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Pulmonology > Asthma Pharmacology > Flashcards

Asthma Pharmacology Flashcards

1
Q

Chronic Asthma

A
  • Tx based on (1) disease severity and (2) level of control for subsequent therapies
  • Personalized care plans
  • Avoidance of triggers
  • As needed for quick relief medications
    • Short acting beta agonists (SABA)
    • Anticholinergics
    • Systemic corticosteroids
  • Long term control medications
    • Inhaled corticosteroids
    • Inhaled LABA
    • Leukotriene modifiers
    • Theophylline
    • Omalizumab
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2
Q

Acute Severe Asthma

A
  • Written action plan
  • Recognition of early indicators of acute exacerbation
  • Appropriate intensification of therapy
  • Removal of triggers or irritants
  • Timely communication b/t pt and clinician

Tx options: oxygen, SABA +/- ipratopium bromide (anticholinergic), systemic corticosteroid, close monitoring

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3
Q

Bronchodilators

A

Reverse the bronchospasm of the immediate asthmatic response

  • B2-Adrenergic Agonists
  • Anticholinergics
  • Methylxanthines
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4
Q

Bronchi Anti-inflammatory Agents

A

Inhibit the inflammatory components of the immediate and late asthmatic responses

  • Corticosteroids
  • Leukotriene modifiers
  • Mast cell inhibitors
  • Anti-IgE antibody
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5
Q

B2-Adrenergic Agonists

A
  • Relax airway smooth muscle by stimulating B2-adrenergic receptors
    • Increase cAMP –> bronchodilation
    • Decrease cAMP –> bronchoconstriction
  • Increase mucociliary clearance
  • Stabilize mast cell membranes & inhibit inflammatory cells

Adverse effects: (worse / PO vs. inhaled)

  • Tachycardia
  • Tremor
  • Hypokalemia
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6
Q

Short-Acting Inhaled B2-Agonists (SABA)

A
  • Drug of choice for quick relief asthma symptoms (severe and chronic) and prevention of exercise-induced bronchospasm
  • Onset of action < 5 min (metered-dose inhaler + spacer is quicker & as effective as NEB)
  • Duration of action 4-6 hours
  1. Albuterol (racemic mixture)
  2. Levalbuterol (R-enantiomer)
    - -much more expensive!

Doses: 2 puffs every 4-6 hours PRN, 2 puffs 5 minutes before exercise, doubled dose for exacerbations

*Regular use of inhaled SABAs is not recommended & indicates need for additional long-term control therapy

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7
Q

Asthma Control Therapy

A

Inhaled corticosteroids:

  • More effective controllers for asthma, anti-inflammatory effects
  • Used in treating asthma of any severity at any age
  • Usually taken twice daily

Systemic steroids:

  • Used in acute asthma via IV or PO
  • Small % of asthma pt’s require this
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8
Q

Leukotrienes

A

Leukotrienes = inflammatory mediators produced by mast cells that cause bronchoconstriction A

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9
Q

Cromones

A

Inhibit mast cells and sensory nerve activation

  • Effective in blocking trigger-induced asthma (early and late-phase responses)
  • Short duration of action–less effective for long-term control (cromolyn nebulizer)
  • Alternative to inhaled corticosteroids in mild persistent asthma*
  • 3-4 times/day
  • Well tolerated
  • Improvement in 1-2 weeks, max benefit in 4-6 weeks
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10
Q

Goals of Chronic Asthma Therapy

A
  1. Reduce/eliminate chronic symptoms
  2. Eliminate exacerbations/ED visits
  3. Reduce side effects of medications
  4. Reduce the need for B-agonists
  5. Eliminate activity restrictions

*Children follow a personalized asthma action plan (begin w/ B2-agonists and add on if needed)

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11
Q

Goals of Acute Asthma Attack Therapy

A
  1. Reverse obstruction very rapidly
  2. Intubate if needed
  3. Administer medications as dictated by the pt
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12
Q

Tx of Acute Asthma Attack

A

Tx is that same for adults and children, except for doses

1st: B2-agonist (i.e., albuterol), NEB or IM
* Combine with anticholinergics (DUONEB) to increase efficacy, continuous x 1 hour
* +/- Magnesium IV x 30 min

2nd: Epinephrine or Terbutaline, SQ if NEB intolerant

Other:

  • Corticosteroids, PO, reduce hospitalization time
  • Heliox: Inhaled mix of helium and oxygen
  • Oxygen between NEB treatments (O2 saturation at least 90%)
  • Intubation w/ severe respiratory compromise, exhaustion, change in mental status, or acidosis
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13
Q

Long-Acting Inhaled B2-Agonists (LABA)

