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Female sex hormones. OestrogensSynthesis
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1. Female sex hormones:Progesterone
2. Female sex hormones Oestrogens
Synthesis & secretion
Regulation
Pharmacological actions
Pharmacokinetics
Preparations
Therapeutic uses
Adverse effects
Anti-Oestrogens
Clomiphene citrate
Cyclofenil
Tamoxifen citrate
Raloxifene
Ormeloxifene Progestrogens
Synthesis& secretion
Regulation
Pharmacological actions
Pharmacokinetics
Preparations
Therapeutic uses
Adverse effects
Anti-progestrogens
Mifepristone
5. http://anatomy.iupui.edu/courses/histo_D502/D502f04/lecture.f04/Female04/cycle.jpg
7. Progestrogen: Actions
8. as OCS
DUB
HRT
dysmenorrhea
premenstrual syndrome endometriosis
threatened abortion
post-partum
lactation
endometrial cancer
hypoventilation
10. Pharmacokinetics Absorption:
progesterone undergoes high first pass metabolism. Therefore synthetic preparations are more commonly used.
Progesterone esters in oily soln. for i.m. admn.
Metabolism:
by liver enzymes
excretion by urine after conjugation
11. Antiprogestin
12. Mifepristone 19-nor-steroid derivative
Mechanism:
Blocks progest. &
glucocorticoid receptors
During luteal phase:
Pregest. PGs
Menstrual bleeding
Sensitize myocardium to PGs.
HCG production falls
ADME:
F: 25 %, CYP3A4 metabolism t˝: 20 h
Uses:
Termination of early pregnancy along with prostaglandin
As a cervical ripening agent
Post-coital contraceptive
Once a month contraceptive
Progesterone sensitive tumors
Cushings syndrome
Side effects:
Vomiting, diarrhoea, pelvic pain or abdominal pain, about 5% have severe vaginal bleeding
13. Next Class is on Oral Contraceptive Steroids