Podcast
Questions and Answers
In the context of respiratory diseases, where in the lungs does tuberculosis typically occur?
In the context of respiratory diseases, where in the lungs does tuberculosis typically occur?
- Bronchioles
- Trachea
- Upper lung lobes (correct)
- Lower lung lobes
Which of the following is the primary mechanism by which Beta2-agonists induce smooth muscle relaxation in the airways?
Which of the following is the primary mechanism by which Beta2-agonists induce smooth muscle relaxation in the airways?
- Blocking muscarinic receptors
- Inhibiting phosphodiesterase (PDE)
- Increasing levels of cyclic AMP (cAMP) (correct)
- Decreasing levels of cyclic AMP (cAMP)
What class of medications is known to prevent smooth muscle contraction and mucus secretion by blocking parasympathetic nerve activation in the lungs?
What class of medications is known to prevent smooth muscle contraction and mucus secretion by blocking parasympathetic nerve activation in the lungs?
- Beta2-agonists
- Muscarinic antagonists (correct)
- Glucocorticosteroids
- Leukotriene inhibitors
Which of the following best describes the function of inhaled corticosteroids (ICS) in asthma therapy?
Which of the following best describes the function of inhaled corticosteroids (ICS) in asthma therapy?
What is the primary mechanism of action of the drug theophylline in treating respiratory diseases?
What is the primary mechanism of action of the drug theophylline in treating respiratory diseases?
Which of the following is a common side effect associated with the inhaled administration of glucocorticosteroids?
Which of the following is a common side effect associated with the inhaled administration of glucocorticosteroids?
Which mediator is primarily responsible for the immediate phase of airway narrowing after allergen exposure in an asthmatic patient?
Which mediator is primarily responsible for the immediate phase of airway narrowing after allergen exposure in an asthmatic patient?
What is the mechanism of action of Cromones, such as sodium cromoglycate, in the treatment of asthma?
What is the mechanism of action of Cromones, such as sodium cromoglycate, in the treatment of asthma?
Which of the following is a recognized side effect of Beta2-adrenoceptor agonists due to their action at extra-pulmonary sites?
Which of the following is a recognized side effect of Beta2-adrenoceptor agonists due to their action at extra-pulmonary sites?
What is the therapeutic rationale behind using muscarinic antagonists like tiotropium bromide in the treatment of COPD?
What is the therapeutic rationale behind using muscarinic antagonists like tiotropium bromide in the treatment of COPD?
Which of the following is the primary target of Omalizumab in the treatment of asthma?
Which of the following is the primary target of Omalizumab in the treatment of asthma?
What is the primary mechanism by which glucocorticosteroids exert their anti-inflammatory effects in the treatment of asthma?
What is the primary mechanism by which glucocorticosteroids exert their anti-inflammatory effects in the treatment of asthma?
Which of the following characterizes the 'delayed phase' of airway narrowing following allergen exposure in an asthmatic individual?
Which of the following characterizes the 'delayed phase' of airway narrowing following allergen exposure in an asthmatic individual?
What is the specific role of Annexin (Lipocortin) in the mechanism of action of glucocorticosteroids?
What is the specific role of Annexin (Lipocortin) in the mechanism of action of glucocorticosteroids?
A patient with asthma is prescribed Zileuton. How does this medication improve the patient's respiratory function?
A patient with asthma is prescribed Zileuton. How does this medication improve the patient's respiratory function?
Which factor is most likely to contribute to the development of 'Airway/Bronchial hyperresponsiveness' (AHR)?
Which factor is most likely to contribute to the development of 'Airway/Bronchial hyperresponsiveness' (AHR)?
In treating active tuberculosis, why is combination therapy with multiple drugs preferred over monotherapy?
In treating active tuberculosis, why is combination therapy with multiple drugs preferred over monotherapy?
Which of the following inhaled medications is considered a short-acting beta2-agonist (SABA) used for immediate relief of asthma symptoms?
Which of the following inhaled medications is considered a short-acting beta2-agonist (SABA) used for immediate relief of asthma symptoms?
A patient with COPD is prescribed roflumilast. What best describes the primary mechanism of action of this drug?
A patient with COPD is prescribed roflumilast. What best describes the primary mechanism of action of this drug?
Which of the following is a potential side effect associated with the use of muscarinic antagonists, like ipratropium bromide, in elderly patients?
Which of the following is a potential side effect associated with the use of muscarinic antagonists, like ipratropium bromide, in elderly patients?
What is a common environmental factor that can lead to exacerbations of Chronic Obstructive Pulmonary Disease (COPD)?
What is a common environmental factor that can lead to exacerbations of Chronic Obstructive Pulmonary Disease (COPD)?
