2023 DUHS DMC 4th YEAR MBBS

REPRODUCTION MODULE-II
PHARMACOLOGY LECTURE

PROGESTINS AND ANTI-PROGESTINS

By
DR AFRINA RAZA
MBBS(MD),M.Phil
Professor(Assistant),Department of Pharmacology
DMC,DUHS
 OBJECTIVES AND REFERENCES
• ILOs:
1. Describe examples, mechanism of action of drugs included in
PROGESTINS.
2. Discuss key indications, adverse effects and drug‐drug interactions
associated with these drugs
3. Describe examples, mechanism of action of drugs included in ANTI-
PROGESTINS.
4. Discuss key indications, adverse effects and drug‐drug interactions
associated with these drugs
REFERENCES:
1.Katzung`s Pharmacology,15th Edition ,Chapter # 40
2.Google Websites.
THE PROGESTINS
THE PROGESTINS…TYPES
• A) Natural Progestins:
• Progesterone; the most important
progestin in humans;
• synthesized mainly in the ovary from
circulating cholesterol.
• Large amounts are also synthesized
and released by the placenta during
pregnancy.
• B) Synthetic Progestins: (examples in
next slide)
• Most of these agents are:
• extensively metabolized to inactive
products by liver and are
• excreted mainly in the urine.
FOUR Examples of synthetic progestins with RODA and DOA
Relationship of estrogen and progesterone
MOA:
Progestins as a drug
Interacts with PR(progestin-
receptor) to mimic the
stimulatory affects of
progesterone.
Physiological Target:
Reproductive Tract
1. Decreases estrogen-
driven endometrium.
2. Establishment/
maintenance of
pregnancy
• FOUR COMMON THERAPEUTIC USES:
1. Hormone replacement therapy (HRT) to limit estrogen’s effects
on the endometrium.
2. Medroxyprogesterone acetate is used to produce prolonged
Anovulation and Amenorrhea.
• This therapy has been employed in the treatment of
Dysmenorrhea, Endometriosis, and Bleeding disorders when
estrogens are contraindicated.
3. Hormonal contraception.PG-only PILLS to decrease full formation of
cyclical endometrium and so NO ovulation
4. Premature labor (decrease uterine contractions**)
DIAGNOSTIC USE:

• 5. Progesterone can be used as a test of estrogen secretion in

amenorrheic patients.
• The administration of progesterone, for 5–7 days, is
• followed by ……withdrawal bleeding in amenorrheic
patients….
• only when the endometrium has been stimulated by
estrogens.
• CONTRAINDICATIONS, CAUTIONS, & ADVERSE EFFECTS
• Alone and with combination oral contraceptives indicate that
the progestin in these agents may:
• increase blood pressure. HOW? WHY?
• More androgenic progestins also
• reduce plasma HDL levels in women.
• In postmenopausal women:Combined Eg-Pg HRT may
increase breast cancer risk as compared to only Eg.
ANTI-PROGESTINS
Ex:Mifepristone (RU 486) (mifeprex):

MOA:PR antagonist

USED IN :
1)First trimester to therapeutically terminate pregnancy
(along with prostaglandins to increase uterine contractions)

2)Post-coital contraceptive (prevent implantation)

3) Investigational: induction of labor after fetal death.

• ADVERSE EFFECTS:
• vaginal bleeding,
• abdominal pain and cramping

• CONTRAINDICATED in patients with

• vaginal bleeding
• INTERACTIONS:
• Decreases efficacy of anticoagulants…so??in post-MI patients??
• Inhibits hepatic metabolism by CYP3A4:eg:
• Anti-retroviral protease inhibitors,
• Calcium-channel Blockers,
ANY QUESTIONS?
THANK YOU