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46 Cards in this Set

  • Front
  • Back
3 Reasons to use resp meds
Bronchoconstriction
inflammation
mucous production
Beta II Selective Agonist: Mechanism of Action
Stimulate B2 adrenergic receptors producing smooth muscle relaxants, mast cell stabilization, and skeletal muscle stimulation
Beta II Selective Agonist: Rescuer or Long acting?
Rescuer
Beta II Selective Agonist: Adverse Effects
Tachycardia due to baroreceptor reflex because of drop in BP from smooth muscle relaxation and direct stimulation of cardiac B2 receptors.
(increased heart rate)

Increased heart rate may increase myocardial o2 demand

Use with caution in heart disease, use b2 sel ago, no reason to use non-sel agents

Hyopkalemia may result from B2 stim in liver (glyconeogensis) which increase insulin secretion and drives K+ intra cellularly

cough due to bronchospasms not mucus production (hence antitussive won't stop coughing)
Short Acting B2 Agonist: Uses
Mostly used as inhaler but can be used as nebulizer
Short Acting B2 Agonist: I.E.
albuterol (Ventolin, proventil)
most common: levoalbuterol (Xopenex)
Short Acting B2 Agonist: Action
Provides quick relief of intermittent episodes of bronchospasm but should only be used as needed.

Used in acute severe asthma

Max 2 puffs QID

Exercise induced asthma onset 10-15 minutes and provides protection for approx 2 hrs.
New Long acting b2 Agonists
arformoterol (Brovana)
formoterol (Performomist)
Solutions for nebulizer use, used for those who can't use inhalers
Long Acting B2 Agonist: Uses
Maint therapy
Controller
Ineffective for acute severe asthma - onset of action is 20 min and may take 1-4 hours for max bronchodilation

Exercise induced asthma provides protection for 8-12 hours.

Must be taken on scheduled basis Q12H
Long Acting B2 Agonist: I.E.
salmeterol (Serevent) inhaler most common; 2 puffs QID hours

Advair diskus 100/50, 250/50, 500/50 is fluticasone proprionate (steroid) + salmeterol (dry powder) for inhaler daily
FDA 2006 LABA Black Box Warning
salmeterol xinafoate inhalation powder (Serevent)

fluticasone propionate and salmeterol inhalation powder (Advair)

formoterol fumarate inhalation powder (Foradil Aerolizer)

LABA may increase the chance of severe asthma episodes and death when they occur
FDA 2006 LABA Black Box Warning: Guidelines
Not first line treatment of asthma

Do not stop without consulting HCP

Do not use if wheezing gets worse

LABA does not relieve sudden wheezing

Always having a short acting bronchodilator avail (rescuer)
Steroid effects
Inflammation r/t steriods
inhale or oral
inhale > oral due to systemic effects
Symbicort:
Combination of corticosteroid (Pulmicort) and long-acting beta-agonist formoterol (Foradil)
Symbicort: Indications
Maintenance therapy of asthma not adequately controlled with corticosteroid alone

2 puffs BID
Anticholinergic Agents: Uses
May provide additive benefit to inhaled B2 agonists in acute exacerbations but are not first line drugs.

Alternative for those who cannot use B2 Agonists
Anticholinergic Agents: I.E.
ipratropium bromide (Atrovent)

tiotropium bromide inhalation powder (SPIRIVA Handihaler)
Anticholinergic Agents: Contraindication
allergy to atropine, soya lecithin peanut or related food
Anticholinergic Agents: Adverse Effects
Nervousness
dizziness
palpitations
cough
Inhaled Corticosteroids: Routes
Inhaled rather than oral because less systemic effects

Nasal acts on nasal mucosa
Inhaled Corticosteroids: Mechanisms of Action
Interference with arachidonic acid metabolism and synthesis of leukotrienes and prostaglandins; reduce vascular permeability which decrease edema; prevent migration of inflammatory cells.
Inhaled Corticosteroids: Uses
Most effective anti-inflammatory agents for the treatment of asthma

Anti-inflam agent of first choice in persistent asthma

Use lowest effective dose to avoid side effects

Use with spacer device to decrease side effects and increase lung deposition

Rinse mouth to decrease topical side effects
Inhaled Corticosteroids: Adverse Effects
Topical -- oral candidiasis, hoarseness