A
  • Add on therapy* for asthma poorly controlled with low-medium doses of ICS
  • Benefits: as effective as doubling dose of ICS, & reduces side effects of ICS
  • Duration of action up to 12 hours

NOTE: Never use as monotherapy for chronic asthma

  • Increased risk of severe asthma exacerbations & related deaths (black box warning)
  • Use only with long-term control medication
  • Discontinue when pt’s asthma is controlled
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14
Q

LABA Drugs

A

Salmeterol (Serevent)

  • Partial agonist
  • Onset of action of ~30 minutes (not quick relief)
  • Caution pt’s not to use as a rescue tx

Formoterol (Foradil)

  • Full agonist
  • Onset of action < 5 minutes
  • Not approved for treatment of acute bronchospasm
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15
Q

LABA Drug Combinations

A
  • Specifically designed for pediatrics*
  • Ensure the pt is not taking a LABA without a control medication

Advair: Fluticasone and salmeterol

Symbicort: Budesonide and formoterol

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16
Q

Corticosteroids

A
  • 1st line for asthma tx, along with B2-agonists*
  • Decrease airway inflammation
  • Decrease hyper-responsiveness
  • Decrease mucus production and secretion
  • Improve response to B2-agonists (d/t a decrease in inflammation)
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17
Q

Inhaled Corticosteroids

A

Preferred therapy for persistent asthma
(any severity, any age, 2x daily)
- Targeted drug delivery to the lungs decreases the risk of systemic effects
- Onset of action within 12 hours (not for quick relief, pt should be taking this daily)
- Significant clinical effects apparent after 2+ weeks

Adverse Effects:

  • Local–Oral candidiasis, cough, hoarseness, dysphonia (reduce by using spacer & rinsing mouth after use)
  • Systemic–adrenal suppression, decreased bone mineral density, skin thinning, cataracts, easy bruising, growth suppression in children (dose dependent)
18
Q

Indications for Systemic Corticosteroids

A

Long-term control:

  • Only if other therapies fail
  • Administer 1 daily or every-other-day
  • Frequently attempt to decrease/discontinue

Asthma exacerbation:

  • Effective for worsening asthma not responding to bronchodilators & for acute severe asthma
  • Short course or “bursts”

Acute severe asthma

  • Hasten recovery, decrease hospital admission (if given w/in 1 hour), reduce relapse rates
  • Onset of effect between 4-12 hours
  • PO is preferred over IV
  • Duration of tx between 3-10 days (no tapering)
19
Q

Systemic Corticosteroid Drugs

A

Prednisone, Methylprednisone, Prednisolone

*Used in acute asthma*
Usual adult dose: IV or PO
- Long term-every other day
- Acute, severe-1 or 2 doses
- Exacerbation-1 or 2 doses x 5-10 days
20
Q

Anticholinergics

A
  • 2nd line or add on therapy to B2-agonists*
  • MOA: Inhibit the effects of acetylcholine on muscarinic receptors in the airways
  • Adverse effects: Blurred vision, dry mouth, urinary retention, constipation
21
Q

Anticholinergic Drugs

A

Ipratropium (Atrovent)

  • Onset of action ~30 minutes
  • Duration of action of 4-8 hours

*Add to B2-agonists in acute severe asthma to improve pulmonary functioning & decrease hospitalization rates (no evidence for long-term control therapy)

22
Q

Leukotriene Modifiers

A

Zileuton
- Inhibits 5-lipoxygenase
Montelukast, Zafirlukast
- Competitiely antagonize the effects of leukotriene D4

  • Improve FEV1 and decrease asthma sxs, frequency of rescue inhaler use and exacerbations
  • Less effective than ICS, can use as combination therapy
23
Q

Montelukast (Singulair)

A

Leukotriene modifier of choice

Dosing: once daily at bedtime

No significant increase in hepatic enzymes (AST, ALT) and NO EFFECT on cytochrome P450 enzymes

24
Q

Zafirlukast (Accolate)

A

Leukotriene Modifier

  • Dosing: BID at least 1 hour before or 2 hours after meals
  • Causes an adverse increase in hepatic enzymes (do NOT need to monitor)
  • Inhibits some cytochrome P450 enzymes (CYP 2C9, CYP 3A4)–drug interactions
25
Q

Zileuton (extended-release tablet, Zyflo CR)

A

Leukotriene Modifier

  • Dosing: BID, within 1 hour after morning and evening meals
  • Causes an adverse increase in hepatic enzymes (must check liver enzymes at baseline, monthly for the first 3 months, every 2-3 months for the 1st year, then periodically)
  • Inhibits one cytochrome P450 enzyme (CYP 1A2)–drug interactions
26
Q

