Asthma

Front 1

Two major strategies for treating asthma?
What classes fall into each strategy?

Back 1

Bronchodilation:
1. Beta-2 receptor agonists
2. Methylxanthines (stimulants)
3. Muscarinic antagonists

Reduce Inflammation:
1. Glucocorticoids
2. Inhibit mast cell degranulation
3. Leukotriene antagonism
4. Anti-IgE antibody

Front 2

Beta-2 Adrenergic Agonists
Action?
Side Effects?
Monotherapy?

Back 2

Therapeutic Action: Bronchodilation secondary to beta-2 receptor activation of cAMP in bronchial smooth muscle

Side effects: Tachycardia, mild hypotension, tremor
Possibly contraindicated in patients with underlying cardiac disease and for people on MAOI's.

Monotherapy: Cannot be used as a longterm monotherapy as it does not do anything for inflammation.

Front 3

Short Acting Beta-2 receptor agonists (symptomatic relief) (4)

Back 3

Albuterol
Levalbuertol [(R)-albuterol]
Metapoterenol (don't need to know)
Terbutaline (Don't need to know)

Front 4

Long acting Beta-2 receptor agonists (prophylactic treatment) (2)

Back 4

1. Salmeterol
2. Formeterol

Front 5

Methylxanthines?

Back 5

Theophylline, Aminophylline

1. Maintenance therapy for asthma/COPD
2. Relaxes smooth muscle/increases cAMP/blocks adenosine A2 receptors

Side Effects: Similar to caffeine - insomnia, agitation, tachycardia, tremor

Not used much since potent, long-acting Beta2 agonists available

Front 6

Ipratropium Bromide, Tiotropium
Class?
Actions?
Uses?
Why is it still useful?

Back 6

Muscarinic antagonists

Pharmacology is similar to atropine but atropine is not used due to CNS toxicity (blocks the muscarinic ACh receptor)

Quaternary (charged) so minimal systemic effects after inhalation since is poorly absorbed. CNS side effects are limited because of the poor distribution.

Uses: COPD, asthma with other bronchodilators
Useful in patients who cannot take Beta-2 agonists (patients taking MAOI inhibitors, patients with cardiac arrhythmias, patients with unstable angina)

Front 7

Glucocorticoids

Back 7

1. Useful in severe asthma attacks refractory to therapy with bronchodilators.
2. Not useful for chronic systemic use because of side effects
3. Beclomethasone dipropionate used in inhaler (daily inhalation) to suppress inflammation
4. Other agents include triamcinolone, flunisolide, fluticasone.

Major side effects: Hoarse voice, oral candidiasis

Concern of systemic absorption with daily use (swallowed: rinse mouth or use spacers in inhalers to minimize deliver of too much drug)

Front 8

Cromolyn, Nedocromil

Back 8

Inhibition of mast cell degranulation

1. Stabilizes mast cells by and as yet unknown mechanism
2. Used by inhalation to prevent mild to moderate asthama attacks by reducing airway reactivity
3. Used with glucocorticoids to prevent moderately severe asthma
4. Minimal adverse side effects including bad taste, cough, wheezing, bronchospasm, headache

Do not relieve acute asthmatic symptoms

Front 9

Montelukast, Zafirlukast

Back 9

Leukotriene Receptor Antagonists

Prevents actions of cysteinyl leukotrienes (LTC4, LTD4, LTE4, and CycLT1 receptors)

Administered orally for prophylactic treatment of mild asthma

Minimal side effects except for a rare inflammatory condition including pulmonary infiltrates, neuropathy, skin rashes, vasculitis.

Front 10

Zileuton

Back 10

5-Lipoxygenase Inhibitor
Inhibits formation of all 5-lipoxygenase products including LEUKOTRIENES
Administered orally for prophylactic treatment of mild asthma
Although this drug has a wider profile of inhibition than cys-LT receptor blockers, it is no significantly more efficacious.
Minimal side effects except for rare elevated liver enzymes.

Front 11

Omalizumab

Back 11

Humanized Monoclonal Anti-IgE Antibody

Binds to Fc domain of IgE (binding site for IgE binding receptor) thus prevents IgE from interacting with mast cell receptor
Administered via IV or subcutaneously every 2-4 weeks
Reduces airway responsiveness to antigens and decreases the need for asthma drugs

Concerns: Infection, pain on injection