What are 2 indications for the use of the β2-agonist Metaproterenol?

- Bronchodilator for bronchial asthma - Reversible bronchospasm which may occur in assoc. w/ bronchitis and COPD

What are the 4 long-acting β2-agonists?

- Fomoterol - Salmeterol - Indacaterol - Olodaterol

Lecture 4: Asthma and COPD Drugs Flashcards by s P

Which 3 major drug classes are used as bronchodilators in the tx of asthma and COPD?

β₂-agonists
Anti-cholinergic
Methylxanthines

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2 most common AE’s assocaited with β₂-agonists?

Muscle tremor and palpitations

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What is the only β₂ drug available for SQ injection?

Who is it not recommended for?

Terbutaline

not for ppl w/ sulfur allergy

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What are the indications for use of Terbutaline?

Tx or prophylaxis of bronchospasm assoc. with asthma, bronchitis and emphysema in pt’s >12 y/o

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What is the black-box warning for Terbutaline?

Not recommended as a medication for tocolysis

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Which β₂-agonist for asthma is not recommended for pt’s with sulfa allergies?

Terbutaline

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What are some of the more serious maternal AE’s associated with Terbutaline?

Cardiac or cardiopulmonary arrhythmias
Pulmonary edema
MI
Hypotension
Tachycardia

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Albuterol may have interactions with what 5 other drug classes?

β-blockers (duh)
Digoxin
Diuretics
MAO inhibitors
Tricyclic antidepressants

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Which life-threatening AE can occur after tx w/ Albuterol?

Paradoxical bronchospasm

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What are 2 indications for the use of the β₂-agonist Metaproterenol?

Bronchodilator for bronchial asthma
Reversible bronchospasm which may occur in assoc. w/ bronchitis and COPD

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Which drug class should not be used concomitantly with Metaproterenol?

Beta-adrenergic aerosol bronchodilators due to additive effects

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What are 2 cautions/warnings associated with the use of Metaproterenol?

Can produce significant cardiovascular effect in some pt’s, as measured by pulse, BP, sx’s and/or ECG changes
Can produce paradoxical bronchospasm (can be life threatening)

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Which β₂-agonist may be used with or without concurrent theophylline and/or corticosteroid therapy?

Pirbuterol

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What are the indications for the use of the β₂-agonist, Levalbuterol?

Tx or prevention of bronchospasm in pt’s > 4 y/o with reversible obstructive airway disease

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What are the 4 long-acting β₂-agonists?

Fomoterol
Salmeterol
Indacaterol
Olodaterol

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What are the 3 indications for use of the LABA, Fomoterol?

Add-on for tx of asthma in pt’s ≥5 y/o in combo w/ long-term asthma control med such as an inhaled corticosteroid
Prevention of exercise-induced bronchospasm (EIB) in pt’s ≥5 y/o
Maintenance tx of bronchoconstriction in pt’s with COPD

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What are cautions/warnings for the use of LABA’s in asthma and COPD?

↑ risk of asthma-related death and asthma-related hospitlizations
MUST be used concomitantly with an inhaled corticosteroid for asthma (fomoterol and salmeterol)

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What is the indication for the use of the LABA, Indacaterol?

Used to tx breathing problems caused by COPD, including chronic bronchitis and emphysema

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What are the 3 indications for use of the LABA, Salmeterol?

Add-on for tx of asthma in pt’s ≥4 y/o in combo w/ long-term asthma control med such as an inhaled corticosteroid
Prevention of exercise-induced bronchospasm (EIB) in pt’s ≥4 y/o
Maintenance tx of bronchoconstriction in pt’s with COPD

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What are the most common AE’s of the LABA, Indacaterol?

Cough + oropharyngeal pain + nasopharyngitis
HA and nausea

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What is the indication for use of the LABA, Olodaterol?

Used as LONG-term, 1x/daily maintenance bronchodilator in pt’s with COPD, including chronic bronchitis and emphysema

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Which anticholinergic drug is indicated for use as a bronchodilator for maintenance tx of bronchospasm associated with COPD, including chronic bronchitis and emphysema?

