Adrenocorticoid Steroids Flashcards
Physio GCs
Immune and metabolism
Physio MCs
Blood presseure (salt stuff)
Pharmaco use of GCs
Inflam and autoimmune dzs
Pharma use of MCs
Hypertension and heart failure
Glucocorticoid metabolic effects
Increase gluconeogenesis
Decrease glucose uptake in muscles and fat
Increase fat breakdown
Net effect is increase in plasma glucose…can worsen glucose control in diabetic patients
PEPCK enzyme is important
Glucocorticoids and stress
Provides body with increased energy via increased glucose levels…causes increased in blood pressure by activating vasoconstrictor stimuli
GC and blood cell levels
Decrease eosinophils, basophils, monocytes, and lymphocytes
Increases Hemoglobin, erythrocytes, platelets, and PMNs
Decrease in Th17s
Both innate nad immune response decreased
Most important therapeutic property of GCs
Anti-inflam
Decrease synthesis of pro inflam cytokines and increase synthesis of anti-inflam cytokines
Bad effects of GCs
Exacerbation of ulcers via gastric acid and pepsin production
Altered mental status
Exaerbate bone loss
GC mechanism of action at nuclear level
Interact with GR…moves to nucleus to increase anti-inflam genes, decrease expression of pro-inflam, interfere with NF-kB to decrease pro-inflam cytokines
Takes a while
GC other mech of action
Decreases expression of COX 2 which decreases prostanoid expression
Also inccreases Annexin 1 when inhibits phospholipase A2 and is also agonist of lipoxin receptor than inhibits inflam response
Decreased AA and decreased prostanoids
Cortisol affinity
Same for Anti-inflam effect and salt effect
Prednisone as a prodrug
Converted to prednisolone…metabolized by CYP3A4…good for tapering
Uses of GCs
Replacement therapy Acute inflammation Neoplastic dz Autoimmune dz Chornic inflammation
Adverse effects of GCs
Decreased growth in children Osteoporosis Glaucoma Increased infection risk Centripetal distr of body fat Hirsutism Increased appetite Hypertension Emotional Peripheral edema Peptic ulcer Hypokalemia
When to withdraw GCs
When max benefit obtained
When indequate benefit obtained after adequate trial
Side effects
Immediate cessation of GCs
Seroid induced acute psychosis unresponse to antipsychotics
Herpes viral corneal infections
Typical withdrawl of GCs
If tx up to 10mg/day, then reduce by 2.5 mg until 5mg/day, after that, reduce by 1 mg/day
Asthma pathology
Bronchial smooth muscle contracts
Bronchial walls inflamed
Mucus secretions are high
GCs to treat asthma
Inhaled is first choice, but can more to oral if there if severe
No others are as effective as inhaled GCs to control long term asthma
Benefits of GCs to tx asthma
Reduced bronchial hyper-responsiveness, prevention of late asthmatic response, and enhanced lung funciton
Inhaled GCs to prevent asthma and advantage
Budesonide
Minimal side effects Low oral bioavailabiltiy Delivered directly to airways Fraction of dose used systemically Small amount absorbed
Undergoes first pass effect
GC adverse effects in the asthmatic patient
Growth retardation…less severe side effects overall than oral
Dysphonia (hoarse voice)
Topical candidiasis (use larger spacer and rinse to prevent)
GCs to treat autoimmunes
Achieve lowest possible disease activity is the goal…improve the quality of life, don’t cure
