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medchem
gardner
| Question | Answer |
|---|---|
| which two glucocorticoids bind to the GR receptor with the greast affinity | Budesonide and Fluticasone |
| Binding to the receptor can either result in the | activation or suppression of genes involved in the inflammatory process.(inhibition of transcription of genes coding for cytokines/activate genes that produce anti-inflammatory mediators) |
| anti-inflammatory mediators | lipocortin-1, endonucleases and endopeptidases |
| Lipocortin is a phospholipase A2 inhibitor and is significant in asthma how | This in turn prevents the conversion of membrane phospholipids to arachidonic acid and the synthesis of the leukotrienes LTC4 and LTD4 and LTB4. This in turns makes it a anti inflammatory mediator |
| by preventing the formation of LTC4 and LTD4 what does this do | limits the amount of bronchonstriction that can happen since these cause contrition in asthma |
| LTB4 is a chemotaxin that | recruits inflammatory cells. |
| The outcome of activating lipocortin synthesis, therefore, is to inhibit production of | LTC4 , LTD4 and LTB4, and consequently, bronchospams prevented and recruitment of inflammatory cells, respectively. |
| what is the most effective drug class for the treatment of chronic asthma | glucocorticoids |
| Used long term, corticosteroids reduce | airway responsiveness to several bronchoconstrictor mediators and block both the early and late reactions to allergen |
| Early anti-inflammatory effects of corticosteroids include | Reduce inflammatory cell activation, reduce mucosal edema, decrease local generation of inflammatory prostaglandins and leukotrienes |
| Long-term anti-inflammatory effects of corticosteroids include | t-cell, mast cell, eosinophil reduction |
| glucocorticosteroids eventually reduces the early-phase response to allergens and prevents exercise-induced asthma by which mechanisms | believed to be through the reduction the synthesis of IL-3, the cytokine that regulates mast cell production. |
| Certain corticosteroids - beclomethasone - | have low absorption across mucosal surfaces, but undergoes slow inactivation once it reaches the systemic circulation. |
| Fluticasone is | very poorly absorbed from the gut and maybe preferred if high doses of inhaled drug are needed, or for the treatment of children. |
| Ciclesonide | is a newly approved ICS for asthma (Alvesco). |
| ciclesonide (alvesco) | delivered as a pro-drug, converted in the lung to (desisobutyryl ciclesonide ) by carboxy- and cholinesterases. also remains in the lung for a prolonged peirod of time because the active metabolite is conjugated to lipids forming a “reservoir” |
| side effects of ICS are | dysphonia horseness and oral candidiasis |
| what are some systemic effects of corticoids | osteoporosis and delayed growth the new drug ciclesonide is not shown to cause either of the side effects local or systemic |
| glucocorticoids affects on bone | Increase osteoclast, increase collagenase gene, inhibit osteoblasts, effect collagen synthesis, decrease anabolic IGF-1, increase Ca2+ clearance by kidneys, increase parathyroid hormone, increase bone loss by decrease sex hormones |
| who should we use glucocorticoids with caution in | rhemotoid athristis, cataract risk, those with glucoma or a risk, those with pancretitis, |
| prednisolone is associated with | increased edema |
| more selective to mineralcorticoid can lead to | muscle weakness and muscle wasteing |
Created by:
lainylaina