Which of the following is the primary goal of treatment for COPD?
Which of the following is the primary goal of treatment for COPD?
Which category of medications used in asthma treatment is known to cause side effects like tremor, increased heart rate, and hypokalemia?
Which category of medications used in asthma treatment is known to cause side effects like tremor, increased heart rate, and hypokalemia?
What is the primary effect of leukotrienes on the respiratory system?
What is the primary effect of leukotrienes on the respiratory system?
Which of the following statements best describes the role of phosphodiesterase (PDE) in airway smooth muscle function?
Which of the following statements best describes the role of phosphodiesterase (PDE) in airway smooth muscle function?
What zone(s) of the lung are affected in a patient with Emphysema?
What zone(s) of the lung are affected in a patient with Emphysema?
What is the mechanism of action of anti-tussives used for treating cough related to respiratory irritations?
What is the mechanism of action of anti-tussives used for treating cough related to respiratory irritations?
A patient with known aspirin-sensitive asthma could benefit most from which asthma medication?
A patient with known aspirin-sensitive asthma could benefit most from which asthma medication?
Which of these is NOT a first-line drug used in the 2-month phase of tuberculosis treatment?
Which of these is NOT a first-line drug used in the 2-month phase of tuberculosis treatment?
Following chronic exposure to allergens, an asthmatic patient's lungs undergo significant remodeling. What is the most influential initial event leading to this?
Following chronic exposure to allergens, an asthmatic patient's lungs undergo significant remodeling. What is the most influential initial event leading to this?
An experimental drug selectively prevents the phosphorylation of Myosin Light Chain Kinase (MLCK) in airway smooth muscle cells. What direct effect would this drug likely have on airway diameter?
An experimental drug selectively prevents the phosphorylation of Myosin Light Chain Kinase (MLCK) in airway smooth muscle cells. What direct effect would this drug likely have on airway diameter?
A researcher is investigating new therapies for COPD. They hypothesize that inhibiting a specific protease could slow disease progression. Which type of protease would be most relevant to target?
A researcher is investigating new therapies for COPD. They hypothesize that inhibiting a specific protease could slow disease progression. Which type of protease would be most relevant to target?
In the context of tuberculosis treatment, ethambutol is often included in the initial drug regimen. What is the primary mechanism of action of ethambutol?
In the context of tuberculosis treatment, ethambutol is often included in the initial drug regimen. What is the primary mechanism of action of ethambutol?
A researcher is developing a novel anti-inflammatory drug targeting asthma. They aim to selectively inhibit the enzyme responsible for converting arachidonic acid into leukotrienes. Which enzyme should they target?
A researcher is developing a novel anti-inflammatory drug targeting asthma. They aim to selectively inhibit the enzyme responsible for converting arachidonic acid into leukotrienes. Which enzyme should they target?
A chronic smoker with COPD develops a secondary bacterial infection in the lungs. The physician prescribes an inhaled corticosteroid to reduce inflammation, but notes a potential risk associated with this treatment in this particular patient population. What is the primary concern?
A chronic smoker with COPD develops a secondary bacterial infection in the lungs. The physician prescribes an inhaled corticosteroid to reduce inflammation, but notes a potential risk associated with this treatment in this particular patient population. What is the primary concern?
A researcher is studying the mechanism of action of a novel bronchodilator. They observe that the drug increases the activity of adenylyl cyclase in airway smooth muscle cells. What downstream effect would this drug likely have?
A researcher is studying the mechanism of action of a novel bronchodilator. They observe that the drug increases the activity of adenylyl cyclase in airway smooth muscle cells. What downstream effect would this drug likely have?
Consider a patient experiencing allergic asthma, exposed to a known allergen. If a drug selectively inhibited the recruitment of eosinophils and T lymphocytes into the airways, how would this most directly affect the course of the late/delayed asthmatic response?
Consider a patient experiencing allergic asthma, exposed to a known allergen. If a drug selectively inhibited the recruitment of eosinophils and T lymphocytes into the airways, how would this most directly affect the course of the late/delayed asthmatic response?
Flashcards
Asthma location
Asthma location
Asthma occurs in the upper airways.
COPD, emphysema location
COPD, emphysema location
COPD small airways disease, and emphysema occur in the transitional zone of the lungs.
Tuberculosis location
Tuberculosis location
Tuberculosis tends to occur in the upper lung lobes.
