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Which of the following statements about nasal decongestants is true regarding their onset and steady-state?
Which of the following statements about nasal decongestants is true regarding their onset and steady-state?
What should be monitored in elderly patients taking nasal decongestants?
What should be monitored in elderly patients taking nasal decongestants?
Which adverse effect is NOT commonly associated with nasal decongestants?
Which adverse effect is NOT commonly associated with nasal decongestants?
What condition contraindicates the use of oxymetazoline for nasal congestion?
What condition contraindicates the use of oxymetazoline for nasal congestion?
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Which of the following statements about Sudafed is correct?
Which of the following statements about Sudafed is correct?
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Which of the following conditions are considered indications for the use of 1st generation antihistamines?
Which of the following conditions are considered indications for the use of 1st generation antihistamines?
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What is a common safety concern when prescribing 1st generation antihistamines to elderly patients?
What is a common safety concern when prescribing 1st generation antihistamines to elderly patients?
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Which of the following statements correctly describes the mechanism of action (MOA) of 2nd generation antihistamines?
Which of the following statements correctly describes the mechanism of action (MOA) of 2nd generation antihistamines?
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What specific caution must be taken when prescribing fexofenadine?
What specific caution must be taken when prescribing fexofenadine?
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Which of the following statements is NOT true regarding the use of 1st generation antihistamines?
Which of the following statements is NOT true regarding the use of 1st generation antihistamines?
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What effect might young children experience as a paradoxical reaction to 1st generation antihistamines?
What effect might young children experience as a paradoxical reaction to 1st generation antihistamines?
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What is a significant consideration regarding the concurrent use of MAO inhibitors with 1st generation antihistamines?
What is a significant consideration regarding the concurrent use of MAO inhibitors with 1st generation antihistamines?
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Which of the following attributes distinguishes cetirizine from other 2nd generation antihistamines?
Which of the following attributes distinguishes cetirizine from other 2nd generation antihistamines?
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What is a primary mechanism of action for 1st generation antihistamines?
What is a primary mechanism of action for 1st generation antihistamines?
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Which of the following is a potential safety concern when using 2nd generation antihistamines like Zyrtec?
Which of the following is a potential safety concern when using 2nd generation antihistamines like Zyrtec?
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What caution is advised for patients with narrow-angle glaucoma when taking 1st generation antihistamines?
What caution is advised for patients with narrow-angle glaucoma when taking 1st generation antihistamines?
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What distinguishes cetirizine from other 2nd generation antihistamines?
What distinguishes cetirizine from other 2nd generation antihistamines?
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What adverse effect may occur with the usage of 1st generation antihistamines in young children?
What adverse effect may occur with the usage of 1st generation antihistamines in young children?
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Which of the following statements about fexofenadine is NOT true?
Which of the following statements about fexofenadine is NOT true?
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Why should patients taking 1st generation antihistamines avoid alcohol?
Why should patients taking 1st generation antihistamines avoid alcohol?
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What should be avoided in patients with benign prostatic hypertrophy when using 1st generation antihistamines?
What should be avoided in patients with benign prostatic hypertrophy when using 1st generation antihistamines?
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What is the primary mechanism of action of oxymetazoline?
What is the primary mechanism of action of oxymetazoline?
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What adverse effect is specifically linked to the rebound phenomenon of nasal decongestants?
What adverse effect is specifically linked to the rebound phenomenon of nasal decongestants?
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Which of the following conditions should be approached with caution when using Sudafed?
Which of the following conditions should be approached with caution when using Sudafed?
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How does Sudafed primarily exert its effect in treating nasal congestion?
How does Sudafed primarily exert its effect in treating nasal congestion?
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What duration of use is recommended for oxymetazoline to prevent rebound congestion?
What duration of use is recommended for oxymetazoline to prevent rebound congestion?
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What is a primary concern when prescribing 1st generation antihistamines, especially to elderly patients?
What is a primary concern when prescribing 1st generation antihistamines, especially to elderly patients?
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Which characteristic of 2nd generation antihistamines contributes to their lower sedative effects?
Which characteristic of 2nd generation antihistamines contributes to their lower sedative effects?
