MCQ Quiz-Methylxanthines and Selective β2-Adrenergic Agonists

MCQ Quiz: Methylxanthines and Selective β2-Adrenergic Agonists

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Methylxanthines and selective β2-adrenergic agonists are foundational drug classes in the management of obstructive lung diseases like asthma and COPD. While β2-agonists are mainstays of therapy, older drugs like theophylline still have a niche role, demanding a pharmacist’s understanding of its complex pharmacology and narrow therapeutic index. This quiz for PharmD students will test your knowledge of the mechanisms, clinical uses, and key safety considerations for these important respiratory medications.

1. What is the primary mechanism of action of selective β2-adrenergic agonists like albuterol?

  • They cause bronchoconstriction by blocking beta-1 receptors.
  • They stimulate beta-2 receptors on airway smooth muscle, leading to bronchodilation.
  • They inhibit the enzyme phosphodiesterase, increasing cAMP levels.
  • They block muscarinic receptors in the lungs.

Answer: They stimulate beta-2 receptors on airway smooth muscle, leading to bronchodilation.

2. The stimulation of beta-2 receptors leads to an increase in which intracellular second messenger, causing smooth muscle relaxation?

  • Inositol triphosphate (IP3)
  • Diacylglycerol (DAG)
  • Cyclic adenosine monophosphate (cAMP)
  • Cyclic guanosine monophosphate (cGMP)

Answer: Cyclic adenosine monophosphate (cAMP)

3. Albuterol is classified as a short-acting β2-agonist (SABA). Its primary role in asthma management is for:

  • Long-term daily maintenance therapy.
  • Quick relief of acute bronchospasm (“rescue” therapy).
  • Preventing exercise-induced bronchospasm when used 2-3 hours before exercise.
  • Reducing airway inflammation.

Answer: Quick relief of acute bronchospasm (“rescue” therapy).

4. Salmeterol and formoterol are classified as long-acting β2-agonists (LABAs). In the treatment of asthma, they should:

  • Be used as monotherapy for long-term control.
  • Only be used for acute rescue of symptoms.
  • Always be used in combination with an inhaled corticosteroid (ICS).
  • Be taken on an as-needed basis only.

Answer: Always be used in combination with an inhaled corticosteroid (ICS).

5. A common and predictable side effect of inhaled β2-agonists, especially at high doses, is:

  • Bradycardia.
  • Tremor, tachycardia, and palpitations.
  • Constipation.
  • Drowsiness.

Answer: Tremor, tachycardia, and palpitations.

6. The “long-acting” property of a LABA like salmeterol is primarily due to its:

  • Rapid metabolism.
  • High water solubility.
  • High lipophilicity and a long side chain that anchors it to the receptor.
  • Ability to irreversibly bind to the beta-2 receptor.

Answer: High lipophilicity and a long side chain that anchors it to the receptor.

7. Which of the following is a potential metabolic side effect of systemic or high-dose β2-agonist use?

  • Hypokalemia and hyperglycemia.
  • Hyperkalemia and hypoglycemia.
  • Hyponatremia.
  • Hypercalcemia.

Answer: Hypokalemia and hyperglycemia.

8. A key counseling point for a patient using any metered-dose inhaler (MDI) is to:

  • Shake the inhaler well before use.
  • Inhale quickly and deeply.
  • Coordinate actuation of the canister with a slow, deep inhalation.
  • Both A and C are correct.

Answer: Both A and C are correct.

9. The mechanism of action of methylxanthines, like theophylline, is complex but is thought to involve:

  • Stimulation of beta-2 receptors.
  • Non-selective inhibition of phosphodiesterase (PDE) enzymes, increasing cAMP.
  • Blockade of adenosine receptors.
  • Both B and C are correct.

Answer: Both B and C are correct.

10. Theophylline has a ________ therapeutic index, which means it requires therapeutic drug monitoring.

  • Wide
  • Narrow
  • Non-existent
  • Variable

Answer: Narrow

11. The therapeutic serum concentration range for theophylline is typically:

  • 1-5 mcg/mL
  • 5-15 mcg/mL
  • 20-30 mcg/mL
  • 30 mcg/mL

Answer: 5-15 mcg/mL

12. A patient with a theophylline level of 25 mcg/mL is at high risk for which signs of toxicity?

  • Nausea, vomiting, tachycardia, and seizures.
  • Sedation and bradycardia.
  • Dry mouth and constipation.
  • Peripheral edema.

