Podcast
Questions and Answers
In the context of managing a patient with severe, persistent allergic asthma currently stabilized on inhaled corticosteroids (ICS) and long-acting beta-agonists (LABA), which of the following represents the MOST nuanced and evidence-based approach to the potential introduction of a leukotriene receptor antagonist (LTRA), considering both efficacy and safety profiles?
In the context of managing a patient with severe, persistent allergic asthma currently stabilized on inhaled corticosteroids (ICS) and long-acting beta-agonists (LABA), which of the following represents the MOST nuanced and evidence-based approach to the potential introduction of a leukotriene receptor antagonist (LTRA), considering both efficacy and safety profiles?
- Prescribe LTRA empirically for all patients with allergic asthma uncontrolled on ICS/LABA to reduce the likelihood of oral corticosteroid bursts, irrespective of their allergic or inflammatory profiles, and encourage shared decision-making regarding potential but rare adverse events.
- Initiate LTRA therapy immediately as an add-on to the existing ICS/LABA regimen, given the synergistic anti-inflammatory effects, without specific regard to individual patient phenotypes or endotypes.
- Conduct comprehensive phenotyping, including assessment for aspirin-exacerbated respiratory disease (AERD) and allergic rhinitis, and reserve LTRA use for patients exhibiting these characteristics, while closely monitoring for neuropsychiatric side effects. (correct)
- Discontinue the LABA component of the ICS/LABA combination and replace it with an LTRA to minimize beta-agonist exposure, which may indirectly address potential tachyphylaxis and beta-receptor downregulation in chronic asthma management.
A patient with a history of COPD and concomitant cardiovascular disease is prescribed ipratropium bromide for bronchodilation. Which of the following considerations is MOST critical in ensuring patient safety and optimizing therapeutic outcomes, given the patient's comorbidities and the pharmacological profile of ipratropium?
A patient with a history of COPD and concomitant cardiovascular disease is prescribed ipratropium bromide for bronchodilation. Which of the following considerations is MOST critical in ensuring patient safety and optimizing therapeutic outcomes, given the patient's comorbidities and the pharmacological profile of ipratropium?
- Recommend concurrent use of a beta-agonist, such as albuterol, to offset the potential for paradoxical bronchoconstriction associated with ipratropium, without regard to the synergistic impact on heart rate and blood pressure.
- Assess the patient's existing cardiovascular medication regimen for potential interactions with ipratropium, and counsel the patient on recognizing and reporting symptoms of anticholinergic excess, while ensuring adequate hydration to mitigate potential constipation. (correct)
- Instruct the patient to administer ipratropium liberally, particularly during episodes of dyspnea, to preemptively counteract bronchospasm, irrespective of the potential for anticholinergic side effects.
- Monitor the patient exclusively for pulmonary function improvements, as cardiovascular effects are negligible with inhaled anticholinergics, and advise the patient to disregard any palpitations or dizziness as unrelated to ipratropium.
A patient with nocturnal asthma poorly controlled on standard-dose inhaled corticosteroids is being considered for salmeterol as an add-on therapy. Considering the specific chronopharmacological aspects of asthma and the pharmacological properties of salmeterol, what instruction would optimize its therapeutic effect while minimizing potential risks?
A patient with nocturnal asthma poorly controlled on standard-dose inhaled corticosteroids is being considered for salmeterol as an add-on therapy. Considering the specific chronopharmacological aspects of asthma and the pharmacological properties of salmeterol, what instruction would optimize its therapeutic effect while minimizing potential risks?
- Prescribe salmeterol as a rescue medication to be used only during acute nocturnal asthma attacks, regardless of its delayed onset of action, and avoid long-term daily use to prevent tachyphylaxis.
- Instruct the patient to inhale salmeterol approximately 30-60 minutes before anticipated nocturnal symptom exacerbation, allowing sufficient time for beta2-adrenoceptor activation and downstream bronchodilation, and emphasize the importance of regular morning peak flow monitoring. (correct)
- Administer salmeterol exclusively at bedtime to directly counteract nocturnal bronchoconstriction, ensuring maximal drug concentration during sleep, and ignore any potential impact on morning peak flow.
- Advise the patient to take salmeterol upon waking and at bedtime, irrespective of symptom control, to maintain consistent bronchodilation throughout the circadian cycle, overlooking potential long-term adverse effects.
A patient with a known history of severe, recurrent bronchospasms is prescribed salmeterol as a monotherapy PRN. Given the established pharmacological guidelines, what is the MOST critical concern regarding this therapeutic regimen?
A patient with a known history of severe, recurrent bronchospasms is prescribed salmeterol as a monotherapy PRN. Given the established pharmacological guidelines, what is the MOST critical concern regarding this therapeutic regimen?
In a patient with moderate persistent asthma experiencing suboptimal control despite consistent adherence to inhaled corticosteroids (ICS) and as-needed short-acting beta-agonists (SABA), what would be the MOST evidence-based stepwise approach to incorporating a long-acting beta-agonist (LABA) for improved symptom management, considering current asthma management guidelines and pharmacological principles?
In a patient with moderate persistent asthma experiencing suboptimal control despite consistent adherence to inhaled corticosteroids (ICS) and as-needed short-acting beta-agonists (SABA), what would be the MOST evidence-based stepwise approach to incorporating a long-acting beta-agonist (LABA) for improved symptom management, considering current asthma management guidelines and pharmacological principles?
A patient taking salmeterol reports increased anxiety, palpitations and insomnia. Considering potential drug-natural product interactions, which of the following concurrent uses is MOST likely contributing to these adverse effects?
A patient taking salmeterol reports increased anxiety, palpitations and insomnia. Considering potential drug-natural product interactions, which of the following concurrent uses is MOST likely contributing to these adverse effects?
A patient on salmeterol therapy is also prescribed a beta-blocker for hypertension management. What is the PRIMARY concern regarding this drug interaction at the receptor level?
A patient on salmeterol therapy is also prescribed a beta-blocker for hypertension management. What is the PRIMARY concern regarding this drug interaction at the receptor level?
