Binds to intracellular steroid receptor complex and interacts with DNA to inhibit airway
remodelling. Up-regulates gene transcription of phospholipase inhibitors (lipocortin-1)
and down-regulates proinflammatory molecules (COX/phospholipase).
Glucocorticoid effect
Decrease recruitment of inflammatory cells decreasing epithelium damage, inhibition of
macrophage function reducing the antigen response, reduction of vascular permeability
decreasing histamine release
Prednisone activation site
Activated in liver, anti-inflammatory, immunosuppressant properties.
Side effects Prednisone
cushing's disease, euphoria, adrenal suppression
SOS
Salbutamol, oxygen, steroids
oral corticosteroid indication and names
severe bronchial asthma, emphysema. Prednisone (oral), fluticasone (inhaled)
Salmeterol (LABA) Indication
long acting beta agonist used for nocturnal asthma, exercise-induced asthma, add-on in
COPD w/ peak effect 1-2 hours. Should always be used with ICS. Only add if standard
ICS has failed to control asthma.
, Salmeterol and salbutamol MoA
Stimulation of beta-2 adrenoreceptors in bronchial smooth muscle inhibits the entry of
calcium ions into muscle tissue through increased conductance of calcium sensitive
potassium channels leading to bronchodilation - hyperpolarization. It also inhibits
release of broncho-constricting agents from mast cells, inhibits microvascular leakage,
and enhances mucociliary clearance through activity of epithelial cAMP. However, there
is no evidence that chronic exposure reduces airway inflammation. It contains a B1
activity that causes cardiac stimulation.
Salbutamol indication (ventolin)
Symptom relief in mild/moderate asthma/copd, acute severe asthma
Salbutamol long-term use problem
B2 down regulation, rebound hyper-responsiveness, increased allergic response -->
"MASKS"
Symbicort indication and names of drugs
Address underlying condition, rather than masks inflammation caused by asthma and
keeping airways open. Budenoside (ICS) and formeterol (LABA)
Fast-acting LABA
Formeterol (used in symbicort)
Tiotropium indication
Long acting muscarinic antagonist. Used in COPD, as the major reversible
broncho-constrictor component is mediated by neural cholinergic effect rather than
eosinophils/TH2 cells
Tiotropium and Ipratropium MoA
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