L30. Pharmacology - Pulmonary Pharmacology

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Questions and Answers

What is the primary cause of Chronic Obstructive Pulmonary Disease (COPD)?

Exposure to outdoor air pollution

Cigarette smoking (correct)

Chronic allergic reactions

Genetic predisposition

Which of the following describes a symptom of COPD?

Night sweats

Increased sensitivity to allergens

Severe headaches

Frequent coughing (correct)

What is the primary function of anti-IL5 and anti-IL5 receptor blocking antibodies in asthma treatment?

To increase the maintenance dose of corticosteroids

To inhibit eosinophilic inflammation (correct)

To promote bronchoconstriction

To enhance eosinophilic inflammation

Which inflammatory cells are primarily involved in the pathophysiology of COPD?

Neutrophils and T lymphocytes Signup and view all the answers

Which antibody specifically blocks the IL5 receptor (IL5Rα)?

Benralizumab Signup and view all the answers

What structural changes occur due to chronic inflammation in COPD?

Basement membrane thickening and airway smooth muscle hypertrophy Signup and view all the answers

Which of the following components is NOT typically released by activated inflammatory cells in the lungs?

Antioxidant enzymes Signup and view all the answers

What percentage reduction in exacerbations do anti-IL5 monoclonal antibodies achieve in severe asthma patients?

50% Signup and view all the answers

What is a major clinical outcome of using anti-IL5 treatments for steroid-dependent asthmatics?

Complete elimination of corticosteroid use Signup and view all the answers

In the context of COPD, what effect does bronchoconstriction primarily have?

Reduces airflow to the airways Signup and view all the answers

What role does Cromolyn play in the treatment of asthma?

It inhibits mast cell degranulation Signup and view all the answers

Which effect of chronic inflammation can lead to mucus hypersecretion in COPD?

Increased number of goblet cells Signup and view all the answers

Which statement best characterizes the progression of Chronic Obstructive Pulmonary Disease (COPD)?

COPD is a treatable disease but is progressive in nature. Signup and view all the answers

Which of the following statements about Cromolyn is true?

It requires large doses due to its insolubility. Signup and view all the answers

Which type of asthma are anti-IL5 treatments primarily indicated for?

Severe eosinophilic asthma Signup and view all the answers

Why have anti-IL5 treatments not been effective in reducing exacerbations in COPD patients?

COPD does not involve eosinophilic inflammation. Signup and view all the answers

What is the primary consequence of the release of proteases in the context of COPD?

Alveolar wall destruction and mucus hypersecretion Signup and view all the answers

Which type of cells are primarily activated by cigarette smoke in the lungs?

Epithelial cells and macrophages Signup and view all the answers

What is a significant advantage of delivering medication via the inhaled route compared to the oral route?

Inhalation provides lower risk of systemic side effects Signup and view all the answers

What typically characterizes the systemic side effects of oral medication compared to inhaled medication?

Higher doses of oral medications commonly lead to more systemic side effects Signup and view all the answers

Which type of inflammatory cells are attracted to the lungs by the mediators released from epithelial cells and macrophages?

Monocytes, neutrophils, and T lymphocytes Signup and view all the answers

What percentage of total drug delivered by a conventional metered dose inhaler typically reaches the lower airways?

10% to 20% Signup and view all the answers

Which condition is primarily associated with the fibrosis of small airways in COPD?

Fibrogenic factors released from cells Signup and view all the answers

What is the direct effect of bronchodilators delivered through inhalation?

Decreased airway resistance Signup and view all the answers

What is the primary effect of PKA activation in airway smooth muscle?

Reduced phosphorylation of myosin light chain Signup and view all the answers

Which of the following best describes short-acting b2-agonists (SABAs)?

They are effective as first-line treatments for acute asthma symptoms. Signup and view all the answers

What characterizes the classification of beta-2 agonists?

Modifications in their molecular structure and action duration Signup and view all the answers

How do muscarinic antagonists promote bronchodilation?

By inhibiting the M3-Gq-PLC-IP3-Ca2+ pathway Signup and view all the answers

In asthma treatment, why are β2 agonists favored over muscarinic antagonists?

They provide greater bronchodilation efficacy. Signup and view all the answers

Which of the following is a common long-acting b2-agonist (LABA)?

Salmeterol Signup and view all the answers

What clinical issue arises with the use of LABAs as monotherapy?

There is controversy regarding their safety and efficacy. Signup and view all the answers

Which effect is NOT associated with the activation of b2 adrenergic receptors?

Increased intracellular calcium levels Signup and view all the answers

What is the primary reason that theophylline is still utilized in the treatment of COPD despite the availability of inhaled antimuscarinics and β2 agonists?

It provides added clinical improvement in severe cases. Signup and view all the answers

Which mechanism does theophylline utilize to promote bronchodilation?

