Anti-asthmatics

Anti- Leukotriene Inhibitors

inflammatory
MOA: Inhibit MOA: Block Cytokine Production MOA: Block 5-LO/Block LT- Receptor
Degranulation (Corticosteriods) Zileuton (5-LO inhibitor)
Block Ca2+ Bind glucocorticoid receptor Zafirlukast (LT-R inhibitor)
influx prevent suppresses expression Montelukast (LT-R inhibitor)
histamine release Block eicosanoid synthesis
Block PDE4??? Block WBC infiltration S/E: Liver toxicity (Zileuton),
vascular permeability Neuropsychiatric events
Cromolyn Sodium
Nedrocromil Beclomethasone DDI:
Sodium Budesonide CYP 1A2- Zileuton
Inhale only Fluticasone CYP 2C9- All 3
No GI absorption Flunisolide CYP 3A4- Monte/Zileuton
Statins liver toxicity (monitor
Good for children Dexamethasone
Triamcinolone liver enzymes)
S/E: cough, throat Prednisolone
irritation, dry mouth Can restore -agonist responsiveness
Most effective for asthma
Urgent treatment discontinue
systemic use gradually (7-10 days)

S/E: bone density, thrush, growth???

-agonists
MOA: activate AC cAMP

Short-acting
Terbutaline
Bitolterol
Levalbuterol
Pirbuterol
Albuterol
Long-acting
Salmeterol
Formoterol
Not first line
Never use alone (always w/ ICS
or anti-cholinergic)
Dont overuse (2-tolerance)
Overuse
cAMP PDE4
cAMP and pro-
inflammation
ARK
phosphorylation
inactivation of -AR
Heparin
blocks PDE4?? and ARK

S/E: Tachycardia, K+ (into muscle

and secreted), muscle tremor,
 Anti-asthmatics
tachyphylaxis, severe asthma
episodes and death (fast-acting)

Methylxanthines Muscarinic Antagonists

MOA: Block MOA: Blocks M receptors Blocks
Adenosine Receptor/ bronchoconstriction (bronchodilation)
Block PDE4 Ipratropium
Block adenosine Tiotropium (longer DOA- slower
as a NT in CNS dissociation)
Block PDE4 Limited GI absorption (quaternary
cAMP ammonium)

Theophylline
Enoprofylline (no S/E: CV-related deaths, peanut allergy
cross into BBB) (emulsifier of Ipratropium)
Narrow
therapeutic
window
Use low doses

S/E:
dose=
convulsions,
medullary
stimulation (Theo)
dose= mild CNS
stimulation (Theo)

DDI:
-agonist more
tachycardia
clearence (CYP
inducers):
rifampin, BC,
phenytoin,
barbiturates
clearance (CYP
inhibitors):
zileuton,
cimetidine,
erythromycin
ANTAGNOSTIC
with
corticosteroids
(lung function)

Anti-IgE Antibody
 Anti-asthmatics
MOA: Blocks IgE interaction with mast cells
Omalizumab
Injection only
>12 yo
dependence on corticosteroids
Expensive ($$$)
Refractory asthma (unrelenting)

S/E: CV-related events