Gonadal Physiology and Pharmacology

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Chapter 31:  Endocrine: Gonadal Hormones

Gonadal Hormones and Inhibitors

Classification

Physiology/Endocrine Background

Estrogens

Menu II

Steroid Hormone Classification

(partial listing)

Some structures of Interest

Estradiol [Estrogen]

 

Clomiphene (Clomid) [Antiestrogen]

 

Tamoxifen (Nolvadex) [Antiestrogen]

 

Medroxyprogesterone [Progestin]

 

Norgestrel [Progestin]

 

Mifepristone [anti-progestin]

 

Testosterone cypionate [androgen]

 

Flutamide [anti-androgen]

 

 

Puberty: Mechanism and ovarian function

 

Estrogens

Some Commonly Used Estrogens
ethinyl estradiol micronized estradiol estradiol cypionate estradiol valerate estropipate
mixed estrogenic agents diethylstilbestrol quinestrol chlorotrianisene methallenestril

Estrogen Biosynthesis/Metabolism

 

Physiological Effects:Estrogens

 

Estrogens: Clinical Uses

 

 

Progestins

Some Progestational Compounds and their Biological Activities

Agent

Activities

Progesterone & derivatives estrogenic androgenic anti-estrogenicccc antiandrogenic anabolic

progesterone

-

-

+

-

-

Hydroxyprogesterone capoate

-/+

-/+

-

-

-

Medroxyprogesterone acetate

-

+

+

-

-

Megestrol acetate

- + - + -
17 ethinyl -testosterone derivatives & testosterone drivatives          

Dimethisterone

- - -/+ - -
19-Nor-testosterone derivatives          
Desogestrel - - - -  
Norethynodrel + - - - -
Norethindrone -/+ + + - +
Ethynodiol acetate -/+ + + -  
L-Norgestrel - + + - +

 

 

 Progesterone effects: Metabolic
stimulates lipoprotein lipase promotes fat deposition limited effect on protein metabolism significant effect on carbohydrate metabolism
increases basal insulin levels increases insulin response to glucose promotes glycogen storage (liver) promotes ketogenesis
Progestins without androgenic activity include:
desogestrel gestodene norgestimate

 

 

Other Ovarian Hormones

Hormonal Contraception

 

 

Clinical Uses

 

Adverse Effects: Contraceptives

   Mild Adverse Effects: contraceptives

  Moderate Adverse Effects:

(these effects may require discontinuation of oral contraceptive use)

   Severe Adverse Effects:

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Primary Reference: Goldfien, A., The Gonadal Hormones and Inhibitors, in Basic and Clinical Pharmacology, (Katzung, B. G., ed) Appleton-Lange, 1998, pp 653-680.
Carr, B. R. and Bradshaw, K.D, Disorders of the Ovary and Female Reproductive Tract , In Harrison's Principles of Internal Medicine 14th edition, (Isselbacher, K.J., Braunwald, E., Wilson, J.D., Martin, J.B., Fauci, A.S. and Kasper, D.L., eds) McGraw-Hill, Inc (Health Professions Division), 1998, pp 2097-2115.
Mitchell-Leef, D.E. Endometriosis in Medicine for the Practicing Physician, Fourth edition, (Hurst, J. Willis, editor in chief) Appleton & Lange, 1996, pp 751-755.

 

 

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