Glucocorticoids DI Flashcards
Bioavailability of glucocorticoids
Range from 60-100%
Distribution of glucocorticoids
Moderate protein binding
Cortisol and prednisolone bind to transcortin with what kind of affinity?
High affinity with non-linear PB
Methylprednisolone binds to albumin with what kind of affinity?
Low affinity with linear PB
Patients with low albumin have more…?
…Cushingnoid symptoms
Free drug is…
…active
Metabolism of glucocorticoids
Varies with each patient
Liver disease will reduce what?
Interconversion to active steroids
Are cortisone and prednisone active or inactive?
Inactive
Drugs that cause metabolic inhibition of glucocorticoids
OCs, conjugated estrogen, macrolide ABX, ketoconazole, isoniazid, naproxen, cyclosporine
Drugs that enhance hypokalemia
Diuretics, amphotericin B, increased digitalis toxicity
Drugs that affect the metabolic induction of glucocorticoids
Phenytoin, phenobarbital, rifampin, carbamazepine, ephedrine (with dexamethasone)
Drugs that have metabolic induction BY glucocorticoids
Tacrolimus, cyclosporine, mycophenolic acid
Drugs that decrease steroid absorption
Cholestyramine, antacids
5mg of prednisone is equal to how many mg of cortisone?
25mg
5mg of prednisone is equal to how many mg of hydrocortisone?
20mg
5mg of prednisone is equal to how many mg of methylprednisolone?
4mg
5mg of prednisone is equal to how many mg of dexamethasone?
0.75mg
Glucocorticoid TDM factors for use
Patient selection- assess their risks
Use evidence-based data
Long-term vs. short-term use
Circadian rhythms (take single dose in the AM)
Monitor and minimize ADEs
Evaluate objective outcomes for disease responses
Adjustment of GLU dosing regimens
Adrenal gland ADEs
Adrenal atrophy, Cushing’s syndrome
CV tissue ADEs
Dyslipidemia, HTN, thrombosis, vasculitis
CNS ADEs
Changes in behavior, cognition, memory, mood, cerebral atrophy
GI tract ADEs
GI bleeding, pancreatitis, peptic ulcers
Immune system ADEs
Broad immunosuppression, activation of latent viruses
