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Questions and Answers
What is a key distinguishing feature of acute asthma compared to chronic asthma?
What is a key distinguishing feature of acute asthma compared to chronic asthma?
Which of the following is an essential component in the management of COPD?
Which of the following is an essential component in the management of COPD?
How do beta-2 adrenergic agonists primarily exert their therapeutic effect in bronchial smooth muscle?
How do beta-2 adrenergic agonists primarily exert their therapeutic effect in bronchial smooth muscle?
What adverse effect is commonly associated with the use of inhaled corticosteroids?
What adverse effect is commonly associated with the use of inhaled corticosteroids?
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Which statement accurately describes the role of leukotriene modifiers in asthma management?
Which statement accurately describes the role of leukotriene modifiers in asthma management?
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In managing chronic asthma, what is the preferred step for long-term control?
In managing chronic asthma, what is the preferred step for long-term control?
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What is a major mechanism by which corticosteroids exert their anti-inflammatory effect in asthma?
What is a major mechanism by which corticosteroids exert their anti-inflammatory effect in asthma?
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Which symptom is often linked to excessive use of short-acting beta-agonists in asthma patients?
Which symptom is often linked to excessive use of short-acting beta-agonists in asthma patients?
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Which of the following is NOT a characteristic of chronic obstructive pulmonary disease (COPD)?
Which of the following is NOT a characteristic of chronic obstructive pulmonary disease (COPD)?
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Patients taking albuterol should be monitored closely if they are also using which medication?
Patients taking albuterol should be monitored closely if they are also using which medication?
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What is the mechanism of action of 1st generation antihistamines like Diphenhydramine?
What is the mechanism of action of 1st generation antihistamines like Diphenhydramine?
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Which drug is specifically contraindicated in patients with coronary artery disease (CAD)?
Which drug is specifically contraindicated in patients with coronary artery disease (CAD)?
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What potential CNS effect can occur from therapeutic doses of antihistamines?
What potential CNS effect can occur from therapeutic doses of antihistamines?
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Which characteristic distinguishes long-acting bronchodilators like Tiotropium from short-acting ones?
Which characteristic distinguishes long-acting bronchodilators like Tiotropium from short-acting ones?
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Which adverse effect is most commonly associated with the use of inhaled corticosteroids?
Which adverse effect is most commonly associated with the use of inhaled corticosteroids?
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What interaction should be carefully monitored when administering antihistamines?
What interaction should be carefully monitored when administering antihistamines?
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What role do leukotriene modifiers play in the management of asthma?
What role do leukotriene modifiers play in the management of asthma?
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How is Levalbuterol different from Albuterol in terms of dosing?
How is Levalbuterol different from Albuterol in terms of dosing?
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What is a potential systemic effect of thyroid hormone interaction with certain cardiac drugs?
What is a potential systemic effect of thyroid hormone interaction with certain cardiac drugs?
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Which respiratory condition does Tiotropium primarily manage?
Which respiratory condition does Tiotropium primarily manage?
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What distinguishes acute asthma from chronic asthma in terms of treatment response?
What distinguishes acute asthma from chronic asthma in terms of treatment response?
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Which side effect is a known risk of Levalbuterol administration?
Which side effect is a known risk of Levalbuterol administration?
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Which statement best describes the management approach for COPD?
Which statement best describes the management approach for COPD?
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In which patient group should caution be exercised when using antihistamines?
In which patient group should caution be exercised when using antihistamines?
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Which mechanism describes how beta-adrenergic agonists lead to bronchodilation?
Which mechanism describes how beta-adrenergic agonists lead to bronchodilation?
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Which of the following is a significant contraindication to prescribing antihistamines?
Which of the following is a significant contraindication to prescribing antihistamines?
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What is a common adverse effect of inhaled corticosteroids?
What is a common adverse effect of inhaled corticosteroids?
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Which of the following statements correctly describes the role of leukotriene modifiers?
Which of the following statements correctly describes the role of leukotriene modifiers?
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In patients experiencing hypokalemia from beta-adrenergic agonist use, how can this condition be managed?
In patients experiencing hypokalemia from beta-adrenergic agonist use, how can this condition be managed?
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What key consideration should be made when prescribing beta-adrenergic agonists to elderly patients?
What key consideration should be made when prescribing beta-adrenergic agonists to elderly patients?