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What paradoxical effect may young children experience when using 1st generation antihistamines?
What paradoxical effect may young children experience when using 1st generation antihistamines?
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Which safety consideration should be followed when prescribing fexofenadine?
Which safety consideration should be followed when prescribing fexofenadine?
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What should patients avoid while taking 1st generation antihistamines?
What should patients avoid while taking 1st generation antihistamines?
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How does cetirizine differ from other 2nd generation antihistamines?
How does cetirizine differ from other 2nd generation antihistamines?
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What condition must be approached with caution regarding the use of 1st generation antihistamines?
What condition must be approached with caution regarding the use of 1st generation antihistamines?
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Which of the following is a contraindication for the use of 1st generation antihistamines?
Which of the following is a contraindication for the use of 1st generation antihistamines?
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What may occur if topical formulations of 1st generation antihistamines are applied to the eyes?
What may occur if topical formulations of 1st generation antihistamines are applied to the eyes?
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What is the primary adverse effect associated with the prolonged use of oxymetazoline?
What is the primary adverse effect associated with the prolonged use of oxymetazoline?
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Which of the following conditions warrants caution when using Sudafed?
Which of the following conditions warrants caution when using Sudafed?
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What mechanism of action does oxymetazoline utilize to relieve nasal congestion?
What mechanism of action does oxymetazoline utilize to relieve nasal congestion?
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Which of the following is a contraindication for using nasal decongestants like oxymetazoline?
Which of the following is a contraindication for using nasal decongestants like oxymetazoline?
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In what timeframe does oxymetazoline typically reach a steady state in the body?
In what timeframe does oxymetazoline typically reach a steady state in the body?
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What systemic effect may occur due to the use of Sudafed?
What systemic effect may occur due to the use of Sudafed?
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Which adverse effect can be observed with both oxymetazoline and Sudafed?
Which adverse effect can be observed with both oxymetazoline and Sudafed?
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For which group of patients should nasal decongestants be used with caution due to increased susceptibility to side effects?
For which group of patients should nasal decongestants be used with caution due to increased susceptibility to side effects?
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Which adverse effect is specifically linked to alpha-adrenergic agonists like Sudafed?
Which adverse effect is specifically linked to alpha-adrenergic agonists like Sudafed?
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What is the recommended duration for the use of oxymetazoline to avoid complications?
What is the recommended duration for the use of oxymetazoline to avoid complications?
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Study Notes
1st Generation Antihistamines (e.g., Benadryl)
- Indications: Flu, colds, allergies, insomnia, anaphylaxis, motion sickness, Parkinsonism, itching.
- Mechanism of Action (MOA): Competes with histamine for receptor sites on effector cells, blocks histaminic and muscarinic receptors, crosses the blood-brain barrier.
- Safety/Contraindications/Drug Interactions (D2D): Caution in elderly and children, do not use in newborns or premature infants, nursing mothers, caution with narrow-angle glaucoma, benign prostatic hypertrophy (increased intraocular pressure). Avoid concurrent use of MAO inhibitors or CNS depressants. CYP2D6 inhibitor, weak anticholinergic effects, CNS depression, central histamine effects.
- Special Considerations: At baseline, young children may experience paradoxical excitation, and patients should avoid activities requiring mental alertness or coordination until effects are realized. Avoid applying occlusive dressings, cosmetics, or other products over treated areas. Avoid alcohol.
2nd Generation Antihistamines (e.g., Zyrtec, Allegra)
- Indications: Allergic rhinitis, sneezing, itchy/watery eyes, itchy nose/throat, chronic idiopathic urticaria.
- MOA: Competes with histamine for receptor sites on effector cells, acts peripherally (less sedating), low lipid solubility, cannot cross blood-brain barrier.
- Special Considerations: Caution in elderly (>65 yo), and periodic monitoring of creatinine. Food can affect absorption; generally well-tolerated, but headache, dry mouth, and fatigue may occur.
Nasal Decongestants (e.g., Afrin)
- Indications: Nasal congestion and sinus congestion/pressure.