Systemic -- the inhaled dose where systemic absorption is unknown
suppression of serum cortisol occurs at dosages

possibly stunts growth
Inhaled Corticosteroids: Dosages
>1500 mcg in adults

>800mcg in children
Inhaled Corticosteroids: Selection
Depends on asthma classification and severity
potency
compliance and number of puffs per dose

cost
Inhaled Corticosteroids: I.E.
fluticasone (Flovent)

triamcinolone (Azmacort)

budesonide (Pulmocort)

flunisolide (Aerobid)

beclomethasone dipropionate (Vanceril, Beclovent)

Dosages vary from daily to QID
Mast Cell Stabilizer: Mechanism of Action
Mast cell stabalization

INhibit in vitro activation of human neutrophils, macrophages, and eosinophils

Inhibit neurally mediated bronchoconstriction do not have bronchodilatory effects
Mast Cell Stabilizer: I.E.
cromolyn sodium (Intal)
nedocromil sodium (Tilade)
Mast Cell Stabilizer: Uses
Maintenance therapy early in mild persistent asthma, particularly for allergy component

Prophylaxis of chronic asthma

May be used in conjunction with B2 agonists for prevention of exercise induced asthma

Due to efficacy and safety may be used in children

Efficacy r/t lung deposition

May take up to 1-2 weeks to achieve effects and max benefit

Start with inhalations QID until symptoms stabilized and reduced to BID or TID
Mast Cell Stabilizer: Adverse Effects
Side Effects minimal due to no systemic absorption

Cough / wheeze reported with dry powder inhalation of cromolyn

Bad taste and headache reported with inhalation of nedocromil
Theophyllines and Derivatives: Mechanism of Action
Thought to have bronchodilator effects due to inhibition of release of intracellular calcium

competitive antagonist of the bronchoconstrictor adenoside.

Inhibits pulmonary edema by decreasing vascular permeability

Enhances mucociliary clearance

Strengthen contraction of the diaphragm

stims adrenergic system
Theophyllines and Derivatives: Classification
Methylxanthine Drugs
Theophyllines and Derivatives: Adverse Effects
Chronotropic and inotropic cardiac effects

Stimulates CNS and produces cerebral vasoconstriction

Decreases lower esophageal sphincter pressure and increases gastric acid secretion

Must monitor serum concentrations!
Theophyllines and Derivatives: Uses
Limited use due to side effects and safer more effective B2 Agonists and anti-inflammatories but 2006 making a come back

Used to be given by drip IV under close supervision in acute care settings for control of asthmatic episodes, may still be used if severe (aminophylline)
Theophyllines and Derivatives: I.E.
theophylline (Theo-24, theo-dur, Uniphyl)
Leukotriene Modifiers: Actions
Increase vasular permeability leading to edema formation

Cause bronchoconstriction

Recruit inflam mediators (eosinophils) to airway tissues

Decrease mucociliary transport
Leukotriene Modifiers: Accolate
zafirlukast
Leukotriene receptor antagonist inhibits the early and late phase response after allergen challenge; long term control or prevention of episodes of bronchospasm. Third line drugs

Rapidly absorbed after oral administration (max 3 hrs)

Food decreases bioavailability by 40%

Half life 8-10 hrs (given PO bid)
Leukotriene Modifiers: Singulair
montelukast (most common)

leukotriene receptor antagonist similar to zafirlukast but once per day oral dosing, also chewable. Not for primary treatment of acute attack
Leukotriene Modifiers: Singulair Adverse Effects
headache
gastritis
pharyngitis
rhinitis
GI upset
myalgias
fever
Leukotriene Modifiers: Singulair Drug interactions
zafirlukast potentiates warfarin (Coumadin) drugs that induce CYP450
Leukotriene Modifiers: Singulair I.E.
erythromycin, rifampin, asparin (decrease concentration)
Leukotriene Modifiers: Ziflo
zileuton
5-lipoxygenase inhibitor, inhibits early and late phase response after allergen challenge

Rapidly absorbed food does not affect bioavailability

Metabolized via CYP450 isoenzymes 1A2, 2C9, 3A4

Not for acute exacerbations
Leukotriene Modifiers: Adverse Effects
headache, dyspepsia

Increases alanine aminotransferase (ALT) need to monitor liver enzymes at baseline & Q3 Months
Leukotriene Modifiers: Drug interactions
warfarin (increase INR)
propanolol (increase beta blocker activity)

theophylline (increase concentrations)
Asthma and GERD
GERD may worsen with asthma symptoms in some

If asthma symptoms increase after meals and are non responsive to tradition treatment, then GERD may be driving asthma

May need to add PPI
I.E. Protonix, prolosec, prevadic

GERD + Astham = Worse Asthma