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Which of the following is an indication for using beta-adrenergic agonists?
Which of the following is an indication for using beta-adrenergic agonists?
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Which anticholinergic drug is specifically used for maintenance therapy in COPD?
Which anticholinergic drug is specifically used for maintenance therapy in COPD?
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What is a significant consideration regarding the use of leukotriene receptor antagonists?
What is a significant consideration regarding the use of leukotriene receptor antagonists?
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When considering adverse effects of beta-adrenergic agonists, which effect is clinically significant?
When considering adverse effects of beta-adrenergic agonists, which effect is clinically significant?
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What is the mechanism of action for anticholinergic medications like Ipratropium?
What is the mechanism of action for anticholinergic medications like Ipratropium?
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Which side effect is most commonly associated with the use of decongestants?
Which side effect is most commonly associated with the use of decongestants?
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What is a potential complication of long-term use of inhaled corticosteroids?
What is a potential complication of long-term use of inhaled corticosteroids?
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Which statement about the use of a DISKUS inhaler is correct?
Which statement about the use of a DISKUS inhaler is correct?
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What challenge do younger kids face when using a nebulizer?
What challenge do younger kids face when using a nebulizer?
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Which of the following best describes the effectiveness of a spacer with a nebulizer?
Which of the following best describes the effectiveness of a spacer with a nebulizer?
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How might treatment strategies differ between acute COPD and chronic COPD?
How might treatment strategies differ between acute COPD and chronic COPD?
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Which of the following correctly reflects a patient's use of inhalers versus nebulizers?
Which of the following correctly reflects a patient's use of inhalers versus nebulizers?
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What is the primary mechanism by which albuterol acts to relieve bronchospasm?
What is the primary mechanism by which albuterol acts to relieve bronchospasm?
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Which adverse effect is likely associated with beta-2 agonist therapy?
Which adverse effect is likely associated with beta-2 agonist therapy?
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What precaution should be taken regarding patients on digoxin who are also prescribed albuterol?
What precaution should be taken regarding patients on digoxin who are also prescribed albuterol?
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Why should patients with pheochromocytoma avoid beta-2 agonists?
Why should patients with pheochromocytoma avoid beta-2 agonists?
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In which situation should beta-2 agonists be avoided?
In which situation should beta-2 agonists be avoided?
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What is a common side effect related to the use of bronchodilators like albuterol?
What is a common side effect related to the use of bronchodilators like albuterol?
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What is the significance of monitoring peak flow measurements in asthma management?
What is the significance of monitoring peak flow measurements in asthma management?
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How is muscle relaxation achieved through the action of beta-2 agonists like albuterol?
How is muscle relaxation achieved through the action of beta-2 agonists like albuterol?
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Which population may particularly need to avoid beta-2 agonists due to specific risks?
Which population may particularly need to avoid beta-2 agonists due to specific risks?
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What is an important consideration in managing patients who are using NSAIDs concurrently with respiratory treatments?
What is an important consideration in managing patients who are using NSAIDs concurrently with respiratory treatments?
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What is a key characteristic of Fexofenadine's distribution in the body?
What is a key characteristic of Fexofenadine's distribution in the body?
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What adverse effect is commonly associated with Fexofenadine?
What adverse effect is commonly associated with Fexofenadine?
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Fexofenadine can be administered to which age group for allergic rhinitis?
Fexofenadine can be administered to which age group for allergic rhinitis?
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What is the percentage of Fexofenadine excreted unchanged by the body?
What is the percentage of Fexofenadine excreted unchanged by the body?
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What distinguishes the administration of Fexofenadine to 2-year-olds?
What distinguishes the administration of Fexofenadine to 2-year-olds?
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Which of the following statements accurately describes Fexofenadine’s mechanism of action?
Which of the following statements accurately describes Fexofenadine’s mechanism of action?
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What is a notable aspect of Fexofenadine's elimination process?
What is a notable aspect of Fexofenadine's elimination process?
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Which of the following conditions might Fexofenadine be prescribed for?
Which of the following conditions might Fexofenadine be prescribed for?
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What is a significant risk associated with severe diastolic hypertension?
What is a significant risk associated with severe diastolic hypertension?
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Which of the following describes a potential effect of thyroid hormones on cardiac drugs?
