N528 Pharmacology - Respiratory

Front 1

Allergic Rhinitis (hay fever)

Signs/Symptoms

Back 1

Tearing
Sneezing
Nasal congestion
Postnasal drip
Itchy throat

Front 2

Allergic Rhinitis

Cause?

Back 2

Due to antigen (allergen) exposure

pollen, mold spores, dust mites certain foods, animal dander

Strong genetic predisposition

Front 3

Allergic Rhinitis

Pathophysiology?

Back 3

Inflammation of the mucous membranes in the noes, throat & airways

Normal nasal mucosa has many mast cells & basophils (try to recognize environmental agents as they enter the body). Allergic rhinitis patients have more mast cells.

Front 4

Allergic Rhinitis

Which chemical mediator & receptor are responsible for allergic symptoms?

Back 4

Histamine (chemical mediator of inflammation) & H1-receptors are responsible for allergic symptoms

Front 5

Allergic Rhinitis Drugs: H1-receptor Antagonists/Antihistamines

1st-Generation Agents?

Back 5

Azelastine (astelin) 1st intranasal
brompheniramine (Dimetapp, others),
Chlorpheniramine (Chlor-Trimeton, others),
Clemastine (Tavist),
Cyproheptadine (Periactin),
Dexchlopheniramine (Dexchlor, Poladex, Polagren, Polaramine),
Diphenhydramine (Benadryl, others),
Promethazine (Phenergan, Anergan, Phenazine, others),
Triprolidine (Actifed, Actidil)

Front 6

Allergic Rhinitis Drugs: H1-receptor Antagonists/Antihistamines

2nd-Generation Agents?

Back 6

Cetirizine (Zyrtec),
desloratidine (Clarinex),
fexofenadine (Allegra),
Loratadine (Claritin)

Front 7

Allergic Rhinitis Drugs: H1-receptor Antagonists/Antihistamines

What is the difference between the 1st & 2nd generations?

Back 7

2nd generation agents are less effective, but they are less sedating.

Front 8

Allergic Rhinitis Drugs: H1-receptor Antagonists/Antihistamines

Method of Action (2)?

Back 8

Block histamine from reaching its receptors, thus alleviating allergic symptoms; provide symptomatic relief.

Block cholinergic receptors to cause typical anticholinergic effects: drying of the mucosa & mouth, urinary hesitancy (especially 1st generation)

Front 9

Allergic Rhinitis Drugs: H1-receptor Antagonists/Antihistamines

With what drugs are they often combined?

Back 9

Often combined with decongestants & antitussives in OTC cold & sinus medications.

Front 10

Allergic Rhinitis Drugs: H1-receptor Antagonists/Antihistamines

What is the most effective way to take them & why?

Back 10

Most effective when taken prophylactically to prevent allergic symptoms; ability to reverse allergic symptoms is limited.

Front 11

Allergic Rhinitis Drugs: H1-receptor Antagonists/Antihistamines

Because of additive sedation, what do you want to avoid?

What is adverse effect related to CNS?

Back 11

Caution with alcohol & other CNS depressants --> additive sedation. Impairs abilities. Sedation.

Some patients experience CNS stimulation (nervousness, insomnia, tremor, etc.) - paradoxical effect

All have potential for palpitations, QT prolongation.

Front 12

Nasal Decongestants: Intranasal Glucocorticoids

Agents?

Back 12

Beclomethasone (Beconase, Vancenase),
budesonide (Rhinocort),
flunisolide (Nasalide, Nasarel),
fluticasone propionate (Flonase),
mometasone furoate (Nasonex),
Triamcinolone acetonide (Nasacort AQ)

Front 13

Nasal Decongestants: Intranasal Glucocorticoids

Method of Action (2)?

Back 13

Decrease secretion of inflammatory mediators
&
Decrease tissue edema

Front 14

Nasal Decongestants: Intranasal Glucocorticoids

Compared with antihistamines?

Back 14

Replacing antihistamines as the DOC for the treatment of perinnial allergic rhinitis.

Front 15

Nasal Decongestants: Intranasal Glucocorticoids

How administered/applied?