Allergic response
Allergic response
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Immediate asthmatic phase
Immediate asthmatic phase
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Delayed asthmatic phase
Delayed asthmatic phase
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SABA examples
SABA examples
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LABA examples
LABA examples
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Beta2-agonists MOA
Beta2-agonists MOA
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Beta2-adrenoceptor agonists
Beta2-adrenoceptor agonists
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Beta2-agonists & cAMP
Beta2-agonists & cAMP
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Muscarinic antagonists
Muscarinic antagonists
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Glucocorticosteroids MOA
Glucocorticosteroids MOA
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Glucocorticosteroids Effect
Glucocorticosteroids Effect
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Steroids & Beta-receptors
Steroids & Beta-receptors
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ICS benefits
ICS benefits
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Leukotriene pathway
Leukotriene pathway
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Zileuton MOA
Zileuton MOA
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Montelukast MOA
Montelukast MOA
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Theophylline
Theophylline
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Cromones Action
Cromones Action
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Omalizumab
Omalizumab
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Roflumilast
Roflumilast
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Study Notes
Respiratory System & Drug Delivery
- Asthma primarily affects upper airways.
- COPD impacts small airways and causes disease.
- Emphysema occurs in the transitional zone of the respiratory system.
Allergic Asthma Response to Antigen
- During an allergic reaction, mast cells release histamines.
- Additionally, prostaglandins, leukotrienes, and cytokines are released.
- Reactions cause Bronchoconstriction, Oedema, Mucus secretion and Inflammation.
- Eosinophils and T lymphocytes are involved in the inflammatory response.
Lung Function Changes After Allergen Exposure
- Reduced lung function in allergic asthma can be aided by local drug administration.
- Immediate asthmatic response is due to bronchospasm which is caused by mediators (PAF, LTs).
- Mediators released from allergen-triggered mast cells act on bronchiolar smooth muscle.
- The delayed phase involves airway narrowing due to mucosal swelling/oedema.
- Mediators are released from inflammatory cells recruited by events of the immediate phase.
- Airway Hyperresponsiveness (AHR) involves bronchospasm effects on an inflamed airway.
Pharmacological Treatment of Asthma: Bronchodilators
- Beta2-agonists help to dilate the airways.
- Muscarinic antagonists, indirectly used in COPD, also relax the airways.
Pharmacological Treatment of Asthma: Anti-Inflammatory Agents
- Glucocorticosteroids reduce inflammation.
- Xanthines are bronchodilators and have anti-inflammatory effects.
- Cromones (like sodium cromoglicate, nedocromil sodium) prevent the release of inflammatory substances.
- Leukotriene antagonists (like montelukast) block the action of leukotrienes to reduce inflammation.
- Anti-IgE (Omalizumab) reduces the allergic response by targeting IgE.
Symptomatic Relief Medications
- Short-acting b2 agonists (SABA) include salbutamol, terbutaline, and fenoterol.
- Long-acting b2 agonists (LABA) include salmeterol and formoterol for asthma/COPD and indacaterol for COPD.
Theophylline
- Theophylline can be used orally and prophylactically, but it is not a first-line treatment.
Beta-Agonist Mechanism of Action
- Binding to a G-protein coupled receptor occurs.
- The G protein activates adenylyl cyclase.
- Adenylyl cyclase converts ATP to cyclic AMP.
- Increased cAMP levels activate protein kinase A.
- Protein Kinase A (PKA) phosphorylates MLCK, inactivating it and preventing myosin light chain phosphorylation.
- This process overall leads to relaxation.
Beta2-Adrenoceptor Agonist Summary
- Includes salbutamol, terbutaline, fenoterol, formoterol, salmeterol, and indacaterol.
- Provides smooth muscle relaxation and inhibits mast cell degranulation.
- Elevates cyclic AMP within effector cells.
- It is administered via the inhaled route using a metered dose inhaler, dry powder, or nebulizer.
- Side effects include tremor, increased heart rate, and hypokalemia due to targeting beta-receptors at extra-pulmonary sites.
Muscarinic Antagonists
- Prevent smooth muscle contraction and mucus secretion.
- Prevents parasympathetic nerve activation.
- Ipratropium bromide lasts ~6 hours.
- Tiotropium bromide lasts ~24 hours.
- Muscarinic antagonists are mainly used for COPD treatment.
- This can cause dry mouth, urinary retention, constipation, and acute angle glaucoma.
Current Anti-Inflammatory Therapies
- Includes inhaled and oral glucocorticosteroids.
- Includes oral theophylline and leukotriene receptor antagonists.
- Anti-IgE: Omalizumab is given subcutaneously.
- Cromones like Sodium cromoglycate, nedocromil are inhaled.
Glucocorticosteroids in Asthma: Mechanism
- Annexin (Lipocortin) is activated.
- NFκB and AP-1 trans-repression occurs.
- Cytokine, chemokine, and adhesion molecule production are affected.
- Inflammatory enzyme production is affected (e.g., COX2, NOS).