Ipratropium

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Which anticholinergic drug is indicated for long-term, 1x/daily, maintenance tx of bronchospasm associated with COPD, and for reducing COPD exacerbations?

Tiotropium

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Caution should be used when co-administering tiotropium or ipratropium with what drug classes, due to additive interactions?

Anticholinergic-containing drugs

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What is the indication for use of the anticholinergic drug, Aclidinium?

**LONG**-term, maintenance tx of **bronchospasm** associated with **COPD**, including **chronic bronchitis** and **emphysema**

What are 3 major AE's associated with the anticholingeric, Aclidinium?

- **Paradoxical bronchospasm** - Worsening of **narrow-angle glaucoma** - Worsening of **urinary retention**

What is a caution/warning related to the use of the anticholingeric, Aclidinium for COPD?

**NOT** for **acute** use or **initial tx** of **bronchospasm**

What are the Methylxanthines, Theophylline and Dyphylline used for?

Tx of **airways obstruction** caused by conditions such as **asthma**, **chronic bronchitis**, or **emphysema**

What are the 2 distinct actions of Theophylline in the airways of pt's w/ reversible obstruction?

- **Smooth m. relaxation** (broncho**dilation**) - **Suppression** of **airways response** to **stimuli** (non-bronchodilator prophylactic effects)

What are some of the AE's associated with Theophylline?

- CNS excitation + irritability + insomnia + restlessness + seizure - HA + diarrhea + N/V + urinary retention

Theophylline should be used with extreme caution in pt's with what 3 underlying clinical conditions?

- **Active peptic ulcer disease** - **Seizure disorders** - **Cardiac arrhythmias** (NOT including bradyarrhythmias)

What is given as the **first-line** therapy for persistent asthma; if sx's are not controlled at low doses you may add what?

**Inhaled corticosteroids** (ICS); can add **LABA** as next step

What are the 2 indications for the use of the ICS, Beclomethasone?

- Maintenance tx and prophylactic for **asthma** in pt's ≥**5 y/o** - Tx of **asthma** in pt's who **require ORAL** corticosteroid therapy to reduce or eliminate the need for systemic corticosteroids

Which 2 ICS's require special care if used in pt's who are transferred from systemically active drugs to less systemically active drugs due to potential for death by adrenal insufficiency?

- Beclomethasone - Triamcinolone

What is the indication for use of the ICS, Budesonide?

Maintenance or prophylactic tx of **asthma** in **adults** and **pediatric** pt's **≥ 6 y/o**

Which CYP is responsible for the metabolism of corticosteroid?

CYP**3A4**

Which pt's should the ICS, Budesonide not be used in?

- For **p****rimary**tx of**status asthmaticus**or other**acute episodes**of**asthma**necessitating**intensive** measures - Pts with **severe hypersenitivity** to **milk proteins**

What is the indication for use of the ICS, Ciclesonide?

Maintenance or prophylactic tx of **asthma** in **adult** and **adolescents** **≥12 y/o**

When is the ICS, Ciclesonide not indicated for use and should be avoided in the presence of what infection?

- Not indicated for the relief of **acute bronchospasm** - Not recommended in presence of **Candida albicans** infection of the mouth and pharynx, **tuberculosis**, **fungal**, **bacterial**, or **parasitic** infections

What are the 2 indication for use of the ICS, Flunisolide?

- Maintenance and prophylactic tx of **asthma** in **adults** and pt's **≥6 y/o** - **Asthma** pt's requiring **oral** corticosteroid therapy, where adding flunisolide may ↓ or eliminate the need for other oral corticosteroids

Use of the ICS, Flunisolide is contraindicated for use in which pt's?

**Primary** tx of **status asthmaticus** or other **acute episodes** of asthma where **intensive measures** are required

The use of strong CYP3A4 inhibitors (i.e., ritonavir, ketoconazole) should not be used in conjuction with what ICS?

Fluticasone

Which ICS for asthma is associated with potential Candida infection of the mouth and required pt to rinse his/her mouth with water after inhaling the drug?

