Drugs Used in the Treatment of Chronic Obstructive Pulmonary Disease (COPD) Flashcards
What largely causes COPD?
Smoking
What is COPD characterized?
increased resistance to air flow during expiration (harder to breath out - inspiration is almost normal)
Is COPD reversible?
Partially reversible in some patients but progressively worsens
What can partially reverse COPD in some patients?
Bronchodilators
What are the two COPD categorizes
Bronchitis and Emphysema
What is the pathway of getting COPD in smoking?
Stimulation of Resident Alveolar Macrophages.
Cytokine production.
Activation of neutrophils, CD8+ T cells, increased macrophage numbers.
Release of matrix metalloproteinases, and free radicals
What symptoms does chronicbronchitis cause?
Inflammation of bronchi and bronchioles. Cough. Clear Mucoid Sputum. Infections with purulent sputum. Increased breathlessness.
What symptoms does Emphysema cause?
Distension and discharge to alveoli.
Destruction of acinial puching in alveolar sacs.
Loss of elastic recoil.
What is the resistance pressure of severe COPD compared to normal in expiration?
Much lower!
What does the muscarinic receptors agonists do?
Reduces parasympathetic neuroeffector transmission. .
What type of antagonist does muscarinic receptor antagonists?
Pharmacological antagonist.
What does muscarinic receptors antagonists cause?
prevents bronchoconstriction caused by smooth muscle M3 receptor activation. (blocks Aceylcholine)
What types of Muscarinic acetylcholine receptors are there?
M1, M2 and M3
What is the location and function of M1?
Ganglia - facilitates fast neurotransmission mediated by Ach acting on nicotinic receptors (increase action potential)
What is the location and function of M2?
Postganglionic neurone terminals - acts as inhibitor on autorecptors which reduce the release of Ach (cause they cause negative feedback control of Ach).
What is the location and function of M3?
Airways smooth muscle - mediate contraction to Ach and present on mucus secreting cells to increase secretion.
Competitive short acting muscarinic receptors (SAMA) antagonists currently licensed are?
Ipratropium (they all end in ium)
Competitive long acting muscarinic antagonists currently licenced are?
Tiotropium
Glycopyrronium
Aclidinium
Umeclidinium (all end in ium)
How are all competitive muscarinic receptors administered?
Inhalation
What group on these competitive muscarinic receptor antagonists reduces absorption and systematic exposure which avoid adverse effects?
Quaternary ammonium (its why they all have ium on the end)
How fast action are muscarinic receptor antagonists?
Relative to SAMA
What do Muscarinic receptors antagonists do?
They reduce bronchospasm causes by irritant stimuli. They also block Ahc-mediated basic tone.
They also decrease mucus secretion.
What effect does muscarinic receptors have on the progression of COPD?
Very little - Their main effect is palliative (reducing pain)
how many adverse effects of the muscarinic receptor antagonists?
Very few adverse effects - they have a Quaternary ammonium group!