Glucocorticosteroids Action in Asthma
- Leukotriene and cytokine synthesis/release are inhibited.
- Inflammatory cell recruitment is inhibited (T cells, eosinophils, mast cells).
- Anti-oedema occurs
Impact of Beta-Adrenoceptor Function
- Beta-adrenoceptor function increases, enhancing the bronchodilator effect of beta2-agonists.
Inhaled Corticosteroids (ICS) Role in Asthma
- Prevents infiltration/activation of inflammatory cells.
- Reduces mucosal oedema (airway wall swelling).
- Improves airflow and lung function.
- Reduces airway hyper-responsiveness.
- Reduces symptoms and exacerbation frequency/severity.
- Improves life quality.
Glucocorticosteroids - Side Effects
- Oral candidiasis, hoarseness, cough and voice problems can result with inhaled use.
- Growth retardation, bruising, immunosuppression, and hypothalamic-pituitary axis suppression can result with oral or prolonged high dose use.
- Osteoporosis, water retention (also binds to mineralcorticosteroid receptor), diabetes, hypertension, weight gain, and ocular hypertension can also result with oral or prolonged high dose use.
Anti-Leukotriene Drugs: Summary
- The 5-lipoxygenase (LO) inhibitors include Zileuton (licensed in USA).
- Leukotriene Receptor antagonists include Montelukast (cysteinyl leukotriene receptor antagonist).
- Provides relatively long action (once per day), greatest benefit in severe asthma, useful for aspirin sensitive, and exercise induced asthma.
- Has oral bioavailability.
- Side effects are rare, including headache and GI disturbance (hepatotoxicity and dyspepsia with zileuton).
Xanthine Summary
- Xanthines inhibit PDE, impairing Cyclic AMP metabolism.
- Theophylline and aminophylline are xanthines.
- The therapeutic window is approximately 10-20 mg/ml.
- Side effects include nausea, vomiting, arrhythmias, hypokalemia, hypotension, and seizures.
- Drug-drug interactions can increase/decrease plasma levels.
- Smoking promotes plasma clearance.
Cromones Summary
- Sodium Cromoglicate and Nedocromil sodium are available via inhalation.
- Cromones act as mast cell stabilizers.
- They reduce inflammatory cell activation and recruitment.
- They are not as effective as glucocorticosteroids.
Omalizumab (Xolair) Summary
- Omalizumab is a biological agent
- It binds to free IgE.
- Must be given as a subcutaneous injection.
- Omalizumab is only used in moderate to severe asthmatics uncontrolled by glucocorticosteroids.
- It is effective in only certain asthma phenotypes.
Other asthma phenotypes
- Certain asthma phenotypes respond better to anti IL-5, IL-13, and IL-4R
Chronic Obstructive Pulmonary Disease (COPD)
- Primary causes include smoking, cooking with coal/biomass fuels, and pollution.
- It causes chronic inflammation of the airways.
- Chronic bronchitis and cough are common symptoms.
- Progressive breathlessness occurs due to emphasema development.
- This can eventually lead to respiratory failure.
Treatment options for COPD
- Quitting smoking will help alleviate negative effects
- Treatment is palliative rather than curative
- Muscarinic receptor antagonists (e.g., tiotropium bromide
- β2 agonists (e.g., salmeterol)
- Dual bronchodilation
- Inhaled corticosteroids (increased risk of Pneumonia)
- PDE4 inhibitor (roflumilast) as add-on therapy for severe COPD
Anti-tussives
- Anti-tussives only treat cough not COPD
- Only indicated if there is severe irritation in bronchi/bronchioles
- Includes codeine and dextromethorphan
- Evidence for effectiveness is poor
Tuberculosis (TB)
- TB is a mycobacterial infection caused by Mycobacterium tuberculosis.
- More deaths than any other single agent (1.5 million/annum/worldwide).
- Historically treated with streptomycin, isoniazid, rifampicin, and ethambutol, but resistance is common.
- Active TB symptoms: chronic cough, bloody mucus, fever and night sweats, weight loss historically called consumption.
Tuberculosis prevention and treatment
- Vaccine BCG can help prevent
- Anti-tuberculosis drugs include first line drugs (Isoniazid, rifampicin, ethambutol, pyrazinamide) and second line drugs (capreomycin, cycloserine, ciprofloxacin, streptomycin)
- Combination therapy is used to reduce emergence of resistant strains.
- Therapy used involves a 2-month phase of first line drugs and 4-month phase of isoniazid and rifampicin.
Respiratory Drugs List
- Lists Salbutamol, Salmeterol, Fluticasone propionate, Montelukast, Theophylline, Cromoglycate, Omalizumab, Ipratropium bromide, Tiotropium bromide and Roflumilast.
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