Presentation1

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.

Medroxyprogesterone acetate
(Provera)

Clinical uses of progestins
Pre-mature labour
Include treating sex
hormone-sensitive cancers
Hormonal deficiency & HRT
Contraception
As anti-androgens n anti-
gonadotropins
Cachexia

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

• 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.
Drug interactions

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.

• 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.

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