PROGESTINS

THE SYNTHETIC
PROGESTRONES
 CONTENT TO BE COVERED
 Definition
 Classification
 Mechanism of action
 Indications
 Contraindications
 Drug interactions
 Adverse reactions
 Nursing responsibilities
 Definitions
o Progesterone
Progesterone is a medication and naturally occurring
steroid hormone. These are substances which convert
the Estrogen primed Endometrium to secretory &
maintain pregnancy in animals after conception.
o Progestins
As If progesterone is given orally, it is quickly
destroyed by liver. So,
Progestins are synthetic progestogens medications
that have effects similar to those of progesterone.
Commonly used
Progestins
Medroxyprogesterone acetate
(Provera)
Dydrogesterone
Norethindrone
Desogestrel

Norgestimate
Mechanism of action
Indications
 Clinical uses of progestins

Contraception
Hormonal deficiency & HRT

As anti-androgens n anti- Pre-mature labour

gonadotropins

Include treating sex

Cachexia
hormone-sensitive cancers
 Basic actions…
• Human body has progesterone receptors.
• But they have very limited distribution.
• They are mostly confined to FGT, breast, CNS n
pitutiary.
• Present in nucleus of target cells.
• They occur in 2 isoforms i.e. PR-A & PR-B
• Both agonist & antagonist bind to these
receptors.
Hormonal variations in cycle…
Other include…
• As antigonadotropins
Progestogens, inhibit the secretion of
the gonadotropins i.e. FSH and LH This effect is a form
of negative feedback through which that the body uses
to prevent sex hormonelevels from becoming too
elevated.
• progestins in sufficient amounts can markedly
suppress the body's normal production of
progestogens, androgens, and estrogens,
• sometimes used to suppress sex hormone levels in a
variety of androgen and estrogen-associated
conditions.
 IN Hormonal deficiency n HRT
• To treat endometrial hyperplasia when used in opposition
to estrogen
• Relieve menopausal symptoms, either alone or in
combination with estrogen ( At menopause and thereafter,
decreased levels of female sex hormones result in atrophy,
thinning, and increased wrinkling of the skin and a
reduction in skin elasticity, firmness, and strength, skin
aging and reduced capillaries and blood flow. The skin also
becomes more dry during menopause, which is due to
reduced skin hydration and surface lipids)
• More reliable in treating menopausal sleep disorders.
 Progestins act by :
Fertilization is prevented due to interference
with passage of spermatozoa from vagina to
uterus by making secretions of the cervix n
fallopian tubes thick, so it become difficult for
sperms to penetrated it
 Menstrual disorders
Primary Dysmenorrhea : At
first, NSAIDs e.g. mefenamic
acid are used; if these fail,
then dydrogesterone or
combined contraceptive
tabs. are employed.
Dysfunctional uterine
bleeding with menorrhagia
here Norethindrone (oral)
or IM Depot provera etc
given.
• Progestins inhibit
ectopic endometrial
tissue by antagonizing
estrogen and by
inhibiting Gn-secretion
which leads to
inhibition of ovarian
function, including
estrogen secretion.
Here
Medroxyprogesterone
acetate IM (Depot
provera) are used.
 Premature labour
• progesterone, often given in
the form of 17-hydroxy
progesterone. It…
 relaxes the uterine
musculature,
 maintains cervical length,
 has anti-inflammatory
properties, and thus exerts
activities expected to be
beneficial in reducing preterm
birth.
 Breast Cancer
 Progesterone also appears to be involved in
the pathophysiology of breast cancer
• though its role, and whether it is a promoter or
inhibitor of breast cancer risk, has not been fully
known.
• most synthetic progestins like medroxy-progesterone
acetate have been found to significantly increase the
risk of breast cancer in postmenopausal women in
when given combination with estrogen as a
component of hormone replacement therapy.
• But the combination Dydrogesterone with estrogen
has been found not to do so.
 Other cancers
o prostate cancer
o endometrial cancer
o benign prostatic hyperplasia
 Cachexia
• In some solid malignancies, especially gastric and
pancreatic cancer, high doses of certain progestins
can be employed to improve appetite and reduce
wasting.
• Used in combination with certain other steroids such
as dexamethasone. Their effects take several weeks
to become apparent, but long-lived when compared
to those of corticosteroids.
• Drugs used are Megestrol acetate
& medroxyprogesterone acetate
contraindications
 Drug interactions
• Amino-glutethimide decreases serum
concentrations of medroxyprogesterone; 
• BARBITURATES, carbamazepine, oxcarbazepin
e, phenytoin, primidone, rifampin, modafinil, 
rifabutin, topiramate can increase metabolism
and decrease serum levels of
medroxyprogesterone.
Nursing
Responsibilities
Advise patient to report
• Signs and symptoms of fluid retention
swelling of ankles and feet, weight gain.
• Thromboembolic disorders
pain, swelling, tenderness in extremities, Headache, chest pain,
blurred vision.
• Mental depression, hepatic dysfunction
yellowed skin or eyes, pruritus, dark urine, light-colored stools),
• Abnormal vaginal bleeding..
• IM injection may be painful. Monitor sites for residual lump
and discoloration of tissue may develop.
• Patient & Family Education
 Teach them breast self-examination.
 Review package insert to ensure complete
understanding of progestin therapy.
 Do not breast feed while using this drug.  
• May cause false interpretations of thyroid
function tests.
• Progesterone contraceptives may cause
increase LDL concentrations, serum alkaline
phosphatase & HDL concentrations.
Thank you
• Progestins are also used to treat 
secondary amenorrhea, 
dysfunctional uterine bleeding and 
endometriosis, and as palliative treatment of 
endometrial cancer, renal cell carcinoma, 
breast cancer, and prostate cancer. High-dose 
megestrol acetate is used to treat anorexia, 
cachexia, and AIDS-related wasting
• Some examples of progestins that are used in
hormonal contraceptives are norethisterone
 (many brand names, most notably Ortho-Novum
and Ovcon), norgestimate (Ortho Tricyclen, Ortho-
Cyclen), levonorgestrel (Alesse, Trivora-28, Plan B, 
Mirena), medroxyprogesterone acetate (Provera,
Depo-Provera), cyproterone acetate (Diane-35), 
desogestrel, etonogestrel (Nexplanon), and 
drospirenone (Yasmin, Yasminelle, YAZ).
 Generations of progestins
• Contraceptive progestins are sometimes grouped,
very inconsistently into generations. One definition
of these generations is as follows
• First generation: Approved for marketing before
1973.
• Examples: Noretynodrel, Norethisteron
(norethindrone)  Lynestrenol , Levonorgestrel.
• In women
• Progestins as hormonal contraception, including 
birth control pills, implants, and the 
intrauterine devices.[6][7]
• prevent endometrial hyperplasia from unopposed
estrogen during hormone replacement therapy.
They also used to treat secondary amenorrhea, 
dysfunctional uterine bleeding and endometriosis.[6]
[7]