Which of the following describes a potential effect of thyroid hormones on cardiac drugs?
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What is a key characteristic of 1st generation antihistamines like Diphenhydramine?
What is a key characteristic of 1st generation antihistamines like Diphenhydramine?
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Which statement accurately reflects the elimination route of Levalbuterol?
Which statement accurately reflects the elimination route of Levalbuterol?
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What is a primary consideration when using antihistamines in elderly patients?
What is a primary consideration when using antihistamines in elderly patients?
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Why is it important to monitor drug interactions with antihistamines such as Diphenhydramine?
Why is it important to monitor drug interactions with antihistamines such as Diphenhydramine?
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What is a contraindication for the use of antihistamines?
What is a contraindication for the use of antihistamines?
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Which effect is commonly associated with the use of short-acting beta agonists like Albuterol?
Which effect is commonly associated with the use of short-acting beta agonists like Albuterol?
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Which of the following is a common side effect of long-acting anticholinergic drugs like Tiotropium?
Which of the following is a common side effect of long-acting anticholinergic drugs like Tiotropium?
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What is a significant characteristic of the second generation of antihistamines?
What is a significant characteristic of the second generation of antihistamines?
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Which of the following allergies is a primary indication for the use of antihistamines?
Which of the following allergies is a primary indication for the use of antihistamines?
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What is a potential consequence of excessive dosing of CNS depressants in combination with antihistamines?
What is a potential consequence of excessive dosing of CNS depressants in combination with antihistamines?
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Levalbuterol is known for its mechanism as a selective:
Levalbuterol is known for its mechanism as a selective:
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What is a common adverse effect associated with first generation antihistamines?
What is a common adverse effect associated with first generation antihistamines?
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Which statement about second generation antihistamines is accurate?
Which statement about second generation antihistamines is accurate?
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What potential contraindication should be considered when prescribing antihistamines?
What potential contraindication should be considered when prescribing antihistamines?
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What is a distinguishing characteristic of brompheniramine compared to second generation antihistamines?
What is a distinguishing characteristic of brompheniramine compared to second generation antihistamines?
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Which adverse effect is specifically associated with increased doses of cetirizine?
Which adverse effect is specifically associated with increased doses of cetirizine?
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When can second generation antihistamines generally be considered safe during pregnancy?
When can second generation antihistamines generally be considered safe during pregnancy?
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What should be monitored when using antihistamines with other H1 blockers?
What should be monitored when using antihistamines with other H1 blockers?
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Which pharmacological property differentiates cetirizine from first generation antihistamines?
Which pharmacological property differentiates cetirizine from first generation antihistamines?
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What is a notable side effect linked to the use of first generation antihistamines?
What is a notable side effect linked to the use of first generation antihistamines?
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How does brompheniramine primarily act on the body?
How does brompheniramine primarily act on the body?
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What factor influences the metabolism of both first and second generation antihistamines?
What factor influences the metabolism of both first and second generation antihistamines?
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What is a possible consequence of excessive doses of antihistamines?
What is a possible consequence of excessive doses of antihistamines?
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What possible condition can arise from dysuria when using antihistamines?
What possible condition can arise from dysuria when using antihistamines?
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What is the risk associated with using first generation antihistamines in elderly individuals?
What is the risk associated with using first generation antihistamines in elderly individuals?
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Study Notes
Beta-Adrenergic Agonists
- Mechanism of Action (MOA): Bind to beta 2 receptors, activating adenylate cyclase; this increases cyclic AMP, decreasing cytosolic calcium, leading to bronchial smooth muscle relaxation and bronchodilation.
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Indications: Reversible bronchospasm in adults and children over 2 years.
- Used for both COPD and asthma, primarily as a PRN treatment
- It is not considered RAD in children over 2 years of age
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Important Adverse Effects (SE): Tremors, heart palpitations, and hypokalemia (clinically significant unless administered orally, and more likely with stacked or nebulizer treatments)
- Reduced oxygen saturation may occur in patients not receiving oxygen supplementation
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Special considerations:
- Positive response in asthma: A 200 ml or 12% increase in FEV1 compared to baseline is considered a positive response
- Drug metabolism: Metabolized in the liver and excreted in the urine
- Dose adjustments: Lower doses are recommended for elderly patients
- Monitoring: Monitor EKG if prescribed with digoxin due to potential increased risk of digoxin toxicity.
