Progesterone and related drugs are hormones that have various effects on the female reproductive system and body. Progesterone was first isolated from animal ovaries in 1933. It supports pregnancy by preventing menstruation and sensitizing the uterus. Synthetic progestins are used in oral contraceptives and hormone replacement therapy. Common side effects include irregular bleeding, but progestins also have therapeutic effects like preventing endometrial cancer. Progestin antagonists like mifepristone are used to terminate early pregnancy.

1. Progesterone and
related drugs
Prepared by:
Soma rashad jawad
Azheen kanabi muhammad
Tamara bakr rasul

2. • Introduction
• Defintion
• History
• Effects of progesterone on the body
• Drugs related to progesterone
• Progesterone antagonists
• Oral contraceptives

3. progestogens
Natural
progesterone
Synthetic
progestins

4. Willard M. Allen
Willard Myron Allen
along with George W.
Corner isolated the
hormone from corpora
lutea of sows and
named it progestin in
1933

5. Progesterone favours
pregnancyby:
• Preventingendomaterial
shedding
• reducingUterine motility
• Inhibitingimmunological
reaction toward the foetus

6. females
Corpus
luteum
Placenta
during
pregnancy
Adrenal
cortex
males
Testes
Adrenal
cortex
brain

8. males
Secrete 1-5
mg /day
Plasma level
0.03mcg/dl
females
During the follicular phase the level is
only slightly higherthanthat
of males
But during the luteal phase
The plasma levels range from 0.5
to 2 mcg/dl
Reaches peak in in the 3rd trimester of
pregancy
Effect=?

9. receptors
The progesterone receptor
(PR) is a progestin-
activated steroid receptor
Also known as NR3C3 ;
Nuclear receptor subfamily 3
group C member 3
It is an intranuclear
receptor
It has 2 isoforms :
PR A
PR B
PR is expressed in the
following organs:
central nervous system (CNS)
Endocrine
gastrointestinal
immune
reproductive
cardiovascular
respiratory
Uterus
ovary
cerebellum
spinal cord
hypothalamus

11. Effects of progesterone on the body

12. Uterus:
Progesterone
brings about the
secretory
changes in the
endometruim

13. Cervix :
Progesterone causes
the production of a
viscid cervical
secretion
Vagina:
It causes leukocyte
infiltration in the
epithelium
Breast:
Progesterone cause
proliferation of the
acini in the
mammary glands
CNS:
High levels
may cause
sedation
Body tempretaure:
It causes a slight
0.5 rise in body
tempreture
Metabolism:
Impairs glucose
tolerance
They may tend to
raise LDL and lower
HDL
It stimulates
respiration
Pituitary:
They have anti
ovulatory activity by
reducing LH secretion

15. Progestin derivatives

16. Synthetic progestin (Agonist)s
Progesterone
derivatives (21 C)
19-nortestosterone
derivatives (18 C)

17. Synthetic progestin (Agonist)s
Progesterone
derivatives (21 C)
These are pure
progestins. They have
weaker anti-ovulatory
action and are used
primarily as adjutants
to estrogens for HRT,
threatened abortion
and edometriosis.
19-nortestosterone
derivatives (18 C)
They have weak estrogenic,
androgenic and anabolic
action but have potent anti-
ovulatory action. They are
mainly used in combined
contraceptive pills. Like
desogestrel and
norgestimate (prodrug)

18. Progesterone
derivatives (21 C)
Medroxyprogesterone
acetate
Megestrol acetate
Dydrogesterone
Hydroxyprogesterone
caproate
Newer compound
Nomegestrol acetate
19-nortestosterone
derivatives (18 C)
old
Norethindrone
(Norethisterone)
Lynestrenol
(Ethinylestrenol)
Allylestrenol
Levonorgestrel
(Gonane)
19-nortestosterone
derivatives (18 C)
new
(Gonanes )
Desogestrel
Norgestimate
Gestodene

19. Pharmacokinetics
• Progesterone undergo high 1st pass metabolism , hence mostly given
by i.m in oily solution .
• they have a short half life in the plasma , so usually prescribed for
twice or thrice-daily administration.
• A micronized preparation of progesterone is rapidly absorbed after its
administrated by any route,
Absorption

20. Distribution
Progesterone is
extensively bound to
plasma proteins, primarily
albumin (50 to 54%) and
cortisol-binding protein
(43 to 48%)

21. • reduction to pregnanediol, pregnanetriol and
pregnanolone.
• Subsequent conjugation results in the
formation of glucuronide and sulfate
metabolites.
• The metabolites of pregnanediol and
pregnanolone are excreted →urine or bile
•
• enterohepatic recycling or feces.
Metabolism
Excretion

22. Clinical uses of progestins
1.Rectify hormonal deficiency
and HRT.
2. Contraception.
3.Control of dysfunctional uterine
bleeding.
4.Treatment of dysmenorrhea.
6.Management of endometriosis.
5.Suppression of postpartum
lactation.
7.Treatment of endometrial carcinoma.