Methylxanthines

A

Theophylline

MOA: Bronchodilation by inhibiting phosphodiesterase and antagonizing adenosine

  • Limited use d/t inferior efficacy compared to ICS, narrow therapeutic index, potentially life-threatening toxicity, & clinically important drug interactions

Adverse Effects: (< 20 mg/dL) = HA, N/V, insomnia, gastric upset & irritability, (> 20 mg/dL) = cardiac arrhythmias, seizures, toxic encephalopathy, & death

27
Q

Theophylline

A

Methylxanthine
[5-15 mg/L], dose: 10-300 mg

Drug Interactions:Metabolized by P450 enzymes

  • Levels increase w/ Cimetidine, Erythromycin, Clarithromycin, Propanolol, Cyprofloxacin
  • Levels decrease with smoking & anti-convulsants (Carbamazepine, Phenytoin)
28
Q

Anti-IgE Antibody Drugs

A

Omalizumab
- Recombinant humanized monoclonal anti-IgE antibody

MOA: Inhibits binding of IgE to receptors on mast cells & basophils, resulting in inhibition of mediator release

Indications: Moderate to severe persistent asthma, 12 years of age or older, not controlled by ICS, + skin test or in vitro reactivity to perennial allergens

CI: Use is limited by high cost

29
Q

Omalizumab

A

Anti-IgE Antibody Drug

Benefits: Decreases ICS use, reduces # and length of exacerbations, increases asthma-related QOL

Adverse Effects:

  • Injection site reactions (bruising, redness, pain, stinging, itching, burning)
  • (Rarely) Anaphylactic reactions (bronchospasm, hypotension, syncope, urticaria, angioedema)–any dose, up to 2 hours after administration
  • Malignancy

Dosing: SQ every 2-4 weeks, based on weight and initial IgE serum concentration

30
Q

Tx of Intermittent Asthma

A
  • Long-term control medications not needed*
  • SABA for prevention or tx
  • 2 puffs of albuterol prior to exposure of known trigger
  • Monitor for heavy use, if > 2x/wk, switch to long term medication
31
Q

Tx of Persistent Asthma

A
  • Daily long-term control therapy required (drug of choice = ICS)
  • SABA as needed

Follow-up:

  • Within 2-6 wks after initiating or increasing therapy
  • Every 1-6 months once controlled
32
Q

Tx of Severe Acute Asthma

A
  • Early & appropriate intensification of therapy is imperative to resolve the exacerbation, prevent relapse, & prevent severe airflow obstruction in the future
  • Therapy should be started at home based on written action plan
33
Q

Tx of Asthma: Children Ages 0-4

A

Initiate long-term control meds if:

  • 4+ episodes of wheezing within last year that lasted for > 1 day & affected sleep
  • Pt w/ 1 major or 2 minor risk factors for developing persistent asthma

Consider long-term control meds if:

  • Require symptomatic tx > 2 days/wk for > 4 weeks
  • 2 exacerbations requiring systemic steroids within 6 months
34
Q

Tx of Asthma During Pregnancy

A
  • ~1/3 of pregnant women w/ asthma experience worsening asthma during pregnancy
  • Safer to treat w/ medications than have uncontrolled asthma
  • Budesonide*–1st line ICS
  • Albuterol*–1st line for sxs & exacerbations
35
Q

Exercise-Induced Asthma

A
  • SOB, wheezing, or chest tightness during or shortly after vigorous exercise
  • Peak 5-10 minutes after stopping activity
  • Resolve within 20-30 minutes
  • Exercise challenge can confirm diagnosis*
  • > or equal to 15% decrease in PEF or FEV1 post-exercise
36
Q

Tx of Exercise-Induced Asthma

A
  • Warm up prior to vigorous exercise
  • Cover mouth & nose w/ scarf or mask during cold weather
  • Cool down prior to stopping
  • Pretreat w/ albuterol 5 minutes prior
  • Albuterol alternatives: Cromolyn, Leukotriene modifier, daily tx w/ ICS
37
Q

DuoNEB

A
  • Combination of Albuterol & Ipratropium*
  • Can and should be used multiple times in acute asthma attacks
  • Advised that children receive DuoNEB continuously for up to 1 hour during an acute attack
38
Q

Magnesium

A
  • Used for acute, severe attacks
  • Bronchodilator
  • Typically used in conjunction after other therapies have been initiated (e.g B2-agonists)
  • Given over 30 minutes
39
Q

Heliox

A
  • Mixture of helium & oxygen
  • Can lower airway resistance
  • Adjunct to other therapies in severe exacerbation
40
Q

Oxygen

A

Given to all pts between NEB treatments to maintain O2 saturation of at least 90%

41
Q

Indications for Intubation

A
  • Severe respiratory compromise
  • Exhaustion
  • Change in mental status
  • Acidosis

Pulmonology (8 decks)

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