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83 Cards in this Set

  • Front
  • Back
Treatment for intermittant asthma
SABA prn

short-acting beta2 agonist
First step to treat persistent asthma
low-dose ICS

inhaled corticosteroid
alternative to low-dose ICS?
cromolyn or montelukast
Summarized the step-ups of asthma therapy
low-dose ICS --> medium-dose ICS -->
then add LABA (long-acting) or montelukast -->
then try high-dose ICS with LABA or montelukast -->
then add oral systemic corticosteroids
Most prescribed drugs (ICS) to treat asthma
Budesonide (Pulmicort)
Fluticasone (Flovent)
Alternative but not perferred treatment of mild persistant Asthma
Cromolyn sodium
Nedocromil (Tilade)
Leukotriene modifiers
Montelukast - leukotriene recep antagonist
Zafirlukast - leukotriene recep antagonist
Zileuton - blocks leukotriene synthesis by inhibiting 5-lipoxygenase,
Adjunctive treatment of adults (12 & older) who have
moderate to severe persistant ALLERGIC asthma
Omalizumab (Xolair)
Adjunctive treatment of adults (12 & older) who have
moderate to severe persistant asthma
Long-Acting Beta2-agonists:
multiple anti-inflammatory effects via ∆ gene expression e.g.:
1.inhibit phosopholipase A2 --> decrease prostaglandins
2.Decreased cytokine & chemokine production
3.Inhibit the accumulation of basophils, eosinophils & other leukocytes in lung tissue
4.Decrease vascular permeability
5.Enhanced responsiveness of Beta2 receptors
corticosteroids can also be given ____ if necessary (higher toxicity) for acute exacerbations or severe asthma
_____ route for corticosteroids is used for ER visits for asthma attacks & for Rx of status asthmaticus
Inhaled Corticosteroids: (3)
Beclomethasone (QVAR ®)
Budesonide (Pulmicort ®)
Fluticasone (Flovent ®)
Beneficial effects may be seen w/in when?
a week, but maximal improvement may require months of therapy
Oral or I.V. Corticosteroids:
Prednisone or Prednisolone (generic)(etc.)
Rx: acute asthma exacerbations & chronic severe asthma.
Oral or I.V. Corticosteroids:
Adverse effects:
: suppression of growth & adrenal axis; cataracts
Rx of Chronic Asthma:
In Persistent or Chronic Asthma:*
1. Inhaled corticosteroid (dose depends on severity)
If needed add
2. Long acting beta2 agonists
tachycardia and hypokalemia at 4-5 times recommended
Rx of Chronic Asthma:
In Persistent or Chronic Asthma:*

Other options:
3. Cromolyn sodium or Nedocromil
4. Leukotriene inhibitors
- can be taken orally (better adherence, esp. in kids)
- less efficacious than corticosteroids
Long acting beta2 agonists
Salmeterol (Serevent ®)
Formoterol (Foradil ®)
Long acting beta2 agonists
quick facts
highly lipid soluble (don’t diffuse away from 2R’s)
bronchodilation lasts >12 hrs
Typically added to drug regimen when a corticosteroid is “not enough” to control asthma (not used in place of a corticosteroid)
Why use Formoterol
Salmeterol over albuterol?
duration of action is much longer (12 hrs vs 4-8 hrs)
Degranulation Inhibitors

aka Mast Cell Stabilizers
Cromolyn sodium (Intal ®)
Nedocromil (Tilade ®)
Degranulation Inhibitors
quick facts
Inhibits release of cell mediators from eosinophiles & lung mast cells (mechanism ???)
Given by inhalation
Less potent than corticosteroids
Must be taken several times a day or before an “attack”
Nedocromil is approved for pts 12 yrs & older; 15-20 % complain of unpleasant taste Cromolyn is approved for all ages
Cromones: MOA
inhibition of mast cell degranulation
inhibition of IL-4 induced IgE synthesis
inhibit the activation of inflammatory cells (in vitro)
local anesthetic effect
Promotes relaxation via interfering with Ca++ influx into the cell
Leukotriene Synthesis Inhibitor
Zileuton (Zyflo ®)
Montelukast (Singulair ®)*
Zafirlukast(Accolate ®)
Zileuton (Zyflo ®)

- inhibits 5-lipoxygenase enz. - blocks formation of leukotrienes from arachidonic acid
- 4 times a day dosing
- occasional liver toxicity
All three LK pathway inhibitors can be used to treat “aspirin _____- (but it is best to just avoid NSAIDs)
Montelukast (Singulair ®)*
points about this drug
- oral route (better compliance in kids)
- 1 time per day dosing (night time -asthma is more common at night) - approved for children 6 yrs & older
- good for exercise induced asthma
Zafirlukast(Accolate ®)