A patient with seasonal allergic rhinitis presents with paradoxical nasal congestion and increased rhinitis symptoms despite consistent use of a first-generation antihistamine (e.g., diphenhydramine). Which of the following mechanisms BEST explains this clinical phenomenon?
A patient with seasonal allergic rhinitis presents with paradoxical nasal congestion and increased rhinitis symptoms despite consistent use of a first-generation antihistamine (e.g., diphenhydramine). Which of the following mechanisms BEST explains this clinical phenomenon?
A patient with persistent asthma despite consistent inhaled corticosteroid use is initiated on salmeterol therapy. After a week, the patient reports no improvement and an increase in nocturnal asthma symptoms. What is the MOST appropriate next step in managing this patient?
A patient with persistent asthma despite consistent inhaled corticosteroid use is initiated on salmeterol therapy. After a week, the patient reports no improvement and an increase in nocturnal asthma symptoms. What is the MOST appropriate next step in managing this patient?
A patient on salmeterol develops hypokalemia. What underlying mechanism involving digoxin could exacerbate this electrolyte imbalance and increase the risk of digoxin toxicity?
A patient on salmeterol develops hypokalemia. What underlying mechanism involving digoxin could exacerbate this electrolyte imbalance and increase the risk of digoxin toxicity?
A patient with COPD and a history of cardiovascular disease is prescribed salmeterol for long-term bronchodilation. Which pre-existing condition requires MOST careful monitoring due to potential exacerbation by Salmeterol?
A patient with COPD and a history of cardiovascular disease is prescribed salmeterol for long-term bronchodilation. Which pre-existing condition requires MOST careful monitoring due to potential exacerbation by Salmeterol?
What is the MOST likely mechanism by which salmeterol alleviates bronchospasm in a patient with COPD?
What is the MOST likely mechanism by which salmeterol alleviates bronchospasm in a patient with COPD?
A patient taking tricyclic antidepressants (TCAs) is newly prescribed salmeterol. What potential interaction warrants heightened clinical vigilance?
A patient taking tricyclic antidepressants (TCAs) is newly prescribed salmeterol. What potential interaction warrants heightened clinical vigilance?
A patient presents to the emergency department with acute bronchospasm despite using their prescribed salmeterol inhaler as directed. Recognizing the limitations of salmeterol, what immediate intervention is MOST appropriate?
A patient presents to the emergency department with acute bronchospasm despite using their prescribed salmeterol inhaler as directed. Recognizing the limitations of salmeterol, what immediate intervention is MOST appropriate?
Following administration of salmeterol via inhalation, a patient's serum digoxin levels are observed to decrease. Which underlying mechanism BEST explains this observation?
Following administration of salmeterol via inhalation, a patient's serum digoxin levels are observed to decrease. Which underlying mechanism BEST explains this observation?
A patient with a long-standing history of nocturnal asthma is currently managed with inhaled fluticasone and salmeterol. Despite adherence, the patient reports persistent nighttime symptoms. Which of the following interventions demonstrates the MOST sophisticated understanding of optimizing beta-adrenergic receptor sensitivity in this context?
A patient with a long-standing history of nocturnal asthma is currently managed with inhaled fluticasone and salmeterol. Despite adherence, the patient reports persistent nighttime symptoms. Which of the following interventions demonstrates the MOST sophisticated understanding of optimizing beta-adrenergic receptor sensitivity in this context?
A patient with severe, chronic COPD exacerbations despite optimal inhaled bronchodilator and corticosteroid therapy exhibits paradoxical bronchospasm following ipratropium administration. Which underlying mechanism MOST plausibly explains this counterintuitive reaction?
A patient with severe, chronic COPD exacerbations despite optimal inhaled bronchodilator and corticosteroid therapy exhibits paradoxical bronchospasm following ipratropium administration. Which underlying mechanism MOST plausibly explains this counterintuitive reaction?
A researcher is investigating novel therapeutic strategies for asthma management. They hypothesize that a specific leukotriene modifier, compound X, exhibits superior efficacy compared to montelukast due to its unique mechanism of action. Which of the following mechanisms would BEST support this hypothesis?
A researcher is investigating novel therapeutic strategies for asthma management. They hypothesize that a specific leukotriene modifier, compound X, exhibits superior efficacy compared to montelukast due to its unique mechanism of action. Which of the following mechanisms would BEST support this hypothesis?
A patient with a history of severe allergic rhinitis and asthma presents with paradoxical worsening of asthma symptoms following the initiation of high-dose fexofenadine therapy. Which of the following mechanisms BEST elucidates this unexpected clinical outcome?
A patient with a history of severe allergic rhinitis and asthma presents with paradoxical worsening of asthma symptoms following the initiation of high-dose fexofenadine therapy. Which of the following mechanisms BEST elucidates this unexpected clinical outcome?
A clinical trial is evaluating the efficacy of a novel inhaled corticosteroid (ICS) with enhanced glucocorticoid receptor (GR) binding affinity and prolonged lung retention. Which of the following biomarkers would provide the MOST compelling evidence of superior anti-inflammatory activity compared to standard ICS?
A clinical trial is evaluating the efficacy of a novel inhaled corticosteroid (ICS) with enhanced glucocorticoid receptor (GR) binding affinity and prolonged lung retention. Which of the following biomarkers would provide the MOST compelling evidence of superior anti-inflammatory activity compared to standard ICS?
A patient with moderate persistent asthma is well-controlled on a combination inhaler containing fluticasone propionate and salmeterol. However, they develop significant hoarseness and dysphonia. What intervention reflects the MOST nuanced strategy for managing this adverse effect while preserving optimal asthma control?
A patient with moderate persistent asthma is well-controlled on a combination inhaler containing fluticasone propionate and salmeterol. However, they develop significant hoarseness and dysphonia. What intervention reflects the MOST nuanced strategy for managing this adverse effect while preserving optimal asthma control?
A patient using a SABA reports increased usage over the past several weeks. Besides stepping up controller medications, what is the MOST critical assessment to perform initially, to differentiate between various underlying causes of increased SABA use?
A patient using a SABA reports increased usage over the past several weeks. Besides stepping up controller medications, what is the MOST critical assessment to perform initially, to differentiate between various underlying causes of increased SABA use?
