Anti-inflammatory and immunosuppressive actions of Glucocorticoids

Remember the synthesis of endogenous corticosteroids the precursor is cholesterol. In the adrenal cortex, there’s the zona glomerulosa and zona fasciculata. The zona fasciculata makes the androgens, the sex hormones. The product of importance of the zona glomerulosa are the hormone corticosterone, from which we get the term corticoid. Cortisol (another term) was originally designated compound F and initially was used in treatment of severe arthritis.


If a pt has insufficient cortical production and becomes stressed, as in a dental procedure, hypotensive shock can occur because of their lack of endogenous glucocorticoids. In normal pts the hypothalamus takes care of this by making ACTH (secreted through the pituitary) which acts on the adrenals and cortisol is secreted. However, if a pt is taking an exogenous steroid the negative feedback is to turn off this hypothalamic-pituitary pathway and ACTH is turned off. So whenever your pt is taking an exogenous steroid as an anti-inflammatory or immunosuppressant drug, they don’t have this pathway and cant produce the normal amount of cortisol under stress.


When you look at the variety of agents available, we rarely utilize the endogenous substance cortisol. A very prominent one used in medicine and dentistry is dexamethasone (Decadron), it is the most potent glucocorticoid and is very long acting. It is used in oral surgery and also has a role in general dentistry. Betamethasone is used to treat asthma; asthma is considered an inflammatory disease. Prednisone is given by mouth and is very effective; many pts with arthritis or autoimmune diseases or other diseases with an inflammatory component will be taking this drug. Cortisone is weak and is the natural corticosteroid. Methylprednisolone is potent and can be given by injection – all can be given by injection, but of those discussed methylprednisone and dexamethasone are most often given by injection.


Some of these compounds have fluorine atoms in the molecule, these enhance the potency of the drug.


The route of administration is important. The choice of any agent is based on route of administration and duration of action. Dexamethasone (Decadron) can be given orally, IM, topically, or IV. Betamethasone is given orally and usually in the inhalational mode. Triamcinolone has an important role in dentistry as a topical agent. In some instances, intraarticular administration is used… the physician will inject the steroid right into the synovial space to reduce swelling and pain. When the steroids are used this way its NOT because they are analgesics (steroids are not analgesics!) it is because they reduce the swelling which reduces the pain.



The primary metabolic action that gives them the name “glucocorticoids” is the fact that they increase glycogenolysis and gluconeogenesis. So there tends to be hyperglycemia, usually in acute settings in dentistry this is not a problem. But if a person takes the corticosteroids chronically they will have elevated blood sugar, this is of concern to diabetics especially. They increase protein catabolism and decrease protein synthesis, this leads to a peculiar type of body mass, there tends to be a loss of muscle protein. There is a decreased osteoblast formation and activity, when given chronically. There is decrease of thyroid-stimulating hormone secretion. These metabolic effects are side effects of the drug.


Their anti-inflammatory action is local and systemic. They decrease the production of prostaglandins, cytokines and interleukins. They are not COX-1 or COX-2 inhibitors, this distinguishes the steroids from the NSAIDs. They decrease proliferation and migration of lymphocytes and macrophages, and therefore slow the healing process.

Category: Pharmacology Notes