How long to achieve peak results?

Back 15

May be applied directly to the nasal mucosa.

Administered by metered-spray device

May take 3-4 weeks to achieve peak results.

Front 16

Nasal Decongestants: Alternatives to IG

Agents?

Back 16

Cromolyn (NasalCrom)
Montelukast (Singulair)
Omalizumab (Xolair)

Front 17

Nasal Decongestants: Alternatives to IG

Cromolyn (NasalCrom) MOA?

When most effective?

Back 17

Alternative for patients who don't respond to intranasal steroids.

Inhibits the release of histamine from mast cells ("mast cell stabilizer")

Most effective when given prior to allergen exposure

Front 18

Nasal Decongestants: Sympathomimetics

Agents?

Back 18

Ephedrine (Pretz-D),
Naphazoline (Privine),
Oxymetazoline (Afrin 12 hour, Neo-Synephrine 12 hour, others),
Phenylephrine (Afrin 4-6 hour, Neo-Synephrine 4-6 hour, other),
Pseudoephedrine,
Tetrahydrozoline (Visine)

Front 19

Nasal Decongestants: Sympathomimetics

Which receptor do they effect?

Why are there few systemic effects?

Back 19

Alpha-adrenergic activity

Few systemic effects b/c almost none of the drug is absorbed into the circulation.

Front 20

Nasal Decongestants: Sympathomimetics

Major SE?

Back 20

Most serious, limiting side effect: Rebound congestion

Prolonged use --> hypersecretion of mucus, worsening nasal congestion once the drugs wear off.

Cycle of increased drug use as the condition worses.

Front 21

Nasal Decongestants: Sympathomimetics

How long shall they be used?

Back 21

Should be used no longer than 3 to 5 days.

Dependent patients should be gradually switched to intranasal steroids

Front 22

Nasal Decongestants: Sympathomimetics

Do oral version cause rebound congestion? Why or why not?

What are SEs?

Back 22

Orally administered sympathomimetics do not cause rebound congestions because of the much slower onset.

SE: HTN, CNS stimulation --> insomnia & anxiety

Front 23

Nasal Decongestants: Sympathomimetics

Why are they often combined with antihistamines?

Back 23

Because the sympathomimetics relieve only nasal congestion, they are often combined with antihistamines to control sneezing and tearing.

Front 24

Nasal Decongestants: Anticholinergics

Agent?

Back 24

ipratroprium bromide (Atrovent nasal spray)

The only anticholinergic indicated for symptoms associated with perennial allergic rhinitis & the common cold.

Front 25

Antitussives: Opioids

Agents?

Back 25

Codeine,
Hydrocodone bitartrate (Hycodan, others)

Front 26

Antitussives: Opioids

MOA?

Back 26

Most efficacious antitussives, act by raising the cough threshold in the CNS

Front 27

Antitussives: Opioids

Most frequently used antitussives?

Back 27

Codeine & hydrocodone are the most frequently used antitussives.

Front 28

Antitussives: Opioids

Do they cause dependence? Why or why not?

Back 28

Minimal dependence as doses needed are very low.

Front 29

Antitussives: Opioids

What schedule(s) are opioid cough mixtures?

Back 29

Most opioid cough mixtures are classified as Schedule III, IV & V.

Front 30

Antitussives: Opioids

With patients with asthma?

Back 30

Use caution in patients with asthma --> bronchoconstriction

Front 31

Antitussives: Non-opioids

Agents?

Back 31

Benzonatate (Tessalon)
Dextromethorphan (Benylin, others)

Front 32

Antitussives: Non-opioids

Dextromethorphan (Benylin, others)
Compared to opioids?
MOA?

Back 32

Chemically similar to the opioids.

Acts on the CNS to raise the cough threshold

Front 33

Most frequently used non-opioid antitussive?

Back 33

Dextromethorphan

Front 34

Antitussives: Non-opioids

Benzonatate (Tessalon)
What drug is it related to?
MOA?

