Asthma Pharmacology Flashcards
What do Relievers do and give examples?
Act as Bronchodilators
SABAs, LABAs and CysLT1 receptor antagonists
What are preventers and give examples?
Act as anti-inflammatory agents that reduce airway inflammation.
Glucocorticoids, Cromoglicate and humanised monoclonal IgE antibodies
Give a named SABA
Salbutamol (aka Albuterol or terbutaline)
What do SABAs do?
Increase mucous clearance and decrease mediator release from last cells and monocytes.
Side effects of SABAs?
Fine Tremor
Tachycardia
Cardiac Dysrhythmia
Hypokalaemia
Give examples of LABAs
Salmeterol
Formoterol
When are LABAs useful?
In treating nocturnal asthma
How should LABAs be prescribed?
Should always be co-administered with a glucocorticoid
Give examples of CysLT1 Receptor Antagonists
Montelukast
Zafirlukast
When are CysLT1s effective?
Against allergen and exercise induced brinchospasm
How are CysLT1s administered?
Through the oral route
Side effects of CysLT1s?
Headache
GI upset
Generally well tolerated
Examples of Methylxanthines
Theophylline
Aminophylline
What do Methylxanthines do?
Combine bronchodilator and inflammatory actions
Inhibit mediator release from mast cells and increases mucous clearance
Increase diaphragmatic contractibility and reduces fatigue.
Theophylline activates HDAC which may potentiate anti-inflammatory action of glucocorticoids
How are Methylxanthines given?
Used in combination with a b2-adrenoreceptor agonist and glucocorticoids
Given through the oral route.
Side effects of Methylxanthines
Nausea, vomiting, abdominal discomfort and headache
Problems of Methylxanthines
Numerous drug interactions involving CYP450s in particular with antibiotics that inhibit CYP450s
Why are synthetic derivatives of cortisol used in the treatment of asthma?
The endogenous steroids posses glucocorticoid and mineralcorticoid actions. The latter is unwanted. So synthetic treatments are frequently used for anti-inflammatory effect.
Examples of glucocorticoids.
Beclometasone
Budesonide
Fluticasone
How are Glucocorticoids delivered?
Used prophylactic and given by inhalational route
What do glucocorticoids do?
Increase the transcription of genes encoding for anti-inflammatory proteins and decrease the transcription of genes coding for inflammatory proteins.
Name some glucocorticoid effects
Decrease the formation of Th2 cytokines and cause apoptosis
Prevent antibody production
Reduce number of mast cells and decrease Fce production
Prevent allergen induced influx into the lung and cause apoptosis
How do glucocorticoids suppress the inflammatory component of asthma?
Prevent inflammation and resolve established inflammation
Effectiveness short and long term of glucocorticoids?
In short term don’t alleviate early stage bronchospasm caused by allergens or exercise
But effective long term when used with LABAs
