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54 Cards in this Set

  • Front
  • Back
asthma is _________
a chronic inflammatory disorder
Many mediators are released that may cause _____ and ________.
edema and bronchoconstriction
Many mediators are released that may cause edema and bronchoconstriction. these are...(3)
Histamine
Leukotrienes
Prostaglandins
_________ and _______ are key in managing asthma.
Bronchodilators

anti-inflammatory corticosteroids
Inhaled Corticosteroids (5)
beclomethasone
triamcinolone
flunisolide
budesonide
fluticasone
Systemic Corticosteroids (3)
prednisone
prednisolone
methylprednisolone
Long acting beta2 agonists (2)
salmeterol
formoterol
Cromones (2)
cromolyn
nedocromil
Leukotriene modifiers (3)

indication?
montelukast
zafirlukast
zileuton

aspirin-sensitive asthma, adjunctive with anti-inflammatory
Long term control meds (Maintenance) (7)
Inhaled Corticosteroids
Systemic Corticosteroids
Cromones
Long acting _2 agonists
Combined medication
Leukotriene modifiers
Theophylline
QUICK RELIEF (RESCUE DRUGS) (3)
Inhaled ß2 agonist
Anticholinergics
Systemic corticosteroids
QUICK RELIEF (RESCUE DRUGS)
Inhaled ß2 agonist (3)

indications?
albuterol
pirobuterol
terbutaline

PRN for acute symptoms, exercise induced asthma
QUICK RELIEF (RESCUE DRUGS)
Anticholinergics


indications?
Ipratropium bromide

acute broncho-spasms
QUICK RELIEF (RESCUE DRUGS)
Systemic corticosteroids


indications?
prednisone
prednisolone
methylprednisolone

acute exacerbations
Step Up treatment?
Start at initial level of severity; gradually step up as needed to gain and maintain control.
Step Down treatment?
Start high to gain control and step down.

Start with higher doses .. Stronger meds to get control …
Review treatment every 1 – 6 months with the idea of a gradual reduction in treatment
Step UP tretament
Start with least intense treatments .. If control is not maintained …. Consider step up
Be sure pt can administer drugs correctly, is complying and avoiding environmental triggers
Asthma under control considered to be? (6)
Minimal need for ‘PRN’ SABA
NO acute episodes (visits to ER)
No limitation of activity
No nocturnal episodes
Normal pulmonary functions
Minimal or no drug adverse effects
SUMMARY OF STEPUP APPROACH
As progress in severity of disorder
Increase the strength, dose, duration, and number of drugs used to control the asthma
The toxicity of the drugs increases as you progress in intensity of treatment
ALL patients will have …. SABA available for PRN use
As severity of disorder progresses .. Dose of ICS will increase … and may eventually use SYSTEMIC CS
Bronchodilatory agents (3)
ß2 agonists
Methylxanthines
Anticholinergics
Antiinflammatory agents (3)
Corticosteroids
Inhibitors of mast cell degranulation
Leukotriene antagonists
BRONCHODILATORS - beta2 agonists
Stimulation of beta2 receptors produces bronchodilation
Non-selective agonists ( isoproterenol, epinephrine and ephedrine) also affect the heart
Epi and iso … have short duration; ephedrine is longer but a risk of CNS
BRONCHODILATORS - beta2 agonists
beta2 agonists act as FUNCTIONAL ANTAGONISTS (physiological antagonists) to produce bronchodilation …minimal effects on heart

TOLERANCE ….. Significance controversial
Occurs with systemic effects but minimal on bronchioles
CS can reverse … and often used in combination

Limiting side effects of oral preps …. MUSCLE TREMOR AND TACHYCARDIA
BRONCHODILATORS - beta2 agonists
Chronic use of long acting beta2 agonists in asthma is controversial
Tendency to produce tolerance making emergency use of SABA less effective

Increased risk of cardiovascular problems

Conflict of interest of docs doing studies to promote long term use as being safe
METHYLXANTHINE BRONCHODILATORS
Secondary agents today
Used as adjuncts of _2 agonists and ICS

Lower efficacy than _2 agonists and ICS

Narrow TI ….. Need to use TDM

Work as functional antagonists
METHYLXANTHINE BRONCHODILATORS
Slower acting than short acting beta2 agonists
NOT USEFUL FOR ACUTE ASTHMA ATTACKS!

