Drugs for Asthma and COPD Flashcards

1
Q

Drugs for asthma

A

B2 adrenergic agonists
Anticholinergics
Corticosteroids (CS)
Methylaxanthine (theophylline)
Leukotriene antagonists (montelukast, zafirlukast, and zileuton)
Cromolyn
Monoclonal antibodies (omalizumab)

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2
Q

Drugs for COPD

A

B2 adrenergic agonists
Anticholinergics
Corticosteroids (CS)
Methylxanthine (theophylline)

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3
Q

Asthma

A

Disease characterized by predisposition to a chronic airway (bronchi) inflammation and bronchoconstriction (narrowed airway)

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4
Q

Asthma
- Airflow obstruction d/t

A

Contraction of airway smooth muscle d/t activation and release of inflammatory medicatos (histamine, leukotrienes, cyotkines) from airway mast cells
Viscous mucus plugs in the airway lumen, swelling and thickening of the bronchial mucosa from edema, cellular infiltration and hyperplasia

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5
Q

Asthma
- Classic symptoms

A

Recurrent episodes of wheezing
Chest tightness
SOB
Coughing

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6
Q

Asthma
- Common complication

A

Exacerbation which can range from mild, severe, to fatal

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7
Q

What contributes to obstructed airflow?

A

Combination of smooth muscle constriction (bronchospasm), inflammatory bronchial thickening and mucous secretion

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8
Q

There is a marked increase in what?

A

Bronchial responsiveness to allergens and inhaled stimuli leads to bronchoconstriction and inflammation with mucous plugging

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9
Q

Strategy of Asthma Therapy
- Bronchodilaters

A

B2 agonists- inhaled
Muscarinic antagonists (anticholinergics)- inhaled
Methylxanthines (theophylline)- less common- oral, IV

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10
Q

Strategy of Asthma Therapy
- Anti-inflammatory drugs

A

Corticosteroids- inhaled, oral, injectible
Leucotriene antagonists- oral
Cromolyn- oral
Monoclonal antibodies- sc or iv

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11
Q

Inhaled forms deliver the drug where?

A

Directly to the lungs

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12
Q

Inhaled forms deliver the drug to the lungs
- have reduced what?

A

Toxicity and preferred form of delivery

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13
Q

Anti-Asthmatic Drugs
- Relievers (rescue drugs) for Quick Relief

A

Inhaled short-acting B2 adrenergic agonists (SABAs)
Exaxerbations

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14
Q

Anti-Asthmatic Drugs
- Relievers–> exacerbations

A

Systemic steroids
Inhaled short-acting muscarinic antagonists (SAMAs)

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15
Q

Anti-Asthmatic Drugs
- Controllers (maintenance drugs) for LT care

A

Inhaled corticosteroids (ICS)
Inhaled long-acting adrenergic agonists (LABAs)
Leukotriene antagonists (zileuton, montelukast), oral
Theophylline (oral or IV)
Inhaled long-acting muscarinic antagonists (LAMAs)
Cromolyn
Monoclonal antibodies (SC or IV)

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16
Q

Quick Relief Short-Acting Beta-2 Agonists (SABAs)
- Albuterol

A

Used as needed in all patients with asthma
Used as monotherapy in low risk patients

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17
Q

Quick Relief Short-Acting Beta-2 Agonists (SABAs)
- Albuterol–> Potent bronchodilators

A

Binds to beta 2 receptors and relaxes bronchial smooth muscle
Inhaled
Rapid onset (5-30 mins)
Duration of action (4-6 hours)
Monotherapy for exercise- induced bronchospasm

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18
Q

Quick Relief Short-Acting Beta-2 Agonists (SABAs)
- Ipratropium

A

Atropine-like drug

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19
Q

Quick Relief Short-Acting Beta-2 Agonists (SABAs)
- Ipratropium–> effective bronchodilator

A

Blocks action of ACh at muscarinic (M3) receptors on airway smooth muscle
Inhaled
Slow onset
Useful in patients who cannot tolerate B2 agonists
Used in combo with SABAs during acute exacerbations

20
Q

Methylxanthines-Theophylline
- Theophylline–> inhibits

A

Phosphodiesterase (PDE) and releases epinephrine from adrenal medulla cells resulting in bronchodilation

21
Q

Methylxanthines-Theophylline
- Theophylline–> limitations

A

Decreased effectiveness
Drug interactions
Adverse effects (increase HR)

22
Q

Methylxanthines-Theophylline
- Theophylline–> main use

A

When B2 agonists and CS are ineffective or contraindicated

23
Q

Methylxanthines-Theophylline
- Theophylline–> can be used in combo with

A

SABAs during acute exacerbations

24
Q

LT Control Inhaled Corticosteroids (ICS)
- Inhaled Corticosteroids

A

Drugs of first choice in patients with any degree of persistent asthma
- Severe attacks often require a short-term oral steroid
Potent and effective inflammatory drug
Reduce bronchial reactivity (hyperresponsiveness)