An investigator is designing a study to evaluate the bronchodilatory efficacy of a novel anticholinergic agent with purported M3 receptor-selective antagonism and rapid dissociation kinetics. Which study design element would be MOST critical to incorporate in order to accurately assess the agent's potential clinical advantages over existing anticholinergics like ipratropium?
An investigator is designing a study to evaluate the bronchodilatory efficacy of a novel anticholinergic agent with purported M3 receptor-selective antagonism and rapid dissociation kinetics. Which study design element would be MOST critical to incorporate in order to accurately assess the agent's potential clinical advantages over existing anticholinergics like ipratropium?
A patient with severe COPD exacerbation is unresponsive to initial SABA therapy. Which of the following mechanisms explains the rationale for adding ipratropium to their treatment regimen?
A patient with severe COPD exacerbation is unresponsive to initial SABA therapy. Which of the following mechanisms explains the rationale for adding ipratropium to their treatment regimen?
A researcher is investigating the effects of ipratropium on airway smooth muscle contractility in vitro. Which signaling pathway would be most directly affected by the administration of ipratropium?
A researcher is investigating the effects of ipratropium on airway smooth muscle contractility in vitro. Which signaling pathway would be most directly affected by the administration of ipratropium?
A patient with chronic bronchitis is prescribed ipratropium via nebulization. The patient reports blurred vision and dry mouth shortly after administration. Which of the following best explains the etiology of these adverse effects?
A patient with chronic bronchitis is prescribed ipratropium via nebulization. The patient reports blurred vision and dry mouth shortly after administration. Which of the following best explains the etiology of these adverse effects?
In the context of managing COPD, what is the primary rationale for choosing ipratropium over a short-acting beta-2 agonist (SABA) as a first-line treatment for patients with predominantly persistent symptoms?
In the context of managing COPD, what is the primary rationale for choosing ipratropium over a short-acting beta-2 agonist (SABA) as a first-line treatment for patients with predominantly persistent symptoms?
A researcher aims to develop a novel drug that selectively enhances the therapeutic effects of ipratropium while minimizing its systemic side effects. Which of the following strategies would be most promising?
A researcher aims to develop a novel drug that selectively enhances the therapeutic effects of ipratropium while minimizing its systemic side effects. Which of the following strategies would be most promising?
A patient using both ipratropium and a SABA reports increased heart rate and anxiety. How would you differentiate whether these side effects are more likely attributable to the SABA or the ipratropium?
A patient using both ipratropium and a SABA reports increased heart rate and anxiety. How would you differentiate whether these side effects are more likely attributable to the SABA or the ipratropium?
What is the predicted impact on mucociliary clearance in COPD patients when initiating ipratropium therapy?
What is the predicted impact on mucociliary clearance in COPD patients when initiating ipratropium therapy?
In a patient with combined asthma and COPD ('overlap syndrome'), what considerations guide the decision to initiate ipratropium, given its mechanism and potential effects?
In a patient with combined asthma and COPD ('overlap syndrome'), what considerations guide the decision to initiate ipratropium, given its mechanism and potential effects?
A clinical trial is designed to compare the efficacy of nebulized ipratropium versus intravenous theophylline in treating acute COPD exacerbations. What are the critical comparative endpoints to assess the relative clinical effectiveness?
A clinical trial is designed to compare the efficacy of nebulized ipratropium versus intravenous theophylline in treating acute COPD exacerbations. What are the critical comparative endpoints to assess the relative clinical effectiveness?
Which of the following interventions would be most effective in mitigating the risk of systemic anticholinergic side effects associated with long-term ipratropium use in elderly patients with COPD?
Which of the following interventions would be most effective in mitigating the risk of systemic anticholinergic side effects associated with long-term ipratropium use in elderly patients with COPD?
In a patient with well-controlled asthma on a medium-dose inhaled corticosteroid, what is the most critical consideration when contemplating the addition of salmeterol?
In a patient with well-controlled asthma on a medium-dose inhaled corticosteroid, what is the most critical consideration when contemplating the addition of salmeterol?
In a pregnant patient with poorly controlled asthma, despite optimized inhaled corticosteroid therapy, what is the most critical factor to consider before initiating salmeterol?
In a pregnant patient with poorly controlled asthma, despite optimized inhaled corticosteroid therapy, what is the most critical factor to consider before initiating salmeterol?
A patient with a history of poorly controlled hypertension and newly diagnosed asthma requires a long-acting bronchodilator. What is the most critical consideration when choosing between salmeterol and theophylline?
A patient with a history of poorly controlled hypertension and newly diagnosed asthma requires a long-acting bronchodilator. What is the most critical consideration when choosing between salmeterol and theophylline?
A pediatric patient is prescribed salmeterol for asthma management. The patient's parent reports regularly administering a herbal supplement containing guarana. What is the most relevant counseling point regarding this concurrent use?
A pediatric patient is prescribed salmeterol for asthma management. The patient's parent reports regularly administering a herbal supplement containing guarana. What is the most relevant counseling point regarding this concurrent use?
A patient taking salmeterol develops a severe asthma exacerbation requiring intubation. Upon further investigation, it is discovered that the patient was self-medicating with an over-the-counter decongestant containing a non-selective beta-adrenergic agonist. What is the most likely mechanism by which this combination contributed to the patient's respiratory failure?
A patient taking salmeterol develops a severe asthma exacerbation requiring intubation. Upon further investigation, it is discovered that the patient was self-medicating with an over-the-counter decongestant containing a non-selective beta-adrenergic agonist. What is the most likely mechanism by which this combination contributed to the patient's respiratory failure?
A patient with a known allergy to milk proteins is prescribed salmeterol via dry powder inhaler (DPI). Which of the following actions is most appropriate?
A patient with a known allergy to milk proteins is prescribed salmeterol via dry powder inhaler (DPI). Which of the following actions is most appropriate?
A patient with well-controlled asthma on salmeterol and an inhaled corticosteroid is started on itraconazole for a fungal infection. Which of the following monitoring parameters is most critical in this patient?