• In a normal menstrual cycle, declining levels of

progesterone triggers menstruation. Norethisterone
acetate and medroxyprogesterone acetate may be
used to artificially induce progestogen-associated 
breakthrough bleeding.[8]
• Contraceptive methods[edit]
• It has been found that the most effective method of hormonal contraception is
with a combination of an estrogen and a progestin. This can be done in a
monophasic, biphasic, or triphasic manner. In the monophasic method, both an
estrogen and a progestin are administered for 20 or 21 days and stopped for a 7- or
8-day period that includes the 5-day menstrual period. Sometimes, a 28-day
regimen that includes 6 or 7 inert tablets is used. Newer biphasic and triphasic
methods are now used to more closely simulate the normal menstrual cycle. Yet
another method is to administer a small dose of progestin only (no estrogen) in
order to decrease certain risks associated with administering estrogen, but a major
side-effect is irregular bleeding usually observed during the first 18 months of such
therapy.
• Some progestins can be delivered by intramuscular injection every several months
or released over time by diffusion from an implant or an IUD (Intra-Uterine-Device)
(intrauterine system) depending on their solubility characteristics.
 As antiandrogens
• In addition to their progestogenic activity,
some progestins are antagonists of the 
androgen receptor and called antiandrogens.
•As antigonadotropins
•Progestogens, inhibit the secretion of the gonadotropins i.e. FSH and LH This effect is
a form of negative feedback through which that the body uses to prevent 
sex hormone levels from becoming too elevated.
•progestins in sufficient amounts can markedly suppress the body's normal production
of progestogens, androgens, and estrogens,
•sometimes used to suppress sex hormone levels in a variety of androgen and
estrogen-associated conditions. Examples of indications include treating sex
hormone-sensitive cancers (e.g., breast cancer, prostate cancer, endometrial cancer), 
benign prostatic hyperplasia, suppressing precocious puberty and puberty in 
transgender youth, suppressing sex hormone production in transgender patients, and
reducing sex drive in sex offenders and individuals with paraphilias or hypersexuality.
Cyproterone acetate and gestonorone caproate have been found to suppress
circulating testosterone levels by up to 70–80% in men at sufficient dosages.[18][19] This
is notably less than that achieved by GnRH analogues, which effectively abolish
gonadal production of testosterone and suppress circulating testosterone levels by as
much as 95%.[20] In addition, it is less than that achieved by estrogens, which can
suppress testosterone levels into the castrate range at sufficiently high dosages
similarly to GnRH analogues.[21]
• Cachexia[edit]
• Further information: Cachexia
• In many people suffering from solid malignancy, especially gastric
and pancreatic cancer, high doses of certain progestins can be
employed to improve appetite and reduce wasting. In general,
they are used in combination with certain other steroids such as 
dexamethasone. Their effects take several weeks to become
apparent, but are relatively long-lived when compared to those
of corticosteroids. Furthermore, they are recognized as being the
only drugs to increase lean body mass. Megestrol acetate is the
lead drug of this class for the management of cachexia, and 
medroxyprogesterone acetate is also used.[22][23]
• Progesterone converts the endometrium to its
secretory stage to prepare the uterus for
implantation. At the same time progesterone
affects the vaginal epithelium and 
cervical mucus, making it thick and
impenetrable to sperm.
Thrombophlebitis is phlebitis or vein
inflammation related to a thrombus, which is a
blood clot.