Anticholinergics
- MOA: Block acetylcholine from binding muscarinic receptors, preventing bronchoconstriction and mucus secretion.
- Indications: Treatment of chronic obstructive pulmonary disease (COPD) and asthma, particularly for patients unable to tolerate beta-agonists or those with a strong parasympathetic component to their bronchospasm.
- Important Adverse Effects (SE): Dry mouth, constipation, blurred vision, urinary retention.
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Special Considerations:
- Dose adjustments: Lower doses recommended for elderly patients and those with impaired renal function.
Inhaled Corticosteroids
- MOA: Reduce inflammation in the airways by suppressing the production of inflammatory mediators such as leukotrienes, histamine, and prostaglandins.
- Indications: Long-term control of asthma and COPD.
- Important Adverse Effects (SE): Oral candidiasis (thrush), hoarseness, dysphonia.
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Special Considerations:
- Rinse mouth after use: May be used with bronchodilators, administer bronchodilator first.
- Tapering: Gradual tapering of dose is necessary to minimize adrenal suppression.
- Potential for bone loss: Long-term use may increase the risk of osteoporosis; therefore, monitor calcium intake and/or bone density.
Leukotriene Modifiers
- MOA: Block the action of leukotrienes, which causes bronchoconstriction, airway inflammation, and mucus production.
- Indications: Prophylaxis and maintenance treatment of mild to moderate asthma, particularly in patients whose asthma is triggered by allergens.
- Important Adverse Effects (SE): Headache, abdominal pain, diarrhea, and elevated liver enzymes.
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Special Considerations:
- May take 1-2 weeks to achieve maximum effect:
- Not for acute attacks:
- Dose adjustments: Lower doses recommended for elderly patients and those with impaired liver function.
Antihistamines
- MOA: Block the action of histamine, a chemical released from mast cells during allergic reactions, causing symptoms such as sneezing, itching, and watery eyes.
- Indications: Relief of allergy symptoms, including hay fever, seasonal allergies, and urticaria (hives).
- Important Adverse Effects (SE): Drowsiness, sedation, dry mouth, and blurred vision.
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Special Considerations:
- Non-drowsy options: Cetirizine, fexofenadine, and loratadine are relatively non-drowsy antihistamines.
- Avoid alcohol: Alcohol can enhance the sedative effects of antihistamines.
- Dose adjustments: May be required for elderly patients and those with impaired liver function.
Decongestants
- MOA: Stimulate the alpha-adrenergic receptors in the nasal mucosa, causing vasoconstriction and reducing nasal congestion.
- Indications: Symptomatic relief of nasal congestion associated with the common cold, sinusitis, and allergies.
- Important Adverse Effects (SE): Rebound congestion, insomnia, nervousness, and hypertension.
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Special Considerations:
- Oral Decongestants: Avoid long term use to prevent rebound congestion.
- Nasal Decongestants: Limit use to 3-5 days to prevent rebound congestion.
- Avoid in patients with hypertension, hyperthyroidism, or glaucoma:
Cough Preparations
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Dextromethorphan
- MOA: Suppresses the cough reflex by acting on the cough center in the brain.
- Indications: Relief of non-productive cough.
- Important Adverse Effects (SE): Drowsiness, dizziness, and nausea.
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Special Considerations:
- Drug Interactions: May increase the risk of serotonin syndrome when combined with certain medications, including selective serotonin reuptake inhibitors (SSRIs).
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Guaifenesin
- MOA: Loosens and thins mucus, making it easier to cough up.
- Indications: Relief of productive cough associated with the common cold, bronchitis, and other respiratory conditions.
- Important Adverse Effects (SE): Nausea, vomiting, and diarrhea.
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Special Considerations:
- Drug Interactions: May interact with other medications that thin mucus, such as acetylcysteine.### Antihistamines
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Antihistamines are drugs that block the action of histamine at the H1 receptor, they do not block H2 receptors.
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Some antihistamines bind to muscarinic receptors.
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Antihistamines strongly block the physiologic effects of histamines, which decreases flare and itch response
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Antihistamines can cause CNS depression in therapeutic doses
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Antihistamines are contraindicated in breastfeeding and given to newborns and premature infants due to possible convulsions
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Use Antihistamines with caution in children because of paradoxical CNS stimulation
1st Generation Antihistamines
- 1st generation antihistamines are lipid-soluble amines that are readily absorbed from the GI tract, metabolized in the liver and contraindicated for breastfeeding.