Fluticasone

Which 2 ICS used for asthma are contraindicated in pt's with status asthmaticus or other acute episodes of asthma where intensive measures are required + pt's with a known hypersensitivity to milk proteins?

- Budesonide - Mometasone

What are the 2 indications for the use of the ICS, Triamcinolone?

- Maintenance and prophylactic tx of **asthma** - **Asthmatic** pt's who require **systemic** corticosteroid administration, where adding this agent may reduce or eliminate the need for the systemic corticosteroid

Which ICS has AE's including oral candidiasis, dysmenorrhea, MSK/back pain, and dyspepsia?

Mometasone

Which ICS has AE's including oral monilia, toothace, weight gain, bursitis, myalgia, rash, and voice alteration?

Triamcinolone

Which antimuscarinic used in asthma/COPD provides **temporary blockade** of the receptor?

Atropine

What are the 3 combos of ICS + LABA available as inhalers?

- Fluticasone + Salmeterol - Mometasone + Formoterol - Budesonide + Formoterol

When are **oral corticosteroids** used for asthma and in conjunction with what other drug class?

With **short-acting** β-agonists for **moderate-severe** asthma **flare-ups**

What is the oral corticosteroid which may be used for moderate to severe asthma flare ups in combo with a short acting beta-agonist?

Prednisone

What are 6 of the common AE's associated with Prednisone?

- **Fluid retention** - Alteration in **glucose tolerance** - **↑ in BP** - Behavioral and **mood changes** - ↑ appetite ---\> **weight gain**

What should patients of Prednisone be monitored for?

- **Cushing's syndrome** due to **HPA-axis** suppression - **Hyperglycemia** w/ chronic use (doses must be tapered gradually)

What are the 3 leukotriene antagonists used for asthma?

- Monte**lukast** - **Z**afir**lukast** - **Z**ileuton

What is the MOA of Montelukast?

Binds w/ **high affinity** and **selectivity** to the **CysLT1 receptor**; **INHIBITING** the physiologic actions of **LTD4**

Montelukast is primarily prescribed for what?

Treat **allergies** and **prevent** asthma attacks

Which leukotriene receptor antagonist used for asthma is associated with **hepatotoxicity** as an AE?

Zafirlukast

What is Zafirlukast prescribed for?

**Prophylaxis** and **chronic tx** of **asthma** in pts **≥5 y/o**

Patients on which other drug need to be monitored clinically if taking Zafirlukast for asthma?

**Warfarin** --\> need to monitor PTT

What is the MOA of Zileuton?

**Inhibitor** of **5-lipoxygenase** and thus **inhibits** leukotriene (LTB4, LTC4, LTD4, and LTE4) formation

3 most common AE's associated with Zileuton?

- Sinusitis - Nausea - Pharyngolaryngeal pain

What is the indication for the use of Zileuton?

**Prophylaxis** and **chronic tx** of **asthma** in pt's **≥12 y/o**

Zileuton is not indicated for use in pt's with what underlying disease/abnormalities?

**- Active liver disease** or **- Persistent hepatic function** enzymes ≥3x upper limit of normal

What are the 2 indications for the use of Omalizumab?

- **Moderate** to **severe** persistent **asthma** in pt's ≥6 y/o w/ (+) skin test for perennial aeroallergen and **sx's inadequately controlled** w/ **ICS** - **Chronic idiopathic urticaria** in pt's ≥12 y/o who remain symptomatic despite H1 antihistamine tx

What is the MOA of Omalizumab?

- Binds to free **IgE** and **blocks** binding to **FC**ε**RI** - Causes **↓ release** of **mediators** from mast cells, basophils, and eosinophils

What is a black box warning for Omalizumab?

Administer **only** in a healthcare setting prepared to manage **anaphylaxis** that can be **life threatening**

What are some of the most common AE's associated with Omalizumab?

- Arthraliga + pain (general) + **fracture** - **Pruritus** + **dermatitis** - Earache - Fatigue + dizziness

Which pt's may benefit from triple therapy with ICS + LABA + LAMA?

Pt's w/ features of **both** asthma + COPD