endocrine drugs pharmacology

1. Dr. Haji Bahadar
Assistant professor, KMU-IPMS
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2.  The study of drugs acting on endocrine
system of the body.
 Endocrine system: The endocrine system is
the collection of glands that produce
hormones that regulate numerous
physiological functions of the body such as
growth, metabolism, sexual functions etc.
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3. 1. Peptide/ Protein (Range from 3
amino acids to hundreds of amino acids in
size. )
2. Steroid?????
3. Amine (Thyroid hormones and
Catecholamines)
4. Eicosanoid (Fatty acid derivatives
,prostaglandins )
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4. Steroid is an organic compound having a core
structure composed of seventeen carbon atoms,
bonded in four "fused" rings.
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5. The water soluble { amine (epinephrine)
and peptide/protein hormones} are
secreted by exocytosis, travel freely in the
bloodstream, and bind to cell-surface
receptors.
The lipid soluble hormones { thyroid
hormone, steroid hormones } diffuse
across cell membranes, travel in the
bloodstream bound to transport proteins,
and diffuse through the membrane of
target cells .
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7. - On cell surface
Peptides and proteins
- In cytoplasm
Steroids
- In nucleus
Thyroid hormones
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8. The adrenal glands are located above the kidney and are
composed of two regions: the cortex and the medulla. The
adrenal cortex consists of three anatomic zones: the outer
zona glomerulosa, which secretes the aldosterone; the
intermediate zona fasciculata, which secretes cortisol; and
the inner zona reticularis, which secretes adrenal
androgens.
The adrenal medulla, lying in the center of the adrenal
gland, is functionally related to the sympathetic nervous
system and secretes the catecholamines epinephrine and
norepinephrine in response to stress.
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9. The adrenal cortex synthesizes and secretes two
steroidal hormones: the glucocorticoids (cortisol) and
the mineralocorticoids (aldosterone).
 Cortisol is involved in the regulation of glucose
metabolism along with anti-inflammatory and
immunosuppressive properties.
 Aldosterone is involved in controlling electrolyte and
fluid levels.
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11. SHORT ACTING
 Plasma t½: 0.5 – 2 hours
 Biological t½: 8 – 12 hours
 Cortisol
 Cortisone
 Fludrocortisone
INTERMEDIATE ACTING
 Plasma t½: 2 – 5 hours
 Biological t½: 18 – 36 hours
 Prednisone
 Prednisolone
LONG ACTING
 Plasma t½: 3 – 6 hours
 Biological t½: 36 – 54 hours
 Dexamethasone
 Betamethasone
 Triamcinolone
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14. All steroidal hormones enter the cell and bind to
receptors present in the cytoplasm. The hormone-
receptor complex translocates into the nucleus, and
alter the gene expression.
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15. Metabolic effects
a) Carbohydrate metabolism
➨ Increased gluconeogenesis (in liver and kidney).
➨ Increased glycogen synthesis and storage (in liver).
b) Lipid metabolism
➨ Increased lipolysis, which leads to an increased plasma levels
of free fatty acids
c)Protein metabolism
➨ Increased protein synthesis in the liver.
➨ Decreased synthesis and increased breakdown of proteins
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16. Gastrointestinal effects:
➨ Increased production of gastric acid and pepsin
Anti inflammatory effects:
➨ Inhibition of phospholipase A2 production (through induction
of lipocortin the synthesis of lipocortin, an enzyme the acts as
an inhibitor of phospholipase A2)
➨ Decreased Transcription ( the first step of gene
expression, in which a particular segment of DNA is
copied into RNA (especially mRNA) by the enzyme
RNA polymerase) of genes coding for cyclooxygenase 2
➨ Decreased production of interleukins (mainly IL-2).
➨ Inhibition of histamine release from basophils and mast cells.
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18. ◦ Acute and chronic adrenocortical insufficiency
◦ Addison's disease: it is a disorder that occurs when the body
produces insufficient amounts of certain hormones produced by
adrenal glands. In Addison's disease, the adrenal glands produce
too little cortisol and often insufficient levels of aldosterone as
well.
◦ Arthritis (rheumatoid arthritis
◦ Systemic Lupus erythematosus or SLE (an inflammatory
autoimmune disease causing scaly red patches on the
skin, especially on the face)
◦ Asthma
◦ Acute allergic reaction
◦ As immune suppressant to prevent transplant rejection
◦ Drug reactions
◦ Insect venom allergy
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20. Short term use
➨ Weight gain
➨ Mood changes (hypomania or depression)
➨ Glucose intolerance
➨ Retarded wound healing
Long-term effects (months, years)
➨ Diabetes: increased transcription of enzymes that
convert amino acids into glucose in liver and kidney
cells.
➨ Osteoporosis(a condition in which the bones become
brittle and fragile due to demineralization )
➨ Opportunistic infections
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22.  Adrenal crisis is acute adrenal insufficiency. It is a
medical emergency and potentially life-threatening
situation requiring immediate emergency treatment.
 Hypothalamic–pituitary–adrenal axis (HPA axis): Cortisol
production is regulated by the pituitary gland. This is a small
gland behind the nose and under the brain. The pituitary
gland releases adrenocorticotropic hormone (ACTH). This is a
hormone that causes the adrenal glands to release cortisol.
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24.  The adrenal gland
 The pituitary gland is injured and cannot release
ACTH
 Stopping treatment too suddenly with
glucocorticoid medicines such as prednisone
or hydrocortisone(abrupt withdrawal )
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25.  Abdominal pain or flank pain
 Confusion, loss of consciousness, or coma
 Dehydration
 Dizziness or light-headedness
 Fatigue, severe weakness
 Headache
 High fever
 Loss of appetite
 Low blood pressure
 Nausea, vomiting
 Rapid heart rate
 Rapid respiratory rate
 Slow, sluggish movement
 Unusual and excessive sweating on face or palms
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26.  In adrenal crisis, a person needs an
immediate injection of hydrocortisone
through a vein (intravenous) .
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27.  A single dose of corticosteroids, even if very large, is virtually
without harmful effects.
 When glucocorticoid therapy is prolonged over periods of
weeks or months, with doses exceeding the equivalent of
substitution therapy, the incidence of adverse effects is
greatly increased.
 When glucocorticoid therapy is prolonged over periods of
weeks or months, then HPA axis is suppressed.
 Abrupt withdrawal should be avoided, and the drug dose
must be gradually reduced(dose tapering).
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