- MOA: Stimulates smooth muscle alpha-adrenergic receptors producing vasoconstriction and reducing nasal congestion.
- Safety/Contraindications/D2D: MAO inhibitor use within 14 days; caution in pts with glaucoma, angle-closure, HTN, cardiovascular disease, diabetes, and hyperthyroidism. D2D with radiolabeled norepinephrine analog effect.
- Special Considerations: Use for 3 days or less; rebound nasal congestion (rhinitis medicamentosa) may occur.
Oral Decongestants (e.g., Sudafed)
- Indications: Nasal congestion due to common cold, hay fever, and upper respiratory allergies.
- MOA: Enhances norepinephrine & epinephrine or adrenergic activity by stimulating the alpha1-adrenergic receptors, which induces vasoconstriction.
- Safety/Contraindications/D2D: Caution with MAO inhibitors within 14 days; caution in pregnancy. Caution against use in individuals with glaucoma, angle-closure, high blood pressure, cardiovascular disease, diabetes, and hyperthyroidism. D2D with radiolabeled norepinephrine analog, hyperglycemic/hypertensive effects.
- Special Considerations: No routine tests are recommended; can result in anticholinergic effects, particularly impacting the elderly. Limited efficacy in children under 4 years of age.
Antitussives (e.g., Benzonatate)
- Indications: Cough suppressants.
- MOA: Anesthetizes the respiratory passage, lungs, and pleural stretch receptors, reducing cough reflex. Codeine, dextromethorphan, and diphenhydramine may also prevent or relieve non-productive coughs; opioids may offer optimal cough suppression.
- Safety/Contraindications/D2D: Hypersensitivity can cause bronchospasm and laryngospasm. May cause bizarre behavior (confusion and visual hallucinations)
- Special Considerations: Use only for non-productive coughs or for bedtime situations; avoid opioids in patients with COPD or substance abuse history.
Expectorants (e.g., Guaifenesin)
- Indications: Helps loosen mucus and thin bronchial secretions to make them more fluidic, improving cough effectiveness.
- MOA: Increases the volume and decreases the viscosity of respiratory tract secretions.
- Safety/Contraindications/D2D: Caution in nephrolithiasis and in pts under 6 years of age.
- Special Considerations: Encourage increased fluid consumption. Most helpful for productive coughs, especially early on.
Intranasal Antihistamines (e.g., Azelastine)
- Indications: Perennial and seasonal allergic rhinitis, vasomotor rhinitis. (also, note MOA)
- MOA: Rapid onset action, antagonizes central and peripheral histamine H1 receptors, inhibits histamine release from mast cells.
- Safety/Contraindications/D2D: Caution with CNS depressant use and in patients with depression hx.
- Special Considerations: Less sedating than oral antihistamines; adverse effects include sedation and bitter taste.
Leukotriene Modifiers/Blockers (e.g., Montelukast)
- Indications: Allergic rhinitis, asthma, bronchoconstriction.
- MOA: Selectively binds to cysteinyl leukotriene receptors, reducing nasal congestion, airway constriction, mucus production, and inflammation.
- Safety/Contraindications/D2D: Caution in severe asthma and PKU; CYP2C8, 2C9, and 3A4 substrates.
- Special Considerations: Monitor for suicidality, aggressive behavior, hallucinations, depression. Can cause pulmonary eosinophilia, hepatic failure, and Churg-Strauss syndrome (blood-vessel inflammation).
Nasal Corticosteroids (e.g., Fluticasone)
- Indications: Allergic rhinitis, nasal polyps, non-allergic rhinitis.
- MOA: Unknown mechanism but inhibits multiple inflammatory cytokines to produce glucocorticoid and mineralocorticoid effects and suppress inflammation.
- Safety/Contraindications/D2D: Use caution in unhealed nasal septal ulcers/wounds, in patients with recent systemic corticosteroid use, glaucoma, cataracts, hepatic impairment. CYP3A4 substrate, and immunosuppressive effects.
- Special Considerations: Requires roughly 5 days to be effective; may cause growth suppression (especially in children with long term use).
Intranasal Cromolyn
- Indications: Allergic rhinitis.
