Module 5 - Respiratory System

Question 1

What class of durg is Beclomethasone [QVAR HFA] and what is it used for?

Answer 1

Class: GLUCOCORTICOIDS (Corticosteroids)

Inhaled corticosteroids are considered 1st line therapy for persistent asthma and are the most potent and effective therapy for long-term treatment of asthma (however they are less effective in COPD than in asthma)

Question 2

What is the MOA of Beclomethasone?

Answer 2

Gluccocorticoids reduce asthma symptoms by suppresing inflammation. Antiinflammatory effects:

• Decrease synthesis and release of inflammatory mediators ( eg, leukotriens, histamine, prostaglandins)
• Decreased infiltration and activity of inflammatory cells (eosinophils, leukocytes)
• Decreased edema of the airway mucosa (secondary to a decrease in vascular permeability)

Question 3

What would you advise patients taking beclomethasone, an inhaled steroid, that are used as adjucts to bronchodilators?

Answer 3

Advise patients using bronchodilators to use the bronchodilator several minutes before the corticosteroid inhalant to enhance penetration of the steroid into the bronchial tree.

Question 4

What are the side and adverse effects of glucocorticoids like Beclomethasone?

Answer 4

1. Hoarseness is a common side effect of inhaled steroids.
2. Overgrowth of oropharyngeal Candida albicans (monilia) is common but can be reduced if the patient used a spacer and swishes his or her mouth with water then expectorates after using the drug.
3. Glucocorticoids may slow skeletal growth in children but do not appear to decrease size.
4. Decreased bone density.
5. Ophthalmic complications

Question 5

What drug class does Albuterol belong to?

Answer 5

• Bronchodilator
• Selectiv B₂ agonist
• Albuterol (# 14) serves as the prototype of the fast-acting beta-2 agonists.

Question 6

What is Albuterol’s MOA?

Answer 6

• Stimulation of beta-2 receptors activates adenylyl cyclase, which promotes the formation of cAMP. cAMP inhibits the action of calcium and promotes smooth muscle relaxation and, in bronchial smooth muscle, causes bronchodilation, decreased mucus secretion, and increased mucocillary clearance.

Question 7

What are indications for albuterol?

Answer 7

• The sympathomimetics are indicated for the relief and prophylaxis of reversible bronchospasm associated with acute and chronic bronchial asthma, exercise-induced bronchospasm, bronchitis, emphysema, bronchiectasis or other obstructive pulmonary diseases.
• Albuterol is fast acting (onset 5 min) and lasts 3-6 hours.

Question 8

What are side and adverse effects of Albuterol?

Answer 8

• Usual adverse events include palpitations, chest pain, rapid heart rate, hyperglycemia, angina, and skeletal muscle tremor or nervousness but are more common with systemic use than with inhalation.
• Other common side effects include headache, skeletal muscle tremors, insomnia, dizziness, hypokalemia, hyperglycemia, and nervousness.
• Administer with caution to patients with CV disorders, diabetes, hyperthyroidism, seizure disorders, and the elderly.

Question 9

How would you instruct a patient to use an Albuterol inhaler?

Answer 9

• Patient should be instructed to thoroughly shake the inhaler for 5 to 10 seconds. Breathe out to the end of a normal breath. Hold the inhaler system upright, place the mouthpiece into the mouth, close the lips tightly and tilt the head back slightly. While activating the inhaler, take a slow, deep breath for 3 to 5 seconds, hold the breath for about 10 seconds, and exhale slowly. Allow 1 minute or more between inhalations (allows the bronchi do dilate and get a deeper penetration with the second inhalation). Rinse mouth after water after each use and do not exceed recommended dose.

Question 10

What drug class does Guaifenesin belong to?

Answer 10

Guaifenesin is an expectorant found in many cough syrups (Robitussin).

Question 11

What is the indication for Guaifensin?

Answer 11

• It is claimed to decrease mucus viscosity and convert a nonproductive cough into a productive one. It is listed for relief of cough associated with respiratory tract infections and “temporary control of nonproductive cough.”
• There is a lack of convincing studies to document efficacy. (Termed GRAS - –Generally Recognized As Safe)

Question 12

What are the side effects of Guaifenesin?

Answer 12

Side effects are nausea, vomiting & GI discomfort. (Some suggest that the nausea increases secretions.)