Used as alternative for Maintenance therapy

Used for long term control and prevention of symptoms … especially NOCTURNAL ASTHMA
METHYLXANTHINE BRONCHODILATORS
Primary drug is THEOPHYLLINE

AMINOPHYLLINE is ethylenediamine complex with theophylline is used most frequently

Theophylline is available in slow release forms for long effects (12 – 24 hours)
METHYLXANTHINE BRONCHODILATORS
MECHANISM OF ACTION:
Primary effect in asthma is bronchodilation
But does have several other effects
Methylxanthines produce effects by:
Inhibiting phosphodiesterase
Blocking adenosine receptors
Altering cellular handling of Ca++
TOLERANCE … does not seem to develop to effects in lung
Primary effects of theophylline
Relax bronchioles
Increase force of diaphragm contraction and decrease fatigue of diaphragm

CNS stimulation
Increase of force and rate of contraction of heart
Increased GI motility and secretions
Mild diuresis
antiinflammatory??
Theophylline (METHYLXANTHINE) interactions
Cimetidine, erythromycin & clarithromycin, ciprofloxacin and fever ….. inhibit theophylline metabolism
Smoking, antiepileptics, and RIFAMPIN induce metabolism of theophylline
METHYLXANTHINE BRONCHODILATORS ADVERSE EFFECTS?
heart and CNS

N & V
CNS stimulation ….. seizures
Anxiety
Tachyarrhythmias
Theophylline
Theophylline has a narrow TI and erratic bioavailability ….. So we need to watch the blood levels!!! TDM

Safe range 5 – 15 µg/ml

Loading dose usually given when therapy is initiated
Theophylline
Useful adjunct to beta2 agonists and ICS

Narrow TI means we have to monitor levels

Often used to control nocturnal episodes
Not useful with an acute asthma attack
Bronchodilators - ANTICHOLINERGICS
Use in asthma is pretty limited

A secondary rescue drug ..
Most effective in cases where significant cholinergic mediated bronchoconstriction
Most useful in chronic bronchitis and COPD
Systemic effects are minimal due to local application and limited absorption

Ipratropium (Atrovent)
Tiotropium – once a day dosing
antiiflammatory agents CORTICOSTEROIDS
Used both systemically & by inhalation (ICS)
Availability of ICS has been a great advance in asthma management
Able to address inflammation and minimize systemic effects
Used in both allergic rhinitis and asthma
CORTICOSTEROIDS Mechanism
Act on intracellular receptors to change gene product expression
Reduce inflammation and edema
Suppress allergic responses
Potentiate beta adrenergic agents by enhancing cAMP production and up regulating receptor level
Decrease production of PGs and LTs by inhibiting arachidonic acid formation

NO DIRECT EFFECT ON MUSCLE TENSION
SYSTEMIC CORTICOSTEROIDS
Used in severe asthma episodes
Primary SYSTEMIC agents:
Prednisone
Prednisolone
Methylprednisolone
Oral for 10 days to control severe asthma
Alternate day therapy (ADT) if used longer .. To avoid adrenal suppression
CORTICOSTEROIDS .. USED SYSTEMICALLY FOR AN EXTENDED PERIOD MAY CAUSE:
Adrenal suppression
Osteoporosis
Muscle wasting
Growth suppression
Diabetes
Cushings syndrome
INHALED CORTICOSTEROIDS
Are not effective in ACUTE asthma attacks
Usually added to drug regimen when _2 agonists alone are not adequate to control asthma
Have minimal side effects because given locally
Unpleasant taste
Hoarseness and weakness of voice (atrophy of vocal cords)
ORAL CANDIDIASIS
INHALED CORTICOSTEROIDS INCLUDE: (5)
beclomethasone (Beclovent)
triamcinolone (Azmacort)
flunisolide (Aerobid)
fluticasone (Flovent)
butesonide (Pulmicort)
Combined use of Long acting beta2 agonists (LABA) and ICS
Address both bronchoconstriction and inflammation
beta2 agonists address early phase
ICS address late phase
Inflammatory mediators make tissue more responsive to other mediators
Combined use of Long acting beta2 agonists (LABA) and ICS
Potentiation
Combined with _2 agonists, dose of ICS needed is less
ICS up regulate _2 receptors making tissue more responsive

