Progesterone
It is an steroid female sex hormone secreted from the corpus luteum
under the control of luteinizing hormone. It is also secreted from
placenta, adrenal medulla
Actions:
 Prepares the uterus for implantation of the fertilized ovum.
 Inhibit uterine contraction that would expel the fetus.
 Development of mammary gland acini.
 Pituitary:-ve feed back effect on luteinizing hormone so, block




ovulation.
Thick cervical secretion so, block sperm penetration.
Thermogenic i.e it increases body temperature.
Kidney:Blocks aldosterone -induced sodium retention.
Decreases the plasma levels of many amino acids.
Progesterone and progestins (progestogens):
Progesterone is the natural hormone is not effective orally due to the
extensive 1 st pass metabolism so, it must be given by i.m injection.
Prontogest amp.100mg , lutoneamp.It has a short duration of action.
Progestins are synthetic derivatives of progesterone, effective orally, and
have a long duration of action.
Some of progestins have androgenic, estrogenic, and even
glucocorticoid-like effects .norethindrone , norethyyndrel ,norgestrel
They are not used to maintain pregnancy because they may cause
virilization of female fetus as a result of androgenic effect.
Therapeutic uses:
1-Progesterone is used to replace deficiency of endogenous progesterone
 Infertility due to progesterone deficiency.
 Habitual abortion due to progesterone deficiency maintainance of
pregnancy.
-Hydroxyprogesterone acetate 150 -250 mg IM are used.
2-progestrins are used to suppress ovulation in cases of:
 Contraceptive pills .either singly (norethinderone mini pills) ,in
combination with estrogen (norethyndrel & norgesterol ) or long
acting progesterone injections or implants ( medroxyprogesterone
acetate).
 Endometriosis
 Dysmenorrhea.
 Dysfunctional uterine bleeding.
Progesterone antagonists
a- Mifepristone is a long acting progesterone antagonist .It has also
inhibitory effect on glucorticoid and estrogen receptors .Its oral
administration causes: block progesterone receptor in uterus.
 Premature degeneration of corpus lutium.
 Increase uterine motility.
 Inhibition of ovulation
Therapeutic uses:
1-Postcoital contraception .
2-Inducton of therapeutic abortion in cases of intrauterine fetal death in
combination with prostaglandin. A single oral dose of 600 mg of
mifepristone and a vaginal pessary containing 1 mg of prostaglandin E1
or oral misoprostol.
3-Treatment of endometriosis.
4-Treatment of dependent cancer as cushing disease or cancer breast.
Side effects:
adverse effects of the medications included vomiting, diarrhea, and
abdominal or pelvic pain. It produces delayed inhibition of ovulation due
to its long action.
b-Danazole
-It is isoxazole derivative of ethisterone.
-It has multiple endocrine effects including:
 Inhibition of overian function due to inhibition of the effects of
LH&FSH on uterus.
 Androgenic effects due to stimulation of androgen receptors.
 Progesterone like effect because it is metabolized to Ethisterone
 Stimulation of corticosteroid receptors.
-It increases clotting factors especially VIII and IX
Therapeutic uses:
1- treatment of endometriosis due to inhibition of overian function in a
dose of of 600 mg/d. The dosage is reduced to 400 mg/d after 1 month
and to 200 mg/d in 2 months. About 85% of patients show marked
improvement in 3–12 months..
2-Treatment of fibrocystic disease of breast 400 mg day for 2 bmonths
3-Treament of hemophilia 600 mg/day for 8weeks.
Side effects:
-Hypertension.
-Hyperlipidemia due to decrease HDL.
-Breast tenderness.
-Weight gain.
-Progestrins have androgenic effect .They may produce hirsutism in
women. and virilization of female fetus if taken during pregnancy.
Properties of Some Progestational Agents.
Route Duration Activities
of
Action
Estrogenic Androgenic Antiestrogenic Antiandrogenic Anab0
Progesterone and derivatives
IM
1 day
–
–
+
–
–
Hydroxyprogesterone IM
caproate
8–14
days
slight
slight
–
–
–
Medroxyprogesterone IM,
acetate
PO
Tabs: 1– –
3 days;
injection:
4–12
weeks
+
+
–
–
1–3 days –
+
–
+
–
Progesterone
Megestrol acetate
PO
17-Ethinyl testosterone derivatives
Dimethisterone
PO
1–3 days
–
–
slight
–
–
19-Nortestosterone derivatives
Desogestrel
PO
1–3 days
–
–
–
–
–
Norethynodrel
PO
1–3 days
+
–
–
–
–
Lynestrenol3
PO
1–3 days
+
+
–
–
+
Norethindrone
PO
1–3 days
slight
+
+
–
+
Norethindrone
acetate2
PO
1–3 days
slight
+
+
–
+
Ethynodiol diacetate PO
1–3 days
slight
+
+
–
–
L-Norgestre
PO
1–3 days
–
+
+
–
+