Respiratory Drugs PDF

Respiratory Drugs Respiratory drugs are essential for treating and managing conditions affecting the lungs and airways. These medications work to alleviate symptoms, improve lung function, and prevent exacerbations. KR by K atie R obins on Diseases of the Lower Respiratory Tract 1 Chronic...

Respiratory Drugs Respiratory drugs are essential for treating and managing conditions affecting the lungs and airways. These medications work to alleviate symptoms, improve lung function, and prevent exacerbations. KR by K atie R obins on Diseases of the Lower Respiratory Tract 1 Chronic Obstructive 2 Asthma Pulmonary Disease (COPD) Asthma is a chronic inflammatory COPD is an umbrella term for a disease of the airways that causes group of chronic lung diseases, recurring episodes of wheezing, such as chronic bronchitis and breathlessness, chest tightness, emphysema, that cause airflow and coughing. obstruction. 3 Emphysema 4 Chronic Bronchitis Emphysema is a lung condition Chronic bronchitis is a condition in that occurs when the tiny air sacs which the airways become in the lungs called alveoli lose their inflamed and swollen, causing elasticity and ability to expand and persistent cough and excessive contract. mucus production. Bronchial Asthma Definition Pathophysiology Bronchial asthma is a chronic inflammatory Asthma is characterized by airway inflammation, disorder of the airways that causes recurrent bronchospasm, and mucus hypersecretion, leading episodes of wheezing, breathlessness, chest to airway obstruction. tightness, and coughing. The inflammation involves the recruitment of These symptoms are usually triggered by various inflammatory cells, such as eosinophils, mast cells, stimuli, including allergens, irritants, exercise, or and lymphocytes, into the airway walls. infections. Asthma Categories Intrinsic Extrinsic Occurs in individuals with no history Develops in individuals exposed to of allergies or specific triggers. known allergens, such as pollen, dust mites, or animal dander. Exercise-induced Drug-induced Triggered by physical exertion, often Caused by exposure to certain in individuals with a history of medications, such as aspirin or beta asthma. blockers. Chronic Obstructive Pulmonary Disease (COPD) Chronic Lung Obstruction Irreversible Changes COPD is a progressive lung disease The lung damage associated with characterized by chronic COPD is generally irreversible. This obstruction of lung airflow. This means that once the damage has obstruction interferes with normal occurred, it is not possible to fully breathing, making it difficult to restore normal lung function. exhale air from the lungs. Combined Conditions COPD encompasses two primary lung conditions: chronic bronchitis and emphysema. While they share some common features, they are distinct in their underlying mechanisms and manifestations. Chronic Bronchitis Chronic Inflammation Excessive Mucus Bronchial Irritants Chronic bronchitis is The inflammation leads to Chronic bronchitis often results characterized by persistent excessive mucus secretion and from prolonged exposure to inflammation and low-grade changes in the bronchial bronchial irritants such as infection of the bronchi, the structure, which can impair cigarette smoke, air pollution, or airways that carry air to and from airflow and lead to breathing dust. the lungs. difficulties. Emphysema Alveolar Destruction Reduced Gas Exchange Emphysema is a chronic lung disease. It causes Emphysema reduces the surface area where gas damage to the alveoli, which are tiny air sacs in the exchange takes place in the lungs. This makes it lungs. The walls of the alveoli are weakened and difficult for the body to get enough oxygen. eventually break down, causing the air sacs to Symptoms of emphysema include shortness of enlarge. breath, wheezing, and chronic cough. Pharmacologic Overview Bronchodilators Beta-Adrenergic Agonists These drugs relax bronchial Beta-adrenergic agonists, such smooth muscle. This action as albuterol, stimulate beta2 widens the bronchi and receptors, leading to