(1.1) Drugs used in Asthma and COPD (Izard) Flashcards by Bridget Tesher

What are examples of aggravating factors for an asthma patient?

—Viral respiratory infections

—Exercise

—Endocrine factors

—Drugs: Aspirin, Beta blockers

—Weather changes : Cold Air

—Allergens

—Emotional expression: Anger, laughter

—Food additives: Sulfites

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What are some examples of comorbid conditions associated with asthma?

—Rhinitis

—Hormonal changes

—Upper airway dysfunction

—Smoking nicotine dependence

—COPD

—Respiratory infections

—Sleep apnea

—Obesity

—GERD

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What are the 2 categories of drugs used for treating asthma?

Anti-Inflammatory drugs

Bronchodilators

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Bronchodilator Therapy : Mechanism of Action

Beta agonists?

Beta agonists stimulate adenylate cyclase to increase cAMP concentrations.

The higher concentration of cAMP leads to bronchodilation

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Bronchodilator Therapy : Mechanism of Action

Theophylline?

Theophylline has 2 sites of action!

Acts as a PDE inhibitor. By decreasing PDE activity, the drug is increasing cAMP concentration. The higher cAMP concentration leads to bronchodilation
Inhibits Adenosine. This inhibits adenosine’s actions to bronchoconstrict, leading to bronchodilation.

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Bronchodilator Therapy : Mechanism of Action

Muscarinic antagonists?

Muscarinic antagonists inhibit acetylcholine which will inhibit bronchoconstriction. This leads to bronchodilation

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Where are the majority of inhaled drugs (corticosteroids/Beta2 agonists) absorbed?

80-90% swallowed and follow GI tract

“Major route/less effect”

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Where do beta2 agonists primarily act?

Airway smooth muscle to reverse the bronchoconstriction of asthma

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What is the primary action of beta2 agonists?

Relax airway smooth muscle cells of all airways

Act as functional antagonists, reversing and preventing contraction of airway smooth muscle cells by all known bronchoconstrictors

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What class of drugs is the most widely used in treatment of asthma/COPD?

Beta2 receptor agonists

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Albuterol

Indications:

Adverse effects:

Contraindications/warnings:

Indications: Asthma, acute bronchitis, COPD, bronchiolitis

Adverse effects: Headache, dizziness, insomnia, dry mouth, cough

Contraindications/warnings: Paradoxical bronchospasm, deterioration of asthma, CV effects, Immediate hypersensitivity reactions

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Tertbutaline

Indications:

Adverse effects:

Contraindications/warnings:

Indications: Prophylaxis of bronchospasm associated with asthma, bronchitis and emphysema in pts. over 12 y/o

Adverse effects: Headache, nausea, tachycardia and palpitations

Contraindications/warnings: Not recommended as a med. for tocolysis

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What is noteworthy about Terbutaline?

ONLY Beta2 drug available by subcutaneous injection

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Metaproterenol

Indications:

Cautions/Warnings:

Indications: Bronchodilator for bronchial asthma and for reversible bronchospasm

Cautions/Warnings: Significant CV effect. Can produce paradoxical bronchospasm

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Pirbuterol

Indications:

Cautions/Warnings:

Indications: Prevention of reversal of bronchospasm

Cautions/Warnings: CV warnings. Can produce a clinically significant CV effect in some patients.

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Levalbuterol

Indications:

Cautions/Warnings:

Indications: Treatment or prevention of bronchospasm in pts >4yo with reversible obstructive airway disease

Cautions/Warnings: Life threatening paradoxical bronchospasm

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Fomoterol-Long Acting Beta Agonist

Indications:

Contraindications/warnings:

Noteworthy:

Indications: Treatment of Asthma in pts greater than/equal to 5 y/o as an add-on to a long term asthma control medication such as an inhaled corticosteroid. Also, maintenance treatment of bronchoconstriction in pts with COPD

Contraindications/warnings: Use of LABA’s increases the risk of asthma-related deaths and asthma related hospitilizations

Noteworthy: Prescribe for asthma ONLY as concomitant therapy with a long-term control medication such as inhaled corticosteroid

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What is a general rule to follow with prescribing LABAs?

LABA should be used in concomitant use of long-term asthma control medication such as an inhaled corticosteroid

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Salmeterol

Indications:

Treatment of asthma in patients aged 4 years and older
Prevention of exercise induced bronchospasm (EIB) in patients aged 4 years and older
Maintenance treatment of bronchospasm with chronic COPD

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Indacaterol and Vilanterol

Indications?

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

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Olodaterol

Indications?

-Used long term, once daily maintenance bronchodilator treatment of airflow obstruction in patients with chronic COPD

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Describe the general guidelines for combination therpies associated with varying degrees of asthma severity:

Generally… Short acting Beta2 agonists are always required for symptom relief. When asthma becomes more severe, you have to consider adding another medication. Start with adding ICS, then ICS and LABA, then ICS + LABA + OCS.

Atropine

MOA:

Indications:

Cautions/warnings:

MOA: muscarinic antagonist

Indications: Temporary blockade of severe/life threatening muscarinic effects

Cautions/warnings: Pts with coronary artery disease should have dose restricted to 2 to 3mg to avoid the detrimental effects of atropine-induced tachycardia

What are the drugs that act here?

