Drug Name Mechanism Application Side Effects Contraindication Drug-Drug

Interactions

BRONCHODILATION THERAPY: Logical b/c immediate phase of asthma is constriction, sole role of these medications is to
counteract the early mast cell mediators. Incl’d β2-Agonists, Muscarinic Antagonists, Adenosine and cAMP phosphodiesterase
inhibitor (Theophylline), & Leukotriene antagonists.
ALBUTEROL Short-Acting β2- ACUTE Tremor (via pKA Steroid prevents the β
TERBUTALINE Agonists ASTHMA (+) pre-synaptic receptor
2+
LAVALBUTEROL Gs  AC  ATTACK Ca influx  Ach desensitization
*Onset 5-15 mins* cAMPphosphorylat release
e MLCKrelaxation! -Cardiovascular
-↑TPR, ↑BP, toxicity
bronchodilation! **Chronic β2 agonist
use leads to receptor
downregulation
(tolerance)

FORMOTEROL Long-Acting β2- ASTHMA incr death rate from Steroid prevents the β
*rapid onset- 3 min Agonists Asthma attacks in receptor
SALMETEROL African Americans! desensitization
*slow onset- 1 hr **Chronic β2 agonist
use leads to receptor
downregulation
(tolerance)
ATROPINE Anti‐cholinergic More effective in *Cause urinary
IPRATROPIUM agents COPD retention in BPH pts*
BROMIDE block M3 receptors Bronchodilation
on mooth muscle is less effective SEE ‘ANTI-
than β2-Agonists CHOLINERGIC’
*Can treat CHART FOR
Bronchospasm ATROPINE ADRs!!
caused by β-
 blockers
ANTI-INFLAMMATORY AGENTS: *Prophylactic agents* Incl’d Mast cell Stabilizers, Glucocorticoids/corticosteroids,
Leukotriene synthesis inhibitors/antagonists, & Anti-IgE Antibody
THEOPHYLLINE Methylxanthines Given to children DOSE P450 inhibitors may
*very narrow -competitive who have DEPENDENT: increase
therapeutic index* antagonist @ difficulty inhaling 1) LOW = ↓fatigue/ theophylline
CAFFEINE adenosine-R (major Aminophylline drowsiness toxicity, causing
effect) IV infusion used in ↓ability for delicate ventricular
-inhibition of status asthmatics muscle coordination tachycardia
phosphodiesterase, 2) MEDIUM = (macrolide,
prevents ↓ in cAMP ↑CNS, anxiety & cimetidine,
-prevents calcium- nervousness quinolones)
mediated contraction ↑risk of nausea &
*Also act as diuretics! vomiting
Tachycardia
CROMOLYN Mast Cell Stabilizers -throat irritation &
SODIUM inhibits pulmonary cough, which can
NEDOCROMIL mast cell trigger asthma!
degranulation
*does not possess
inherent
bronchodilating
capacity*
-must be taken a few
hours in advance to be
effective
BUDESONIDE Glucocorticoids/ -Improvement of **Oral Candidiasis Low dosage prevent
Corticosteroids asthma symptoms (thrush), so do an the desensitization of
-suppress immune -Lowers oral rinse after puff of β receptor when
response requirements of β2 corticosteroid** using B2 agonist
(1) Inhibits agonist usage
phospholipase A2 -Only used Long-term use =
(prevents PG and systemically for osteoporosis &
 Leukotriene acute asthma cataracts (in DM &
production) attacks and old ppl)
(2) Act as chronic severe
Transcription asthma
Factors (b/c
glucocorticoid
receptors are nuclear
receptors)
ZILEUTON Leukotriene More potent All these drugs Zileuton has liver
inhibitors response than inhibit chemotaxis, toxicity, SO not for
5-lipoxygenase blocking so risk for severe pts w/ liver damage!
inhibitor histamines bacterial infection!
MONTELUKAST/ LTD4 receptor -orally available -RARE ADRs:
ZAFIRLUKAST antagonist -Approved for suicide, agitation,
↓Bronchoconstriction young kids (6 yrs insomnia,
↓ Bronchial reactivity old) hallucination
↓Mucosal edema **MONTELUKA
↓Mucus ST is taken once
hypersecretion daily (prefer!)

OMALIZUMAB Anti-IgE Antibody If Fluticasone + Anaphylaxis (rare)

Anti-Asthma
*binds to free IgE in drugs
Salmeterol inhaler
cAMP phosphorylates myosin light chain kinase (MLCK)
the blood* but not to cannot control
Bronchoconstriction
IgE already bound to asthma symptoms,
mast cells & basophil this drug is added
cells. ↓IgE
Acetylcholine leads to
Adenosine for those who are
Leukotriene
downregulation of FC IgE mediated
receptor on mast cells sensitive & have
Ipratropium Theophylline Lukast
↑↑bld IgE!Zileuton
OTHER DRUGS: Incl’d Epinephrine (in Status Asthmatics), Antibiotics if infection persists. Also Antitussives like opioids
inactivate
(Codeine), Opioid derivatives (Dextromethorphan), Anti-histamines (Promethazine, Diphenhydramine), & Expectorants
Bronchodilation
(Ammonium salts-NH4Cl-, Acetyl cysteine). NO

cAMP
B2 agonist Theophylline

ATP AMP cGMP dephosphorylates myosin light chain (MLC) 13