asthma

s/s - sense of breathlessness, tightness in chest, w/ wheezing, dyspnea (shortness of breath) & cough

sometimes caused by allergies. In most cases don't know cause

chronic inflammatory airway d/o

cause immune mediated airway inflammation

bronchoconstrictions

resulting in spasms & activation of inflammatory cells w/ airway inflammation & edema, excessive mucus secrections & plugging, smooth muscle atrophy, all resulting in obstruction of airflow

in addition inflammation causes bronchial hyper reactivity to mild triggers (cold air, exercise, smoke)

metered-dose inhalers (MDI's)

1 to 2 puffs, 1 minute between puffs

start inhaling before activation

delivers 10% to lungs; if spacer is used - 20% delivered

propellants

CFC - off market by 12/2013 due to ozone damage

HFA - hydrofluralkanes

dry-powder inhalers (DPI's)

breath-activated

delivers 20% to lungs more than MDI alone

nebulizer (SVN - small volume nebulizer)

creates a mist

delivered by face mask or mouth piece

several minutes to deliver a 1 puff MDI equivalent

budesonide (Pulmicort)

fluticasone propionate (Flovent)

prophylaxis anti-inflammatory (long term tx):

"inhaled glucocorticoid"

suppresses inflammation, reducing bronchial hyperreactivity; ↓ airway mucus production; ↑ # of bronchial beta2 receptors & their responsiveness to beta2 agonist

Route: inhaled

Use: prophylaxis of chronic asthma (fixed schedule(daily, BID, etc), not PRN)

Effect: ↓ intensity & frequency of asthma attacks

AE: oropharyngeal candidiasis (thrush), dysphonia (horse voice)(lessened w/ use of spacer); slow growth in children & adolescents; prolonged therapy - risk of bone loss, cataracts & glaucoma

prednisone

prednisolone

prophylaxis anti-inflammatory (long term tx):

"oral glucocorticoid"

similar in action to inhaled glucocorticoids

Route: PO

Use: prophylaxis of asthma

Effect: ↓ intensity & frequency of asthma attacks

AE: adrenal suppression; osteoporosis; hyperglycemia; peptic ulcer disease (PUD); suppression of growth (youth)

zileuton (Zyflo)

prophylaxis anti-inflammatory (long term tx):

"leukotriene modifier"

inhibits leukotriene synthesis (leukotrienes promote bronchoconstriction, mucus production & airway edema)

Route: PO

Use: prophylaxis & maintenence therapy for asthma

Effect: ↓ bronchoconstriction, inflammation, mucus & edema

AE: hepatotoxicity to symptomatic hepatitis (reversible) - monitor LFT's (liver function tests); neuropsychiatric effects (depression, anxiety, agitation, abnormal dreams, hallucinations, insomnia, irritiability, restlessness, SI (suicidal ideation))

DD: ↑ theophylline levels; ↑ warfarin levels; ↑ propranolol levels (↓ BP, ↓ HR)

zafirlukast (Accolate)

prophylaxis anti-inflammatory (long term tx):

"leukotriene modifier"

leukotriene antagonist

Route: PO (1 hr AC or 2 hr PC)

Use: maintenance therapy for chronic asthma

Effect: reduced filtration of inflammatory cells; ↓ bronchoconstriction

AE: rare - liver injury; common - HA; GI disturbance & some incidence of neuropsych s/s - both infrequent

DD: ↑ theophylline & warfarin levels

montelukast (Singulair)

prophylaxis anti-inflammatory (long term tx):

"leukotriene modifier"

leukotriene antagonist

Route: PO

Use: maintenance therapy for asthma, use in exercise induced asthma

Effect: ↓ asthma-related nocturnal awakening (take at HS); ↑ morning lung function; ↓ need for inhaled beta2 agonists

AE: no hepatotoxicity

DD: none noted at this time

cromolyn (Intal)

prophylaxis anti-inflammatory (long term tx):