Answer: Nausea, vomiting, tachycardia, and seizures.

13. Theophylline is primarily metabolized by which cytochrome P450 enzyme in the liver?

  • CYP2D6
  • CYP2C19
  • CYP3A4
  • CYP1A2

Answer: CYP1A2

14. A patient who is a heavy smoker is taking theophylline. Smoking is a known CYP1A2 inducer, which would lead to ________ theophylline levels, requiring a ________ dose.

  • Increased; lower
  • Decreased; higher
  • Unchanged; standard
  • Decreased; lower

Answer: Decreased; higher

15. A patient on a stable dose of theophylline is newly prescribed ciprofloxacin, a potent CYP1A2 inhibitor. The pharmacist should be concerned about:

  • A decrease in theophylline levels and loss of efficacy.
  • An increase in theophylline levels and risk of toxicity.
  • A severe allergic reaction.
  • No interaction between these two drugs.

Answer: An increase in theophylline levels and risk of toxicity.

16. From a medicinal chemistry perspective, theophylline and caffeine belong to which class of heterocyclic compounds?

  • Pyridines
  • Purines (specifically, xanthines)
  • Pyrimidines
  • Thiazoles

Answer: Purines (specifically, xanthines)

17. A key difference between a dry powder inhaler (DPI) and a metered-dose inhaler (MDI) is that a DPI requires the patient to:

  • Coordinate actuation with inhalation.
  • Use a spacer device.
  • Inhale forcefully and deeply to aerosolize the powder.
  • Shake the device before use.

Answer: Inhale forcefully and deeply to aerosolize the powder.

18. Overuse of a SABA (e.g., more than one canister per month) in an asthma patient is a marker of:

  • Excellent asthma control.
  • Poor underlying asthma control and the need for better maintenance therapy.
  • The patient correctly using their medication.
  • A mild form of asthma.

Answer: Poor underlying asthma control and the need for better maintenance therapy.

19. Which of the following conditions can decrease the clearance of theophylline, requiring a dose reduction?

  • Heavy smoking
  • Liver disease or heart failure
  • A high-protein diet
  • Concurrent use of phenobarbital

Answer: Liver disease or heart failure

20. Levalbuterol is the R-enantiomer of albuterol. It is marketed with the claim that it:

  • Is more potent than racemic albuterol.
  • Causes fewer side effects, like tachycardia, compared to racemic albuterol (though clinical significance is debated).
  • Has a longer duration of action.
  • Is less expensive than generic albuterol.

Answer: Causes fewer side effects, like tachycardia, compared to racemic albuterol (though clinical significance is debated).

21. A patient with COPD is prescribed a LABA as monotherapy. This is considered:

  • An inappropriate therapy for COPD.
  • An appropriate and standard maintenance therapy for COPD.
  • Only to be used for acute exacerbations.
  • To be a curative treatment for COPD.

Answer: An appropriate and standard maintenance therapy for COPD.

22. The use of a “spacer” or “valved holding chamber” with a metered-dose inhaler is a best practice that helps to:

  • Increase the speed of the aerosolized particles.
  • Improve drug delivery to the lungs and reduce deposition in the oropharynx.
  • Make the inhaler more difficult to use.
  • Clean the inhaler after each use.

Answer: Improve drug delivery to the lungs and reduce deposition in the oropharynx.

23. The “black box warning” for LABAs in asthma is related to the finding that, when used as monotherapy, they can increase the risk of:

  • Asthma-related death.
  • Liver failure.
  • Kidney stones.
  • Severe skin rashes.

Answer: Asthma-related death.

24. A key counseling point for any inhaled medication used for maintenance therapy is:

  • To only use it when symptoms occur.
  • The importance of using it every day as prescribed, even when feeling well.
  • To stop using it as soon as you feel better.
  • To share the inhaler with other family members.

