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Prednisone
steroid glucocorticoid used primarily as an immunosuppressant
- uses
- mechanism
- preparations
- dose and half-life
- side effects
- counter-indications
- metabolism and excretion
- dependency
Uses
- anti-inflammatory
- 2
Mechanism
- very similar to cortisone
- given as prednosone; metabolized in the liver into prednisolone
- prednisolone travels in blood bound to cortisone-bindign proteins
- crosses plasma membrane alone
- binds to receptors, activates transcription after binding to HREs
- increases serum glucose, increasing insulin and lipogenesis
- inhibits glucose uptake in muscle while stimulating hormone sensitive lipase, causing lipolysis
- increased neutrophils, decreased B and T cells, monocytes, eosinophils and basophils
- decreased IL-12 and IFN-gamma
- complement
- antibody production decreased by large doses but not by moderate
- affects NCS - insomnia, euphoria
- affects pituitary, suppresses ACTH
- get peptic ulcers
- decreases vitamin D
- inhibits wound healing
Preparations
Dose and Half Life
- glucocorticoids are absorbed rapidly when given orally
- prednisolone has a half-life of about one hour
- alternate day dosing decreases side effects and keeps ACTH production going
Side Effects
short term
- high blood glucose
- insomnia
- euphoria
long term
- Cushing's-like syndrome
- huge appetite; weight gain
- osteoporosis
- glaucoma (cataracts)
- diabetes type II
- increased risk of infection
- gingival hyperplasia
- altered hair growth
- growth suppression in children
Counter-Indications
- fungal/other infections
Metabolism and Excretion
- reduced by hepatic 11βHSD1 to form biologically active prednisolone
Dependency
- very difficult to stop; must be decreased gradually
- stopping too quickly can cause some serious side effects as natural cortisol is shut down and must be revamped