Back 34

Chemically related to Tetracaine (Pontocaine) - a local anesthetic

Anesthetizes the stretch receptors in the lungs, thus suppressing cough.

Front 35

Antitussives: Non-opioids

Benzonatate (Tessalon)
What happens if you chew it?
SEs?

Back 35

If chewed, can cause numbing of the mouth & pharynx.

SE are uncommon: Sedation, nausea, headache & dizziness.

Front 36

FDA Statements: OTC Cold Products

RE: Children < 6 years of age

RE: Children < 2 years of age

Back 36

OTC cold products containing decongestants, antihistamines, & antitussives are NOT effective in children < 6 years of age & may cause serious side effects.

Strongly recommend NOT using such OTC products in children < 2 years of age.

Front 37

Expectorant

Guafenesin (Robitussin, others)
MOA

Back 37

Reduces the thickness/viscosity of bronchial secretions, thus increasing mucus flow.

"As effective as water"

Front 38

Expectorant

Guafenesin (Mucinex)

Back 38

Most effective OTC expectorant

Few adverse effects

Common ingredient in many OTC preparations.

Front 39

Mucolytic: N-Acetylcysteine (Mucomyst)

Indications?

Back 39

Adjuvant therapy in patients with abnormal or viscid mucous secretions in acute and chronic broncho-pulmonary disease.

Front 40

Mucolytic: N-Acetylcysteine (Mucomyst)

MOA?

Back 40

Exerts mucolytic action through its free sulfhydryl group which opens up the disulfide bonds in the mucoproteins, thus lowering mucous viscosity.

Front 41

Mucolytic: N-Acetylcysteine (Mucomyst)

AEs?

Back 41

Nausea, vomiting, bronchospasm, bad smell

Front 42

Mucolytic: N-Acetylcysteine (Mucomyst)

Special administration?

Back 42

Patients should receive a bronchodilator prior to administration.

Front 43

Mucolytic: Dornase Alfa (Pulmozyme)

Indications?

Back 43

Adjunct management of Cystic Fibrosis to reduce the frequency of respiratory infections, and to improve pulmonary function.

Front 44

Mucolytic: Dornase Alfa (Pulmozyme)

MOA?

Back 44

Recombinant Human Deoxyriboneclease (rHDNase) selectively cleavse DNA of neutrophils thereby decreasing mucous viscosity.

Front 45

Mucolytic: Dornase Alfa (Pulmozyme)

AEs?

Back 45

Chest pain, pharyngitis, cough, dyspnea, hemoptysis, wheezing, rash, conjunctivits

Front 46

Mucolytic: Dornase Alfa (Pulmozyme)

Use with non-CF patients?

Back 46

Should not be used routinely as a mucolytic outside CF patients.

Front 47

Asthma Drugs: Beta-Agonists/Sympathomimetics (SABAs)

Agents?

Back 47

albuterol (Proventil);
levalbuterol (Xopenex);
metaproterenol (Alupent);
pirbuterol (Maxair);
terbutaline (oral; Brethine)

Front 48

Asthma Drugs: Beta-Agonists/Sympathomimetics (SABAs)

Indications?

Back 48

DOC for acute bronchoconstriction;
Intermittent symptoms;
Exercise-Induced Bronchospasm (EIB)

Scheduled daily use not recommended
DPIs not indicated for acute severe exacerbations

Front 49

Asthma Drugs: Beta-Agonists/Sympathomimetics (SABAs)

MOA?

Back 49

Cause bronchial smooth muscle relaxation

Quick onset of action; duration 5-6 hrs

Front 50

Asthma Drugs: Beta-Agonists/Sympathomimetics (SABAs)

Adverse Effects?

Back 50

dose-related tachycardia; tremor; palpitations; nausea; headache; hypokalemia

Front 51

Asthma Drugs: Inhaled Corticosteroids (ICS)

Agents?

Back 51

Bethclomethasone (Beclovent);
budesonide (Pulmicort);
flunisolide (Aerobid);
fluticasone (Flovent);
mometasone (Asmanex)

Front 52

Asthma Drugs: Inhaled Corticosteroids (ICS)

Indications?