Answer: The importance of using it every day as prescribed, even when feeling well.

25. In which practice setting is a pharmacist most likely to manage an intravenous aminophylline (the water-soluble salt of theophylline) drip for a patient with severe asthma or COPD?

  • Community pharmacy
  • Ambulatory care clinic
  • Hospital/Institutional setting
  • Mail-order pharmacy

Answer: Hospital/Institutional setting

26. The primary therapeutic effect of a selective β2-agonist in asthma is:

  • Bronchodilation.
  • Anti-inflammatory.
  • Mucolytic.
  • Antibacterial.

Answer: Bronchodilation.

27. Theophylline’s bronchodilator effect is generally considered to be ________ than that of inhaled β2-agonists.

  • More potent
  • Weaker
  • Faster in onset
  • Longer in duration

Answer: Weaker

28. A patient on theophylline who quits smoking will likely need:

  • A higher dose of theophylline.
  • A lower dose of theophylline, due to a reduction in CYP1A2 induction.
  • No change in their theophylline dose.
  • To switch to an inhaled medication.

Answer: A lower dose of theophylline, due to a reduction in CYP1A2 induction.

29. The “selective” in selective β2-agonist refers to the drug’s:

  • Higher affinity for beta-2 receptors compared to beta-1 receptors.
  • Ability to only affect the lungs.
  • Lack of any side effects.
  • Unique chemical structure.

Answer: Higher affinity for beta-2 receptors compared to beta-1 receptors.

30. The ultimate reason theophylline is no longer a first-line therapy for asthma is its:

  • High cost.
  • Poor efficacy.
  • Narrow therapeutic index and significant potential for drug interactions and toxicity.
  • Lack of an oral formulation.

Answer: Narrow therapeutic index and significant potential for drug interactions and toxicity.

31. A pharmacist’s knowledge of __________ is essential for managing theophylline therapy.

  • Drug interactions
  • Therapeutic drug monitoring
  • Patient counseling on signs of toxicity
  • All of the above

Answer: All of the above.

32. Which of the following is an ultra-long-acting β2-agonist (ultra-LABA), often dosed once daily?

  • Albuterol
  • Salmeterol
  • Indacaterol
  • Levalbuterol

Answer: Indacaterol

33. In the management of an acute, severe asthma exacerbation in the emergency department, a SABA is typically administered via:

  • A dry powder inhaler.
  • A nebulizer, often continuously or with back-to-back treatments.
  • An oral tablet.
  • A transdermal patch.

Answer: A nebulizer, often continuously or with back-to-back treatments.

34. The development of selective β2-agonists was a major medicinal chemistry advancement over older, non-selective sympathomimetics like:

  • Epinephrine and isoproterenol.
  • Atropine.
  • Ipratropium.
  • Theophylline.

Answer: Epinephrine and isoproterenol.

35. A pharmacist providing MTM for a patient with asthma should assess their SABA use to:

  • Evaluate the patient’s adherence to their maintenance therapy.
  • Determine if the patient’s asthma is well-controlled.
  • Identify the need for a step-up in maintenance therapy.
  • All of the above.

Answer: All of the above.

36. A key part of the “Business Plan” for a new pharmacist-led asthma management service would involve protocols for:

  • Assessing inhaler technique.
  • Educating on the difference between rescue and controller medications.
  • Monitoring for appropriate SABA use.
  • All of the above.

Answer: All of the above.

37. From a “human factors” perspective, the wide variety of different inhaler devices can lead to:

  • Improved patient adherence.
  • Patient confusion and misuse if not properly taught.
  • A lower cost for medications.
  • A reduction in medication errors.

Answer: Patient confusion and misuse if not properly taught.

38. The leadership skill of “advocacy” could be used by a pharmacist to:

  • Negotiate with an insurance company to get a preferred LABA/ICS combination product covered for a patient.
  • Insist all asthma patients receive theophylline.
  • Promote the overuse of SABAs.
  • Avoid all communication with prescribers.

Answer: Negotiate with an insurance company to get a preferred LABA/ICS combination product covered for a patient.

39. Forging ahead in pharmacy practice means using __________ to identify patients with poor asthma control (e.g., high SABA use) who would benefit from a pharmacist’s intervention.

