhibit the mediators of mast cells?
Prevent Mast Cell Degranulation

Prevent IgE from binding to Mast Cell

Block Leukotrienes
"Crom"
Mast Cell Stabilizers
Cromolyn

Nedocromil
Mast Cell Stabilizers
MOA of Cromolyn?

Mast Cell Stabilizer
Prevents degranulation and the relase of mediators

*↓Histamine
*↓Leukotriene
*↓Cytokines
Which Mast Cell Stabilizer affects a broader range of inflammatory cells?
Nedocromil
Would cromolyn reverse acute bronchospasm?
NO!
Side effects of Mast Cell Stabilizers?
Irritate the throat
-Cough
-Transient bronchospasm

Nedocromil--> unpleasant taste
How can you prevent/modify the action of leukotrienes?
Affect conversion of Arachodonic Acid to Leukotriene

Inhibit LT1 receptors
"-leu/luk"
Leukotriene Modifiers
"leu"
Leukotriene Modifers

-Zyleutron

**Inhibit leukotriene production**
"luk"
Leukotriene Modifiers

-Montelukast
-Zafirlukast

**Block LT1 receptor**
Which Leukotriene modifiers block the LT1 receptor?
-Montelukast
-Zafirlukast
Which leukotriene modifier inhibits leukotriene production?
Zyleutron
Anti-IgE therapy drug?
Omalizumab
What is omalizumab?
Recombinant humanized monoclonal antibody to IgE

**Anti-IgE Therapy**
When treating with omalizumab, is there allergen induced activation of mast cells?
No
What is an adverse side effect of omalizumab?
Anaphylaxis
Mast Cell stabilizers are ___ line for Asthma
2nd line
Leukotriene Modifiers are taken _____
orally
Are leukotriene modifiers good for acute asthma?
No
Which members of the population are more responsive to Leukotriene modifiers?
Aspirin-Sensitive Asthmatics
Why would montelukast reduce bronchoconstriction from aspirin induced asthma?
Montelukast blocks LT1 receptors that bind to leukotrienes.
When is omalizumab used to treat asthma?
SubQ injection every 2-4 weeks

Adjunctive therapy in patients with severe persistent asthma that is INADEQUATELY controlled with the combination of high dose ICS and LABAs
What are the three classes of bronchodilators?
β2 agonists

M blockers

Methylxanthines
Metaproterenol

Albuterol

Levalbuterol

Pirbuterol

Terbutaline
Short Acting β2 Agonists
Salmeterol

Formoterol

Arformoterol
Long Acting β2 Agonists
"-meterol/-moterol"
LA β2 Agonists
M Blocker
Ipratropium Bromide
What type of β and M receptors are in the lungs? what do they do?
β2 --> bronchodilation

M3 --> bronchoconstriction
Why is the use of β2 agonists considered functional/physiological antagonism?
β2 agonists counteract (bronchodilate) M3 bronchoconstriction
What drug would you use to block M3 receptors causing bronchoconstriction?
Ipratropium bromide
β2 agonists can cause palpitations, sinus tachycardia and ↑BP. Why?
Higher doses of β2 agonists activate β1 receptors
Adverse Effects

Tremor, HYPOkalemia, palpitations, sinus tachy, ↑BP
β2 agonists
What is the signaling pathway by which β2 agonists cause bronchodilation?
↑cAMP
What enzyme breaks down cAMP?
PDE
"-phylline"
Methylxanthines
Theophylline

Aminophylline
Methylxanthines
The chemical structure of Methylxanthine drugs closely imitates what?
caffeine
MOA: Methylxanthines
Inhibits PDE (especially PDE-4)

Inhibits adenosine receptors
MOA: Methylxanthines on smooth muscle cells
↑cAMP ---> block adensoine receptors

** smooth m. RELAXATION**
MOA: Methylxanthines on T cells, Eosinophils and Mast Cells
↑cAMP --> block adenosine receptors

**Anti-inflammatory**
Problems with methylxanthines
Narrow TI

Erratic bioavailability
Are problems with CNS stimulation from methylxanthine use more common in children or adults?
Children
Adverse Effects

-Irritate GI mucosa

-CNS Stimulation

-CV effects
Methylxanthines

CV and CNS problems stem from Caffeine-like effects
What is the drug of choice for treating ACUTE asthma symptoms and exacerbations?
Short Acting β2 Agonists
What is the drug of choice for preventing excercise-induced asthma?
Short Acting β2 Agonists
What drug is adminstered with SABAs in moderate to severe asthma cases in the ER?
ipratropium bromide
(M blocker)
Are LABAs recommended to treat acute asthma attacks?
NO
Longterm Asthma Therapy

-used adjunct to corticosteroids

-may be used before excercise

- not recommended as a monotherapy for long-term, persistent asthma

-not recommended for acute asthma attacks
LABAs
Which Methylxanthine drug can be used as an alternative, but not preferred, adjunctive therapy with inhaled corticosteroids for long-term control of moderate or persistent asthma?
Theophylline
What are the "quick relief" drugs for asthma?
Inhaled SABAs, M blockers -->bronchodilate

Systemic corticosteroids --> anti-inflammatory
What drugs can be used long-term for anti-inflammatory effects to treat asthma?
-Inhaled Corticosteroids

-Leukotriene Modifiers

-Mast Cell Modifiers

-IgE-Antibodies
What drugs can be used long-term for bronchodilation to treat asthma?
LABAs

Methylxanthines
Corticosteroids don't work well for COPD. Why?
Corticosteroids don't really affect PMNs.

COPD is mostly a PMN-mediated problem
Are anti-inflammatory agents useful for COPD?
No, don't affect PMNs
What drugs are useful for acute attacks of COPD?
SABAs

**If prompt bronchodilation doesn't occur, ADD AN M BLOCKER**
What drugs are useful for management of Stable COPD?
β2 Agonists

M-blocker

Methylxanthine

**These are Bronchodilators**
When should you use corticosteroids in treating COPD?
Add inhaled glucocorticoid to bronchodilator tx for more severe symptomatic COPD (chronic therapy)

Systemic glucocorticoids for acute attacks of COPD