Back 52

Preferred therapy for long-term control of persistent asthma in all patients.

Administer on scheduled basis, not PRN
NOT used to treat an acute asthma attack

Front 53

Asthma Drugs: Inhaled Corticosteroids (ICS)

MOA?

Back 53

Anti-inflammatory; inhibitis inflammatory cells & release of inflammatory mediators.

Front 54

Asthma Drugs: Inhaled Corticosteroids (ICS)

Adverse Effects?

Back 54

headache, pharyngitis, dysphonia, oral candidiasis

Rinse mouth thoroughly after inhalation
Systemic adverse effects can occur with any ICS

Front 55

Asthma Drugs: Beta-Agonists/Sympathomimetics (LABAs)

Agents?

Back 55

arformoterol (Brovana)*,
formoterol (Foradil),
indacaterol (Arcapta)*,
salmeterol (Serevent)

*FDA labeled only for COPD

Front 56

Asthma Drugs: Beta-Agonists/Sympathomimetics (LABAs)

Indications?

Back 56

Treatment & prevention of bronchospasm only; as concomittant therapy inhaled corticosteroid; Exercise-Induced Bronchospasm (EIB)

NOT for acute symptom management
Should not be used as monotherapy

Front 57

Asthma Drugs: Beta-Agonists/Sympathomimetics (LABAs)

MOA?

Back 57

Cause bronchial smooth muscle relaxation

Do NOT act quickly!
Duration of action: 12 hours

Front 58

Asthma Drugs: Beta-Agonists/Sympathomimetics (LABAs)

Adverse Effects?

Back 58

tachycardia, tremor, palpitations, nausea, headache, hypokalemia

Front 59

Asthma Drugs: Methylxanthines

Agents?

Back 59

aminophylline (IV) theophylline (oral; Theo-Dur)

Front 60

Asthma Drugs: Methylxanthines

Indications?

Back 60

Alternative, not preferred, therapy for mild persistent asthma, or as adjunct therapy with ICS

Added when nothing else is working, not monotherapy
Clinical utility limited by low TI; monitor drug levels.

Front 61

Asthma Drugs: Methylxanthines

MOA?

Back 61

Bronchodilation through smooth muscle relaxation

Metabolism/clearance is age dependent

Front 62

Asthma Drugs: Methylxanthines

Adverse effects?

Back 62

Nausea, vomiting, headache, insomnia, tremor, irritability, restlessness, tachycardia, seizures

Many drug-drug interactions

Front 63

Asthma Drugs: Mast Cell Stabilizers
Agents?

Back 63

cromolyn (Intal)

Front 64

Asthma Drugs: Mast Cell Stabilizers

Indications?

Back 64

Alternative, but not preferred for mild, persistent asthma; Exercise-induced Bronchospasm (EIB)

Not a substitute for ICS
Not as effective as beta-agonist for EIB
As effective as theophylline or leukotriene antagonists

Front 65

Asthma Drugs: Mast Cell Stabilizers
MOA?

Back 65

Anti-inflammatory; prevents bronchoconstriction; blocks the release of histamine

May take up to 4 weeks to achieve benefit

Front 66

Asthma Drugs: Mast Cell Stabilizers
Adverse Effects?

Back 66

Relatively non-toxic; taste disturbances, cough

Front 67

Asthma Drugs: Leukotriene Modifiers

Agents?

Back 67

montelukast (Singulair),
zafirlukast (Accolate),
zileuton (Zyflo)

Front 68

Asthma Drugs: Leukotriene Modifiers

Indications?

Back 68

Alternative, but not preferred for mild persistent asthma; Exercise-Induced Bronchospasm (EIB)

Not 1st line, does not replace ICS
Not all pts report a benefit w/Tx, difficult to predict who will respond

Front 69

Asthma Drugs: Leukotriene Modifiers

MOA?

Back 69

Inhibit bronchoconstriction, may prevent airway edema and smooth muscle constraction

Drug interactions

Front 70

Asthma Drugs: Leukotriene Modifiers

Adverse Effects?

