Glucocorticoids Flashcards
(28 cards)
Glucocorticoids are a ______ group of ______. They are ________ mediators and have _______ effects
Specific - Steroids - Inflammatory - Metabolic
Why should glucocorticoids not be subscribed whilst investigation into a disease is ongoing?
They diminish efficacy of further investigtion by suppressing symptoms
Where do glucocorticoids act on a cellular level?
Intracellulary by acting on gene expression
What does tachyphylaxis of glucocorticoids mean?
They increase their own metabolism meaning that as the period of treatment increases the half life decreases - body gets better at metabolising the drug
Never prescribe a ____ dose of glucocorticoids for a ____ period of time
Low - Long
Name 4 effects of glucocorticoids on body systems
Immunomodification - Carbohydrate, lipid and protein metabolism pathways - Endocrine function - Pyschogenic effects
On the inflammatory pathway, where and on what do glucocorticoids act?
High up - Stop cell membrane phospholipids being changed into arachidonic acid (by phosphlipase A2)
What are the net anti-inflammatory effects of glucocorticoids?
Depress: Oedema - fibrin deposition - capillary dilation - leukocyte migration - phagocytic activity - capillary & fibroblast proliferation - collagen deposition
Glucocorticoids inhibit both ____ and _____ manifestations of inflammation
Early and late
What is the main difference between glucocorticoid anti-inflammatory action and NSAIDs?
Glucocorticoids suppress T-lymphocyte function, inhibit monocyte-macrophage activities, suppress fibroblast function, reduce histamine from mast cells and decrease synthesis of lymphokines
Chronic administration of glucocorticoids will cause _____ ______
Immune suppression
Which glucocorticoids are short acting? (<12 hours)
Cortisone - Hydrocortisone
Which glucocorticoids are intermediate acting? (48 hours)
Prednisone - Prednisilone - Methylprednisilone - Triamcinolone
Which glucocorticoids are long acting? (>48 hours)
Flumethasone - Dexamethasone - Betamethasone
What three factors of a glucocorticoid affect the duration of action?
Half-life - Ester’s solubility in formulation - Dose of drug
Name two esters that are very soluble
Succinate - Phosphate
Name a soluble ester
Polyethylene glycol
Name three moderately insoluble esters
Acetate - Phenylproprionate - Isoincotinate
Name a poorly soluble ester
Acetonide
How does an ester alter the time of action of a glucocorticoid?
Determines the solubility so if it very soluble the glucocorticoid will be released in minutes, if the ester is very insoluble the glucocorticoid will be released over a matter of weeks
What are inhaled glucocorticoids used for? Give some examples
Immune-mediated bronchial inflammation - Fluticasone proprionate, Beclomethasome diproprionate, Budesonide, Flunisolide, Triamcinolone acetonide
Why are glucocorticoids such as Fluticasone proprionate used for inhaled glucocorticoids?
Increased glucocorticoid receptor affinity particularly in the respiratory tract - Less systematic side effects
When treating immune-mediated disease what are the two phases when using glucocorticoids? Explain the difference
Induction of remission - Maintenance of remission
Induction centred around high dose once daily glucocorticoid - Remission centred around alternate day therapy with synergistic immunosupressant
What glucocorticoid is almost always used in immune-mediated disease treatment?
Prednisone or prednisolone
