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Short Acting Beta 2 Adrenergic Agonists
- Albuterol (Proventil)
- Bitolterol (Tornalate)
- Levalbuterol (Xopenex)
- Pirbuterol (Maxair)
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Long Acting Beta 2 - Adrenergic Agonists
- Formeterol (Foradil Aerolizer)
- Salmeterol (Serevent Diskus)
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Oral Beta 2 - Adrenergic Agonists
- Albuterol (Proventil, Volmax)
- Terbutaline (Brethine)
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Beta 2 - Adrenergic Agonist
Mechanism of Action
- Selectively activate beta 2 adrenergic receptors in smooth muscle of the lung
- 1. causes bronchodilation
- Supresses histamine release
- Increases ciliary motility
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Long Acting & Oral - Beta 2 Adrenergic Agonists
- Last up to 12 hrs
- Prolonged prophylaxis only
- Should never be used alone to prevent asthma related death
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Beta 2 Adrenergic Agonists - Adverse Effects
tachycardia, angina, tremor
Long Acting - can cause respiratory arrest, death, severe asthma
Oral - dysrythmias
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Inhalers
- Metered Dose
- Dry Powder
- Nebulizers
- Metered Dose:
- 1 minute interval
- Administer Short acting Beta 2 Agonist before glucocorticoids
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Methylxanthines
- Theophylline oral - Theolair
- Theophysine IV - emergencies
- Aminophylline (IV) - Truphylline
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Theophylline (oral and IV)
- Relaxes smooth muscle causing bronchodilation
- Maintenance therapy for chronic, stable asthma
- Decreases frequency and severity (though less effective)
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Theophylline & Theophylline SR - absorption
- Do not chew SR (sustained release)
- SR more stable plasma level
- SR affected by food
- Metabolized in liver
- 10-20 mcg/ml plasma drug level
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Theophylline - Toxicity
- Drug levels between 20-25 mcg/ml
- Nausea / Vomiting
- Diarrhea
- Insomnia
- Restlessness
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Theophylline - drug interactions
- Caffeine
- Phenobarbital
- Phenytoin
- Rifampin
- Fluoroquinolone antibiotics (Cipro, Levaquin, Avelox)
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Theophylline
Usual adult dose: 200-300 mg, 2-3 times / day
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Anticholinergics
- Ipratropium (Atrovent HFA)
- Tiotropium (Spiriva)
Both inhaled
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Ipratropium (Atrovent)
- Blocks muscarcinic receptors in bronchi
- Used for COPD
- Less effective for asthma
- Additive effects with Beta 2 agonists
- Not for acute attacks
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Ipratropium (Atrovent) - Adverse Effects
- Common: Dry mouth, irritation of pharynx
- Rare: increase in intraoccular pressure in patients with glaucoma, urinary retention
Contraindicated in those allergic to soy / peanuts
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Ipratropium (Atrovent) - dosage
2-4 puffs QID
Combivent or DuoNeb (Combined with Beta 2 agonists - albuterol)
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Tiotropium (Spiriva)
- blocks muscarcinic receptors in lung - bronchodilation
- Long acting, approved for COPD bronchospasm
- Usual dosing: 18 mcg capsules in dry powder inhaler
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Tiotropium (Spiriva) - adverse effects
- Most common: dry mouth
- teach to suck on sugarless candy for relief
- Systemic: constipation, urinary retention, tachycardia, blurred vision
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Leukotriene Modifiers
- Montelukast (Singulair)
- Zafirlukast (Accolate)
- Zileuton (Zyflo)
all PO
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Montelukast (Singulair)
- Antiinflammatory - blocks leukotriene receptors
- Not for quick relief
- For all patients over 1 yo
- Once a day dosing (give in evening)
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Montelukast (Singulair) - pharmacokinetics
- Rapidly absorbed: peak in 3-4 hours
- Maximal effects: 24 hrs
- Metabolized in liver, excreted in bile
- Available in standard and chewable tablets, granules
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Montelukast (Singulair) - adverse effects
- CNS: headache, anxiety fatigue
- Resp: cough
- GI: abdominal discomfort, diarrhea, nausea, dyspepsia (heartburn)
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Zileuton (Zyflo)
- Antiinflammatory for > 12 yo
- not for acute asthma
Asthma prophylaxis and maintenance
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Zileuton (Zyflo) - pharmacokinetics
