(1.1) Drugs used in Asthma and COPD (Izard) Flashcards
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
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
What are the 2 categories of drugs used for treating asthma?
Anti-Inflammatory drugs
Bronchodilators
Bronchodilator Therapy : Mechanism of Action
Beta agonists?
Beta agonists stimulate adenylate cyclase to increase cAMP concentrations.
The higher concentration of cAMP leads to bronchodilation
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.
Bronchodilator Therapy : Mechanism of Action
Muscarinic antagonists?
Muscarinic antagonists inhibit acetylcholine which will inhibit bronchoconstriction. This leads to bronchodilation
Where are the majority of inhaled drugs (corticosteroids/Beta2 agonists) absorbed?
80-90% swallowed and follow GI tract
“Major route/less effect”
Where do beta2 agonists primarily act?
Airway smooth muscle to reverse the bronchoconstriction of asthma
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
What class of drugs is the most widely used in treatment of asthma/COPD?
Beta2 receptor agonists
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
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
What is noteworthy about Terbutaline?
ONLY Beta2 drug available by subcutaneous injection
Metaproterenol
Indications:
Cautions/Warnings:
Indications: Bronchodilator for bronchial asthma and for reversible bronchospasm
Cautions/Warnings: Significant CV effect. Can produce paradoxical bronchospasm
Pirbuterol
Indications:
Cautions/Warnings:
Indications: Prevention of reversal of bronchospasm
Cautions/Warnings: CV warnings. Can produce a clinically significant CV effect in some patients.
Levalbuterol
Indications:
Cautions/Warnings:
Indications: Treatment or prevention of bronchospasm in pts >4yo with reversible obstructive airway disease
Cautions/Warnings: Life threatening paradoxical bronchospasm
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
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
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
Indacaterol and Vilanterol
Indications?
Used to treat breathing problems caused by COPD, including bronchitis and emphysema
Olodaterol
Indications?
-Used long term, once daily maintenance bronchodilator treatment of airflow obstruction in patients with chronic COPD
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!!!
- Smooth muscle relaxation (bronchodilation)
- 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
