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ADRENAL HORMONES & ITS PREPARATIONS
1. Kindness always succeed, no matter with whom
ADRENAL HORMONES
By
Mr.S.KAMESHWARAN.,M.Pharm.,(Ph.D).
Associate Professor, Excel College of Pharmacy
Komarapalayam, Namakkal, Tamilnadu, India
2. ADRENAL GLAND
Adrenal gland is also known as suprarenal glands
They are chiefly responsible for releasing of
hormones in response to stress through the
synthesis of corticosteroids such as cortisol and
catecholamines such as epinephrine (adrenaline)
and norepinephrine
Each adrenal gland has two distinct structures:
Outer adrenal cortex & The inner medulla, both
of which produce hormones.
The adrenal cortex is devoted to production of
corticosteroid and androgen hormones
3.
4. Adrenal cortex contains three different layers:
ZONA GLOMERULOSA (OUTER)
The outermost layer,
It is the main site for production of aldosterone,
It is a mineralocorticoid,
Produced by the action of the enzyme aldosterone synthase.
ZONA FASCICULATA (MIDDLE)
Situated between the glomerulosa and reticularis,
It is responsible for producing glucocorticoids,
Such as 11-deoxycorticosterone, corticosterone and cortisol.
ZONA RETICULARIS (INNER)
The inner most cortical layer,
It produces androgens, mainly dehydroepiandrosterone (DHEA),
DHEA sulfate (DHEA-S), and androstenedione (the precursor to
testosterone).
All adrenocortical steroid hormones are synthesized from cholesterol.
5. MEDULLA:
The medulla chiefly produces epinephrine
and norepinephrine,
It is the core of the adrenal gland,
It is surrounded by the adrenal cortex.
It secretes approximately 20%
noradrenaline (norepinephrine) and 80%
adrenaline (epinephrine).
6.
7. CORTICOSTEROIDS
Adrenal cortex secretes 2 steroidal hormones.
GLUCOCORTICOIDS
MINERALOCORTICOIDS
BIO SYNTESIS:
Corticoids - 21 carbon containing compounds,
Having cyclo pentano perhydro
phenanthrene nucleus,
Synthesized in the adrenal cortical cells
from cholesterol.
8. ACTIONS OF MINERALOCORTICOIDS:
The primary mineralocorticoid is aldosterone,
It is produced in the adrenocortical zona
glomerulosa by the action of the enzyme aldosterone
synthase
FUNCTIONS OF MINERALOCORTICOIDS:
♥ largely responsible for the long-term regulation of
blood pressure
♥ it causes increased reabsorption of sodium in distal
convoluted tubule and collecting duct of the kidney
and increases the excretion of both potassium and
hydrogen ions.
♥ Controls body’s water volume & concentration of
electrolytes.
9. GLUCOCORTICOIDS:
☻They are produced in the zona fasciculata
☻The primary glucocorticoid released by the
adrenal gland in the human is cortisol.
☻Its secretion is regulated by the hormone ACTH
from the anterior pituitary.
FUNCTIONS OF GLUCOCORTICOIDS
CARBOHYDRATE & GLUCOSE METABOLISM
FAT METABOLISM
CALCIUM METABOLISM
WATER EXCRETION
MAINTAIN MUSCLAR ACTIVITY
MAINTAIN MYOCARDIAL CONTRACTALITY
INCREASES GASTRIC ACID & PEPSIN
SECRETION
10. MECHANISM OF ACTION OF CORTICOSTEROIDS:
LIPID SOLUBLE CORTICOSTEROID DIFFUSE ACROSS THE
CELL MEMBRANE
↓
BINDS TO THE CYTOPLASMIC RECEPTOR
↓
STRUCTURAL CHANGE IN STEROID - RECEPTOR COMPLEX
↓
ACTIVATION OF STEROID - RECEPTOR COMPLEX
↓
MIGRATION OF NUCLEUS AND BINDS TO GLUCOCORTICOID
RESPONSE ELEMENT
↓
TRANSCRIPTION OF SPECIFIC mRNA
↓
REGULATION OF PROTEIN SYNTHESIS
↓
BIOLOGICAL EFFECT
11.
12. PHARMACOKINETICS:
♣ All natural and synthetic corticoids
(MINERALO & GLUCOCORTICOIDS)
are absorbed orally,
♣ Hydrocortisone undergoes high first
pass metabolism,
♣ Its 90% bound to plasma protein
♣ Metabolized in liver by hydroxylation
and conjugation with glucaronic acid &
sulfate
♣ Excreted through urine
14. HYDROCORTISONE:
It has short duration of action, mainly has
glucocorticoid action.
In addition to that it also have little
mineralocorticoid action.
Used for
Replacement therapy – 20mg morning +
10mg after noon
Shock, Adrenal insufficiency – 100mg i.v
injection + 100mg 8 hourly i.v injection.
Topically & as suspension it is used in
eneme in ulcerative colitis
15. PREDNISOLONE:
4 times potent than hydrocortisone.
Has Selective glucocorticoid action
Intermediate duration of action.
Produce less side effects than other drugs
Used for:
Allergy, Inflammation, Auto immune
disease & cancer at the dose of 5- 60mg
orally, 10-40mg i.m.
Also administered intraarticular and to
topical routes.
16.
17. FLUDROCORTISONE:
Potent mineralocorticoid
Have some glucocorticoid action
Active orally
Used for replacement therapy in addisons
disease at the dose of 50- 200 micro gm
daily
addisons disease : (adrenal insufficiency)
Most people with primary Addison's have darkening
(hyperpigmentation) of the skin, including areas not
exposed to the sun;
19. ADR:
Sodium & water retention,
Edema,
Hypokalaemic alkalosis,(alkalosis is said to
occur when pH of the blood exceeds 7.45)
(may lead to muscular weakness, myalgia, and
muscle cramps and muscle spasms)
Increase in B.P,
Obesity,
Osteoporosis,
Ulcer.