25
Q

LT Control Inhaled Corticosteroids (ICS)
- Inhaled Corticosteroids–> MOA

A

Directly targets underlying airway inflammation
Decrease inflammatory cascade
Reversing mucosal edema
Decreasing permeability of capillaries (decrease prostaglandin production)
Inhibit the release of leukotrienes

26
Q

Results of glucocorticoids suppressing phospholipase A2 action

A

Decrease synthesis of prostaglandins (mediators of pain and inflammation) and leukotrienes (mediators of asthma and bronchoconstriction)

27
Q

LT Control Inhaled Corticosteroids (ICS)
- Beclomethasone, Budesonide, Fluticasone

A

Inhalation via metered dose inhaler (MDI) or dry powder inhaler (DPI)

28
Q

LT Control Inhaled Corticosteroids (ICS)
- Beclomethasone, Budesonide, Fluticasone–> WARNING

A

High doses for prolonged period of time can cause adrenal suppression, risk of fracture and immunosuppression

29
Q

LT Control Inhaled Corticosteroids (ICS)
- Beclomethasone, Budesonide, Fluticasone–> Side effects

A

Hoarseness
Oral candidiasis (thrush) can be avoided with “Swish and spit” method after each use, or use spacer with a MDI

30
Q

Corticosteroid deposition on the oral and laryngeal mucosa

A

Spacer can be attached to MDI to decrease the deposition of drug in mouth caused by improper techniques
Reduces adrenal suppression by reducing the amount of CS deposited in the oropharynx

31
Q

LT Control - LABAs
- Salmeterol

A

Long duration of action (12 hours)
Prescribed as adjunctive therapy

32
Q

LT Control - LABAs
- Salmeterol–> BOXED WARNING

A

Increased risk of asthma-related death

33
Q

LT Control - LABAs
- Salmeterol–> should be used with?

A

ICS
Fluticasone and salmeterol
Budesonide and formoterol

34
Q

LT Control - LABAs
- What are LABAs not used for?

A

Acute bronchospasm
Combo therapy ICS/LABA inhalers do not have boxed warning that the LABA has alone

35
Q

LT Control- LAMAs
- Tiotropium

A

Atropine-like drug
Inhalation
Approved by FDA for asthma in patients six y/o or older with hx of exacerbations, despite ICS/LABA therapy

36
Q

LT Control- Leukotriene Antagonists
- Leukotrienes

A

Constrict bronchiolar smooth muscle
Increase permeability and promote mucus secretion

37
Q

LT Control- Leukotriene Antagonists
- Zileuton

A

Specific and selective inhibitor of 5-lipoxygenase
Prevents formation of leukotrienes

38
Q

LT Control- Leukotriene Antagonists
- Montelukast, Zafirlukast

A

Selective and reversible inhibitors of the cysteinyl-leukotriene-1 receptor
Approved for prophylaxis of asthma therapy
Not effective when immediate bronchodilation is required

39
Q

LT Control- Leukotriene Antagonists
- Zileuton and Zafirlukast–> Side Effects

A

Liver toxicity

40
Q

LT Control- Leukotriene Antagonists
- Montelukast, Zafirlukast, Zileuton–> side effects

A

Neuropsychiatric events (mood and behavioral changes)
Churg-Strauss syndrome, also known as eosinophilic granulomatous polyangiitis (EGPA)

41
Q

Churg-Strauss syndrome

A

Rare syndrome marked by blood vessel inflammation
Inflammation restricts blood flow to organs and tissues

42
Q

LT Control- Cromolyn
- Cromolyn

A

Prophylactic anti-inflammatory agents
No bronchodilator action
Used basically in children

43
Q

LT Control- Cromolyn
- Cromolyn–> MOA

A

Inhibition of mast cell degeneration can block the initiation and delayed asthmatic responses (mediated via Cl- channels)

44
Q

LT Control- Cromolyn
- Cromolyn–> inhalation

A

Short duration of action–> requires frequent daily dosing
Pretreatment can block allergy and exercise-induced bronchoconstriction

45
Q

LT Control Monoclonal Antibody
- Omalizumab

A

Humanized monoclonal antibody to IgE
Prevents IgE from binding allergen and thereby activating mast cells
Reserved for treatment of asthma not responsive to other less expensive therapies

46
Q

LT Control Monoclonal Antibody
- Omalizumab–> BOXED WARNING

A

Anaphylaxis as early as after the first dose and also occurred beyond 1 year after beginning treatment