- MOA: Inhibits mast cell degranulation (mast cell stabilizer), thus inhibiting histamine release, and suppressing inflammation.
- Special Considerations: Less effective than intranasal corticosteroids, requires frequent dosing (3-4x daily).
Optic Decongestant/Antihistamine
- Indications: Decreasing eye redness.
- MOA: Binds to histamine 1 receptors, inhibiting phospholipase A2 and production of endothelium-derived relaxing factor. Naphazoline is a decongestant, pheniramine is an antihistamine.
- Safety/Contraindications/D2D: Caution with diabetes, glaucoma, cardiac issues, HTN, hyperthyroidism, eye infection/injury. D2D includes hypertensive effects and interaction with radiolabelled norepinephrine analog.
- Special considerations: Not recommended for children under 6; may cause dilated pupils, blurred vision, and eye pain.
Short-acting Beta-2 Agonists (SABA) (e.g., Albuterol)
- Indications: Reversing reversible airway obstruction in asthma and COPD.
- MOA: Activates beta-adrenergic receptors, causing relaxation of smooth airway muscles and dilation.
- Safety/Contraindications/D2D: Caution with ischemic heart disease, HTN, arrhythmias, hypokalemia, diabetes, seizure disorder, hyperthyroidism, and elderly individuals. May worsen glycemic control.
Long-acting Beta-2 Agonists (LABA)
- Indications: Similar to SABA and indicated for asthma and COPD.
- MOA: Similar to SABA but with longer duration of action.
- Safety Considerations: Can cause nervousness, tremor, palpitations and prolonged QT-interval in some individuals.
Inhaled Glucocorticoids (ICS) (e.g., Fluticasone)
- Indications: Asthma.
- MOA: Inhibits inflammatory cytokines and produce glucocorticoid and mineralocorticoid effects, thus decreasing inflammation.
- Safety/Contraindications/D2D: Sever hypersensitivity to milk products, Status asthmaticus, hepatic impairment. Use caution in patients with immunosuppression or active infection. CYP3A4 substrate and immunosuppressive effects.
- Special Considerations: Oral antihistamine is generally recommended for the first 5 days because it takes time for nasal steroids to be effective.
Oral Glucocorticoids (e.g., Prednisone/Dexamethasone)
- Indications: Diverse inflammatory conditions.
- MOA: Exact mechanism unknown but inhibits multiple inflammatory cytokines, producing glucocorticoid and mineralocorticoid effects.
- Safety/Contraindications/D2D: Systemic fungal infections, cerebral malaria, HTN, CHF, recent MI, diabetes, PUD, ulcerative colitis, psychiatric disorders, thyroid conditions, osteoporosis. D2D includes CYP3A4, and effects on liver enzymes, heart, or neurological function.
- Special Considerations: Avoid abrupt withdrawal (particularly in patients on high doses or long-term use). May cause immunosuppression, diabetes, and Cushing's syndrome (adrenal suppression) Monitor weight, blood pressure, depression symptoms, and unusual behavior.
Methylxanthines (e.g., Theophylline)
- Indications: Asthma.
- MOA: Exact mechanism unknown; increases cyclic AMP (cAMP), and antagonizes adenosine receptors.
- Safety/Contraindications/D2D: Caution with other medications that decrease seizure threshold (active PUD, seizure disorder, arrhythmias, CHF, pulmonary edema, cor pulmonale, renal impairment, or in patients with fluctuating thyroid function, active infections, smoking habits). D2D includes CYP1A2 and CYP3A4 enzyme substrate effects; and hypokalemia.
- Special Considerations: Toxicity; monitor therapeutic drug levels (10-15 mcg/ml). May cause gastrointestinal distress (nausea, heartburn).
Immunomodulators (e.g., Omalizumab/Reslizumab)
- Indications: Severe asthma, chronic idiopathic urticaria, nasal polyps, eosinophilic granulomatosis with polyangiitis, eosinophilic syndromes.
- MOA: Inhibits IgE binding to mast cells/basophils/dendritic cells, downregulates IgE receptors, thus reducing inflammation, and decreasing eosinophils and inflammatory mediators.
