PHARM Steroidal Anti-Inflammatory Drugs Flashcards
Endogenous steroids vs synthetic steroids.
Endogenous steroids (e.g., hydrocortisone) – possesses mineralocorticoid activity
Synthetic steroids (e.g., prednisolone) – lack mineralocorticoid activity of other drugs, but widely used in inflammatory/allergic diseases and offers more anti-inflammatory activity than endogenous counterparts.
Time delay of synthetic steroid action.
4-6 hrs.
Steroid classes:
• Mineralocorticoids – affect water & electrolyte balance (Na+/K+)
o E.g., aldosterone (endogenous steroid)
• Glucocorticoids – affect carbohydrate and protein metabolism
o E.g., hydrocortisone/cortisol (endogenous steroid)
Anti-inflammatory action of steroids:
• Decreased vasodilation/oedema
• Decreased number/activity of leukocytes
• Decreased fibroblast function (collagen)
• Described production of eicosanoids
• Decreased production of cytokines
• Decreased synthesis of NO
• Decreased histamine release from basophils
Side effects of glucocorticoid steroids:
• Increased susceptibility to hyperglycaemia (diabetes)
• Growth suppression in children/muscle wasting
• Osteoporosis
• Hypertension
• Increased risk of infection
Also, Cushing’s syndrome.
Cushing’s syndrome symptoms
Euphoria, buffalo hump, hypertension, thinning of the skin, thin arms & legs/muscle wasting, osteoporosis, tendency to hyperglycaemia, negative nitrogen balance, increased appetite, increased susceptibility to infection, obesity, cataracts, increased abdominal fat, easy bruising, poor wound healing.
What enzyme in the ecoisanoid synthesis pathway do glucocorticoids target?
Phospholpise A2
Why is it important to wean pt’s off glucocorticoid steroids?
Avoid adrenal insufficiency -> Addison’s disease (characterised by lethargy, weakness, hypotension & dehydration).
What do glucocorticoid steroids target?
Cytosolic receptors -> decreased transcription of proteins -> reduced synthesis of inflammatory products.