bronchioles, which are narrowed bronchodilation. by disease. Anticholinergics Xanthine Derivatives Anticholinergics, like Xanthines, such as theophylline, ipratropium, block the action of inhibit phosphodiesterase, acetylcholine, a increasing cAMP levels, which neurotransmitter that constricts relaxes smooth muscle and bronchioles. dilates bronchioles. Bronchodilators: Short-acting Beta-Agonists (SABAs) Rapid Relief for Acute Episodes Mechanism of Action Considerations for Use Short-acting beta agonists, such as SABAs work by stimulating beta-2 SABAs are typically used for short-term albuterol, are often prescribed as rescue adrenergic receptors in the smooth muscle relief of symptoms. Frequent or persistent inhalers for individuals with asthma or of the bronchioles, leading to relaxation and use may indicate a need for a long-acting chronic obstructive pulmonary disease bronchodilation. This allows for increased bronchodilator or other medication (COPD). These medications provide quick airflow and improved lung function. adjustments. relief from bronchospasm, helping to open up the airways and ease breathing difficulties. Bronchodilators: Long-acting Beta- Agonists (LABAs) Mechanism of Action LABAs relax the muscles of the airways, making it easier to breathe. Duration of Action LABAs provide long-lasting relief from asthma symptoms, lasting for 12 hours or more. Important Note LABAs are never used for acute asthma attacks; they are for long-term management of asthma symptoms. Bronchodilators: Beta- Adrenergic Agonists: Newest LABA 1 1. Indacaterol (Arcapta 2 2. Vilanterol Neohaler) Vilanterol is a long-acting beta- Indacaterol is a long-acting agonist (LABA) that is available beta-agonist (LABA) indicated in combination with fluticasone for the long-term, once-daily (Breo Ellipta) or the maintenance treatment of anticholinergic, umeclidinium airflow obstruction in patients (Anoro Ellipta). with chronic obstructive pulmonary disease (COPD). 3 3. Ellipta Delivery System The term "Ellipta" refers to a unique dry powder inhaler delivery system that is designed to improve patient adherence and compliance with medication regimens. Bronchodilators: Acute Phase Rapid Relief Airflow Restoration Short-Term Use Beta-adrenergic agonists are used These drugs help restore normal Beta-adrenergic agonists are to quickly relieve airway airflow by relaxing the smooth generally used for short-term constriction during acute asthma muscle in the bronchioles. relief of acute asthma symptoms. attacks. Bronchodilators: Types Nonselective Adrenergics Nonselective Beta- Selective Beta2 Drugs Adrenergics These drugs stimulate alpha, These drugs only stimulate beta2 beta1, and beta2 receptors. These drugs stimulate both beta1 receptors. and beta2 receptors. Beta-Adrenergic Agonists: Mechanism of Action 1 Beta2 Receptor Stimulation The mechanism of action begins when a beta-adrenergic agonist drug binds to a specific beta2 receptor. 2 Activation of cAMP Activation of the beta2 receptor triggers the production of cyclic adenosine monophosphate (cAMP). 3 Smooth Muscle Relaxation cAMP relaxes smooth muscle in the airways, resulting in bronchial dilation and improved airflow. Beta-Adrenergic Agonists: Indications Bronchospasm Relief Acute Attack Management Hypotension and Shock Beta-adrenergic agonists are These medications are used both In addition to their respiratory effective in relieving in the treatment and prevention applications, beta-adrenergic bronchospasm associated with of acute asthma attacks, agonists can be used to treat conditions like asthma, providing quick and effective hypotension and shock by bronchitis, and other pulmonary relief. stimulating the heart and diseases. increasing blood pressure. Beta-Adrenergic Agonists: Contraindications 1 1. Known Drug Allergy 2 2. Uncontrolled Hypertension Avoid beta-adrenergic agonists if a patient has a history of allergic Beta-adrenergic agonists can reactions to them. worsen hypertension, so use cautiously or avoid in patients with uncontrolled blood pressure. 