Inhibition of phosphodiesterase 3 (PDE3). Signup and view all the answers

What is the relationship between antimuscarinic drugs and β2 agonists in managing asthma?

Antimuscarinic drugs enhance the effect of β2 agonists. Signup and view all the answers

In patients with COPD, what effect do anticholinergic drugs have on airway resistance?

They significantly reduce airway resistance and improve airflow. Signup and view all the answers

What is a significant role of Interleukin IL-10 in the context of theophylline's pharmacological action?

It has broad-spectrum anti-inflammatory effects. Signup and view all the answers

In patients with asthma, what is the main mechanism through which adenosine contributes to bronchoconstriction?

Adenosine promotes the release of histamine and leukotrienes. Signup and view all the answers

Which of the following statements regarding the use of LAMAs in asthma management is correct?

LAMAs serve as additional bronchodilators when patients are not well-controlled on LABA. Signup and view all the answers

What type of drug is theophylline commonly classified as?

A nonselective phosphodiesterase inhibitor. Signup and view all the answers

Study Notes

Anti-IL-5 Therapies

Anti-IL-5 and anti-IL5 receptor (IL5Rα) blocking antibodies inhibit eosinophilic inflammation in asthmatic patients.
Mepolizumab and Reslizumab block circulating IL-5
Benralizumab blocks IL5Rα
Anti-IL5 therapies reduce exacerbations in severe asthma patients by 50%
Anti-IL5 medications reduce the maintenance dose of oral corticosteroids by at least 50%
Anti-IL5 treatments have not been effective in reducing exacerbations in COPD patients

Cromolyn

Cromolyn inhibits mast cell degranulation
It prevents the release of inflammatory mediators like histamine and leukotrienes
Cromolyn has no bronchodilator action, but it can prevent bronchoconstriction
Cromolyn is used prophylactically for mild to moderate bronchial asthma
It is used as a preventative measure for asthma attacks

COPD

COPD refers to a group of diseases that cause breathing-related problems, including emphysema and chronic bronchitis
COPD is associated with an abnormal inflammatory response of the lungs to noxious particles or gases, the primary cause is cigarette smoking
Symptoms include: frequent coughing, wheezing, excess phlegm or mucus production, and dyspnea

Cellular Mechanism of COPD

Cigarette smoke and other irritants activate epithelial cells and macrophages in the lung to release mediators that attract circulating inflammatory cells

Inflammation in Airways

Inflammatory cells are recruited and activated in the airways
They release multiple inflammatory mediators
Mediators lead to bronchoconstriction, plasma exudation and edema, vasodilation, mucus hypersecretion, and activation of sensory nerves
Chronic inflammation can lead to structural changes, including subepithelial fibrosis, airway smooth muscle hypertrophy and hyperplasia, angiogenesis, and hyperplasia of mucus secreting cells

Routes of Drug Delivery to the Lungs

Inhaled route: The major advantage of inhalation is the delivery of drug to the airways in doses that are effective with a much lower risk of systemic side effects.

β2 Adrenergic Agonists

β2-adrenergic receptor agonists are first-line drugs for treatment of bronchial asthma and COPD.
Short-acting β2-agonists (SABAs): shortest half-life. Commonly used in conjunction with LABAs, inhaled corticosteroids, or long-acting muscarinic antagonists in treatment for COPD.
Long-acting β2-agonists (LABAs): Generally added as second-line treatment in asthma that has failed symptomatic relief with SABAs and ICS.

Muscarinic Antagonists

Muscarinic antagonists inhibit the M3-Gq-PLC-IP3-Ca2+ pathway, decreasing intracellular calcium
This promotes bronchodilation and reduces mucous secretion from glandular cells
In asthma, anti-muscarinic drugs are less effective than β2 agonists.
In COPD, anticholinergic drugs are as effective or superior to β2 agonists.
Anti-muscarinic drugs inhibit vagally mediated airway tone thereby producing bronchodilation.

Methylxanthines

Theophylline is the major methylxanthine in clinical use.
It is a nonselective phosphodiesterase (PDE) inhibitor.
Theophylline inhibits PDE3, antagonizes adenosine receptors and increases interleukin IL10 release.
Theophylline is used in the management of mild persistent asthma.

Theophylline in COPD

Theophylline is used as a bronchodilator in COPD, but inhaled antimuscarinics and β2 agonists are preferred.
Theophylline can be added to these inhaled bronchodilators in patients with more severe form of COPD.

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Description

Explore the roles of anti-IL-5 therapies and Cromolyn in managing asthma and COPD. This quiz covers the mechanisms of action, efficacy, and clinical applications of these treatments. Understand how these therapies impact inflammation and exacerbations in respiratory conditions.