Asthma

Front 1

Albuterol

Back 1

• Inhaled short-acting β2-Agonists
• Mechanism: Relax airway smooth muscle by stimulating β2 receptor which ↑ cAMP which results in functional antagonism to bronchoconstriction. They also inhibit the function of inflammatory cells.
• Uses:
o Relief of acute symptoms
o Prevention of exercise induced bronchoconstriction
o Most effective medicine for acute bronchospasm
o Regularly scheduled daily uses not recommended

Front 2

Budesonide

Back 2

• Inhaled corticosteroid for asthma
• Long-term control

Front 3

Cromolyn

Back 3

• Inhaled cromolyn sodium
• Mechanism: largely unknown but inhibition of the activation and release of mediators from the mast cells, eosinophils, and other inflammatory cells.
• Clinical Use:
o Mild asthma
o Prophylaxis of anticipated allergen exposure
o Anti-inflammatory action
o No useful for acute attacks (response takes ~ 2 weeks)
• Except, in exercise, cold asthma → seem to work acutely
• Adverse Effects:
o Transient cough
o Does not work well in kids

Front 4

Fluticasone

Back 4

• Inhaled corticosteroid for asthma
• Long-term control

Front 5

Formoterol

Back 5

• Inhaled long-acting β2-agonists (LABA)
• NOT used alone – always with inhaled steroids
o Contraindicated as monotherapy for asthma
o Can use alone for COPD
• Use:
o long-term control of moderate to severe asthma
o nocturnal symptoms.
o COPD
• Prevents bronchospasms
• Duration = 12 hours
• No used for acute attacks

Front 6

Ipratropium

Back 6

• Inhaled anticholinergic
• Mechanism: competitive inhibitor of muscarinic cholinergic receptors
• No CNS activity (quarternary amines)
• Uses
o Relief of bronchospasm in chronic bronchitis and COPD
o Does NOT block exercise induced bronchoconstriction
o Ipratropium nasal spray for allergic rhinitis
• Adverse Effects
o Dry mouth
o Bitter taste
o Other anticholinergic effects(constipation, tachycardia, blurred vision, and narrow angle glaucoma) are rare

Front 7

Levalbuterol

Back 7

• Inhaled short-acting β2-Agonists
• Mechanism: Relax airway smooth muscle by stimulating β2 receptor which ↑ cAMP which results in functional antagonism to bronchoconstriction. They also inhibit the function of inflammatory cells.
• Uses:
o Relief of acute symptoms
o Prevention of exercise induced bronchoconstriction
o Most effective medicine for acute bronchospasm
o Regularly scheduled daily uses not recommended

Front 8

Mometasone

Back 8

• Inhaled corticosteroid for asthma
• Long-term control

Front 9

Montelukast (Singulair)

Back 9

• Systemic Leukotriene Modifier (inhibits 5-lipoxygenase)
• Used with inhaled steroids often (less effective than LABAs)
• Not useful in acute asthma
• Use:
o Asthma
o Allergic Rhinitis (w/ antihistamine or intranasal corticosteroid)
• May ↑ t1/2 of warfarin

Front 10

Omalizumab

Back 10

• Recombinant humanized IgG1 mab which inhibits the binding of IgE to the high-affinity IgE receptor on mast cells and basophils → limits the amount of mediator release and the allergic response
• Adverse Effects:
o Some evidence of malignancy
o Anaphylaxis (must carry epi-pen)
o Narrow therapeutic index)
o Toxicity – looks like amphetamine use

Front 11

Prednisone

Back 11

• For long-term prevention (> 2 weeks), suppression and control of symptoms and the reversal of inflammation in severely uncontrolled asthma
• Restricted to severely uncontrolled asthma

Front 12

Salmeterol

Back 12

• Inhaled long-acting β2-agonists (LABA)
• Use: concomitant w/ inhaled coritosteroids for the long-term control of moderate to severe asthma, including nocturnal symptoms.
• Prevents bronchospasms
• Contraindicated as monotherapy for asthma
• Duration = 12 hours
• No used for acute attacks

Front 13

Theophylline

Back 13

• Mechanism: SM relaxation via inhibition of PDE → ↑ amp
• Use:
o Moderate bronchodilator (adjuvant to inhaled corticosteroids)
• Adverse Effects:
o Narrow concentration requirements
o Serum [ ] monitoring
o Seizures at high [ ]

Front 14

Tiotropium

Back 14

• Inhaled Muscarinic receptors Blocker (not CNS activity)
• Use:
o COPD
o NOT FDA approved for asthma
• Adverse Effects:
o Dry mouth
o Bitter taste
o Other anticholinergic effects (constipation, tachycardia, blurred vision, narrow angle glaucoma)

Front 15

Zileuton

Back 15

• Systemic leukotriene modifier (inhibits 5-lipoxygenase)
• Mechanism: Inhibits synthesis of ALL leukotrienes by inhibiting the 5-lipoxygenase enzyme, which catalyzes the conversion of arachidonic acid to leukotrienes
• Use:
o Asthma
o Allergic rhinitis (combo with antihistamine or intranasal corticosteroid)
o Exercise induced asthma
o NOT useful for acute asthma attack
o Must be taken QID
• Adverse Effects:
o Hepatotoxic (monitor ALT)
o Avoid if pregnant
• Metabolized by Cyp3A4, 1A2, and 2C9 → may inhibit metabolism of warfarin and theophylline