3 3. Cardiac Dysrhythmias 4 4. High Risk of Stroke Beta-adrenergic agonists can Avoid beta-adrenergic agonists in trigger or worsen cardiac patients with a high risk of stroke, dysrhythmias. Exercise caution in as the vasoconstrictive effects can patients with pre-existing cardiac increase the risk of stroke. rhythm abnormalities. Beta-Adrenergic Agonists: Adverse Effects Alpha and Beta Effects Cardiovascular Effects Insomnia Beta-agonists can stimulate the heart, leading to Restlessness tachycardia, palpitations, and potentially arrhythmias. Anorexia Vascular headache Central Nervous System Effects Hyperglycemia Commonly, they can cause restlessness, tremor, Tremor anxiety, and insomnia. Cardiac stimulation Beta-Adrenergic Agonists: Adverse Effects (Cont.) Cardiac Stimulation Tremor Beta1 agonists can cause tachycardia, Beta2 agonists can cause fine tremors, palpitations, and arrhythmias, particularly in usually in the hands, which may be patients with pre-existing cardiac disease. bothersome to some patients. Vascular Headache Hypotension or Hypertension Beta agonists can cause a throbbing Beta2 agonists can cause a decrease in blood headache, particularly in patients with a pressure, while beta1 agonists can cause an history of migraines. increase in blood pressure. Beta-Adrenergic Agonists: Interactions 1 1. Nonselective Beta Blockers 2 2. Monoamine Oxidase Inhibitors (MAOIs) Beta-adrenergic agonists should not be used with MAOIs can increase the risk of hypertensive crisis and nonselective beta blockers. The beta-blockers counteract cardiac arrhythmias. It is important to monitor patients the bronchodilation effects of the beta agonists. for adverse effects. 3 3. Sympathomimetics 4 4. Diabetes Sympathomimetics can potentiate the effects of beta Beta agonists can increase blood glucose levels. Monitor agonists and may lead to an increase in the risk of adverse patients with diabetes carefully and adjust their effects. medications accordingly. Beta-Adrenergic Agonists: Albuterol (Proventil) Albuterol Important Considerations Albuterol is a short-acting beta2-specific Albuterol should not be used too frequently as it bronchodilator, meaning it selectively stimulates can increase systemic effects, such as tachycardia, beta2 receptors in the lungs. palpitations, and tremors. It's the most commonly used drug in this class due Albuterol is available in both oral and inhalational to its effectiveness and proven safety. dosage forms, with the inhalational form preferred for most patients. Beta-Adrenergic Agonists: Salmeterol (Serevent) Long-Acting Beta2 Maintenance Therapy Agonist Salmeterol is not for acute Salmeterol is a long-acting treatment, but for beta2-agonist maintenance therapy of bronchodilator that provides asthma and COPD. sustained relief from bronchospasm. Dosage Salmeterol should not be used more than twice daily, and the maximum dose is one puff twice a day. Anticholinergics: Mechanism of Action Acetylcholine (ACh) Acetylcholine (ACh) causes bronchial constriction and narrowing of the airways. Anticholinergics Anticholinergics bind to the ACh receptors, preventing ACh from binding. Bronchodilation As a result, bronchoconstriction is prevented, and the airways dilate. Anticholinergics: Mechanism of Action (Cont.) Blocking Acetylcholine Airway Relaxation Reduced Secretions Anticholinergics, such as Blocking these receptors prevents Anticholinergics indirectly help ipratropium, tiotropium, and acetylcholine from triggering reduce airway secretions, making it aclidinium, block acetylcholine bronchoconstriction, promoting easier for patients with COPD to from binding to muscarinic airway relaxation and dilation. breathe. receptors in the airway. Anticholinergics: Adverse Effects Dry Mouth Nasal Congestion Dryness in the mouth is Anticholinergics can a common side effect of also cause nasal anticholinergics. congestion, which can be uncomfortable. Headache Anxiety Patients may experience In some cases, anxiety headaches as a side may occur with effect of anticholinergic anticholinergic use. use. Anticholinergics: Ipratropium (Atrovent) Ipratropium (Atrovent) Other Anticholinergics Ipratropium is the oldest and most commonly used 1. Tiotropium (Spiriva) anticholinergic bronchodilator. 