- 1st generation antihistamines are well-absorbed from the GI tract.
- 1st generation antihistamines are metabolized in the liver.
- 1st generation antihistamines are contraindicated for breastfeeding and giving to neonates or pre-mature infants due to possible convulsions
- Use 1st generation antihistamines with caution in children due to paradoxical CNS stimulation
2nd Generation Antihistamines
- 2nd generation antihistamines are rapidly absorbed from the GI tract.
- It is best to take the 2nd generation antihistamine with food.
- Taking a 2nd generation antihistamine with food decreases or delays absorption
- 2nd generation antihistamines are more generic and inexpensive
- 2nd generation antihistamines do not impair daytime functioning.
- 2nd generation antihistamines are longer-acting with more convenience- allowing for 1-2x/d dosing
- 2nd generation antihistamines are well tolerated and preferred
Diphenhydramine
- Diphenhydramine is a 1st generation H1 receptor agonist that competes with Histamine for the h1 receptor sites on the effector cells
- Diphenhydramine is highly sedating, resulting in fatigue/lassitude.
- Diphenhydramine is contraindicated in newborns and infants.
- Diphenhydramine can be used in pregnancy but should be used with caution (category B pregnancy)
Asthma Trigger Management
- Avoid NSAIDs to prevent exacerbations
- Use inhalers BEFORE your controller medication, not after
- Monitor asthma control via peak flow measurements
- There are no specific monitoring requirements for bronchodilators
Albuterol (SABA)
- Short-acting beta-2 adrenergic agonist. Used for treatment of bronchospasm in asthma, COPD, RAD and bronchitis
- Works by stimulating B2 receptors in the smooth muscle of the airways, leading to muscle relaxation and bronchodilation.
- Be aware of side effects such as increased heart rate, palpitations, tremors, anxiety, headaches, throat irritation/cough, dizziness, muscle cramps, insomnia, nausea.
- Pts on digoxin may require close monitoring as albuterol can increase the volume of distribution and decrease digoxin levels in the blood
- Patients with pheochromocytoma should avoid B2 agonists as they can cause tachycardia and high blood pressure.
Asthma and COPD Treatment
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Treatment of Asthma:
- Acute asthma: Relieved with albuterol (SABA).
- Chronic asthma: Requires long-term controller medications, such as inhaled corticosteroids.
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Treatment of COPD:
- Acute COPD: Relieved with albuterol (SABA).
- Chronic COPD: Long-term management includes bronchodilators and inhaled corticosteroids.
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Albuterol (SABA):
- Mechanism of action: Stimulates beta-2 receptors in airway smooth muscle, leading to muscle relaxation and bronchodilation.
- Use: First-line therapy for acute asthma and COPD exacerbations, as well as for rapid relief of symptoms.
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Side effects:
- Increased heart rate.
- Heart palpitations.
- Tremors.
- Anxiety.
- Headaches.
- Throat irritation or cough.
- Dizziness.
- Muscle cramps.
- Insomnia.
- Nausea.
- Decreased digoxin levels in the blood (for patients on digoxin).
- May cause worsening of symptoms in patients with pheochromocytoma.
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Monitoring of Bronchodilator Therapy:
- Acute asthma: Crucial to monitor effectiveness with peak flow measurements.
- Chronic asthma: Monitoring is critical to ensure patient is adequately controlled.
- Chronic COPD: No specific monitoring required for bronchodilators.
Medication Delivery Devices
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DISKUS:
- Type: Provides medication in a dry powder form.
- Patient should not exhale or blow into DISKUS.
- DISKUS should not be washed or taken apart.
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Nebulizer:
- Effectiveness: Most effective when used with a spacer.
- Challenges: Coordination required for proper use, may be difficult for younger children.
- Spacer: Helps enhance medication delivery and reduce side effects.
Antihistamines
- Antihistamines antagonize the effects of Histamine at H1 receptors
- Antihistamines do not block H2 receptors
- Some Antihistamines bind to muscarinic receptors
- Antihistamines decrease flare and itch responses caused by histamines
Considerations for Antihistamines
- Overdose can cause CNS stimulation, convulsions, and sensitivity in children.
