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corticosterone (C21H30O4),
aldosterone
Biosynthesis
Classes of corticosteroids
Group A
(short to medium acting glucocorticoids)
Hydrocortisone, Hydrocortisone acetate,
Cortisone acetate, Tixocortol pivalate,
Prednisolone, Methylprednisolone, and
Prednisone.
Group B
Triamcinolone acetonide, , Mometasone,
Amcinonide, Budesonide, Desonide,
Fluocinonide, Fluocinolone acetonide, and
Halcinonide.
Group C
Betamethasone, Betamethasone sodium
phosphate, Dexamethasone,
Dexamethasone sodium phosphate, and
Fluocortolone.
Group D
Hydrocortisone-17butyrate,Betamethasone valerate,
Betamethasone dipropionate, Prednicarbate
, , , , , and Fluprednidene acetate
Glucocorticoids
Knowledge Objectives
1. Synthesis, regulation and
mechanisms of action
2. Physiological effects
3. Pharmacological effects
4. Glucocorticoid drugs
5. Clinical uses
6. Side effects
Adrenal Medulla
Adrenal Cortex
Zona Glomerulosa
Zona Faciculata
Cortex Zona Reticularis
Medulla
Mineralocorticoid
Glucocorticoid
Sex steroids
8-10 am
-100
LKS
2
am
12
Midnight
12
Noon
12
Midnight
ACTH
Biosynthesis of corticosteroids
and adrenal androgens
Cholesterol
Mineralocorticoid
Mechanism of Action
S: steroid
CBG: corticosteroidbinding globulin
HSP: heat shock protein
GRE: glucocorticoid
response element
Liver
Skeletal Muscle
Adipose Tissue
Bone
Brain
Skin
Retina
Kidneys
Heart
Lymphoids
Smooth Muscle
Lung
Stomach
Intestines
Fibroblast
Testes
= Most Important
Physiological Effects
Physiological Effects
1. Metabolic Effects: Catabolic, glucose
2. Antiinflammatory and
Immunosuppressive Effects
3. Other Effects
Metabolic effects
Glucose
Influence carbohydrate and fat metabolism to
ensure adequate delivery of glucose to the brain
Increase gluconeogenesis, decrease peripheral
use of glucose
Fat
Increase in free fatty acids (increased lipolysis)
Redistribution of fat from the extremities to the
trunk and face (buffalo hump)
Protein
Favors protein breakdown and helps mobilize
amino acids to the liver for gluconeogenesis
Other Effects
1. Electolytes: Decrease absorption of Ca2+ from
the intestine and increase renal excretion of Ca2+
Increased Na+ and H2O reabsorption, increased
K+ excretion.
2. Cardiovascular effects: Facilitates the effects
of catecholamine, Maintenance of BP
3. Respiratory: Facilitates action of
catecholamines (relax airway smooth muscle)
Fetal lung maturation, increased surfactant
secretion
4. Muscle: Maintain normal skeletal muscle
5. CNS Effects: mood, sleep patterns, and EEG
Pharmacokinetic Features
Osteoporosis of Bone
Skin Thinning and Wasting
Connective Tissue Breakdown
Blood Changes
H2O Retention
Phospholipase A2
Molecular mechanism of
Anti-inflammatory effect
Mechanism of Action of
Anti-Inflammatory Steroids
Glucocorticoid Drugs
Endogenous Glucocorticoids
Synthetic Glucocorticoids
Comparison of Corticosteroids
Synthetic
1. Stronger potency
Drugs2. Lower dose
3. Longer duration
Replacement Therapy
Anti-Inflammatory
Immuno-suppression
Treatment of Allergic Disorders
Glucocorticoid Insufficiency
(Addisons Disease)
Hypoglycemia, hypotension,
weakness, anorexia, irritability
Hyperpigmentation,
hyperkalemia, hyponatremia
Immuno-suppression
Arthritis
Allergic reactions
Asthma
Autoimmune diseases
Collagen disease
Collagen vascular
diseases polymyalgia
rheumatica, temporal
arteritis
Nephrotic syndrome
Prevention of graft
rejection (transplant)
Dermatological disorders
Respiratory distress
syndrome
Side Effects
Cushings Syndrome
Cushings
Syndrome
HyperAdrenalism
Primarily the
Glucocorticoids
Side effects
Side effects
Withdrawal
1. Cold turkey if glucocorticoid therapy of less than 2 weeks duration
2. Taper off if Glucocorticoid therapy of greater than 2 weeks duration.
3. Rate of taper should be proportional to duration of prior therapy.
4. The longer the original therapy, the slower the rate of dose reduction.
.