2. Aclidinium (Tudorza) It is available as a liquid aerosol for inhalation and 3. Umeclidinium (Incruse Ellipta) as a multidose inhaler. Usually dosed twice daily, ipratropium is a commonly prescribed bronchodilator for patients with COPD. Xanthine Derivatives Plant Alkaloids Caffeine, theobromine, and theophylline are naturally occurring in plants. Theophylline Theophylline is the only xanthine derivative used for bronchodilation. Synthetic Xanthines Aminophylline and dyphylline are synthetic xanthines, often used in medical settings. Xanthine Derivatives: Mechanism of Action Inhibition 1 Xanthines inhibit phosphodiesterase. cAMP 2 Phosphodiesterase breaks down cAMP. Increased cAMP 3 Inhibition of phosphodiesterase increases cAMP. Bronchodilation 4 Increased cAMP causes smooth muscle relaxation. Xanthines are a class of drugs that act as bronchodilators. They exert their effects by inhibiting phosphodiesterase, the enzyme that breaks down cyclic adenosine monophosphate (cAMP). Xanthine Derivatives: Drug Effects Bronchodilation Increased Airflow CNS Stimulation Cardiovascular Stimulation Xanthines relax the Bronchodilation Xanthine derivatives smooth muscle in the improves airflow into also stimulate the These drugs increase airways, resulting in and out of the lungs, central nervous system. heart rate and force of bronchodilation. relieving bronchospasm. contraction, enhancing cardiac output and blood flow to the kidneys. Xanthine Derivatives: Indications Bronchodilation Acute Asthma Xanthine derivatives dilate These drugs may be used to airways in chronic respiratory manage mild to moderate acute conditions, including asthma, asthma attacks. However, they chronic bronchitis, and are not the first-line treatment emphysema. for severe attacks. COPD Management Limited Use Xanthine derivatives may be Xanthine derivatives are not used as an adjunct treatment in commonly used due to potential COPD, often in combination with drug interactions and variability other bronchodilators. in blood levels, which requires careful monitoring. Xanthine Derivatives: Adverse Effects Gastrointestinal Cardiovascular Nausea, vomiting, and loss of appetite are common side Xanthines can increase heart rate and cause effects. Gastroesophageal reflux can occur, especially arrhythmias, such as extrasystoles, palpitations, and during sleep. ventricular dysrhythmias. Urinary Metabolic Transient increased urination is a possible adverse Hyperglycemia is a potential risk, especially in patients effect. with diabetes. Xanthine Derivatives: Caffeine Over-the-Counter Use Pediatric Uses Caffeine is used over-the-counter as a central Caffeine is used as a cardiac stimulant in infants nervous system stimulant or analeptic to promote with bradycardia. alertness. It can be used by people who drive for Caffeine can also be used to enhance respiratory long durations, study for long periods, or combat drive in infants. sleepiness. Xanthine Derivatives: Theophylline Dosage Forms Theophylline is available in oral, rectal, injectable, and topical forms. Aminophylline Aminophylline is an intravenous (IV) form used for patients with status asthmaticus who have not responded to fast-acting beta agonists such as epinephrine. Therapeutic Range The therapeutic range for theophylline blood levels is 10 to 20 mcg/mL, though most clinicians advise levels between 5 and 15 mcg/mL. Nonbronchodilating Respiratory Drugs Leukotriene Receptor Corticosteroids Mast Cell Stabilizers Antagonists (LTRAs) These drugs are used to reduce Mast cell stabilizers help to These drugs are used to prevent inflammation in the airways, prevent the release of histamine, asthma attacks, not to treat acute which helps to prevent asthma which is a substance that causes attacks. They are sometimes attacks. inflammation and airway called leukotriene modifiers. constriction in the lungs. Leukotriene Receptor Antagonists (LTRAs) Nonbronchodilating Newer Class LTRAs are a