A patient with well-controlled asthma on salmeterol and an inhaled corticosteroid is started on itraconazole for a fungal infection. Which of the following monitoring parameters is most critical in this patient?
A patient with severe persistent asthma is prescribed salmeterol as adjunctive therapy to high-dose inhaled corticosteroids and montelukast. Despite optimal adherence, the patient continues to experience frequent exacerbations. Pulmonary function testing reveals significant air trapping and hyperinflation. Which of the following interventions is most likely to provide additional benefit in this patient?
A patient with severe persistent asthma is prescribed salmeterol as adjunctive therapy to high-dose inhaled corticosteroids and montelukast. Despite optimal adherence, the patient continues to experience frequent exacerbations. Pulmonary function testing reveals significant air trapping and hyperinflation. Which of the following interventions is most likely to provide additional benefit in this patient?
A patient with nocturnal asthma is prescribed salmeterol to improve their symptoms. What is the MOST important information to give to the patient?
A patient with nocturnal asthma is prescribed salmeterol to improve their symptoms. What is the MOST important information to give to the patient?
A patient who is prescribed Salmeterol also reports that they take St. John's Wort for their anxiety and depression. As St. John's Wort is a CYP3A4 inducer, what is the MOST important information to tell the patient
A patient who is prescribed Salmeterol also reports that they take St. John's Wort for their anxiety and depression. As St. John's Wort is a CYP3A4 inducer, what is the MOST important information to tell the patient
Flashcards
SABA
SABA
Rapid relief of acute bronchospasm.
SABA side effects
SABA side effects
Tremors, tachycardia, nervousness.
LABA
LABA
Long-term bronchodilation as maintenance, not for acute relief.
Anticholinergics
Anticholinergics
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Anticholinergic side effects
Anticholinergic side effects
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Inhaled Corticosteroids (ICS)
Inhaled Corticosteroids (ICS)
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ICS Usage Tip
ICS Usage Tip
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Proper Inhaler Technique
Proper Inhaler Technique
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Salmeterol & MAO inhibitors:
Salmeterol & MAO inhibitors:
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Salmeterol & Beta Blockers:
Salmeterol & Beta Blockers:
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Salmeterol & Digoxin:
Salmeterol & Digoxin:
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Salmeterol & Tricyclic Antidepressants:
Salmeterol & Tricyclic Antidepressants:
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Salmeterol & Potassium-Losing Diuretics:
Salmeterol & Potassium-Losing Diuretics:
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Salmeterol & Caffeine:
Salmeterol & Caffeine:
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Salmeterol Action:
Salmeterol Action:
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Salmeterol Use:
Salmeterol Use:
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Salmeterol - Specific Use:
Salmeterol - Specific Use:
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Salmeterol - Not Used For:
Salmeterol - Not Used For:
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ICS+LABA Combinations
ICS+LABA Combinations
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Methylxanthines (Theophylline)
Methylxanthines (Theophylline)
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Leukotriene Modifiers (Montelukast)
Leukotriene Modifiers (Montelukast)
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Oral Corticosteroids (Prednisone)
Oral Corticosteroids (Prednisone)
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Medication Adherence
Medication Adherence
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Anticholinergic Action
Anticholinergic Action
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Ipratropium Class
Ipratropium Class
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Ipratropium Mechanism
Ipratropium Mechanism
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Symptoms Relieved by Ipratropium
Symptoms Relieved by Ipratropium
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Main COPD Conditions Treated by Ipratropium
Main COPD Conditions Treated by Ipratropium
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Inhalation Mechanism of Ipratropium
Inhalation Mechanism of Ipratropium
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Inhaled Ipratropium Advantage
Inhaled Ipratropium Advantage
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Intranasal Ipratropium Action
Intranasal Ipratropium Action
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Ipratropium First-Line Use
Ipratropium First-Line Use
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How Ipratropium Works
How Ipratropium Works
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LABA monotherapy in asthma
LABA monotherapy in asthma
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LABA contraindications
LABA contraindications
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LABA risk with no ICS
LABA risk with no ICS
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LABA caution conditions
LABA caution conditions
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LABA in pregnancy
LABA in pregnancy
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LABA while breastfeeding
LABA while breastfeeding
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LABA interaction with beta blockers
LABA interaction with beta blockers
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LABA interaction with MAOIs/TCAs
LABA interaction with MAOIs/TCAs
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LABA interaction with CYP3A4 inhibitors
LABA interaction with CYP3A4 inhibitors
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LABA interaction with caffeine
LABA interaction with caffeine
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Study Notes
Bronchodilators
- Therapeutic action: bronchodilation
Adrenergic Bronchodilators: Albuterol (Proventil)
- Therapeutic action: a sympathomimetic that increases cyclic adenosine monophosphate (cAMP) in bronchial tissue cells, leading to bronchodilation and relieving bronchospasms
- The drug stimulates beta-2 adrenergic receptors in the smooth muscles of the airways, causing these muscles to relax, decreasing airway resistance and facilitating airflow to the lungs
- Beta2 agonists have a limited role in suppressing histamine release in the lung and increasing ciliary motility
Indications for Albuterol
- Functions as a short-acting bronchodilator (SABA)
- Used as a "rescue inhaler"
- Functions as selective beta2 agonist
- Commonly used as a first-line therapy PRN (as needed) for SOB (shortness of breath) associated with COPD
- Used for the quick relief of acute bronchospasm in conditions like asthma and COPD