Atropine
Ipratropium
Tiotropium
Aclidinium

**Ipratropium** Uses? Noteworthy?

Uses: Bronchodilator for **maintenance treatment of bronchospasm** associated with chronic obstructive pulmonary disease Noteworthy: Relatively **free of systemic atropine-like effects**

**Tiotropium** Uses?

**Long term**, once-daily, **maintenance** treatment of bronchospasm associated with COPD

**Aclidinium** Uses?

**Long term** maintenance treatment of **bronchospasm** associated with **COPD**

What are **methylxanthines?**

Unique class of drug that are derived from the **purine base XANTHINE**

What are the (3) drugs that are classified as **Methylxanthines?**

Theophylline Theobromine Caffeine

What are the actions of **Theophylline?**

2 distinct actions!!! 1. Smooth muscle relaxation (bronchodilation) 2. Suppression of the response of the airways to stimuli (non-bronchodilator prophylactic effects)

\_\_\_\_\_\_\_\_\_\_ are by far the most effective controllers for asthma, and their early use has revolutionized asthma therapy

**Inhaled corticosteroids (ICS)** are by far the most effective controllers for asthma, and their early use has revolutionized asthma therapy

Inhaled corticosteroids are the \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_, reducing inflammatory cell numbers and their activation in the airways

Inhaled corticosteroids are the **most effective anti-inflammatory agents used in asthma therapy** reducing inflammatory cell numbers and their activation in the airways

ICS __________ in the airways and \_\_\_\_\_, and numbers of activated ____________ and surface ________ in the airway mucosa

ICS **reduce eosinophils** in the airways and **sputum**, and numbers of activated **T lymphocytes** and surface **mast cells** in the airway mucosa

The molecular mechanism of action of corticosteroids involves \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_

The molecular mechanism of action of corticosteroids involves **several effects on the inflammatory process**

The major effect of corticosteroids is to \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_

The major effect of corticosteroids is to **switch off the transcription of multiple activated genes that encode inflammatory proteins**

What is the first line therapy for patients with persistent asthma?

Inhaled corticosteroids (ICS)

**Beclomethasone** Drug class: Indications: Cautions/Warnings:

Drug class: **Inhaled corticosteroids (ICS)** Indications: Maintenance treatment for asthma as a **prophylactic therapy** in patients 5 y/o and older Cautions/Warnings: Need to SLOWLY withdraw pt.s from ICS therapy, can result in death due to *adrenal insufficiency* from abrupt transition

**Budesonide** Indications? Cautions/warnings?

Indications = Maintenance treatment of asthma as **prophylactic therapy** Cautions/warnings= This drug should NOT be used where primary treatment of **status asthmaticus** or other **acute episodes of asthma** are required. Severe **hypersensitivity** to **MILK** proteins are contradindicated

**Ciclesonide** Uses: Cautions/warnings:

Uses: **Maintenance** treatment of asthma as **prophylactic therapy** in adult and adolescent pts 12 y/o and older Cautions/warnings: Ciclesonide is not indicated for the relief of **acute bronchospasm**. Use is NOT RECOMMENDED in presence of **candida albicans infection** of the mouth and pharynx, TB, fungal, bacterial, viral or parasitic infection

**Flunisolide** Uses? Contraindications?

Uses: **Maintenance** treatment of asthma as a **prophylactic therapy** in adult and pediatric patients 6 y/o and older. Also for **asthma pts requiring oral corticosteroid therapy** Contraindicated: Pts w/ primary treatment of **status asthmaticus** or other episodes of acute asthma attacks

**Fluticasone** Uses: Cautions/warnings:

Uses: Maintenance treatment of asthma as **prophylactic therapy** in pts aged 4 y/o and older Cautions/warnings: **Candida albicans** infection of mouth and pharynx MAY OCCUR!!!

**Mometasone** Uses: Cautions/warnings:

Uses: **Maintenance** treatment of asthma as **prophylactic therapy** Cautions/warnings: Contraindicated in pt.s with **status asthmaticus** or other **acute episodes of asthma** and pts with known hypersensitivity to **milk proteins**

**Triamcinolone** Uses: Cautions warnings:

Uses: **Maintenance** treatment of asthma as **prophylactic therapy** Cautions/warnings: Contraindicated in the primary treatment of **status asthmaticus** or other **acute episodes of asthma.**

Oral corticosteroids are ________________ than inhaled corticosteroids

Oral corticosteroids are **more likely to cause side effects** than inhaled corticosteroids

**Prednisone** Uses? Cautions/warnings?

Uses: **Anti-inflammatory** or **immunosuppresive agent**, or treatment of certain **endocrine conditions** Cautions/warnings: May lead to **HPA axis suppression**

Leukotriene antagonists are the most prescribed drugs for....

Both the **treatment** and **prevention** of **_ACUTE ASTHMATIC ATTACKS_**

What is the MOA of **Leukotriene antagonists?**

Binding to cysteinyl leukotriene **(CysLT)** receptors and blocking their activation and the subsequent **inflammatory cascade**

**Montelukast** MOA?

Inhibits physiologic actions of **LTD4** at the **CysLT1 receptor** without any agonist activity

**Montelukast** Indications? Cautions/warnings?

Indications: Treat **allergies** and **prevent asthma attacks** Cautions/warnings: NOT INDICATED for use in the **reversal of bronchospasm** in acute asthma attacks

**Zafirlukast** MOA? Indications? Cautions/warnings?

MOA = Selective and competitive receptor antagonist of **leukotriene D4 and E4** (LTD4 and LTE4) components of slow reacting substance of anaphylaxis Indications = **Prophylaxis** and **chronic treatment of asthma** Cautions/warnings = HEPATOTOXICITY

**Zileuton** Uses? Cautions/warnings?

Uses = Prophylaxis and **chronic treatment of asthma** Cautions/warnings = NOT RECOMMENDED in cases where **active liver disease** is present

**Omalizumab** Drug class? Uses? Cautions/warnings?

Drug class: Monoclonal antibody Uses: Chronic idiopathic **uticaria** and **asthma** Cautions/warnings: **ANAPHYLAXIS**