- Antihistamines can interact with CNS depressants.
- Use with caution in the third trimester, nursing mothers, newborn infants, the elderly, young children, and patients with conditions that may be exacerbated by blocking muscarinic receptors.
- There is no lab monitoring for Antihistamines
First Generation Antihistamines
- They are lipid soluble amines
- They are well absorbed from GI tract
- They are metabolized in the liver.
- They are contraindicated in breastfeeding and giving to newborns/premature infants due to potential convulsions
- Use with caution in children due to potential paradoxical CNS stimulation
Second Generation Antihistamines
- They are rapidly absorbed from the GI tract.
- Taking with food delays/decreases absorption.
- Second generation drugs are more generic, less expensive, and have more convenient dosing, typically 1-2x/day
- These drugs are well tolerated and preferred.
Levalbuterol
- Levalbuterol is short-acting beta agonist
- Levalbuterol stimulates the enzyme
- Levalbuterol is FDA approved for use in children
- It is half the dosage of Albuterol
- Levalbuterol has inactive metabolites
- Levalbuterol is 50% excreted unchanged in the urine
Tiotropium
- Tiotropium is a long-acting anticholinergic
- It is used to treat COPD
- Tiotropium is 99% protein bound and not studied in humans (no human studies related to BBB and breast milk)
- In rats, Tiotropium did cross the BBB and into breast milk.
Diphenhydramine
- Diphenhydramine is a H1 receptor agonist
- It competes with Histamine at H1 receptors
- It is highly sedating
- It can cause fatigue, lassitude, and dizziness
- It is contraindicated in newborns and infants
- It can be used in pregnancy (category B)
First Generation Antihistamines
- First generation antihistamines are metabolized primarily by the liver.
- They do not prevent histamine release or bind with histamine that has already been released.
- They have numerous side effects including: disturbed coordination, nausea and vomiting, irritability/nervousness, blurred vision, diplopia (double vision), tremors, increased/decreased appetite, epigastric distress, constipation, diarrhea, dry mouth, urinary retention, dysuria, tachycardia.
- They are contraindicated in narrow-angle glaucoma, lower respiratory infections, stenosing peptic ulcer, symptomatic BPH (benign prostatic hyperplasia), bladder neck obstruction, pyloroduodenal obstruction, and MAOI (monoamine oxidase inhibitor) use.
- First-generation antihistamines cannot be used in newborns and premature infants, or while breastfeeding.
- Beers criteria medications include first-generation antihistamines.
- First generation antihistamines are metabolized by the liver and renally eliminated.
- First generation antihistamines cross the BBB and are in breast milk.
Brompheniramine (1st gen)
- Brompheniramine is a first generation antihistamine.
- It binds non-selectively to central H1 receptors.
- It is used for allergic and vasomotor rhinitis.
- It causes side effects similar to other first-generation antihistamines.
Second Generation Antihistamines
- 2nd generation antihistamines are minimally sedating.
- They can be used during pregnancy (category B & C).
- Using a second-generation antihistamine with another H1 blocker can cause sedation.
Cetirizine (2nd gen)
- Cetirizine selectively blocks peripheral H1 receptors.
- It is used for allergic rhinitis, chronic urticaria, and pruritus.
- It does not cross the BBB in appreciable amounts.
- It can be given to children aged 6 months and older.
- Cetirizine is contraindicated in hypersensitivity to levocetirizine and hydroxyzine.
- It is less contraindicated than first generation antihistamines.
- It cannot be taken during the third trimester of pregnancy.
- It is widely distributed except in the CNS.
- It crosses breast milk.
- Cetirizine is minimally excreted (60% excreted unchanged), renal and fecal elimination.
Fexofenadine (2nd gen)
- Fexofenadine blocks H1 receptors.
- It is prescribed for allergic rhinitis.
- It causes dry mouth, sedation, and occasional headache.
- It can be given to children aged 6 years and older, and 2-year olds for allergic rhinitis (but not recommended).
- Fexofenadine can be given to children aged 6 years and older.
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Description
This quiz covers the mechanism of action, indications, and side effects of beta-adrenergic agonists. It highlights their role in treating reversible bronchospasm in COPD and asthma, along with important considerations for safe administration and patient response evaluation.
