Corticosteroids Flashcards
Hypothalamus
Produces hormones (CRH) Regulating body temperature Physiological cycles Controls appetite Managing sexual behavior & emotional responses
Anterior Pituitary Gland
Adrenocorticotropic hormone (ACTH) Thyroid stimulating hormone (TSH)
Posterior Pituitary Gland
Oxytocin & ADH
Adrenal Gland
Adrenal cortex
- Zona glomerulosa (aldosterone)
- Zona fasiculata (cortisol)
- Zona reticularis (sex hormones)
Adrenal medulla - Epi & NE
Hypothalamic Pituitary Adrenal Axis
Hypothalamus releases CRH
Anterior pituitary release ACTH
Cortisol
Cortisol (Hydrocortisone)
Carbohydrate metabolism (gluconeogenesis)
↑ protein catabolism
Inhibits insulin from shuttling into cells
Mobilized free fatty acids
Pro-inflammatory cytokine suppression
Suppress immune system
When are cortisol levels highest?
8am
Normal Cortisol Production
15-30mg/day
Surgery Cortisol Levels
Minor 50mg/day returns to baseline w/in 24hrs
Moderate 75-100mg/day returns to baseline day 5
Major 200mg/day returns to baseline day 5
Cushing’s Syndrome
Corticosteroids overuse
Adrenal gland abnormality
Pituitary gland tumors
Ectopic adrenocorticotropic ACTH-releasing tumors
Addison’s Disease
Primary adrenocortical insufficiency
Tuberculosis worldwide
Autoimmune destruction
Congenital, malignancy, infection
2nd Adrenal Insufficiency
Traumatic brain injury
Ischemic or hemorrhagic lesions HPA
Chronic glucocorticoid treatment 3-4wks
Topical administration
Adrenal Crisis
Acute health deterioration Hypotension - absolute & relative Acute abdominal symptoms N/V Altered mental state Fatigue Fever Hyponatremia Hyperkalemia Hypoglycemia
Adrenal Crisis Causes
Glucocorticoid intake interruption Infection Surgery Gastroenteritis Stress
Mineralocorticoid Effect
Na+/K+ reabsorption
Exchange in renal distal tubules
Receptors at kidney
Glucocorticoid Effect
Anti-inflammatory properties
Corticosteroids MOA
Stimulate changes in 456 DNA transcription
- Protein synthesis
Target cells contain 11-beta hydroxysteroid dehydrogenase (Etomidate)
Cortisol (active) to Cortisone (inert)
Corticosteroids PK
Antacids interfere w/ PO absorption Highly protein 90% Readily crosses placenta Elimination half-life 1.5-3hrs 70% conjugated in liver to inactive metabolites
Corticosteroid Clinical Uses
Anti-emetic Analgesia Immunosuppression Laryngeal edema Regional blocks Asthma Cerebral edema Adrenal insufficiency
Hydrocortisone
Cortisol
Short-acting
Prednisolone
Sole replacement therapy in adrenocortical insufficiency
Prednisone
PO administration
Rapidly converted to prednisolone after absorption from GI tract
Methylprednisolone
Used to produce intense glucocorticoid effect
Dexamethasone
Multiple uses
Primarily inflammation
Drug Interactions
Enzyme inhibition
- Ketoconazole
- Fluconazole
- Etomidate
- Metapyrone
Accelerate metabolism
- Phenytoin
- Rifampin
- Phenobarbital
- Ephedrine
Corticosteroid Chronic SE
HPA suppression Corticosteroid supplementation Electrolyte & metabolic changes CNS dysfunction Peptic ulcer disease Skeletal muscle myopathy
Corticosteroid Acute SE
Hyperglycemia Delayed wound healing Infection Cancer recurrence CNS/GI disturbances Affects on Sugammadex
Primary Glucocorticoids
Anti-inflammatory
Prednisolone/Prednisone, Methylprednisolone, Betamethasone, Dexamethasone, Triamcinolone
Primary Mineralocorticoids
Sodium retention
Fludrocortisone & Aldosterone