- If SABA is needed more than 2-3 times a week suggests asthma is poorly controlled, and adjustments to baseline therapy may be needed
Pharmacokinetics of Albuterol
- Onset for inhaled: rapid onset (1-15 min), peak in 30-60 min, and duration lasts for 3-6 hours
- Onset for oral: onset 15-30 min, peak 2-3 hours, and duration lasts for 4-6 hours or more
- Absorption: oral administration is well absorbed in the GI tract and rapidly enters the bloodstream; systemic concentration is low when inhaled
- Distribution: widely distributed in the body tissues; small amounts appear in breast milk
- Metabolism: extensively metabolized by the liver
- Excretion: primarily in the urine as metabolites (~75%) and feces (~10%)
Contraindications of Albuterol
- Hypersensitivity to adrenergic amines
Precautions for Albuterol Use
- Used cautiously in patients with cardiac disease, hypertension, hyperthyroidism, diabetes, glaucoma, and seizure disorders
- Excess inhaler use may lead to tolerance and paradoxical bronchospasm
- Use during pregnancy only if potential maternal benefit justifies potential fetal risk
- Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
- Its safety and effectiveness has not been established for children younger than 2 years
- There is an increased risk of adverse reactions in older adults, and may require dose reduction
Adverse Reactions for Albuterol
- High doses may cause some degree of beta1 responses
- Reactions occur more often when given orally
- Side effects may diminish after a week or longer
- May cause paradoxical bronchospasm (excessive use of inhalers; wheezing)
- Results in central nervous system reactions: nervousness, tremors, insomnia, hyperactivity (in children), and headache
- Can cause cardiovascular system reactions: tachycardia, heart palpitations (high doses), elevated BP, angina, arrhythmias, and chest pain
- May result in gastrointestinal upset: nausea and vomiting
- Hyperglycemia and hypokalemia may occur
Drug-to-drug Interactions of Albuterol
- Concurrent use with other adrenergic agents will increase adrenergic side effects
- Use with MAO inhibitors may lead to hypertensive crisis
- Use with beta blockers may negate therapeutic effect
- May decrease serum digoxin levels (hypokalemia increases the risk)
- Use with Tricyclic antidepressants may potentiate cardiovascular effects
- Use of potassium-losing diuretics increases the risk of hypokalemia
- Use with caffeine-containing herbs (cola nut, guarana, tea, coffee) can increase stimulant effect
Salmeterol (Serevent Diskus)
- Therapeutic action: bronchodilation
Therapeutic Action of Salmeterol
- Mechanism of action is similar to SABA: produces accumulation of cAMP at beta2-adrenergic receptors
Indications of Salmeterol
- Functions as a long-acting bronchodilator (LABA)
- Used for long-term maintenance and prevention of bronchospasm in conditions like asthma, COPD, and exercise induced asthma
- Used concomitantly in patients who are currently taking but are inadequately controlled on an inhaled corticosteroid
- Typically used as a LABA and inhaled corticosteroid in combination to control asthma symptoms
- Not suitable for the relief of acute symptoms
Pharmacokinetics of Salmeterol
- Inhaled only: onset 10-25 min, peak 3-4 hours, duration 12 hours or 9 hours in adolescents.
- Half-life: 3-4 hrs
- Absorption: Slow absorption when inhaled, minimal systemic absorption
- Distribution: action is primarily local
- Metabolism: Metabolized in the liver via the CYP3A4 isoenzyme
- Excretion: 60% excreted in feces, 25% excreted in urine
Contraindications of Salmeterol
- Not suitable for relief of acute symptoms (PRN)
- Should not be used more than BID
- LABAs are not indicated for abortive therapy for bronchospasm; using this medication could result in unrelieved bronchospasm
- LABA usage is associated with increased risk of asthma related death, intubation or hospitalization is no longer recommended as monotherapy for asthma
- Contraindicated in hypersensitivity to salmeterol or milk proteins, acute attack of asthma (onset of action is delayed)
- Contraindicated in patients whose asthma is currently controlled on low- or medium-dose inhaled corticosteroid therapy
- Contraindicated in patients not receiving an inhaled corticosteroid because this increases the risk of asthma-related death
Precautions for Salmeterol Use
- Used cautiously in patients with cardiovascular disease (including angina and hypertension), seizure disorders, Diabetes, Glaucoma, Hyperthyroidism, Pheochromocytoma
- Use during pregnancy only if potential maternal benefit justifies potential fetal risk; may inhibit contractions during labor
- Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
- Safety and effectiveness has not been established for children under 4 years
Adverse Reactions of Salmeterol
- Cardiovascular: palpitations, tachycardia
- Gastrointestinal: abdominal pain, diarrhea, nausea
- Musculoskeletal: muscle cramps/soreness
- Neurological: headache, nervousness, tremor
- Respiratory: cough, paradoxical bronchospasm
Drug-to-drug Interactions of Salmeterol
- Beta blockers may decrease therapeutic effects
- MAO inhibitors and tricyclic antidepressants may potentiate cardiovascular effects
- Strong CYP3A4 inhibitors, including ketoconazole, itraconazole, ritonavir, atazanavir, clarithromycin, nefazodone, or nelfinavir, may increase levels and the risk of toxicity; concurrent use not recommended.
- Use with caffeine-containing herbs (cola nut, guarana, mate, tea, coffee) can increase stimulant effect
Methylxanthines (Theophylline)
- Therapeutic action: bronchodilation
Therapeutic Action of Theophylline
- Increases cAMP which relaxes the smooth muscles of the airways and pulmonary vessel and suppresses the response of the airways to stimuli
- Increases the force of contraction of diaphragmatic muscles, enhancing respiratory function
- IV theophylline is employed in emergencies
- Has impact on most body systems including: powerful CNS stimulants, dilates coronary vessels, and causes a diuretic effect
Indications of Theophylline
- Functions as a treatment option for COPD but not very frequently used in COPD and asthma
- Use only if beta2 agonists and anticholinergics are unavailable or if the patient cannot afford long-term therapy with other drugs
- Often used in combination with other medications for better control of symptoms
- Used to treat apnea of prematurity (AOP) due to its effect on CNS stimulation and effect on diaphragmatic contraction
Pharmacokinetics of Theophylline
- Onset: 30 min (for SR caps: 1-2 hours), duration for SR 8-25 hours or 6 hrs for IV or Oral theophylline
- Large volumes of fluid and high-protein meals may increase the rate of absorption
- Rapid and complete absorption in the GI tract after oral administration; ER tablets are affected by gastric pH and food
- Distribution: distributes freely into fat-free tissues but poorly into body fat; its volume of distribution may increase in certain conditions like prematurity, hepatic cirrhosis, and acidemia; crosses BBB and placenta
- Extensively metabolized in the liver by CYP450 enzymes (CYP 1A2, CYP 2E1, and CYP 3A4); medications that induce CYP450 can increase clearance of theophylline and it forms active metabolites such as caffeine and 3-methylxanthine.