23. CONTRAINDICATIONS
Other contraindications
• Undiagnosed vaginal bleeding.
• Missed abortion.
• Known sensitivity to Progesterone
injection.

24. 1.Breast
engorgement,
headache, ↑in body
temperature, acne,
esophageal reflux
and mood swings .
2.Irregular bleeding
or amenorrhoea .
3.The 19-
nortestosterone
derivatives ↓plasma
HDL level .
4.In HRT may ↑the
risk of breast cancer .
5. Diabetes may be
precipitated by long term
uses of potent agents like
levonorgestrol.

25. Antiprogestin (antagonist):
Mifepristone

26. 19-norsteroid.
with potent competitive anti-progestational, anti-glucocorticoid,
anti-androgenic and partial agonist activity.
It is administered during different phases of ovarian cycle.
Mifepristone
Pharmacokinetics
Is orally active , bioavailability → 25%
Mainly metabolized → liver & excreted → bile.

27. Uses
1.termination of early
pregnancy
2.As a contraceptive
given once a month
3.Cervical ripening
4.cushing’s syndrome
Side effects
Main side effects are
significant uterine
bleeding and possibility
of an incomplete
abortion
Also Uterine cramps

28. Contraceptive

29. The birth control pill (also called "the Pill") is a
daily pill that contains hormones to change the way
the body works and prevent pregnancy. Hormones
are chemical substances that control the functioning
of the body's organs. In this case, the hormones in
the Pill control the ovaries and the uterus.

30. Major classes of oral contraceptive

31. Combination pills
• Products containing a
combination of an estrogen and
progestin are the most common
type of oral contraceptives .
The estrogens that are
commonly used in combination
pills are
Ethinyl estradiol and mestranol
The progestin in this
preparations is norethindrone

32. Progestin pills
Products containing a progestin
only usually
• Norethindrone or norgestrel
(called a “mini_pill”)

33. Progestin implants
• Subdermal capsules containing
levonorgestrel offer long term
contraception
• Six capsules each the size of a
matchstick are placed
subcutaneously in the upper arm
the progestin is slowly released
from the capsules
• Provide contraceptive protection
for approximately five years
Totally reversible if the implants are
surgically removed

34. Mechanism
• Inhibition of release of FSH and
LH
• Increase viscosity of cervical
mucus
• Endometrial changes
• Contraction of cervix , uterus
and fallopian tube

35. Effects on the body

37. Therapeutic uses
• Numerous studies have shown that oral contraceptives (OC) provide
protection against a wide variety of illnesses and conditions, including
:

39. Adverse effects

41. Contraindications

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• Laurance L. Brunton , john S.Lazo , Keith L.Parker .
Goodman and gilman’s the pharmacologicalbasis of
theraputics.11th edition.mcGraw-hill:New york;2005.

44. List of refrences (cont.):
• Bertram g. Katzung , Susan B.Masters, Anthony J.Trevor. Basic
and clinical pharmacology.12th edition. mcGraw-hill :New
york;2012.
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pharmacology and therapeutics . Fifth edition . Great britain:
Hodder armond ;2008 .
• Teferra A , Srinivasa A , Amare M , Solomomon W , Eshetu L
, Musie A , Dawet . Lecture notes for health science students
.ethiopia 2004

45. List of refrences (cont.):
• progeterone receptors [Internet] :NURSA; 2014[cited 25 April
2015] Available from:
https://www.nursa.org/nursa/molecules/nr.jsf?doi=10.1621/9
NIE3U3DI6
• progesterone[Internet] :Drugs.com;2013[cited 25 April 2015]
.Available from:
http://www.drugs.com/pro/progesterone.html
• Therapeutic use of contraceptive [Internet] london:
contraceptive; 1999 [cited 2015 april 15 ].available from:
http://www.ncbi.nlm.nih.gov/pubmed/10342095

46. List of refrences (cont.):
• Combined oral contraceptive pill [internet] U.S.A
:contraindications of contraceptive ; 2015 [cited 2015 april
21] . Available from:
http://en.wikipedia.org/wiki/Combined_oral_contraceptive_
pill#Development_of_an_effective_combined_oral_contrace
ptive