Question 13

What are hypersensitivity reactions?

Answer 13

Hypersensitivity reactions are pathologic processes that result from specific interactions between antigens and either humoral antibodies or sensitized lymphocytes.

Question 14

How do you treat hypersensitivity reactions?

Answer 14

Treatment may include avoidance, desensitization, or treatment with:

1. Antihistamines
2. Epinephrine is required if anaphylaxis occurs.
3. Aminophylline
4. Glucocorticoids

Question 15

What drug class does Montelukast (Singulair) belong to?

Answer 15

• LEUKOTRIENE 4 RECEPTOR ANTAGONISTS
• Montelukast is the currently recommended drug.

Question 16

What is the MOA of Montelukast?

Answer 16

Montelukast is a LTD4 antagonist, blocking the cysteinyl leukotriene receptor (LTD4). LTD4 is an inflammatory substance

Montelukast is considered the leukotriene blocker of choice for patients with persistent asthma.

Question 17

What are the indications for Montelukast?

Answer 17

Montelukast, a non-steroidal oral anti-inflammatory drug is indicated for the prophylaxis and chronic treatment of asthma in individuals over 1 year. It is also approved for the relief of symptoms of seasonal allergic rhinitis in adults and children as young as 2 years of age and for perennial allergic rhinitis in patients 6 months and older.

It is used for mild persistent asthma as an alternative to inhaled steroids. It may provide an additive effect to inhaled steroids and may decrease the needed dose of inhaled steroids while maintaining control of symptoms.

Question 18

What are adverse effects of Montelukast?

Answer 18

Adverse effects include fatigue, fever, dyspnea, and nasal congestion (none significantly different from placebo). Post marketing adverse events include suicidal thoughts.

Pregnancy Category B: Animal studies show no risks, but there are no controlled studies onpregnant women

Question 19

When should Montelukast be taken?

Answer 19

It is taken once daily in the evening with or without food. It is given at bedtime to produce the highest serum level during the night and early morning when asthma symptoms are the worst.

As monotherapy it is less effective than inhaled steroids but it may improve asthma control and permit a reduction in steroid dosage

Question 20

What class of drugs doesTiotropium inhaler belong to?

Answer 20

It is a antimuscarinic quaternary bronchodilator

inhaled anticholinergic

Question 21

What is the MOA of Tiotropium [Spiriva Handihaler}

Answer 21

is a quaternary ammonium compound that binds with high affinity to muscarinic receptors in airway smooth muscle cells and mucus glands, inhibiting the bronchoconstrictive and secretory effects of acetylcholine.

Upon inhalation, the bronchodilator effect begins in about 30 minutes, reaches a peak in 3 hours, and persists for more than 24 hours.

Inspiration of tiotropium from the Handihaler depends on the strength of the patient’s breath intake to deliver the drug to the lungs;

Question 22

What is Tiotropium indicated for?

Answer 22

It is indicated for once daily treatment of bronchospasm associated with chronic obstructive pulmonary disease (It is not indicated for asthma although some studies have shown that it is as effective as a long-acting beta-2 agonist.).

It is not metabolized; 74% of a dose is excreted unchanged in the urine. The terminal half-life is 5-6 days following inhalation

Question 23

What are the side effects of Tiotropium?

Answer 23

Systemic anticholinergic effects are minimal. The tiotropium literature has warnings of about paradoxical bronchospasm, narrow angle glaucoma and urinary retention. Dry mouth was the most commonly reported adverse reaction (precipitation of the drug in the mouth on inhalation).

Question 24

What class of drugs does Loratadine (Claritin) belong to?

Answer 24

Histamine-1 receptor antagonists (antihistamine)

Antihistamines are divided into 1st & 2nd generation agents. All are useful in treating allergic rhinitis and extrinsic asthma. Loratadine is a 2nd generation.

Question 25

What is the MOA of Loratadine?

Answer 25

Histamine-1 antagonists (“antihistamines”)”chemically replace the imidazole ring of histamine. They are fairly nonspecific and also often block muscarinic receptors. In allergic rhinitis in which histamine is the primary mediator, the H1 antagonists are the drugs of choice. They are all useful in the treatment of allergic disorders, acting by blocking histamine receptors, not by preventing release of histamine.