- Tobacco smoking increases metabolism of theophylline, thereby decreasing the half-life of the drug.
- Excretion: Excreted mainly in the urine, with about 50% excreted unchanged in neonates and about 10% in older children and adults
Contraindications of Theophylline
- Patients with cardiac issues due to its stimulatory effects
- Patients with renal or hepatic dysfunction
Adverse Reactions of Theophylline
- Nausea/vomiting and gastric pain due to increased gastric acid secretion
- Tachycardia and irritability
- May cause seizures, cardiorespiratory collapse
- Signs of theophylline toxicity: none, can result in death
Drug-to-drug Interactions of Theophylline
- Beta-blockers and erythromycin: decrease liver metabolism of theophylline - thereby increasing the half-life and adverse effects of theophylline
- Barbiturates: induce CP450, stimulating theophylline metabolism which can result in subtherapeutic levels of theophylline
- Macrolide antibiotics: inhibits metabolism of theophylline and increases renal clearance of erythromycin
- Digoxin: increased risk of digoxin toxicity
- Lithium: theophylline decreases the effects of lithium
- Smoking: decreases theophylline levels; smoking cessation
- Caffeine: the effects of theophylline can be increased by foods containing caffeine
Monitoring for Theophylline
- Serum theophylline levels
- Toxicity is likely to occur when level exceeds 20 mcg/ml
- When levels exceed 30 mcg/ml: hyperglycemia; hypotension, seizures, brain damage and death can occur
- Screen client's diet, other drugs being taken (OTC drugs), smoking habits and adherence to prescribed regimen if serum levels of theophylline have not been stabilized
Theophylline Toxicity Treatment
- Charcoal, emesis, gastric lavage to decrease absorption of the oral medication
- Lidocaine: to treat dysrhythmias
- Diazepam: to control seizures
Anticholinergics: Ipratropium (Atrovent)
- Therapeutic action: bronchodilation
Therapeutic Action of Ipratropium
- Antagonizes the action of acetylcholine by blocking receptors
- Blocks muscarinic acetylcholine receptors in the airways, which leads to bronchodilation and reduced bronchospasm
- Decreases contractility of smooth muscle thereby reducing bronchospasm
- Is an atropine derivative
- Can be administered by oral inhalation or intranasal spray
- Inhalation inhibits cholinergic receptors in bronchial smooth muscle, resulting in decreased concentrations of cyclic guanosine monophosphate (cGMP). Decreased levels of cGMP produce local bronchodilation
Indications of Ipratropium
- Functions as a long-acting muscarinic antagonist (LAMA)
- Inhaled anticholinergic drugs are considered first treatment for COPD whose symptoms have become persistent
- Inhalation: bronchodilation without systemic anticholinergic effects
- Intranasal: Local application inhibits secretions from glands lining the nasal mucosa, reducing rhinorrhea
- Helps to relieve symptoms such as wheezing, coughing, chest tightness, and SOB
- Primarily used to manage and prevent symptoms of COPD, including chronic bronchitis and emphysema.
- It is also used in combination with other medications for severe asthma exacerbations
- Used off-label for asthma and is included in current evidence-based guidelines for asthma management
- Ipratropium with albuterol (Combivent) is used to treat chronic bronchitis
- The combination is more effective and has a longer duration of action that if either agent is used alone
- The combination is more effective in increasing FEV1 (which is the parameter used to evaluate asthmatics and obstructive lung disease and response to the bronchodilators)
Pharmacokinetics of Ipratropium
- Inhalation: onset 1-3 min, peak 1-2 hrs, duration 4-6 hrs
- Intranasal: onset 15 min, peak unknown, duration 6-12 hrs.
- Absorption: Minimal systemic absorption when inhaled (1-2% for inhalation solution; 20% for inhalation aerosol; <20% following nasal use), poorly absorbed from the lungs and GI tract
- Distribution: distributed throughout the body but does not significantly penetrate into body fat leaving 15% of dose reaching lower airways after inhalation
- Metabolism: Metabolized in the liver by cytochrome P450 enzymes.
- Excretion: Primarily excreted in the urine, with a small amount excreted unchanged; majority of swallowed dose excreted in feces unchanged
Contraindications of Ipratropium
- Acute bronchospasm
- Hypersensitivity to ipratropium, atropine, belladonna alkaloids, or bromide
- Cautious use in bladder-neck obstruction, prostatic hyperplasia, glaucoma, or urinary retention
- Safety not established in gestational breastfeeding
- Older adults may be more sensitive to effects
Adverse Reactions of Ipratropium
- Paradoxical bronchospasm with aerosol (especially with 1st inhalation in newly opened MDI)
- Dry mouth and irritation of the pharynx
- Cardiovascular: hypotension and palpitations
- Dermatological/rash
- Eyes, ears, nose, throat/blurred vision and sore throat, nasal dryness/irritation
- Gastrointestinal: GI irritation and nausea
- Neurological: dizziness, headache, nervousness
- Respiratory: bronchospasm and cough
- Miscellaneous hypersensitivity reactions: anaphylaxis
Drug-to-drug Interactions of Ipratropium
- Combined use with other drugs having anticholinergic properties (antihistamines, phenothiazines, and disopyramide) will increase anticholinergic effects
Teaching for Ipratropium
- Beta-agonist inhalant should administer it 5 min before using ipratropium
- When using this with an inhaled glucocorticoid or cromolyn, ipratropium should be used 5 minutes before the steroid or cromolyn
- Use causes the bronchioles to dilate so the steroid or cromolyn can be deposited in the bronchioles
- Use of aerosols can produce paradoxical acute bronchospasm that can be life-threatening, usually seen with the first inhalation from a newly opened MDI
- New MDI should be primed with 2 sprays before use
Inhaled Glucocorticoid Steroids (ICS): Flunisolide (AeroBid)
- Therapeutic action: anti-inflammatory
Therapeutic Action of Flunisolide
- Flunisolide is a synthetic corticosteroid that functions by decreasing airway inflammation
- The medication is used to prevent (not treat) an acute bronchoconstriction attack
- Inhibits the production of leukotrienes and prostaglandins through interference with arachidonic acid metabolism
- Reduces the migration and activity of the inflammatory cells
- Exerts its effects by binding to glucocorticoid receptors, leading to the suppression of inflammatory cytokines and mediators
- Increases the number and responsiveness of beta receptors in airway smooth muscles
- Diminishes airway inflammation, bronchial hyperresponsiveness, and mucus production, characteristics of asthma
Indications of Flunisolide
- First line treatment for persistent asthma
- Maintenance treatment of asthma as a prophylactic therapy in adults and pediatric patients >6 years and older
- Reduction or elimination of the need for oral corticosteroids in asthma patients requiring oral corticosteroid therapy
- Treatment of allergic rhinitis
Pharmacokinetics of Flunisolide
- Inhaled delivery: onset 5-10 min, peak 30-60 min, duration 12-24 hours, half-life 1.3-1.7 hours
- Absorbed through the lungs into bloodstream with minimal systemic absorption to decrease systemic side effects
- Widely Distributed throughout the body reaching various tissues to its anti-inflammatory effects
- Metabolized by the liver & excreted primarily in the urine
Contraindications of Flunisolide
- Primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required
- Use in children younger than 6 years of age.