"mast cell stabilizer"

prevents histamine release from mast cells, ↓ inflammation

Route: MDI; nebulizer

Use: prophylaxis for moderate asthma; ineffective for ongoing attack; use prior to allergen exposure; exercise-induced bronchospasm; allergic rhinitis (inflammation of the nasal passage)

Effects: ↓ frequency/intensity of asthma attacks

AE: safest antiasthmatic

omalizumab (Xoliar)

prophylaxis anti-inflammatory (long term tx):

"monoclonal antibody"

antagonizes IgE; limits the ability of allergens to release histamine

Route: SC

Use: second line agent for allergy related asthma; last resort

AE: injection site irritation (45%), viral infections (23%), URI(upper respiratory infection)(20%), sinusitis (inflammation of the sinus), HA, pharyngitis (inflammation of the pharynx); also a risk for anaphylaxis, cancer

used in pts > 12 yrs of age

albuterol (Proventil), levalbuterol (Xopenex), pirbuterol (Maxair)

acute attack tx bronchodilators (short term tx):

"beta2-adrenergic agonist"

short acting beta agonist (SABA)

Route: inhaled (immediate onset, 30-60 min peak)

Action: simpathomimetic (stimulates resp); stimulates beta2 receptors in smooth muscle (bronchodilation); suppresses histamine release; ↑ ciliary motility

Use: quick relief of ongoing asthma attack & long term control; used prior to exercise as prophylaxis

Effect: bronchodilation, relieves bronchospasm

AE: systemic effects (tacycardia, angina, tremor), aggravated in excessive dosages

formoterol (Fordil), arformoterol (Brovana)

acute attack tx bronchodilators (short term tx):

"beta2-adrenergic agonist"

long acting beta agonist (LABA)

Route: PO

Action: simpathomimetic (stimulates resp); stimulates beta2 receptors in smooth muscle (bronchodilation); suppresses histamine release; ↑ ciliary motility

Use: quick relief of ongoing asthma attack & long term control; used prior to exercise as prophylaxis

Effect: bronchodilation, relieves bronchospasm

AE: tremors, may activate beta1 receptors in heart; angina, tachy dysrhythmia

theophylline (Theo-24)

"methylxanthine"

bronchodilation by relaxing bronchi smooth muscle

Route: PO (used for chronic asthma), IV (acute attack)

Use: maintenance therapy of chronic stable asthma

Effect: ↓ intensity & frequency of asthma attacks; appropriate for nocturnal attacks r/t prolonged effects when used regularly

AE: at 20-25 mcg/mL - GI (N, V, diarrhea); insomnia; restlessness

Toxcity: above 30 mcg/mL - severe dysrhythmias (v. fib), convulsions; death from cardiorespiratory collapse. 

DD: caffeine - intensifies AE of theophylline; cimetidine (Tagamet), fluoroquinolone antibiotics - ↑ levels of theophylline; phenobarbital, phenytoin, rifampin - ↓ levels of theophylline

aminophylline

"methylxanthine"

theophylline salt; more soluable than theophylline - in solution, becomes theophylline

1 aminophylline = 2 theophylline (dose differently)

monitor frequently; therapeutic reange 10-20 mcg/mL

ipratropium (Atrovent) - short acting

tiotropium (Spiriva) - long acting

anticholinergic:

"atropine derivative"

bronchodilator, relieves bronchospasm in COPD; used in asthma

Route: MDI (Atrovent) - onset 30 seconds; spinhaler (Spiriva)

Use: allergen-induced asthma; exercise-induced bronchospasm (less effective than beta2 agonist, additive effect w/ beta2 agonist)

Effect:  bronchodilation

AE: dry mouth, irritation of pharnyx; raise intraocular pressure in glaucoma pts

fluticasone/salmeterol (Advair)

