Progesterone

1/18/2020 16th batch B.pharm (SMTC)

Sanjay kumar yadav by:
Introduction of progestrone
Menstruation & Uterine cycle
Role of Progestrone
Alteration of progesterone
Release and regulation
Sources of progesterone (site of
synthesis)
Sources of progesterone
Types of progesterone
Route of administration
of progesterone
Pharmacokinetics
Clinical uses of progestin
Contraceptives
Emergency contraceptive
 Combination pills
 Progestin only pills
Sangita Dhungana by:
Anti-progestrin : Mifeprestone
 Mechanism of action
 pharmacokinetics
 Side effect
 Drug interactions
 Uses & doses
References

• Is hormones which stimulates and regulates
various functions.
• Produce secondary sexual character in mature
girls. Like enlargement of breast & buttock ,
release of pubic hair on sex organ etc.
• Causes attracts towards the sex /sex drive.
• Plays a role in maintaining pregnancy.
• Helps to regulates the monthly menstrual
cycle.

Periodic discharge of blood and cellular debris
from the female genital tract is termed
menstruation.
Cyclical changes occurring from one
menstruation to the next comprises a
menstrual cycle.
The duration of menstrual cycle is about 28 ±
4 days.

1. Menstrual phase (3 – 5 days):
If ovum is not fertilized, corpus luteum regresses
from 24th day of cycle
Causes decrease in estrogen and progesterone levels.
Results in shrinkage of endometrium.
Flow of menses normally serves as a sign that a
woman has not become pregnant.
Average blood loss during menstruation is 10 – 80 ml.
When menstruation begins, dysmenorrhea , breast
tenderness occurs.1/18/2020 86th batch B.pharm (SMTC)

1/18/2020 6th batch B.pharm (SMTC) 9

2. Proliferative phase ( follicular phase):
Starts at the end of menstrual phase
Duration is about 10 days
Later endometrium starts healing and then
proliferates rapidly from 5th – 14th day of menstrual
cycle.
Endometrium increases in thickness to about 3 -
5mm.
The endometrial glands produce a thick mucus.
At the end of proliferative phase ovulation occurs.10

3. Secretory phase (luteal phase):
 This phase lasts for about 14 days.
It starts after ovulation and extends upto the next
menstrual phase.
Endometrium thickens upto 6 mm.
Glands become bigger, tortuous and filled with
secretions.
Stromal cells proliferate, spiral arteries become more
coiled and dilated.
due to action of progesterone & estrogen on uterine
endometrium. 12

Low progesterone in women
• Depression,
• migraine headache
• Weight gain
• Infertility
• Miscarriage
• Polycystic ovary syndrome
• Menstrual problems
High progesterone in women
• High levels before cycle
• Headaches
• Moodiness
• Pre_menstrual symptoms
(PMS)

1. Hypothalamus
2. Gn.R.H.
3. anterior lobe of
pituitary gland
4. L.H.
5. corpus luteum of
ovary
6. Progesterone

Females
• Corpus luteum
• Placenta during pregnancy
• Adrenal cortex
Males
• Testes
• Adrenal cortex

Plant (Dioscorea mexicana)----- diosgenin
production ----progesterone.
Mammals, progestrone, like all other steroid
hormones, is synthesized from pregnenolone
which is derived from cholesterol.
Chemically or synthetic prepared
progesterone inside labs.

Oral
Vaginal suppositories
Deep intramuscular injection
Implant
Intrauterine system

Absorption: Progesterone undergo high 1st pass
metabolism ,
 hence mostly given by i.m in oily solution .
 have a short half life in the plasma,
 So, usually prescribed for twice or thrice-daily
administration.
Distribution: extensively bound to plasma proteins,
primarily albumin (50 to 54%) and cortisol-
binding protein (43 to 48%).
Metabolism: reduction to pregnanediol,
pregnanetriol and pregnanolone. Subsequent
conjugation results in the formation of
glucuronide and sulfate metabolites.
Excreation: Metabolites of pregnanediol and
pregnanolone are excreted →urine or bile
(enterohepatic recycling or feces.)
1/18/2020 22

MOA:
 inhibition of release of FSH and
LH,
 increase viscosity of cervical
mucus,
 endometrial changes,
 contraction of cervix, uterus
and fallopian tube
S.E.: agglomeration of RBC, liver &
breast cancer, jaundice, stone
formation in gall bladder,
depression, headache etc.
C.I.: liver & heart diseases,
hypersensitivity.

 Follicular phase: attenuates mid-cycle gonadotrophin (FSH/LH) surge
from pituitary (antiprogestrin activity)  slowing of follicle development
and delay/failure of ovulation.
 Secretory/Lutael phase: prevents secretory changes by blocking
progesterone action on endometrium.
 Later stages of cycle: blocks progesterone support to endometrium and
increases prostaglandin(PG) release  stimulates uterine contraction
 Sensitizes myometrium to PG and induces mensturation.
 Post implantation: blocks decidualization  conceptus gets dislodged
 human chorionic gonadotrophin (hCG) falls, luteolysis occurs
decreased endogenous progesterone and cervix softens abortion.

1. chlorpromazine ↔ mifepristone: can increase
the risk of an irregular heart rhythm.
2. haloperidol ↔ mifepristone : can increase the
risk of an irregular heart rhythm.
3. norfloxacin ↔ mifepristone: can increase the
4. halothane ↔ mifepristone: can increase the
5. heparin ↔ mifepristone: may increase the risk
and/or severity of vaginal bleeding in women.1/18/2020 33

1. http://cephalicvein.com/wp-
content/uploads/2016/08/pituitary-gland-definition-
endocrine-system-members-anatomy-physiology.jpg
2. https://www.slideshare.net/azheenkmuhamad/proge
sterone-and-related-drugs
3. https://www.slideshare.net/namkhadorji/use-of-
progesterone-in-obstetrics-amp-gynaecology-
namkha-presents
4. https://www.slideshare.net/LifecareCentre/role-of-
progesterone-in-pregnancy-27354617
5. https://en.wikipedia.org/wiki/Menstrual_cycle#Cycles
_and_phases

Progesterone

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