Back 70

Abdominal pain, dizziness, rash, dyspepsia, hepatotoxicity

Front 71

Asthma Drugs: Anticholinergics

Agents?

Back 71

ipratropium bromide (Atrovent)

*Not FDA labeled for asthma, additional long-term studies are needed to determine its role in asthma.

Front 72

Asthma Drugs: Anticholinergics

Indications?

Back 72

Adjunct therapy in acute asthma exacerbation, not completely responsive to beta agonist.

ipratropium + beta agonists = greater & prolonged bronchoconstriction than using either separately

Front 73

Asthma Drugs: Anticholinergics

MOA?

Back 73

Blocks acetylcholine at parasympathetic sites in bronchial smooth muscle causing bronchodilation

Front 74

Asthma Drugs: Anticholinergics

Adverse Effects?

Back 74

Rare: mydriasis, dry mouth, taste disturbances

Front 75

Asthma Drugs: Systemic Corticosteroids

Agents?

Back 75

prednisone (Deltasone),
methylprednisolone (Solu-Medrol),
prednisolone (Millipred)

Front 76

Asthma Drugs: Systemic Corticosteroids

Indications?

Back 76

Acute severe exacerbations not responding completely to initial inhaled beta-agonist therapy.

Should not be used as chronic maintenance therapy

Front 77

Asthma Drugs: Systemic Corticosteroids

MOA?

Back 77

Anti-inflammatory; inhibits inflammatory cells & release of inflammatory mediators

Front 78

Asthma Drugs: Systemic Corticosteroids

Adverse Effects?

Back 78

nausea, hyperglycemia, psychosis, weight gain, osteoporosis

High-dose regimens do not enhance outcomes & are associated with higher rate of side effects.

Front 79

Asthma Drugs: Systemic Corticosteroids

Administration issues?

Back 79

IV therapy offers no therapeutic advantage over oral administration.

Duration of therapy 5-10 days

If > 10 days, need to taper dose down to prevent adrenal suppression/crisis

Front 80

Asthma Drugs: Recombinant Anti-IgE Antibody

Agent?

Back 80

Omalisumab (Xolair)

Front 81

Asthma Drugs: Recombinant Anti-IgE Antibody

Indications?

Back 81

Treatment of allergic asthma not well controlled on oral corticosteroids or ICS

Do not abruptly stop systemic or ICS upon initiation of therapy

Front 82

Asthma Drugs: Recombinant Anti-IgE Antibody

MOA?

Back 82

Binds to the mast cells limiting the release of mediators in response to allergen exposure

Dose is based on total serum IgE level & weight

Front 83

Asthma Drugs: Recombinant Anti-IgE Antibody

Adverse Effects?

Back 83

Injection site reaction, headache, pharyngitis, sinusitis, thrombocytopenia, anaphylaxis

Front 84

Asthma Drugs: Recombinant Anti-IgE Antibody

Administration issues?

Back 84

Subcutaneous injection
Cost of therapy is significant

Due to potential for anaphylaxis, patients should be observed for 2 hours after injection.

Front 85

COPD Drugs: Anticholinergics

Agents?

Back 85

Short Acting: ipratropium bromide (Atrovent)
Long Acting: tiotropium (Spiriva)

Consider tiotropium when patients require short acting agents on a scheduled basis

Front 86

COPD Drugs: Anticholinergics

Indications?

Back 86

DOC for COPD; use tiotropium for frequent & persistent symptoms.

Not used as monotherapy for acute exacerbations.
Improve symptoms; do not slow decline of COPD
Frequently used in combination with beta-agonist.

Front 87

COPD Drugs: Anticholinergics

MOA?

Back 87

Blocks acetylcholine at parasympathetic sites in bronchial smooth muscle causing bronchodilation

Slower onset & more prolonged effect compared with beta-agonist

Front 88

COPD Drugs: Anticholinergics

Adverse Effects?

Back 88

Rare: mydriasis, dry mouth, taste disturbances

Front 89

COPD Drugs: Beta-Agonists/Sympathomimetics

Agents?

