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• Pulmonary drugs are for asthma and chronic obstructive pulmonary disease.

Asthma and COPD Drugs

• Two main drug classes: anti-inflammatory agents and bronchodilators.
• Anti-inflammatory agents includes glucocorticoids like Prednisone.
• Bronchodilators includes Beta₂ agonists, such as Albuterol.

Inhalation Drug Therapy

• It has three advantages: enhanced therapeutic effects, minimized systemic effects, and rapid relief of acute attacks.
• Options for this include: Metered-dose inhalers (MDIs), Respimats, Dry-powder inhalers (DPIs), and Nebulizers.

Anti-Inflammatory Drugs

• They form the foundation of asthma therapy and are taken daily for long-term control.
• Principal anti-inflammatory drugs are the glucocorticoids, examples being Budesonide and Fluticasone.

Anti-Inflammatory Drugs: Glucocorticoids' Mechanism of Action

• They reduce inflammation by decreasing the synthesis and release of inflammatory mediators.
• These drugs reduce the infiltration and activity of inflammatory cells.
• They decrease edema of the airway mucosa caused by beta₂ agonists.
• The most effective antiasthma drugs available.
• They are usually administered by inhalation, but IV and oral routes exist.
• Glucocorticoids reduce bronchial hyperreactivity and airway mucus production.
• They may increase bronchial beta₂ receptors and their responsiveness to beta₂ agonists.

Anti-Inflammatory Drugs: Glucocorticoids Use

• Primarily for prophylaxis of chronic asthma.
• Dosing must occur on a fixed schedule, not as needed (PRN).
• Glucocorticoids cannot abort an ongoing attack due to slow development of the anti-inflammatory effects.

Anti-Inflammatory Drugs: Glucocorticoids Inhaled Use

• It is the first-line therapy for managing the inflammatory component of asthma.
• Most patients with persistent asthma will use these drugs daily.
• Inhaled glucocorticoids are effective and safer than systemic ones.

Anti-Inflammatory Drugs: Glucocorticoids Oral Use

• For patients with moderate to severe persistent asthma or for managing acute exacerbations of asthma or COPD.
• Use when symptoms can't be controlled with safer medications (inhaled glucocorticoids, inhaled beta₂ agonists) due to potential toxicity.
• Treatment should be as brief as possible.

Anti-Inflammatory Drugs: Glucocorticoids Adverse Effects of Inhaled Forms

• Can cause adrenal suppression, oropharyngeal candidiasis, and dysphonia.
• Glucocorticoids can slow growth in children/adolescents, but do not decrease adult height.
• They promote bone loss, increase the risk of cataracts and glaucoma.

Anti-Inflammatory Drugs: Glucocorticoids Adverse Effects of Oral Forms

• Adverse effects include short-term or log-term therapy, adrenal suppression, osteoporosis, hyperglycemia, peptic ulcer disease.
• Oral forms in young patients could cause growth suppression.

Anti-Inflammatory Drugs: Glucocorticoids Adrenal Suppression

• Prolonged use can decrease the adrenal cortex's ability to produce its own glucocorticoids.
• This can be life-threatening during severe physiologic stress like surgery, trauma, or systemic infection.
• Adrenal suppression prevents production of endogenous glucocorticoids with high levels of the hormone required to survive stress.
• Patients must receive increased doses of oral or IV glucocorticoids during stress to avoid potentially fatal outcomes.

Anti-Inflammatory Drugs: Glucocorticoids Adrenal Suppression; Discontinuation of Treatment

• Must be done slowly.
• Adrenocortical function recovery takes several months.
• The dosage of exogenous sources must be reduced gradually.
• During this time, patients must be given supplemental oral or IV glucocorticoids during severe stress, even after switching to inhaled glucocorticoids.