- Safety/Contraindications/D2D: Bronchospasm, status asthmaticus, hypersensitivity to the product (anaphylaxis), or severe/hx of anaphylaxis.
- Special considerations: Watch for anaphylaxis symptoms for 2 hours after the first dose and 30 minutes following subsequent doses.
IL-4 Receptor Alpha-Antagonist (e.g., Dupilumab)
- Indications: Moderate to severe asthma, atopic dermatitis, and rhinosinusitis.
- Mechanism: Binds to IL-4 receptor alpha subunit, interfering with IL-4 and IL-13 cytokines affecting inflammation and the immune response.
- Safety Considerations: Patients <12 years old (pen form); asthma, acute bronchospasm, status asthmaticus; caution if corticosteroids are in use; D2D includes immunosuppressive effects.
- Special Considerations: Patient eosinophil count must be 300+ or they must use oral steroids; subcutaneous injections are common and can be administered in a home setting.
Anticholinergics/Antimuscarinics (e.g., Tiotropium/Ipratropium)
- Indications: Asthma, COPD
- MOA: Blocks acetylcholine receptors to produce bronchodilation.
- Safety/Contraindications/D2D: Caution with CrCl <60, glaucoma, angle-closure, urinary retention, and with hypertrophic prostate. D2D for anticholinergic effects.
- Special Considerations: Can increase intraocular pressure, cause dry mouth, urinary retention, and pharyngeal irritation.
Combination Inhalers (e.g., Albuterol/Ipratropium)
- Indications: Primarily for use in asthma and COPD.
- MOA: Combination of short-acting and long-acting agents, which may reduce the need for multiple inhalers and potentially improve symptom control.
- Special Considerations: Combination products may vary regarding their contents.
Phosphodiesterase-4 (PDE4) Inhibitors(e.g.,roflumilast)
- Indications: COPD exacerbations (reduction in frequency), not for acute asthma or bronchospasm.
- MOA: Inhibits breakdown of intracellular cyclic AMP which slows COPD progression by reducing inflammation.
- Safety/Contraindications/D2D: Caution with liver problems, or a history of suicidal ideation or depression; CYP1A2, CYP2C19 and CYP3A4 substrates.
- Special Considerations: Monitor for weight loss, gastrointestinal symptoms (diarrhea), and neuropsychiatric side effects (depression, insomnia, anxiety).
Nicotine Replacement Therapy (NRTs)( e.g., Nicoderm, Nicorette)
- Indications: Smoking cessation.
- MOA: Binds to CNS and peripheral nicotinic-cholinergic receptors.
- Safety/Contraindications/D2D: Allergy to soy/soybean; Arrhythmias, MI, angina, Pregnancy. D2D includes CYP2A6 substrates; caution against concurrent use with other medications, especially in pregnancy.
- Special Considerations: Can lead to nicotine dependence.
Nicotine Receptor Agonist (e.g., Varenicline)
- Indications: Smoking cessation.
- MOA: Partial neuronal nicotinic receptor agonist, which prevents nicotine stimulation of the dopaminergic system and binds to the 5-HT3 receptor.
- Safety/Contraindications/D2D: Caution with CrCl <30, or with significant psych history. D2D includes effects on seizure threshold.
- Special Considerations: Can cause various psychiatric effects (depression, suicidal thoughts).
Bupropion SR (e.g., Zyban)
- Indications: Smoking cessation.
- MOA: Exact mechanism unknown; inhibits neuronal uptake of norepinephrine and dopamine.
- Safety/Contraindications/D2D: Caution in persons with seizure disorder, bulimia, or anorexia; use with abrupt cessation of alcohol, benzodiazepines, or other sedatives. D2D with MAO inhibitors.
- Special Considerations: Watch for suicidal thoughts, mood changes, or hallucinations in patients. Monitor blood pressure at baseline and periodically.
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Test your knowledge on nasal decongestants with this quiz. Explore topics such as their onset, monitoring elderly patients, common adverse effects, contraindications, and facts about Sudafed. Ideal for pharmacy or healthcare students looking to review essential information.