newer class of LTRAs offer an alternative asthma medications that do to traditional asthma not directly relax airway medications, such as beta- smooth muscle. Instead, agonists and they block the action of corticosteroids. leukotrienes. Currently Available Drugs The most common LTRAs include montelukast, zafirlukast, and zileuton. LTRAs: Mechanism of Action Leukotrienes are substances that are released when a trigger, such as cat hair or dust, starts a series of chemical reactions in the body. Leukotrienes cause inflammation, bronchoconstriction, and mucus production, leading to coughing, wheezing, and shortness of breath. Prevent Leukotriene Binding 1 LTRAs block leukotrienes from attaching to their receptors. Reduced Inflammation 2 Inflammation in the lungs is reduced. Asthma Symptom Relief 3 Asthma symptoms are relieved. LTRAs: Drug Effects Bronchial Airways Mucus Secretion Leukotriene receptor antagonists (LTRAs) LTRAs reduce the secretion of mucus, which block leukotrienes, preventing smooth can contribute to airway obstruction. muscle contraction in the bronchi and decreasing airway constriction. Inflammation Black Box Warning By blocking leukotrienes, LTRAs decrease Montelukast, an LTRA, carries a black box inflammation in the lungs, reducing warning for serious mood changes and neutrophil and leukocyte infiltration. behaviors. LTRAs: Indications Prophylaxis & Long-Term Treatment Management LTRAs are used to prevent LTRAs provide long-term and treat asthma in adults control of asthma and children 12 years or symptoms and reduce the older. frequency of attacks. Not for Acute Attacks Allergic Rhinitis LTRAs are not meant for Montelukast is also immediate relief of acute approved for treating asthma exacerbations. allergic rhinitis symptoms. LTRAs: Contraindications Known Drug Allergy Previous Adverse Drug Inactive Ingredients Reaction Patients with a known drug It is important to note allergies allergy to leukotriene receptor If a patient has experienced a to inactive ingredients such as antagonists should not receive previous adverse drug reaction povidone, lactose, titanium these medications. to leukotriene receptor dioxide, or cellulose derivatives, antagonists, these medications which are present in these should be avoided. drugs. LTRAs: Adverse Effects Headache Nausea Diarrhea Dizziness Headache is a common Nausea is another Diarrhea, although less Dizziness can occur with adverse effect of frequent side effect of common, is a potential zileuton, especially leukotriene receptor LTRAs, often adverse effect of LTRAs, during the initial stages antagonists (LTRAs). accompanied by particularly zafirlukast of treatment. headache. and montelukast. Corticosteroids (Glucocorticoids) 1 1. Anti-inflammatory Properties 2 2. Chronic Asthma Corticosteroids have potent anti-inflammatory effects, Corticosteroids are crucial for managing chronic reducing inflammation in the airways. asthma, preventing exacerbations. 3 3. Systemic Effects 4 4. Long-Term Use Oral corticosteroids have systemic effects, while It takes several weeks for corticosteroids to achieve full inhaled forms are more localized, minimizing side therapeutic effects. effects. Corticosteroids: Mechanism of Action Stabilize Membranes Corticosteroids work by stabilizing the membranes of cells that release harmful bronchoconstricting substances, such as leukocytes. Increase Responsiveness Corticosteroids also increase the responsiveness of bronchial smooth muscle to beta-adrenergic stimulation. Dual Effect This results in a dual effect of both reducing inflammation and enhancing the activity of beta agonists. Corticosteroids: Mechanism of Action (Cont.) 1 Increased Receptor Responsiveness Corticosteroids also help to increase the sensitivity of bronchial smooth muscle to beta-adrenergic receptor stimulation. 2 Beta-Agonist Stimulation Corticosteroids enhance the stimulation of beta2 receptors by beta agonist drugs like albuterol. 