Adverse Reactions of Flunisolide
- During inhalation (especially when a spacer is not used) flunisolide is deposited in the mouth and pharynx where some of the drug is swallowed which allows some systemic absorption to occur
- Sore throat (pharyngitis) and hoarseness
- Dry mouth
- Coughing (typically mild and transient)
- Runny nose (rhinitis) & sinusitis
- Oral fungal infections (candidiasis/thrush of mouth and pharynx)
- Paradoxical bronchospasms immediately after dosing
- Suppression of the hypothalamic-pituitary-adrenal (HPA) axis is possible with long term daily use, but this effect is very rare. ***
- Patients transitioning from oral to inhaled steroids have an increased risk of adrenal insufficiency if they experience trauma, surgery, or infections
Drug-to-drug Interactions of Flunisolide
- Desmopressin: can increase risk of hyponatremia
- Systemic corticoids: When transitioning from systemic corticosteroids to flunisolide, taper the systemic corticosteroids slowly to avoid adrenal insufficiency
- Immune suppressing medications: can exacerbate infections.
Leukotriene Receptor Antagonists: Zafirlukast (Accolate)
- Therapeutic action: prevent bronchoconstriction and vasodilation
Therapeutic Action of Zafirlukast
- Zafirlukast functions as a leukotriene receptor antagonist (LTRA) that works by blocking the action of leukotrienes, which are inflammatory chemicals the body releases in response to allergens
- The drug helps decrease inflammation, bronchoconstriction, and mucus production in the airways, making it effective in managing asthma symptoms
- The drug also decreases airway edema, smooth muscle constriction, and mucus production, thereby alleviating asthma symptoms
Indications of Zafirlukast
- Primarily for the prophylaxis and chronic treatment of asthma in adults and children aged 5 years and older
- Used as a long-term control medication to prevent asthma attacks and improve lung function
- Off-label uses include the management of chronic urticaria, prevention of exercise-induced bronchospasm, and treatment of allergic rhinitis
- Can be used as an alternative to inhaled corticosteroids, but is less effective
Pharmacokinetics of Zafirlukast
- Taken orally with an onset between 1-2 hours, peak at 3 hours, and duration lasts for 24 hours
- Half-life lasts 10 hours
- Absorption: rapidly absorbed after oral administration
- Distribution: highly protein bound in plasma (>99%, primarily to albumin) with moderate volume of distribution
- Metabolism: extensively metabolized by the liver, primarily by CYP2C9
- Excretion: mainly in the feces
- Effects take up to 2 weeks to be fully realized
- Should be taken on an empty stomach, either 1 hour before or 2 hours after meals to optimize absorption
Contraindications of Zafirlukast
- Patients with known hypersensitivity to the drug
- Should not be used to control acute asthma/asthma attack
- Severe liver disease (including cirrhosis) or with increased transaminases
- Should not be used in children >5 years
- Should not be used during an acute asthmatic attack
- Patients with Churg-Strauss syndrome (a rare blood condition) - should use with caution because it may make the condition worse
Adverse Reactions of Zafirlukast
- Headache
- Gastrointestinal: nausea, diarrhea, anorexia, abdominal pain
- Upper respiratory tract infections & cold symptoms
- Elevated liver enzymes
- Unusual changes in mood/behavior such as agitation, aggression, restlessness, irritability, anxiety, depression, confusion, problems with memory/attention, stuttering, tremors, uncontrolled muscle movements, suicidal thoughts, hallucinations, sleep problems, vivid dreams, sleep-walking, compulsive or repetitive behaviors
Drug-to-drug Interactions of Zafirlukast
- CYP3A4 Inhibitors: Drugs like erythromycin and ketoconazole can increase Zafirlukast levels
- CYP2C9 Inhibitors: Drugs like fluconazole and valproic acid can also increase Zafirlukast levels
- Drugs Metabolized by CYP3A4: Zafirlukast can increase the levels of drugs like warfarin, leading to an increased risk of bleeding
- There is increased warfarin elimination and anticoagulant dosages should be adjusted
- Theophylline levels may increase while on Zafirlukast monitor serum theophylline levels
- Aspirin increases the plasma concentration of Zafirlukast by 45%
Mast Cell Stabilizers: Cromolyn (Intal)
- Therapeutic action: anti-inflammatory
Therapeutic Action of Cromolyn
- Functions by inhibiting the release histamine and other inflammatory mediators of Type-I allergic reactions from mast cells, thereby preventing allergic reactions
- Works at the surface of the mast cell to inhibit its rupture and degranulation after contact with an antigen
- Suppresses bronchial inflammation causing a reduction in inflammatory cells and macrophages
Indications of Cromolyn
- Asthma: Prophylaxis of allergic and exercise-induced asthma
- Alternative to inhaled glucocorticoids
- Allergic Rhinitis: Symptomatic treatment of perennial allergic rhinitis
- Conjunctivitis: Treatment of vernal keratoconjunctivitis and vernal conjunctivitis
- Mastocytosis: Symptomatic treatment of systemic mastocytosis
- Food Allergy: Adjunct therapy in the treatment of food allergies
Pharmacokinetics of Cromolyn
- Administered via nebulizer
- onset 15 min, peak 30-60 min, duration 8-12 hours, half-life 80-90 min
- Maximal effects may take weeks to develop
- Approximately 8% of the inhaled dose is absorbed systemically through the lungs.
