Anti-Inflammatory Corticosteroids Flashcards
What is hydrocortisone’s:
• Anti-inflammatory activity
1
What is hydrocortisone’s:• Topical activity
1
What is hydrocortisone’s:• Salt retaining activity
1
What is hydrocortisone’s:• Potency
20
What is hydrocortisone’s:• Routes of administration?
oral, injectable, topical
What is prednisone’s • Anti-inflammatory activity
4
What is prednisone’s • Topical activity
0
What is prednisone’s • Salt retaining activity
0.3
What is prednisone’s • Potency
5
What is prednisone’s • Routes of administration?
oral
What is metylprednisolone’s topical activity
5
What is metylprednisolone’s salt retaining activity
5
What is metylprednisolone’s potency
0
What is metylprednisolone’s routes of administration
Oral and injectable
What is metylprednisolone’s anti-inflammatory activity
Four
What is Triamcinolone’s:
• Anti-inflammatory activity
5
What is Triamcinolone’s:• Topical activity
5^3
What is Triamcinolone’s: • Salt retaining activity
0
What is Triamcinolone’s: • Potency
4
What is Triamcinolone’s: • Routes of administration?
oral, injectable, topical
What is Dexamethasone’s:
• Anti-inflammatory activity
30
What is Dexamethasone’s: • Topical activity
10
What is Dexamethasone’s: • Salt retaining activity
0
What is Dexamethasone’s: • Potency
0.75
What is Dexamethasone’s: • Routes of administration?
oral, injectable, topical
What are the 5 corticosteroid drugs that Dr. French would like us to know?
Hydrocortisone, prednisone, methylprednisolone, triamcinolone, dexamethasone
What’s the goofy pneumonic I use to keep track of the 5 corticosteroid drugs I should know about?
H - Hyper (Hydrocortisone) P - Pigs (Prednisone) M - Mangle (Methylprednisolone) T - Tomatoes (Triamcinolone) D - Dramatically (Dexamethasone)
Which of the 5 drugs we are supposed to know are able to be used topically?
H, T, D (Hydrocortisone, Triamcinolone, Dexamethasone). All of these drugs have a 0 in the salt retaining category, which has to do with Mineralocorticoid activity
Where in the pathway of prostaglandin and leukotriene synthesis do Glucocortocoids work?
UPSTREAM, they inhibit phospholipase A2, which inhibits the production of Arachidonic Acid, the precursor to both leukotrienes and prostaglandins
What is the primary gland affected by chronic GC use?
Adrenal gland. With chronic GC use you can get adrenal atrophy and Iatrogenic Cushing’s
What are the main scary/concerning side effects in mineralocorticoids?
Hypertension, Hypokalemia (low potassium) Metabolic Alkalosis
What are the PHYSIOLOGIC (not pharmocologic) Metabolic effects of Glucocorticoids?
Carbohydrates, Protein, Fat (increase gluconeogenesis and blood glucose, leading to increased insulin), (decreased protein synthesis as a result of more amino acids made into glucose), (increased lipolysis in the periphery and a resultant increase in free fatty acids)
What is the PHARMACOLOGIC Metabolic effects of excess GC use?
Carbohydrate, Protein, Fats, Sodium reabsorption (diabetes like state), (muscle wasting and skin/connective tissue atrophy), (increased lipogenesis centrally leading to centripetal obesity seen in moon facies, buffalo hump), (sodium-fluid retention, hypertension, hypokalemia, metabolic alkalosis) ALL THIS LEADING TO IATROGENIC CUSHINGS DISEASE
What adverse effect can GC use have on the fluid retention system on the body?
Can lead to sodium reabsorption at kidney and thus fluid retention (normally helps increase blood volume and blood pressure). IN EXCESS, you see hypertenstion, hypokalemia (body getting rid of K to compete with increased Na) and metabolic alkalosis
What is GC effect on vascular events systemically?
reduced vasodilators (prostaglandins), decreased fluid exudation
What is the GC effect on cellular events?
overall decrease in accumulation-activation of inflammatory and immune cells
What is the GC systemic effec on inflammatory and immune mediator production?
overall DECREASE in production of inflammatory mediators
For a GC chemical to properly work, what Carbon need have an OH group?
11’. The 11-Carbon position needs to have an OH. If it doesn’t, it first needs to be metabolized into having the OH at that position (it is likely an 11-KETO)
can you use GC in pregnancy without affecting fetus
yes, depending on agent (needs to avoid fetal enzyme)
why is prednisone so commonly prescribed?
Oral administration, and 5:1 GC:MC action
which of the GC’s we are supposed to know is the most potent anti-inflammatory?
Daxamethasone
How are GC’s usually used in RA treatment?
As the “bridge” between NSAID and DMARD use. Use as low dose therapy
What is the primary clinical benefit to the alternate day glucocorticoid regimen?
Minimizes clucocorticoid block of ACTH release which can significantly reduce adrenal atrophy