3 Improved Bronchodilation This results in more pronounced bronchodilation and a more effective response to beta-agonist therapy. Inhaled Corticosteroids Beclomethasone Budesonide (Pulmicort Ciclesonide (Omnaris) dipropionate (Beclovent) Turbuhaler) Ciclesonide is a newer inhaled Beclomethasone dipropionate is an Budesonide is another inhaled corticosteroid for asthma, with a inhaled corticosteroid used for corticosteroid, also used for long- longer duration of action than some long-term control of asthma. term asthma management and other options. reducing exacerbations. Flunisolide (AeroBid) Fluticasone Mometasone (Asmanex) Flunisolide is an inhaled Fluticasone is available in both Mometasone is an inhaled corticosteroid indicated for the inhaled (Flovent) and intranasal corticosteroid used for long-term treatment of asthma in adults and (Flonase) forms, used for asthma control of asthma in adults and children. and allergic rhinitis respectively. children. Triamcinolone acetonide (Azmacort) Triamcinolone acetonide is an inhaled corticosteroid used for the treatment of asthma. Inhaled Corticosteroids: Indications Asthma Management Persistent Asthma Combined Therapy Inhaled corticosteroids are They are often prescribed for Inhaled corticosteroids are primarily used to control persistent asthma, which frequently used alongside beta- inflammation in the airways, requires ongoing management to adrenergic agonists for which is a key factor in asthma. prevent symptoms. comprehensive asthma control. Inhaled Corticosteroids: Contraindications Drug Allergy Acute Asthma Attacks Inhaled corticosteroids are not Inhaled corticosteroids are not a suitable for patients who have a primary treatment for acute known allergy to these drugs. asthma attacks; other treatments are used for this purpose. Hypersensitivity Fungal Infection Patients who have Inhaled corticosteroids should not hypersensitivity to be administered to patients with glucocorticoids, which is a family systemic fungal infections or who of hormones that includes have a positive sputum test for corticosteroids, should not use Candida organisms. these medications. Inhaled Corticosteroids: Adverse Effects Pharyngeal Irritation Coughing Inhaled corticosteroids can cause irritation and Some individuals may experience coughing as a side inflammation of the throat, leading to a scratchy effect of inhaled corticosteroids, particularly when feeling or sore throat. starting treatment. Dry Mouth Oral Fungal Infections Dry mouth can occur due to the drying effect of Inhaled corticosteroids can increase the risk of oral inhaled corticosteroids on the oral mucosa. fungal infections, commonly known as thrush, due to the moist environment in the mouth. Systemic effects are rare because low doses are used for inhalation therapy. However, higher doses or prolonged use can lead to systemic effects, such as adrenal suppression, osteoporosis, and cataracts. Inhaled Corticosteroids: Drug Interactions Systemic vs. Inhaled Common Interactions Drug interactions are more likely to occur with May increase serum glucose levels, possibly systemic (versus inhaled) corticosteroids. requiring adjustments in dosages of antidiabetic drugs. Inhaled corticosteroids are generally safe and well- Cyclosporine and tacrolimus: May increase the risk tolerated. of infections, particularly in patients with renal They are less likely to cause systemic effects, such as impairment. adrenal suppression. Itraconazole, ketoconazole, and other strong inhibitors of CYP3A4: May increase the risk of adverse effects of inhaled corticosteroids. Phenytoin, phenobarbital, and rifampin: May decrease the effectiveness of inhaled corticosteroids. Inhalers: Patient Education Inhaler Technique Dose Tracking Educate patients on proper Ensure patients can monitor inhaler technique to ensure their medication use. effective medication delivery. 1. Explain how to count 1. Demonstrate and practice remaining doses. inhaler use. 2. Encourage patients to refill 2. Emphasize correct timing of prescriptions before running inhalation and activation. out. 3. Provide a spacer for patients 3. Advise patients to keep with coordination difficulties. inhalers in a safe and accessible location.