Asthma

Question 1

Albuterol (ProAir, Ventolin, Proventil)

Answer 1

Short acting Beta2-adrenergic Agonists (SABA)
Used extensively in infants & children
Absorption: bronchi, systemic concentration low
Metabolism & Excretion: Liver and urine

Question 2

Levalbuterol (Xopenex)

Answer 2

Short acting Beta2-adrenergic Agonists (SABA)

In theory, this med may have less side effects because it is missing the S isomer that is associated with tachycardia. The R isomer causes bronchodilation. Albuterol is a mixture of R and S isomers and Levalbuterol only contains the R-isomer. However, the evidence is inconclusive whether there are fewer side effects with Levalbuterol. We prescribe this drug for older pts, but it costs $$ more than albuterol.

Question 3

Metaproterenol (Alupent)

Answer 3

Short acting Beta2-adrenergic Agonists (SABA)

Question 4

Terbutaline (Brethine, Brethaire)

Answer 4

Short acting Beta2-adrenergic Agonists (SABA)

Preg category B, others C

Question 5

Bitolterol (Tornalate)

Answer 5

Short acting Beta2-adrenergic Agonists (SABA)

Question 6

Pirbuterol (Maxair)

Answer 6

Short acting Beta2-adrenergic Agonists (SABA)

Question 7

Multidose Inhaler (MDI)

Answer 7

MDI is the inhaler that contains a solution (what we usually see). The problem is that it can be challenging for patients who have difficulty with coordinating their hand/ breath- a spacer can help. These pts may miss getting in the drug.

Question 8

Dry Powder Inhaler (DPI)

Answer 8

DPI contains solid particles and depends on the inspiratory effort of the patient. The nice thing is that the pt can breathe in again if they didn’t get the med in. If the pt can suck water through a straw, then s/he can use a DPI. Pts with severe lactose allergy may react to respiratory drugs in DPI form because the large particles are bound to lactose (e.g., Spiriva HandiHaler, etc.)

Question 9

Short Acting Beta2-adrenergic Agonists (SABA)

Answer 9

MOA:
act on smooth muscle of bronchial tree to reverse bronchospasm
Adverse events:
tachycardia, palpitations, tremors, dizziness, restlessness, H/A
Drug Interactions:
Digitalis glycosides, beta blockers, TCA, MOIs
Cautions:
ischemic heart disease, CHF, stroke, hypertension, cardiac arrhythmias, seizure disorder, hyperthyroidism

Question 10

Salmeterol (Serevent)

Answer 10

Long Acting Beta2-adrenergic Agonists (LABA)

Administered via inhaler: Absorption: bronchi, systemic concentration low

Question 11

Formoterol (Foradil)

Answer 11

Long Acting Beta2-adrenergic Agonists (LABA)

Inhaled dry powder administered via aerolizer inhaler

Question 12

Indacaterol (Arcapta Neohaler)

Answer 12

Long Acting Beta2-adrenergic Agonists (LABA)

Question 13

Arformoterol (Brovana)

Answer 13

Long Acting Beta2-adrenergic Agonists (LABA)

Question 14

Long Acting Beta2-adrenergic Agonists (LABA)

Answer 14

MOA:
Act on smooth muscle of bronchial tree to reverse bronchospasm
Adverse events:
tachycardia, palpitations, tremors, dizziness, restlessness, h/a
Drug Interactions:
Digitalis glycosides, beta blockers, TCA, MOIs
Cautions:
ischemic heart disease, CHF, stroke, hypertension, cardiac arrhythmias, seizure disorder, hyperthyroidism
Black Box warning (Salmeterol and Formoterol): Do not use as single agent
Contraindicated without use of other controller med (ICS)
Long term use only when other controllers have failed adequate control
Use shortest duration
Pediatrics: only use combination product (ICS + LABA)

Question 15

Beclomethasone dipropionate (QVAR)

Answer 15

Inhaled Corticosteroids (ICS)

Question 16

Triamcinolone acetonide (Azmacort)

Answer 16

Inhaled Corticosteroids (ICS)

Question 17

Budesonide (Pulmicort)

Answer 17

Inhaled Corticosteroids (ICS)

Question 18

Flunisolide (Aerobid)

Answer 18

Inhaled Corticosteroids (ICS)

Question 19

Mometasone furoate (Asmanex Twisthaler)

Answer 19

Inhaled Corticosteroids (ICS)

Question 20

Fluticasone (Flovent)

Answer 20

Inhaled Corticosteroids (ICS)

Question 21

Ciclesonide (Alvesco)

Answer 21

Inhaled Corticosteroids (ICS)

Question 22

Inhaled Corticosteroids (ICS)

Answer 22

MOA:
anti-inflammatory, inhibit the IgE and mast cell-mediated migration of inflammatory cells into bronchial tissue
Adverse events:
xerostomia, hoarseness, tongue/mouth irritation, oral candidiasis
Drug Interactions:
Ritonavir increases fluticasone, ketoconazole and fluticasone/budesonide
Cautions:
potential decrease in linear growth in children, ocular HSV, tuberculosis, oral or nasal surgery or trauma, healing nasal septal ulcers, untreated resp infection. Avoid in Cushing’s syndrome.
Please note that we advise patients to rinse their mouth after an ICS inhaler to avoid thrush in mouth and pharynx (oropharyngeal candidiasis and dysphonia).

