1. Endocrine PharmacologyEndocrine Pharmacology

2. Basic principlesBasic principles
 Endocrine SystemEndocrine System
- Uses chemical signals (hormones) for cell to- Uses chemical signals (hormones) for cell to
cell communicationcell communication
- Coordinates the function of cells- Coordinates the function of cells
- Response to an endocrine signal occurs- Response to an endocrine signal occurs
within minutes to hours (ductless glands)within minutes to hours (ductless glands)

3.  HormonesHormones
- Cell to cell communication molecules- Cell to cell communication molecules
- Made in glands or cells
- Transported by blood
- Distant or local target tissue receptors
- Activates physiological response

5.  Hormonal regulation ↑↓Hormonal regulation ↑↓
- Growth & development- Growth & development
- Reproduction, fertility, sexual function- Reproduction, fertility, sexual function
- Response to environmental situations- Response to environmental situations
(stress..)(stress..)
- Maintenance of normal homeostasis- Maintenance of normal homeostasis

6.  Chemical nature of hormonesChemical nature of hormones
- a. a derivatives:- a. a derivatives:
T3; T4; Dopamine (precursor; Tyrosine)T3; T4; Dopamine (precursor; Tyrosine)
- Small peptides; polypeptides; large proteins or- Small peptides; polypeptides; large proteins or
glycoproteins:glycoproteins:
Hypothalamic hormones; GH; PRL; Insulin;Hypothalamic hormones; GH; PRL; Insulin;
Glucagon; LH; FSH; TSHGlucagon; LH; FSH; TSH……..
- Steroids- Steroids
Cortisol; Aldosterone; Estrogen; Progesterone;Cortisol; Aldosterone; Estrogen; Progesterone;
AndrogensAndrogens

7.  Amine HormonesAmine Hormones
- Derived from the amino acid tyrosine- Derived from the amino acid tyrosine
- Include catecholamines (Dopamine) &- Include catecholamines (Dopamine) &
thyroid hormonesthyroid hormones
- Stored until secreted- Stored until secreted
* Receptor locations* Receptor locations
Surface (Dopamine)
Intracellular (nuclear; T3 & T4)

8. Protein and Polypeptide Hormones:Protein and Polypeptide Hormones:
Synthesis and ReleaseSynthesis and Release

9. Protein and Polypeptide Hormone ReceptorsProtein and Polypeptide Hormone Receptors
 Bind to surface receptorBind to surface receptor
 TransductionTransduction
- System activation- System activation
- Open ion channel
 Enzyme activation
 Second messenger systems
 Protein synthesis

10. Steroid Hormones ReceptorsSteroid Hormones Receptors

11.  Basal conditionsBasal conditions...minimal release...minimal release
 Stimuli:Stimuli:
- Nerve impulse- Nerve impulse
- Change in composition of ECF- Change in composition of ECF
- Another hormone (trophic hormone)- Another hormone (trophic hormone)
blood → target cells → receptors → initialblood → target cells → receptors → initial
change → cascade of reactions →change → cascade of reactions →
recognizable changerecognizable change……

12. - Change in cell permeability- Change in cell permeability
- Stimulation or inhibition of protein synthesis- Stimulation or inhibition of protein synthesis
** Transcription or translation** Transcription or translation
- Stimulation or inhibition of mediator release- Stimulation or inhibition of mediator release
(second messenger)(second messenger)
** cAMP; DAG; Ca** cAMP; DAG; Ca++++
; ITP (IP; ITP (IP33)...)...

13.  How long a hormone stays high in blood?How long a hormone stays high in blood?
Depends on:Depends on:
- Extent of protein binding- Extent of protein binding
- Efficiency of degradable enzymes &- Efficiency of degradable enzymes &
clearanceclearance
Metabolism & excretionMetabolism & excretion
- Efficiency of negative feedback mechanisms- Efficiency of negative feedback mechanisms

14. CRH GnRHCRH GnRH
- ↓ ↓ -- ↓ ↓ -
ACTH LH; FSHACTH LH; FSH
- ↓ ↓ -- ↓ ↓ -
CortisolCortisol EE22; Progesterone; Progesterone

15.  Sources of hormones:Sources of hormones:
- Natural- Natural
Human (GH; LH & FSH; hCG); AnimalHuman (GH; LH & FSH; hCG); Animal
(Insulin, T(Insulin, T33 & T& T44))
- Biosynthetic- Biosynthetic
Insulin (Porcine & Bovine)Insulin (Porcine & Bovine)
- Synthetic- Synthetic
Most hormones and their antagonistsMost hormones and their antagonists

16.  Disorders affecting endocrine glands:Disorders affecting endocrine glands:
- Deficiency states- Deficiency states
HRTHRT

17. - Excess production of a specific hormone- Excess production of a specific hormone
Inhibitors to the synthetic machinery orInhibitors to the synthetic machinery or
Release inhibitors orRelease inhibitors or
Specific antagonistsSpecific antagonists

18.  Clinical pharmacology of hormones:Clinical pharmacology of hormones:
- Major clinical use of hormones- Major clinical use of hormones
HRT ( physiological doses)HRT ( physiological doses)
- Supra-physiological doses (pharmacological- Supra-physiological doses (pharmacological
doses)doses)
Anti-inflammatory effects (non-endocrine-Anti-inflammatory effects (non-endocrine-
related diseases)...related diseases)...
- Use as diagnostic tool (TRH test ....)- Use as diagnostic tool (TRH test ....)

19. - The use of some drugs which are not- The use of some drugs which are not
hormones, but used in the management ofhormones, but used in the management of
diseases of endocrine origindiseases of endocrine origin
Antithyroid drugs, oral hypoglycemic agentsAntithyroid drugs, oral hypoglycemic agents……
- Some drugs are used to treat diseases not- Some drugs are used to treat diseases not
related to the endocrine system but affectingrelated to the endocrine system but affecting
itit
Anticancerous drugs → ♂ & ♀ infertilityAnticancerous drugs → ♂ & ♀ infertility
- The use of hormones as contraceptives???- The use of hormones as contraceptives???