- Minimally distributed throughout the body due to its poor systemic absorption and remains largely within the respiratory tract
- Not extensively metabolized in the body; most of the drug is excreted unchanged
- Majority of the drug is excreted unchanged in the feces, with a small amount excreted in the urine
Contraindications of Cromolyn
- The drug should not be used during an acute asthma attack becuase this may worsen symptoms
- This drug shouldn't be used in patients who are allergic to cromolyn or any of its components
- Pts with severe renal or hepatic impairment
- Antiinflammatory effects are less than with glucocorticoids; therefore cromolyn is not a preferred drug for asthma therapy
- This drug has been presribed alternative therapy when glucocorticoids create problems
Adverse Reactions of Cromolyn
- Adverse effects occur in less than 1 of every 10,000 patients
- Nausea, vomiting, diarrhea, abdominal pain, bitter taste.
- Headache, dizziness, difficulty speaking
- Rash and itching
- Cough and throat irritation, bronchospasm
Drug-to-drug Interactions of Cromolyn
- Decreased potential for drug interactions due to minimal systemic absorption
Patient Education for Cromolyn
- Effective use requires regular administration
- Helps prevent but will not stop an attack in progress
- Effects may not be apparent until used regularly for at least 1 month
- If used to prevent exercise-induced bronchospasm: use 15-20 minutes prior to activity
- Rarely used but important to remember the medication is not a bronchodilator- it’s contraindicated for treating acute bronchospasm.
Drug Classes: Asthma and COPD
- Beta agonist: asthma & COPD, bronchodilation; symptom relief, improved airflow.
- Anticholinergics: COPD & asthma, bronchodilation, reduced mucus production, control of symptoms.
- Inhaled Corticosteroids: asthma & severe COPD, anti-inflammatory, prevention of exacerbations, airway remodeling control.
- Leukotriene Modifiers: asthma, anti-inflammatory, reduced bronchoconstriction, prevention of exercise-induced induced bronchospasm.
- PDE4 Inhibitors: COPD, inflammation, reduction in exacerbations.
- Immunomodulators: severe asthma, reduces number of exacerbations, and controls symptoms in allergic or eosiniphilic asthma.
- Methylxanthines: asthma & COPD, long term bronchodilation, symptom reduction, used less frequently.
- Systemic Corticosteroids: both asthma and COPD
- quick relief from inflimation and control during exacerbations.
Asthma vs. COPD Management
COPD management focuses on long-term control with symptom relief and reducing exacerbations Asthma management is focused on preventing inflammation, and controlling symptoms with fewer acute exacerbations.
- *Both use ICS, beta agonist, and leukotriene modifiers.
Beta2-Adrenergic Agonists: Side Effects
May diminish after a week or longer
Bronchodilation effects may decrease with continued use
Adverse effects occur more frequently when taken orally that when taken inhaled
Inhaled; tremors, palpitations/tachycardia and angina
Long acting (LABA) increases sever asthma/asthma related death when used for monotherapy treatment. Shouldn’t be used first line of treatment
Theophyline: Side Effects and Drug Interactions
Side Effects; CNS Stimulation: insomnia, nervousness, anxiety and tremors GI Disturbacnes: nausea, vomiting and abdominal discomfort Drug interactions ; CYP450 metabolism in liver. Drugs include erythromycin and ciproflaxin. Caffeine Narrow therapeutic index. Effective = 10-20 mcg/ml
Teaching Common Drugs: Asthma and COPD
- *Inhaled Bronchodilators SABA- Albuterol- quick relief of acute bronchosapsm, instruct patient how to use nebulizers; demonstrate correct inhaler use, tremor side effects. LABA- salmeterol (long acting).- long term bronchodilator, NOT FOR ACute syomptom relief. Often combined with ICS. Use as prescribed BID. Anticholinergics- ipratropium- opens air ways. Proper technique critical. Drink water!
- *Inhaled Corticosteroids - reduce inflammation and prevent exacerbation. Use spacer and rinse mouth!!
- *oral medications
- **Theophylline- blood monitoring
- Leukotrine modifiers- taken daily, report mood changes.
- *oral corticosteroids!
Asthma and COPD Teaching
- Medication Adherence- Consistency
- Proper Techique Lifestyle factors; triggers- Educate about identifying and avoiding triggers (e.g., allergens, smoke, pollution). Smoking Cessation: For COPD patients, stress the importance of quitting smoking and offer resources or referrals.
COPD: GOLD STANDARDS
Spirometric confirmation- COPD is confirmed with post bronchodilator (FEV1)/FVC ration.70 Assessment and Classification- Spirometrict staging GOLD 1-4. ABCD group. Management strategies- non pharm: stop smoking, encourage pulmonary rehab and vaccinations. Pharm, bronchodilators
Antihistmines!
- Allergic Reactions
- Respiratory Conditions
- Skin Conditions
- Motion Sickness
- Sleep Disorders
- Anxiety
- other! Parkinson's Dz H1 RECEPTORS: Both Classes Target H1 Receptors: Both diphenhydramine and fexofenadine block histamine H1 receptors to relieve allergy symptoms such as itching, sneezing, and runny nose! 1st vs 2nd!! 1st Generation Antihistamines (Non-Selective): diphenhydramine, promethazine, chlorpheniramine.. interacts with mucus receptors. SEDATION! 2nd generation H1 Antagonists (Selective): fexofenadine.. Less Sedation:. better for daytime
GOLD guidelines:
Patients MUST stop smoking, exercise, be vaccinated.
GOLD criteria:
Monitor lung functions, pt education, and treatment plans!
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