  • A pharmacist’s intuition only.
  • Analytics and reporting systems.
  • The pharmacy’s daily sales reports.
  • A patient’s physical appearance.

Answer: Analytics and reporting systems.

40. A “Clinical Decision Support” alert in the EHR should fire if a physician tries to:

  • Prescribe a SABA for a patient with a new diagnosis of asthma.
  • Prescribe a LABA without a concomitant inhaled corticosteroid for an asthma patient.
  • Prescribe an inhaled corticosteroid.
  • Order a nebulizer treatment in the ER.

Answer: Prescribe a LABA without a concomitant inhaled corticosteroid for an asthma patient.

41. The cardiovascular principle to remember with beta-blockers and beta-agonists is that:

  • They are synergistic and should always be used together.
  • Non-selective beta-blockers can antagonize the effects of beta-2 agonists in the lungs.
  • Cardioselective beta-blockers have no effect on the lungs.
  • Beta-agonists can cause bradycardia.

Answer: Non-selective beta-blockers can antagonize the effects of beta-2 agonists in the lungs.

42. A pharmacist’s “geriatric sensitivity” is important when counseling an elderly patient on a new inhaler because:

  • The patient may have physical (e.g., arthritis) or cognitive challenges that make using the device difficult.
  • All elderly patients have perfect inhaler technique.
  • Elderly patients do not get asthma.
  • Inhalers are more effective in the elderly.

Answer: The patient may have physical (e.g., arthritis) or cognitive challenges that make using the device difficult.

43. The use of a “Dashboard Presentation” in a hospital could be used by a pharmacy leader to track:

  • The appropriate use of SABAs on the general medical floors.
  • The pharmacy’s daily profit.
  • The number of technicians on the schedule.
  • The time it takes for a drug to be delivered from the wholesaler.

Answer: The appropriate use of SABAs on the general medical floors.

44. An effective “negotiation” with a patient who is overusing their albuterol inhaler would involve:

  • A shared decision-making approach to understand why they are using it so much and to explain the importance of controller therapy.
  • Telling the patient they can no longer have their rescue inhaler.
  • Accusing the patient of being non-compliant.
  • Refusing to fill the prescription.

Answer: A shared decision-making approach to understand why they are using it so much and to explain the importance of controller therapy.

45. The service of “deprescribing” might be considered for a patient on theophylline if:

  • The risks of toxicity and drug interactions are thought to outweigh the modest clinical benefit.
  • The patient is well-controlled on their current dose.
  • The patient has no other medical conditions.
  • The patient enjoys getting their blood drawn for drug levels.

Answer: The risks of toxicity and drug interactions are thought to outweigh the modest clinical benefit.

46. Which of the following is NOT a primary role for a selective β2-agonist?

  • Treatment of acute bronchospasm.
  • Prevention of exercise-induced bronchospasm.
  • As a core anti-inflammatory agent in asthma.
  • As a bronchodilator in COPD.

Answer: As a core anti-inflammatory agent in asthma.

47. A pharmacist providing “Antidotal Therapy” would need to know how to manage an overdose of:

  • Albuterol
  • Salmeterol
  • Theophylline
  • Ipratropium

Answer: Theophylline

48. In which “practice setting” is a pharmacist most likely to counsel a patient on the correct use of a newly prescribed Diskus or Ellipta inhaler?

  • Hospital ICU
  • Nuclear Pharmacy
  • Community Pharmacy
  • Managed Care Organization

Answer: Community Pharmacy

49. A patient’s “adherence” to a once-daily LABA/ICS inhaler is generally ________ than for a regimen requiring multiple inhalers multiple times a day.

  • Worse
  • Better
  • The same
  • Not a factor in asthma control

Answer: Better

50. The ultimate goal of using these medication classes is to:

  • Maximize the number of prescriptions a patient is taking.
  • Control symptoms, improve lung function, and enhance the patient’s quality of life.
  • Ensure the pharmacy is profitable.
  • Use the newest and most expensive inhaler available.

Answer: Control symptoms, improve lung function, and enhance the patient’s quality of life.

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