Question 26

What are indications for Loratadine (claratin)?

Answer 26

• 2nd generation antihistamines are considered 1st line drugs in patients with mild to moderate allergic rhinitis and allergic conjunctivitis.
• useful in extrinsic asthma.
• The antihistamines relieve sneezing, rhinorrhea, and nasal itching in allergic rhinitis. They do not reduce nasal congestion. They are most effective when taken prophylactically.

Question 27

List a few 2nd generation antihistamine drugs and which is more effective?

Answer 27

• The 2nd generation. Fexofenadine [Allegra # 45], cetirizine [Zyrtec] and loratadine [Claritin] are all OTC. They have less anticholinergic effects than 1st generation agents attributed to less complete distribution into the CNS.
• “no well-controlled clinical trials have established that any second-generation H1 antihistamine is more effective overall than any other
• The 2nd generation agents cause less (or no) drowsiness and anticholinergic effects than the 1st generation agents.

Question 28

What class of drugs does Benzonatate [Tessalon Perles] belong to?

Answer 28

Antitussives

It is believed to exert its antitussive action on stretch or cough receptors in the lung.

Question 29

What are adverse effects of Benzonatate?

Answer 29

Do not chew or dissolve capsules; benzonatate can cause local anesthesia of the oral mucosa, choking laryngospasm, bronchospasm and circulatory collapse. It may cause sedation, dizziness, constipation, and GI upset.

The FDA has warned that ingestion (as few as 1 or 2 capsules in very young) by children less than 10 years old can be fatal. Overdoses can cause seizures, cardiac arrhythmias and death

Question 30

What class of drug does Fluticasone Nasal Spray (Flonse) belong to?

Answer 30

Intranasal Steroids

Question 31

What are indications for (Fluticasone) Flonase?

Answer 31

Intranasal steroids are indicated for relief of symptoms of seasonal or perennial rhinitis (effective in 90% of patients).

They suppress the major symptoms (congestion, rhinorrhea, sneezing, itching, and erythema). They are considered 1st line therapy for moderate to severe disease and are all equal in effectiveness.

Initial effects may be seen within hours but maximal effects may require a week or more.

Question 32

What are adverse effects of Flonase?

Answer 32

Adverse effects include mucus burning or itching, caused by the vehicle (alcohol; polyethylene glycol) and occur less commonly in aqueous preparations Systemic effects are minimal at recommended doses. Excessive use may inhibit HPA function.

Preg Category C (Animal studies have shown risk to the fetus, there are no controlled studies in women)

Question 33

What class of drugs does Pseudoephedrine (Sudafed) belong to?

Answer 33

Nasal Decongestant

Nasal decongestants are sympathomimetics that stimulate alpha-adrenergic receptors of vascular smooth muscle producing vasoconstriction, pressor effects, and nasal decongestion.

Question 34

Why is Pseudoephedrine access is being controlled?

Answer 34

Pseudoephedrine access is being controlled in many pharmacies because of the ease of its use in making methamphetamine.

Oral phenylephrine has replaced pseudoephedrine in many OTC formulations when access to pseudoephedrine-containing products was restricted in an effort to reduce their use in the synthesis of methamphetamine.

Question 35

What is pseudoephedrine used for?

Answer 35

In allergic rhinitis and congestion associated with colds, the sympathomimetics only reduce nasal congestion. They do not reduce rhinorrhea, sneezing, or itching.

Question 36

What side effects does pseudoephedrine have?

Answer 36

The oral preparations cause CNS stimulation (restlessness, nervousness, agitation, irritability, anxiety, and insomnia).

They are contraindicated in patients receiving MAO inhibitors or those with severe hypertension and coronary artery disease. Special risk patients include those with hyperthyroidism, diabetes mellitus, cardiovascular disease (coronary artery disease; ischemic heart disease), increased intraocular pressure or prostatic hypertrophy.

Question 37

What should patients be instructed about pseudoephedrine?

Answer 37

Patients should be instructed to not exceed recommended dosage or use longer than 3 to 5 days. Excessive use with oral drugs may cause systemic effects (e.g., nervousness, sleeplessness) and rebound congestion may occur with intranasal preparations after the vasoconstriction subsides. Increasing the amount of drug or frequency of use may produce toxicity and perpetuate rebound congestion.