Anti-Inflammatory Drugs: Leukotriene Modifiers

• These suppress the effects of leukotrienes which promote smooth muscle constriction, blood vessel permeability, and inflammatory responses.
• The modifiers directly act and recruit eosinophils and other inflammatory cells .
• In asthma patients, these can reduce bronchoconstriction and inflammatory responses like edema and mucus secretion.

Anti-Inflammatory Drugs: Leukotriene Modifiers Risks and Agents

• They are generally well tolerated but can cause adverse neuropsychiatric effects.
• These effects may present as, depression, suicidal thinking, and suicidal behavior.
• Available agents: Zileuton [Zyflo], Zafirlukast [Accolate], Montelukast [Singulair].

Monoclonal Antibody: Omalizumab [Xolair]

• Action: antagonism of immunoglobulin E (IgE).
• Indicated for patients 12 years+ with moderate to severe allergy-related asthma not controlled by an inhaled glucocorticoid.

Monoclonal Antibody: Omalizumab [Xolair] Adverse Effects

• Injection-site reactions, viral/upper respiratory infections, sinusitis, headache, and pharyngitis.
• Cardiovascular events and malignancy could also be adverse reactions.
• Life-threatening anaphylaxis.

Bronchodilators

• Provide symptomatic relief but do not alter the underlying disease inflammation.
• Patients taking a bronchodilator usually also take a glucocorticoid for inflammation suppression.
• Beta₂-adrenergic agonists are principle bronchodilators.

Bronchodilators: Beta₂-Adrenergic Agonists' Mechanism of Action

• Activation of beta₂ receptors in the smooth muscle of the lung promote bronchodilation.
• The bronchodilation relieves bronchospasm.
• Beta₂ agonists have a limited role in suppressing histamine release and increasing ciliary motility.

Bronchodilators: Beta₂-Adrenergic Agonists Use in Asthma and COPD

• Inhaled short-acting beta₂ agonists (SABAs) are taken PRN to abort an ongoing attack.
• They can also be taken before exercise (EIB) to prevent an attack.
• Nebulized SABA is the traditional treatment of choice for hospitalized patients undergoing a severe acute attack.
• Delivery with an MDI in the outpatient setting can be equally effective.

Bronchodilators: Beta₂-Adrenergic Agonists Inhaled Long-Acting Use in Asthma and COPD

• LABAs are for long-term control in patients who experience frequent attacks.
• They are dosed on a fixed schedule, not PRN,.
• Effective in treating stable COPD, they must always be combined with a glucocorticoid when used to treat asthma: use alone is contraindicated.

Bronchodilators: Beta₂-Adrenergic Agonists Adverse Effects

• Inhaled preparations can cause systemic effects like tachycardia, angina, and tremor.
• Excessive dosage of oral preparations can cause angina pectoris, tachydysrhythmias, possibly tremor.

Anticholinergic Drugs: Ipratropium

• Improves lung function by blocking muscarinic receptors in the bronchi, thereby reducing bronchoconstriction.
• Administered by inhalation to relieve bronchospasm.
• Therapeutic effects begin within 30 seconds, reach 50% in 3 minutes, and persist about 6 hours.
• Adverse effects: dry mouth and irritation of the pharynx, glaucoma and cardiovascular events.

Anticholinergic Drugs: Tiotropium

• Long-acting inhaled anticholinergic agent used for maintenance therapy of bronchospasm with COPD.
• Not approved for asthma.
• Relieves bronchospasm by blocking muscarinic receptors in the lung.
• Therapeutic effects begin in 30 minutes, peak in 3 hours, and persist about 24 hours.
• Subsequent doses improve bronchodilation, reaching a plateau after 8 consecutive doses (8 days).

Anticholinergic Drugs: Aclidinium

• Newest long-acting anticholinergic agent for managing COPD-associated bronchospasm.
• Relieves bronchospasm by blocking muscarinic receptors in the lung.
• Drug delivery's peak levels occur within 10 minutes.
• Intended only for maintenance therapy, not for acute symptom relief.