- with or without food
- peak in 2-3 hours
- metabolized in liver
- excreted in urine
- usual dosage: 600 mg QID
- Interacts with theophylline, warfarin, propanolol (Can increase their levels)
- Adverse Effects: Similar to Singulair
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Zafirlukast (Accolate)
- Antiinflammatory
- Use for asthma in > 5 yo
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Zafirlukast (Accolate) - pharmacokinetics
- give 1 hr before meals (or 2 hrs after)
- metabolized in liver
- excreted in feces
- usual dosage: 10-20 mg BID
- interacts with: theophylline, warfarin, propanolol (can increase their levels)
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IgE Antagonist - Omalizumba (Xolair)
- expensive
- antiinflammatory
- unknown long term safety
- for moderate to severe asthma
- > 12 yo
- sub-q absorption
- peak in 7-8 days
- half-life: 26 days
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Omalizumba (Xolair) - adverse effects
- pain at injection site
- upper respiratory infections
- sinusitis
- headache
- cancer & anaphylaxis
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Mast Cell Stabilizers
- Cromolyn (Intal)
- Nedocromil (Tilade)
by inhalation
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Cromolyn (Intal)
- prophylaxis of asthma
- not for acute attack
- exercise induced asthma
- allergic rhinitis
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Cromolyn (Intal) - pharmacokinetics
- full effects may take several weeks
- 2-4 puffs QID (MDI, nebulizer)
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Nedocromil (Tilade)
- Usual dosage: 2 puffs daily, MDI
- Most common adverse effect: unpleasant taste
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Glucocorticoids
- Inhaled
- - Beclometasone
- - Budesonide (Pulmicort)
- - Flunisolide (Aerobid)
- - Flucticasone propionate (Flovent)
- - Triamcinolone acetonide (Azmacort)
- Oral
- - Prednisone, Prednisolone
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Glucocorticoids
- anti-inflammatory
- prophylaxis for asthma
increases beta 2 agonists
cannot be used in times of stress
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Glucocorticoids - adverse effects
adrenal suppresion
Most common: bone loss and adrenal supression
Gargle after use, use spacer
- Infection
- Fluid & Electrolyte imbalance
- Cataracts and glaucoma
- Mood changes
- Cushing's Syndrome
Withdrawl must be done slowly
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Glucocorticoids - acute attacks
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Glucocorticoid / Beta 2 Agonist Combination
- Advair Diskus - flovent & serevent
- Bronchodilation & antiinflammatory
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Glucocorticoid / Beta 2 Agonist Combination
- Therapeutic uses: Asthma & COPD
- 50/100 mcg, 50/250 mcg, 50/500 mcg
- BID inhalation
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Allergic Rhinitis Symptoms
- inflammatory disorder of the airways and eyes
- Symptoms:
- sneezing
- rhinorrhea
- pruritus
- nasal congestion
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Allergic Rhinitis
- Seasonal - outdoor allergens (fungi, pollen)
- Perennial - indoor allergens (dust mites, pet dander)
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Drugs for Allergic Rhinitis
- Oral antihistamines
- Intranasal glucocorticoids
- Intranasal cromolyn
- Sympathomimetics (oral/nasal)
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Oral Antihistamines
- relieve itching, rhinorrhea, sneezine
- NOT congestion
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Oral Antihistamine - adverse effects
- Sedation
- Anticholinergic effects:
- dry mouth, constipation, urinary retention
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Intranasal Glucocorticoids
- antiinflammatory (MDI, QD or BID)
- suppresses symptoms of allergic rhinitis and congestion
- adverse effects:
- drying of nasal mucosa, epistaxis, burning or itching, may suppress adrenal glands
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Sympathomimetics (Decongestants)
- stimulates alpha 1 adrenergic receptors
- adverse effects:
rebound congestion, rebound rhinitis
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Cough Drugs
- Antitussives
- opiod: codeine and hydrocodone
- nonopiod: dextromethorphan and diphenhydramine
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Opiod Antitussives
- Increases cough threshold
- Sedation / Drowsiness
- Dizziness, Fatigue, Dry Mouth, Constipation, Euphoria, Hallucinations, Resp. Depression
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Nonopiod Antitussives
- Dextromethorphan (Robitussin) most effective
- Diphenhydramine
- Benzonatate (Tessalon)
Side Effects: Dizziness, constipation, dry mouth
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