- 2 times per day dosing
- patients must be 12 yrs & older
- liver tests needed
Rx for Acute Asthma and prevention of exercise induced asthma
Short acting beta2 agonists
SABAs are The most effective drugs for _____
SABAs with Half lives of 6 hrs or less
Albuterol (Proventil, Ventolin ®)
Terbutaline (Brethine, Bricanyl ®)
Mechanism of SABAs:
stimulate AdCyl -->
increase cAMP -->
decrease [Ca]I
Adverse effects of SABAs
tachycardia, skeletal muscle tremor
If a beta2 efficacy is “lost” over time (destabilization of asthma), another drug such as an ____
anti-inflammatory drug
mechanism of theophylline
Adenosine R antagonist
PDE inhibitor (toxic doses)
Bronchodilation & anti-inflammatory actions
Vagal mediated broncho-_________ contributes to asthma in some patients (M3)
Ipratropium bromide (quaternary)
drugs: metered dose and metered dose with albuterol
Atrovent ® - metered dose
Combivent ® - metered dose combo w/ albuterol
Take every 4-6 hrs
Muscarinic Antagonists for COPD
Tiotropium (Spiriva®) –for COPD
24 hr duration of action
Slow dissociation from receptor
Capsule inhaled dose
Handihaler device (dry powder; no flurocarbons)
Beta Agonists for acute asthma treatment
Albuterol, levalbuterol, pirbuterol, bitolterol, isoproterenol, & epinephrine
PDE inhibitors for acute asthma treatment
Anticholinergics for acute asthma treatment
Inhaled beta-2 adrenergics
salbutamol / Ventolin
fenoterol / Berpotec
procaterol / Pro-Air
Cromoglycate / chromolyn
inhaled nedocrimil sodium (Tilade)
Oral Ketotifen (Zaditen)
Inhaled Steroids
beclovent, budesonide
Oral Steriods
Anti-IgE Antibody drug
Omalizumab (Xolair ®)
What does Omalizumab (Xolair ®)
- Antibody targeted against the portion of IgE that binds to receptors on mast cells & other inflammatory cells (see next slide)
Lowers free circulating IgE & prevents antigen induced degranulation
A multi week treatment w/ Omalizumab can lower plasma IgE & reduce______
responses to antigens

Down regulation of FcRI binding sites on immune cells also occurs
humanized chimeric monoclonal antibody against high-affinity receptor-binding domain of human ____.
acts by complexing free ___, preventing its binding to effector cells.

enzyme converting histidine to histamine
histadine decarboxylase
H1 histamine receptor Found on ___-
smooth muscle, endothelium, and central nervous system tissue
H1 histamine receptor Activation results in vasodilatation, _____, smooth muscle activation, and separation of endothelial cells.
H2 histamine receptor
Found on _____
parietal cells
H3 histamine receptor Found in the ______
central nervous system
H4 histamine receptor Recently discovered in different parts of the body including organs of the digestive tract, basophils, and ________ cells
bone marrow
When Histamine is Stimulated, what symptoms?
Allergic Rhinitis

Allergic Bronchitis

Allergic Conjunctivitis

Allergic Dermatitis

Stimulation of H2 Receptors causes what?
Incr Gastric Acid and Pepsin --> Abdominal Pain
Incr Rate & Force of Myocardial Contraction --> tachycardia
Incr Vasodilation --> Hypotension, Flushing, HA
H1 Type of receptor
G-protein coupled, linked to intercellular Gq, which activates phospholipase C
H2 type of receptor
G-protein coupled, linked to intercellular Gs
H3 type of receptor
G-protein coupled, possibly linked to intercellular Gi
H1 antagonists are really called ______ agonists

b/c when they bind to receptor, they put it in an inactive state.
H1 receptor Couples to G__?–protein to activate phospholipase C; inc. inositol triphosphate (IP3 ), diacylglycerol (DAG)
First Generation Antihistamines
Oldest and most effective antihistamine on the market

Also inhibits the reuptake of serotonin, which led to the search for viable antidepressants with similar structures (prozac)
Diphenhydramine (Benedryl)

Exhibits fewer side effects than most antihistamines
Widely used as an antiprurtic (stops itching)
Clemastine (Tavist)
Anti-emetic (anti nausea)
Also causes strong sedation
Readily crosses the BBB
Dimenhydrinate (Dramamine)
Ethanolamines (4)
Clemastine (Tavist®)
Dimenhydrinate (Dramamine®)
Diphenhydramine (Benadryl®)
Doxylamine (Unisom®)
Second Generation Antihistamines More selective for H1 receptors where?

Doesn't cross the BBB like 1st generation
examples of Second Generation Antihistamines
loratadine [Claritin]
cetirizine (Zytric) #12
Examples of "Next” Generation Antihistamines
Highly selective for H1 where?
Piperidines Have no significant _____ effects
Third generation H1-receptor antagonists
Levocetirizine (Zyzal)
Deslortadine (Clarinex)
Fexofenadine (Allegra)
What 3rd gen H1-receptor blocker?
It is the active metabolite of Lortadine
Even though it is thought to be more effective, there is no concrete evidence to prove this
Deslortadine (Clarinex)
Which 3rd gen H1 receptor blocker?
It was developed as an alternative to Terfenadine
It was proven to be more effective and safe
Fexofenadine (Allegra)
Ethanolamine to know for test
Piperidines to know for the test
Others to know for the test
Loratadine, Cetirizine
Common side effects of 1st gen drugs?
sedation, dizziness, tinnitus, blurred vision, euphoria, lack of coordination, anxiety, insomnia, tremor, nausea and vomiting, constipation, diarrhea, dry mouth, and dry cough
Common side effects of 2nd gen drugs?
drowsiness, fatigue, headache, nausea and dry mouth
H4 receptors Couples with G__?-protein to inhibit adenylyl cyclase
Just recently discovered
The H4 receptor is highly expressed in peripheral blood leukocytes and ______ tissue, making this receptor a potentially interesting target in allergic and inflammatory diseases