Glucocorticoid/LABA Combinations

• Available combinations include: Fluticasone/salmeterol [Advair], Budesonide/formoterol [Symbicort], Mometasone/formoterol [Dulera].
• Indicated for adults and children needing long-term maintenance.
• It is not recommended for initial therapy.

Management of Asthma

• Four classes of asthma severity: intermittent, mild persistent, moderate persistent, and severe persistent.
• Treatment goals include reducing impairment and risk.
• Stepwise therapy: initial step chosen based on pretreatment classification of asthma severity, moving up or down is based on assessment of asthma control.

Drugs for Acute Severe Exacerbation

• Requires immediate attention.
• Goals include: relieve airway obstruction/hypoxemia, and normalize lung function quickly.
• Initial therapy: oxygen to relieve hypoxemia, a systemic glucocorticoid to reduce airway inflammation, a nebulized high-dose SABA to relieve airflow obstruction, and nebulized ipratropium to further reduce airflow obstruction.

Management of Stable COPD

• Pharmacologic management includes bronchodilators, glucocorticoids, and phosphodiesterase-4 inhibitors.

Management of COPD Exacerbations

• Pharmacologic management includes preferred SABAs for bronchodilation which is specifically inhaled, either alone or in combination with inhaled anticholinergics.
• Systemic glucocorticoids and antibiotics are also included.
• Supplemental oxygen helps to maintain an oxygen saturation of 88% to 92%.

Allergic Rhinitis

• Definition: Inflammatory disorder of the upper airway, lower airway, and eyes.
• Symptoms: Sneezing, rhinorrhea, pruritus, nasal congestion, and conjunctivitis.
• Sometimes conjunctivitis, sinusitis, and asthma.
• Allergens trigger the release of inflammatory mediators such as histamine, leukotrienes, and prostaglandins.
• Seasonal and perennial, triggered by airborne allergens.

Classes of Drugs for Allergic Rhinitis

• Glucocorticoids (intranasal), antihistamines (oral and intranasal), and sympathomimetics (oral and intranasal).

Intranasal Glucocorticoids

• First choice and most effective for treatment and prevention of rhinitis.
• Mild adverse effects include drying of nasal mucosa/sore throat, epistaxis, and headache.
• Systemic effects are rare, but adrenal suppression and slowed linear pediatric growth may occur.

Oral Antihistamines

• Use for allergic rhinitis.
• They do not reduce nasal congestion.
• Most effective if taken prophylactically.
• Should be taken regularly throughout allergy season, preventing initial histamine receptor activation, even when symptoms are absent.
• Mild adverse effects include sedation, more common with first generation, less with second.

Sympathomimetics

• Reduce nasal congestion, but do not reduce rhinorrhea, sneezing, or itching.
• These activate alpha₁-adrenergic receptors on nasal blood vessels.
• Rebound congestion, CNS stimulation, cardiovascular effects, stroke, and abuse are some adverse effects.

Sympathomimetics (Oral/Nasal)

• Topical administration should not last longer than 5 consecutive days.
• Topical agents act more quickly than oral agents and are more effective.
• Oral agents act longer than topical preparations.
• Systemic effects occur primarily with oral agents, and responses to topical agents are elicited when the recommended dosage is higher.
• Rebound congestion is common with prolonged topical use but rare with oral agents.

Sympathomimetics (Oral/Nasal) Specific Agents

• Phenylephrine, ephedrine, pseudoephedrine.
• With the following drugs it becomes Antihistamine-sympathomimetic combinations: Ipratropium bromide [Atrovent], Montelukast [Singulair], Omalizumab [Xolair].

Drugs for Cough

• Antitussives: Drugs that suppress cough.
• Opioid options; codeine and hydrocodone.
• Nonopioid choices; dextromethorphan, diphenhydramine, and benzonatate.

Expectorants

• Guaifenesin [Mucinex, Humibid].
• Renders cough more productive by stimulating flow of respiratory tract secretions, higher doses may be effective.