Back 89

LABA's:
arformeterol (Brovana)*,
formoterol (Foradil),
indacaterol (Arcapta)*,
salmeterol (Serovent)

*FDA labeled for COPD

Front 90

COPD Drugs: Beta-Agonists/Sympathomimetics

Indications?

Back 90

Frequent & persistent symptoms of COPD; utilized when patients require short acting agents on a scheduled basis

NOT for acute symptom management
Useful for nocturnal symptoms

Front 91

COPD Drugs: Beta-Agonists/Sympathomimetics

MOA?

Back 91

cause bronchial smooth muscle relaxation

Improve symptoms & reduce exacerbations
12 hr duration makes more convenient
No does titration; standard dosage for all agents

Front 92

COPD Drugs: Beta-Agonists/Sympathomimetics

Adverse Effects?

Back 92

tachycardia, tremor, palpitations, nausea, headache, hypokalemia

Front 93

COPD Drugs: Methylxanthines

Agents?

Back 93

Theophylline (oral; Theo-Dur)

Front 94

COPD Drugs: Methylxanthines

Indications?

Back 94

Adjunct therapy for patients who have not achieved optimal response to ipratropium/beta-agonist

Clinical utility limited by low therapeutic index; need to monitor drug levels

Considered only for those who are intolerant or unable to use an inhaled bronchodilator

Front 95

COPD Drugs: Methylxanthines

MOA?

Back 95

bronchodilation through smooth muscle relaxation; respiratory stimulant; reduces diaphragmatic fatigue

Front 96

COPD Drugs: Methylxanthines

Adverse Effects?

Back 96

Nausea, vomiting, headache, insomnia, tremor, irritability, restlessness, tachycardia, seizures

Many drug-drug interactions

Front 97

COPD Drugs: Inhaled Corticosteroids (ICS)

Agents?

Back 97

beclomethasone (Beclovent),
budesonide (Pulmicort),
flunisolide (Aerobid),
fluticasone (Flovent),
mometasone (Asmanex)

Front 98

COPD Drugs: Inhaled Corticosteroids (ICS)

Indications?

Back 98

Symptomatic patients with an FEV1 < 50% & repeated exacerbations (Stage III & IV)

Combination therapy with LABA > either agent alone
Not all patients will benefit from ICS

Front 99

COPD Drugs: Inhaled Corticosteroids (ICS)

MOA?

Back 99

Anti-inflammatory; inhibits inflammatory cells & release of inflammatory mediators

Does not modify long-term decline of FEV1 in COPD
Reduces frequency of exacerbations

Front 100

COPD Drugs: Inhaled Corticosteroids (ICS)

Adverse Effects?

Back 100

headache, pharyngitis, dysphonia, oral candidiasis

Rinse mouth thoroughly after inhalation
Systemic adverse effects can occur with any ICS

Front 101

COPD Drugs: Systemic Corticosteroids

Agents?

Back 101

prednisone (Deltasone),
methylprednisolone (Solu-Medrol),
prednisolone (Millipred)

Front 102

COPD Drugs: Systemic Corticosteroids

Indications?

Back 102

Acute exacerbations; chronic therapy should be avoided if possible.

NOT considered as routine maintenance therapy.
If required, use lowest effective dose.

Front 103

COPD Drugs: Systemic Corticosteroids

MOA?

Back 103

Anti-inflammatory, inhibits inflammatory cells & release of inflammatory mediators

Front 104

COPD Drugs: Systemic Corticosteroids

Adverse Effects?

Back 104

Nausea, hyperglycemia, psychosis, weight gain, osteoporosis

Clinical benefit in chronic management not evident & risk of toxicity is extensive.

Front 105

Pneumonia: Outpatient Management

Agents for Healthy Patients (< 60 yo w/o comorbidities)

Back 105

Macrolide:
azithromycin (Zithromax),
clarithromycin (Biaxin),
Erythromycin

Doxycylcine

Front 106

Pneumonia: Outpatient Management

Agents for Patient w/Other Health Problems (e.g. COPD, diabetes, heart failure, cancer or >/= 60 yo)

Back 106

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