Pharmacology Asthma COPD Flashcards
Muscarinic Antagonists
Site of action:Bronchial Smooth muscle and mucosal glands
MOA: Acetylcholine stimulates muscarinic receptors
Outcome:Bronchial Constriction and mucus Secretion
Beta 2 agonists
Site of Action: Bronchial smooth muscle and mast cells
MOA: NE stimulates Beta 2 adrenergic Receptors
Outcome: Bronchial Dilation, mucus clearance, and mast cell stabilization preventing degranulation.
What helps with the onset and duration of Beta 2 agonists?
water and lipid solubility.
Examples:
Albuterol: Hydrophillic, Rapid onset, short duration
Formoterol: Amphiphillic, Long duration and rapid onset
Salmeterol: Lipophillic, long duration, slow onset
Side effects of Beta 2 Agonists
Anxiety/restlessness, tremors, Reflex Tachycardia, and Tolerance
Why is M3 Antagonism preferred compared to M2
M3 receptors mediate constriction of bronichal smooth muscle
M2 receptors act as negative feedback to inhibit Ach Release
Leukotriene Modifying agents
Inhibit the synthesis of leukotrienes or inhibit Leukotriene receptors.
Zileuton inhibits 5-lipooxygenase
Montelukast inhibits Leukotriene D4
Zariflukast inhibits Leukotriene E4
Why are corticosteroids more effective than treating asthma than COPD
Beneficial target for corticosteroids is histone deacetylase which is found to be reduced in COPD
Adverse Effects of Oral Corticosteroids and Inhaled corticosteroids
Hypertension, Cataracts/glaucoma, infections, myopathy, osteoporosis, skin thinning, Hyperglycemia (weight gain) and HPA insufficeny
Side effects from inhaled corticosteroids
Oral Candidiasis, dysphonia, cough, Pneumonia (COPD)
Can inhaled Corticosteroids reach systemic circulation?
It depends on the amount of drug reaching the lungs plus the oral bio-available fraction, but yes it is possible.