"glucocorticoid/LABA combination"

anti-inflammatory and bronchodilation

Use: long term maintenance - reserved for pts not adequatly controlled w/ inhaled glucocorticoid, not initial therapy

fixed dose combinations

AE: none

allergic rhinitis

inflammatory d/o of the upper airway, lower airway and eyes

s/s: sneezing, rhinorrhea (runny nose), conjuctivitis, sinusitis, asthma; secondary to histamine, leukotriene & prostagliandin release (response to allergies)

hay fever; perennial rhinitis (indoor allergens)

beclomethasone (Beconade)

"intranasal glucocorticoid"

anti-inflammatory

Route: intranasal

Use: seasonal & perennial rhinitis

Effect: suppresses major s/s of allergic rhinitis - congestion, rhinorrhea, sneezing, nasal pruritis & erythema

AE: drying of nasal mucoas; sensation of burning or itching (r/t vehicle), sore throat, epistaxis (severe nose bleed), HA

diphenhydramine (Benadryl)

"antihistamine"

histamine receptor antagonist

Route: PO

Use: prophylaxis for allergic rhinitis & allergic reaction

Effect: relieve sneezing, rhinorrhea, nasal pruritis; no ↓ in nasal congestion

AE: sedation, anticholinergic effects (dry mouth, C , urinary hesitancy)

cromolyn sodium (NasalCrom)

"intranasal mast cell stabilizer"

suppressess histamine release from mast cells

Route: intranasal

Use: prophylaxis - prevent allergic rhinitis

Effect: relieve s/s of allergic rhinitis

AE: minimal

phenylephrine (Neo-synephrine), pseudo ephedrine (Sudafed)

"decongestant (sympathomimetic)"

stimulates alpha-adrenergic receptors on nasal blood vessels, causes vasoconstriction shrinking swollen membranes

Route: intranasal drops/spray, PO (Sudafed)

Use: only relieves stuffiness in allergic rhinitis, no other symptom relief

Effect: reduce congestion

AE: intranasal (rebound congestion - limit to 3-5 days use); oral (CNS stimulation - restlessness, irritability, anxiety, insomnia; CV effects - vasoconstriction (hazardous in pts w/ HTN or CAD); abuse potential r/t CNS stimulation

montelukast (Singulair)

leukotriene antagonist

Route: PO

Use: seasonal & perennial allergic rhinitis

Effect: ↓ nasal congestion

AE: rare - neuropsychiatric (agitation, aggression, hallucination, depression, insomnia, restlessness, SI

last drug of choice due to AEs

codiene (Paveral), hydrocodone (Hycodan)

"opioid antitussive(cough)"

CNS elevation of cough threshold

Route: PO (doses are about 1/10 of those used in pain relief)

Use: cough suppressant

Effect: reduce frequency & intensity of cough

AE: respiratory suppression (do not use w/ nocturnal apnea); abuse potential (Schedule II - codeine alone; Schedule V for codeine in antitussive mixtures)

dextromethorphan (Drixoral, Pertussin, Robitussin DM)

"nonopioid antitussive"

raise cough threshold in CNS

Route: PO

Use: cough suppressant

Effect: reduce frequency & intensity of cough; enhance analgesic effects of opioids (doubles morphine's analgesia)

AE: minimal (no euphoria or dependence; no resp depression)

benzonatate (Tessalon)

"nonopioid antitussive"

derivative of tetracaine & procaine; ↓ sensitivity of resp tract stretch receptors

Route: PO capsules (cannot be opened or crushed)

Use: cough suppressant

Effect: reduce frequency & intensity of cough

AE: mild sedation, dizziness; C

expectorant

agent that stimulates the flow of respiratory secretions to yield a "productive" cough

guaifenesin (Musinex, Humbid)

mucolytic

acts directly w/ mucus to make it "watery" and make cough more productive

acetylcysteine (Mucomyst) - nebulizer; hypertonic saline (3%)

caution: both mucolytics can cause bronchospasm