Question 23

Zafirlukast (Accolate)

Answer 23

Leukotriene receptor antagonists (LTRA) (Leukotriene Modifiers)

Question 24

Montelukast (Singulair)

Answer 24

Leukotriene receptor antagonists (LTRA) (Leukotriene Modifiers)

Question 25

Leukotriene receptor antagonists (LTRA) (Leukotriene Modifiers)

Answer 25

MOA: Block binding of leukotrienes to the receptor, prevent leukotriene-modulated bronchospasm; may also have anti-inflammatory properties Cautions: not for acute episodes, breast feeding, may need lower doses in liver disease Adverse events: elevated liver enzymes (zafirlukast), h/a, N/D, abd pain, insomnia Drug interactions: multiple with zafirlukast

Question 26

Zileutin (Zyflo)

Answer 26

Leukotriene Synthesis Inhibitor MOA: inhibits 5-lipoxygenase, interfering with leukotriene formation Cautions: Not recommended for children, over age 12 only; contraindicated in acute liver disease Adverse events: hepatotoxicity, behavioral disturbance, hypersensitivity Drug interactions: Many (CYP1A2 substrate, CYP3A4 substrate) Evaluate liver function prior to initiating therapy and routinely

Question 27

Mast Cell Stabilizers

Answer 27

MOA: inhibits mast cell degranulation, thus decreasing bronchial hyperactivity Adverse events: transient bronchospasm, cough, unpleasant taste, throat irritation Cautions: not used in acute episodes or status asthmaticus, caution if arrhythmias

Question 28

Cromolyn (Intal)

Answer 28

Mast Cell Stabilizer

Question 29

Neodocromil (Tilade)

Answer 29

Mast Cell Stabilizer

Question 30

Theophylline

Answer 30

Methylxanthines MOA: unknown mechanism mediated by selective inhibition of PDEs; dilates pulmonary blood vessels Adverse events: Toxicity Some pts with seizures 15 to 20 mcg/mL CNS: Irritability, restlessness, seizures, insomnia GI: reflux, heartburn Cardiac: palpitations, tachycardia, hypotension, arrhythmias

Question 31

Theophylline Toxicity

Answer 31

Toxicity >20 mcg/mL: N/V/D, H/A, insomnia, & irritability Toxicity > 35 mcg/mL: hyperglycemia, hypotension, arrhythmias, tachycardia, seizures, brain damage, death

Question 32

Theophylline Drug interactions

Answer 32

Many due to metabolism through CYP 450 Smoking increases clearance Benzodiazepines are antagonized Beta agonists may cause additive toxicity Reduced lithium level Low-carb/high protein diet increases clearance (ex: Atkins diet) Charcoal-broiled foods accelerate metabolism

Question 33

Theophylline Contraindications/cautions:

Answer 33

Monitor pts: HTN, HD, CHF, h/o stroke and arrhythmia Monitor for toxicity Prolonged clearance & half life with neonates and elderly

Question 34

Omalizumab (Xolair)

Answer 34

Immunomodulator MOA: Inhibits IgE binding to mast cells and basophils, decreasing mediator release Adverse events: Black box warning: anaphylaxis, cardiovascular & cerebrovascular event risk, injection site rxn, URI sx, migraine/ha Cautions: acute bronchospasm, status asthmaticus, caution if anaphylaxis hx Indicated for pts with moderate to severe persistent asthma with proven sensitivity to a perennial aeroallergen and symptoms that are inadequately controlled with inhaled corticosteroids

Question 35

Prednisone

Answer 35

Oral systemic Steroids MOA: Inhibit release of inflammatory mediators, decrease mucous secretion, upregulate beta-adrenergic receptor numbers Contraindications: untreated infection, chronic use in lactation, alcohol dependence; Caution: Diabetics Adverse events: Psychosis, peptic ulcers, hyperglycemia, elevated BP, edema, bruising Interactions: OCs may block metabolism, increased risk of tendon rupture with combined with fluoroquinolones, decreased effectiveness of phenytoin, phenobarbital, rifampin Clinical use: Used for acute episodes not controlled with SABAs; More than 3 courses in a year indicates poor control of asthma (see dosage in exacerbation slide)

Question 36

Step Therapy for Asthma Pts 12 yrs and older

Answer 36

Step 1: SABA prn Step 2: Low dose ICS (or cromolyn, LTRA, theophyline) Consider desensitization Step 3: Low dose ICS + LABA or Medium dose ICS or Low dose ICS + LTRA/ theophyline/zileutin Step 4: Medium dose ICS + LABA or Medium dose ICS + LRTA/theophyline/zileutin Step 5: Change to high dose ICS + other med Consider omalizumab Step 6: add oral steroid

Question 37

“Rule of Twos” to measure control

Answer 37

Rescue inhaler more than 2 times/week Night time symptoms more then 2x/month Refill rescue inhaler more than 2x/year Peak flow over 20% less than baseline with symptoms

Question 38

Combivent

Answer 38

Ipratropium + albuterol (Combivent) is a second line quick relief medication in the treatment of asthma,

Question 39

Special populations: Pregnancy

Answer 39

Inhaled beta-agonists are drug of choice | Inhaled corticosteroids are the long-term DOC