Drugs for Asthma and COPD Flashcards
Drugs for asthma
B2 adrenergic agonists
Anticholinergics
Corticosteroids (CS)
Methylaxanthine (theophylline)
Leukotriene antagonists (montelukast, zafirlukast, and zileuton)
Cromolyn
Monoclonal antibodies (omalizumab)
Drugs for COPD
B2 adrenergic agonists
Anticholinergics
Corticosteroids (CS)
Methylxanthine (theophylline)
Asthma
Disease characterized by predisposition to a chronic airway (bronchi) inflammation and bronchoconstriction (narrowed airway)
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
Asthma
- Classic symptoms
Recurrent episodes of wheezing
Chest tightness
SOB
Coughing
Asthma
- Common complication
Exacerbation which can range from mild, severe, to fatal
What contributes to obstructed airflow?
Combination of smooth muscle constriction (bronchospasm), inflammatory bronchial thickening and mucous secretion
There is a marked increase in what?
Bronchial responsiveness to allergens and inhaled stimuli leads to bronchoconstriction and inflammation with mucous plugging
Strategy of Asthma Therapy
- Bronchodilaters
B2 agonists- inhaled
Muscarinic antagonists (anticholinergics)- inhaled
Methylxanthines (theophylline)- less common- oral, IV
Strategy of Asthma Therapy
- Anti-inflammatory drugs
Corticosteroids- inhaled, oral, injectible
Leucotriene antagonists- oral
Cromolyn- oral
Monoclonal antibodies- sc or iv
Inhaled forms deliver the drug where?
Directly to the lungs
Inhaled forms deliver the drug to the lungs
- have reduced what?
Toxicity and preferred form of delivery
Anti-Asthmatic Drugs
- Relievers (rescue drugs) for Quick Relief
Inhaled short-acting B2 adrenergic agonists (SABAs)
Exaxerbations
Anti-Asthmatic Drugs
- Relievers–> exacerbations
Systemic steroids
Inhaled short-acting muscarinic antagonists (SAMAs)
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)
Quick Relief Short-Acting Beta-2 Agonists (SABAs)
- Albuterol
Used as needed in all patients with asthma
Used as monotherapy in low risk patients
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
Quick Relief Short-Acting Beta-2 Agonists (SABAs)
- Ipratropium
Atropine-like drug
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
