Drugs for Asthma and COPD Flashcards by Katie Bendersky

Drugs for asthma

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

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Drugs for COPD

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

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Asthma

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

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Asthma
- Airflow obstruction d/t

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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Asthma
- Classic symptoms

Recurrent episodes of wheezing
Chest tightness
SOB
Coughing

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Asthma
- Common complication

Exacerbation which can range from mild, severe, to fatal

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What contributes to obstructed airflow?

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

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There is a marked increase in what?

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

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Strategy of Asthma Therapy
- Bronchodilaters

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

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Strategy of Asthma Therapy
- Anti-inflammatory drugs

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

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Inhaled forms deliver the drug where?

Directly to the lungs

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

Toxicity and preferred form of delivery

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

Inhaled short-acting B2 adrenergic agonists (SABAs)
Exaxerbations

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Anti-Asthmatic Drugs
- Relievers–> exacerbations

Systemic steroids
Inhaled short-acting muscarinic antagonists (SAMAs)

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

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

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

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

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

Atropine-like drug

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

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

Methylxanthines-Theophylline
- Theophylline–> inhibits

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

Methylxanthines-Theophylline
- Theophylline–> limitations

Decreased effectiveness
Drug interactions
Adverse effects (increase HR)

Methylxanthines-Theophylline
- Theophylline–> main use

When B2 agonists and CS are ineffective or contraindicated

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

SABAs during acute exacerbations

LT Control Inhaled Corticosteroids (ICS)
- Inhaled Corticosteroids

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)

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

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

Results of glucocorticoids suppressing phospholipase A2 action

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

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

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

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

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

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

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

Corticosteroid deposition on the oral and laryngeal mucosa

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

LT Control - LABAs - Salmeterol

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

LT Control - LABAs - Salmeterol--> BOXED WARNING

Increased risk of asthma-related death

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

ICS Fluticasone and salmeterol Budesonide and formoterol

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

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

LT Control- LAMAs - Tiotropium

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

LT Control- Leukotriene Antagonists - Leukotrienes

Constrict bronchiolar smooth muscle Increase permeability and promote mucus secretion

LT Control- Leukotriene Antagonists - Zileuton

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

LT Control- Leukotriene Antagonists - Montelukast, Zafirlukast

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

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

Liver toxicity

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

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

Churg-Strauss syndrome

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

LT Control- Cromolyn - Cromolyn

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

LT Control- Cromolyn - Cromolyn--> MOA

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

LT Control- Cromolyn - Cromolyn--> inhalation

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

LT Control Monoclonal Antibody - Omalizumab

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

LT Control Monoclonal Antibody - Omalizumab--> BOXED WARNING

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