Female sex hormones: Progesterone

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Female sex hormonesProgesterone
By C.Adithan
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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

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Cholesterol
Oestriol
17-a- Hydroxy pregnenolone
Dehydro-epi androsterone
Pregnenolone
Andro-stenedione
Progesterone
17- Hydroxy progesterone
Oestrone
OESTRADIOL
TESTOSTERONE
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Oestrogen
Progesterone
LH
FSH
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http//anatomy.iupui.edu/courses/histo_D502/D502f0
4/lecture.f04/Female04/cycle.jpg
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Progestrogen Actions
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Clinical uses of Progesterones

• as OCS
• DUB
• HRT
• dysmenorrhea
• premenstrual syndrome

• endometriosis
• threatened abortion
• post-partum
• lactation
• endometrial cancer
• hypoventilation

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Adverse effects of Progesterone

• breast engorgement, headache, rise in body
  temp.,
• oedema, acne mood swings
• masculinization of external genitalia in the
  foetus
• Increased incidences of congenital abnormalities
• irregular bleeding or amenorrhea
• lower HDL (19-nortestosterone derivatives)
• hyperglycaemia

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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

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Antiprogestin
Mifepristone
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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 t½ 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

Precaution Not to be given to a woman with
suspected ectopic pregnancy, hematological
disorders, receiving oral anticoagulants, Liver/re
nal diseases
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Next Class is on Oral Contraceptive Steroids