Compliance ….Improved compliance when the two agents are combined in same product dispenser
ADVAIR DISKUS – fluticasone + salmeterol
inhibitors of Mast cell degranulation CROMOLYN
Used prophylactically in allergic rhinitis and asthma
May take a couple of weeks for full effectiveness … soooo not useful for acute asthmatic attacks

Not a bronchodilator
Inhibits release of histamine from mast cells
CROMOLYN
Adjunctive agent
May serve as alternative to ICS or added to reduce the dose of ICS needed
May be useful to help decrease frequency of nocturnal episodes
No tolerance
Primary adverse effect…. May cause coughing when inhale powder
NEDOCROMIL similar to Cromolyn
LEUKOTRIENE PATHWAY INHIBITORS
LTs are mediators of asthma

Produced as lipoxygenase acts on arachidonic acid
LEUKOTRIENE PATHWAY INHIBITORS
LTs produced by lots of inflammatory cells in airways
Basophils mast cells eosinophils macrophages

LTB4 …. a chemoattractant LTC3 & LTD4 produce:
Bronchonstriction increased bronchial reactivity
Mucosal edema mucous hypersecretion
LEUKOTRIENE PATHWAY INHIBITORS
Interfering with actions of LTs or their production is a sound approach to treating asthma
Three main agents:
zileuton ….. A lipoxygenase inhibitor
zafirlukast … LTD4 receptor inhibitor
montelukast …. LTD4 receptor inhibitor
LEUKOTRIENE PATHWAY INHIBITORS
All three are orally effective … but less so than ICS …. Zileuton the least effective

Not effective in acute asthma …

Aspirin-sensitive asthmatics (~ 10% of asthma population) are much more responsive
Zileuton and zafirlukast inhibit P450 metabolism of warfarin
LEUKOTRIENE PATHWAY INHIBITORS
Adverse effects
Churg – Strauss syndrome*
Montelukast
Zafirlukast

Hepatotoxic potential for all three
ANTIHISTAMINES
1ST generation aren’t very useful … and some suggest to avoid them cause they tend to dry secretions to aggravate asthma

2nd generation don’t have that problem …. desloratadine has shown potential utility in asthma (antiinflammatory effects)
IMMUNOSUPPRESSANTS
Might be used in steroid-resistant asthmatics
Inhibiting the immune system plasma cells may reduce inflammation process
Marginally successful but high risks of toxicity
Methotrexate
Cyclosporine
IMMUNOSUPPRESSANTS

Omalizumab (Xolair)
Omalizumab (Xolair)
Anti-IgE antibody
Targeted against portion of IgE molecule that binds to its receptors on Mast cells.
Prevents IgE from interacting with cell surface receptors
ASTHMA PATIENT MANAGEMENT
PATIENT EDUCATION

CONTROLLING FACTORS CONTRIBUTING TO ASTHMA SEVERITY

PHARMACOLOGICAL THERAPY
FYI CHURG – STRAUSS SYNDROME
One of many forms of vasculitis (inflammation of vessels)

Occurs in pts with history of asthma or allergy

Angiitis in lungs, skin, nerves, abdomen

Cause unknown …. But overactivity of immune system suspected

Involves … fever, weight loss, sinus inflammation in asthmatics, cough shortness of breath, numbness and weakness of extremities, seizures